JP2013534906A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2569000B1 (enExample) |
| JP (1) | JP6121323B2 (enExample) |
| KR (1) | KR20130062931A (enExample) |
| CN (1) | CN103079587B (enExample) |
| AR (1) | AR081043A1 (enExample) |
| BR (1) | BR112012028704A2 (enExample) |
| CA (1) | CA2797095A1 (enExample) |
| ES (1) | ES2661228T3 (enExample) |
| MX (1) | MX2012013001A (enExample) |
| RU (1) | RU2604067C2 (enExample) |
| WO (1) | WO2011143209A1 (enExample) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2628241C (en) | 2005-11-07 | 2016-02-02 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| CN101578102B (zh) | 2007-01-05 | 2013-07-17 | 印第安纳大学研究及科技有限公司 | 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物 |
| MX2009008241A (es) | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| JP5631201B2 (ja) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ステッチングされたポリペプチド |
| CA2707861A1 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| JP5771005B2 (ja) | 2007-10-30 | 2015-08-26 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ | グルカゴンアンタゴニスト及びｇｌｐ−１アゴニスト活性を示す化合物 |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| TWI541023B (zh) | 2008-06-17 | 2016-07-11 | 印第安納大學科技研究公司 | 在生理ｐｈ緩衝液中呈現增強之溶解度及穩定性之升糖激素類似物 |
| TWI474835B (zh) | 2008-06-17 | 2015-03-01 | Univ Indiana Res & Tech Corp | 用於治療代謝病症及肥胖症之基於ｇｉｐ之混合激動劑 |
| RU2550696C2 (ru) | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
| 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 |
| MX2012014576A (es) | 2010-06-24 | 2013-02-21 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida. |
| KR102104762B1 (ko) | 2010-08-13 | 2020-04-24 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티도미메틱 거대고리 |
| WO2012088116A2 (en) | 2010-12-22 | 2012-06-28 | 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 |
| CN103857408B (zh) | 2011-06-22 | 2017-04-12 | 印第安那大学科技研究公司 | 胰高血糖素/glp‑1受体协同激动剂 |
| MX2013015168A (es) | 2011-06-22 | 2014-03-31 | Univ Indiana Res & Tech Corp | Co-agonista del receptor de glucagon/glp-1. |
| EP2768518A4 (en) | 2011-10-18 | 2015-05-27 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES |
| HK1198810A1 (en) | 2011-11-17 | 2015-06-12 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting glucocorticoid receptor activity |
| RU2642299C2 (ru) | 2012-02-15 | 2018-01-24 | Эйлерон Терапьютикс, Инк. | P53 пептидомиметические макроциклы |
| CA2864120A1 (en) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| EP2827883B1 (en) | 2012-03-21 | 2019-05-08 | Baxalta GmbH | Tfpi inhibitors and methods of use |
| SG11201407860PA (en) * | 2012-06-14 | 2014-12-30 | Sanofi Sa | Exendin-4 peptide analogues |
| CN104583233B (zh) * | 2012-06-21 | 2018-10-23 | 印第安纳大学研究及科技有限公司 | 表现出gip受体活性的胰高血糖素的类似物 |
| US9340600B2 (en) | 2012-06-21 | 2016-05-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| WO2014057687A1 (ja) | 2012-10-11 | 2014-04-17 | 第一三共株式会社 | 抗体－薬物コンジュゲート |
| WO2014061277A1 (ja) | 2012-10-19 | 2014-04-24 | 第一三共株式会社 | 親水性構造を含むリンカーで結合させた抗体－薬物コンジュゲート |
| BR112015009470A2 (pt) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | aminoácidos dissubstituídos e seus métodos de preparação e uso |
| TWI674270B (zh) * | 2012-12-11 | 2019-10-11 | 英商梅迪繆思有限公司 | 用於治療肥胖之升糖素與glp-1共促效劑 |
