Novo Nordisk - organic-reaction.com

A MAGNETIC TIME DELAY INDICATOR AND AN INJECTION DEVICE INCORPORATING SUCH (Fri, 24 May 2013)
The present invention relates to a time delay indicator (1) for an injection device for administering a drug into the body of a subject user wherein the time delay indicator is configured for indicating after administration that a dose of the drug actually has been administered and for maintaining this indication until lapse of a pre-determined time interval. The time delay indicator is based on a magnetic liquid (6) being physically moved by a magnet (10).
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MEDICAL INJECTION SYSTEM COMPRISING A MEDICAL INJECTION DEVICE AND A DOSE LIMITER MODULE (Fri, 17 May 2013)
The present invention relates to a medical injection system comprising a medical injection device (100) of the type comprising a rotatable dose setting member (160). The system further comprises a dose limiter module (200) adapted for being releasably coupled to the injection device (100). The dose limiter module (200) comprises a dose limiter base (201) and a limiter (240) arranged relative to the dose limiter base (201) so that their relative position is adjustable to set an adjusted dose limiting position. When the dose limiter module (200) is coupled to the injection device (100), the limiter (240) cooperates with the dose setting member (160) to define a blocking means for preventing rotation of the dose setting member (160) beyond the adjusted dose limiting position. The dose limiter module (200) further comprises a user operable lock (210,212,232,223,243) configured for operation between a locked state and an unlocked state to respectively prevent and enable modification of the adjusted dose limiting position, the lock (210,212,232,223,243) being configured for maintaining the lock in the locked state at least when the dose limiter module (200) is not coupled with the injection device (100).
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PROCESS FOR SHAPING A NEEDLE CANNULA (Sat, 11 May 2013)
A regular metallic, cylindrical tubular needle cannula (1) is subjected to a metal etching liquid (5) in the inside lumen (11) thereby increasing the inside diameter and enhancing the flow properties while maintaining the outside appearance. The inside diameter is only increased over a controlled length (14) of the full length of the needle cannula (10) leaving sufficient length and wall thickness to also taper the outside diameter if so wanted.
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(Fri, 03 May 2013)

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Hyperglycosylated Human Coagulation Factor IX (Fri, 19 Apr 2013)
The invention relates to hyperglycosylated human coagulation factor IX polypeptides, to processes for preparing said polypeptides, to pharmaceutical compositions comprising said polypeptides and to the use of the compounds for the treatment of diseases alleviated by human coagulation factor IX, in particular, but not exclusively hemophilia.
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LONG-ACTING Y2 RECEPTOR AGONISTS (Fri, 19 Apr 2013)
The present invention relates to PYY derivatives comprising a serum albumin binding side chain, wherein said derivative has a half-life of at least 7 hours as determined by Assay (IV) described herein as well as compositions comprising said derivative and its use in therapy.
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Novel Glucagon Analogues (Fri, 29 Mar 2013)
The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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NOVEL GLUCAGON ANALOGUES (Fri, 29 Mar 2013)
The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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SELECTIVE MODIFICATION OF PROTEINS (Fri, 22 Mar 2013)
A method of selectively introducing a substituent into a protein proximal to a binding site on the protein for a homing peptide, comprising: (a) contacting the protein with a compound comprising a homing peptide having the ability to bind to the binding site of the protein; and (b) allowing a moiety on the protein proximal to the binding site to react with the compound comprising the homing peptide, thereby to transfer the substituent G onto the protein.
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GLP-1 DERIVATIVES (Fri, 22 Mar 2013)
The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC-(CH 2 ) x -CO-*, and Chem. 16: HOOC-C 6 H 4 -O-(CH 2 ) y -CO-*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *-NH-CH(CH 2 OH)-CO-*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.
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A PISTON ROD FOOT (Fri, 15 Mar 2013)
The invention relates to a medical drug delivery apparatus which comprises a cartridge (1) being closed at one end by a membrane (12) and at the opposite end by a movable piston (15). A piston rod foot (1) is provided for transferring the pressure from the piston rod (20) of the drug delivery apparatus and onto the piston (15). The piston rod foot (1) comprises a centre part (2) abutting the piston rod (20) and an outer part (3) which centre part (2) and outer part (3) are releasable coupled together such that the two (2, 3) can be released when a force above a certain threshold limit is applied to the outer part (3).
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PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION OF INSULIN PEPTIDES (Fri, 08 Mar 2013)
The invention is related to pharmaceutical compositions suitable for oral administration of insulin peptides, methods of making such and treatment with such.
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Long-Acting Gastrin Derivatives (Fri, 08 Mar 2013)
The present invention relates to gastrin derivatives comprising gastrin or an analogue or fragment thereof and a derivatisation group and therapeutic use thereof.
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POLYPEPTIDES (Fri, 08 Mar 2013)
The invention relates to polypeptides comprising an amino acid sequence which is an analogue of pramlintide, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
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SELECTIVE MODIFICATION OF PROTEINS (Thu, 28 Feb 2013)
A method of selectively introducing a substituent into a protein proximal to a binding site on the protein for a homing peptide, comprising: (a) contacting the protein with a compound comprising a homing peptide having the ability to bind to the binding site of the protein; and (b) allowing a moiety on the protein proximal to the binding site to react with the compound comprising the homing peptide, thereby to transfer the substituent G onto the protein.
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NOVEL GLUCAGON ANALOGUES (Thu, 07 Feb 2013)
The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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NOVEL GLUCAGON ANALOGUES (Thu, 07 Feb 2013)
The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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NOVEL GLUCAGON ANALOGUES (Thu, 07 Feb 2013)
The present invention relates to glucagon peptide agonists which have improved solubility and stability, to the use of the peptides in therapy, to methods of treatment comprising administration of the peptides to patients in need thereof, and to the use of the peptides in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hypoglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hypoglycemia, diabetes and obesity.
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NOVEL NIDDM REGIMEN (Fri, 01 Feb 2013)
The present invention relates to the use of a short-acting oral hypoglycemic agent and to a novel regimen in the treatment of type 2 diabetes in which the endogenous secretion of insulin is stimulated in connection with meals by administering in connection with the meals a short-acting oral hypoglycaemic agent. Also, the present invention relates to a method of achieving significantly improvement in the glycaemic control by a combined use of repaglinide and metformin in NIDDM patients poorly controlled on metformin alone.
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ANTAGONISTIC ANTIBODIES AGAINST OSCAR (Fri, 25 Jan 2013)
The present disclosure relates to antagonistic antibodies against OS-CAR. The present disclosure furthermore relates to use of such antibodies.
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ANTAGONIST ANTIBODIES AGAINST OSCAR (Fri, 25 Jan 2013)
The present disclosure relates to antagonistic antibodies against OSCAR. The present disclosure furthermore relates to use of such antibodies.
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ANTAGONISTIC ANTIBODIES AGAINST OSCAR (Fri, 25 Jan 2013)
The present disclosure relates to therapeutic antagonistic OSCAR antibodies. The present disclosure furthermore relates to use of such antibodies.
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ANTAGONISTIC ANTIBODIES AGAINST OSCAR (Fri, 25 Jan 2013)
The present disclosure relates to antagonistic antibodies against OSCAR. The present disclosure furthermore relates to use of such antibodies.
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PREPARATIVE RP-HPLC METHOD FOR PURIFYING PEPTIDES (Thu, 10 Jan 2013)
A method for separating on a RP-HPLC system a polypeptide of interest from at least one unwanted component is described, wherein at least one of the elution steps is performed at or in close proximity to the pl value of the peptide of interest.
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PEPTIDES FOR TREATMENT OF OBESITY (Thu, 03 Jan 2013)
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
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EFFICIENT INDUCTION OF DEFINITIVE ENDODERM FROM PLURIPOTENT STEM CELLS (Fri, 28 Dec 2012)
The present invention relates to a method to differentiate pluripotent stem cells to a primitive streak cell population, in a stepwise manner for further maturation to definitive endoderm.
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MULTI SUBSTITUTED INSULINS (Fri, 21 Dec 2012)
The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical cpmrising such an insulin derivative.
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SELECTIVE ELIMINATION OF EROSIVE CELLS (Fri, 21 Dec 2012)
The current invention relates to the treatment of diseases characterized by cartilage destruction and/or bone erosion. In particular the present invention relates to the treatment of osteoarthritis, osteoporosis, psoriatic arthritis or rheumatic arthritis with an anti-NKG2A antibody.
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POLYPEPTIDES (Fri, 14 Dec 2012)
The invention relates to polypeptides comprising an amino acid sequence which is an analogue of pramlintide, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
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POLYPEPTIDES (Fri, 14 Dec 2012)
The invention relates to polypeptides comprising an amino acid sequence which is an analogue of pramlintide, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
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POLYPEPTIDES (Fri, 14 Dec 2012)
The invention relates to polypeptides comprising an amino acid sequence which is an analogue of pramlintide, pharmaceutical compositions comprising these polypeptides, and these polypeptides for use as medicaments.
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THERAPEUTIC ANTIBODIES (Fri, 14 Dec 2012)
The present invention concerns human antibodies recognising the human C5a receptor. By binding to C5aR the antibodies inhibit C5a signalling, whereby the pro- inflammatory signal is inhibited. Based on the role of C5a and its receptor in stimulation of inflammation the invention further relates to therapeutic use of said human anti-C5aR antibodies and in particular in relation to treatment of immunological disorders.
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CRYSTAL OF CYTOKINE RECEPTOR (Fri, 07 Dec 2012)
Provided is a co-crystal of IL-21R and IL-21 based on its structural model. Also provided is a method of preparing a crystal of a class I cytokine receptor.
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MEDICAL DEVICE HAVING USER FRIENDLY CONTROL INPUT (Fri, 07 Dec 2012)
The present invention relates to a medical delivery comprising a) a housing (101) adapted to accommodate a drug in a drug reservoir (110), the housing (101) having an exterior surface defining at least one non-circular section, b) a drive mechanism for expelling doses of drug from the drug reservoir (110) and c) an operable control member (150) arranged at the non-circular section of the housing, the operable control member (150) being movable relative to the non-circular section of the housing for altering a parameter relating to the operation of the medical delivery device. The operable control member (150) comprises a belt-like structure arranged to move along the non-circular section of the housing so that respective portions of the operable control member change radius of curvature as the respective portions move relative to the non-circular section of the housing.
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IL-21 EPITOPE AND IL-21 LIGANDS (Fri, 07 Dec 2012)
The present invention relates to IL-21 ligands, such as e.g. antibodies, as well as use thereof.
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PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION OF INSULIN PEPTIDES (Thu, 22 Nov 2012)
The invention is related to pharmaceutical compositions suitable for oral administration of insulin peptides, methods of making such and treatment with such.
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GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS (Thu, 25 Oct 2012)
The invention relates to GLP-1 receptor agonist compounds with a modified N- terminus. The compounds are of the formula Chem. 1: Y-Z-P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y-Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration. The invention also relates to intermediate products for use in the preparation of the GLP-1 receptor agonist compounds of the invention.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES (Thu, 25 Oct 2012)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1 (7-37), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37), wherein the first K residue is designated K<sp>37</sp>, and the second K residue is designated K<sp>26</sp>, which derivative comprises two albumin binding moieties attached to K<sp>26</sp> and K<sp>37</sp>, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1 : HOOC-(CH<sb>2</sb>)<sb>X</sb>-CO-* Chem. 2: HOOC-C<sb>6</sb>H<sb>4</sb>-O-(CH<sb>2</sb>)<sb>y</sb>-CO-* Chem. 3: R<sp>1</sp>-C<sb>6</sb>H<sb>4</sb>-(CH<sb>2</sb>)<sb>Z</sb>-CO-* Chem. 4: HOOC-C<sb>4</sb>SH<sb>2</sb>-(CH<sb>2</sb>)<sb>W</sb>-CO-* in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, R<sp>1</sp> is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH<sb>2</sb>)<sb>2</sb>-(O-(CH<sb>2</sb>)<sb>2</sb>)<sb>k</sb>-O-(CH<sb>2</sb>)<sb>n</sb>-CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
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Spontaneously dispersible preconcentrates including a peptide drug in a solid or semisolid carrier (Thu, 25 Oct 2012)
The present invention relates to a solid or semisolid composition comprising a polypeptide (a), at least one polar organic solvent (b) for the polypeptide, at least one surfactant (c), at least one lipophilic component (d), and optionally at least one solid hydrophilic component (e), wherein said pharmaceutical composition is spontaneously dispersible, is provided.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES (Fri, 19 Oct 2012)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1 ); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K27, and the second K residue is designated KT; which derivative comprises two albumin binding moieties attached to K27 and KT, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC-(CH2)x-CO- and HOOC-C6H4-0-(CH2)y-CO-; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula -NH-(CH2)2-(O-(CH2)2)k-O-(CH2)n-CO-, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel GLP-1 analogues. The derivatives are suitable for oral administration.
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FATTY ACID ACYLATED AMINO ACIDS FOR ORAL PEPTIDE DELIVERY (Fri, 19 Oct 2012)
The present invention relates to fatty acid acylated amino acids (FA-aa's) acting as permeation enhancers for oral delivery of therapeutic macromolecules such as peptides and pharmaceutical compositions comprising such FA-aa's.
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NOVEL PEPTIDYL ALPHA-HYDROXYGLYCINE ALPHA-AMIDATING LYASES (Thu, 11 Oct 2012)
The present patent application concerns an enzyme capable of catalysing the conversion of a α-hydroxyglycine to an α-amide and the use of such enzymes for producing a C-terminal α-amidated peptide.
