HRP20040343A2 - Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions - Google Patents
Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditionsInfo
- Publication number
- HRP20040343A2 HRP20040343A2 HR20040343A HRP20040343A HRP20040343A2 HR P20040343 A2 HRP20040343 A2 HR P20040343A2 HR 20040343 A HR20040343 A HR 20040343A HR P20040343 A HRP20040343 A HR P20040343A HR P20040343 A2 HRP20040343 A2 HR P20040343A2
- Authority
- HR
- Croatia
- Prior art keywords
- bip
- phe
- group
- alkyl
- amino acid
- Prior art date
Links
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical class 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 title claims description 52
- 238000011282 treatment Methods 0.000 title claims description 24
- 206010012601 diabetes mellitus Diseases 0.000 title claims description 14
- 101500028774 Homo sapiens Glucagon-like peptide 1 Proteins 0.000 title description 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 212
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical group OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 206
- -1 hydroxy, mercapto Chemical class 0.000 claims description 186
- 125000000217 alkyl group Chemical group 0.000 claims description 129
- 125000000539 amino acid group Chemical group 0.000 claims description 128
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 117
- 229910052739 hydrogen Inorganic materials 0.000 claims description 112
- 229910052799 carbon Inorganic materials 0.000 claims description 107
- 238000006467 substitution reaction Methods 0.000 claims description 107
- 239000001257 hydrogen Substances 0.000 claims description 100
- 229920001184 polypeptide Polymers 0.000 claims description 87
- 238000000034 method Methods 0.000 claims description 81
- 150000001875 compounds Chemical class 0.000 claims description 80
- 150000002431 hydrogen Chemical group 0.000 claims description 68
- 125000000623 heterocyclic group Chemical group 0.000 claims description 65
- 125000003118 aryl group Chemical group 0.000 claims description 63
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 62
- 125000001072 heteroaryl group Chemical group 0.000 claims description 62
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 54
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 51
- 125000001424 substituent group Chemical group 0.000 claims description 50
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 claims description 44
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 42
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 38
- 150000001413 amino acids Chemical class 0.000 claims description 36
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 35
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 33
- 239000003112 inhibitor Substances 0.000 claims description 33
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 29
- 230000000694 effects Effects 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 27
- 150000002367 halogens Chemical class 0.000 claims description 27
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 27
- JCZLABDVDPYLRZ-AWEZNQCLSA-N biphenylalanine Chemical group C1=CC(C[C@H](N)C(O)=O)=CC=C1C1=CC=CC=C1 JCZLABDVDPYLRZ-AWEZNQCLSA-N 0.000 claims description 26
- 229940124530 sulfonamide Drugs 0.000 claims description 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 25
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical group OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 23
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical group OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims description 23
- 125000003368 amide group Chemical group 0.000 claims description 23
- 150000003456 sulfonamides Chemical class 0.000 claims description 23
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims description 22
- 150000003857 carboxamides Chemical class 0.000 claims description 22
- 239000003795 chemical substances by application Substances 0.000 claims description 22
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 22
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 21
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical group OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims description 20
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 20
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical group OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 20
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 18
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 claims description 18
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 17
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 17
- 125000003342 alkenyl group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 16
- 125000004104 aryloxy group Chemical group 0.000 claims description 16
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 16