| JP2016506401A (ja) | 2012-12-21 | 2016-03-03 | サノフイ | 二重ｇｌｐ１／ｇｉｐまたは三方ｇｌｐ１／ｇｉｐ／グルカゴンアゴニストとしてのエキセンジン−４誘導体 |
| AU2014230472A1 (en) * | 2013-03-14 | 2015-10-01 | Medimmune Limited | Pegylated glucagon and GLP-1 co-agonists for the treatment of obesity |
| CA2909941A1 (en) | 2013-04-24 | 2014-10-30 | Salk Institute For Biological Studies | Vitamin d receptor/smad genomic circuit gates fibrotic response |
| BR112015030518A2 (pt) | 2013-06-05 | 2017-08-29 | Salk Inst For Biological Studi | Composição farmacêutica, uso de um ou mais agonistas do receptor da vitamina d (vdr), e, método para a redução da atividade biológica do ligante 12 do motivo c-x-c (cxcl12) |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| TW201609799A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／ｇｉｐ受體促效劑 |
| TW201609796A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 非醯化之艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物 |
| EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | 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 |
| PT3088419T (pt) | 2013-12-25 | 2019-01-11 | Daiichi Sankyo Co Ltd | Conjugado de anticorpo anti-trop2-fármaco |
| HRP20190431T1 (hr) | 2014-01-31 | 2019-04-19 | Daiichi Sankyo Company, Limited | Anti-her2 antitijelo-lijek konjugat |
| 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 |
| 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 |
| 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 |
| ES2754348T3 (es) | 2014-04-10 | 2020-04-17 | Daiichi Sankyo Co Ltd | Conjugado de (anticuerpo anti-HER2)-fármaco |
| CN111228511B (zh) | 2014-04-10 | 2024-06-18 | 第一三共株式会社 | 抗her3抗体-药物偶联物 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| EP3197478A4 (en) | 2014-09-24 | 2018-05-30 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| WO2016093599A1 (ko) | 2014-12-08 | 2016-06-16 | 재단법인 아산사회복지재단 | 박테로이데스 에시디페시언스를 유효성분으로 포함하는, 대사성 질환 예방 또는 치료용 약학적 조성물 |
| JP2018516844A (ja) | 2015-03-20 | 2018-06-28 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | ペプチド模倣大環状分子およびその使用 |
| 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 |
| CN116059395A (zh) | 2015-06-29 | 2023-05-05 | 第一三共株式会社 | 用于选择性制造抗体-药物缀合物的方法 |
| TW201706291A (zh) | 2015-07-10 | 2017-02-16 | 賽諾菲公司 | 作為選擇性肽雙重ｇｌｐ－１／升糖素受體促效劑之新毒蜥外泌肽（ｅｘｅｎｄｉｎ－４）衍生物 |
| 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 |
| EP3393496B1 (en) | 2015-12-23 | 2023-10-11 | The Johns Hopkins University | Long-acting glp-1r agonist as a therapy of neurological and neurodegenerative conditions |
| 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 |
| KR102706686B1 (ko) * | 2016-05-06 | 2024-09-19 | 아이오니스 파마수티컬즈, 인코포레이티드 | Glp-1 수용체 리간드 모이어티 컨쥬게이트된 올리고뉴클레오티드 및 이의 용도 |
| 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 |
| EP3552626A4 (en) | 2016-12-12 | 2020-06-10 | Daiichi Sankyo Company, Limited | ASSOCIATION OF AN ANTIBODY DRUG CONJUGATE AND AN IMMUNE CONTROL POINT INHIBITOR |
| EP3572428A4 (en) | 2017-01-17 | 2020-12-30 | Daiichi Sankyo Company, Limited | ANTI-BODY ANTI-GPR20 AND ANTI-BODY-DRUG CONJUGATE ANTI-GPR20 |
| TWI855528B (zh) | 2017-05-15 | 2024-09-11 | 日商第一三共股份有限公司 | 抗體-藥物結合物之製造方法 |
| 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 |
| JP7248578B2 (ja) | 2017-08-31 | 2023-03-29 | 第一三共株式会社 | 抗体－薬物コンジュゲートの新規製造方法 |
