PATENTSCOPE: EN_ALL:nmr AND PA:roche

CYCLIC PEPTIDE ANTIBIOTICS (Fri, 22 Mar 2019)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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DIHYDROQUINOLINONES (Fri, 08 Mar 2019)
The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.
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NOVEL PHARMACEUTICAL COMPOSITIONS FOR BASIC OR NEUTRAL, LOW MOLECULAR WEIGHT COMPOUNDS (Fri, 22 Feb 2019)
The present invention provides novel, solid or liquid pharmaceutical preparations comprising a basic or neutral, low molecular weight active pharmaceutical ingredient and the polymer Eudragit® EPO, optionally together with additional pharmaceutically acceptable excipients.The present preparations are for oral or topical administration.
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ANTI-CD8 ANTIBODIES AND USES THEREOF (Fri, 15 Feb 2019)
Provided are anti-CD8 antibodies that bind human CD8 and do not stimulate or inhibit the activation of CD8+ T cells. Also provided are nucleic acids encoding such anti-CD8 antibodies, vectors comprising such nucleic acids, host cells comprising same, and methods of making such anti-CD8 antibodies. Also provided are anti-CD8 antibodies conjugated to a detectable label. Provided are methods of using such anti-CD8 antibodies to detect CD8+ T cells in a subject, monitor disease progress in a subject having cancer, and monitor treatment progress in a subject having cancer.
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THREE-DIMENSIONAL STRUCTURE-BASED HUMANIZATION METHOD (Fri, 08 Feb 2019)
Herein is reported a method for the humanization of non-human antibodies using a structure-based scoring matrix. With the scoring matrix it is possible to determine (the requirement for and) the suitability of specific (back)mutations of amino acid residues at defined positions of a selected human germline sequence. The scoring matrix takes into account the topology, the three-dimensional structure and the interactions of the respective residue and change. Thereby the influence on antigen binding of a specific amino acid residue change can be determined.
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BICYCLIC KETONE COMPOUNDS AND METHODS OF USE THEREOF (Fri, 18 Jan 2019)
The invention provides novel compounds having the general formula (I): (I) wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
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MULTIPLE COUPLING & OXIDATION METHOD (Fri, 04 Jan 2019)
The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers and methods of synthesis of stereodefined oligonucleotides using said monomer. Herein are disclosed oligonucleotide enhanced synthesis methods where within a single elongation cycle there are repeated coupling and oxidation steps. The method results in an enhanced yield and higher purity of stereodefined phosphorothioate oligonucleotides
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ISOINDOLINONE DERIVATIVES AS IRAK4 MODULATORS (Fri, 28 Dec 2018)
Compounds of Formula (0), and stereoisomers and pharmaceutically acceptable salts thereof, as well as methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS (Fri, 28 Dec 2018)
Compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), and methods of use as lnterleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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BENZOFURANS AS IRAK4 MODULATORS (Fri, 28 Dec 2018)
Compounds of Formula (0), and stereoisomers and pharmaceutically acceptable salts thereof, as well as methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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FATTY ACID BINDING PROTEIN 3 FOR THE ASSESSMENT OF ATRIAL FIBRILLATION (AF) (Fri, 21 Dec 2018)
The present invention relates to a method for diagnosing paroxysmal atrial fibrillation in a subject, comprising: determining the amount of FABP-3 (Fatty acid binding protein 3) in a sample from a subject suspected to suffer from paroxysmal atrial fibrillation, and comparing the determined amount to a reference amount. The method of the present invention may further comprise the determination of a BNP-type peptide. Further encompassed by the present invention is a device adapted to carry out the method of the present invention.
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TYPE II ANTI-CD20 ANTIBODY AND ANTI-CD20/CD3 BISPECIFIC ANTIBODY FOR TREATMENT OF CANCER (Fri, 07 Dec 2018)
The present invention relates to methods of treating a disease, and methods for reduction of cytokine release associated with the administration of a T-cell activating therapeutic agent. The present invention in particular relates to a Type II anti-CD20 antibody for the use in a method for treating or delaying progression of cancer of an individual, wherein the Type II anti-CD20 antibody is used in combination with an anti-CD20/anti-CD3 bispecific antibody.
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CATALYSTS FOR REVERSING FORMALDEHYDE ADDUCTS AND CROSSLINKS (Fri, 07 Dec 2018)
Catalysts act to release formaldehyde cross-linking that occurs in biological samples. Thus, contacting catalysts to formaldehyde fixed samples is a useful way to render biological components of the samples, including nucleic acids or proteins, more accessible to detection and characterization.
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THERAPEUTIC COMPOUNDS AND COMPOSITIONS, AND METHODS OF USE THEREOF (Fri, 30 Nov 2018)
Compounds and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
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THERAPEUTIC COMPOUNDS AND COMPOSITIONS, AND METHODS OF USE THEREOF (Fri, 30 Nov 2018)
Compounds and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
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PROCESS FOR GALNAC OLIGONUCLEOTIDE CONJUGATES (Fri, 30 Nov 2018)
The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.
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PROCESS FOR GALNAC OLIGONUCLEOTIDE CONJUGATES (Fri, 30 Nov 2018)
The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.
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REDUCTION OF APPLICATION-RELATED SIDE REACTION OF A THERAPEUTIC ANTIBODY (Fri, 23 Nov 2018)
Herein is reported an anti-brain target therapeutic agent, which is an anti-brain target/human transferrin receptor (1) antibody, wherein the anti-brain target/human transferrin receptor (1) antibody has two binding sites (VH/VL pairs) that specifically bind to the brain target, one binding site (VH/VL pair) that specifically binds to the human transferrin receptor (1) and an effector function competent (native) Fc-region, for use in anti-brain target treatment in an individual with reduced undesired body-temperature drop after intravenous application.
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POLYMORPHS AND SOLID FORMS OF (S)-2-((2-((S)-4-(DIFLUOROMETHYL)-2-OXOOXAZOLIDIN-3-YL)-5,6-DIHYDROBENZO[F]IMIDAZO[1,2-D][1,4]OXAZEPIN-9-YL)AMINO)PROPANAMIDE, AND METHODS OF PRODUCTION (Fri, 02 Nov 2018)
The present invention relates to crystalline polymorph forms of (5)-2-((2-((5)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[ƒ]imidazo[ 1,2-J] [ 1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
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A METHOD FOR LABELING OF ALDEHYDE CONTAINING TARGET MOLECULES (Fri, 19 Oct 2018)
The present invention relates to a method for binding to a target molecule comprising an aldehyde a compound derived from N- (2-aminoethyl)pyrrole, which compound also comprises a moiety of interest, to compounds (conjugates) obtained by this method, comprising both the target molecule and the moiety of interest and to novel substances derived from N-(2-aminoethyl)pyrrole.
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