JP2013534906A5 - - Google Patents
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- JP2013534906A5 JP2013534906A5 JP2013510240A JP2013510240A JP2013534906A5 JP 2013534906 A5 JP2013534906 A5 JP 2013534906A5 JP 2013510240 A JP2013510240 A JP 2013510240A JP 2013510240 A JP2013510240 A JP 2013510240A JP 2013534906 A5 JP2013534906 A5 JP 2013534906A5
- Authority
- JP
- Japan
- Prior art keywords
- amino acid
- alkyl
- receptor
- group
- substitution
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 150000001413 amino acids Chemical group 0.000 claims 68
- 235000001014 amino acid Nutrition 0.000 claims 50
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 19
- 238000006467 substitution reaction Methods 0.000 claims 19
- 108060003199 Glucagon Proteins 0.000 claims 15
- 230000004048 modification Effects 0.000 claims 15
- 238000012986 modification Methods 0.000 claims 15
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 12
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 12
- 102000051325 Glucagon Human genes 0.000 claims 11
- 230000000694 effects Effects 0.000 claims 11
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical group 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 claims 11
- 229960004666 glucagon Drugs 0.000 claims 11
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 9
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 9
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 8
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 8
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-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
- -1 Ala Chemical compound 0.000 claims 6
- 238000012217 deletion Methods 0.000 claims 6
- 230000037430 deletion Effects 0.000 claims 6
- 125000002252 acyl group Chemical group 0.000 claims 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-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
- 125000004429 atom Chemical group 0.000 claims 4
- 238000003776 cleavage reaction Methods 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 108090000765 processed proteins & peptides Proteins 0.000 claims 4
- 230000007017 scission Effects 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 3
- 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 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
- 102100040918 Pro-glucagon Human genes 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 claims 3
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 238000001727 in vivo Methods 0.000 claims 3
- 239000003446 ligand Substances 0.000 claims 3
- 230000035945 sensitivity Effects 0.000 claims 3
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl 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
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 102100039994 Gastric inhibitory polypeptide Human genes 0.000 claims 2
- 108010063919 Glucagon Receptors Proteins 0.000 claims 2
- 102100040890 Glucagon receptor Human genes 0.000 claims 2
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 2
- 102100032882 Glucagon-like peptide 1 receptor Human genes 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
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-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
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-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
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 2
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Chemical compound CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000002378 acidificating effect Effects 0.000 claims 2
- 150000001408 amides Chemical group 0.000 claims 2
- 210000004899 c-terminal region Anatomy 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 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
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000002148 esters Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 238000003780 insertion Methods 0.000 claims 2
- 230000037431 insertion Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims 1
- SNRCMWGPCHPRBP-YFKPBYRVSA-N (2s)-2-(hydroxyamino)-3-(1h-imidazol-5-yl)propanoic acid Chemical compound ON[C@H](C(O)=O)CC1=CNC=N1 SNRCMWGPCHPRBP-YFKPBYRVSA-N 0.000 claims 1
- PSWSDQRXCOJSFC-FJXQXJEOSA-N (2s)-2-acetamido-3-(1h-imidazol-5-yl)propanoic acid;hydrate Chemical compound O.CC(=O)N[C@H](C(O)=O)CC1=CN=CN1 PSWSDQRXCOJSFC-FJXQXJEOSA-N 0.000 claims 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 1