| KR20250084239A (ko) | 2017-08-31 | 2025-06-10 | 다이이찌 산쿄 가부시키가이샤 | 항체-약물 콘주게이트의 개량 제조 방법 |
| WO2019092618A2 (en) * | 2017-11-08 | 2019-05-16 | Ionis Pharmaceuticals, Inc | Glp-1 receptor ligand moiety conjugated oligonucleotides and uses thereof |
| RU2020136305A (ru) | 2018-05-04 | 2022-05-05 | Ново Нордиск А/С | Производные gip и пути их применения |
| HRP20240756T1 (hr) | 2018-05-18 | 2024-09-13 | Daiichi Sankyo Co., Ltd. | Anti-muc1-eksatekan antitijelo-lijek konjugat |
| 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 |
| EP3831412A4 (en) | 2018-07-31 | 2022-04-27 | Daiichi Sankyo Company, Limited | TREATMENT OF METASTATIC BRAIN TUMOR BY ADMINISTRATION OF AN ANTIBODY-DRUG CONJUGATE |
| 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 |
| BR112021012222A8 (pt) | 2018-12-21 | 2023-04-25 | Univ Berlin Charite | Molécula de ligação direcionada à célula melhorada |
| 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 |
| US20250161241A1 (en) * | 2022-03-02 | 2025-05-22 | Boyce Thompson Institute For Plant Research, Inc. | Cysteamides, therapeutic compositions thereof, and related methods |
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 |
| WO1987005330A1 (en) | 1986-03-07 | 1987-09-11 | Michel Louis Eugene Bergh | Method for enhancing glycoprotein stability |
| DE69020143T2 (de) | 1989-02-17 | 1996-01-25 | Chiron Mimotopes Pty Ltd | Verfahren zur verwendung und herstellung von peptiden. |
| 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 |
| IL121070A (en) | 1995-10-12 | 2004-06-20 | Supergen Inc | LIPOSOME FORMULATIONS OF 5beta STEROIDS |
| WO1997029180A1 (en) | 1996-02-06 | 1997-08-14 | Eli Lilly And Company | Diabetes therapy |
| EP0932614A1 (en) | 1996-09-09 | 1999-08-04 | 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 |
| AU5518798A (en) | 1996-12-03 | 1998-06-29 | Trustees Of Boston University | Specific antagonists for glucose-dependent insulinotropic polypeptide (gip) |
| AU757658B2 (en) | 1998-03-09 | 2003-02-27 | Zealand Pharma A/S | Pharmacologically active peptide conjugates having a reduced tendency towards enzymatic hydrolysis |
| US20030236190A1 (en) | 1998-09-02 | 2003-12-25 | Renuka Pillutla | Isulin and IGF-1 receptor agonists and antagonists |
| AU6294899A (en) | 1998-10-07 | 2000-04-26 | Medical College Of Georgia Research Institute, Inc. | Glucose-dependent insulinotropic peptide for use as an osteotropic hormone |
| 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 |
| DE60012721T4 (de) | 1999-03-29 | 2010-09-09 | Uutech Ltd., Coleraine | Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes |
| US7601691B2 (en) | 1999-05-17 | 2009-10-13 | Conjuchem Biotechnologies Inc. | Anti-obesity agents |
| SI1180121T1 (en) | 1999-05-17 | 2004-04-30 | Conjuchem, Inc. | Long lasting insulinotropic peptides |
| WO2001081919A2 (en) | 2000-04-27 | 2001-11-01 | Bionebraska, Inc. | Gastric inhibitory polypeptide diagnostic test for detecting susceptibility to type-2 diabetes, impaired glucose tolerance, or impaired fasting glucose |
| 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 |
| PT1695983E (pt) | 2000-06-16 | 2009-05-05 | Lilly Co Eli | Análogos do peptídeo-1 do tipo glucagon |
| EP1305338A2 (en) | 2000-08-02 | 2003-05-02 | 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 |
