PATENTSCOPE: EN_ALL:nmr AND PA:novo nordisk

EGF(A) ANALOGUES, PREPARATION, FORMULATIONS AND USES THEREOF (Fri, 25 Jan 2019)
The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293- 332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.
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MIC-1 COMPOUNDS AND USES THEREOF (Fri, 30 Nov 2018)
The invention relates to MIC-1 compounds. More specifically it relates to compounds comprising a MIC-1 polypeptide with an N-terminal amino acid extension and a protractor wherein the amino acid extension comprises 3 to 36 amino acid residues and where the MIC-1 polypeptide and the N-terminal amino acid extension together have a calculated pI lower than 6.5. The compounds of the invention have MIC-1 activity. The invention also relates to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable excipients, as well as the medical use of the compounds.
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OLIGOMER EXTENDED INSULIN-FC CONJUGATES (Fri, 12 Oct 2018)
This invention is in the field of protein conjugates. More specifically the invention relates to oligomer extended insulins with covalently attached Fc monomer polypeptides, for use in the treatment of a metabolic disorder or condition, and to methods of producing such oligomer extended insulin-Fc conjugates. The invention also relates to novel Fc fragments, to intermediate products, and to the use of such intermediate products in processes for the synthesis of the oligomer extended insulin-Fc conjugates of the invention. Finally the invention provides pharmaceutical compositions comprising the oligomer extended insulin-Fc conjugates of the invention, and relates to the use of such compositions for the treatment or prevention of medical conditions relating to metabolic disorders or conditions.
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PROCOAGULANT ANTIBODIES (Fri, 10 Aug 2018)
The present invention relates to improved procoagulant antibodies including bispecific antibodies capable of binding to coagulation Factor IX (FIX) or the activated form thereof Factor IXa (FIXa) and optionally Factor X (FX) and the activated form thereof Factor Xa (FXa) and promoting FX activation by FIXa, antibodies binding their epitopes and methods and composition for treating subjects suffering from a coagulopathy such as haemophilia A.
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PREPARATION OF SUGAR-NUCLEOTIDES (Fri, 29 Jun 2018)
The present invention relates to methods for preparation of glyco-conjugated proteins and in particular to processes for preparation of sugar-nucleotides and modified sugar-nucleotides.
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DCHBS-ACTIVE ESTERS OF PEG COMPOUNDS AND THEIR USE (Sat, 12 May 2018)
The present invention relates to a novel acylating agent, a method for its preparation, and a method of using it for acylating one or more amino groups of an amino acid, a peptide, or a protein. The novel acylating agent may be a compound which comprises a structural element -HN-(CH2)2-(O-((CH2)2)k-O-(CH2)n-CO-, wherein k is an integer in the range of 1-10, and n is an integer in the range of 1-2, being esterified at its -CO-end to the hydroxy group of 3,5-dichloro-2-hydroxy-benzenesulfonic acid (3,5-DC-2-HBSA). This novel acylating agent has an improved stability. Using this agent the acylation process is improved as regards robustness, as well as improving yield and overall production economy. The novel acylating agent is useful for acylating pharmaceutical peptides and proteins such as GLP-1, insulin, pYY, and amylin. The invention also relates to a number of novel GLP-1 precursor peptides and derivatives in which the two N-terminal amino acids have been deleted.
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AMPLIFYING BETA CELL DIFFERENTIATION WITH SMALL MOLECULES BET (BROMODOMAIN AND EXTRATERMINAL FAMILY OF BROMODOMAIN-CONTAINING PROTEINS) INHIBITORS (Fri, 05 Jan 2018)
The present invention provides an in vitromethod for obtaining cells of the pancreatic endocrine lineage, comprising a step of culturing pancreatic progenitor cells, wherein said pancreatic progenitor cells are in a cell culture medium comprising at least one BET inhibitor.
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PHARMACEUTICAL COMPOSITIONS OF FGF21 DERIVATIVES AND USES THEREOF (Fri, 29 Dec 2017)
The present invention relates to pharmaceutical compositions. In particular compositions comprising derivatives of analogues of FGF21, more in particular to analogues of FGF21 having a side chain attached to a cysteine in the C-terminal part of FGF21. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of such compositions.
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EGF(A) ANALOGUES WITH FATTY ACID SUBSTITUENTS (Fri, 21 Jul 2017)
The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293- 332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.
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PROTEIN CONJUGATES (Fri, 07 Apr 2017)
The invention relates to protein conjugates and in particular conjugates of more than two protein or polypeptides. The compounds include a trivalent linker moiety that enables efficient production of desired products.
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NOVEL INSULIN DERIVATIVES AND THE MEDICAL USES HEREOF (Fri, 03 Mar 2017)
The present invention is in the therapeutic fields of drugs for medical conditions relating to diabetes. More specifically the invention relates to novel acylated derivatives of human insulin analogues. The invention also provides pharmaceutical compositions comprising such insulin derivatives, and relates to the use of such derivatives for the treatment or prevention of medical conditions relating to diabetes.
