JP2005514373A5 - - Google Patents
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- JP2005514373A5 JP2005514373A5 JP2003547365A JP2003547365A JP2005514373A5 JP 2005514373 A5 JP2005514373 A5 JP 2005514373A5 JP 2003547365 A JP2003547365 A JP 2003547365A JP 2003547365 A JP2003547365 A JP 2003547365A JP 2005514373 A5 JP2005514373 A5 JP 2005514373A5
- Authority
- JP
- Japan
- Prior art keywords
- benzyl
- hydroxypentyl
- benzamide
- formula
- alkyl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 21
- -1 3,3-dimethyl-butylcarbamoyl Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- WNTHNJJLRUXUSD-UHFFFAOYSA-N n-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C=1C=CC=CC=1C(=O)NN1CCCC1=O WNTHNJJLRUXUSD-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- PQNBMVYYZQSYKU-IMZWENMBSA-N 1-n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-n-methyl-5-(2-oxopyrrolidin-1-yl)-3-n-propylbenzene-1,3-dicarboxamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)C(=O)N(C)CCC)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)C1=CC=CC=C1 PQNBMVYYZQSYKU-IMZWENMBSA-N 0.000 claims 1
- DPPLEDWDEUCIBP-KSBJOJRMSA-N 3-[(4r)-4-benzyl-2-oxo-1,3-oxazolidin-3-yl]-n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C=C(C=CC=1)N1C(OC[C@H]1CC=1C=CC=CC=1)=O)C1=CC=CC=C1 DPPLEDWDEUCIBP-KSBJOJRMSA-N 0.000 claims 1
- HSMIQHKGVOFGKT-NWPQMPMLSA-N 3-acetamido-n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C=C(C=C(NC(C)=O)C=1)N1C(CCC1)=O)C1=CC=CC=C1 HSMIQHKGVOFGKT-NWPQMPMLSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- LOAODSDDDWBSTH-WWEDSPNTSA-N n-[(2s,3s,5r)-3-hydroxy-5-methyl-6-(2-methylpropylamino)-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propan-2-yloxybenzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCC(C)C)NC(=O)C=1C=C(C=C(OC(C)C)C=1)N1C(CCC1)=O)C1=CC=CC=C1 LOAODSDDDWBSTH-WWEDSPNTSA-N 0.000 claims 1
- UBZJRFZZBTVLFL-ZUVGRRGESA-N n-[(2s,3s,5r)-5-(3-bicyclo[2.2.1]heptanylcarbamoyl)-3-hydroxy-1-phenyloct-7-yn-2-yl]-3,5-bis(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@H](C[C@@H](CC#C)C(=O)NC1C2CCC(C2)C1)O)NC(=O)C=1C=C(C=C(C=1)N1C(CCC1)=O)N1C(CCC1)=O)C1=CC=CC=C1 UBZJRFZZBTVLFL-ZUVGRRGESA-N 0.000 claims 1
- RGVBWXQYQAJRIU-KDGCPDPYSA-N n-[(2s,3s,5r)-5-(3-bicyclo[2.2.1]heptanylcarbamoyl)-3-hydroxy-8-methyl-1-phenylnonan-2-yl]-3,5-bis(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](CCC(C)C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C=C(C=C(C=1)N1C(CCC1)=O)N1C(CCC1)=O)C1=CC=CC=C1 RGVBWXQYQAJRIU-KDGCPDPYSA-N 0.000 claims 1
- KIBZOPBJGHBVBM-LNMMVMNESA-N n-[(2s,3s,5r)-6-(2-cyclohexylethylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propan-2-yloxybenzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OC(C)C)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NCCC1CCCCC1)C1=CC=CC=C1 KIBZOPBJGHBVBM-LNMMVMNESA-N 0.000 claims 1
- OBUJHUKTPPJUEC-LNMMVMNESA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-phenoxybenzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C=C(OC=2C=CC=CC=2)C=1)N1C(CCC1)=O)C1=CC=CC=C1 OBUJHUKTPPJUEC-LNMMVMNESA-N 0.000 claims 1
- XCDJJGUZKRCHNU-LNMMVMNESA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-phenylbenzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C=C(C=1)N1C(CCC1)=O)C=1C=CC=CC=1)C1=CC=CC=C1 XCDJJGUZKRCHNU-LNMMVMNESA-N 0.000 claims 1
- IPNQEHUEACIZGQ-MGONOCMRSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-prop-2-enoxybenzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C=C(OCC=C)C=1)N1C(CCC1)=O)C1=CC=CC=C1 IPNQEHUEACIZGQ-MGONOCMRSA-N 0.000 claims 1