- 102100032187 Androgen receptor Human genes 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 102100038495 Bile acid receptor Human genes 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 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
- 108010016626 Dipeptides Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102100038595 Estrogen receptor Human genes 0.000 claims 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims 1
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims 1
- 108090000079 Glucocorticoid Receptors Proteins 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
- 101000603876 Homo sapiens Bile acid receptor 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
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 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
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 1
- 102100021316 Mineralocorticoid receptor Human genes 0.000 claims 1
- 125000000534 N(2)-L-lysino group Chemical group [H]OC(=O)[C@@]([H])(N([H])[*])C([H])([H])C([H])([H])C(C([H])([H])N([H])[H])([H])[H] 0.000 claims 1
- PSFABYLDRXJYID-VKHMYHEASA-N N-Methylserine Chemical compound CN[C@@H](CO)C(O)=O PSFABYLDRXJYID-VKHMYHEASA-N 0.000 claims 1
- PSFABYLDRXJYID-UHFFFAOYSA-N N-methyl-DL-serine Natural products CNC(CO)C(O)=O PSFABYLDRXJYID-UHFFFAOYSA-N 0.000 claims 1
- 102100038494 Nuclear receptor subfamily 1 group I member 2 Human genes 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 108010001511 Pregnane X Receptor Proteins 0.000 claims 1
- 108091008680 RAR-related orphan receptors Proteins 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
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 150000003973 alkyl amines Chemical class 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 108010080146 androgen receptors Proteins 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000003613 bile acid Substances 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 150000001886 cortisols Chemical class 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940039227 diagnostic agent Drugs 0.000 claims 1
- 239000000032 diagnostic agent Substances 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 125000002228 disulfide group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960005309 estradiol Drugs 0.000 claims 1
- 229930182833 estradiol Natural products 0.000 claims 1
- 108010038795 estrogen receptors Proteins 0.000 claims 1
- 229960003399 estrone Drugs 0.000 claims 1
- 125000001033 ether group Chemical group 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 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
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 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
- 125000005647 linker group Chemical group 0.000 claims 1
- 102000004311 liver X receptors Human genes 0.000 claims 1
- 108090000865 liver X receptors Proteins 0.000 claims 1
- 108010054155 lysyllysine Proteins 0.000 claims 1
- 229930182817 methionine Natural products 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
- 102000039446 nucleic acids Human genes 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 150000007523 nucleic acids Chemical class 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000004962 physiological condition Effects 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 102000003998 progesterone receptors Human genes 0.000 claims 1
- 108090000468 progesterone receptors Proteins 0.000 claims 1
- 239000002096 quantum dot Substances 0.000 claims 1
- 102000003702 retinoic acid receptors Human genes 0.000 claims 1
- 108090000064 retinoic acid receptors Proteins 0.000 claims 1
- 150000003384 small molecules Chemical class 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 229960003604 testosterone Drugs 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 108090000721 thyroid hormone receptors Proteins 0.000 claims 1
- 102000004217 thyroid hormone receptors Human genes 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- 102000009310 vitamin D receptors Human genes 0.000 claims 1
- 108050000156 vitamin D receptors Proteins 0.000 claims 1
- 229910052727 yttrium Inorganic materials 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33443510P | 2010-05-13 | 2010-05-13 | |
| US61/334,435 | 2010-05-13 | ||