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NOVEL GLUCAGON ANALOGUES (Fri, 05 Oct 2012)
The present invention relates to novel glucagon peptides with improved stability and solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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MEDICAL INJECTION DEVICE WITH LARGE, MECHANICAL CIPHER DOSE DISPLAY (Fri, 05 Oct 2012)
An injection device is disclosed which comprises a housing (10) with a display for showing the size of a set dose. The display is formed from a number of individual ciphers (11, 40) which each comprises a plurality of segments (13, 14) extending horizontally and vertically. At the end of the injection device a dose setting element (20) is provided for allowing the user to set the size of the dose to be injected. Further, the display mechanism comprises a first pattern (35) for showing the vertical segments (14), and a second pattern (25) for showing the horizontal segments (13). The patterns (25, 35) are associated with the dose setting button (20) and arranged to be moved when the dose setting button (20) is operated. The injection device disclosed can have any number of ciphers (11, 40) which is coupled to each other in order to show to the user the size of any dose set.
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HUMAN INSULIN ANALOGUES AND DERIVATIVES COMPRISING CYSTEINE SUBSTITUTIONS (Fri, 21 Sep 2012)
The present invention relates to human insulin analogues containing a substituting cysteine, to human insulin derivatives containing a PEGylated substituting cysteine and methods of making such. The compounds of the invention may be useful for the treatment of diabetes.
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Stable non-aqueous pharmaceutical compositions (Thu, 13 Sep 2012)
The present invention relates to shelf stable non-aqueous pharmaceutical compositions, and to the use thereof in methods of treating diabetes and hyperglycaemia. The composition comprises a dehydrated therapeutically active insulinotropic peptide, and at least one semi-polar protic organic solvent which insulinotropic peptide has been dehydrated at target pH which is at least 1pH unit from the pI of the peptide in aqueous solution.
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ANTAGONISTIC DR3 LIGANDS (Sat, 08 Sep 2012)
The present disclosure relates to treatment of inflammatory diseases. In particular, the present disclosure relates to antagonistic DR3 ligands useful for treating inflammatory diseases.
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COAGULATION FACTOR-TARGETING TO TLT-1 ON ACTIVATED PLATELETS (Sat, 08 Sep 2012)
The current invention relates to: procoagulant proteins which may, for example, be fusion proteins or chemical conjugates; methods of producing said procoagulant proteins; polynucleotides that encode said fusion proteins and cells that expresses them. Furthermore, the current invention relates to procoagulant proteins for use as a medicament. Individuals that have a coagulopathy, such as haemophilia A and B with or without inhibitors, may be treated with the procoagulant proteins of the current invention.
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Stable formulations of GLP-1 (Thu, 06 Sep 2012)
Stable pharmaceutical composition comprising insulinotropic peptide.
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LONG-ACTING IL-1 RECEPTOR ANTAGONISTS (Fri, 24 Aug 2012)
The present invention relates to IL-1 receptor antagonist compounds, compositions and use thereof as well as methods for preparation thereof.
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PURIFICATION OF INSULIN (Fri, 10 Aug 2012)
The present application discloses a chromatographic process for separating protein components of a protein-containing solution, said solution comprising an insulin peptide and one or more di- or polyvalent metal ions, said insulin peptide being capable of self- association and/or structural change in the presence of di- or polyvalent metal ions, said process comprising the steps of: a) applying the protein-containing solution to a column of a chromatographic solid phase material, wherein the loading of the insulin peptide is at least 6.0 g per litre of column volume (g/Lcv ); and b)eluting the insulin peptide from said solid phase material by means of an eluent having a pH of at the most 8.5; and collecting a pool of the insulin peptide corresponding to at least 75 % by weight of the insulin peptide applied to the column in step (a).
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LEPTIN DERIVATIVES (Fri, 03 Aug 2012)
The invention relates to Leptin derivatives, compositions and therapeutic use there-of.
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GLP-1 COMPOSITIONS (Fri, 27 Jul 2012)
The present invention relates to pharmaceutical compositions comprising a GLP-1 compound, a divalent metal and a polycationic compound. The invention is characterised in that the GLP-1:divalent metal molar ratio is 1:>2. The compositions of the invention are particularly useful in the treatment of diabetes.
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IL-21 LIGANDS (Fri, 27 Jul 2012)
The present invention relates to IL-21 ligands binding to a discontunous epitope on the surface of the IL-21 molecule as well as use thereof.
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GLP-1 PARTICLES AND COMPOSITIONS (Fri, 27 Jul 2012)
The present invention relates to compositions and particles comprising a GLP-1 compound, a divalent metal and a polycationic compound. The invention is characterised that the particle comprises a core and a surrounding layer, the core comprising the GLP-1 compound and the divalent metal, and the surrounding layer comprising the polycationic compound. The invention is particularly useful for the treatment of metabolic diseases, including diabetes.
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MEDICAL INJECTION DEVICE (Fri, 06 Jul 2012)
The present invention relates to injection devices for injecting a dose of a medicament. The injection device (100) incorporates a housing (101), a needle assembly (150) and a cover (200). The needle assembly (150) comprises an injection needle (152, 153) accommodated in a needle container (151) having an opening which in a storage state of the injection device (100) is sealed by a film seal (155). The cover may include sections (201, 202) arranged movable relative to the housing (101). The injection device (100) is so configured that upon movement of the cover sections (201, 202) relative to the housing (101) the film seal (155) is changed from a sealing state to an unsealing state for shifting the injection device (100) into a ready-to-administer state.
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Urea glucokinase activators (Fri, 29 Jun 2012)
This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.
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A NEEDLE CANNULA WITH A COLLAPSE ZONE (Fri, 22 Jun 2012)
A metallic cylindrical tubular needle cannula (1) is subjected to a metal etching liquid inside the lumen (7) thereby increasing the inside diameter and enhancing the flow properties while maintaining the outside appearance. The inside wall (5) is further provided with a collapse zone (10) manufactured by radiating heat (11) to a specific outside area of the needle cannula (1 ) thereby increasing the aggression of the etchant. Further two different methods of in- process testing of the inside diameter of the needle cannulae using any fluid gas are disclosed.
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FAST-ACTING INSULIN IN COMBINATION WITH LONG-ACTING INSULIN (Fri, 22 Jun 2012)
Insulin preparations comprising a long-acting insulin compound, a fast-acting insulin compound, a nicotinic compound and an amino acid.
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PREPARATION COMPRISING INSULIN, NICOTINAMIDE AND AN AMINO ACID (Fri, 22 Jun 2012)
Insulin preparations comprising an insulin compound or a mixture of two or more insulin compounds, a nicotinic compound and an amino acid.
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AQUEOUS FACTOR VIII SOLUTION (Fri, 22 Jun 2012)
The present invention relates to methods for stabilizing FVIII in aqueous solutions comprising a relatively high concentration of FVIII. The invention furthermore relates to such aqueous solutions as well as use thereof.
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SOLID COMPOSITIONS COMPRISING A GLP-1 AGONIST AND A SALT OF N-(8-(2-HYDROXYBENZOYL)AMINO)CAPRYLIC ACID (Fri, 22 Jun 2012)
The present invention relates to solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.
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Preparation comprising insulin, nicotinamide and an amino acid (Fri, 01 Jun 2012)
Insulin preparations comprising an insulin compound or a mixture of two or more insulin compounds, a nicotinic compound and an amino acid.
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Ion exchange chromatography of proteins and peptides (Thu, 31 May 2012)
The present invention relates to an ion exchange chromatography process for purifying a peptide from a mixture containing said peptide and related impurities, and to an industrial method including such ion exchange chromatography process.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES (Sat, 19 May 2012)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1 (7-37) (SEQ ID NO: 1 ), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem. : HOOC-(CH2)x-CO-* Chem. 2: HOOC-C6H4-0-(CH2)y-CO-* Chem. 3: R2-C6H4-(CH2)z-CO-*, in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *-NH-(CH2)2-(0-(CH2)2)k-0-(CH2)n-CO-*. wherein k is an integer in the range of 1 -5, and n is an integer in the range of 1 -5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER (Sat, 19 May 2012)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1 : HOOC-(CH2)x-CO-*, and Chem. 2: HOOC-C6H4-0-(CH2)y-CO-*, in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises Chem. 3: *-NH-(CH2)q-CH[(CH2)w-NH2]-CO-*, wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are potent, protracted, and suitable for oral administration.
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TREATING DIABETES MELITUS USING INSULIN INJECTIONS ADMINISTERED WITH VARYING INJECTION INTERVALS (Fri, 04 May 2012)
The present invention relates to methods for treatment of a condition or disease where administration of insulin will be of benefit, comprising administering, to a patient in need thereof, effective dosages of an insulin, insulin analogue or derivative thereof,which exhibits a prolonged profile of action, wherein said dosages are administered at intervals of varying length.
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NOVEL N-TERMINALLY MODIFIED INSULIN DERIVATIVES (Fri, 20 Apr 2012)
The invention is related to novel N-terminally modified insulin derivatives, pharmaceutical compositions comprising such and methods of making such.
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GLP-1 AND FGF21 COMBINATIONS FOR TREATMENT OF DIABETES TYPE 2 (Thu, 19 Apr 2012)
The invention relates to the use of a Fibroblast Growth Factor 21 (FGF21 ) compound and a Glucagon-Like Peptide 1 (GLP-1 ) compound in combination for the preparation of a medicament for the treatment of diabetes, more in particular type 2 diabetes, as well as pharmaceutical compositions comprising certain FGF21 and GLP-1 compounds in combination, together with a pharmaceutically acceptable carrier. The combination has a significant effect on parameters of relevance for diabetes type 2, viz. on the viability of beta cells ex vivo in the presence of free fatty acids, on caspase activity of beta cells ex vivo (a measure of cell apoptosis), and a blood glucose lowering effect on db/db mice in vivo.
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Drug delivery device with cap functions for needle assembly (Thu, 19 Apr 2012)
Drug delivery system comprising a main portion with a cap as well as a needle assembly with a needle mounted in a hub and a needle cap releasably mountable on the hub to cover the needle. The cap comprises gripping means reversibly operatable between a first condition in which there is no gripping engagement between the mounted cap portion and the needle cap, this allowing the cap portion to be removed from the main portion without removing the needle cap from the hub, and a second condition in which the cap portion grippingly can engage the needle cap of a needle assembly, this allowing the needle cap to be removed from the hub together with the cap. The cap further comprises user actuation means for operating the gripping means between the two conditions.
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IL-21 variant nucleic acids (Fri, 06 Apr 2012)
IL-21 variants nucleic acid sequences are provided that encode a peptide having deletions and zero to ten conservative amino acid substitutions in the region of amino acid residues 65-96 of SEQ ID. NO:2.
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Basic protein purification tags from thermophilic bacteria (Fri, 06 Apr 2012)
The invention is related to a method for purification of recombinant proteins using highly basic proteins from thermophilic bacteria as purification tags for use in a cation-exchange chromatography purification step. The basic proteins may be ribosomal proteins. The recombinant proteins are expressed in eukaryotic or prokaryotic host cells. The purification tag will typically have a pl above about 9 and comprise from about 15 to about 250 amino acid residues.
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THERAPEUTIC FACTOR VIII ANTIBODIES (Fri, 30 Mar 2012)
The present invention relates to therapeutic FVIII antibodies. In particular, the present invention relates to FVIII antibodies having the ability to prolong the circulatory half life of FVIII. The present invention furthermore relates to use of such antibodies in treatment and prophylaxis of haemophilia A.
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FACTOR VIII VARIANTS HAVING A DECREASED CELLULAR UPTAKE (Fri, 23 Mar 2012)
The present invention relates to modified coagulation factors. In particular, the present invention relates to modied Factor VIII molecules having decreased cellular uptake.
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STABLE PHARMACEUTICAL COMPOSITIONS OF PEPTIDE DERIVATIZED USING AN OXIME LINKER (Thu, 15 Mar 2012)
The invention relates to stable pharmaceutical compositions comprising a therapeutic peptide derivatized with a property-modifying group, wherein the property-modifying group is conjugated to the peptide by use of a linker comprising an oxime bond.
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Anti-NKG2A antibodies and uses thereof (Thu, 08 Mar 2012)
Described herein are anti-NKG2A antibodies suitable for human therapy, including humanized versions of murine anti-NKG2A antibody Z270, as well as related methods and materials for producing and using such antibodies. Exemplary complementarity-determining regions (CDRs) sequences and sites for optional amino acid back-substitutions in framework region (FR) and/or CDRs of such antibodies are also described.
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MEDICAL INJECTION DEVICE (Fri, 02 Mar 2012)
The present invention relates to injection devices for injecting a medicament from a cartridge (600) through a needle cannula (510). The injection device (100) includes an actuator (330, 360) for driving a piston driver (310) and includes an end of stroke limiter (341, 611). When the piston driver (310) is arrested by the end of stroke limiter (341, 611) a shielding driver (370) is automatically triggered to actively shift the needle cannula (510) into a shielded state. The injection device may include a fluid dispensing interruption mechanism that automatically interrupts fluid flow when the piston driver has moved a predetermined stroke length. The injection device may also include a single pre-stressed spring acting exclusively in a linear compression mode or exclusively in a torsion mode and adapted to sequentially drive the device to enable fully automatic operation. The invention also relates to a method of sterilizing a needle cannula assembly.
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MEDICAL AUTO-INJECTION DEVICE FOR MANUAL NEEDLE INSERTION HAVING NEEDLE SHIELD, DAMPING MECHANISM AND AUDIBLE AND TACTILE FEEDBACK (Fri, 24 Feb 2012)
The present invention relates to medicament injection devices (100). A cartridge (600) with a septum and a needle unit (500) having front and rear needles (510, 520) are configured for relative movement from a state where the septum is sealed to a state where the septum is pierced by the rear needle (520). The injection device (100) may include a needle shield (350) and be configured for piercing the septum by the rear needle (520) when the front needle (510) is operated relative to the needle shield (350). The injection device (100) may also include a damping mechanism configured for limiting the speed of movement of the cartridge relative to the needle unit. The injection device (100) may also include an indicator generating a signal when a piston driver has travelled the complete stroke length, wherein the indicator has a deflection element that is deflected prior to or during movement of the cartridge relative to the housing.