| US6528520B2 (en) | 2000-08-15 | 2003-03-04 | 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 |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| ATE516820T1 (de) | 2000-09-29 | 2011-08-15 | Schering Corp | Pegyliertes interleukin 10 |
| US7199217B2 (en) | 2000-12-13 | 2007-04-03 | Eli Lilly And Company | Amidated glucagon-like peptide-1 |
| JP2005501058A (ja) | 2001-07-31 | 2005-01-13 | ザ ガバメント オブ ザ ユナイテッドステイツ オブ アメリカ アズ リプレゼンテッド バイ ザ セクレタリー デパートメント オブ ヘルス アンド ヒューマン サービシーズ ザ ナショナル インステ | Ｇｌｐ−１、ｅｘｅｎｄｉｎ−４、そのペプチド・アナログ及びその使用 |
| AU2002327430A1 (en) | 2001-08-08 | 2003-02-24 | Genzyme Corporation | Methods for 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 |
| 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 |
| 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 |
| KR20040054729A (ko) | 2001-10-18 | 2004-06-25 | 브리스톨-마이어스 스큅 컴퍼니 | 인간 글루카곤-유사-펩티드-1 모방체, 및 당뇨병 및 이와관련된 증상의 치료에 있어서 이의 용도 |
| CA2463803A1 (en) | 2001-10-19 | 2003-05-01 | Eli Lilly And Company | Biphasic mixtures of glp-1 and insulin |
| AU2002351752A1 (en) | 2001-12-29 | 2003-07-30 | Novo Nordisk A/S | Combined use of a glp-1 compound and another drug for treating dyslipidemia |
| BR0306706A (pt) | 2002-01-08 | 2007-03-27 | Lilly Co Eli | peptìdeo glp-1 estendido, métodos de estimulação do receptor de glp-1 em um indivìduo necessitando de normalização de glicose sanguìnea, de tratamento de um indivìduo profilaticamente para diabetes independente de insulina, de redução ou de manutenção do peso corporal, de tratamento da obesidade, e de tratamento de doenças, em um indivìduo necessitando do mesmo, uso de um composto de glp-1, processo de preparação de uma formulação farmacêutica, e, formulação farmacêutica |
| 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 |
| CA2489323A1 (en) | 2002-06-15 | 2003-12-24 | 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 |
| EP2368578A1 (en) | 2003-01-09 | 2011-09-28 | Macrogenics, Inc. | Identification and engineering of antibodies with variant Fc regions and methods of using same |
| 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 |
| AU2004231461B2 (en) | 2003-03-19 | 2009-11-12 | Eli Lilly And Company | Polyethelene glycol linked 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 |
| CN1822851B (zh) | 2003-05-15 | 2011-04-13 | 塔夫茨大学信托人 | 肽和多肽药物的稳定类似物 |
| WO2004105781A2 (en) | 2003-06-03 | 2004-12-09 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| WO2004105790A1 (en) | 2003-06-03 | 2004-12-09 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| JP4629047B2 (ja) | 2003-06-12 | 2011-02-09 | イーライ リリー アンド カンパニー | Ｇｌｐ−１アナログ複合タンパク質 |
| WO2004111078A2 (en) | 2003-06-18 | 2004-12-23 | Theratechnologies Inc. | 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 |
| JP2007537141A (ja) | 2003-12-18 | 2007-12-20 | ノボ ノルディスク アクティーゼルスカブ | 新規なｇｌｐ−１化合物 |
| 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 |
| US20070128193A1 (en) | 2004-12-22 | 2007-06-07 | O'neil Karyn T | GLP-1 agonists, compositions, methods and uses |
| BRPI0606992A2 (pt) | 2005-02-11 | 2009-07-28 | Amylin Pharmaceuticals Inc | análogo e polipeptìdeos hìbridos de gip com propriedades selecionáveis |
| EP1863537A2 (en) | 2005-03-18 | 2007-12-12 | 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 |
