COMPOSITIONS AND METHODS FOR IN VIVO DELIVERY OF ANTISENSE COMPOUNDS (Fri, 13 Jun 2014)
The present invention provides compositions and methods for improved in vivo delivery of oligomeric compounds. In particular, the compositions and methods provide for administration of a small delivery peptide with an antisense compound. A membrane active melittin peptide is functionalized with masking and targeting groups prior to administration to mask its membrane activity until it is inside a targeted cell. It is expected that inclusion of the small delivery peptide will enhance the delivery and potency of antisense compounds. In certain embodiments, the compositions and methods provided herein are expected to enhance the delivery of antisense compounds to liver cells in a mammal.
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MODULATION OF APOLIPOPROTEIN CIII (APOCIII) EXPRESSION (Fri, 09 May 2014)
<p id="p-0001" num="0000">Provided herein are methods, compounds, and compositions for reducing expression of ApoCIII mRNA and protein in an animal. Also provided herein are methods, compounds, and compositions for increasing HDL levels and/or improving the ratio of TG to HDL and reducing plasma lipids and plasma glucose in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate any one or more of cardiovascular disease or metabolic disorder, or a symptom thereof.</p>
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CHIRAL FLUORINATING REAGENTS (Fri, 09 May 2014)
This invention relates to fluorinating agents and, more particularly, to chiral non-racemic fluorinating agents useful for enantioselective fluorination, as well as to their synthesis and use and other subject matter. The fluorinating agents are based on a substituted 1,4-diazabicyclo[2.2.2]octane (DABCO) skeleton and provide electrophillic fluorine enantioselectively.
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BIFUNCTIONAL ORGANIC CATALYSTS (Fri, 02 May 2014)
The present invention provides a bifunctional catalyst of the formula (1): wherein: each R1 is independently selected from an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted aralkyl group and an optionally substituted alkaryl group; Z represents a divalent organic linking moiety optionally containing one or more stereocentres; and EWG represents an electron-withdrawing group.
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MODIFICATION OF TREHALOSE-6-PHOSPHATE LEVELS IN PLANTS (Fri, 25 Apr 2014)
<p id="p-0001" num="0000">Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="37.17mm" wi="63.25mm" file="US20140113820A1-20140424-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SUBSTITUTED 2'-THIO-BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 18 Apr 2014)
<p id="p-0001" num="0000">Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4′-methylene group attached to a 2′-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4′-methylene and or the 5′-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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TREATMENT OF BIPOLAR DISORDER (Fri, 04 Apr 2014)
<p id="p-0001" num="0000">The invention relates to sulphur- and/or selenium-containing compounds that can inhibit the enzyme inositol mono-phosphatase (IMPase), and which can be used in treating conditions that are treatable through inhibition of this enzyme, such as bi-polar disorder, the compounds having a structure of Formula (I), or is a pharmaceutically acceptable salt thereof; Formula (I); in which: E is S or Se and each of phenyl rings A and B is optionally substituted with one or more substituents, in which each substituent is selected independently from: (1) a halogen, which is preferably selected from F, Cl and Br; (2) C<sub>1</sub>-C<sub>4 </sub>alkyl, such as C<sub>1</sub>-C<sub>2 </sub>alkyl or C<sub>1 </sub>alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and (3) C<sub>1</sub>-C<sub>4 </sub>alkoxy, such as C<sub>1</sub>-C<sub>2 </sub>alkoxy or C<sub>1 </sub>alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.97mm" wi="60.88mm" file="US20140094449A1-20140403-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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CYCLOHEXENYL NUCLEIC ACIDS ANALOGS (Fri, 14 Mar 2014)
<p id="p-0001" num="0000">The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclohexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Compositions and methods for optimizing cleavage of RNA by RNASE H (Thu, 27 Feb 2014)
The present invention provides compositions and methods for the optimization of cleavage of RNA species by RNase H. In some emboediments, the invention provides oligonucleotides that possess two or more regions of differing conformation, and at least one transitional nucleobase positioned between the regions that is capable of modulating transfer of the helical conformation characteristic of the region bound to the 3'hydroxy thereof, to the region bound to the 5' hydroxyl thereof.
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Vaccine (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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METHOD FOR ASSAYING OGFOD1 ACTIVITY (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to assays for monitoring activity of OGFOD1 activity, in particular, to assays for identifying modulators of OGFOD1 activity. The invention also relates to assays to monitor the prolyl hydroxylase activity of OGFOD1 on its substrate, the human ribosomal protein RPS23. The invention also enables the introduction of 3-hydroxyprolyl residues into peptides and proteins.</p>
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INFLAMMATION IMAGING AND THERAPY (Fri, 21 Feb 2014)
An imaging agent comprising a conjugate of an oligosaccharide moiety with an imaging moiety. The oligosaccharide is Lewis A or Lewis B or a mimetic thereof, or a pharmaceutically acceptable salt or PEGylated form of Lewis A or Lewis B or its mimetics. Lewis A and Lewis B and its mimetics are also provided for use in the therapeutic treatment of inflammatory diseases, autoimmune diseases and cancer.
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LEVITATION DEVICE WITH HORIZONTAL SPIN AXIS (Fri, 31 Jan 2014)
A levitation device including an object levitatable at a predetermined position, wherein the object comprises a spinning magnet, the spinning magnet having a substantially horizontal spin axis defining an axial direction and the spinning magnet having a magnetization direction parallel to the spin axis, the device further comprising: a pusher magnet arrangement configured to produce a magnetic field at the predetermined position that is in the opposite direction to the magnetization direction of said spinning magnet; a lifter magnet arrangement lower than and to either side of the predetermined position, having a magnetization direction parallel to the magnetization direction of the spinning magnet, and having a recess under the predetermined position; and a puller magnet arrangement above said predetermined position and having a magnetization direction antiparallel to the magnetization direction of the spinning magnet.
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ASSAY (Fri, 31 Jan 2014)
The present invention provides a way to treat cancer by modulating JMJD4 activity. The invention also relates to assays for monitoring activity of JMJD4 activities, in particular, to assays for identifying modulators of JMJD4 activities. The invention further relates to assays to monitor the lysyl hydroxylase activity of JMJD4 on its substrate, the translation termination protein eRFl. The invention also enables the introduction of hydroxylysyl residues into peptides and proteins. The invention further provides a way to modulate translation termination and hence to stimulate readthrough of nonsense mutations associated with disease.
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TRICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 18 Oct 2013)
The present disclosure provides tricyclic nucleosides and oligomeric compounds prepared therefrom. More particularly, the tricyclic nucleosides provided herein comprise a tricyclic ribosyl sugar moiety having a bridge between the 4' and 2' ring carbon atoms and a further fused carbocyclic or heterocyclic ring at the 3' and 4' carbon atoms. The tricyclic nucleosides are expected to be useful for enhancing properties of oligomeric compounds including for example binding affinity and nuclease resistance.
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TRICYCLIC NUCLEIC ACID ANALOGS (Fri, 18 Oct 2013)
The present disclosure provides tricyclic nucleosides and oligomeric compounds prepared therefrom. The tricyclic nucleosides each have a tricyclic ribosyl sugar moiety wherein a bridge between the 2' and 4' ribosyl ring carbon atoms further comprises a fused carbocyclic or heterocyclic ring. The tricyclic nucleosides are expected to be useful for enhancing properties of oligomeric compounds including for example binding affinity and nuclease resistance.
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Tetrahydropyran nucleic acid analogs (Fri, 16 Aug 2013)
<p id="p-0001" num="0000">The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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DIAGNOSING MULTIPLE SCLEROSIS (Fri, 16 Aug 2013)
There is provided an in vitro method for diagnosing Multiple Sclerosis (MS) in a human test subject, comprising (i) determining the concentrations of two or more metabolites in a sample from said subject, wherein said two or more metabolites are selected from: blood metabolites, wherein said blood metabolites comprise: alanine, ascorbic acid, choline, fatty acid, glucose, lactate, N-acetyl aspartate, N-acetyl glycoprotein, n-butyrate, oxyglutaric acid, phosphocholine, taurinebetaine, tyrosine, L-glutamine, N-acetyl species, and beta-hydroxybutyrate; and/or urine metabolites, wherein said urine metabolites comprise: citrate, creatinine, inositol, lactate and trimethylamine N-oxide (TMAO); (ii) comparing the concentrations of said two or more metabolites in the sample with the concentrations of the same metabolites in at least one reference standard; and (iii) identifying a concentration difference for each of said two or more metabolites in the sample relative to the reference standard; wherein said concentration differences correlate with the presence of MS.
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OLIGOMERIC COMPOUNDS COMPRISING TRICYCLIC NUCELOSIDES AND METHODS FOR THEIR USE (Fri, 02 Aug 2013)
<p id="p-0001" num="0000">The present disclosure provides tricyclic nucleosides, oligomeric compounds comprising at least one of the tricyclic nucleosides and methods of using the oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Methods for inhibiting expression of connective tissue growth factor (Fri, 26 Jul 2013)
<p id="p-0001" num="0000">This invention provides compounds which comprise modified oligonucleotides capable of inhibitory expression of connective tissue factor and composition containing same as well as methods of treating hyperprolific disorders and fibrotic diseases, and of reducing scarring resulting from wound healing using such compounds.</p>
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MODULATION OF EIF4E EXPRESSION (Fri, 12 Jul 2013)
<p id="p-0001" num="0000">Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided.</p>
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LIPID FORMULATED SINGLE STRANDED RNA (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">The present invention provides compositions comprising a nucleic acid lipid particle and an oligomeric compound and uses thereof. In certain embodiments, such compositions are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.</p>
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BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">The present invention provides novel 3′,5′-linked bicyclic nucleosides and oligomeric compounds prepared therefrom. The bicyclic nucleosides provided herein are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.</p>
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Antibacterial 4,6-substituted 6′, 6″ and 1 modified aminoglycoside analogs (Fri, 07 Jun 2013)
<p id="p-0001" num="0000">The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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SUBSTITUTED 2'-AMINO AND 2'-THIO-BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 24 May 2013)
<p id="p-0001" num="0000">Provided herein are 2′-amino and 2′-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.</p>
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MULTISOMES: ENCAPSULATED DROPLET NETWORKS (Sat, 11 May 2013)
The invention provides a droplet encapsulate comprising: a drop of a hydrophobic medium; a peripheral layer of non-polymeric amphipathic molecules around the surface of the drop; and an aqueous droplet within the peripheral layer, the aqueous droplet comprising: (a) an aqueous medium and (b) an outer layer of non-polymeric amphipathic molecules around the surface of the aqueous medium. The invention also provides processes for preparing the droplet encapsulates. Various uses of the droplet encapsulates are also described, including their use as drug delivery vehicles, in synthetic biology, and in the study of membrane proteins.
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5' MODIFIED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 10 May 2013)
<p id="p-0001" num="0000">The present invention provides 5′ modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5′-substituent and an optional 2′ substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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(Fri, 03 May 2013)

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ASYMMETRIC SYNTHESIS OF ORGANIC COMPOUNDS (Fri, 19 Apr 2013)
The present invention provides processes for the production of chiral compounds in a stereoisomeric excess. The present processes involve reacting a hydrometallated alkene compound with a compound comprising a conjugated -bond system under conditions such that the compounds undergo an asymmetric 1,4- or 1,6-conjugate addition reaction, generating a chiral compound in a stereoisomeric excess. The reaction is performed in the presence of a metal catalyst, which catalyst preferably comprises a non-racemic chiral ligand.
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MODIFIED NUCLEOSIDES, ANALOGS THEREOF AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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CANNABINOID-2-RECEPTOR AGONISTS (Fri, 29 Mar 2013)
The present invention relates to cannabinnoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions).
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MODULATION OF GLUCOSE-6-PHOSPHATASE TRANSLOCASE EXPRESSION (Fri, 08 Mar 2013)
<p id="p-0001" num="0000">Compositions and methods are provided for decreasing blood glucose levels in an animal, comprising administering to said animal an antisense inhibitor of glucose-6-phosphatase translocase expression alone or in combination with at least one glucose-lowering drug. Also provided are compositions and methods for treating diabetes and other metabolic disorders.</p>
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Base modified bicyclic nucleosides and oligomeric compounds prepared therefrom (Fri, 15 Feb 2013)
<p id="p-0001" num="0000">Provided herein are novel base modified bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel pyrimidine bicyclic nucleosides are provided wherein each pyrimidine base is substituted at the 5 position with an optionally substituted, aromatic or heteroaromatic ring system comprising from 5 to 7 ring atoms selected from C, N, O and S. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Modulation of forkhead box O1A expression (Fri, 01 Feb 2013)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding forkhead box O1A. Methods of using these compounds for modulation of forkhead box O1A expression and for treatment of diseases associated with expression of forkhead box O1A are provided, in particular, for methods of treating diabetes.</p>
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ASSAY FOR HISTIDINYL HYDROXYLASE ACTIVITY (Fri, 01 Feb 2013)
The present invention relates to assays for monitoring activity of Mina53 and NO66 activities, in particular, to assays for identifying modulators of Mina53 and NO66 activities. The invention also relates to assays to monitor the histidinyl hydroxylase activity of Mina53 and NO66 on their substrates, the human ribosomal protein Rpl27a and Rpl8 respectively. The invention also enables the introduction of S-3-hydroxyhistidinyl residues into peptides and proteins.