| US201161432077P | 2011-01-12 | 2011-01-12 | |
| US61/432,077 | 2011-01-12 | ||
| PCT/US2011/035913 WO2011143209A1 (en) | 2010-05-13 | 2011-05-10 | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013534906A JP2013534906A (ja) | 2013-09-09 |
| JP2013534906A5 true JP2013534906A5 (https=) | 2014-06-19 |
| JP6121323B2 JP6121323B2 (ja) | 2017-05-10 |
Family
ID=44914673
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013510240A Active JP6121323B2 (ja) | 2010-05-13 | 2011-05-10 | 核内ホルモン受容体の活性を示すグルカゴンスーパーファミリーのペプチド |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US9127088B2 (https=) |
| EP (1) | EP2569000B1 (https=) |
| JP (1) | JP6121323B2 (https=) |
| KR (1) | KR20130062931A (https=) |
| CN (1) | CN103079587B (https=) |
| AR (1) | AR081043A1 (https=) |
| BR (1) | BR112012028704A2 (https=) |
| CA (1) | CA2797095A1 (https=) |
| ES (1) | ES2661228T3 (https=) |
| MX (1) | MX2012013001A (https=) |
| RU (1) | RU2604067C2 (https=) |
| WO (1) | WO2011143209A1 (https=) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2570133B1 (en) | 2005-11-07 | 2016-03-23 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| RU2477286C2 (ru) | 2007-01-05 | 2013-03-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | АНАЛОГИ ГЛЮКАГОНА, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ В БУФЕРАХ С ФИЗИОЛОГИЧЕСКИМ ЗНАЧЕНИЕМ pH |
| AU2008216265B2 (en) | 2007-02-15 | 2014-04-03 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| AU2008232709C1 (en) | 2007-03-28 | 2015-01-15 | President And Fellows Of Harvard College | Stitched polypeptides |
| WO2009058662A2 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| US8980830B2 (en) | 2007-10-30 | 2015-03-17 | Indiana University Research And Technology Corporation | Peptide compounds exhibiting glucagon antagonist and GLP-1 agonist activity |
| DK2300035T3 (en) | 2008-06-17 | 2015-11-16 | Univ Indiana Res & Tech Corp | Mixed GIP-based agonists for the treatment of metabolic diseases and obesity |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| WO2009155257A1 (en) | 2008-06-17 | 2009-12-23 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability physiological ph buffers |
| CN102325539A (zh) | 2008-12-19 | 2012-01-18 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
| WO2010148089A1 (en) | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| US8703701B2 (en) | 2009-12-18 | 2014-04-22 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| EP2528618A4 (en) | 2010-01-27 | 2015-05-27 | Univ Indiana Res & Tech Corp | GLUCAGON ANTAGONISTE AND GIP AGONISTS CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLISM DISEASES AND ADIPOSITAS |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| CA2797095A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity |
| RU2580317C2 (ru) | 2010-06-24 | 2016-04-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов |
| KR20170058446A (ko) | 2010-08-13 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| US8507428B2 (en) | 2010-12-22 | 2013-08-13 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| CN102643339B (zh) * | 2011-02-21 | 2014-04-09 | 天津药物研究院 | 一种glp-1类似物、制备方法及其应用 |
| RS56173B1 (sr) | 2011-06-22 | 2017-11-30 | Univ Indiana Res & Tech Corp | Koagonisti receptora za glukagon/glp-1 receptora |
| BR112013032717A2 (pt) | 2011-06-22 | 2017-01-24 | Univ Indiana Res & Tech Corp | coagonistas do receptor de glucagon/glp-1 |
| AR088392A1 (es) | 2011-10-18 | 2014-05-28 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos |
| RU2014117678A (ru) * | 2011-11-17 | 2015-12-27 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептиды глюкагонового суперсемейства, обладающие глюкокортикоидной рецепторной активностью |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| CA2862038C (en) | 2012-02-15 | 2021-05-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| WO2013141965A1 (en) | 2012-03-21 | 2013-09-26 | Baxter International Inc. | Tfpi inhibitors and methods of use |
| KR20150023690A (ko) * | 2012-06-14 | 2015-03-05 | 사노피 | 엑센딘-4 펩타이드 유사체 |
| CA2877358A1 (en) | 2012-06-21 | 2013-12-27 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| HRP20180936T1 (hr) * | 2012-06-21 | 2018-12-14 | Indiana University Research And Technology Corporation | Analozi glukagona koji pokazuju aktivnost prema receptoru za gip |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| DK2907824T3 (en) | 2012-10-11 | 2018-07-23 | Daiichi Sankyo Co Ltd | ANTIBODY-drug conjugate |