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Peptide purification by means of hard metal ion affinity chromatography (Thu, 02 Feb 2012)
A polymer substrate functionalized with a functionality comprising at least one cyclic, metal ion coordinating ligand group which comprises at least 3 nitrogen donor atoms in the ring of the cyclic group, at least one of the nitrogen atoms having an optionally substituted carboxy(lower alkyl) or optionally substituted phosphono(lower alkyl) group covalently attached thereto, is well suited for use in conjunction with "hard" metal ions of low toxicity (such as Ca 2+ , Mg 2+ or Fe 3+ ) in the separation/purification of appropriately "tagged" polypeptides by I mmobilized M etal ion A ffinity C hromatography (IMAC).
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REMODELING AND GLYCOCONJUGATION OF PEPTIDES (Tue, 31 Jan 2012)
REMODELING AND GLYCOCONJUGATION OF PEPTIDES ABSTRACT The invention includes methods and compositions for forming a covalent conjugate of a peptide, including the addition or deletion of one more glycosyl groups to a peptide, and/or the addition of a modifying group (e.g., polymer) to a peptide. (no figure)
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GROWTH HORMONE CONJUGATES (Fri, 27 Jan 2012)
The present invention relates to growth hormone conjugates comprising a bile acid residue, said conjugation may occur through wt or mutant amino acid residues. The growth hormone polypeptide may be wt human growth hormone or a growth hormone variant.
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N-TERMINAL MODIFIED FGF21 COMPOUNDS (Fri, 27 Jan 2012)
Analogues of FGF21 carrying a modifying, substituted ethylene or benzyl group can be used for treatment or prevention of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD).
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STABILIZED FACTOR VIII VARIANTS (Fri, 20 Jan 2012)
The present invention relates to modified coagulation factors. In particular, the present invention relates to stabilized Factor VIII molecules conjugated with a half life extending moiety as well as use of such molecules.
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A PISTON ROD FOOT (Fri, 20 Jan 2012)
The invention relates to a medical drug delivery apparatus which comprises a cartridge (1) being closed at one end by a flexible membrane (2) and at the opposite end by a movable piston (10). The movable piston rod (19) is moved forward by a piston rod (20). In order to distribute the force from the piston rod (20) to the movable piston (10) a piston rod foot (30) is provided sandwiched between the piston rod (29) and the movable piston (10) The piston rod foot (30) provided between the piston rod (20) and the movable piston (10) has a plurality of arms (34) extending in a direction perpendicular to a longitudinal axis (X) of the cartridge (1) and which arms (34) engages the inner wall (4) of the cartridge (1) thereby obtaining geometric guidance or generating a force of friction between the piston rod foot (30) and the inner wall (4) of the cartridge (1).
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INTERLEUKIN-21 VARIANTS HAVING ANTAGONISTIC BINDING TO THE IL-21 RECEPTOR (Thu, 19 Jan 2012)
The invention relates to isolated IL-21 variant peptides having antagonistic binding to the common gamma chain (yC) of the IL-21 receptor, to pharmaceutical compositions comprising said peptides and to the use of said peptides in therapy.
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SYSTEM FOR INDICATING LIFETIME STATUS FOR MEDICAL COMPONENT (Fri, 13 Jan 2012)
A drug delivery system (105, 500) is provided comprising means for receiving a reservoir assembly (230, 521) containing an amount of drug having a recommended maximum service lifetime, a delivery assembly (220, 510) adapted for cooperation with the reservoir to deliver drug there from, display means (515) for displaying information to a user, and electronic control means (210). The control means is adapted to store information representing the recommended maximum service lifetime of the reservoir assembly, detect an initial time when an operation associated with the initial use of the reservoir assembly takes place, calculate the time left until the recommended maximum service lifetime has been reached, and control the display to indicate the time left. In this way the user is automatically kept informed as to when the reservoir assembly should be replaced.
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Protease resistant insulin analogues (Thu, 12 Jan 2012)
The present invention relates to novel insulin analogues exhibiting resistance towards protease, wherein at least two amino acids are substituted and/or deleted relative to the parent insulin molecule. A method for the preparation of such insulin analogues, insulin preparations containing the insulin analogues of the invention and a method of treating diabetes mellitus using these insulin analogues is also provided.
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Liquid, aqueous pharmaceutical compositions of factor VII polypeptides (Fri, 06 Jan 2012)
The present invention is directed to liquid, aqueous pharmaceutical compositions stabilized against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilizing agent (iii) comprising a —C(═N—Z1—R1)—NH—Z2—R2 motif, e.g. benzamidine compounds and guanidine compounds such as arginine.
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ANTIBODIES THAT ARE CAPABLE OF SPECIFICALLY BINDING TISSUE FACTOR PATHWAY INHIBITOR (Fri, 06 Jan 2012)
The invention relates to antibodies that are capable of specifically binding tissue factor pathway inhibitor (TFPI), neutralising free TFPI and reducing the clotting time of blood. Furthermore, the invention relates to polynucleotides that encode such antibodies and to cells that comprise the polynucleotides or that express the antibodies of the invention. Such antibodies have utility in the treatment of subjects with a coagulopathy, alone as well as in combination with a second agent.
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IMPROVED ANTIBODY BINDING AFFINITY LIGANDS (Fri, 06 Jan 2012)
The present invention discloses particularly useful ligands covalently bound to a solid support material, such as a polymer matrix, and uses thereof in the purification and/or isolation of biomolecules, such as proteins, in particular antibodies, such as monoclonal antibodies. The ligands include compounds of the formula (3,5-di-tert-butyl-4-hydroxy-benzoyl)-Arg-Arg-.
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Antibodies against tissue factor pathway inhibitor (Fri, 30 Dec 2011)
The invention relates to antibodies that specifically bind to tissue factor pathway inhibitor (TFPI) and that reduce the clotting time of blood. Such antibodies have utility in the treatment of subjects with a coagulopathy.
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Process for the Purification of Antibodies Using Affinity Resins Comprising Specific Ligands (Fri, 30 Dec 2011)
The present invention relates to a novel process for the purification of antibodies, e.g. monoclonal antibodies. The process utilizes an affinity resin comprising a solid phase material having immobilized thereto one or more low-molecular weight synthetic ligands. The affinity resins enable the separation of antibodies from even closely related proteins.
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PEGYLATED, EXTENDED INSULINS (Fri, 30 Dec 2011)
PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regular insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.
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HUMAN INSULIN CONTAINING ADDITIONAL DISULFIDE BONDS (Fri, 30 Dec 2011)
The present invention is related to human insulin containing additional disulfide bonds and methods of making such.
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INSULIN ANALOGUES CONTAINING ADDITIONAL DISULFIDE BONDS (Fri, 30 Dec 2011)
The present invention is related to insulin analogues containing additional disulfide bonds and methods of making such.
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INSULIN DERIVATIVES CONTAINING ADDITIONAL DISULFIDE BONDS (Fri, 30 Dec 2011)
The present invention is related to insulin derivatives containing additional disulfide bonds and methods of making such.
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MEDICAL CONTAINER PROTECTED AGAINST CRACKING (Fri, 30 Dec 2011)
Medical containers made of plastic can be protected against cracking by adding a layer of a poly-paraxylylene structure to said container.
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Peptide purification by means of hard metal ion affinity chromatography (Thu, 29 Dec 2011)
A polymer substrate functionalized with a functionality comprising at least one cyclic, metal ion coordinating ligand group which comprises at least 3 nitrogen donor atoms in the ring of the cyclic group, at least one of the nitrogen atoms having an optionally substituted carboxy(lower alkyl) or optionally substituted phosphono(lower alkyl) group covalently attached thereto, is well suited for use in conjunction with "hard" metal ions of low toxicity (such as Ca 2+ , Mg 2+ or Fe 3+ ) in the separation/purification of appropriately "tagged" polypeptides by Immobilized Metal ion Affinity Chromatography (I MAC).
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MODIFICATION OF FACTOR VIII (Thu, 29 Dec 2011)
A Factor VIII derivative of formula (I): wherein: B represents C<sb>2</sb> to C<sb>10</sb> alkylene; m represents 0 or an integer from 1 to 19, n represents an integer from 1 to 20, and the sum of m and n is from 1 to 20; P represents a mono or polyradical of Factor VIII obtained by removing m + n carbamoyl groups from the side chains of glutamine residues in Factor VIII; and M represents a moiety (M<sp>1</sp>) that increases the plasma half-life of the Factor VIII derivative or a reporter moiety (M<sp>2</sp>); or a pharmaceutically acceptable salt thereof.
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Modification of Factor VIII (Fri, 16 Dec 2011)
A Factor VIII derivative of formula (I): wherein: B represents C2 to C10 alkylene; m represents 0 or an integer from 1 to 19, n represents an integer from 1 to 20, and the sum of m and n is from 1 to 20; P represents a mono or polyradical of Factor VIII obtained by removing m+n carbamoyl groups from the side chains of glutamine residues in Factor VIII; and M represents a moiety (M1) that increases the plasma half-life of the Factor VIII derivative or a reporter moiety (M2); or a pharmaceutically acceptable salt thereof. <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="17.53mm" wi="76.12mm" file="US20110306551A1-20111215-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> 
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STABLE GROWTH HORMONE COMPOUNDS (Fri, 16 Dec 2011)
The present invention relates to stable growth hormone (GH) compounds, which through the introduction of cysteine residues have disulphide bridges, which make the compounds resistant to proteolytic degradation.
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FGF21 ANALOGUES AND DERIVATIVES (Fri, 16 Dec 2011)
Derivatives of Fibroblast Growth Factor 21 which have improved properties for treating diabetes can be prepared by a recombinant process.
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Propylene Glycol-containing peptide formulations which are optimal for production and for use in injection devices (Thu, 15 Dec 2011)
The present invention relates to pharmaceutical formulations comprising a peptide and propylene glycol, to methods of preparing such formulations, and to uses of such formulations in the treatment of diseases and conditions for which use of the peptide contained in such formulations is indicated. The present invention further relates to methods for reducing the clogging of injection devices by a peptide formulation and for reducing deposits on production equipment during production of a peptide formulation.
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Protracted Exendin-4 Compounds (Fri, 09 Dec 2011)
Novel protracted exendin-4 compounds and therapeutic uses thereof.
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ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS (Fri, 09 Dec 2011)
This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
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Coagulation factor VII polypeptides (Thu, 08 Dec 2011)
The present invention relates to novel coagulation Factor VII polypeptides, polynucleotide constructs encoding such polypeptides, as well as vectors and host cells comprising and expressing the polynucleotide, pharmaceutical compositions, uses and methods of treatment.
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ANTI-KIR COMBINATION TREATMENTS AND METHODS (Fri, 02 Dec 2011)
Compositions comprising anti-KIR antibodies and one or more secondary anti-cancer agents or anti-viral agents and methods of using such combinations (as combination compositions or in separate administration protocols) in the treatment of cancers (e.g., lung cancer) or viral infection (e.g., HIV or HCV infection) are provided.
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PHARMACEUTICAL COMPOSITIONS SUITABLE FOR ORAL ADMINISTRATION OF DERIVATIZED INSULIN PEPTIDES (Fri, 02 Dec 2011)
The invention is related to a water-free liquid or semisolid pharmaceutical composition comprising a derivatized insulin peptide, at least one polar organic solvent and at least one lipophilic component and a method of treatment using such.
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Novel Insulin Analogues (Fri, 02 Dec 2011)
Insulin analogues wherein the B25 amino acid residue is His or Asn with the proviso that if the B25 amino acid residue is His, then the B27 amino acid residue is Asp or Glu and the A14 amino acid residue is different from Glu, have liver preferential actions.
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BENDED INJECTION NEEDLE (Fri, 02 Dec 2011)
A method of manufacturing a bended injection needle assembly comprising the steps of: mounting a straight one-piece metallic needle cannula (20) in a hub (1), securing the straight needle cannula (20) to the hub (1) and bending the needle cannula (20) such that at least a part of the needle cannula deflects away from the first axis (X).
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MEDICAL ASSEMBLY WITH MONITORING DEVICE (Fri, 02 Dec 2011)
An assembly comprises a drug delivery device and a monitoring device adapted to detect an action taking place in the drug delivery device. The drug delivery device comprises a main portion having a drug expelling mechanism for expelling drug from a reservoir through an outlet, a housing in which at least a portion of the expelling mechanism is arranged, and coupling means for a cover. The cover is adapted to cover the outlet when mounted on the main portion. The monitoring device comprises a housing portion, means for detecting an action taking place in the drug delivery device, and coupling means adapted to engage the coupling means on the main portion. By this arrangement the monitoring device can be placed in a pre-determined position relative to the main portion when the coupling means engage each other, this allowing efficient transmission of information between the monitoring device and the main portion.
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STABLE MULTI-DOSE COMPOSITIONS COMPRISING AN ANTIBODY AND A PRESERVATIVE (Fri, 02 Dec 2011)
The invention relates to stable, multi-dose liquid compositions containing proteins, in particular, but not exclusively stable antibodies, and to the use of said compositions in therapy, in particular for the subcutaneous delivery of said stable protein.
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G6PC2-Encoded Beta Cell Surface Tags (Fri, 25 Nov 2011)
The invention relates to G6PC2-encoded beta cell surface markers, methods of identifying and obtaining a culture cells comprising fully differentiated beta cells. Also contemplated is a method of sorting such cells, isolated cells and compositions thereof.