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Mutant enzymes (Thu, 24 Jan 2013)
This invention relates to mutant enzymes with enhanced properties and processes for oxidation of organic compound substrates using such enzymes.
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BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 14 Dec 2012)
The present invention provides novel bicyclic nucleosides and oligomeric compounds prepared therefrom. Incorporation of one or more of the bicyclic nucleosides into an oligomeric compound is expected to enhance one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in double stranded compositions. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Antisense oligonucleotide modulation of stat3 expression (Thu, 29 Nov 2012)
Compounds, compositions and methods are provided for inhibiting the expression of human STAT3. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding STAT3. Methods of using these oligonucleotides for inhibition of STAT3 expression and for promotion of apoptosis are provided. Methods for treatment of diseases, particularly inflammatory diseases and cancers, associated with overexpression or constitutive activation of STAT3 or insufficient apoptosis are also provided.
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Diffusion-weighted magnetic resonance imaging using 3D mosaic segmentation and 3D navigator phase correction (Fri, 16 Nov 2012)
<p id="p-0001" num="0000">In a magnetic resonance apparatus and operating method therefore, 3D navigator data are acquired and are used to correct spatially varying phase errors in contemporaneously acquired imaging data in each shot of a multi-shot data acquisition sequence. A mosaic sampling scheme is used to enter the diffusion-weighted magnetic resonance data and the navigator data into k-space respectively in blocks that each form a subset of the entirety of k-space. The navigator data in each shot are entered into a block that is located at the center of k-space, and, in each shot, the corresponding image data are entered into an offset block in k-space, that is offset in at least one spatial direction from the navigator data block. The offset is varied from shot-to-shot.</p>
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Modulation of eIF4E expression (Fri, 09 Nov 2012)
<p id="p-0001" num="0000">Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided.</p>
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MODIFICATION OF TREHALOSE-6-PHOSPHATE LEVELS IN PLANTS (Fri, 02 Nov 2012)
Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.
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METHOD FOR ASSAYING OGFOD1 ACTIVITY (Fri, 24 Aug 2012)
The present invention relates to assays for monitoring activity of OGFOD1 activity, in particular, to assays for identifying modulators of OGFOD1 activity. The invention also relates to assays to monitor the prolyl hydroxylase activity of OGFOD1 on its substrate, the human ribosomal protein RPS23. The invention also enables the introduction of 3-hydroxyprolyl residues into peptides and proteins.
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PROCESS FOR PRODUCING METHANOL (Thu, 23 Aug 2012)
The present invention relates to a novel process for the production of methanol. The process comprises the heterolytic cleavage of hydrogen by a frustrated Lewis pair comprising a Lewis acid and a Lewis base; and the hydrogenation of CO<sb>2</sb> with the heterolytically cleaved hydrogen to form methanol.
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TREATMENT OF BIPOLAR DISORDER (Fri, 17 Aug 2012)
The invention relates to sulphur- and/or selenium-containing compounds that can inhibit the enzyme inositol monophosphatase (IMPase), and which can be used in treating conditions that are treatable through inhibition of this enzyme, such as bipolar disorder, the compounds having a structure of Formula (I), or is a pharmaceutically acceptable salt thereof; Formula (I); in which: E is S or Se and each of phenyl rings A and B is optionally substituted with one or more substituents, in which each substituent is selected independently from: (1) a halogen, which is preferably selected from F, Cl and Br; (2) C1-C4 alkyl, such as C1-C2 alkyl or C1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and (3) C1-C4 alkoxy, such as C1-C2 alkoxy or C1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br.
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Antisense oligonucleotide modulation of STAT3 expression (Fri, 10 Aug 2012)
<p id="p-0001" num="0000">Compounds, compositions and methods are provided for inhibiting the expression of human STAT3. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding STAT3. Methods of using these oligonucleotides for inhibition of STAT3 expression and for promotion of apoptosis are provided. Methods for treatment of diseases, particularly inflammatory diseases and cancers, associated with overexpression or constitutive activation of STAT3 or insufficient apoptosis are also provided.</p>
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ASSAY FOR ARGINYL HYDROXYLASE ACTIVITY (Fri, 10 Aug 2012)
The present invention relates to assays for monitoring activity of YcfD activity, in particular, to assays for identifying modulators of YcfD activity. The present invention also relates to the use of YcfD inhibitors as antibiotics. The invention also relates to methods for introducing hydroxyarginine residues into proteins.
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Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase (Fri, 29 Jun 2012)
<p id="p-0001" num="0000">The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.</p>
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Supports for oligomer synthesis (Fri, 29 Jun 2012)
<p id="p-0001" num="0000">Universal linkers, their facile processes of manufacture and methods of using the same are provided.</p>
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SOLID-STATE HETEROJUNCTION DEVICE (Fri, 08 Jun 2012)
The present invention relates to a solid-state p-n heterojunction such as in a solar cell comprising an organic p-type material in contact with a porous layer of n-type material, characterised in that the thickness of the porous layer of n-type material is 2 µm or greater. The invention also relates to a solid-state p-n heterojunction such as in a solar cell comprising an organic p-type material in contact with a porous layer of n-type material, characterised in that the pore-filling-fraction of the porous layer of n-type material by the organic p-type material is no more than 50%. The invention further comprises devices such as solar cells or photodetector devices formed from such heterojunctions, methods of forming the same and the use of a polymeric p-type material in such a device or method.
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Optimization of ligand affinity for RNA targets using mass spectrometry (Wed, 30 May 2012)
<p id="p-0001" num="0000">The present invention provides methods for the identification ligand compounds that bind to target molecules such as proteins or structured RNA with as little as millimolar (mM) affinity using mass spectrometry. The methods may be used to determine the mode of binding interaction between two or more of these ligand compounds to the target as well as their relative affinities. Also provided are methods for designing compounds having greater affinity to a target molecule by identifying two or more ligands using mass spectrometry methods of the invention and linking the ligands together to form a novel compound.</p>
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Vaccine (Fri, 18 May 2012)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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Antisense modulation of C-reactive protein expression (Fri, 30 Mar 2012)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for treatment of diseases associated with expression of C-reactive protein are provided.</p>
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Tetrahydropyran nucleic acid analogs (Fri, 23 Mar 2012)
<p id="p-0001" num="0000">The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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IDENTIFICATION OF LIGANDS AND THEIR USE (Fri, 24 Feb 2012)
A method to identify a peptide and/or its encoding DNA, wherein the peptide binds to a T-cell receptor and/or an NK-cell receptor and/or an NKT-cell receptor, the method comprising: providing a carrier to which is attached a peptide and its encoding DNA; providing an MHC and/or an MHC-like molecule; and exposing the peptide to a T-cell receptor and/or an NK-cell receptor and/or an NKT-cell receptor in the presence of the MHC or MHC- like molecule.
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TUNICAMYCIN GENE CLUSTER (Fri, 03 Feb 2012)
The invention relates to a gene cluster for the production of tunicamycins and derivatives thereof. The invention also relates to individual polynucleotides from the gene cluster, variants thereof and the polypeptides they encode. The invention further relates to heterologo-us expressions systems and their use to produce a tunicamycin or a derivative thereof.
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CATALYSTS FOR HYDROGEN GENERATION AND FUEL CELLS (Fri, 03 Feb 2012)
The invention provides a process for producing H2 from a compound of formula (I), (II), (III) or (IV): R1COOH (I); R2OH (II); R3CHO (III); R4NH2 (IV); wherein R1 is H or unsubstituted or substituted C1-10 alkyl; R2 is unsubstituted or substituted C1-10 alkyl; R3 is H or unsubstituted or substituted C1-10 alkyl; R4 is H, unsubstituted or substituted C1-10 alkyl, or C(0)NR5R6; and R5 and R6, which are the same or different, are independently selected from H and unsubstituted or substituted C1-10 alkyl; which process comprises contacting a liquid phase which comprises said compound of formula (I), (II), (III) or (IV) with a catalyst, which catalyst comprises: (a) polymetallic nanoparticles, each of which comprises a first metal and a second metal, which first metal is selected from a Group (9), Group (10), Group (11) or Group (12) d-block metal, and which second metal is other than said first metal, wherein the polymetallic nanoparticles comprise a core which comprises said second metal and a shell surrounding said core, which shell comprises said first metal; or (b) nanoparticles which comprise a metal selected from palladium, rhodium, ruthenium, iridium, copper and silver, and which have a mean particle size of less than or equal to 50 nm;_provided that when said compound is a compound of formula (II), the catalyst comprises (a) said polymetallic nanoparticles. Further provided is a catalyst for the production of hydrogen from a compound of formula (I)-(IV) or for the electro-oxidation of a compound of formula (I)-(IV), which catalyst comprises polymetallic nanoparticles, which polymetallic nanoparticles comprise a core and a shell surrounding the core; wherein the shell comprises a first metal which is palladium, and the core comprises a second metal, wherein the second metal is other than palladium, platinum, gold, iron, cobalt, nickel, titanium, tungsten, tantalum, vanadium and niobium. Further provided is a process for producing the catalysts of the invention, and the following uses of the catalysts of the invention: use for the electro-oxidation of a compound of formula (I)-(IV); use for the electro-oxidation of formic acid; use in a fuel cell; use for the electro-oxidation of a compound of formula (I)-IV) in a fuel cell; and use for the electro-oxidation of formic acid in a direct formic acid fuel cell. Further provided is an electrode suitable for use in a fuel cell, comprising a catalyst of the invention, and a fuel cell comprising a catalyst or an electrode of the invention. A process for the electro-oxidation of a compound of formula (I)-(IV) with a catalyst of the invention is also provided.
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Tetrahydropyran nucleic acid analogs (Fri, 27 Jan 2012)
<p id="p-0001" num="0000">The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel tetrahydropyran nucleoside analogs are provided having at least one chiral substituent that are expected to be useful for enhancing one or more properties of oligomeric compounds such as nuclease resistance and/or binding affinity. In certain embodiments, the oligomeric compounds are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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5′-modified bicyclic nucleic acid analogs (Fri, 13 Jan 2012)
<p id="p-0001" num="0000">The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.</p>
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FLUORINE RADIOLABELLING PROCESS (Fri, 13 Jan 2012)
The invention relates to a process for producing a process for producing an 18F-labelled compound, the process comprising treating a compound of formula (I): wherein EDG is an electron-donating group selected from -OH, -OR4, -NHR5 and -NR55R5; R1, R2, X1 and X2 are as defined herein; and R3 is selected from H, X3 and X4, wherein X3 is a monodentate cleavable surrogate group, and X4 is a bidentate cleavable surrogate group which is bonded (a) to said X or X and (b) to the ring carbon atom para to EDG; with [18F]fluoride in the presence of an oxidant, thereby producing, when R3 in the compound of formula (I) is H, an 18F-labelled compound of formula (II), wherein EDG is as defined above and R1, R2, X1 and X2 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said monodentate cleavable surrogate group X4, a compound of formula (Ilc), wherein EDG' is O, NR5, -NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X3 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said bidentate cleavable surrogate group X4, a compound of formula (IIc) or a compound of formula (IId), wherein EDG' is O, NR5, -NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X4 are as defined herein.
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Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase (Thu, 29 Dec 2011)
The present invention provides nucleoside derivatives (principally uracil, cytosine and uridine derivatives) which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside derivatives alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside derivatives of the present invention.
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OLIGOMERIC COMPOUNDS AND METHODS (Fri, 23 Dec 2011)
<p id="p-0001" num="0000">The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.</p>
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BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 16 Dec 2011)
The present invention provides novel 3', 5 '-linked bicyclic nucleosides and oligomeric compounds prepared therefrom. The bicyclic nucleosides provided herein are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
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SUBSTITUTED 2 '-AMINO AND 2 '-THIO-BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 16 Dec 2011)
Provided herein are 2'-amino and 2'-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
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Oligomeric compounds and compositions for the use in modulation of micrornas (Thu, 24 Nov 2011)
Compounds, compositions and methods are provided for modulating the levels expression, processing and function of miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and miRNAs. The oligomeric compounds possess potent miRNA inhibitory activity, and further exhibit improved therapeutic index. Further provided are methods for selectively modulating miRNA activity in a cell.
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Oligomeric compounds and compositions for the use in modulation of micrornas (Thu, 24 Nov 2011)
Compounds, compositions and methods are provided for modulating the levels expression, processing and function of miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and miRNAs. The oligomeric compounds possess potent miRNA inhibitory activity, and further exhibit improved therapeutic index. Further provided are methods for selectively modulating miRNA activity in a cell.
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Antisense modulation of connective tissue growth factor expression (Thu, 24 Nov 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of connective tissue growth factor. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding connective tissue growth factor. Methods of using these compounds for modulation of connective tissue growth factor expression and for treatment of diseases associated with expression of connective tissue growth factor are provided.