- SPPLJFPHJLHTOB-MGONOCMRSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propoxybenzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OCCC)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)C1=CC=CC=C1 SPPLJFPHJLHTOB-MGONOCMRSA-N 0.000 claims 1
- JFBNTINWKSRMCU-BQQUOAEZSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-hydroxy-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C=C(O)C=1)N1C(CCC1)=O)C1=CC=CC=C1 JFBNTINWKSRMCU-BQQUOAEZSA-N 0.000 claims 1
- LXMHKVZXLJCHDW-PSUQPPDWSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-4-fluoro-3-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C(F)=CC=1)N1C(CCC1)=O)C1=CC=CC=C1 LXMHKVZXLJCHDW-PSUQPPDWSA-N 0.000 claims 1
- ZYZBMJGMAZDXME-IJVOHCTGSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-2-fluoro-3,5-bis(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C(=C(N2C(CCC2)=O)C=C(C=1)N1C(CCC1)=O)F)C1=CC=CC=C1 ZYZBMJGMAZDXME-IJVOHCTGSA-N 0.000 claims 1
- STJQNJREMJPCCI-MQOPCWFGSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-2-fluoro-3-(2-oxopyrrolidin-1-yl)-5-(trifluoromethyl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C(=C(N2C(CCC2)=O)C=C(C=1)C(F)(F)F)F)C1=CC=CC=C1 STJQNJREMJPCCI-MQOPCWFGSA-N 0.000 claims 1
- BRSYDVMCNWCJTB-IABUABSESA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-2-fluoro-3-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C(=C(N2C(CCC2)=O)C=CC=1)F)C1=CC=CC=C1 BRSYDVMCNWCJTB-IABUABSESA-N 0.000 claims 1
- SWHIKWQQPQXHAQ-JANXGGRPSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-2-methoxy-6-(2-oxopyrrolidin-1-yl)pyridine-4-carboxamide Chemical compound N=1C(OC)=CC(C(=O)N[C@@H](CC=2C=CC=CC=2)[C@@H](O)C[C@@H](C)C(=O)NC2C3CCC(C3)C2)=CC=1N1CCCC1=O SWHIKWQQPQXHAQ-JANXGGRPSA-N 0.000 claims 1
- NFXCWOXGGHRVTQ-LTXCQHPESA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propan-2-yloxybenzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OC(C)C)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)C1=CC=CC=C1 NFXCWOXGGHRVTQ-LTXCQHPESA-N 0.000 claims 1
- OTMFGIDOSDNFFD-DNFDBSLJSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(4-methoxybutoxy)-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OCCCCOC)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)C1=CC=CC=C1 OTMFGIDOSDNFFD-DNFDBSLJSA-N 0.000 claims 1
- GSKQPBJFQWHKEE-HJRDSUCGSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(cyclopropylmethoxy)-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C=C(C=C(OCC2CC2)C=1)N1C(CCC1)=O)C1=CC=CC=C1 GSKQPBJFQWHKEE-HJRDSUCGSA-N 0.000 claims 1
- ZQXHHXRANFKMJJ-UXEANBLESA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-[(2s)-butan-2-yl]oxy-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)O[C@@H](C)CC)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)C1=CC=CC=C1 ZQXHHXRANFKMJJ-UXEANBLESA-N 0.000 claims 1
- MHZHWUXLTWDLRF-XDLNGMLJSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-[(4s)-2-oxo-4-propan-2-yl-1,3-oxazolidin-3-yl]benzamide Chemical compound CC(C)[C@H]1COC(=O)N1C1=CC=CC(C(=O)N[C@@H](CC=2C=CC=CC=2)[C@@H](O)C[C@@H](C)C(=O)NC2C3CCC(C3)C2)=C1 MHZHWUXLTWDLRF-XDLNGMLJSA-N 0.000 claims 1
- MMVKWQJIMGCYDA-JIHHKYRASA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-cyclobutyloxy-5-(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)NC(=O)C=1C=C(C=C(OC2CCC2)C=1)N1C(CCC1)=O)C1=CC=CC=C1 MMVKWQJIMGCYDA-JIHHKYRASA-N 0.000 claims 1