| CN101166545B (zh) | 2005-05-13 | 2011-06-15 | 伊莱利利公司 | Glp-1聚乙二醇化的化合物 |
| CA2612063A1 (en) | 2005-06-13 | 2006-12-21 | Imperial Innovations Limited | Oxyntomodulin analogues and their effects on feeding behaviour |
| AU2006279680B2 (en) | 2005-08-11 | 2012-12-06 | Amylin Pharmaceuticals, Llc | Hybrid polypeptides with selectable properties |
| AU2006289259A1 (en) | 2005-09-08 | 2007-03-15 | Uutech Limited | Analogs of gastric inhibitory polypeptide as a treatment for age related decreased pancreatic beta cell function |
| KR20080052649A (ko) | 2005-09-08 | 2008-06-11 | 트러스티즈 오브 터프츠 칼리지 | 안정화된 ｇｌｐ―1 유사체 |
| WO2007028633A2 (en) | 2005-09-08 | 2007-03-15 | Uutech Limited | Treatment of diabetes related obesity |
| US7846445B2 (en) | 2005-09-27 | 2010-12-07 | Amunix Operating, Inc. | Methods for production of unstructured recombinant polymers and uses thereof |
| CA2628241C (en) | 2005-11-07 | 2016-02-02 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| EP2471810A1 (en) | 2006-02-22 | 2012-07-04 | Merck Sharp & Dohme Corporation | Oxyntomodulin derivatives |
| US20090054305A1 (en) | 2006-03-15 | 2009-02-26 | Novo Nordisk A/S | Mixtures of Amylin and Insulin |
| EP2004238A2 (en) | 2006-03-21 | 2008-12-24 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| AU2007240313B2 (en) | 2006-04-20 | 2012-02-02 | Amgen Inc. | GLP-1 compounds |
| WO2007133747A2 (en) | 2006-05-15 | 2007-11-22 | Wisconsin Alumni Research Foundation | PULMONARY DELIVERY OF 1α,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 |
| WO2008021560A2 (en) | 2006-08-17 | 2008-02-21 | Amylin Pharmaceuticals, Inc. | Dpp-iv resistant gip hybrid polypeptides with selectable properties |
| EP2057189B1 (en) | 2006-08-25 | 2013-03-06 | Novo Nordisk A/S | Acylated exendin-4 compounds |
| WO2008030558A2 (en) | 2006-09-08 | 2008-03-13 | Ambrx, Inc. | Modified human plasma polypeptide or fc scaffolds and their uses |
| US8617531B2 (en) | 2006-12-14 | 2013-12-31 | Bolder Biotechnology, Inc. | Methods of making proteins and peptides containing a single free cysteine |
| CN101578102B (zh) | 2007-01-05 | 2013-07-17 | 印第安纳大学研究及科技有限公司 | 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物 |
| MX2009008241A (es) | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| MX2010001684A (es) | 2007-08-15 | 2010-04-21 | Amunix Inc | Composiciones y metodos para modificar propiedades de polipeptidos biologicamente activos. |
| ES2672770T3 (es) | 2007-09-05 | 2018-06-18 | Novo Nordisk A/S | Derivados del péptido-1 similar al glucagón y su uso farmacéutico |
| WO2009030774A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Truncated glp-1 derivatives and their therapeutical use |
| JP2010538069A (ja) | 2007-09-07 | 2010-12-09 | イプセン ファルマ ソシエテ パール アクシオン サンプリフィエ | エキセンディン−４およびエキセンディン−３の類似体 |
| EP2036923A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Improved derivates of amylin |
| EP2036539A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Stable formulations of amylin and its analogues |
| WO2009034117A1 (en) | 2007-09-11 | 2009-03-19 | Novo Nordisk A/S | Mixture comprising an amylin peptide and a protracted insulin |
| JP5771005B2 (ja) | 2007-10-30 | 2015-08-26 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ | グルカゴンアンタゴニスト及びｇｌｐ−１アゴニスト活性を示す化合物 |