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Aryl-aryl dendrimers (Fri, 11 Nov 2011)
<p id="p-0001" num="0000">Light emitting devices are described which incorporate, as the light emitting element, a dendrimer of which the constituent dendrons include a conjugated dendritic structure comprising aryl and/or heteroaryl groups connected to each other via bonds between sp<sup>2 </sup>hybridised ring atoms of said aryl or heteroaryl groups.</p>
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LIPID FORMULATED SINGLE STRANDED RNA (Fri, 11 Nov 2011)
The present invention provides compositions comprising a nucleic acid lipid particle and an oligomeric compound and uses thereof. In certain embodiments, such compositions are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.
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MODIFIED 5' DIPHOSPHATE NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 11 Nov 2011)
Provided herein are modified 5' diphosphate nucleosides and oligomeric compounds prepared therefrom. More particularly, modified 5' diphosphate nucleosides are provided that can be further modified at the 2' and 5' positions. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The oligomeric compounds are also expected to be useful as primers and probes in diagnostic applications.
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5' MODIFIED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 11 Nov 2011)
The present invention provides 5' modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5'- substituent and an optional 2' substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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MODIFIED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 11 Nov 2011)
The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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SUPERCONDUCTING MATERIALS (Fri, 04 Nov 2011)
<p id="p-0001" num="0000">Partially or fully saturated doped graphene materials are found to be superconducting. The saturation is with hydrogen or halogen. Doping is performed by substitution of carbon atoms or by applying an electric field. Diamond nano-rods are also found to be superconducting. These materials can be used in electronic devices having a gate.</p>
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5' AND 2' BIS-SUBSTITUTED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 04 Nov 2011)
<p id="p-0001" num="0000">The present invention provides modified nucleosides and oligomeric compounds prepared therefrom. More particularyl, the present invention provides modified nucleosides having at least one 5′-substituent and a 2′-O-substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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5'-END DERIVATIVES (Fri, 28 Oct 2011)
The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
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BIS-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS (Thu, 20 Oct 2011)
The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5'- methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.
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Antibacterial 4,6-substituted 6′, 6″ and 1 modified aminoglycoside analogs (Fri, 07 Oct 2011)
<p id="p-0001" num="0000">The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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5-azaindole bisphosphonates (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.</p>
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Hydroxybutyrate ester and medical use thereof (Fri, 30 Sep 2011)
<p id="p-0001" num="0000">A compound which is 3-hydroxybutyl 3-hydroxybutyrate enantiomerically enriched with respect to (3R)-hydroxybutyl (3R)-hydroxybutyrate of formula (I) is an effective and palatable precursor to the ketone body (3R)-hydroxybutyrate and may therefore be used to treat a condition which is caused by, exacerbated by or associated with elevated plasma levels of free fatty acids in a human or animal subject, for instance a condition where weight loss or weight gain is implicated, or to promote alertness or improve cognitive function, or to treat, prevent or reduce the effects of neurodegeneration, free radical toxicity, hypoxic conditions or hyperglycaemia.</p>
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IMIDAZO[1,2-a] PYRIDINYL BISPHOSPHONATES (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.</p>
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METHODS OF PREPARING 2'-O-SUBSTITUTED PURINE NUCLEOSIDES (Fri, 23 Sep 2011)
Provided herein are methods for preparing 2'-O-substituted purine nucleosides without protecting exocyclic amino groups on the base during alkylation. The methods are particularly useful in that the products are crystalline enabling purification without chromatography.
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5'-SUBSTITUTED BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 23 Sep 2011)
Provided herein are novel 5'-(S)-CH3 substituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the furanose ring of each of the novel 5'-(S)-CH3 substituted bicyclic nucleosides includes a 2' to 4' bridging group. The 5'-(S)-CH3 substituted bicyclic nucleosides are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as for example increasing the binding affinity. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Antisense modulation of PTP1B expression (Thu, 15 Sep 2011)
Compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.
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Vaccine against neisseria infection (Thu, 15 Sep 2011)
The invention relates to a vaccine for the treatment of disease caused by Neisseria, the vaccine comprising one or more immunogenic components for Neisseria serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating Neisseria infections. The immunogens are based on elements of the inner core lipopolysaccharide.
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ANTISENSE MODULATION OF STEAROYL-COA DESATURASE EXPRESSION (Fri, 02 Sep 2011)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of stearoyl-CoA desaturase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding stearoyl-CoA desaturase. Methods of using these compounds for modulation of stearoyl-CoA desaturase expression and for treatment of diseases associated with expression of stearoyl-CoA desaturase are provided.</p>
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Oligoribonucleotides and ribonucleases for cleaving RNA (Thu, 01 Sep 2011)
Oligomeric compounds including oligoribonucleotides and oligoribonucleosides are provided that have subsequences of 2'-pentoribofuranosyl nucleosides that activate dsRNase. The oligoribonucleotides and oligoribonucleosides can include substituent groups for increasing binding affinity to complementary nucleic acid strand as well as substituent groups for increasing nuclease resistance. The oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics. Also included in the invention are mammalian ribonucleases, i.e., enzymes that degrade RNA, and substrates for such ribonucleases. Such ribonuclease is referred to herein as a dsRNase, wherein "ds" indicates the RNase's specificity for certain double-stranded RNA substrates. The artificial substrates for the dsRNases described herein are useful in preparing affinity matrices for purifying mammalian ribonuclease as well as non-degradative RNA-binding proteins.
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CYCLOHEXENYL NUCLEIC ACID ANALOGS (Thu, 01 Sep 2011)
The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo- hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase (Thu, 25 Aug 2011)
The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside derivatives alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside derivatives of the present invention.
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PEPTIDE TAG SYSTEMS THAT SPONTANEOUSLY FORM AN IRREVERSIBLE LINK TO PROTEIN PARTNERS VIA ISOPEPTIDE BONDS (Fri, 19 Aug 2011)
The present invention concerns the use of a protein capable of spontaneously forming an isopeptide bond for the development of a peptide tag and binding partner pair wherein said peptide tag and binding partner are capable of covalently binding to each other via an isopeptide bond. The invention also provides a method for developing a peptide tag and binding partner pair which are capable of covalently binding to each other based on a protein which is capable of spontaneously forming an isopeptide bond. Additionally provided are peptide tag and binding partner pairs which are obtainable from isopeptide proteins. Further, specifically developed peptide tags and binding partners are encompassed, together with nucleic acid molecules and vectors which encode those peptides or proteins.
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SUBSTITUTED ALPHA-L-BICYCLIC NUCLEOSIDES (Thu, 18 Aug 2011)
The present disclosure describes substituted α-L-bicyclic nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, substituted α-L-bicyclic nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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IMIDAZO[1,2- ALPHA]PYRIDINYL BISPHOSPHONATES (Thu, 04 Aug 2011)
Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
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Vaccine (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine comprising one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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Conjugates For Use In Hepatocyte Free Uptake Assays (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The present invention provides methods of identifying oligomeric compounds, such as siRNA and double-stranded RNA compounds, having bioactivity in vivo, and kits.</p>
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Cyclohexenyl nucleic acids analogs (Fri, 15 Jul 2011)
<p id="p-0001" num="0000">The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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BASE MODIFIED BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 15 Jul 2011)
Provided herein are novel base modified bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel pyrimidine bicyclic nucleosides are provided wherein each pyrimidine base is substituted at the 5 position with an optionally substituted, aromatic or heteroaromatic ring system comprising from 5 to 7 ring atoms selected from C, N, O and S. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Metal-containing dendrimers (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">This invention relates to a hat emitting device which comprises at least one layer that contains an organometallic dendrimer having a core comprising a metal cation. The invention also relates to organometallic dendrimers and methods for producing the same.</p>
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Modulation of glucose-6-phosphatase translocase expression (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">Compositions and methods are provided for decreasing blood glucose levels in an animal, comprising administering to said animal an antisense inhibitor of glucose-6-phosphatase translocase expression alone or in combination with at least one glucose-lowering drug. Also provided are compositions and methods for treating diabetes and other metabolic disorders.</p>
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Antibacterial 4,5-substituted aminoglycoside analogs having multiple substituents (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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Substituted alpha-L-bicyclic nucleosides (Fri, 08 Jul 2011)
<p id="p-0001" num="0000">The present disclosure describes substituted α-L-bicyclic nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, substituted α-L-bicyclic nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Antisense modulation of acyl CoA cholesterol acyltransferase-2 expression (Thu, 16 Jun 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of acyl CoA cholesterol acyltransferase-2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding acyl CoA cholesterol acyltransferase-2. Methods of using these compounds for modulation of acyl CoA cholesterol acyltransferase-2 expression and for treatment of diseases associated with expression of acyl CoA cholesterol acyltransferase-2 are provided.
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Antisense inhibition of PTP1B expression (Thu, 09 Jun 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.
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Assay for Monitoring Activity of Jmjd6 (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">The invention provides a method for assaying Jmjd6 activity.</p>
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OLIGOMERIC COMPOUNDS HAVING AT LEAST ONE NEUTRALLY LINKED TERMINAL BICYCLIC NUCLEOSIDES (Fri, 03 Jun 2011)
<p id="p-0001" num="0000">The present disclosure describes oligomeric compounds having at least one bicyclic nucleoside attached to the 3′ or 5′ termini by a neutral internucleoside linkage and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Compounds and methods for modulating protein expression (Fri, 27 May 2011)
<p id="p-0001" num="0000">The present invention provides compounds and methods for modulating expression of a protein, including, but not limited to, modulating splicing of a pre-mRNA to modulate the amount of one or more variants of a protein.</p>
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Antisense modulation of C-reactive protein expression (Fri, 20 May 2011)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for treatment of diseases associated with expression of C-reactive protein are provided.</p>
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OLIGOMERIC COMPOUNDS COMPRISING BICYCLIC NUCLEOSIDES AND HAVING REDUCED TOXICITY (Fri, 13 May 2011)
<p id="p-0001" num="0000">In certain embodiments, the present invention provides oligomeric compounds having favorable toxicity profiles and therapeutic indexes. Compounds of the present invention comprise bicyclic nucleosides. Certain such bicyclic nucleosides are pyrimidines that do not include a methyl group at the 5-carbon. Oligomeric compounds comprising such nucleosides are less toxic than compounds comprising bicyclic nucleosides that do include a methyl group at the 5-carbon. In certain embodiments, the present invention provides methods of preparing and using such compounds.</p>
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1,4-QUINONES AND THEIR SULFUR ANALOGUES USEFUL AS LIGANDS OF N-ACETYLTRANSFERASES (Fri, 13 May 2011)
The invention provides 1,4-quinones, 1,4-naphthoquinones and their sulphur analogues as inhibitors of hNAT1, an enzyme which is both a diagnostic marker and drug target for breast cancer. Some of the compounds of the invention are also chromogenic in the presence of hNAT1. The compounds of the invention are used for detecting for and/or measuring hNAT1 and for inhibiting hNAT1 in the treatment of disease.
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Compositions and their uses directed to gemin genes (Fri, 06 May 2011)
<p id="p-0001" num="0000">Disclosed herein are compounds, compositions and methods for modulating the expression of a Gemin Gene. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.</p>
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TISSUE EXPANDER (Fri, 06 May 2011)
This invention relates to a tissue expander for use in medical, veterinary and dental applications. The tissue expander comprises a self-inflating polymer network and a biodegradable polymer having a non-degraded state and a degraded state which in the non- degraded state constrains the inflation of the self-inflating polymer network and in the degraded state allows inflation of the self-inflating polymer network. In a preferred embodiment, the self-inflating polymer network and the biodegradable polymer form an interpenetrating polymer network or a semi-interpenetrating polymer network. Alternatively or in addition, the self-inflating polymer network forms a core and the biodegradable polymer forms coating which partially or fully surrounds the core.
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CATALYSTS (Fri, 06 May 2011)
The present invention relates to novel metallocene catalysts of formula I, which is defined herein. The present invention also provides processes for making these catalysts and their use in olefin polymerisation reactions.
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TISSUE EXPANDER (Fri, 06 May 2011)
This invention relates to a tissue expander for use in medical, veterinary and dental applications. The tissue expander comprises a self-inflating polymer network and a biodegradable polymer having a non-degraded state and a degraded state which in the non- degraded state constrains the inflation of the self-inflating polymer network and in the degraded state allows inflation of the self-inflating polymer network. In a preferred embodiment, the self-inflating polymer network and the biodegradable polymer form an interpenetrating polymer network or a semi-interpenetrating polymer network. Alternatively or in addition, the self-inflating polymer network forms a core and the biodegradable polymer forms coating which partially or fully surrounds the core.</p>
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Antisense modulation of apolipoprotein (A) expression (Thu, 05 May 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of apolipoprotein(a). The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding apolipoprotein(a). Methods of using these compounds for modulating of apolipoprotein(a) expression and for treatment of diseases associated with expression of apolipoprotein(a) are provided.