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Polypeptide Purification (Fri, 25 Nov 2011)
The invention relates to the purification of different gamma carboxylated forms of a polypeptide using ion exchange chromatography. In particular, the invention provides a method for purifying a polypeptide having a desired content of gamma-carboxyglutamic acid from a sample comprising mixture of species of said polypeptide having different contents of gamma-carboxyglutamic acid, said method comprising the steps of: (a) loading said sample onto an anion exchange chromatography material; (b) eluting said polypeptide using a solution at a pH of less than pH 9.0 comprising at least one salt selected from ammonium acetate, ammonium chloride and sodium acetate; and (c) selecting a fraction obtained from said elution wherein the polypeptides in the fraction have the desired content of gamma-carboxyglutamic acids.
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PROCESS FOR THE PREPARATION OF INSULIN-ZINC COMPLEXES (Fri, 18 Nov 2011)
The invention concerns a process for preparing a pharmaceutical formulation comprising an insulin derivative, wherein the process comprises dissolving an insulin derivative in water, adjusting the pH of the solution to a pH above 7.2, adding a zinc solution while stirring continuously and adjusting the pH to the target pH of the formulation.
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Insulin derivative (Thu, 17 Nov 2011)
The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.
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Long-Acting Y2 and/or Y4 Receptor Agonists (Fri, 11 Nov 2011)
The present invention relates to a PYY or PP peptide derivative or analogue thereof derivatised with one or more serum albumin binding side chains comprising a dis-tal tetrazole or carboxylic acid group. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y receptor modulation.
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A spherical encoded bead with an ultrasonic identification chip (Thu, 10 Nov 2011)
The present application discloses spherical polymer bead comprising embedded therein an ultrasonic identification chip, said chip comprising one or more resonator cavities, the dimensions of each of the one or more resonator cavities giving rise to an ultrasonic resonance frequency of 20 kHz or more. The application also discloses a bead sorting apparatus equipped with at least one ultrasonic transmitter and at least one ultrasonic receiver, and a method of measuring the ultrasonic code of an ultrasonic encoded bead using the bead sorting apparatus.
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Method of Quality Control Testing a Factor XIII Containing Sample (Fri, 04 Nov 2011)
The invention relates to a method of quality control testing a Factor XIII (FXIII) containing sample which comprises the step of detecting the presence of and/or measuring the concentration of pre-activated FXIII (FXIIIao) in said sample and to a quality control kit for determining the quality of a Factor XIII (FXIII) containing sample. Preferably, an anion-exchange chromatographic column is used, as well as the fluorescent substrate Abz-NE (Cad-Dnp) EQVS PLTLLK-OH.
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Antibodies Against Tissue Factor Pathway Inhibitor (TFPI) (Fri, 04 Nov 2011)
The invention relates to antibodies that specifically bind to tissue factor pathway inhibitor (TFPI) and that reduce clotting time in (a) human FVIII-deficient plasma and/or (b) human whole blood. Such antibodies have utility in the treatment of bleeding disorders and in the stimulation of blood clotting.
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Method for Selectively Modifying a Protein (Fri, 04 Nov 2011)
The present invention relates generally to a novel method of introducing property modifying groups to a protein. In particular, the present invention relates to the derivatization of lysine residues, as well as new conjugates of growth hormones with improved pharmacological properties, and methods for their preparation and use in therapy.
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Skin Retention Device for a Medical Jet Injection Kit (Fri, 04 Nov 2011)
A skin retention device 10 for a medical jet-injection unit 20 comprises a contact face provided with adhesive 12 in the area surrounding and close to the injection opening(s) 11 of the nozzle 21 which ensures god contact between the nozzle 21 and the skin 30 of a subject in the area chosen for an injection. Consequently the injection force can be lowered dramatically. In case of two-stage jet-injections, the initial injection force can be lowered because the skin retention close to the injection point significantly reduces the energy consuming elastic expansion of the skin 30 in the injection area, and the second injection force can be lowered because of the high degree of fixed positioning of the injection opening of the nozzle 21 relative to the injection channel in the skin 30 made during the initial injection stage. Thus a high degree of injection safety is achieved, minimizing the risk of whet shots, while skin lift and lower injection force decreases the risk of damage of the underlying tissue.
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ELECTRONICALLY ASSISTED DRUG DELIVERY DEVICE (Fri, 04 Nov 2011)
The present invention relates to electronically assisted drug delivery devices (100). The drug delivery device may include a Gray code type detector for sensing dosage data, wherein the detector comprises a code track consisting of a sequence of alternating markings and a plurality of detectors that are mutually spaced in a direction extending along the code track. The drug delivery device may also include a dosage selector (260) which is moved in a proximal direction upon dose setting and in a distal direction upon dose injection, where the dosage selector is latched in the end of dose position by a latching element, the latching element actuating an end of dose switch for signalling the end of dose state. The drug delivery device may also incorporate power-management arrangements which effectively minimizes power consumption for the incorporated electronic circuitry.
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COVER WITH DEVICE ACTUATION FEATURE (Fri, 28 Oct 2011)
The invention provides an assembly comprising a cover and a device arranged fully or partly in the cover. The device comprises a first portion, and a second portion moveable relative to the first portion between an initial and an actuated position, and the cover comprises a cavity portion and a closure portion which together form an enclosure in which the device is arranged initially. Movement of the closure portion from an initial position in a first direction results in the second portion of the device being moved in a second direction between the initial and the actuated position, the first direction being different from the second direction. By this arrangement it is possible to provide a cover-device assembly which is easy and intuitive to use and open and at the same time ensures that the enclosed device is actuated correctly.
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SELECTIVE MODIFICATION OF PROTEINS (Fri, 28 Oct 2011)
A method of selectively introducing a substituent into a protein proximal to a binding site on the protein for a homing peptide, comprising: (a) contacting the protein with a compound comprising a homing peptide having the ability to bind to the binding site of the protein; and (b) allowing a moiety on the protein proximal to the binding site to react with the compound comprising the homing peptide, thereby to transfer the substituent G onto the protein.
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LONG-ACTING GASTRIN DERIVATIVES (Fri, 28 Oct 2011)
The present invention relates to gastrin derivatives comprising gastrin or an analogue or fragment thereof and a derivatisation group and therapeutic use thereof.
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Method and an Apparatus for Sterilizing Packaging Material (Fri, 21 Oct 2011)
A method and an apparatus for sterilizing packaging material for use in packaging for protein containing products, such as food products or medical drugs. The packaging material is sterilized by irradiating it using a beam of ionizing radiation, such as an electron beam or a beam of gamma rays. Afterwards, the packaging material is processed in such a manner that protein reactive substances or compounds formed in the packaging material during the irradiation step are at least partly removed or rendered inreactive with respect to proteins. The processing step may advantageously be performed by heating the packaging material. Preferably, the processing step involves accelerating diffusion from the packaging material of protein reactive substances or compounds. Since the protein reactive substances or compounds are removed or rendered inreactive with respect to proteins, degradation of the product which is later stored in the packaging material is considerably reduced. The packaging material needs to be stored under sterile conditions for a shorter period of time. Thereby the space needed for sterile storage, as well of the risk of contamination, is considerably reduced.
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Urea glucokinase activators (Thu, 20 Oct 2011)
The invention provides a compound of general formula (1) wherein the substituents are defined futher in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
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REMINDER PROGRAMMING DEVICE AND METHOD (Fri, 14 Oct 2011)
An electronically controlled reminder device is adapted to be set in a programming mode by a user, perform a user-actuated operation, and detect when a user-actuated operation is performed. When in programming mode the device is adapted to record and set reminders in accordance with a detected time pattern of operation(s) of the device, wherein the programming mode is activated for a pre-determined number of operations or for a pre-determined period of time, after which the device automatically returns to the operational mode in which it provides reminders to the user based on the recorded time pattern of operations. Thus, normal use of the device provides automatic programming of the reminder scheme.
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Stabilised Insulin Compositions (Fri, 07 Oct 2011)
The present invention relates to human insulin analogues having a fast onset of action. These analogues may have amino acid in position B26 substituted with Phe, or be Des(B30) analogues of human insulin. The invention also relates to compositions comprising such insulin analogues, and to compositions comprising a mixture of an insulin analogue having a fast onset of action and insulin having a protracted action.
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PHARMACEUTICAL COMPOSITIONS SUITABLE FOR ORAL ADMINISTRATION OF DERIVATIZED INSULIN PEPTIDES (Thu, 06 Oct 2011)
The invention is related to a water-free liquid or semisolid pharmaceutical composition comprising a derivatized insulin peptide, at least one polar organic solvent and at least one lipophilic component and a method of treatment using such.
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PEPTIDES FOR TREATMENT OF OBESITY (Thu, 06 Oct 2011)
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
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E. COLI BL21 STRAIN LACKING A FUNCTIONAL GROUP II CAPSULAR GENE CLUSTER (Fri, 30 Sep 2011)
The present invention relates to a novel non-pathogenic Escherichia coli (E. coli) B BL21 strain comprising a deletion of group II capsular gene cluster, and the use thereof for the production of peptides.
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Novel NIDDM Regimen (Fri, 30 Sep 2011)
The present invention relates to the use of a short-acting oral hypoglycemic agent and to a novel regimen in the treatment of type 2 diabetes in which the endogenous secretion of insulin is stimulated in connection with meals by administering in connection with the meals a short-acting oral hypoglycaemic agent. Also, the present invention relates to a method of achieving significantly improvement in the glycaemic control by a combined use of repaglinide and metformin in NIDDM patients poorly controlled on metformin alone.
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NOVEL GLUCAGON ANALOGUES (Fri, 30 Sep 2011)
The present invention relates to glucagon peptide agonists which have improved solubility and stability, to the use of the peptides in therapy, to methods of treatment comprising administration of the peptides to patients in need thereof, and to the use of the peptides in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hypoglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hypoglycemia, diabetes and obesity.
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NOVEL GLUCAGON ANALOGUES (Fri, 30 Sep 2011)
The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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NOVEL GLUCAGON ANALOGUES (Fri, 30 Sep 2011)
The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.
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Transglutaminase mediated conjugation of peptides (Thu, 29 Sep 2011)
Methods for conjugating peptides are provided comprising i) reacting a peptide with a first compound comprising a functional group in the presence of a transglutaminase capable of incorporating said compound into the peptide to form a transaminated peptide, and ii) reacting said transaminiated peptide with e.g. a functionalised polymer capable of reacting with the functional group incorporated in the peptide in the enzymatic reaction.
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Insulin and IGF-1 receptor agonists and antagonists (Thu, 29 Sep 2011)
Peptide sequences capable of binding to insulin and/or insulin-like growth factor receptors with either agonist or antagonist activity and identified from various peptide libraries are disclosed. This invention also identifies at least two different binding sites which are present on insulin and insulin-like growth factor receptors which selectively bind the peptides of this invention. As agonists, certain of the peptides of this invention may be useful for development as therapeutics to supplement or replace endogenous peptide hormones. The antagonists may also be developed as therapeutics. In one embodiment, the receptor-binding peptides comprise the core motive B6: X 6 X 7 X 8 X 9 X 10 X 11 X 12 X 13 wherein X 6 and X 7 are aromatic, and X 10 and X 13 are hydrophobic residues.
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BLOOD COAGULATION FACTOR INHIBITORS (Fri, 23 Sep 2011)
The invention relates to novel compounds with formula (I) useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIa, Factor VII variants, or Factor VII derivatives.
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TREATING DIABETES MELITUS USING INSULIN INJECTIONS WITH LESS THAN DAILY INJECTION FREQUENCY (Fri, 23 Sep 2011)
The present invention relates to an insulin derivative for the treatment of a condition or disease where administration of insulin will be of benefit, comprising administering, to a patient in need thereof, effective dosages of the insulin derivative, wherein said insulin derivative exhibits a prolonged profile of action and wherein said dosages are administered at intervals longer than 24 hours.
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GLP-I Agonist And Cardiovascular Complications (Fri, 23 Sep 2011)
Methods and uses for the treatment and prevention of cardiac and cardiovascular diseases comprising administration of a GLP-1 agonist.
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IL-21 DERIVATIVES (Fri, 23 Sep 2011)
PROBLEM TO BE SOLVED: To provide derivatives of IL-21 or variants thereof.SOLUTION: There are provided various derivatives of human interleukin 21 (IL-21), including the following chemically modified peptides, (a) a derivative of a human IL-21 polypeptide comprising a mature IL-21 polypeptide or a mature IL-21 polypeptide with the N-terminal Met, and (b) a derivative including at least one lipophilic substituent attached in the N-terminal or the C-terminal of the IL-21 polypeptide, or variants of the IL-21 peptides.COPYRIGHT: (C)2011,JPO&INPIT
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CONJUGATED PROTEINS WITH PROLONGED IN VIVO EFFICACY (Fri, 16 Sep 2011)
The invention relates to conjugated proteins, in particular but not exclusively, blood coagulation factors, to processes for preparing said conjugates, to pharmaceutical compositions comprising said conjugates and to the use of the conjugates in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.
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TWO-PART HINGED NEEDLE MAGAZINE (Sat, 10 Sep 2011)
A needle magazine (10, 110) for storing a plurality of pen needle assemblies in combination with a plurality of pen needle units is disclosed. The magazines each comprise a first part (11, 111) and a second part (12, 112), each holding a number of pen needle assemblies. The first part (11, 111) and the second part (12, 112) are hinged together by a hinge mechanism (13, 113) such that the pen needle magazine (10, 110) can be folded to be easily carried by a user. The needle magazine (10, 110) also comprises an irreversible locking mechanism (30, 31, 130) such that the needle magazine (10, 110) can be used as a waste bin when discarding the used pen needle assemblies.
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PREPARATIVE RP-HPLC METHOD FOR PURIFYING PEPTIDES (Sat, 10 Sep 2011)
A method for separating on a RP-HPLC system a polypeptide of interest from at least one unwanted component is described, wherein at least one of the elution steps is performed at or in close proximity to the pl value of the peptide of interest.
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Method of Acylating a Peptide or Protein (Fri, 02 Sep 2011)
A method has for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.