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 16
- 125000000304 alkynyl group Chemical group 0.000 claims description 15
- LJLSJYDMNNKCHK-UHFFFAOYSA-N (diaminomethylideneamino)-diazonioazanide Chemical compound NC(=N)NN=[N+]=[N-] LJLSJYDMNNKCHK-UHFFFAOYSA-N 0.000 claims description 14
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical group C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims description 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 14
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 14
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims description 13
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 125000004442 acylamino group Chemical group 0.000 claims description 12
- 125000004423 acyloxy group Chemical group 0.000 claims description 12
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 12
- 125000004470 heterocyclooxy group Chemical group 0.000 claims description 12
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 11
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 11
- 229910052757 nitrogen Inorganic materials 0.000 claims description 11
- 239000000018 receptor agonist Substances 0.000 claims description 11
- 229940044601 receptor agonist Drugs 0.000 claims description 11
- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical group C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 claims description 10
- 239000003524 antilipemic agent Substances 0.000 claims description 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 125000004963 sulfonylalkyl group Chemical group 0.000 claims description 10
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims description 9
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims description 9
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims description 9
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical group NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 9
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 9
- 239000004202 carbamide Substances 0.000 claims description 9
- 239000000126 substance Substances 0.000 claims description 9
- 102000004877 Insulin Human genes 0.000 claims description 8
- 108090001061 Insulin Proteins 0.000 claims description 8
- SNDPXSYFESPGGJ-UHFFFAOYSA-N L-norVal-OH Natural products CCCC(N)C(O)=O SNDPXSYFESPGGJ-UHFFFAOYSA-N 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 102000005962 receptors Human genes 0.000 claims description 8
- 108020003175 receptors Proteins 0.000 claims description 8
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 8
- 239000000556 agonist Substances 0.000 claims description 7
- 150000001414 amino alcohols Chemical class 0.000 claims description 7
- 239000000883 anti-obesity agent Substances 0.000 claims description 7
- 229940125710 antiobesity agent Drugs 0.000 claims description 7
- 125000004122 cyclic group Chemical group 0.000 claims description 7
- 229940125396 insulin Drugs 0.000 claims description 7
- 201000001320 Atherosclerosis Diseases 0.000 claims description 6
- CKLJMWTZIZZHCS-UHFFFAOYSA-N D-OH-Asp Natural products OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 claims description 6
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical group C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims description 6
- CKLJMWTZIZZHCS-UWTATZPHSA-N D-aspartic acid Chemical compound OC(=O)[C@H](N)CC(O)=O CKLJMWTZIZZHCS-UWTATZPHSA-N 0.000 claims description 6
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims description 6
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical group C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 6
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 6
- 108010016731 PPAR gamma Proteins 0.000 claims description 6
- 230000003178 anti-diabetic effect Effects 0.000 claims description 6
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- 239000003937 drug carrier Substances 0.000 claims description 6
- JBKVHLHDHHXQEQ-UHFFFAOYSA-N epsilon-caprolactam Chemical compound O=C1CCCCCN1 JBKVHLHDHHXQEQ-UHFFFAOYSA-N 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
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- 101100268670 Caenorhabditis elegans acc-3 gene Proteins 0.000 claims description 5
- DCXYFEDJOCDNAF-UWTATZPHSA-N D-Asparagine Chemical compound OC(=O)[C@H](N)CC(N)=O DCXYFEDJOCDNAF-UWTATZPHSA-N 0.000 claims description 5
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 claims description 5
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 5
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical group OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims description 5
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims description 5
- 108010028924 PPAR alpha Proteins 0.000 claims description 5