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ANTISENSE MODULATION OF BCL2-ASSOCIATED X PROTEIN EXPRESSION (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of BCL2-associated X protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding BCL2-associated X protein. Methods of using these compounds for modulation of BCL2-associated X protein expression and for treatment of diseases associated with expression of BCL2-associated X protein are provided.</p>
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Compounds for imaging and therapy (Fri, 29 Apr 2011)
<p id="p-0001" num="0000">A metal complex of formula (III) wherein: M is a transition metal and A1, A2, X, X′, Y, L1′, R1′ and R2′ are as defined herein, is useful in medical imaging and therapy.</p>
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6-modified bicyclic nucleic acid analogs (Thu, 28 Apr 2011)
The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either ( R ) or ( S )-chirality at the 6-position. These bicyclic-nucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
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Oligomeric compounds comprising tricyclic nucelosides and methods for their use (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">The present disclosure provides tricyclic nucleosides, oligomeric compounds comprising at least one of the tricyclic nucleosides and methods of using the oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Modification of MYD88 splicing using modified oligonucleotides (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of MyD88. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding MyD88. Methods of using these compounds for modulation of MyD88 expression and for treatment of diseases associated with expression of MyD88 are provided.</p>
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PROCESS FOR PRODUCING METHANOL (Fri, 22 Apr 2011)
The present invention relates to a novel process for the production of methanol. The process comprises the heterolytic cleavage of hydrogen by a frustrated Lewis pair comprising a Lewis acid and a Lewis base; and the hydrogenation of CO2 with the heterolytically cleaved hydrogen to form methanol.
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Receptor Modulators (Fri, 15 Apr 2011)
<p id="p-0001" num="0000">Method of identifying a modulator of CD28 comprising comparing a structural model of a candidate modulator with a structural model of CD28 to thereby determine whether the modulator will bind to CD28, wherein the structural model is derived from, or comprises, structural coordinates of a crystal of: (i) CD28, (ii) a fragment of CD28, or (iii) a homologue of (i) or (ii). The crystal of CD28 in a soluble form complexed with the Fab fragment of a mitogenic (superagonistic) antibody has been obtained and used for the determination of the 3D-structure of the receptor. The application also relates to modulators of superagonistic signalling for any receptor of the CD28 family, i.e. to superagonistic antibodies and chimeric proteins thereof, and to the screening of the superagonistic modulators. In the methods of screening, the binding of the candidate modulators to a portion of the receptor proximal to the cell membrane is investigated.</p>
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Bicyclic cyclohexitol nucleic acid analogs (Fri, 01 Apr 2011)
<p id="p-0001" num="0000">The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.79mm" wi="56.73mm" file="US08530640-20130910-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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JMJD2 DEMETHYLASE INHIBITORS (Fri, 18 Mar 2011)
The present invention relates to inhibitors of JMJD2 subfamily histone lysyl demethylase enzymes. In particular, the invention relates to compounds that are capable of inhibiting a JMJD2 subfamily histone lysyl demethylase without also inhibiting a 2-oxoglutarate dependent oxygenase that is not a JMJD2 subfamily histone lysyl demethylase, and to assays for the identification of inhibitors of JMJD2 subfamily histone lysyl demethylase enzymes.
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DETECTION OF MYCOBACTERIA (Fri, 18 Mar 2011)
A method for determining the presence of mycobacteria species in an organism or biological sample, the method comprising adding to the organism or biological sample a probe molecule comprising a substrate and a label, which probe molecule can be incorporated into mycobacteria, the presence of mycobacteria being determined by a detector responsive to the presence of the label, optionally after applying a stimulus; suitable probe molecules include compounds comprising a label and a substrate, which label is can be detected by a detector responsive to the presence of the label, optionally after applying a stimulus, characterised by compound being able to engage with the active site of Antigen 85B (Ag85B) such that it can form simultaneous hydrogen bonds with two or more amino acids in the active site selected from Arg 43, Trp 264, Ser126, His 262 and Leu 42, or the corresponding amino acids in Antigen 85A (Ag85A) or Antigen 85C (Ag85C), at least one of which is with Ser126.
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Protein Glycosylation (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">The present invention relates to methods for glycosylating a protein in which the protein is modified to include an alkyne and/or an azide group. The invention further relates to a protein glycosylated by these methods.</p>
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Branched materials for photovoltaic devices (Fri, 11 Mar 2011)
<p id="p-0001" num="0000">The invention provides a dye-sensitized photovoltaic device which comprises: a first electrode; a second electrode; and, disposed between the first and second electrodes: an electron acceptor material which comprises a semiconductive metal oxide, a redox mediator material, and a photosensitizing dye which comprises a dendrimer of formula (I): [X]<sub>m</sub>-CORE-[[Y]<sub>p</sub>-[DENDRON]]<sub>n </sub>wherein n, m, p, CORE, DENDRON, X and Y are as defined herein. The invention further provides a photosensitizing dye which is a dendrimer of formula (I), and the use, as a photosensitizing dye in a dye-sensitized photovoltaic device, of a compound which is a dendrimer of formula (T). Novel dendrimers of formula (T) are also provided. Novel catechol-based compounds are also provided. The catechol-based compounds can be used together with the dendrimers of formula (T) as the photosensitizing dyes in a photovoltaic device. Accordingly, the invention further provides photosensitizing dyes and dye-sensitized photovoltaic devices comprising such catechol compounds, and the use of such catechol compounds as photosensitizing dyes in a dye-sensitized photovoltaic device.</p>
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Antisense oligonucleotide modulation of STAT3 expression (Fri, 04 Mar 2011)
<p id="p-0001" num="0000">Compounds, compositions and methods are provided for inhibiting the expression of human STAT3. The compositions comprise antisense oligonucleotides targeted to nucleic acids encoding STAT3. Methods of using these oligonucleotides for inhibition of STAT3 expression and for promotion of apoptosis are provided. Methods for treatment of diseases, particularly inflammatory diseases and cancers, associated with overexpression or constitutive activation of STAT3 or insufficient apoptosis are also provided.</p>
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OLIGOMERIC COMPOUNDS COMPRISING NEUTRALLY LINKED TERMINAL BICYCLIC NUCLEOSIDES (Thu, 24 Feb 2011)
The present disclosure describes oligomeric compounds having at least one bicyclic nucleoside attached to the 3' or 5' termini by a neutral internucleoside linkage and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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ANTISENSE MODULATION OF HYDROXYSTEROID 11-BETA DEHYDROGENASE 1 EXPRESSION (Fri, 18 Feb 2011)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of hydroxysteroid 11-beta dehydrogenase 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hydroxysteroid 11-beta dehydrogenase 1. Methods of using these compounds for modulation of hydroxysteroid 11-beta dehydrogenase 1 expression and for treatment of diseases associated with expression of hydroxysteroid 11-beta dehydrogenase 1 are provided.</p>
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ASSAY FOR MONITORING ACTIVITY OF JMJD6 (Thu, 17 Feb 2011)
The invention provides a method for assaying Jmjd6 activity.
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BICYCLIC CYCLOHEXOSE NUCLEIC ACID ANALOGS (Fri, 11 Feb 2011)
The present invention provides bicyclic cyclohexose nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
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METHOD OF PREPARING POLYPEPTIDES FOR CRYO-TRANSMISSION ELECTRON MICROSCOPY (CRYO-EM) AND STRUCTURE DETERMINATION USING DNA LATTICES (Fri, 04 Feb 2011)
The present invention relates to method for preparing a substance for cryo-transmission electron microscopy (cryo-EM). The present invention also relates to a method for determining the three-dimensional structure of a substance using cryo-EM. The substance is a polypeptide incorporated in a DNA/RNA lattice. The polypeptide may comprise a ligand and may be linked to the DNA nanostructure via tags such as a poly histidine tag.
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Antisense modulation of C-reactive protein expression (Thu, 03 Feb 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for treatment of diseases associated with expression of C-reactive protein are provided.
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Modulation of forkhead box O1A expression (Thu, 13 Jan 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding forkhead box O1A. Methods of using these compounds for modulation of forkhead box O1A expression and for treatment of diseases associated with expression of forkhead box O1A are provided, in particular, for methods of treating diabetes.
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Antisense modulation of apolipoprotein (A) expression (Thu, 13 Jan 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of apolipoprotein(a). The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding apolipoprotein(a). Methods of using these compounds for modulating of apolipoprotein(a) expression and for treatment of diseases associated with expression of apolipoprotein(a) are provided.
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Antisense modulation of superoxide dismutase 1, soluble expression (Thu, 06 Jan 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of superoxide dismutase 1, soluble. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding superoxide dismutase 1, soluble. Methods of using these compounds for modulation of superoxide dismutase 1, soluble expression and for treatment of diseases associated with expression of superoxide dismutase 1, soluble are provided.
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Antisense modulation of insulin-like growth factor binding protein 5 expression (Thu, 06 Jan 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of insulin-like growth factor binding protein 5. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding insulin-like growth factor binding protein 5. Methods of using these compounds for modulation of insulin-like growth factor binding protein 5 expression and for treatment of diseases associated with expression of insulin-like growth factor binding protein 5 are provided.
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Antisense modulation of insulin-like growth factor binding protein 5 expression (Thu, 06 Jan 2011)
Antisense compounds, compositions and methods are provided for modulating the expression of insulin-like growth factor binding protein 5. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding insulin-like growth factor binding protein 5. Methods of using these compounds for modulation of insulin-like growth factor binding protein 5 expression and for treatment of diseases associated with expression of insulin-like growth factor binding protein 5 are provided.
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Carbocyclic alpha-L-bicyclic nucleic acid analogs (Fri, 31 Dec 2010)
<p id="p-0001" num="0000">The present invention provides novel carbocyclic α-L-bicyclic nucleosides and oligomeric compounds comprising at least one of these carbocyclic α-L-bicyclic nucleosides. The carbocyclic α-L-bicyclic nucleosides are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into including nuclease resistance.</p>
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Oligomeric compounds comprising 4′-thionucleosides for use in gene modulation (Fri, 24 Dec 2010)
<p id="p-0001" num="0000">The present invention provides modified oligomeric compounds and compositions of oligomeric compounds for use in the RNA interference pathway of gene modulation. The modified oligomeric compounds include siRNA and asRNA having at least one affinity modification.</p>
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MODULATION OF HIF1 BETA EXPRESSION (Fri, 17 Dec 2010)
<p id="p-0001-en" num="0000">Compounds, compositions and methods are provided for modulating the expression of HIF1-beta. The compositions comprise oligonucleotides, targeted to nucleic acid encoding HIF1-beta. Methods of using these compounds for modulation of HIF1-beta expression and for diagnosis and treatment of diseases and conditions associated with expression of HIF1-beta are provided.</p>
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Modulation of forkhead box O1A expression (Fri, 10 Dec 2010)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding forkhead box O1A. Methods of using these compounds for modulation of forkhead box O1A expression and for treatment of diseases associated with expression of forkhead box O1A are provided, in particular, for methods of treating diabetes.</p>
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Drug delivery system (Fri, 10 Dec 2010)
<p id="p-0001" num="0000">A drug delivery system for the controlled release of a pharmaceutically-active compound by oral route comprises an intercalate of a layered double hydroxide having, before intercalation, layers of metal hydroxides, and having intercalated therein a pharmaceutically-active compound having at least one anionic group. A preferred layered double hydroxide is one that has layers which comprise [LiAl<sub>2</sub>(OH)<sub>6</sub>]<sup>+</sup>. The drug delivery system has use in the delivery of drugs such as 4-biphenylacetic acid, Diclofenac, Gemfibrozil, Ibuprofen, Naproxen, 2-Propylpentanoic acid and Tolfenamic acid.</p>
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CHEMICAL MODIFICATION OF PROTEINS (Thu, 02 Dec 2010)
The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
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Modulation of eIF4E expression (Thu, 02 Dec 2010)
Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided.
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Modulation of eIF4E expression (Thu, 02 Dec 2010)
Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided.
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MOLECULAR ADAPTORS (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">The invention relates to transmembrane protein pore for use in detecting a analyte in a sample. The pore comprises a molecular adaptor that facilitates an interaction between the pore and the analyte. The adaptor is covalently attached to the pore in an orientation that allows the analyte to be detected using the pore.</p>
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PREPARATION OF LABELLED COMPOUNDS (Fri, 26 Nov 2010)
The invention relates to a process for producing a labelled compound, which process comprises treating a compound of formula (I), wherein X is a moiety to be labelled or a detectable label, and R1, R2, R3 and R4 are substitutent groups as defined herein; with a compound of formula (II) : N3-L-Y (π) wherein Y is a detectable label or a moiety to be labelled, provided that if X in the compound of formula (I) is a moiety to be labelled, then Y is a detectable label and if X in the compound of formula (I) is a detectable label, then Y is a moiety to be labelled; and L is a bond or a linking group, thereby producing a labelled compound of formula (IH) by Staudinger Ligation. Groups R3 and R4 may comprise fluorous moieties, in order to facilitate purification of the labelled compound of formula (IH). The invention also provides methods of imaging a human or non-human patient or a cell or in vitro sample, using the labelled compound of formula (III) thus produced, as well as imaging methods in which the compounds of formulae (I) and (II) are administered to the patient, cell or sample. The invention further provides novel compounds of formula (I) and formula (III), a process for producing the compounds of formula (T), and a combination product for medical imaging comprising a compound of formula (I) and a compound of formula (II).