| CA2707861A1 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| CN101910171A (zh) | 2007-11-01 | 2010-12-08 | 百时美施贵宝公司 | 可用作糖皮质激素受体AP-1和/或者NF-κB活性调节剂的非甾类化合物及其用途 |
| WO2009099763A1 (en) | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| CA2712224C (en) | 2008-02-01 | 2016-03-08 | Ascendis Pharma As | Prodrug comprising a drug linker conjugate |
| EP2300037B1 (en) | 2008-06-17 | 2016-03-30 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| TWI541023B (zh) | 2008-06-17 | 2016-07-11 | 印第安納大學科技研究公司 | 在生理ｐｈ緩衝液中呈現增強之溶解度及穩定性之升糖激素類似物 |
| TWI474835B (zh) | 2008-06-17 | 2015-03-01 | Univ Indiana Res & Tech Corp | 用於治療代謝病症及肥胖症之基於ｇｉｐ之混合激動劑 |
| EP2303890A4 (en) | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| KR101419583B1 (ko) | 2008-10-15 | 2014-07-25 | 인타르시아 세라퓨틱스 인코포레이티드 | 고농축 약물 입자, 제형, 현탁액 및 이들의 용도 |
| KR20110114568A (ko) | 2008-12-19 | 2011-10-19 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 디펩티드 링크된 약효 물질 |
| RU2550696C2 (ru) | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
| 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 |
| JO2976B1 (en) | 2009-12-22 | 2016-03-15 | ايلي ليلي اند كومباني | Axentomodulin polypeptide |
| 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 |
| CA2797095A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| MX2012014576A (es) | 2010-06-24 | 2013-02-21 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida. |
| 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 ES ES11781137.2T patent/ES2661228T3/es active Active
- 2011-05-10 KR KR20127029663A patent/KR20130062931A/ko not_active Ceased
- 2011-05-10 RU RU2012153755/04A patent/RU2604067C2/ru not_active IP Right Cessation
- 2011-05-10 JP JP2013510240A patent/JP6121323B2/ja active Active
- 2011-05-10 BR BR112012028704A patent/BR112012028704A2/pt not_active IP Right Cessation
- 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 WO PCT/US2011/035913 patent/WO2011143209A1/en not_active Ceased
- 2011-05-10 MX MX2012013001A patent/MX2012013001A/es active IP Right Grant
- 2011-05-10 US US13/697,018 patent/US9127088B2/en not_active Expired - Fee Related
- 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
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013533849A5 (enExample) | ||
| CA2797095A1 (en) | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity | |
| RU2012153753A (ru) | Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов | |
| RU2014117678A (ru) | Пептиды глюкагонового суперсемейства, обладающие глюкокортикоидной рецепторной активностью | |
| JP2015504431A5 (enExample) | ||
| JP6538645B2 (ja) | インスリン‐インクレチン複合物 | |
| ES2822994T3 (es) | Conjugados de incretina-insulina | |
| JP6179864B2 (ja) | グルカゴン／ｇｌｐ−１レセプタコ−アゴニスト | |
| RU2580317C2 (ru) | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов | |
| JP2012512903A5 (enExample) | ||
| JP2011520847A (ja) | 遅効型ｙ２及び／又はｙ４レセプターアゴニスト | |
| WO2017210242A1 (en) | Insulin-nuclear hormone conjugates | |
| TW201143790A (en) | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity | |
| HK1183824A (en) | Amide based glucagon superfamily peptide prodrugs | |
| HK1183240A (en) | Glucagon superfamily peptides exhibiting nuclear hormone receptor activity | |
| HK1165711A (en) | Amide based glucagon superfamily peptide prodrugs |