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- 125000000267 glycino group Chemical group [H]N([*])C([H])([H])C(=O)O[H] 0.000 claims description 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 5
- 125000005358 mercaptoalkyl group Chemical group 0.000 claims description 5
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 5
- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical compound CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 claims description 5
- 229960001243 orlistat Drugs 0.000 claims description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 5
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- 239000004059 squalene synthase inhibitor Substances 0.000 claims description 5
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 5
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- KAFHLONDOVSENM-HNNXBMFYSA-N O-Benzyl-L-tyrosine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1OCC1=CC=CC=C1 KAFHLONDOVSENM-HNNXBMFYSA-N 0.000 claims description 4
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- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims description 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 4
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims description 4
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
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- 125000005026 carboxyaryl group Chemical group 0.000 claims description 4
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- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims description 3
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- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims description 3
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- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
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- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34201501P | 2001-10-18 | 2001-10-18 | |
| PCT/US2002/033386 WO2003033671A2 (en) | 2001-10-18 | 2002-10-18 | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20040343A2 true HRP20040343A2 (en) | 2005-08-31 |
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| Application Number | Title | Priority Date | Filing Date |
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| HR20040343A HRP20040343A2 (en) | 2001-10-18 | 2004-04-15 | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
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| US (3) | US7238670B2 (ko) |
| EP (1) | EP1572892A4 (ko) |
| JP (1) | JP2005514337A (ko) |
| KR (1) | KR20040054729A (ko) |
| CN (1) | CN1630709A (ko) |
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| BR (1) | BR0213377A (ko) |
| CA (1) | CA2463908A1 (ko) |
| GE (1) | GEP20063908B (ko) |
| HR (1) | HRP20040343A2 (ko) |
| HU (1) | HUP0700151A2 (ko) |
| IL (1) | IL160917A0 (ko) |
| IS (1) | IS7185A (ko) |
| MX (1) | MXPA04003553A (ko) |
| NO (1) | NO20041203L (ko) |
| NZ (1) | NZ531788A (ko) |
| PL (1) | PL377687A1 (ko) |
| RU (1) | RU2353625C2 (ko) |
| WO (1) | WO2003033671A2 (ko) |
| YU (1) | YU31004A (ko) |
| ZA (1) | ZA200402846B (ko) |
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| US7238671B2 (en) | 2001-10-18 | 2007-07-03 | Bristol-Myers Squibb Company | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
| NZ531788A (en) | 2001-10-18 | 2008-01-31 | Bristol Myers Squibb Co | Human glucagon-like-peptide-1 mimics and their use in the treatment of diabetes and related conditions |
| WO2004022083A1 (en) * | 2002-09-04 | 2004-03-18 | Dsm Ip Assets B.V. | A nutritional and therapeutic composition of an insulin sensitizer and a peptide fraction |
| ES2737835T3 (es) | 2003-04-23 | 2020-01-16 | Valeritas Inc | Bomba accionada hidráulicamente para la administración de medicamentos de larga duración |
| CN104826116A (zh) | 2003-11-20 | 2015-08-12 | 诺沃挪第克公司 | 对于生产和用于注射装置中是最佳的含有丙二醇的肽制剂 |
| AR047776A1 (es) * | 2003-12-16 | 2006-02-22 | Sod Conseils Rech Applic | Composiciones farmaceuticas glp - 1 |
| CA2568640C (en) | 2004-06-04 | 2011-08-09 | Teva Pharmaceutical Industries Ltd. | Pharmaceutical composition containing irbesartan |
| US7534763B2 (en) | 2004-07-02 | 2009-05-19 | Bristol-Myers Squibb Company | Sustained release GLP-1 receptor modulators |
| TW200611704A (en) * | 2004-07-02 | 2006-04-16 | Bristol Myers Squibb Co | Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions |
| US20070021346A1 (en) * | 2005-05-26 | 2007-01-25 | Ewing William R | N-terminally modified GLP-1 receptor modulators |
| US7145040B2 (en) * | 2004-07-02 | 2006-12-05 | Bristol-Myers Squibb Co. | Process for the preparation of amino acids useful in the preparation of peptide receptor modulators |
| WO2006014425A1 (en) * | 2004-07-02 | 2006-02-09 | Biovalve Technologies, Inc. | Methods and devices for delivering glp-1 and uses thereof |
| AR051446A1 (es) | 2004-09-23 | 2007-01-17 | Bristol Myers Squibb Co | Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2) |
