RU2012153753A - Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов - Google Patents
Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов Download PDFInfo
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- RU2012153753A RU2012153753A RU2012153753/04A RU2012153753A RU2012153753A RU 2012153753 A RU2012153753 A RU 2012153753A RU 2012153753/04 A RU2012153753/04 A RU 2012153753/04A RU 2012153753 A RU2012153753 A RU 2012153753A RU 2012153753 A RU2012153753 A RU 2012153753A
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- amino acid
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- alkyl
- receptor
- glucagon
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- 108060003199 Glucagon Proteins 0.000 title claims abstract 16
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title claims abstract 14
- 229960004666 glucagon Drugs 0.000 title claims abstract 14
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 title claims abstract 11
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 title claims abstract 11
- 230000000694 effects Effects 0.000 title claims abstract 8
- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract 5
- 102400000321 Glucagon Human genes 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 24
- 102000051325 Glucagon Human genes 0.000 claims abstract 13
- 239000003446 ligand Substances 0.000 claims abstract 6
- 102000005962 receptors Human genes 0.000 claims abstract 6
- 108020003175 receptors Proteins 0.000 claims abstract 6
- 108091006027 G proteins Proteins 0.000 claims abstract 5
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims abstract 5
- 102000030782 GTP binding Human genes 0.000 claims abstract 5
- 108091000058 GTP-Binding Proteins 0.000 claims abstract 5
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims abstract 5
- 102100040918 Pro-glucagon Human genes 0.000 claims abstract 5
- 150000001408 amides Chemical class 0.000 claims abstract 5
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 claims abstract 5
- 108010063919 Glucagon Receptors Proteins 0.000 claims abstract 4
- 102100040890 Glucagon receptor Human genes 0.000 claims abstract 4
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims abstract 4
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 claims abstract 4
- 235000021588 free fatty acids Nutrition 0.000 claims abstract 4
- 102100039994 Gastric inhibitory polypeptide Human genes 0.000 claims abstract 3
- QPIZDZGIXDKCRC-JTCWOHKRSA-N 2,4-dihydroxy-6-methyl-3-[(2e,6e)-3,7,11-trimethyldodeca-2,6,10-trienyl]benzoic acid Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\CC1=C(O)C=C(C)C(C(O)=O)=C1O QPIZDZGIXDKCRC-JTCWOHKRSA-N 0.000 claims abstract 2
- BREBKAKBNYXIOP-UHFFFAOYSA-N 4-(phenoxymethyl)piperidine Chemical compound C1CNCCC1COC1=CC=CC=C1 BREBKAKBNYXIOP-UHFFFAOYSA-N 0.000 claims abstract 2
- 102100026148 Free fatty acid receptor 1 Human genes 0.000 claims abstract 2
- 102100023328 G-protein coupled estrogen receptor 1 Human genes 0.000 claims abstract 2
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims abstract 2
- 101000912510 Homo sapiens Free fatty acid receptor 1 Proteins 0.000 claims abstract 2
- 101000829902 Homo sapiens G-protein coupled estrogen receptor 1 Proteins 0.000 claims abstract 2
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims abstract 2
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 claims abstract 2
- QPIZDZGIXDKCRC-UHFFFAOYSA-N ilicicolinic acid B Natural products CC(C)=CCCC(C)=CCCC(C)=CCC1=C(O)C=C(C)C(C(O)=O)=C1O QPIZDZGIXDKCRC-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000005647 linker group Chemical group 0.000 claims abstract 2
- 150000003904 phospholipids Chemical class 0.000 claims abstract 2
- 229930002330 retinoic acid Natural products 0.000 claims abstract 2
- 150000003431 steroids Chemical class 0.000 claims abstract 2
- 150000001467 thiazolidinediones Chemical class 0.000 claims abstract 2
- 229960001727 tretinoin Drugs 0.000 claims abstract 2
- 235000001014 amino acid Nutrition 0.000 claims 47
- 150000001413 amino acids Chemical class 0.000 claims 46
- 125000003275 alpha amino acid group Chemical group 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 238000012986 modification Methods 0.000 claims 14
- 230000004048 modification Effects 0.000 claims 14
- 238000006467 substitution reaction Methods 0.000 claims 14
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 10
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 9
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000006702 (C1-C18) alkyl group Chemical group 0.000 claims 7
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 7
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- 238000012217 deletion Methods 0.000 claims 6
- 230000037430 deletion Effects 0.000 claims 6
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 5
- -1 His Chemical compound 0.000 claims 5
- AYFVYJQAPQTCCC-HRFVKAFMSA-N L-allothreonine Chemical compound C[C@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-HRFVKAFMSA-N 0.000 claims 5
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 5
- 230000001270 agonistic effect Effects 0.000 claims 5
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 4
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 4
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical compound OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 claims 4
- CBQJSKKFNMDLON-JTQLQIEISA-N N-acetyl-L-phenylalanine Chemical compound CC(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 CBQJSKKFNMDLON-JTQLQIEISA-N 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 238000003776 cleavage reaction Methods 0.000 claims 4
- 125000004185 ester group Chemical group 0.000 claims 4
- 230000007017 scission Effects 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- VBOQYPQEPHKASR-VKHMYHEASA-N L-homocysteic acid Chemical compound OC(=O)[C@@H](N)CCS(O)(=O)=O VBOQYPQEPHKASR-VKHMYHEASA-N 0.000 claims 3