- UIWIIOONOIPLEC-ZLRPTZMNSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-methoxy-5-(2-oxopiperidin-1-yl)benzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OC)N1C(CCCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)C1=CC=CC=C1 UIWIIOONOIPLEC-ZLRPTZMNSA-N 0.000 claims 1
- BTXZKLNQHGCMMS-RAHIQWLESA-N n-[(2s,3s,5r)-6-(cyclobutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-2-fluoro-3,5-bis(2-oxopyrrolidin-1-yl)benzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NC1CCC1)NC(=O)C=1C(=C(N2C(CCC2)=O)C=C(C=1)N1C(CCC1)=O)F)C1=CC=CC=C1 BTXZKLNQHGCMMS-RAHIQWLESA-N 0.000 claims 1
- FCYSMQZPNCJLNM-MHWRTBLVSA-N n-[(2s,3s,5r)-6-(cyclopropylmethylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propan-2-yloxybenzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OC(C)C)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NCC1CC1)C1=CC=CC=C1 FCYSMQZPNCJLNM-MHWRTBLVSA-N 0.000 claims 1
- WRXNUCYBHSBQSM-GTTXMTDLSA-N n-[(2s,3s,5r)-6-[(4,4-dimethylcyclohexyl)amino]-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-(2-oxopyrrolidin-1-yl)-5-propan-2-yloxybenzamide Chemical compound C([C@H](NC(=O)C=1C=C(C=C(C=1)OC(C)C)N1C(CCC1)=O)[C@@H](O)C[C@@H](C)C(=O)NC1CCC(C)(C)CC1)C1=CC=CC=C1 WRXNUCYBHSBQSM-GTTXMTDLSA-N 0.000 claims 1
- 238000001556 precipitation Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0128748A GB0128748D0 (en) | 2001-11-30 | 2001-11-30 | Novel compounds |
| GB0214090A GB0214090D0 (en) | 2002-06-18 | 2002-06-18 | Novel compounds |
| PCT/EP2002/013515 WO2003045913A1 (en) | 2001-11-30 | 2002-11-29 | Benzamide derivatives, processes for their preparation, and their pharmaceutical use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005514373A JP2005514373A (ja) | 2005-05-19 |
| JP2005514373A5 true JP2005514373A5 (https=) | 2006-01-05 |
Family
ID=26246821
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003547365A Pending JP2005514373A (ja) | 2001-11-30 | 2002-11-29 | ベンズアミド誘導体、その製造方法およびその医薬的使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US6992103B2 (https=) |
| EP (1) | EP1448520A1 (https=) |
| JP (1) | JP2005514373A (https=) |
| AR (1) | AR037460A1 (https=) |
| AU (1) | AU2002365516A1 (https=) |
| TW (1) | TW200304374A (https=) |
| WO (1) | WO2003045913A1 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0314302D0 (en) * | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Novel compounds |
| AR045219A1 (es) * | 2003-08-08 | 2005-10-19 | Pharmacopeia Inc | Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico |
| EP1673078B1 (en) * | 2003-10-03 | 2008-05-28 | Merck & Co., Inc. | Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease |
| CA2543756A1 (en) * | 2003-10-30 | 2005-05-12 | Elan Pharmaceuticals, Inc. | Hydroxypropyl amides for the treatment of alzheimer's disease |
| EP1685142B1 (en) | 2003-11-11 | 2008-01-09 | F. Hoffmann-La Roche Ag | Phosphinic acid derivatives, beta-secretase inhibitors for the treatment of alzheimer's disease |
| ATE517861T1 (de) * | 2003-11-24 | 2011-08-15 | Merck Sharp & Dohme | Benzylether und benzylaminoverbindungen als inhibitoren von beta-secretase zur behandlung von alzheimer-krankheit |
| US7550481B2 (en) * | 2003-12-19 | 2009-06-23 | Merck & Co., Inc. | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
| JP2007533743A (ja) * | 2004-04-20 | 2007-11-22 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病治療のためのβ−セクレターゼ阻害薬として有用な１，３，５−置換フェニル誘導体化合物 |
| ITTO20040343A1 (it) * | 2004-05-24 | 2004-08-24 | Rotta Res Lab Spa | Uso di neboglamine (cr2249) come neuropsicotico e neuroprotettivo |