| EP2910573B1 (en) | 2012-10-19 | 2020-02-19 | Daiichi Sankyo Company, Limited | Antibody-drug conjugate produced by binding through linker having hydrophilic structure |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| TWI617574B (zh) * | 2012-12-11 | 2018-03-11 | 梅迪繆思有限公司 | 用於治療肥胖之升糖素與ｇｌｐ－１共促效劑 |
| HK1211232A1 (en) | 2012-12-21 | 2016-05-20 | Sanofi | Exendin-4 derivatives as dual glp1/gip or trigonal glp1/gip/glucagon agonists |
| AU2014230472A1 (en) * | 2013-03-14 | 2015-10-01 | Medimmune Limited | Pegylated glucagon and GLP-1 co-agonists for the treatment of obesity |
| CN105473147A (zh) | 2013-04-24 | 2016-04-06 | 萨克生物研究学院 | 维生素d受体/smad基因组回路门纤维化反应 |
| WO2014197680A1 (en) | 2013-06-05 | 2014-12-11 | Salk Institute For Biological Studies | Vitamin d receptor agonists to treat diseases involving cxcl12 activity |
| EP3080152A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Non-acylated exendin-4 peptide analogues |
| TW201609799A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／ｇｉｐ受體促效劑 |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| AR098616A1 (es) | 2013-12-18 | 2016-06-01 | Lilly Co Eli | Péptido para el tratamiento de hipoglicemia severa |
| LT3424955T (lt) * | 2013-12-25 | 2025-06-25 | Daiichi Sankyo Company, Limited | Anti-trop2 antikūno ir vaisto konjugato gamybos būdas |
| SI3466976T1 (sl) | 2014-01-31 | 2021-12-31 | Daiichi Sankyo Company, Limited | Anti-her2 konjugat protitelesa-zdravila |
| TW201625670A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑 |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物 |
| TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑 |
| JP6612738B2 (ja) | 2014-04-10 | 2019-11-27 | 第一三共株式会社 | 抗ｈｅｒ２抗体−薬物コンジュゲート |
| KR102399277B1 (ko) | 2014-04-10 | 2022-05-18 | 다이이찌 산쿄 가부시키가이샤 | 항her3 항체-약물 콘주게이트 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| WO2016049359A1 (en) | 2014-09-24 | 2016-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| JP6393425B2 (ja) | 2014-12-08 | 2018-09-19 | ジ アサン ファウンデーション | バクテロイデス・アシジファシエンスを有効成分として含む、代謝性疾患の予防又は治療用薬学的組成物 |
| US10253067B2 (en) | 2015-03-20 | 2019-04-09 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| TWI726889B (zh) | 2015-06-10 | 2021-05-11 | 英商梅迪繆思有限公司 | 蛋白酶抗性之脂化肽 |
| EP4180455A1 (en) | 2015-06-29 | 2023-05-17 | Daiichi Sankyo Company, Limited | Method for selectively manufacturing antibody-drug conjugate |
| AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
| CN108602894A (zh) * | 2015-10-30 | 2018-09-28 | 纽约州立大学研究基金会 | 胃泌酸调节素类似物及其制备和使用方法 |
| CN108697768B (zh) | 2015-12-23 | 2022-07-22 | 约翰霍普金斯大学 | 长效glp-1r激动剂作为神经系统病状和神经退行性病状的治疗方法 |
| CN106046145B (zh) * | 2016-04-22 | 2022-11-04 | 深圳市图微安创科技开发有限公司 | Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化 |
| JP7091255B2 (ja) * | 2016-05-06 | 2022-06-27 | アイオニス・ファーマシューティカルズ・インコーポレイテッド | Ｇｌｐ－１受容体リガンド部分コンジュゲート化オリゴヌクレオチドおよびその使用 |
| WO2017210242A1 (en) * | 2016-06-02 | 2017-12-07 | Indiana University Research And Technology Corporation | Insulin-nuclear hormone conjugates |
| US20190388510A1 (en) * | 2016-06-02 | 2019-12-26 | Indiana University Research And Technology Corporation | Glucagon-t3 conjugates |
| EP3463424A1 (en) * | 2016-06-02 | 2019-04-10 | Indiana University Research & Technology Corporation | Glucagon-like peptide-1-t3 conjugates |
| BR112019011794A2 (pt) | 2016-12-12 | 2019-10-29 | Daiichi Sankyo Co Ltd | composição farmacêutica, e, método terapêutico. |
| CA3050668C (en) | 2017-01-17 | 2023-08-15 | Daiichi Sankyo Company, Limited | Anti-gpr20 antibody and anti-gpr20 antibody-drug conjugate |
| TW202532102A (zh) | 2017-05-15 | 2025-08-16 | 日商第一三共股份有限公司 | 抗體－藥物結合物及其用途 |
| WO2019023149A1 (en) | 2017-07-24 | 2019-01-31 | Salk Institute For Biological Studies | USE OF BROMODOMAIN-CONTAINING PROTEIN-9 ANTAGONISTS IN ASSOCIATION WITH VITAMIN D RECEPTOR AGONISTS IN THE TREATMENT OF DIABETES |
| BR112020003466B1 (pt) | 2017-08-31 | 2023-12-12 | Daiichi Sankyo Company, Limited | Métodos de produção de composto, e, composto |
| ES3057444T3 (en) | 2017-08-31 | 2026-03-02 | Daiichi Sankyo Co Ltd | Improved method for producing antibody-drug conjugate |
| US20200268898A1 (en) * | 2017-11-08 | 2020-08-27 | Astrazeneca Ab | Glp-1 receptor ligand moiety conjugated oligonucleotides and uses thereof |