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 3
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Chemical compound CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000000404 glutamine group Chemical group N[C@@H](CCC(N)=O)C(=O)* 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 238000001727 in vivo Methods 0.000 claims 3
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 2
- 125000006689 (C2-C5) heterocyclyl group Chemical group 0.000 claims 2
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 claims 2
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 2
- OYIFNHCXNCRBQI-BYPYZUCNSA-N L-2-aminoadipic acid Chemical compound OC(=O)[C@@H](N)CCCC(O)=O OYIFNHCXNCRBQI-BYPYZUCNSA-N 0.000 claims 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 2
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims 2
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 claims 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 2
- 210000004899 c-terminal region Anatomy 0.000 claims 2
- 235000013477 citrulline Nutrition 0.000 claims 2
- 229960002173 citrulline Drugs 0.000 claims 2
- XVOYSCVBGLVSOL-UHFFFAOYSA-N cysteic acid Chemical compound OC(=O)C(N)CS(O)(=O)=O XVOYSCVBGLVSOL-UHFFFAOYSA-N 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000001360 methionine group Chemical group N[C@@H](CCSC)C(=O)* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- NPUSYSKUENYRAN-UHFFFAOYSA-N 2-(1h-imidazol-2-yl)-2-methylpropanoic acid Chemical compound OC(=O)C(C)(C)C1=NC=CN1 NPUSYSKUENYRAN-UHFFFAOYSA-N 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- HNDVDQJCIGZPNO-RXMQYKEDSA-N D-histidine Chemical compound OC(=O)[C@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-RXMQYKEDSA-N 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 102100040134 Free fatty acid receptor 4 Human genes 0.000 claims 1
- IKAIKUBBJHFNBZ-LURJTMIESA-N Gly-Lys Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)CN IKAIKUBBJHFNBZ-LURJTMIESA-N 0.000 claims 1
- 101000890672 Homo sapiens Free fatty acid receptor 4 Proteins 0.000 claims 1
- 125000000998 L-alanino group Chemical group [H]N([*])[C@](C([H])([H])[H])([H])C(=O)O[H] 0.000 claims 1
- NVGBPTNZLWRQSY-UWVGGRQHSA-N Lys-Lys Chemical compound NCCCC[C@H](N)C(=O)N[C@H](C(O)=O)CCCCN NVGBPTNZLWRQSY-UWVGGRQHSA-N 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 150000003973 alkyl amines Chemical class 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 150000001483 arginine derivatives Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000002228 disulfide group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000003379 elimination reaction Methods 0.000 claims 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 1
- 108010015792 glycyllysine Proteins 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000005597 hydrazone group Chemical group 0.000 claims 1
- 150000001261 hydroxy acids Chemical class 0.000 claims 1
- PRJKNHOMHKJCEJ-UHFFFAOYSA-N imidazol-4-ylacetic acid Chemical compound OC(=O)CC1=CN=CN1 PRJKNHOMHKJCEJ-UHFFFAOYSA-N 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 108010054155 lysyllysine Proteins 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000004962 physiological condition Effects 0.000 claims 1
- 150000003354 serine derivatives Chemical group 0.000 claims 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 150000003587 threonine derivatives Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US33443310P | 2010-05-13 | 2010-05-13 | |
| US61/334,433 | 2010-05-13 | ||
| PCT/US2011/035912 WO2011143208A1 (en) | 2010-05-13 | 2011-05-10 | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
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| RU2012153753A true RU2012153753A (ru) | 2014-06-20 |
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| RU2012153753/04A RU2012153753A (ru) | 2010-05-13 | 2011-05-10 | Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов |
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| EP (1) | EP2568993A4 (OSRAM) |
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| WO (1) | WO2011143208A1 (OSRAM) |
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-
2011
- 2011-05-10 CA CA 2797089 patent/CA2797089A1/en not_active Abandoned
- 2011-05-10 MX MX2012013005A patent/MX2012013005A/es not_active Application Discontinuation
- 2011-05-10 CN CN2011800371114A patent/CN103179976A/zh active Pending
- 2011-05-10 KR KR20127029584A patent/KR20130111923A/ko not_active Withdrawn
- 2011-05-10 JP JP2013510239A patent/JP6050746B2/ja not_active Expired - Fee Related
- 2011-05-10 RU RU2012153753/04A patent/RU2012153753A/ru not_active Application Discontinuation
- 2011-05-10 BR BR112012028707A patent/BR112012028707A2/pt not_active IP Right Cessation
- 2011-05-10 US US13/697,017 patent/US9145451B2/en not_active Expired - Fee Related
- 2011-05-10 WO PCT/US2011/035912 patent/WO2011143208A1/en not_active Ceased
- 2011-05-10 EP EP20110781136 patent/EP2568993A4/en not_active Withdrawn
- 2011-05-12 AR ARP110101648 patent/AR081042A1/es unknown
- 2011-05-13 TW TW100116894A patent/TW201143791A/zh unknown
-
2015
- 2015-08-28 US US14/838,991 patent/US20160051688A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2568993A4 (en) | 2014-02-19 |
| JP6050746B2 (ja) | 2016-12-21 |
| CA2797089A1 (en) | 2011-11-17 |
| EP2568993A1 (en) | 2013-03-20 |
| MX2012013005A (es) | 2013-02-26 |
| AR081042A1 (es) | 2012-05-30 |
| US20130116172A1 (en) | 2013-05-09 |
| KR20130111923A (ko) | 2013-10-11 |
| WO2011143208A1 (en) | 2011-11-17 |
| TW201143791A (en) | 2011-12-16 |
| JP2013533849A (ja) | 2013-08-29 |
| US20160051688A1 (en) | 2016-02-25 |
| CN103179976A (zh) | 2013-06-26 |
| US9145451B2 (en) | 2015-09-29 |
| BR112012028707A2 (pt) | 2019-09-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20160412 |