| US7872009B2 (en) * | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| US7745484B2 (en) * | 2005-11-21 | 2010-06-29 | Amgen Inc. | Beta-secretase modulators and methods of use |
| US7838676B2 (en) | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
| WO2007061670A1 (en) | 2005-11-21 | 2007-05-31 | Amgen Inc. | Beta-secretase modulators and methods of use |
| EP2038264B1 (en) * | 2006-06-29 | 2016-10-26 | F.Hoffmann-La Roche Ag | Tetrazole-substituted arylamides |
| WO2008137954A2 (en) * | 2007-05-07 | 2008-11-13 | Environmental Packaging Technologies Limited | Universal shipping container |
| WO2008147544A1 (en) | 2007-05-25 | 2008-12-04 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| CL2008001500A1 (es) | 2007-05-25 | 2008-12-26 | Amgen Inc | Compuestos derivados de hidroxietil amina sustituidas, moduladores de betasecretasa; proceso de preparacion de dichos c ompuestos; composicion farmaceutica que los comprende; y su uso para tratar un trastorno neurologico, tal como alzheimer, sindrome de down, demencia degenerativa, entre otros. |
| US7803809B2 (en) | 2008-11-12 | 2010-09-28 | Amgen Inc. | Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use |
| CA2715835C (en) | 2008-02-29 | 2017-03-21 | Renovis, Inc. | Amide compounds, compositions and uses thereof |
| MY148558A (en) * | 2008-09-11 | 2013-04-30 | Amgen Inc | Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use |
| JP5608655B2 (ja) * | 2008-09-18 | 2014-10-15 | エヴォテック アーゲー | Ｐ２ｘ３受容体活性のモジュレーター |
| WO2011063233A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| EP2504330A1 (en) | 2009-11-23 | 2012-10-03 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| CA2788363A1 (en) | 2010-01-19 | 2011-07-28 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2547685A1 (en) | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| EP2949648A1 (en) | 2014-05-30 | 2015-12-02 | IEO - Istituto Europeo di Oncologia Srl | Cyclopropylamine derivatives as histone demethylase inhibitors |
| WO2015181380A1 (en) | 2014-05-30 | 2015-12-03 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Cyclopropylamine compounds as histone demethylase inhibitors |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL96324A (en) * | 1989-11-29 | 1995-01-24 | Squibb & Sons Inc | 5-Amino-2, 4, 6-triiodo-1, 3-benzenecarboxylic acid derivatives, processes for their preparation, and methods utilizing them as contrast agents |
| US5869024A (en) * | 1989-11-29 | 1999-02-09 | Bracco International B.V. | Methods and compositions for using non-ionic contrast agents to reduce the risk of clot formation in diagnostic procedures |
| WO1998038167A1 (en) * | 1997-02-26 | 1998-09-03 | Pfizer Inc. | Heteroaryl-hexanoic acid amide derivatives, their preparation and their use as selective inhibitors of mip-1-alpha binding to its ccr1 receptor |
| DE60124080T2 (de) * | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| AU2002359376B2 (en) * | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
-
2002
- 2002-11-28 AR ARP020104587A patent/AR037460A1/es not_active Application Discontinuation
- 2002-11-28 TW TW091134543A patent/TW200304374A/zh unknown
- 2002-11-29 JP JP2003547365A patent/JP2005514373A/ja active Pending
- 2002-11-29 WO PCT/EP2002/013515 patent/WO2003045913A1/en not_active Ceased
- 2002-11-29 AU AU2002365516A patent/AU2002365516A1/en not_active Abandoned
- 2002-11-29 US US10/496,269 patent/US6992103B2/en not_active Expired - Fee Related
- 2002-11-29 EP EP02790460A patent/EP1448520A1/en not_active Withdrawn
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