| KR102379958B1 (ko) | 2018-05-04 | 2022-04-01 | 노보 노르디스크 에이/에스 | Gip 유도체 및 이의 용도 |
| HUE067382T2 (hu) | 2018-05-18 | 2024-10-28 | Daiichi Sankyo Co Ltd | Anti-MUC1-exatecan antitest-hatóanyag konjugátum |
| TWI846717B (zh) | 2018-07-27 | 2024-07-01 | 日商第一三共股份有限公司 | 辨識抗體-藥物結合物之藥物部位的蛋白質 |
| TW202537643A (zh) | 2018-07-31 | 2025-10-01 | 日商第一三共股份有限公司 | 抗體-藥物結合物之用途 |
| JP2022503793A (ja) * | 2018-09-24 | 2022-01-12 | 武田薬品工業株式会社 | Ｇｉｐ受容体アゴニストペプチド化合物及びその使用 |
| US12453782B2 (en) | 2018-12-21 | 2025-10-28 | Sapreme Technologies B.V. | Antibody-oligonucleotide conjugate |
| CN111825758B (zh) * | 2019-04-19 | 2024-11-22 | 上海翰森生物医药科技有限公司 | Glp-1和gip共激动剂化合物 |
| EP4486318A4 (en) * | 2022-03-02 | 2026-02-25 | Boyce Thompson Institute For Plant Res Inc | Cysteamides, related therapeutic compositions and associated processes |
Family Cites Families (127)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4275152A (en) | 1977-02-03 | 1981-06-23 | Eastman Kodak Company | Hydrolysis of protein-bound cholesterol esters |
| PT83613B (en) | 1985-10-28 | 1988-11-21 | Lilly Co Eli | Process for the selective chemical removal of a protein amino-terminal residue |
| AU597574B2 (en) | 1986-03-07 | 1990-06-07 | Massachusetts Institute Of Technology | Method for enhancing glycoprotein stability |
| JPH04504416A (ja) | 1989-02-17 | 1992-08-06 | コセルコ・ミモトープス・ピィ・ティ・ワイ．エル・ティ・ディ． | ペプチドの使用方法と合成方法 |
| CA2024855C (en) | 1990-09-07 | 1997-12-09 | Boehringer Ingelheim (Canada) Ltd./ Boehringer Ingelheim (Canada) Ltee | Process and intermediates for producing glucagon |
| JPH04145099A (ja) | 1990-10-05 | 1992-05-19 | Sanwa Kagaku Kenkyusho Co Ltd | Ｇｉｐ様活性を有するポリペプチド誘導体及びその用途 |
| US5510459A (en) | 1991-01-17 | 1996-04-23 | Zymogenetics, Inc. | Glucagon antagonists |
| JP3266311B2 (ja) | 1991-05-02 | 2002-03-18 | 生化学工業株式会社 | 新規ポリペプチドおよびこれを用いる抗ｈｉｖ剤 |
| US5359030A (en) | 1993-05-10 | 1994-10-25 | Protein Delivery, Inc. | Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same |
| US5480867A (en) | 1993-12-29 | 1996-01-02 | The Rockefeller University | Glucagon analogs with serine replacements |
| US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| US5691309A (en) | 1995-01-31 | 1997-11-25 | Eli Lilly And Company | Anti-obesity proteins |
| US5869602A (en) | 1995-03-17 | 1999-02-09 | Novo Nordisk A/S | Peptide derivatives |
| DE19530865A1 (de) | 1995-08-22 | 1997-02-27 | Michael Dr Med Nauck | Wirkstoff sowie Mittel zur parenteralen Ernährung |
| HUP9801834A3 (en) | 1995-10-12 | 2000-06-28 | Supergen Inc Emeryville | Liposome formulations of 5beta steroids |
| WO1997029180A1 (en) | 1996-02-06 | 1997-08-14 | Eli Lilly And Company | Diabetes therapy |
| WO1998011126A1 (en) | 1996-09-09 | 1998-03-19 | Zealand Pharmaceuticals A/S | Peptide prodrugs containing an alpha-hydroxyacid linker |
| UA65549C2 (uk) | 1996-11-05 | 2004-04-15 | Елі Ліллі Енд Компані | Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція |
| WO1998024464A1 (en) | 1996-12-03 | 1998-06-11 | Trustees Of Boston University | Specific antagonists for glucose-dependent insulinotropic polypeptide (gip) |
| JP4394279B2 (ja) | 1998-03-09 | 2010-01-06 | ジーランド ファーマ アクティーゼルスカブ | 酵素加水分解に対する傾向が減少した薬理学的に活性なペプチド複合体 |
| US20030236190A1 (en) | 1998-09-02 | 2003-12-25 | Renuka Pillutla | Isulin and IGF-1 receptor agonists and antagonists |
| JP2002526554A (ja) | 1998-10-07 | 2002-08-20 | メディカル カレッジ オブ ジョージア リサーチ インスティチュート，インコーポレイテッド | 骨親和性ホルモンとして用いられるグルコース依存性インスリン親和性ペプチド |
| JP2002534512A (ja) | 1999-01-15 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 非ペプチドｇｌｐ−１アゴニスト |
| GB0404124D0 (en) | 2004-02-25 | 2004-03-31 | Univ Ulster | Antagonists of GIP |
| PT1171465E (pt) | 1999-03-29 | 2004-12-31 | Uutech Ltd | Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes |
| CA2363712C (en) | 1999-05-17 | 2011-05-10 | Conjuchem Inc. | Long lasting insulinotropic peptides |
| US7601691B2 (en) | 1999-05-17 | 2009-10-13 | Conjuchem Biotechnologies Inc. | Anti-obesity agents |
| KR20020097236A (ko) | 2000-04-27 | 2002-12-31 | 바이오네브라스카, 인코포레이티드 | 타입-2 당뇨병, 내당능 장애, 또는 공복 혈당 장애에 대한감수성을 검출하기 위한 위억제성 폴리펩티드 진단 시험 |
| US6677136B2 (en) | 2000-05-03 | 2004-01-13 | Amgen Inc. | Glucagon antagonists |
| AU2001269833A1 (en) | 2000-06-14 | 2001-12-24 | Cytovax Biotechnologies, Inc. | Use of coiled-coil structural scaffold to generate structure-specific peptides |
| ATE424413T1 (de) | 2000-06-16 | 2009-03-15 | Lilly Co Eli | Analoge des glucagon-ähnlichen peptids-1 |