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NOVEL INSULIN DERIVATIVES AND THE MEDICAL USES HEREOF (Fri, 03 Mar 2017)
The present invention is in the therapeutic fields of drugs for medical conditions relating to diabetes. More specifically the invention relates to novel acylated derivatives of human insulin analogues. The invention also provides pharmaceutical compositions comprising such insulin derivatives, and relates to the use of such derivatives for the treatment or prevention of medical conditions relating to diabetes.
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NOVEL INSULIN DERIVATIVES AND THE MEDICAL USES HEREOF (Fri, 03 Mar 2017)
The present invention is in the therapeutic fields of drugs for medical conditions relating to diabetes. More specifically the invention relates to novel acylated derivatives of human insulin analogues. The invention also provides pharmaceutical compositions comprising such insulin derivatives, and relates to the use of such derivatives for the treatment or prevention of medical conditions relating to diabetes.
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SELECTIVE PYY COMPOUNDS AND USES THEREOF (Fri, 16 Dec 2016)
The invention relates to PYY compounds with the amino acid modifications 7Lys, 30Trp, and 31Leu, and in addition to these, 22Ile and/or 28Tyr, and derivatives thereof. The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.
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SELECTIVE PYY COMPOUNDS AND USES THEREOF (Fri, 12 Aug 2016)
The invention relates to PYY compounds having the amino acid in the position corresponding to position 30 of hPYY(1-36) substituted with tryptophan and derivatives thereof with a modifying group attached to the position corresponding to position 10 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.
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PHARMACEUTICAL COMPOSITION FOR ORAL INSULIN ADMINISTRATION COMPRISING A TABLET CORE AND A POLYVINYL ALCOHOL COATING (Fri, 05 Aug 2016)
The present invention relates to a solid oral insulin composition comprising a salt of capric acid which enhances the bioavailability and/or the absorption of said acylated insulin in combination with a polyvinyl alcohol coating, which is soluble in aqueous media independent of pH.
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FGF21 DERIVATIVES AND USES THEREOF (Fri, 01 Jul 2016)
The invention relates to a derivative of a FGF21 protein having a cysteine residue at a position corresponding to position 167, 169, 170, 171, 172, 173, 174, 175 and in particular position 180 or position 181 of mature human FGF21 and derivatives thereof having a side chain attached to this cysteine. The FGF21 derivatives of the invention display high potency towards the FGF receptors. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of the FGF21 derivatives.
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GLP-1 DERIVATIVES AND USES THEREOF (Fri, 03 Jun 2016)
The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1st and a 2nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1st or 2nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
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STABLE GLP-1 BASED GLP-1/GLUCAGON RECEPTOR CO-AGONISTS (Fri, 15 Apr 2016)
The application concerns stable and protracted GLP-1 derivatives which are GLP-l/glucagon receptor co-agonists, compositions thereof, use of the GLP-1 derivatives in medicine, and to methods of treatment comprising administration of the GLP-1 derivatives to patients, including treatment of diabetes, obesity and related diseases and conditions. Prefered GLP-1 derivatives comprise a polypeptide consisting of the amino acid sequence of Formula I: lmp-X8-His-Gly-Thr-Phe-Thr-Ser-Asp-Xl 6-Ser-Xi 8-Tyr-Leu-Glu-X22- X23-Ala-Ala -X26-X27-Phe-I le-Ala-Trp-Leu-X33-X34-X35-X36-X37 [I], wherein - X8 is Ala, Aib, Acb, or Gly; - X16 is Val, Leu, lie, or Tyr; - X18 is Lys or Arg; - X22 is Gly, Ala, Glu, Lys, Arg, Ser, orAib; - X23 is Gin, Arg, or Lys; - X26 is Lys or Arg; - X27 is Glu or Lys; - X33 is Val, Leu, or lle; - X34 is Lys or Arg; - X35 is Gly, Thr, Lys, or is absent; - X36 is Ala, Gly, Lys, Ser, or is absent; - X37 is Gly or is absent; wherein said GLP-i derivative further comprises a substituent comprising a lipophilic moiety and at least two negatively charged moieties, wherein one of said negatively charged moieties is distal of a lipophilic moiety; wherein said polypeptide optionally comprises a C-terminal amide; or a pharmaceutically acceptable salt and/or ester thereof.
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ANTIBODIES CAPABLE OF BINDING TWO EPITOPES ON TISSUE FACTOR PATHWAY INHIBITOR (1-161) (Fri, 25 Mar 2016)
The application discloses bispecific TFPI antibodies that are capable of specifically and simultaneously binding two epitopes within TFPI (1-161). Such bispecific antibodies strongly enhance thrombin generation by neutralising TFPI, even where the concentration of TFPI is elevated. Bispecific antibodies of the invention or compositions comprising them may be used for the treatment of subjects with a coagulopathy.
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