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PEPTIDES FOR TREATMENT OF OBESITY (Fri, 02 Sep 2011)
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
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STABLE ANTIBODY CONTAINING COMPOSITIONS (Fri, 02 Sep 2011)
The invention relates to stable and low viscous (< 50 cP) protein containing compositions, in particular, but not exclusively stable antibody containing compositions and to the use of said stable proteins in therapy, in particular for the subcutaneous delivery of said stable protein.
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PEPTIDES FOR TREATMENT OF OBESITY (Fri, 02 Sep 2011)
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
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MEDICAL INJECTION DEVICE WITH TIME DELAY INDICATOR (Fri, 26 Aug 2011)
The present invention relates to an indicating device for use with medical injection devices for administering a drug into the body of a subject user wherein the indicating device is configured for indicating after administration that a dose of the drug actually has been administered and for maintaining this indication until lapse of a pre-defined time interval. The time delay indicator disclosed is based on a mechanical time delay device and includes a visual indicator that is controlled by the mechanical time delay device for signalling the status of the device during lapse of the pre-defined time interval.
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FACTOR VIII FUSION PROTEIN (Fri, 26 Aug 2011)
The present invention relates to modified coagulation factors. In particular, the present invention relates to conjugated Factor VIII molecules fused to a polypeptide such as e.g. an antibody binding protein or a Fc domain.
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FACTOR VIII MOLECULES WITH REDUCED VWF BINDING (Fri, 26 Aug 2011)
The present invention relates to a recombinant Factor VIII molecule, wherein said molecule has reduced vWF binding capacity, and wherein said molecule is covalently conjugated with at least one side group.
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CONJUGATED PROTEINS (Fri, 26 Aug 2011)
The present invention relates to modified therapeutic proteins, such as e.g. coagula- tion factors. In particular, the present invention relates to conjugated Factor VIII molecules such as e.g. FVII, FVIII, or FIX comprising a hydrophobic side group.
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ACTIVATABLE CONSTRUCTS (Fri, 26 Aug 2011)
The current invention relates to a construct, a polynucleotide that encodes said construct and a cell that expresses said construct. Furthermore, the current invention relates to the use of said construct for the treatment of bleedings and their associated co-morbidities and to a method of treatment of bleedings, inflammation and metastasis of cancer cells.
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CONJUGATED FVIII VARIANTS (Fri, 26 Aug 2011)
The present invention relates to conjugated Factor VIII variants. The present invention in particular relates to conjugated FVIII variants comprising different polymeric groups as well as use thereof.
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PURIFICATION METHOD (Fri, 26 Aug 2011)
The present invention provides a method for purification of a protein that is conjugated to an albumin binding moiety from a mixture comprising (i) said protein in said conjugated form and (ii) said protein in a form that is not conjugated to said albumin-binding moiety, the method comprising: (a) providing a solid support comprising a substance capable of specifically binding to the albumin binding moiety; (b) contacting said solid support of (a) with said mixture comprising protein and conjugated protein under suitable conditions for binding of the albumin binding moiety to the substance as defined in (a); and (c) eluting components bound to the solid support.
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Reduction of the content of protein contaminants in compositions comprising a vitamin K-dependent protein of interest (Thu, 25 Aug 2011)
The present invention relates to Vitamin K-dependent protein compositions having a very low, or negligible, content of protein contaminants. The present invention also relates to method applicable in the preparation of such Vitamin K-dependent protein compositions. Such methods may either be used alone or in sequential combination with the purpose of reducing the relative content of protein contaminants. The present invention is particularly relevant in the preparation of compositions of coagulation factors selected from Factor X polypeptides (FX/FXa), Factor IX polypeptides (FIX/FIXa), Factor VII polypeptides (FVII/FVIIa), and the anticoagulant Protein C, in particular Factor VII polypeptides.
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Selective reduction and derivatization of engineered proteins comprinsing at least one non-native cysteine (Thu, 25 Aug 2011)
The present invention relates to method for selective reduction and derivatization of recombinantly prepared engineered proteins comprising at least one non-native cysteine, wherein the reduction reaction is conducted in the presence of a redox buffer or in the presence of a triarylphosphine reducing agent.
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IL-21 variants (Thu, 25 Aug 2011)
A peptide, comprising a sequence obtained by: (a) deleting at least four amino acids and (b) conservatively substituting one to ten amino acids within amino acids 65-96 of SEQ ID NO:2.
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E. COLI BL21 STRAIN LACKING A FUNCTIONAL GROUP II CAPSULAR GENE CLUSTER (Thu, 18 Aug 2011)
The present invention relates to a novel non-pathogenic Escherichia coli (E. coli) B BL21 strain comprising a deletion of group Il capsular gene cluster, and the use thereof for the production of peptides.
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FACTOR VII FUSION POLYPEPTIDES (Fri, 05 Aug 2011)
The present invention relates to a Factor VII (FVII) fusion polypeptide with a prolonged half-life, wherein the FVII polypeptide can be activated or is in the activated form.
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O-LINKED GLYCOSYLATION OF PEPTIDES (Mon, 01 Aug 2011)

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STABLE GROWTH HORMONE COMPOUNDS (Fri, 29 Jul 2011)
The present invention relates to growth hormone (GH) compounds having additional disulphide bridges and at least one additional single point mutation making the compounds resistant to proteolytic degradation.
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GROWTH HORMONES WITH PROLONGED IN-VIVO EFFICACY (Fri, 29 Jul 2011)
The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there althered profile considered particular useful in therapy.
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PROCESS FOR PREPARING FGF-21 WITH LOW DEGREE OF O-GLYCOSYLATION (Fri, 29 Jul 2011)
Expression of FGF21 in a S. cerevisiae pmt2 knock out strain reduces the O-glycosylation significantly and does not decrease the expression level. Expression in mkc7 knock out strain can decrease degradation of FGF21 and analogues thereof. Point mutations at position R17 and R36 can decrease degradation of FGF21 and analogues thereof when they are expressed in yeast.
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Ion exchange chromatography of GLP-1, analogs and derivatives thereof (Thu, 28 Jul 2011)
The present invention relates to an ion exchange chromatography process for purifying GLP-1 or an analog or a derivative thereof from a mixture containing said GLP-1 and related impurities, and to an industrial method including such ion exchange chromatography process
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O-LINKED GLYCOSYLATION USING N-ACETYLGLUCOSAMINYL TRANSFERASES (Fri, 22 Jul 2011)
The present invention provides covalent conjugates between a polypeptide and a modifying group, such as a water-soluble polymer (e.g., PEG). The amino acid sequence of the polypeptide includes one or more O-linked glycosylation sequence, each being a substrate for a GIcNAc transferase. The modifying group is covalently linked to the polypeptide via a glycosyl-linking group interposed between and covalently linked to both the polypeptide and the modifying group. In one embodiment, a glucosamine linking group is directly attached to an amino acid residue of the O-linked glycosylation sequence. The invention further provides methods of making polypeptide conjugates. The present invention also provides non-naturally occurring polypeptides that include at least one O-linked linked glycosylation sequence of the invention, wherein each glycosylation sequence is a substrate for a GIcNAc transferase. The invention further provides pharmaceutical compositions that include a polypeptide conjugate of the invention.
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Method of Controlling a Polypeptide Modification Reaction (Fri, 22 Jul 2011)
The invention relates to a method of controlling a polypeptide modification reaction, in particular but not exclusively, a method of controlling the activation of human factor VII (FVII) to produce human factor VII(a) (FVII(a)). The invention also relates to polypeptides obtainable by the polypeptide modification reaction and to pharmaceutical compositions comprising said polypeptides.
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PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION OF INSULIN PEPTIDES (Fri, 22 Jul 2011)
The invention is related to pharmaceutical compositions suitable for oral administration of insulin peptides, methods of making such and treatment with such.
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PURIFICATION OF BLOOD COAGULATION FACTORS (Fri, 22 Jul 2011)
The present invention relates to the purification of vitamin K-dependent blood coagulation factors, such as Factor IX (FIX). In particular, the invention provides a method for purifying Factor IX having a desired content of gamma-carboxyglutamic acid from a sample comprising a mixture of species of said Factor IX having different contents of gamma-carboxyglutamic acid, said method comprising the steps of: (a) loading said Factor IX sample onto an immunoaffinity chromatography material coupled to a binding moiety for gamma-carboxyglutamic acid; (b) eluting said Factor IX; and (c) selecting a fraction obtained from said elution wherein the polypeptides in the fraction have the desired content of gamma-carboxyglutamic acids; characterised in that the total concentration of Factor IX within said sample exceeds the binding ability of the immunoaffinity chromatography material.
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METHOD FOR FORMING COLLAPSIBLE RESERVOIR (Fri, 15 Jul 2011)
A method for manufacturing a reservoir comprising the steps of (a) providing a generally rigid reservoir member in which a first generally concave cavity with a peripheral portion is formed, (b) providing a generally planar flexible foil member, (c) sealing the rigid reservoir member and the flexible foil member to each other corresponding to the peripheral portion 5 thereby forming a reservoir cavity, and (d) moving the flexible foil member into contact with the first concave cavity to thereby form a second generally concave cavity in the flexible foil member.
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Medical injection device mountable to the skin (Thu, 14 Jul 2011)
A skin-mountable drug delivery device (1) is provided comprising a transcutaneous device unit (2) and a reservoir unit (5). The transcutaneous device unit comprises a transcutaneous device for transporting a fluid through a skin portion of a subject, and a mounting surface adapted for application to the skin of the subject. The reservoir unit comprises a reservoir adapted to contain a fluid drug, the reservoir comprising an outlet means allowing the transcutaneous device to be arranged in fluid communication with an interior of the reservoir, and an expelling assembly for expelling a fluid drug out of the reservoir and through the skin of the subject via the transcutaneous device. The transcutaneous device unit and the reservoir unit further comprise coupling means allowing the reservoir unit to be secured to the transcutaneous device unit in the situation of use. By this arrangement a two-unit system is provided which can be used in a convenient and cost-effective manner.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES (Fri, 08 Jul 2011)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: <?in-line-formulae description="In-line Formulae" end="lead"?>HOOC—(CH2)x—CO—* Chem. 1:<?in-line-formulae description="In-line Formulae" end="tail"?> <?in-line-formulae description="In-line Formulae" end="lead"?>HOOC—C6H4—O—(CH2)y—CO—* Chem. 2:<?in-line-formulae description="In-line Formulae" end="tail"?> <?in-line-formulae description="In-line Formulae" end="lead"?>R1—C6H4—(CH2)z—CO—* Chem. 3:<?in-line-formulae description="In-line Formulae" end="tail"?> <?in-line-formulae description="In-line Formulae" end="lead"?>HOOC—C4SH2—(CH2)w—CO—* Chem. 4:<?in-line-formulae description="In-line Formulae" end="tail"?> in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, R1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *—NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
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Actuator System Comprising Lever Mechanism (Fri, 08 Jul 2011)
The invention provides a pump assembly comprising an actuator lever, a supporting structure, a pump comprising a pump member moveable by actuation of the actuator lever, and an actuator for moving the actuator lever. A first stationary pivoting joint is formed between the actuator lever and the supporting structure, and a second floating pivoting joint is formed between the actuator lever and the pump member allowing the pump member to float relative to the actuator lever, the floating pivoting point providing a constant-length actuator arm defined between the first pivoting joint and the second pivoting joint.
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DOUBLE-ACYLATED GLP-1 DERIVATIVES (Fri, 08 Jul 2011)
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1 (7-37), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1 : HOOC-(CH2)X-CO-* Chem. 2: HOOC-C6H4-O-(CH2)y-CO-* Chem. 3: R1-C6H4-(CH2)Z-CO-* Chem. 4: HOOC-C4SH2-(CH2)W-CO-* in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1 -5, R1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH2)2-(O-(CH2)2)k-O-(CH2)n-CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.
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GLP-1 ANALOGUES AND DERIVATIVES (Fri, 08 Jul 2011)
The invention relates to a GLP-1 analogue which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ I D NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogues and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.
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METHOD OF ACYLATING A PEPTIDE OR PROTEIN (Thu, 07 Jul 2011)
A method for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.
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Vented drug reservoir unit (Fri, 01 Jul 2011)
A reservoir unit is provided comprising a housing in which a reservoir with a transparent portion is arranged, the housing comprising a window allowing a portion of the reservoir to be inspected. The reservoir unit is adapted to be moved from a first “cold” condition to a second “warm” condition with no visible water condensing on the interior surface of the window portion. Further, the vent is adapted to provide pressure equalization between the interior of the housing and the exterior. In this way it is possible to perform visual inspection of the reservoir at all times without being confused by dew or condensed water drops, e.g. when a prefilled reservoir unit containing a drug which requires storage at a given low temperature, as is the case for insulin-containing drugs, is taken out in ambient temperature.
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O-LINKED GLYCOSYLATION OF PEPTIDES (Fri, 01 Jul 2011)

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Pharmaceutical Compositions Comprising GLP-1 Peptides or Extendin-4 and a Basal Insulin Peptide (Fri, 24 Jun 2011)
Pharmaceutical composition for parenteral administration comprising a basal insulin peptide and an insulinotropic GLP-1 peptide comprising at least 6 zinc atoms per 6 insulin molecules.
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DERIVATISED HYBRID PEPTIDES OF AMYLIN AND SALMON CALCITONIN (Fri, 24 Jun 2011)
Described are derivatives of hybrid peptides and pharmaceutical compositions comprising such, wherein said hybrid peptides comprise the C-terminal end of the human amylin peptide sequence, the middle portion of the salmon calcitonin peptide sequence and the N-terminal end of the human amylin peptide sequence, and wherein an albumin binding moiety is attached to the hybrid peptide, optionally via a linker.
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GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS (Fri, 24 Jun 2011)
The invention relates to GLP-1 receptor agonist compounds with a modified N- terminus. The compounds are of the formula Chem. 1: Y-Z-P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y-Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration. The invention also relates to intermediate products for use in the preparation of the GLP-1 receptor agonist compounds of the invention.