| WO2002010195A2 (en) | 2000-08-02 | 2002-02-07 | Theratechnologies Inc. | Modified peptides with increased potency |
| US20020045572A1 (en) | 2000-08-15 | 2002-04-18 | Cpd, Llc | Method of treating the syndrome of type 2 diabetes in humans |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| US6846831B2 (en) | 2000-08-15 | 2005-01-25 | Cpd, Llc | Method of treating the syndrome of lipodystrophy |
| US6528520B2 (en) | 2000-08-15 | 2003-03-04 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| US7052686B2 (en) | 2000-09-29 | 2006-05-30 | Schering Corporation | Pegylated interleukin-10 |
| EP1351984A2 (en) | 2000-12-13 | 2003-10-15 | Eli Lilly And Company | Amidated glucagon-like peptide-1 |
| EP1411968B1 (en) | 2001-07-31 | 2008-09-17 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Glp-1 exendin-4 peptide analogs and uses thereof |
| US20040002468A1 (en) | 2001-08-08 | 2004-01-01 | Genzyme Corporation | Methods of treating diabetes and other blood sugar disorders |
| CA2458371A1 (en) | 2001-08-23 | 2003-03-06 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| CA2452044A1 (en) | 2001-08-28 | 2003-03-13 | Eli Lilly And Company | Pre-mixes of glp-1 and basal insulin |
| GB0121709D0 (en) | 2001-09-07 | 2001-10-31 | Imp College Innovations Ltd | Food inhibition agent |
| AR036711A1 (es) | 2001-10-05 | 2004-09-29 | Bayer Corp | Peptidos que actuan como agonistas del receptor del glp-1 y como antagonistas del receptor del glucagon y sus metodos de uso farmacologico |
| US7041646B2 (en) | 2001-10-05 | 2006-05-09 | Bayer Pharmaceuticals Corporation | Methods of treating type 2 diabetes with peptides acting as both GLP-1 receptor agonists and glucagon receptor antagonists |
| CA2463908A1 (en) | 2001-10-18 | 2003-04-24 | Bristol-Myers Squibb Company | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
| WO2003035099A1 (en) | 2001-10-19 | 2003-05-01 | Eli Lilly And Company | Biphasic mixtures of glp-1 and insulin |
| JP2005518408A (ja) | 2001-12-29 | 2005-06-23 | ノボ ノルディスク アクティーゼルスカブ | 異常脂肪血症を治療するための、ｇｌｐ−１化合物と他の薬物との組み合わせ使用 |
| MXPA04006679A (es) | 2002-01-08 | 2004-11-10 | Lilly Co Eli | Analogos extendidos de peptido-1 de tipo glucagon. |
| US20030232761A1 (en) | 2002-03-28 | 2003-12-18 | Hinke Simon A. | Novel analogues of glucose-dependent insulinotropic polypeptide |
| AU2003239478A1 (en) | 2002-06-04 | 2003-12-22 | Eli Lilly And Company | Modified glucagon-like peptide-1 analogs |
| EP1515746A2 (en) | 2002-06-11 | 2005-03-23 | Eisai Co. Ltd | Use of compounds having gip activity for the treatment of disorders associated with abnormal loss of cells and/or for the treatment of obesity |
| AU2003248676A1 (en) | 2002-06-15 | 2003-12-31 | Enteromed, Inc. | Treatment of non-alcoholic fatty liver disease |
| JP2006501820A (ja) | 2002-09-06 | 2006-01-19 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 修飾ｇｌｐ−１受容体アゴニストおよびそれらの薬理学的使用法 |
| US7192922B2 (en) | 2002-11-19 | 2007-03-20 | Allegheny-Singer Research Institute | Method of treating left ventricular dysfunction |
| JP2006524039A (ja) | 2003-01-09 | 2006-10-26 | マクロジェニクス，インコーポレーテッド | 変異型Ｆｃ領域を含む抗体の同定および作製ならびにその利用法 |
| US20050059605A1 (en) | 2003-01-31 | 2005-03-17 | Krishna Peri | Chemically modified metabolites of regulatory peptides and methods of producing and using same |
| WO2004078777A2 (en) | 2003-03-04 | 2004-09-16 | Biorexis Pharmaceutical Corporation | Dipeptidyl-peptidase protected proteins |
| EP1605897B1 (en) | 2003-03-19 | 2012-07-25 | Eli Lilly And Company | Polyethelene glycol link glp-1 compounds |
| CA2521784C (en) | 2003-04-08 | 2012-03-27 | Yeda Research And Development Co. Ltd. | Reversible pegylated drugs |
| TWI353991B (en) | 2003-05-06 | 2011-12-11 | Syntonix Pharmaceuticals Inc | Immunoglobulin chimeric monomer-dimer hybrids |
| AU2004240630B2 (en) | 2003-05-15 | 2010-10-07 | Trustees Of Tufts College | Stable analogs of peptide and polypeptide therapeutics |
| EP1633391B1 (en) | 2003-06-03 | 2011-10-19 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| CA2527743A1 (en) | 2003-06-03 | 2004-12-09 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| MXPA05013565A (es) | 2003-06-12 | 2006-03-09 | Lilly Co Eli | Proteinas de fusion analogas al glp-1. |
| US20050124550A1 (en) | 2003-06-18 | 2005-06-09 | Peri Krishna G. | Compounds that modulate the glucagon response and uses thereof |