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Antisense modulation of PTP1B expression (Thu, 04 Nov 2010)
Compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.
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Assay for identifying a modulator of HIF hydroxylase (Fri, 29 Oct 2010)
<p id="p-0001" num="0000">A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.</p>
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PROCESS FOR THE PREPARATION OF (3R)-HYDR0XYBUTYL (3R) -HYDROXYBUTYRATE BY ENZYMATIC ENANTIOSELECTIVE REDUCTION EMPLOYING LACTOBACILLUS BREVIS ALCOHOL DEHYDROGENASE (Fri, 22 Oct 2010)
A process for producing a compound which is (3R)-hydroxybutyl (3R)- hydroxybutyrate of formula (I) which process comprises submitting, to enantioselective reduction, a compound of the following formula (II), (III) or (IV).
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PROCESS FOR THE PREPARATION OF (3R)-HYDR0XYBUTYL (3R) -HYDROXYBUTYRATE BY ENZYMATIC ENANTIOSELECTIVE REDUCTION EMPLOYING LACTOBACILLUS BREVIS ALCOHOL DEHYDROGENASE (Fri, 22 Oct 2010)
A process for producing a compound which is (3R)-hydroxybutyl (3R)- hydroxybutyrate of formula (I) which process comprises submitting, to enantioselective re-duction, a compound of the following formula (II), (III) or (IV). </p>
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MUTANT ENZYMES (Fri, 24 Sep 2010)
<p id="p-0001-en" num="0000">This invention relates to mutant enzymes with enhanced properties and processes for oxidation of organic compound substrates using such enzymes.</p>
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Supports for oligomer synthesis (Fri, 17 Sep 2010)
<p id="p-0001" num="0000">Universal linkers, their facile processes of manufacture and methods of using the same are provided.</p>
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Reactive organometallic dendrimers (Fri, 10 Sep 2010)
<p id="p-0001" num="0000">A process for modifying at least one dendron that is intended to form part of a dendrimer is disclosed. One reacts at least one reactable unsaturated group in a chemoselective manner to form a less unsaturated group. Also disclosed is a process for modifying dendrimers in a similar manner.</p>
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USE OF ANTISENSE OLIGONUCLEOTIDE LIBRARIES FOR IDENTIFYING GENE FUNCTION (Fri, 03 Sep 2010)
<p id="p-0001-en" num="0000">A method for identifying one or more genes involved in a phenotype of cells, tissues or organisms, comprising the steps of contacting cells, tissues or organisms which exhibit the phenotype with a library of antisense oligonucleotides and performing a primary phenotypic assay to determine which antisense oligonucleotides in the library attenuate the phenotype. These antisense oligonucleotides correspond to genes involved in the phenotype. The method may be used to identify genes involved in various disease states.</p>
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6-modified bicyclic nucleic acid analogs (Fri, 27 Aug 2010)
<p id="p-0001" num="0000">The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 6-position. These bicyclicnucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.</p>
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Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation (Fri, 27 Aug 2010)
<p id="p-0001" num="0000">Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modification comprising a polycyclic sugar surrogate. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleoside of the oligomer has a polycyclic sugar surrogate modification.</p>
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Method for assaying FTO (2-oxoglutarate dependent oxygenase) activity (Fri, 27 Aug 2010)
<p id="p-0001" num="0000">The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO.</p>
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Antisense modulation of superoxide dismutase 1, soluble expression (Thu, 26 Aug 2010)
Antisense compounds, compositions and methods are provided for modulating the expression of superoxide dismutase 1, soluble. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding superoxide dismutase 1, soluble. Methods of using these compounds for modulation of superoxide dismutase 1, soluble expression and for treatment of diseases associated with expression of superoxide dismutase 1, soluble are provided.
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OLIGOMERIC COMPOUNDS AND METHODS (Fri, 13 Aug 2010)
The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds, as RNAi compounds, and/or as modulators of splicing.
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TETRAHYDROPYRAN NUCLEIC ACID ANALOGS (Fri, 13 Aug 2010)
The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel tetrahydropyran nucleoside analogs are provided having at least one chiral substituent that are expected to be useful for enhancing one or more properties of oligomeric compounds such as nuclease resistance and/or binding affinity. In certain embodiments, the oligomeric compounds are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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ANTISENSE MODULATION OF ACYL COA CHOLESTEROL ACYLTRANSFERASE-2 EXPRESSION (Fri, 06 Aug 2010)
<p id="p-0001-en" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of acyl CoA cholesterol acyltransferase-2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding acyl CoA cholesterol acyltransferase-2. Methods of using these compounds for modulation of acyl CoA cholesterol acyltransferase-2 expression and for treatment of diseases associated with expression of acyl CoA cholesterol acyltransferase-2 are provided.</p>
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Antisense inhibition of PTP1B expression (Thu, 05 Aug 2010)
Antisense compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.
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5'-Substituted-2-F' Modified Nucleosides and Oligomeric Compounds Prepared Therefrom (Fri, 30 Jul 2010)
<p id="p-0001-en" num="0000">The present invention provides 5′-substituted-2′-F nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In one preferred embodiment the nucleoside analogs have either (R) or (5)-chirality at the 5′-position. These nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance.</p>
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5′-modified bicyclic nucleic acid analogs (Fri, 23 Jul 2010)
<p id="p-0001" num="0000">The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.</p>
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Identification of novel pathways, genes and promoter motifs regulating adipogenesis (Wed, 21 Jul 2010)
<p id="p-0001-en" num="0000">The present invention provides compounds, compositions, and methods for identification of motifs within regulatory regions of genes involved in adipogenesis and adipocyte differentiation. Compounds and compositions are provided for modulating expression of nuclear receptor/transcription factor-regulated genes. Methods for modulating the function of PPAR-γ as well as PPAR-γ-regulated gene promoters, and methods of using oligomeric compounds for diagnosis and treatment of diseases such as obesity and diabetes are also provided.</p>
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Compositions and their uses directed to Gemin Genes (Wed, 21 Jul 2010)
<p id="p-0001-en" num="0000">Disclosed herein are compounds, compositions and methods for modulating the expression of a Gemin Gene. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.</p>
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BIS-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 09 Jul 2010)
The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5'- methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.
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Antisense modulation of survivin expression (Thu, 24 Jun 2010)
Antisense compounds, compositions and methods are provided for modulating the expression of Survivin. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding Survivin. Methods of using these compounds for modulation of Survivin expression and for treatment of diseases associated with expression of Survivin are provided.
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OLIGORIBONUCLEOTIDES AND RIBONUCLEASES FOR CLEAVING RNA (Fri, 18 Jun 2010)
<p id="p-0001-en" num="0000">Oligomeric compounds including oligoribonucleotides and oligoribonucleosides are provided that have subsequences of 2′-pentoribofuranosyl nucleosides that activate dsRNase. The oligoribonucleotides and oligoribonucleosides can include substituent groups for increasing binding affinity to complementary nucleic acid strand as well as substituent groups for increasing nuclease resistance. The oligomeric compounds are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics. Also included in the invention are mammalian ribonucleases, i.e., enzymes that degrade RNA, and substrates for such ribonucleases. Such a ribonuclease is referred to herein as a dsRNase, wherein “ds” indicates the RNase's specificity for certain double-stranded RNA substrates. The artificial substrates for the dsRNases described herein are useful in preparing affinity matrices for purifying mammalian ribonuclease as well as non-degradative RNA-binding proteins.</p>
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Aryl-aryl dendrimers (Fri, 28 May 2010)
<p id="p-0001" num="0000">Light emitting devices are described which incorporate, as the light emitting element, a dendrimer of which the constituent dendrons include a conjugated dendritic structure comprising aryl and/or heteroaryl groups connected to each other via bonds between sp<sup>2 </sup>hybridized ring atoms of said aryl or heteroaryl groups.</p>
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Benzimidazoles and analogs thereof as antivirals (Fri, 28 May 2010)
<p id="p-0001" num="0000">Provided are compounds of the formula:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.98mm" wi="37.42mm" file="US08207173-20120626-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">wherein R<sup>N1 </sup>is a substituent of formula G<sup>1</sup>-NX<sup>1</sup>X<sup>2</sup>, wherein G<sup>1 </sup>is an optionally further substituted alkylene, which optionally forms, together with R<sup>N2</sup>, a cyclic group, and each of X<sup>1 </sup>and X<sup>2 </sup>is independently H or an N-substituent, or X<sup>1 </sup>and X<sup>2 </sup>together form a heterocyclic ring, or X<sup>1 </sup>together with G<sup>1 </sup>forms a cyclic group and X<sup>2 </sup>is H or an N-substituent; and each of Z<sup>1</sup>, Z<sup>2</sup>, Z<sup>3 </sup>and Z<sup>4 </sup>is H or a substituent, or two of Z<sup>1</sup>, Z<sup>2</sup>, Z<sup>3 </sup>and Z<sup>4 </sup>together form an optionally substituted ring, and further wherein at least one of Z<sup>1</sup>, Z<sup>2</sup>, Z<sup>3 </sup>and Z<sup>4 </sup>is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.</li> </ul> </li> </ul> </p>
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Antisense oligonucleotides directed against connective tissue growth factor and uses thereof (Fri, 28 May 2010)
<p id="p-0001" num="0000">This invention provides compounds which comprise modified oligonucleotides capable of inhibitory expression of connective tissue factor and composition containing same as well as methods of treating hyperprolific disorders and fibrotic diseases, and of reducing scarring resulting from wound healing using such compounds.</p>
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TETRAHYDROPYRAN NUCLEIC ACID ANALOGS (Thu, 27 May 2010)
The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Bis-modified bicyclic nucleic acid analogs (Fri, 14 May 2010)
<p id="p-0001" num="0000">The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5′-methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.</p>
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PYRROLIDINE COMPOUNDS (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">The present invention relates to a process for the preparation of a pyrrolidone compound of the formula (I): where R<sup>1 </sup>is substituted or unsubstituted alkyl, alkenyl, or alkynyl, or an aromatic or non-aromatic cyclic or heterocyclic structure, R<sup>2 </sup>is substituted or unsubstituted alkyl or cycloalkyl, and each P is independently a protecting group.</p> <p id="p-0002-en" num="0000"/>
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Modulation of HIF1-beta expression (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">Compounds, compositions and methods are provided for modulating the expression of HIF1-beta. The compositions comprise oligonucleotides, targeted to nucleic acid encoding HIF1-beta. Methods of using these compounds for modulation of HIF1-beta expression and for diagnosis and treatment of diseases and conditions associated with expression of HIF1-beta are provided.</p>
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Modulation of EIF4E expression (Thu, 06 May 2010)
Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided
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Pentalenes (Fri, 30 Apr 2010)
<p id="p-0001" num="0000">The present invention relates to per-substituted pentalene compounds, including permethylpentalene and precursors thereof. In particular, the invention provides substituted pentalene compounds and methods of preparing substituted pentalene compounds; complexes of metals with substituted pentalene compounds and methods for their production; and the use of complexes of metals with substituted pentalene compounds in catalysis.</p>
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METHODS FOR PREPARING HETEROCYCLIC RINGS (Fri, 30 Apr 2010)
A process for preparing an enantiomerically enriched compound containing a substituted heterocyclic ring, said process comprising a carbon-carbon bond formation reaction in the presence of a crotonase superfamily protein or a homolog or variant thereof.
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METHODS OF USING OLIGOMERIC COMPOUNDS COMPRISING 2'-SUBSTITUTED NUCLEOSIDES (Fri, 30 Apr 2010)
The present disclosure provides oligomeric compounds comprising at least one 2'-fluoroethoxy modified nucleoside of formula I and methods of using these oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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OLIGOMERIC COMPOUNDS AND METHODS (Fri, 30 Apr 2010)
The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds or as RNAi compounds.
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5' AND 2' BIS-SUBSTITUTED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 30 Apr 2010)
The present invention provides modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5'-substituent and a 2'-O-substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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5' AND 2' BIS-SUBSTITUTED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 30 Apr 2010)
The present invention provides modified nucleosides and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides having at least one 5'- substituent and a 2'-O-substituent, oligomeric compounds comprising at least one of these modified nucleosides and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. </p>
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HISTONE LYSINE DEMETHYLASE INHIBITORS (Fri, 23 Apr 2010)
The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression.