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METHOD FOR MAKING MATURE INSULIN POLYPEPTIDES (Thu, 23 Jun 2011)
The invention is related to a method for making human insulin analogues by culturing an fungi cell comprising a DNA vector encoding a precursor for human insulin analogue , wherein the said precursor comprises a connecting peptide flanked with cleavage sites at both junctions with the A- and the B-chain of the insulin peptide, respectively said cleavage sites being cleaved within the fungi cell allowing the cell to secrete high amount of correctly processed, mature two chain human insulin analogue to the culture media.
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Spontaneously Dispersible Preconcentrates Including a Peptide Drug in a Solid or Semisolid Carrier (Fri, 17 Jun 2011)
The present invention relates to a solid or semi-solid pharmaceutical composition that includes a polypeptide drug, at least one polar organic solvent, at least one surfactant, at least one hydrophilic component and which composition is spontaneously dispersible.
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Protein conjugates and methods for their preparation (Fri, 17 Jun 2011)
Reductive amination of peptide-derived aldehydes with anilines or heteroarylamines containing a property-modifying group provides new, hydrolytically stable protein conjugates, suitable for therapy.
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HYPERGLYCOSYLATED HUMAN COAGULATION FACTOR IX (Fri, 10 Jun 2011)
The invention relates to hyperglycosylated human coagulation factor IX polypeptides, to processes for preparing said polypeptides, to pharmaceutical compositions comprising said polypeptides and to the use of the compounds for the treatment of diseases alleviated by human coagulation factor IX, in particular, but not exclusively hemophilia.
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Medical Skin Mountable Device (Fri, 10 Jun 2011)
A medical device is provided comprising a transcutaneous device unit and a reservoir unit. The transcutaneous device unit comprises a transcutaneous device for transporting a fluid through a skin portion of a subject, and a mounting surface adapted for application to the skin of the subject. The reservoir unit comprises a reservoir adapted to contain a fluid drug, the reservoir comprising an outlet means allowing the transcutaneous device to be arranged in fluid communication with an interior of the reservoir, and an expelling assembly for expelling a fluid drug out of the reservoir and through the skin of the subject via the transcutaneous device. The transcutaneous device unit and the reservoir unit further comprise coupling means allowing the reservoir unit to be secured to the transcutaneous device unit in the situation of use. By this arrangement a two-unit system is provided which can be used in a convenient and cost-effective manner.
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NOVEL PEPTIDYL ALPHA-HYDROXYGLYCINE ALPHA-AMIDATING LYASES (Fri, 10 Jun 2011)
The present patent application concerns an enzyme capable of catalysing the conversion of a α-hydroxyglycine to an α-amide and the use of such enzymes for producing a C-terminal α-amidated peptide.
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Protracted exendin-4 compounds (Thu, 09 Jun 2011)
Novel protracted exendin-4 compounds and therapeutic uses thereof.
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METHOD OF PURIFYING PEGYLATED PROTEINS (Sat, 04 Jun 2011)
The invention relates to a method of purifying PEGylated proteins by removing impurities from samples containing PEGylated proteins, in particular, but not exclusively vitamin K-dependent blood coagulation factors such as Factor IX (FIX), to proteins purified by said method and to the use of said purified proteins in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.
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METHOD FOR MAKING POLYPEPTIDES (Sat, 04 Jun 2011)
The invention provides an improved method for producing polypeptides with a C-terminal glycine in a yeast transformant being characterized in having a non functional KEX1 gene. The method is in particular well suited to produce polypeptides with an aromatic amino acid residue attached to the C-terminal glycine. The yeast strain may have further non-functional protease genes selected from PEP4, YPS1, MKCl, YPS3, YPS5, YPS6, YPS7, PRB1, STE13 and KEX2.
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HETEROAROMATIC GLUCOKINASE ACTIVATORS (Fri, 03 Jun 2011)
The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.
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Insulin and IGF-1 Receptor Agonists and Antagonists (Fri, 27 May 2011)
Peptide sequences capable of binding to insulin and/or insulin-like growth factor receptors with either agonist or antagonist activity and identified from various peptide libraries are disclosed. This invention also identifies at least two different binding sites, which are present on insulin and insulin-like growth factor receptors, and which selectively bind the peptides of this invention. As agonists, certain of the peptides of this invention may be useful for development as therapeutics to supplement or replace endogenous peptide hormones. The antagonists may also be developed as therapeutics.
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N-GLYCOSYLATED HUMAN GROWTH HORMONE WITH PROLONGED CIRCULATORY HALF-LIFE (Fri, 20 May 2011)
The present invention relates to novel human growth hormone (hGH) variant(s) with one or more N-glycans. The hGH variants of the invention comprises an amino acid sequence which includes at least one N-glycosylation motif (N-X-S/T) arising from one or more mutations not present in the wild type hGH. The hGH variants of the invention have a prolonged circulatory half-life and thus can be effectively used as a protein therapeutic for disease states that will benefit from increased levels of hGH. The process of obtaining the hGH variants is also encompassed by the invention.
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LONG-ACTING Y2 RECEPTOR AGONISTS (Fri, 20 May 2011)
The present invention relates to PYY derivatives comprising a serum albumin binding side chain, wherein said derivative has a half-life of at least 7 hours as determined by Assay (IV) described herein as well as compositions comprising said derivative and its use in therapy.
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Acylated GLP-1 compounds (Thu, 19 May 2011)
Protracted GLP-1 compounds and therapeutic uses thereof.
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Compositions and methods for treating proliferative disorders (Thu, 19 May 2011)
The present invention relates to methods of treating proliferative disorders, particularly immunoproliferative and autoimmune disorders, and methods of producing antibodies which bind NK cell receptors for use in therapeutic strategies for treating such disorders, particularly to deplete cells involved in the immunoproliferative pathology.
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Remodelling and glycoconjugation of Granulocyte Colony Stimulating Factor (G-CSF) (Thu, 19 May 2011)
The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group a peptide.
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Method for Making Mature Insulin Polypeptides (Fri, 13 May 2011)
The invention is related to a method for making human insulin analogues by culturing an fungi cell comprising a DNA vector encoding a precursor for human insulin analogue, wherein the said precursor comprises a connecting peptide flanked with cleavage sites at both junctions with the A- and the B-chain of the insulin peptide, respectively said cleavage sites being cleaved within the fungi cell allowing the cell to secrete high amount of correctly processed, mature two chain human insulin analogue to the culture media.
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LOW VISCOSITY COMPOSITIONS COMPRISING A PEGYLATED GLA-DOMAIN CONTAINING PROTEIN (Fri, 13 May 2011)
The present invention relates to a method for lowering the viscosity of compositions comprising Vitamin K-dependent proteins.
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FORMULATIONS OF PEG-FUNCTIONALISED SERINE PROTEASES WITH HIGH CONCENTRATIONS OF AN AROMATIC PRESERVATIVE (Fri, 06 May 2011)
The invention relates to a liquid, aqueous pharmaceutical composition comprising a Factor VII polypeptide (i) functionalised with one or more polyethylene glycol (PEG) moieties, said PEG moieties having a molecular weight of at least 300 Da; a buffering agent (ii) suitable for keeping pH in the range of from about 5.0 to about 9.0; and at least one aromatic preservative (iii) in a concentration of at least 0.1 mg/mL.
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Amylin Derivatives (Fri, 06 May 2011)
The present invention relates to novel amylin derivatives, pharmaceutical compositions containing such derivatives and to methods of treating diabetes and hyperglycaemia using the amylin derivatives of the invention.
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PHARMACEUTICAL SOLUTION OF NON COVALENTLY BOUND ALBUMIN AND ACYLATED INSULIN (Fri, 06 May 2011)
If albumin is added to a pharmaceutical formulation containing acylated insulin described in WO 2009/022005 and WO 2009/022013, the acylated insulin can be kept in solution after subcutaneous injection.
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DERIVATIVES OF CGRP (Fri, 06 May 2011)
Acylated CGRP compounds with a linker have prolonged action and are valuable as medicaments.
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Counteracting drug-induced obesity using GLP-1 agonists (Thu, 05 May 2011)

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Human coagulation factor VII polypeptides (Thu, 05 May 2011)

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Novel peptides for use in the treatment of obesity (Fri, 29 Apr 2011)
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
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Insulin Analogues with an Acyl and Alkylene Glycol Moiety (Fri, 29 Apr 2011)
An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.
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INSULINS WITH AN ACYL MOIETY COMPRISING REPEATING UNITS OF ALKYLENE GLYCOL CONTAINING AMINO ACIDS (Fri, 29 Apr 2011)
Acylated insulins wherein an acyl moiety is attached to the parent insulin and wherein said acyl moiety comprises repeating units of alkylene glycol containing amino acids and wherein there is only one lysine residue (K & Lys) in the parent insulin have satisfactory properties when administered pulmonary.
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INJECTION DEVICE HAVING MODE DEFINING ELEMENTS (Fri, 29 Apr 2011)
An injection device (1) for injecting predetermined doses of liquid drug is disclosed. The injection device (1) comprises a dose setting mechanism and an injection mechanism. A torsion spring (12) is connected to the dose setting mechanism and to the injection mechanism in such a manner that energy is stored in the torsion spring (12) during dose setting, and the energy is released during injection, the stored energy being used for causing the set dose to be injected. A first mode defining element (8) and a second mode defining element (9) are angularly movable relative to each other in response to operation of the dose setting mechanism. They are also axially movable relative to each other between a first position in which the dose setting mechanism can be operated to set a dose and a second position in which the injection mechanism can be operated to inject a set dose. The mode defining elements (8, 9) are shaped in such a manner that mutual axial movements between the first position and the second position are only possible at a limited number of mutual angular positions, said angular positions each corresponding to setting of a predetermined dose of liquid drug. Thereby the risk of setting and/or injecting an incorrect dose is considerably reduced. Furthermore, the torsion spring (12) ensures easy operability for persons having poor dexterity or low finger strength.
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Anti-human interleukin-20 antibodies (Fri, 22 Apr 2011)
Anti-human IL20 monoclonal antibodies that can reduce IL20 mediated activation of both IL20R1/IL20R2 and IL22R1/IL20R2 receptor complexes in one or more species, including humans, are described, as well as antigen-binding molecules such as, e.g., antigen-binding antibody fragments, antibody derivatives, and multi-specific molecules designed or derived from such antibodies, and methods or producing such antibodies or other antigen-binding molecules. Such antibodies or other antigen-binding molecules can be used for treating various diseases and disorders, including autoimmune or inflammatory diseases or disorders.
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PROTEASE-STABILIZED INSULIN ANALOGUES (Fri, 22 Apr 2011)
The present invention relates to novel insulin analogues comprising mutations at position A14 in the A chain and at positions B27, B28, B29 and B30 in the B chain and exhibiting resistance towards protease; a method for the preparation of such insulin analogues; insulin preparations containing the insulin analogues of the invention; and, a method of treating diabetes mellitus using these insulin analogues.
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Stabilised compositions of factor VII polypeptides (Thu, 21 Apr 2011)
The invention relates to chemically as well as physically stable kits and compositions comprising polypeptides, in particular Factor VII or Factor VII-related polypeptides, such that these compositions can be stored, handled and used at room temperature.
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Factor VII glycoforms (Thu, 21 Apr 2011)
The present invention relates to compositions comprising Factor VII and other blood clotting factors having altered patterns of asparagine-linked glycosylation.
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Method for the Production of Proteins (Fri, 08 Apr 2011)
The present invention relates to a process for the purification of a protease.
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GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE (Fri, 08 Apr 2011)
The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.
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Amide derivatives useful as glucokinase activators (Thu, 07 Apr 2011)
This invention relates to acetamide derivatives of the general formula (II) which are activators of glucokinase (GK), and which may be useful for the management, treatment, control, or adjunct treatment of diseases or conditions, where increasing glucokinase activity is beneficial, for example diseases such as IGT, Syndrome X, type 2 diabetes, type 1 diabetes, dyslipidemia, hyperlipidemia, hypertension, and obesity.
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Urea Glucokinase Activators (Fri, 01 Apr 2011)
The invention provides a compound of general formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.80mm" wi="50.29mm" file="US20110077234A1-20110331-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
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REMODELING AND GLYCOCONJUGATION OF PEPTIDES (Fri, 01 Apr 2011)

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HUMAN COAGULATION FACTOR VII VARIANTS, METHOD FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM (Fri, 01 Apr 2011)

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High moisture barrier container for medical liquid compositions (Thu, 31 Mar 2011)
A container consisting of at least two layers, the inner layer consisting of a PE or PP film and the PCTFE layer consisting of a PCTFE film, and the thickness of the PCTFE layer being about 40-100 µm, which container is equipped with a device where the liquid can be lead out through when desired and which container is transparent, shows superior properties for storing liquid pharmaceutical compositions, especially insulin compositions containing preservatives.
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Processing enzymes fused to basic protein tags (Fri, 25 Mar 2011)
The invention is related to processing enzyme comprising an N-terminally attached tag derived from highly basic proteins from thermophilic bacteria. The processing enzymes are useful for modifying proteins. They can be produced in high yields and can be effectively separated from the modified protein after use.
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STABLE NON-AQUEOUS LIQUID PHARMACEUTICAL COMPOSITIONS COMPRISING AN INSULIN (Fri, 25 Mar 2011)
The invention describes a non-aqueous liquid pharmaceutical composition comprising at least one lipid and at least one insulin. Also described is a method of producing a pharmaceutical composition comprising a lipid and a method of purifying a lipid, a cosolvent, a surfactant or a pharmaceutical composition comprising a lipid.