| KR101241862B1 (ko) | 2003-09-19 | 2013-03-13 | 노보 노르디스크 에이/에스 | 신규 ｇｌｐ-1 유도체 |
| US7364875B2 (en) | 2003-10-30 | 2008-04-29 | Cresent Innovations, Inc. | Method for producing medical and commercial grade poly-gamma-glutamic acid of high molecular weight |
| MXPA06006745A (es) | 2003-12-18 | 2006-08-18 | Novo Nordisk As | Compuestos glp-1 novedosos. |
| US20060286129A1 (en) | 2003-12-19 | 2006-12-21 | Emisphere Technologies, Inc. | Oral GLP-1 formulations |
| US20080318837A1 (en) | 2003-12-26 | 2008-12-25 | Nastech Pharmaceutical Company Inc. | Pharmaceutical Formation For Increased Epithelial Permeability of Glucose-Regulating Peptide |
| KR20070090036A (ko) | 2004-12-22 | 2007-09-04 | 센토코 인코포레이티드 | Ｇｌｐ-1 작용제, 조성물, 방법 및 용도 |
| BRPI0606992A2 (pt) | 2005-02-11 | 2009-07-28 | Amylin Pharmaceuticals Inc | análogo e polipeptìdeos hìbridos de gip com propriedades selecionáveis |
| WO2006097536A2 (en) | 2005-03-18 | 2006-09-21 | Novo Nordisk A/S | Dimeric peptide agonists of the glp-1 receptor |
| WO2006121904A1 (en) | 2005-05-06 | 2006-11-16 | Bayer Pharmaceuticals Corporation | Glucose-dependent insulinotropic polypeptide (gip) receptor agonists and their pharmacological methods of use |
| PT1881850E (pt) | 2005-05-13 | 2010-11-26 | Lilly Co Eli | Compostos peguilados de glp-1 |
| RU2485135C2 (ru) | 2005-06-13 | 2013-06-20 | Импиэриэл Инноувейшнс Лимитид | Соединения оксинтомодулина (варианты), фармацевтическая композиция на их основе, способы лечения и профилактики ожирения и сопутствующих заболеваний (варианты) и лекарственное средство (варианты) |
| EP2330124B1 (en) | 2005-08-11 | 2015-02-25 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
| BRPI0615573A2 (pt) | 2005-09-08 | 2011-05-24 | Tufts College | análogos de glp-1 estabilizados |
| EP1943274A2 (en) | 2005-09-08 | 2008-07-16 | Uutech Limited | Treatment of diabetes related obesity |
| US20090286722A1 (en) | 2005-09-08 | 2009-11-19 | Utech Limited | Analogs of Gastric Inhibitory Polypeptide as a Treatment for Age Related Decreased Pancreatic Beta Cell Function |
| US7846445B2 (en) | 2005-09-27 | 2010-12-07 | Amunix Operating, Inc. | Methods for production of unstructured recombinant polymers and uses thereof |
| EP2570133B1 (en) | 2005-11-07 | 2016-03-23 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| CN101389648B (zh) | 2006-02-22 | 2013-07-17 | 默沙东公司 | 肽胃泌酸调节素衍生物 |
| JP5312054B2 (ja) | 2006-03-15 | 2013-10-09 | ノボ・ノルデイスク・エー／エス | アミリンとインスリンの混合物 |
| WO2007109354A2 (en) | 2006-03-21 | 2007-09-27 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| ES2495741T3 (es) | 2006-04-20 | 2014-09-17 | Amgen, Inc | Compuestos de GLP-1 |
| US20080031957A1 (en) | 2006-05-15 | 2008-02-07 | Deluca Hector F | Pulmonary delivery of 1alpha,25-dihydroxyvitamin D3 and co-administration of parathyroid hormone or calcitonin |
| FR2902092B1 (fr) | 2006-06-07 | 2008-09-05 | Sapelem Soc Par Actions Simpli | Appareil de manutention de charge |
| WO2008022015A2 (en) | 2006-08-11 | 2008-02-21 | Trustees Of Tufts College | Retro-inverso incretin analogues, and methods of use thereof |
| AU2007284365A1 (en) | 2006-08-17 | 2008-02-21 | Amylin Pharmaceuticals, Inc. | DPP-IV resistant GIP hybrid polypeptides with selectable properties |
| US20090318353A1 (en) | 2006-08-25 | 2009-12-24 | Novo Nordisk A/S | Acylated Exendin-4 Compounds |
| CN106008699A (zh) | 2006-09-08 | 2016-10-12 | Ambrx公司 | 经修饰的人类血浆多肽或Fc骨架和其用途 |
| US8617531B2 (en) | 2006-12-14 | 2013-12-31 | Bolder Biotechnology, Inc. | Methods of making proteins and peptides containing a single free cysteine |
| RU2477286C2 (ru) | 2007-01-05 | 2013-03-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | АНАЛОГИ ГЛЮКАГОНА, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ В БУФЕРАХ С ФИЗИОЛОГИЧЕСКИМ ЗНАЧЕНИЕМ pH |
| AU2008216265B2 (en) | 2007-02-15 | 2014-04-03 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| US8933197B2 (en) | 2007-08-15 | 2015-01-13 | Amunix Operating Inc. | Compositions comprising modified biologically active polypeptides |
| EP2190872B1 (en) | 2007-09-05 | 2018-03-14 | Novo Nordisk A/S | Glucagon-like peptide-1 derivatives and their pharmaceutical use |
| WO2009030774A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Truncated glp-1 derivatives and their therapeutical use |
| US20100256056A1 (en) | 2007-09-07 | 2010-10-07 | Zheng Xin Dong | Analogues of exendin-4 and exendin-3 |