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6-DISUBSTITUTED BICYCLIC NUCLEIC ACID ANALOGS (Thu, 22 Apr 2010)
The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2'-O-C(Ri)(R2)-4' or 2'-O- C=(R3)(R.4)-4' bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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NOVEL ENZYME (Fri, 16 Apr 2010)
The invention provides an isolated formate dehydrogenase (FDH) polypeptide specific for NADP+and an isolated FDH polypeptide having an adenine ribose recognition loop comprising a first large amino acid and a second amino acid, wherein the first and second amino acid are arranged in space to allow the second amino acid to bond with a phosphate group. Also provided is a variant of an BAD+specific FDH polypeptide, wherein the adenine ribose recognition loop has been mutated at least one position to alter the three dimensional polypeptide structure of the adenine ribose recognition loop to allow a phosphate group to be recognised. The polypeptides of the invention can be used in the conversion of NADP+to NADP or in the conversion of BAD+ to NASH.
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ANTISENSE OLIGONUCLEOTIDES DIRECTED AGAINST CONNECTIVE TISSUE GROWTH FACTOR AND USES THEREOF (Fri, 16 Apr 2010)
This invention provides compounds which comprise modified oligonucleotides capable of inhibitory expression of connective tissue growth factor and composition containing same as well as methods of treating hyperprolific disorders and fibrotic diseases, and of reducing scarring resulting from wound healing using such compounds.
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ANTISENSE OLIGONUCLEOTIDES DIRECTED AGAINST CONNECTIVE TISSUE GROWTH FACTOR AND USES THEREOF (Fri, 16 Apr 2010)
This invention provides compounds which comprise modified oligonucleotides capable of inhibitory expression of connective tissue growth factor and composition containing same as well as methods of treating hyperprolific disorders and fibrotic diseases, and of reducing scarring resulting from wound healing using such compounds. </p>
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A METHOD FOR ASSAYING FTO (2-OXOGLUTARATE DEPENDENT OXYGENASE) ACTIVITY (Thu, 08 Apr 2010)
The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO.
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CYCLOHEXENYL NUCLEIC ACID ANALOGS (Fri, 02 Apr 2010)
The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo- hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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SUBSTITUTED ALPHA-L-BICYCLIC NUCLEOSIDES (Fri, 02 Apr 2010)
The present disclosure describes substituted α-L-bicyclic nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, substituted α-L-bicyclic nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Metal-containing dendrimers (Fri, 26 Mar 2010)
<p id="p-0001" num="0000">This invention relates to a light emitting device which comprises at least one layer that contains an organometallic dendrimer having a core comprising a metal cation. The invention also relates to organometallic dendrimers and methods for producing the same.</p>
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4-AZAINDOLE BISPHOSPHONATES (Fri, 26 Mar 2010)
Novel 4-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
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IMIDAZO[1,2-α ]PYRIDINYL BISPHOSPHONATES (Fri, 26 Mar 2010)
Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
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5-AZAINDOLE BISPHOSPHONATES (Fri, 26 Mar 2010)
Novel 5-azaindole bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.
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ANTIBACTERIAL 4,6-SUBSTITUTED 6', 6" AND 1 MODIFIED AMINOGLYCOSIDE ANALOGS (Fri, 19 Mar 2010)
The present invention is directed to aminoglycoside compounds of general formula (I) as well as their preparation and use as prophylactic or therapeutics against microbial infection.
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NOVEL RECEPTOR AND USES THEREOF (Fri, 19 Mar 2010)
The invention provides agents that modulate the effect of a two pore calcium channel (TPC) polypeptide for use in the treatment or prophylaxis of a condition, disease or disorder associated with NAADP receptor-mediated biological activity. The invention also provides methods of identifying agents that modulate the effect of NAADP receptor mediated biological activity, and kits for use in such methods. Methods for the treatment or prophylaxis of a condition, disease or disorder associated with NAADP receptor- mediated biological activity are also provided.
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METHOD FOR REDUCING SCARRING DURING WOUND HEALING USING ANTISENSE COMPOUNDS DIRECTED TO CTGF (Fri, 12 Mar 2010)
This invention provides a method for reducing hypertropic scarring resulting from dermal wound healing in a subject in need which comprises administering to the subject an antisense oligonucleotide which inhibits expression of connective tissue growth factor (CTGF) in an amount effective to inhibit expression of CTGF and thereby reduce hypertrophic scarring.
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METHOD FOR REDUCING SCARRING DURING WOUND HEALING USING ANTISENSE COMPOUNDS DIRECTED TO CTGF (Fri, 12 Mar 2010)
This invention provides a method for reducing hypertropic scarring resulting from dermal wound healing in a subject in need which comprises administering to the subject an antisense oligonucleotide which inhibits expression of connective tissue growth factor (CTGF) in an amount effective to inhibit expression of CTGF and thereby reduce hypertrophic scarring.
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Compositions and their uses directed to HBXIP (Fri, 05 Mar 2010)
<p id="p-0001" num="0000">Disclosed herein are compounds, compositions and methods for modulating the expression of HBXIP in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.</p>
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HYDROXYBUTYRATE ESTER AND MEDICAL USE THEREOF (Fri, 26 Feb 2010)
A compound which is 3-hydroxybutyl 3-hydroxybutyrate enantiomerically enriched with respect to (3Λ)»hydroxybutyl (3i?)-hydroxybutyrate of formula (I): is an effective and palatable precursor to the ketone body (3Λ)-hydroxybutyrate and may therefore be used to treat a condition which is caused by, exacerbated by or associated with elevated plasma levels of free fatty acids in a human or animal subject, for instance a condition where weight loss or weight gain is implicated, or to promote alertness or improve cognitive function, or to treat, prevent or reduce the effects of, neuro degeneration, free radical toxicity, hypoxic conditions or hyperglycaemia.
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HYDROXYBUTYRATE ESTER AND MEDICAL USE THEREOF (Fri, 26 Feb 2010)
A compound which is 3-hydroxybutyl 3-hydroxybutyrate enantiomerically enriched with respect to (3.LAMBDA.) hydroxybutyl (3i?)-hydroxybutyrate of formula (I): is an effective and palatable precursor to the ketone body (3.LAMBDA.)-hydroxybutyrate and may therefore be used to treat a condition which is caused by, exacerbated by or associated with elevated plasma levels of free fatty acids in a human or animal subject, for instance a condition where weight loss or weight gain is implicated, or to promote alertness or improve cognitive function, or to treat, prevent or reduce the effects of, neuro degeneration, free radical toxicity, hypoxic conditions or hyperglycaemia. </p>
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Modulators of asparaginyl hydoxylase activity of FIH (Thu, 25 Feb 2010)
A method of identifying, screening, characterising or designing a chemical entity, which mimics or binds to FIH, is described. The method comprises comparing a structural model of FIH with a structural model for said chemical entity, wherein said structural model of FIH is derived from structural factors or structural coordinates determined by subjecting to X-ray diffraction measurements a crystal comprising FIH. Such chemical entities may be used in the treatment of a condition associated with increased or decreased HIF levels or activity.
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Antisense modulation of connective tissue growth factor expression (Fri, 12 Feb 2010)
<p id="p-0001-en" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of connective tissue growth factor. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding connective tissue growth factor. Methods of using these compounds for modulation of connective tissue growth factor expression and for treatment of diseases associated with expression of connective tissue growth factor are provided.</p>
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Vaccine (Fri, 22 Jan 2010)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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Vaccine (Fri, 22 Jan 2010)
<p id="p-0001-en" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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PREPARATION OF FLUORINE-LABELLED COMPOUNDS (Fri, 22 Jan 2010)
The invention relates to a process for producing a fluorine-labelled compound, the process comprising: (a) treating a compound of formula (I) wherein R1, R2 and the C(H) group to which R1 and R2 are bonded together form a moiety to be labelled with fluorine; and the fluorous tag is a group of formula (II) wherein Rf is a straight-chained or branched C4-I2 perfluoroalkyl group; and L is a single bond, -alk-, -arylene-, -alk-arylene-, alk-X-, -arylene-X-, -alk-arylene-X, -alk- X-arylene-, -alk-X-arylene-X-, -arylene-alk-, -arylene-X-alk-, -arylene-alk-X- or - arylene-X-alk-X-, wherein X is N(R"), O, S, C(O) or C(O)N(R") and wherein alk is unsubstituted or substituted C1-10 alkylene which is optionally interrupted by N(R"), O, S, C(O), C(O)N(R") or arylene, wherein R" is C1-6 alkyl or aryl; with [nF], wherein nF is 18F or 19F, thereby fluorinating and detagging the compound of formula (I) to produce a fluorine-labelled compound of formula (III) The invention further relates to compounds of formula (I), a process for producing such compounds, and a combination product which comprises the two reactants used in that process.
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Vaccine (Fri, 15 Jan 2010)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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Vaccine (Fri, 15 Jan 2010)
<p id="p-0001" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine comprising one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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ANTISENSE MODULATION OF APOLIPOPROTEIN B EXPRESSION (Fri, 01 Jan 2010)
<p id="p-0001-en" num="0000">Methods for the rapid and long-term lowering of lipid levels in human subjects and for the treatment of conditions associated with elevated LDL-cholesterol and elevated apolipoprotein B are provided.</p>
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Asymmetric dendrimers (Fri, 01 Jan 2010)
<p id="p-0001" num="0000">Asymmetric light-emitting dendrimers having the formulae: (a) CORE-[DENDRITE1]n[DENDRITE2]m and (b) CORE-[DENDRITE]n are disclosed.</p>
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PYRIDO-INDOLE-CARBOXYLIC ACID COMPOUNDS (Thu, 31 Dec 2009)
A compound according to formula (I), (IA), (II)a or (II)band uses thereof.
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OLEFIN METATHESIS REACTIONS OF AMINO ACIDS, PEPTIDES AND PROTEINS CONTAINING ALLYL SULFIDE GROUPS (Fri, 11 Dec 2009)
A method for the modification of an amino acid, protein or peptide is disclosed. The method comprises reacting a carbon-carbon double bond-containing compound with an amino acid, a protein or a peptide containing an allyl sulfide group in the presence of a catalyst which promotes olefin metathesis, to form a modified amino acid, protein or peptide. Preferred carbon-carbon double bond-containing compounds include carbohydrates.
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METHOD OF PREPARING NUCLEOSIDES AND ANALOGS THEREOF WITHOUT USING CHROMATOGRAPHY (Fri, 27 Nov 2009)
Provided herein are methods for preparing purified modified nucleosides from reaction mixtures using precipitation as opposed to traditional chromatographic methods. The methods are particularly amenable to protected nucleosides and nucleoside phosphoramidites wherein the nucleosides can be modified.
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ASSAY FOR MONITORING ACTIVITY OF JMJD6 (Fri, 27 Nov 2009)
The invention provides a method for assaying Jmjd6 activity.
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POLYMERIC BEADS FOR OLIGOMER SYNTHESIS (Fri, 20 Nov 2009)
<p id="p-0001-en" num="0000">The present invention provides solid support media for use in oligomer synthesis, methods of producing the media, and methods of using the media. In some embodiments, the processes of the invention comprise (a) providing an organic phase comprising an olefin monomer, a cross-linker, a functionalizing reagent and an initiator; and (b) contacting the organic phase with an aqueous phase under conditions of time and temperature effective to form the polymeric bead.</p>
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ASSAYS FOR MODULATORS OF ASPARAGINYL HYDROXYLASE (Fri, 20 Nov 2009)
<p id="p-0001-en" num="0000">The present invention is directed to methods of identifying an agent which modulates hydroxylation of hypoxia inducible factor (HIF), comprising contacting a HIF asparagine hydroxylase and a test substance in the presence of a substrate of the hydroxylase under conditions in which asparagine in the substrate is hydroxylated in the absence of the test substance; and determining hydroxylation of the substrate.</p>
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Antisense modulation of C-reactive protein expression (Fri, 06 Nov 2009)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of C-reactive protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding C-reactive protein. Methods of using these compounds for modulation of C-reactive protein expression and for treatment of diseases associated with expression of C-reactive protein are provided.</p>
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Vaccine against neisseria infection (Thu, 22 Oct 2009)
The invention relates to a vaccine for the treatment of disease caused by Neisseria, the vaccine comprising one or more immunogenic components for Neisseria serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating Neisseria infections. The immunogens are based on elements of the inner core lipopolysaccharide.
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Chimeric oligomeric compounds comprising alternating regions of northern and southern conformational geometry (Fri, 16 Oct 2009)
<p id="p-0001" num="0000">The present invention relates to novel chimeric oligomeric compounds having a plurality of alternating regions having either RNA like having northern or 3′-endo conformational geometry (3′-endo regions) or DNA like having southern or C2′-endo/O4′-endo conformational geometry. The oligomeric compounds of the present invention have shown reduction in mRNA levels in multiple in vitro and in vivo assay systems and are useful, for example, for investigative and therapeutic purposes.</p>
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OLIGOMERIC COMPOUNDS COMPRISING NEUTRALLY LINKED TERMINAL BICYCLIC NUCLEOSIDES (Fri, 09 Oct 2009)
The present disclosure describes oligomeric compounds having at least one bicyclic nucleoside attached to the 3' or 5' termini by a neutral internucleoside linkage and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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OLIGOMERIC COMPOUNDS COMPRISING BICYCLIC NUCLEOSIDES AND HAVING REDUCED TOXICITY (Fri, 09 Oct 2009)
In certain embodiments, the present invention provides oligomeric compounds having favorable toxicity profiles and therapeutic indexes. Compounds of the present invention comprise bicyclic nucleosides. Certain such bicyclic nucleosides are pyrimidines that do not include a methyl group at the 5-carbon. Oligomeric compounds comprising such nucleosides are less toxic than compounds comprising bicyclic nucleosides that do include a methyl group at the 5-carbon. In certain embodiments, the present invention provides methods of preparing and using such compounds.