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LONG-ACTING Y2 RECEPTOR AGONISTS (Fri, 25 Mar 2011)
The present invention relates to PYY analogues or derivatives thereof comprising at least one alteration selected from the group consisting of substitutions, insertions, deletions and modifications and optionally a serum albumin binding side chain comprising an alkyl chain with at least 14 carbon atoms. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y2 receptor modulation.
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DRUG DELIVERY SYSTEM AND DEVICE WITH CAP FUNCTION (Fri, 25 Mar 2011)
A system comprising first and second drug delivery devices (1) based on the same technology platform, each comprising a main portion (3) with a reservoir holding a type of drug, a drug outlet, and drug expelling means for expelling drug from the reservoir through the drug outlet, as well as a cap (100) releasably mountable to the main portion to enclose the drug outlet, each cap comprising a unique user-identifiable marking indicating the corresponding type of drug. The cap and main portion of each drug delivery device comprise a pair of corresponding key structures preventing the first cap from being mounted on the second main portion, and the second cap from being mounted on the first main portion.
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A METHOD FOR CHEMICAL ETCHING OF A NEEDLE CANNULA (Fri, 25 Mar 2011)
A regular metallic, cylindrical tubular needle cannula (1) is subjected to a metal etching liquid (21) in the inside lumen (4) thereby increasing the inside diameter and enhancing the flow properties while maintaining the outside appearance. The inside diameter is only increased over a controlled length (7) of the full length of the needle cannula (1) leaving sufficient length and wall thickness to also taper the outside diameter.
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Stabilised compositions of factor VII polypeptides (Thu, 24 Mar 2011)
The invention relates to chemically as well as physically stable kits and compositions comprising polypeptides, in particular Factor VII or Factor VII-related polypeptides, such that these compositions can be stored, handled and used at room temperature.
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Regulation of food preference using GLP-1 agonists (Thu, 24 Mar 2011)

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HYDROPHOBIC INTERACTION CHROMATOGRAPHY PURIFICATION OF FACTOR VII POLYPEPTIDES (Fri, 18 Mar 2011)
The invention described herein provides new methods of preparing purified Factor VII polypeptide drug substances in large quantities (industrial scale levels) that are associated with reduced content of product-related impurities (e.g., late eluting peaks) and/or that exhibit a relatively uniform glycosylation pattern.
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DERIVATISED HYBRID PEPTIDES OF AMYLIN AND SALMON CALCITONIN (Thu, 17 Mar 2011)
Described are derivatives of hybrid peptides and pharmaceutical compositions comprising such, wherein said hybrid peptides comprise the C-terminal end of the human amylin peptide sequence, the middle portion of the salmon calcitonin peptide sequence and the N-terminal end of the human amylin peptide sequence, and wherein an albumin binding moiety is attached to the hybrid peptide, optionally via a linker.
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An appetite-suppressing peptide, its compositions and use (Thu, 17 Mar 2011)
Appetite-suppressing peptide or an appetite-suppressing peptide-containing fraction for the treatment of obesity or type II diabetes.
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Heteroaryl-ureas and their use as glucokinase activators (Fri, 11 Mar 2011)
This invention relates to compounds of formula (I) <chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.80mm" wi="50.21mm" file="US08263634-20120911-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. 
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INTEGRATED PACKAGE (Fri, 11 Mar 2011)
The present invention generally relates to skin-mountable devices. A device in accordance with the invention comprises a first skin-mountable unit having a mounting surface comprising adhesive means for adhering the unit to the skin of a subject, and a second handling unit releasably attached to the skin-mountable unit. The handling unit comprises an interior space at least partially accommodating the skin-mountable unit and has an opening through which the skin-mountable member can be moved when detached from the handling unit, the handling unit having a portion surrounding the opening. The device further comprises a seal member releasably attached to the circumferential portion, thereby providing a closed space for the skin-mountable unit. In this way a device is provided allowing for easy handling as a user can use the handling unit to grip and handle the combined device during operation thereof, just as the second unit can be designed and optimized for ease of use during manipulation of the skin-mountable unit.
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Polypeptide protracting tags comprising a tetrazole moiety (Thu, 10 Mar 2011)
Method for increasing half-life of compounds in plasma and novel derivatives of such compounds.
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Novel insulin derivatives (Thu, 10 Mar 2011)
The present invention is related to insulin derivatives having a side chain attached either to the ±-amino group of the N-terminal amino acid residue of B chain or to an µ-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethylenglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from -NH 2 and -COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.
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Stabilized pharmaceutical peptide compositions (Thu, 10 Mar 2011)
Method for increasing the shelf-life of a pharmaceutical composition for parenteral administration comprising a glucagon-like peptide which is prepared from a peptide product that has been subjected to treatment at a pH above neutral pH.
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Stabilized pharmaceutical peptide compositions (Thu, 10 Mar 2011)
Method for increasing the shelf-life of a pharmaceutical composition comprising a glucagon-like peptide which is prepared from a peptide product that has been dried at a pH above neutral pH.
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GLP-1 Derivatives II (Fri, 04 Mar 2011)
The present invention relates to a derivative of GLP-1(7-C), wherein C is 35 or 36 which derivative has just one lipophilic substituent which is attached to the C-terminal amino acid residue.
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TARGETING TISSUE FACTOR TO ACTIVATED PLATELETS (Fri, 04 Mar 2011)
The current invention relates to procoagulant fusion proteins, polynucleotides that encode said fusion proteins and cells that expresses said fusion proteins. Furthermore, the current invention relates to fusion proteins for use as a medicament. Individuals that have a coagulopathy, such as haemophilia A and B with or without inhibitors, may be treated with fusions proteins of the current invention.
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Polypeptide protracting tags comprising a tetrazole moiety (Thu, 03 Mar 2011)
Method for increasing half-life of compounds in plasma and novel derivatives of such compounds.
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Soluble, stable insulin-containing formulations with a protamine salt (Fri, 25 Feb 2011)
The present invention relates to pharmaceutical formulations comprising insulin, an insulin analog, an insulin derivative, or a combination of any of the foregoing, and a salt of protamine, to methods of preparing such formulations, and to uses of such formulations in the treatment of diseases and conditions for which use of the insulin peptide(s) contained in such formulations is indicated. The present invention further relates to methods for increasing the stability and/or solubility of insulin in insulin-containing formulations at a pH less than 7.0 by adding a salt of protamine to the insulin-containing formulations.
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INJECTION DEVICE FOR PERFORMING MEDICAL INJECTIONS (Fri, 25 Feb 2011)
The present invention concerns a prefilled injection device having a container and a dose setting mechanism encapsulated inside the housing. The injection device incorporates an axial variable connection such that the distance between the distal end of the piston rod means and the plunger is minimized preferably to zero.
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Medical Delivery System Comprising Locking Ring with L-Shaped Grooves (Fri, 25 Feb 2011)
A medical delivery system (100) comprising a container (102) which is adapted to be fastened to a dosing assembly (104). One of the container and the dosing assembly comprises a rotatable element (106) adapted to cooperate with the other one of the container and the dosing assembly, so as to lock/fasten the container to the dosing assembly. Furthermore, the present application relates to a container and a dosing assembly for use in the medical delivery system.
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INSULIN ALBUMIN CONJUGATES (Fri, 18 Feb 2011)
Insulin albumin conjugates consisting of an insulin analogue, a bifunctional linker and albumin can efficiently be used to treat diabetic patients.
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Covalent Factor VII-Tissue Factor Complex (Fri, 18 Feb 2011)
The present invention relates to novel covalent complexes of a Factor VII polypeptide and a Tissue Factor polypeptide, in particular to such complexes which are functionally active and which have an enhanced proteolytic activity towards Factor X compared to the corresponding free Factor VII polypeptide as well as methods for production of these novel complexes.
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METHOD OF PURIFYING PEGYLATED PROTEINS (Fri, 18 Feb 2011)
The invention relates to a method of purifying PEGylated proteins ( which comprises anion exchange chromatography with an elution buffer comprising MgC12), in particular, but not exclusively vitamin K-dependent blood coagulation factors such as Factor VII (FVII), to proteins purified by said method and to the use of said purified proteins in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.
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PROCESS (Thu, 17 Feb 2011)
A process for performing a ring closure on a fully protected peptide to form a protected cyclic peptide comprising the steps of: i) selectively deprotecting the connectable portions of the ring to be closed; ii) connecting the deprotected connectable portions of step i) to form the protected cyclic peptide.
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Stabilised solid compositions of factor VII polypeptides (Thu, 17 Feb 2011)
The invention relates to chemically as well as physically stable compositions comprising Factor VII or a Factor VII-related polypeptide such that these compositions can be stored, handled and used at room temperature.
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GROWTH HORMONES WITH PROLONGED IN-VIVO EFFICACY (Fri, 11 Feb 2011)
The present invention relates to polypeptide compound optimized for subcutaneous administration, exemplified by growth hormone conjugates having a linker providing non-covalent binding to albumin.
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PURIFICATION OF PEPTIDES PREPARED BY SOLID PHASE SYNTHESIS (Thu, 10 Feb 2011)
The invention relates to an effective process for purifying a peptide which has been prepared by solid phase peptide synthesis. Also encompassed by the invention is a kit comprising reagents for said process and the purified peptide obtained by said process.
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Use of GLP-1 Peptides (Fri, 04 Feb 2011)
GLP-1(1-45) or a fragment or an analogue thereof can be used in the preparation of a medicament for peripheral administration in the suppression of appetite or induction of satiety.
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LONG-ACTING Y2 AND/OR Y4 RECEPTOR AGONISTS (Thu, 03 Feb 2011)
The present invention relates to a PYY or PP peptide derivative or analogue thereof derivatised with one or more serum albumin binding side chains comprising a dis-tal tetrazole or carboxylic acid group. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y receptor modulation.
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Remodeling and glycoconjugation of peptides (Thu, 03 Feb 2011)
The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group a peptide.
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Use of the extracellular marker DNER for identification and selection of specific pancreatic cells (Fri, 28 Jan 2011)
The invention relates to a method of identifying and obtaining cells that have the potential to differentiate into pancreatic cells, having the step of contacting a cell population containing endocrine pre-progenitor cells, endocrine progenitor cells, early endocrine cells, and/or fully differentiated endocrine cells with a DNER binding agent; as well as isolating and/or expanding cells obtained by the method and compositions thereof.
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DDR1-Mediated Cell Purification of Pancreatic Endocrine Cells Through Their Progenitors (Fri, 21 Jan 2011)
The invention relates to a method of identifying, obtaining and/or quantifying a culture of pancreatic cells selected from the group consisting of ductal/endocrine progenitor cells, endocrine progenitor cells, early endocrine cells, and fully differentiated endocrine cells. Also contemplated is a method of expanding the numbers of such cells as well as sorting such cells. The invention further relates to a selective cell surface marker, DDR1, that permits the selection of a unique subset of cells with pancreatic endocrine progenitor phenotype. Furthermore, the invention relates to isolated cells selected from such cells and compositions thereof.
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Novel NIDDM Regimen (Fri, 21 Jan 2011)
The present invention relates to the use of a short-acting oral hypoglycemic agent and to a novel regimen in the treatment of type 2 diabetes in which the endogenous secretion of insulin is stimulated in connection with meals by administering in connection with the meals a short-acting oral hypoglycaemic agent. Also, the present invention relates to a method of achieving significantly improvement in the glycaemic control by a combined use of repaglinide and metformin in NIDDM patients poorly controlled on metformin alone.
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Nanofiltration of factor VII solutions to remove virus (Thu, 20 Jan 2011)
The present invention relates to a novel method for improving the viral safety of liquid Factor VII compositions, in particular those comprising active Factor VII polypeptides (a Factor VIIa polypeptide).
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Novel insulin derivatives (Thu, 20 Jan 2011)
The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have a side chain attached either to the ±-amino group of the N-terminal amino acid residue of the B chain or to the µ-amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula: -W-X-Y-Z wherein W, X, Y and Z are as defined in the disclosure.
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Non-Porous Material as Sterilization Barrier (Fri, 14 Jan 2011)
The invention provides a device comprising a sealed interior portion with at least one opening covered by a sterilization barrier formed from a non-porous material allowing a sterilization gas to penetrate but prevents germs from penetrating. The size and configuration of the at least one sterilization barrier formed from a non-porous material are adapted to allow at least 50% of the sterilization gas, that would pass between a sterilization gas-containing exterior and the sealed interior portion when a pressure difference is created there between, to pass through the non-porous material.
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Single-Chain Insulin Analogues and Pharmaceutical Formulations Thereof (Fri, 14 Jan 2011)
The present invention is related to fast acting single-chain insulin comprising a modified B-chain and the A-chain of human insulin or an analogue thereof connected by a connecting peptide wherein one or more of the amino acid residues in position B25, B26 or B27 in the human B-chain are Glu or Asp or are deleted and/or B28 is Glu, Asp, Lys or is deleted, and the amino acid residue in position B10 in the human insulin B-chain is Gln, Ala, Val, Thr or Ser. The invention is also related to pharmaceutical compositions being a mixture of the rapid acting single-chain insulin and the protracted acylated insulin.
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Reduction of Dimer Content in Factor VII Polypeptide Compositions by Heat Treatment (Fri, 07 Jan 2011)
The present application relates to a method of reducing the content of dimers in Factor VII polypeptide composition by heat treatment.
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New Blood Coagulation Factor Inhibitors (Fri, 07 Jan 2011)
The invention relates to novel compounds with formula (I) X1-X2-X3-X4-X5-(X6)n-(X7)m-Y useful as blood coagulation factor inhibitors. The compounds (I) may be used for treatment of thrombotic conditions or as stabilizers of liquid formulations of blood coagulation factors, in particular liquid formulations of FVIIa, Factor VII variants, or Factor VII derivatives.
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Glycopegylated Erythropoietin Formulations (Fri, 07 Jan 2011)
The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.
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INSULIN DERIVATIVES (Fri, 07 Jan 2011)
The novel insulin derivates delivers, after administration to humans, insulin as a function of the glucose concentration in the tissue.