| US20100222251A1 (en) | 2007-09-11 | 2010-09-02 | Novo Nordisk A/S | Mixture comprising an amylin peptide and a protracted insulin |
| EP2036539A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Stable formulations of amylin and its analogues |
| EP2036923A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Improved derivates of amylin |
| WO2009058662A2 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| US8980830B2 (en) | 2007-10-30 | 2015-03-17 | Indiana University Research And Technology Corporation | Peptide compounds exhibiting glucagon antagonist and GLP-1 agonist activity |
| ES2448839T3 (es) | 2007-11-01 | 2014-03-17 | Bristol-Myers Squibb Company | Compuestos no esteroideos útiles como moderadores de la actividad del receptor de glucocorticoides AP-1 y/o NF-kappa b y uso de los mismos |
| AU2009210570B2 (en) | 2008-01-30 | 2014-11-20 | Indiana University Research And Technology Corporation | Ester-based insulin prodrugs |
| MX2010008024A (es) | 2008-02-01 | 2010-12-21 | Ascendis Pharma As | Profarmaco que comprende un enlazador que se puede separar por si mismo. |
| WO2009155257A1 (en) | 2008-06-17 | 2009-12-23 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability physiological ph buffers |
| DK2300035T3 (en) | 2008-06-17 | 2015-11-16 | Univ Indiana Res & Tech Corp | Mixed GIP-based agonists for the treatment of metabolic diseases and obesity |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| EP2303890A4 (en) | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| JP5643762B2 (ja) | 2008-10-15 | 2014-12-17 | インターシア セラピューティクス，インコーポレイティド | 高濃度薬物粒子、製剤、懸濁液、及びこれらの使用 |
| CN102300580A (zh) | 2008-12-19 | 2011-12-28 | 印第安纳大学研究及科技有限公司 | 二肽连接的药剂 |
| CN102325539A (zh) | 2008-12-19 | 2012-01-18 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
| WO2010096052A1 (en) | 2009-02-19 | 2010-08-26 | Merck Sharp & Dohme Corp. | Oxyntomodulin analogs |
| WO2010148089A1 (en) | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| US20110009347A1 (en) | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| US8703701B2 (en) | 2009-12-18 | 2014-04-22 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| AR079345A1 (es) | 2009-12-22 | 2012-01-18 | Lilly Co Eli | Analogo peptidico de oxintomodulina |
| AR079344A1 (es) | 2009-12-22 | 2012-01-18 | Lilly Co Eli | Analogo peptidico de oxintomodulina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar diabetes no insulinodependiente y/u obesidad |
| EP2528618A4 (en) | 2010-01-27 | 2015-05-27 | Univ Indiana Res & Tech Corp | GLUCAGON ANTAGONISTE AND GIP AGONISTS CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLISM DISEASES AND ADIPOSITAS |
| AR080592A1 (es) | 2010-03-26 | 2012-04-18 | Lilly Co Eli | Peptido con actividad para el gip-r y glp-1-r, formulacion famaceutica que lo comprende, su uso para preparar un medicamento util para el tratamiento de diabetes mellitus y para inducir la perdida de peso |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| CA2797095A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity |
| RU2580317C2 (ru) | 2010-06-24 | 2016-04-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов |
| WO2011163473A1 (en) | 2010-06-25 | 2011-12-29 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability in physiological ph buffers |
-
2011
- 2011-05-10 CA CA 2797095 patent/CA2797095A1/en not_active Abandoned
- 2011-05-10 CN CN201180037112.9A patent/CN103079587B/zh not_active Expired - Fee Related
- 2011-05-10 EP EP11781137.2A patent/EP2569000B1/en not_active Not-in-force
- 2011-05-10 BR BR112012028704A patent/BR112012028704A2/pt not_active IP Right Cessation
- 2011-05-10 US US13/697,018 patent/US9127088B2/en not_active Expired - Fee Related
- 2011-05-10 RU RU2012153755/04A patent/RU2604067C2/ru not_active IP Right Cessation
- 2011-05-10 KR KR20127029663A patent/KR20130062931A/ko not_active Ceased
- 2011-05-10 JP JP2013510240A patent/JP6121323B2/ja active Active
- 2011-05-10 MX MX2012013001A patent/MX2012013001A/es active IP Right Grant
- 2011-05-10 WO PCT/US2011/035913 patent/WO2011143209A1/en not_active Ceased
- 2011-05-10 ES ES11781137.2T patent/ES2661228T3/es active Active
- 2011-05-12 AR ARP110101649 patent/AR081043A1/es unknown
-
2015
- 2015-07-24 US US14/808,668 patent/US9783592B2/en not_active Expired - Fee Related
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