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OLIGOMERIC COMPOUNDS COMPRISING TRICYCLIC NUCLEOSIDES AND METHODS FOR THEIR USE (Fri, 25 Sep 2009)
The present disclosure provides tricyclic nucleosides, oligomeric compounds comprising at least one of the tricyclic nucleosides and methods of using the oligomeric compounds. The methods provided herein include contacting a cell or administering to an animal at least one of the oligomeric compounds. In certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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Vaccine (Wed, 09 Sep 2009)
<p id="p-0001-en" num="0000">The invention relates to a vaccine for the treatment of disease caused by <i>Neisseria</i>, the vaccine including one or more immunogenic components for <i>Neisseria </i>serogroups, as well as antibodies to the immunogenic components and methods of preventing and treating <i>Neisseria </i>infections. The immunogens are based on elements of the inner core lipopolysaccharide.</p>
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Oligomeric compounds and compositions for the use in modulation of microRNAs (Fri, 04 Sep 2009)
<p id="p-0001" num="0000">Compounds, compositions and methods are provided for modulating the levels expression, processing and function of miRNAs. The compositions comprise oligomeric compounds targeted to small non-coding RNAs and miRNAs. The oligomeric compounds possess potent miRNA inhibitory activity, and further exhibit improved therapeutic index. Further provided are methods for selectively modulating miRNA activity in a cell.</p>
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CHEMICAL MODIFICATION OF PROTEINS (Fri, 28 Aug 2009)
The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
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Mina53 assays (Fri, 21 Aug 2009)
<p id="p-0001" num="0000">The present invention comprises a method for assaying oxygenase activity the method comprising monitoring oxygenase activity of Mina53.</p>
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(1R,6S)-2-AZABICYCLO[4.3.0] NONANE-8,8-DIPHOSPHONIC ACID AND ITS USE IN TREATING OR PREVENTING BONE DISORDERS, FOR EXAMPLE, OSTEOPOROSIS OR PAGET'S DISEASE (Thu, 20 Aug 2009)
Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.
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BICYCLIC CYCLOHEXITOL NUCLEIC ACID ANALOGS (Fri, 14 Aug 2009)
The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance.
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2'-Modified Oligonucleotides (Fri, 07 Aug 2009)
<p id="p-0001-en" num="0000">Compositions and methods are provided for the treatment and diagnosis of diseases amenable to modulation of the production of selected proteins. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the 2′-deoxyfuranosyl moieties of the nucleoside unit is modified. Treatment of diseases caused by various viruses and other causative agents is provided.</p>
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MULTIMERIC PARTICLES (Thu, 06 Aug 2009)
The invention provides multimeric particle comprising metal-containing particles covalently bonded to one another by linker groups wherein at least some of said linker groups are cleavable. The invention further provides a contrast agent comprising said multimeric particles, along with a method of improving contrast of an image using said contrast agent.
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Compounds and methods for synthesis of bicyclic nucleic acid analogs (Wed, 05 Aug 2009)
<p id="p-0001-en" num="0000">The present invention provides compounds and methods of using them for preparing bicyclic nucleosides. The bicyclic nucleosides are useful for preparing chemically modified oligomeric compounds. Oligomeric compounds comprising these bicyclic nucleosides have enhanced properties such as increased nuclease resistance.</p>
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Modulation of eIF4E expression (Fri, 31 Jul 2009)
<p id="p-0001-en" num="0000">Oligomeric compounds, compositions and methods are provided for modulating the expression of eIF4E. The antisense compounds may be single- or double-stranded and are targeted to nucleic acid encoding eIF4E. Methods of using these compounds for modulation of eIF4E expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E are provided.</p>
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5′-modified bicyclic nucleic acid analogs (Fri, 31 Jul 2009)
<p id="p-0001-en" num="0000">The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.</p>
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Modified carbohydrate processing enzyme (Fri, 17 Jul 2009)
<p id="p-0001-en" num="0000">A modified polypeptide having carbohydrate processing enzymatic activity is provided, said polypeptide comprising an amino acid sequence selected from: (a) the amino acid sequence of SEQ ID NO:2 comprising a mutation in at least one of W433, E432 and M439; (b) the amino acid sequence of an enzyme of glycosyl hydrolase family 1, comprising at least one mutation at an amino acid residue equivalent to W433, E432 or M439 of SEQ ID NO:2; and (c) a variant of (a) or (b) having carbohydrate processing enzymatic activity and comprising at least one amino acid mutation at a position equivalent to W433, E432 or M439 of SEQ ID NO:2.</p>
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Bis-modified bicyclic nucleic acid analogs (Fri, 19 Jun 2009)
<p id="p-0001-en" num="0000">The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5′-methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.</p>
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ANTISENSE OLIGONUCLEOTIDE TARGETED TO INSULIN-LIKE GROWTH FACTOR BINDING PROTEIN 5 (Tue, 16 Jun 2009)

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CARBOCYCLIC ALPHA-L-BICYCLIC NUCLEIC ACID ANALOGS (Fri, 29 May 2009)
The present invention provides novel carbocyclic α-L-bicyclic nucleosides and oligomeric compounds comprising at least one of these carbocyclic α-L-bicyclic nucleosides. The carbocyclic α-L-bicyclic nucleosides are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into including nuclease resistance.
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COMPOUNDS AND METHODS FOR MODULATING PROTEIN EXPRESSION (Sat, 23 May 2009)
The present invention provides compounds and methods for modulating expression of a protein, including, but not limited to, modulating splicing of a pre-mRNA to modulate the amount of one or more variants of a protein.
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Supports for oligomer synthesis (Fri, 22 May 2009)
<p id="p-0001-en" num="0000">Universal linkers, their facile processes of manufacture and methods of using the same are provided.</p>
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Antisense modulation of PTP1B expression (Fri, 15 May 2009)
<p id="p-0001" num="0000">Compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.</p>
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BRANCHED MATERIALS FOR PHOTOVOLTAIC DEVICES (Fri, 24 Apr 2009)
The invention provides a dye-sensitized photovoltaic device which comprises: a first electrode; a second electrode; and, disposed between the first and second electrodes: an electron acceptor material which comprises a semiconductive metal oxide, a redox mediator material, and a photosensitizing dye which comprises a dendrimer of formula (I): [X]m-CORE-[[Y]p-[DENDRON]]n wherein n, m, p, CORE, DENDRON, X and Y are as defined herein. The invention further provides a photosensitizing dye which is a dendrimer of formula (I), and the use, as a photosensitizing dye in a dye-sensitized photovoltaic device, of a compound which is a dendrimer of formula (T). Novel dendrimers of formula (T) are also provided. Novel catechol-based compounds are also provided. The catechol-based compounds can be used together with the dendrimers of formula (T) as the photosensitizing dyes in a photovoltaic device. Accordingly, the invention further provides photosensitizing dyes and dye-sensitized photovoltaic devices comprising such catechol compounds, and the use of such catechol compounds as photosensitizing dyes in a dye-sensitized photovoltaic device.
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MUTANT ENZYMES (Fri, 17 Apr 2009)
This invention relates to mutant enzymes with enhanced properties and processes for oxidation of organic compound substrates using such enzymes.
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Tetrahydropyran nucleic acid analogs (Fri, 10 Apr 2009)
<p id="p-0001" num="0000">The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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MOLECULAR ADAPTORS (Fri, 10 Apr 2009)
The invention relates to transmembrane protein pore for use in detecting a analyte in a sample. The pore comprises a molecular adaptor that facilitates an interaction between the pore and the analyte. The adaptor is covalently attached to the pore in an orientation that allows the analyte to be detected using the pore.
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MOLECULAR ADAPTORS (Fri, 10 Apr 2009)
The invention relates to transmembrane protein pore for use in detecting a analyte in a sample. The pore comprises a molecular adaptor that facilitates an interaction between the pore and the analyte. The adaptor is covalently attached to the pore in an orientation that allows the analyte to be detected using the pore. </p>
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METHOD OF SELECTING AN ACTIVE OLIGONUCLEOTIDE PREDICTIVE MODEL (Fri, 27 Mar 2009)
<p id="p-0001-en" num="0000">The present invention provides a method of identifying a predictor of antisense oligonucleotide activity by identifying properties of oligonucleotides, evaluating oligonucleotide activity of the oligonucleotides, and correlating oligonucleotide activity with the properties. A high correlation between oligonucleotide activity and a property indicates that the property is a predictor of oligonucleotide activity.</p>
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Composition for treating bone disorders (Fri, 13 Mar 2009)
<p id="p-0001-en" num="0000">Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.</p>
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TETRAHYDROPYRAN NUCLEIC ACID ANALOGS (Fri, 20 Feb 2009)
The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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TETRAHYDROPYRAN NUCLEIC ACID ANALOGS (Fri, 20 Feb 2009)
The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. </p>
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USE OF ANTISENSE OLIGONUCLEOTIDE LIBRARIES FOR IDENTIFYING GENE FUNCTION (Fri, 23 Jan 2009)
<p id="p-0001-en" num="0000">A method for identifying one or more genes involved in a phenotype of cells, tissues or organisms, comprising the steps of contacting cells, tissues or organisms which exhibit the phenotype with a library of antisense oligonucleotides and performing a primary phenotypic assay to determine which antisense oligonucleotides in the library attenuate the phenotype. These antisense oligonucleotides correspond to genes involved in the phenotype. The method may be used to identify genes involved in various disease states.</p>
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6-modified bicyclic nucleic acid analogs (Fri, 09 Jan 2009)
<p id="p-0001-en" num="0000">The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 6-position. These bicyclicnucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.</p>
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6-DISUBSTITUTED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 09 Jan 2009)
The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2'-O-C(Ri)(R2)-4' or 2'-O- C=(R3)(R.4)-4' bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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6-DISUBSTITUTED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 09 Jan 2009)
The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6- disubstituted bicyclic nucleosides each comprise a 2'-O- C(Ri)(R2)-4' or 2'-O- C=(R3)(R.4)-4' bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. </p>
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A METHOD FOR ASSAYING FTO (2-OXOGLUTARATE DEPENDENT OXYGENASE) ACTIVITY (Thu, 25 Dec 2008)
The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO.
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A METHOD FOR ASSAYING FTO (2-OXOGLUTARATE DEPENDENT OXYGENASE) ACTIVITY (Thu, 25 Dec 2008)
The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO. </p>
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Imaging Agent (Fri, 19 Dec 2008)
<p id="p-0001-en" num="0000">The invention provides a conjugate comprising an iron containing colloidal particle, the particle being conjugated to one or more sugar targeting moieties. The conjugate is useful as a contrast agent in medical imaging, particularly in magnetic resonance imaging (MRI). The agents of the present invention may cross the blood brain barrier and so may be particularly useful in the monitoring or diagnosis of conditions affecting the brain.</p>
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CARBOCYCLIC BICYCLIC NUCLEIC ACID ANALOGS (Fri, 19 Dec 2008)
Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance.
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Antisense inhibition of PTP1B expression (Thu, 18 Dec 2008)
Antisense compounds, compositions and methods are provided for modulating the expression of PTP1B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTP1B. Methods of using these compounds for modulation of PTP1B expression and for treatment of diseases associated with expression of PTP1B are provided.
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N-SUBSTITUTED-AMINOMETHYLENE BRIDGED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 12 Dec 2008)
Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bi cyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
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N-SUBSTITUTED-AMINOMETHYLENE BRIDGED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 12 Dec 2008)
Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bi cyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.</p>
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Antibacterial 4,5-substituted aminoglycoside analogs having multiple substituents (Fri, 28 Nov 2008)
<p id="p-0001" num="0000">The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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Synthesis of sulfurized oligonucleotides (Fri, 28 Nov 2008)
<p id="p-0001-en" num="0000">Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.</p>
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6-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS (Thu, 30 Oct 2008)
The present invention provides 6-modified bicyclic nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In preferred embodiments the nucleoside analogs have either <i>(R)</i> or <i>(S)</i>-chirality at the 6-position. These bicyclicnucleoside analogs are useful for enhancing properties of oligomeric compounds including nuclease resistance.
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Compositions and methods for the modulation of JNK proteins (Fri, 17 Oct 2008)
<p id="p-0001" num="0000">The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK1 protein.</p>
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PORPHYRIN COMPOUNDS (Fri, 10 Oct 2008)
The present invention relates to porphyrin compounds of formula (I), to processes for preparing said compounds, to pharmaceutical compositions comprising said compounds and their use in photodynamic therapy. The porphyrin compounds exhibit high two photon absorption cross section values, are soluble and are readily absorbed by cells making them suitable for use in two photon photodynamic therapy.