| US7589088B2 (en) | 2004-12-29 | 2009-09-15 | Bristol-Myers Squibb Company | Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| US7635699B2 (en) | 2004-12-29 | 2009-12-22 | Bristol-Myers Squibb Company | Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| DOP2006000008A (es) * | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| US7521557B2 (en) | 2005-05-20 | 2009-04-21 | Bristol-Myers Squibb Company | Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods |
| WO2007030519A2 (en) * | 2005-09-08 | 2007-03-15 | Trustees Of Tufts College | Stabilized glp-1 analogs |
| NZ566799A (en) | 2005-09-14 | 2011-04-29 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors for treating diabetes |
| CN101360723A (zh) | 2005-09-16 | 2009-02-04 | 武田药品工业株式会社 | 制备嘧啶二酮衍生物的方法 |
| EP1943215A2 (en) | 2005-10-31 | 2008-07-16 | Brystol-Myers Squibb Company | Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase iv and methods |
| WO2007051987A1 (en) * | 2005-11-01 | 2007-05-10 | Activotec Spp Limited | Insulinotropic compounds and uses thereof |
| CA2913805A1 (en) * | 2005-11-07 | 2007-05-18 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| EP1976873A2 (en) * | 2006-01-11 | 2008-10-08 | Brystol-Myers Squibb Company | Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions |
| CN101389648B (zh) * | 2006-02-22 | 2013-07-17 | 默沙东公司 | 肽胃泌酸调节素衍生物 |
| PE20080168A1 (es) * | 2006-03-23 | 2008-02-25 | Bristol Myers Squibb Co | Preparacion enzimatica de (s)-aminoacido a partir del (r,s)-aminoacido o a partir del ceto acido |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| ES2566058T3 (es) | 2006-03-30 | 2016-04-08 | Valeritas, Inc. | Dispositivo de suministro de fluidos de múltiples cartuchos |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| WO2007120689A2 (en) | 2006-04-11 | 2007-10-25 | Arena Pharmaceuticals, Inc. | Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual |
| WO2007124463A1 (en) * | 2006-04-20 | 2007-11-01 | Amgen Inc. | Glp-1 compound/glucagon antibody compositions |
| WO2007139589A1 (en) * | 2006-05-26 | 2007-12-06 | Bristol-Myers Squibb Company | Sustained release glp-1 receptor modulators |
| US7919598B2 (en) | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| US20080044326A1 (en) * | 2006-07-04 | 2008-02-21 | Esencia Co., Ltd. | Sterilizer for baby products |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| PE20121528A1 (es) | 2006-09-13 | 2012-12-12 | Smithkline Beecham Corp | Metodos para administrar agentes hipoglucemiantes de larga duracion |
| AU2007323035B2 (en) * | 2006-10-03 | 2011-11-24 | Cadila Healthcare Limited | Antidiabetic compounds |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| EP2124974B1 (en) * | 2007-01-05 | 2017-03-15 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
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2002
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- 2002-10-18 BR BRPI0213377-6A patent/BR0213377A/pt not_active IP Right Cessation
- 2002-10-18 PL PL377687A patent/PL377687A1/pl not_active Application Discontinuation
- 2002-10-18 HU HU0700151A patent/HUP0700151A2/hu unknown
- 2002-10-18 MX MXPA04003553A patent/MXPA04003553A/es active IP Right Grant
- 2002-10-18 CN CNA028205588A patent/CN1630709A/zh active Pending
- 2002-10-18 AU AU2002348469A patent/AU2002348469B2/en not_active Ceased
- 2002-10-18 US US10/273,975 patent/US7238670B2/en not_active Expired - Lifetime
-
2004
- 2004-03-16 IS IS7185A patent/IS7185A/is unknown
- 2004-03-23 NO NO20041203A patent/NO20041203L/no not_active Application Discontinuation
- 2004-04-15 ZA ZA200402846A patent/ZA200402846B/en unknown
- 2004-04-15 HR HR20040343A patent/HRP20040343A2/hr not_active Application Discontinuation
-
2007
- 2007-04-25 US US11/740,031 patent/US20070287670A1/en not_active Abandoned
-
2010
- 2010-04-30 US US12/771,096 patent/US20100210552A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2463908A1 (en) | 2003-04-24 |
| JP2005514337A (ja) | 2005-05-19 |
| BR0213377A (pt) | 2006-05-23 |
| CN1630709A (zh) | 2005-06-22 |
| US20100210552A1 (en) | 2010-08-19 |
| EP1572892A4 (en) | 2007-08-22 |
| NZ531788A (en) | 2008-01-31 |
| US7238670B2 (en) | 2007-07-03 |
| US20070287670A1 (en) | 2007-12-13 |
| ZA200402846B (en) | 2005-08-16 |
| PL377687A1 (pl) | 2006-02-06 |
| KR20040054729A (ko) | 2004-06-25 |
| WO2003033671A3 (en) | 2005-12-29 |
| RU2353625C2 (ru) | 2009-04-27 |
| IS7185A (is) | 2004-03-16 |
| NO20041203L (no) | 2004-06-10 |
| WO2003033671A2 (en) | 2003-04-24 |
| GEP20063908B (en) | 2006-08-25 |
| EP1572892A2 (en) | 2005-09-14 |
| US20030195157A1 (en) | 2003-10-16 |
| HUP0700151A2 (en) | 2007-05-29 |
| IL160917A0 (en) | 2004-08-31 |
| YU31004A (sh) | 2006-08-17 |
| AU2002348469B2 (en) | 2008-03-13 |
| RU2004114836A (ru) | 2005-04-10 |
| MXPA04003553A (es) | 2004-07-22 |
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