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GLYCOPEGYLATED FACTOR IX (Fri, 31 Dec 2010)
The present invention provides conjugates between Factor IX and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.
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ONE POT DESIALYLATION AND GLYCOPEGYLATION OF THERAPEUTIC PEPTIDES (Fri, 31 Dec 2010)
The present invention provides conjugates between peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention.
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PREPARATION COMPRISING INSULIN, NICOTINAMIDE AND AN AMINO ACID (Thu, 30 Dec 2010)
Insulin preparations comprising an insulin compound or a mixture of two or more insulin compounds, a nicotinic compound and an amino acid.
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IN VITRO MODIFICATION OF GLYCOSYLATION PATTERNS OF RECOMBINANT GLYCOPEPTIDES (Fri, 24 Dec 2010)
This invention provides methods for modifying glycosylation patterns of glycopeptides, including recombinantly produced glycopeptides. Also provided are glycopeptide compositions in which the glycopeptides have a uniform glycosylation pattern.
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Injection Device (Fri, 24 Dec 2010)
An injection device with a travelling clutch which can be shifted between two different positions by the activation of an injection button. In the first position, the injection button and the driver is allowed to rotate relatively to the piston rod, which is blocked from rotation by the clicker element. In the second position, the drive sleeve and the injection button is axially movable while the piston rod is allowed to rotate.
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Medical delivery system comprising a container and a dosing assembly with radially moving fastening means (Fri, 24 Dec 2010)
A medical delivery system wherein one of a container and a dosing assembly comprises a first fastening means (116) and the other one of the container and the dosing assembly comprises a second fastening means (114); and wherein the second fastening means is adapted to move at least a part of the first fastening means in a radial direction upon rotation of the container in a first rotational direction relative to the dosing assembly, whereby the first and second fastening means engage such that the container and the dosing assembly are locked for relative translational movement. A container and a dosing assembly for use in the medical delivery system.
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IL-21 derivatives (Thu, 23 Dec 2010)
There is provided a derivative of human Interleukin 21 (IL-21) comprising: (a) a human IL-21 polypeptide comprising: (i) amino acids residues 30 to 102 of SEQ ID NO:2 or (ii) amino acid residues 32 to 162 of SEQ ID NO:2; and (b) at least one lipophilic substituent, wherein the lipophilic substituent is at the IL-21 polypeptide N-terminus or C-terminus.
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Novel insulin derivatives (Thu, 23 Dec 2010)
The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have a side chain attached either to the ±-amino group of the N-terminal amino acid residue of the B chain or to the µ-amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula: -W-X-Y-Z wherein W, X, Y and Z are as defined in the disclosure.
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Novel Insulin Derivatives (Thu, 23 Dec 2010)
The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have a side chain attached either to the ±-amino group of the N-terminal amino acid residue of the B chain or to the µ-amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula: -W-X-Y-Z wherein W, X, Y and Z are as defined in the disclosure.
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SEMI-RECOMBINANT PREPARATION OF GLP-1 ANALOGUES (Fri, 17 Dec 2010)
A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.
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Injection device with rotatable dose setting (Fri, 17 Dec 2010)
An injection device comprising a housing and a dose setting mechanism including a dose setting element. Contrary to prior art injection devices, the dose setting element can only be set at a few different dose settings. This is established by forming the dose setting element as a rotatable dish concealed within the housing and having a number of projections projecting outside the boundaries of the housing through a slot in the housing. A dose is set by activating a projection which in addition provides the user with a tactile guidance. Usually one projection is provided for one dose setting limiting the number of doses to be set to the number of projections.
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A METHOD FOR MANUFACTURING A NEEDLE CANNULA HAVING IMPROVED FLOW PROPERTIES (Fri, 17 Dec 2010)
A method of manufacturing a needle cannula (1) by applying electro polishing to the inside lumen (4) of the needle cannula (1). A cathode (10) is inserted into the lumen (4) of the needle cannula (1) and an electric current (21) is introduced between the cathode (10) and the needle cannula (1) which works as the anode. A liquid acid (31) is preferably flushed into the inside lumen (4) of the needle cannula (1) during the process.
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GLP-1 AND FGF21 COMBINATIONS FOR TREATMENT OF DIABETES TYPE 2 (Fri, 17 Dec 2010)
The invention relates to the use of a Fibroblast Growth Factor 21 (FGF21 ) compound and a Glucagon-Like Peptide 1 (GLP-1 ) compound in combination for the preparation of a medicament for the treatment of diabetes, more in particular type 2 diabetes, as well as pharmaceutical compositions comprising certain FGF21 and GLP-1 compounds in combination, together with a pharmaceutically acceptable carrier. The combination has a significant effect on parameters of relevance for diabetes type 2, viz. on the viability of beta cells ex vivo in the presence of free fatty acids, on caspase activity of beta cells ex vivo (a measure of cell apoptosis), and a blood glucose lowering effect on db/db mice in vivo.
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DRUG DELIVERY DEVICE WITH CAP FUNCTIONS FOR INSPECTION (Fri, 17 Dec 2010)
A drug delivery device is provided comprising a main portion with a drug reservoir, and mounting means adapted for mounting a needle assembly distally relative to the drug reservoir. A cap portion is releasably mountable to the main portion and comprises a proximal portion adapted to cover the reservoir, and a distal portion adapted to cover the space distally of the reservoir adapted to house a needle assembly mounted on the main portion. The cap is provided with one or more inspection openings allowing a user to inspect the distal space, this allowing a user to inspect at least a portion of a needle assembly mounted on the main portion when the cap portion is mounted on the main portion.
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DRUG DELIVERY DEVICE WITH CAP FUNCTIONS FOR NEEDLE ASSEMBLY (Fri, 17 Dec 2010)
Drug delivery system comprising a main portion with a cap as well as a needle assembly with a needle mounted in a hub and a needle cap releasably mountable on the hub to cover the needle. The cap comprises gripping means reversibly operatable between a first condition in which there is no gripping engagement between the mounted cap portion and the needle cap, this allowing the cap portion to be removed from the main portion without removing the needle cap from the hub, and a second condition in which the cap portion grippingly can engage the needle cap of a needle assembly, this allowing the needle cap to be removed from the hub together with the cap. The cap further comprises user actuation means for operating the gripping means between the two conditions.
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Factor VII Glycoforms (Thu, 16 Dec 2010)
The present invention relates to compositions comprising Factor VII and other blood clotting factors having altered patterns of asparagines-linked glycosylation.
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LONG-ACTING Y2 AND/OR Y4 RECEPTOR AGONISTS (Wed, 15 Dec 2010)
The present invention relates to a PYY or PP peptide derivative or analogue thereof derivatised with one or more serum albumin binding side chains comprising a dis-tal tetrazole or carboxylic acid group. Moreover, the invention relates to compositions hereof and methods of treatment of conditions responsive to Y receptor modulation.
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Use of GLP-1 compound for treatment of critically ill patients (Fri, 10 Dec 2010)
Use of medicament for life saving treatment of critically ill patients and method of treatment. The medicament comprises a GLP-1 compound which effectively controls the blood glucose level.
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Novel GLP-1 Derivatives (Fri, 03 Dec 2010)
Novel polypeptide derivatives having protracted profile of action.
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Stabilisation of Liquid-Formulated Factor VII(A) Polypeptides by Aldehyde-Containing Compounds (Fri, 03 Dec 2010)
The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilising agent (iii) comprising a R—CHO motif, e.g. Benzaldehyde, 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, or 5-formyl-4-methylimidazole.
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Novel insulin derivatives (Thu, 02 Dec 2010)
The present invention relates to insulin derivatives having a side chain attached either to the ±-amino group of the N-terminal amino acid residue of the B chain or to the µ-amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.
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Insulin derivatives (Thu, 02 Dec 2010)
The present invention is related to insulin derivatives having a side chain attached to an µ-amino group of a Lys residue present in the A-chain or to an µ -amino group of a Lys residue in the B-chain.
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High Concentration Factor VII Polypeptide Formulations Comprising an Aromatic Preservative and an Antioxidant (Fri, 26 Nov 2010)
The present invention relates to pharmaceutical compositions comprising at least 10 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 5.0 to about 9.0; at least one aromatic preservative (iii) in a concentration of at least 0.1 mg/mL; and at least one antioxidant (iv) in a concentration of at least 0.1 mg/mL; the composition optionally comprising further components, with the proviso that none of such further components are Factor VII polypeptide stabilizing agents selected from (a) metal-containing agents, wherein said metal is selected from the group consisting of first transition series metals of oxidation state +II, except zinc; and (b) stabilising agent comprising a —C(═N—Z1-R1)-NH—Z2-R2 motif.
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Pharmaceutically Active Insulin Receptor-Modulating Molecules (Fri, 26 Nov 2010)
The invention described herein provides novel pharmaceutically active molecules (including novel peptide derivatives and peptides) that bind to an insulin receptor; compositions comprising such molecules; methods of modulating insulin receptor activity comprising the delivery of such molecules and related insulin-binding molecules (e.g., in the context of treating and/or preventing insulin receptor-related diseases such as diabetes); nucleic acids encoding such peptides; vectors and host cells comprising such nucleic acids; and methods of producing such molecules and compositions.
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Human coagulation factor VII variants (Thu, 25 Nov 2010)
The present invention relates to novel human coagulation Factor VIIa variants having coagulant activity as well as nucleic acid constructs encoding such variants, vectors and host cells comprising and expressing the nucleic acid, pharmaceutical compositions, uses and methods of treatment.
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Compositions and Methods for Regulating NK Cell Activity (Fri, 19 Nov 2010)
The present invention relates to novel compositions and methods for regulating an immune response in a subject. More particularly, the invention relates to specific antibodies that regulate the activity of NK cells and allow a potentiation of NK cell cytotoxicity in mammalian subjects. The invention also relates to fragments and derivatives of such antibodies, as well as pharmaceutical compositions comprising the same and their uses, particularly in therapy, to increase NK cell activity or cytotoxicity in subjects.
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TRUNCATED GLP-1 DERIVATIES AND THEIR THERAPEUTICAL USE (Fri, 19 Nov 2010)
The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.
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Novel Prolactin Compounds (Fri, 19 Nov 2010)
The present invention relates to prolactin analogues, which analogues have increased resistance to deamidation.
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INJECTION DEVICE HAVING MODE DEFINING ELEMENTS (Thu, 18 Nov 2010)
An injection device (1) for injecting predetermined doses of liquid drug is disclosed. The injection device (1) comprises a dose setting mechanism and an injection mechanism. A torsion spring (12) is connected to the dose setting mechanism and to the injection mechanism in such a manner that energy is stored in the torsion spring (12) during dose setting, and the energy is released during injection, the stored energy being used for causing the set dose to be injected. A first mode defining element (8) and a second mode defining element (9) are angularly movable relative to each other in response to operation of the dose setting mechanism. They are also axially movable relative to each other between a first position in which the dose setting mechanism can be operated to set a dose and a second position in which the injection mechanism can be operated to inject a set dose. The mode defining elements (8, 9) are shaped in such a manner that mutual axial movements between the first position and the second position are only possible at a limited number of mutual angular positions, said angular positions each corresponding to setting of a predetermined dose of liquid drug. Thereby the risk of setting and/or injecting an incorrect dose is considerably reduced. Furthermore, the torsion spring (12) ensures easy operability for persons having poor dexterity or low finger strength.
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STABLE PHARMACEUTICAL COMPOSITIONS OF PEPTIDE DERIVATIZED USING AN OXIME LINKER (Fri, 12 Nov 2010)
The invention relates to stable pharmaceutical compositions comprising a therapeutic peptide derivatized with a property-modifying group, wherein the property-modifying group is conjugated to the peptide by use of a linker comprising an oxime bond.
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MEDICAL DELIVERY DEVICE WITH TIME LAPSE INDICATOR (Fri, 12 Nov 2010)
The present invention relates to medical delivery devices for administering a dose of a drug into the body of a subject user and incorporating a time lapse indicator which is configured for indicating after administration that a dose of the drug actually has been administered and for maintaining this indication until lapse of a pre-defined time interval. The time lapse indicator disclosed is based on a pressure sensitive substance which exhibits a change in a visual property in response to an action associated with administering a dose and wherein the pressure sensitive substance exhibits a further change in a visual property after lapse of a pre-defined time interval subsequent to said action.
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Insulin Derivative (Fri, 05 Nov 2010)
The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to pharmaceutical compositions containing such derivatives and to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention.
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ESTIMATING A NUTRITIONAL PARAMETER FOR ASSISTING INSULIN ADMINISTRATION (Fri, 05 Nov 2010)
A device for estimating a nutritional parameter of a meal consumed by an individual is disclosed. The apparatus comprises processing means adapted to obtain input values of at least a physiological parameter of the user measured prior to and after intake of a meal by the user, and of at least a dose of medication administered to the user. Based on the input values the apparitus is adapted to determine from at least the obtained input values, an estimate of a nutritional parameter of the meal and to generate an output to a user indicative of the determined estimate.
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Antibodies Against Human NKG2D and Uses Thereof (Fri, 29 Oct 2010)
The present invention provides isolated anti-human NKG2D monoclonal antibodies useful for therapeutic applications in humans. Typically, the antibodies are fully human or humanized to minimize the risk for immune responses against the antibodies when administered to a patient. Preferred antibodies include human monoclonal antibodies MS and 21F2. As described herein, other antigen-binding molecules such as, e.g., antigen-binding antibody fragments, antibody derivatives, and multi-specific molecules, can be designed or derived from such antibodies.
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Mixtures of Amylin and Insulin (Thu, 21 Oct 2010)
The present invention relates to a soluble pharmaceutical composition for parenteral administration, which comprises an amylin peptide, and a meal-related insulin peptide, and to the use of such compositions for treatment of e.g. hyperglycemia.
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