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Assays for identifying modulators of the hydroxylation of ankyrin repeat proteins by 2-oxoglutarate dependent oxygenase and methods of using the same (Fri, 19 Sep 2008)
<p id="p-0001-en" num="0000">A method of identifying an agent which modulates 2-oxoglutarate dependent oxygenase activity, the method comprising contacting a 2-oxoglutarate dependent oxygenase and a test agent in the presence of a substrate comprising one or more ankyrin repeat, or fragment thereof, in conditions under which the substrate is hydroxylated in the absence of the test agent; and determining hydroxylation of the substrate.</p>
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PENTALENES (Fri, 19 Sep 2008)
The present invention relates to per-substituted pentalene compounds, including permethylpentalene and precursors thereof. In particular, the invention provides substituted pentalene compounds and methods of preparing substituted pentalene compounds; complexes of metals with substituted pentalene compounds and methods for their production; and the use of complexes of metals with substituted pentalene compounds in catalysis.
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Biomolecular Structure Determination Involving Swarm Intelligence (Fri, 12 Sep 2008)
<p id="p-0001-en" num="0000">A method and computer program for determining biomolecular structures from experimental data that includes ambiguous experimental observables comprising the steps of: creating a swarm of molecular structure generators; having the ability to allow the communication between said generators via a global set of molecular restraints; determining said molecular structure in a cooperative manner by using self-optimization of a multi-agent system. In one embodiment, NOESY spectra are used to calculate inter-proton distances of the biomolecular structure and said distances are used as molecular restraints. Moreover, the method involves restrained molecular dynamics simulations, e.g. by simulated annealing.</p>
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ANTIBACTERIAL 6'-MODIFIED 4,5-SUBSTITUTED AMINOGLYCOSIDE ANALOGS (Fri, 05 Sep 2008)
<p id="p-0001-en" num="0000">The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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Compositions and methods for optimizing cleavage of RNA by RNase H (Fri, 29 Aug 2008)
<p id="p-0001" num="0000">The present invention provides compositions and methods for the optimization of cleavage of RNA species by RNase H. In some embodiments, the invention provides oligonucleotides that possess two or more regions of differing conformation, and at least one transitional nucleobase positioned between the regions that is capable of modulating transfer of the helical conformation characteristic of the region bound to the 3′hydroxy thereof, to the region bound to the 5′ hydroxyl thereof.</p>
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5'-SUBSTITUTED-2'-F MODIFIED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM (Fri, 22 Aug 2008)
The present invention provides 5'-substituted-2'-F nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In one preferred embodiment the nucleoside analogs have either (R) or (5)-chirality at the 5'-position. These nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance.
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Antisense modulation of p38 mitogen activated protein kinase expression (Fri, 15 Aug 2008)
<p id="p-0001" num="0000">Compositions and methods for the treatment and diagnosis of diseases or conditions amenable to treatment through modulation of expression of a gene encoding a p38 mitogen-activated protein kinase (p38 MAPK) are provided. Methods for decreasing airway hyperresponsiveness or airway inflammation in an animal are also provided.</p>
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Drug delivery system (Fri, 08 Aug 2008)
<p id="p-0001" num="0000">A drug delivery system for the controlled release of a pharmaceutically-active compound by oral route comprises an intercalate of a layered double hydroxide having, before intercalation, layers of metal hydroxides, and having intercalated therein a pharmaceutically-active compound having at least one anionic group. A preferred layered double hydroxide is one that has layers which comprise [LiAl<sub>2</sub>(OH)<sub>6</sub>]<sup>+</sup>. The drug delivery system has use in the delivery of drugs such as 4-biphenylacetic acid, Diclofenac, Gemfibrozil, Ibuprofen, Naproxen, 2-Propylpentanoic acid and Tolfenamic acid.</p>
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ANTISENSE MODULATION OF ACYL COA CHOLESTEROL ACYLTRANSFERASE-2 EXPRESSION (Fri, 01 Aug 2008)
<p id="p-0001-en" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of acyl CoA cholesterol acyltransferase-2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding acyl CoA cholesterol acyltransferase-2. Methods of using these compounds for modulation of acyl CoA cholesterol acyltransferase-2 expression and for treatment of diseases associated with expression of acyl CoA cholesterol acyltransferase-2 are provided.</p>
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Modulation of FR-alpha expression (Fri, 11 Jul 2008)
<p id="p-0001-en" num="0000">Disclosed herein are compounds, compositions and methods for modulating the expression of FR-alpha in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.</p>
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IMAGING AGENT COMPRISING IRON CONTAINING COLLOIDAL PARTICLE CONJUGATED TO OLIGOSACCHARIDES (Thu, 03 Jul 2008)
The invention provides a conjugate comprising an iron containing colloidal particle, the particle being conjugated to one or more sugar targeting moieties. The conjugate is useful as a contrast agent in medical imaging, particularly in magnetic resonance imaging (MRI). The agents of the present invention may cross the blood brain barrier and so may be particularly useful in the monitoring or diagnosis of conditions affecting the brain.
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Modulation of forkhead box O1A expression (Fri, 27 Jun 2008)
<p id="p-0001-en" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding forkhead box O1A. Methods of using these compounds for modulation of forkhead box O1A expression and for treatment of diseases associated with expression of forkhead box O1A are provided, in particular, for methods of treating diabetes.</p>
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Antisense modulation of stearoyl-CoA desaturase expression (Fri, 27 Jun 2008)
<p id="p-0001" num="0000">Antisense compounds, compositions and methods are provided for modulating the expression of stearoyl-CoA desaturase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding stearoyl-CoA desaturase. Methods of using these compounds for modulation of stearoyl-CoA desaturase expression and for treatment of diseases associated with expression of stearoyl-CoA desaturase are provided.</p>
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Positionally modified siRNA constructs (Fri, 20 Jun 2008)
<p id="p-0001" num="0000">The present invention provides oligomeric compounds having sufficient complementarity to hybridize to a nucleic acid target and methods for their use in modulating gene expression. In one embodiment the oligomeric compounds comprise double stranded constructs wherein one of the strands capable of hybridizing to a nucleic acid target, and has a plurality of modified ribofuranosyl nucleosides at defined locations. The presence of modifications at such defined positions greatly enhances the properties of the corresponding compositions.</p>
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BIOMOLECULAR STRUCTURE DETERMINATION INVOLVING SWARM INTELLIGENCE (Thu, 12 Jun 2008)
A method and computer program for determining biomolecular structures from experimental data that includes ambiguous experimental observables comprising the steps of : creating a swarm of molecular structure generators; having the ability to allow the communication between said generators via a global set of molecular restraints; determining said molecular structure in a cooperative manner by using self-optimization of a multi-agent system. In one embodiment, NOESY spectra are used to calculate inter-proton distances of the biomolecular structure and said distances are used as molecular restraints. Moreover, the method involves restrained molecular dynamics simulations, e.g. by simulated annealing.
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Amidites and Methods of Rna Synthesis (Fri, 23 May 2008)
<p id="p-0001-en" num="0000">The present invention is directed to amidites useful in the synthesis of oligonucleotides comprising at least one RN moiety, and to methods of using such amidites in the synthesis of such oligonucleotides. The inventive amidites possess surprising coupling efficiency as compared to prior art amidites, while providing convenient intermediates in the synthesis of oligonucleotides possessing at least one free 2′-OH moiety.</p>
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Polymeric beads for oligomer synthesis (Fri, 25 Apr 2008)
<p id="p-0001-en" num="0000">The present invention provides solid support media for use in oligomer synthesis, methods of producing the media, and methods of using the media. In some embodiments, the processes of the invention comprise (a) providing an organic phase comprising an olefin monomer, a cross-linker, a functionalizing reagent and an initiator; and (b) contacting the organic phase with an aqueous phase under conditions of time and temperature effective to form the polymeric bead.</p>
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MULTIMERIC PARTICLES (Fri, 28 Mar 2008)
The invention provides multimeric particle comprising metal-containing particles covalently bonded to one another by linker groups wherein at least some of said linker groups are cleavable. The invention further provides a contrast agent comprising said multimeric particles, along with a method of improving contrast of an image using said contrast agent.
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COMPOUNDS FOR IMAGING AND THERAPY (Fri, 07 Mar 2008)
The invention provides metal complexes of formula (I), wherein M is a transition metal or a p-block metal, and a, b, c, n, L, X, X', Y, Y', L1, L1', R1, R1', R2 and R2' are defined herein. Such complexes are useful in medical imaging and therapy, in particular, in the treatment of conditions characterised by undesirable cellular proliferation. The invention further provides processes for producing the complexes of the invention.
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Receptor modulators (Fri, 22 Feb 2008)
<p id="p-0001-en" num="0000">Method of identifying a modulator of CD28 comprising comparing a structural model of a candidate modulator with a structural model of CD28 to thereby determine whether the modulator will bind to CD28, wherein the structural model is derived from, or comprises, structural coordinates of a crystal of: (i) CD28, (ii) a fragment of CD28, or (iii) a homologue of (i) or (ii). The crystal of CD28 in a soluble form complexed with the Fab fragment of a mitogenic (superagonistic) antibody has been obtained and used for the determination of the 3D-structure of the receptor. The application also relates to modulators of superagonistic signalling for any receptor of the CD28 family, i.e. to superagonistic antibodies and chimeric proteins thereof, and to the screening of the superagonistic modulators. In the methods of screening, the binding of the candidate modulators to a portion of the receptor proximal to the cell membrane is investigated.</p>
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Antimicrobial 2-deoxystreptamine compounds (Fri, 22 Feb 2008)
<p id="p-0001" num="0000">The present invention is directed to analogs of paromomycin having a variety of chemical functional groups attached at the 2″-O-position as well as their preparation and use as prophylactic or therapeutics against microbial infection.</p>
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2'-MODIFIED OLIGONUCLEOTIDES (Fri, 08 Feb 2008)
<p id="p-0001-en" num="0000">Compositions and methods are provided for the treatment and diagnosis of diseases amenable to modulation of the production of selected proteins. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the 2′-deoxyfuranosyl moieties of the nucleoside unit is modified. Treatment of diseases caused by various viruses and other causative agents is provided. </p>
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COMPOSITIONS AND METHODS FOR THE MODULATION OF JNK PROTEINS (Fri, 08 Feb 2008)
The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK l protein.
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COMPOSITIONS AND METHODS FOR THE MODULATION OF JNK PROTEINS (Fri, 08 Feb 2008)
The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK l protein.</p>
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Oligonucleotide compositions and methods for the modulation of the expression of B7 protein (Fri, 01 Feb 2008)
<p id="p-0001" num="0000">Compositions and methods for the treatment of asthma with oligonucleotides which specifically hybridize with nucleic acids encoding B7 proteins.</p>
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ANTISENSE MODULATION OF APOLIPOPROTEIN B EXPRESSION (Thu, 31 Jan 2008)
</p> <p>^ B. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding
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Supports for oligomer synthesis (Fri, 25 Jan 2008)
<p id="p-0001-en" num="0000">Universal linkers, their facile processes of manufacture and methods of using the same are provided.</p>
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COMPOSITIONS AND THEIR USES DIRECTED TO HBXIP (Fri, 25 Jan 2008)
Disclosed herein are compounds, compositions and methods for modulating the expression of HBXIP in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.
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Human RNase H1 oligonucleotide compositions thereof (Fri, 21 Dec 2007)
<p id="p-0001-en" num="0000">The present invention provides oligonucleotides that can serve as substrates for human Type 2 RNase H. The present invention is also directed to methods of using these oligonucleotides in enhancing antisense oligonucleotide therapies. </p>
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5′-modified bicyclic nucleic acid analogs (Fri, 14 Dec 2007)
<p id="p-0001-en" num="0000">The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.</p>
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MODULATION OF CHREBP EXPRESSION (Fri, 30 Nov 2007)
Disclosed herein are compounds, compositions, and methods for modulating the expression of ChREBP in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and conditions.
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Compositions and methods for modulation of Mcl-1 expression (Fri, 23 Nov 2007)
<p id="p-0001-en" num="0000">Disclosed herein are compounds, compositions and methods for modulating the expression of Mcl-1 in a cell, tissue or animal. Also provided are methods of target validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders.</p>
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5'-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 23 Nov 2007)
The present invention provides 5'-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5'-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.
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5'-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS (Fri, 23 Nov 2007)
The present invention provides 5'-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5'-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.</p>
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Lectin-directed prodrug delivery system (Fri, 02 Nov 2007)
<p id="p-0001-en" num="0000">The invention provides a kit for lectin-directed prodrug delivery comprising a prodrug and a lectin-directed glycoconjugate, wherein the glycoconjugate is adapted to cleave the prodrug and thereby release the drug. The glycoconjugate generally comprises an enzyme conjugated to a carbohydrate moiety which binds to a lectin. The invention also provides novel glycoconjugates and novel methods of synthesizing prodrugs. </p>
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