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 (enExample) | 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 (enExample) |
| EP (1) | EP1448520A1 (enExample) |
| JP (1) | JP2005514373A (enExample) |
| AR (1) | AR037460A1 (enExample) |
| AU (1) | AU2002365516A1 (enExample) |
| TW (1) | TW200304374A (enExample) |
| WO (1) | WO2003045913A1 (enExample) |
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 |
| US7598250B2 (en) * | 2003-08-08 | 2009-10-06 | Schering Corporation | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
| CA2540452A1 (en) * | 2003-10-03 | 2005-04-14 | Merck & Co., Inc. | Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease |
| WO2005042472A2 (en) * | 2003-10-30 | 2005-05-12 | Elan Pharmaceuticals, Inc. | Hydroxypropyl amides for the treatment of alzheimer’s disease |
| RU2367666C2 (ru) * | 2003-11-11 | 2009-09-20 | Ф.Хоффманн-Ля Рош Аг | Производные фосфиновой кислоты, ингибиторы бета-секретазы, предназначенные для лечения болезни альцгеймера |
| ATE517861T1 (de) * | 2003-11-24 | 2011-08-15 | Merck Sharp & Dohme | Benzylether und benzylaminoverbindungen als inhibitoren von beta-secretase zur behandlung von alzheimer-krankheit |
| JP2007517781A (ja) * | 2003-12-19 | 2007-07-05 | 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用のフェニルアミドおよびピリジルアミド系β−セクレターゼ阻害薬 |
| CA2563615A1 (en) * | 2004-04-20 | 2005-11-03 | Merck & Co., Inc. | 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| ITTO20040343A1 (it) | 2004-05-24 | 2004-08-24 | Rotta Res Lab Spa | Uso di neboglamine (cr2249) come neuropsicotico e neuroprotettivo |
| JP5274258B2 (ja) | 2005-11-21 | 2013-08-28 | アムジエン・インコーポレーテツド | β−セクレターゼ調節物質及び使用方法 |
| US7838676B2 (en) | 2005-11-21 | 2010-11-23 | 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 |
| US7872009B2 (en) * | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| EP2592070B1 (en) * | 2006-06-29 | 2016-08-31 | F. Hoffmann-La Roche AG | Tetrazole-substituted arylamides |
| WO2008137954A2 (en) * | 2007-05-07 | 2008-11-13 | Environmental Packaging Technologies Limited | Universal shipping container |
| EP2167471B1 (en) * | 2007-05-25 | 2013-10-16 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| WO2008147547A1 (en) | 2007-05-25 | 2008-12-04 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| 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 |
| CN104058999A (zh) | 2008-02-29 | 2014-09-24 | 伊沃泰克股份公司 | 酰胺化合物、组合物及其应用 |
| US8426447B2 (en) * | 2008-09-11 | 2013-04-23 | Amgen Inc. | Spiro-tricyclic ring compounds as beta-secretase 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 |
| EP2504315A1 (en) | 2009-11-23 | 2012-10-03 | 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 |
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| 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 |
| JP2014526560A (ja) | 2011-09-21 | 2014-10-06 | アムジエン・インコーポレーテツド | β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法 |
| 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 |
| JP6320570B2 (ja) | 2014-05-30 | 2018-05-09 | イエオ−イスティトゥート・エウロペオ・ディ・オンコロジア・エッセ・エッレ・エッレ | ヒストンデメチラーゼ阻害剤としてのシクロプロピルアミン化合物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CA2029830A1 (en) * | 1989-11-29 | 1991-05-30 | Ramachandran S. Ranganathan | Nonionic radiographic 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 |
| AU745687B2 (en) * | 1997-02-26 | 2002-03-28 | Pfizer Inc. | Heteroaryl-hexanoic acid amide derivatives, their preparation and their use as selective inhibitors of MIP-1-alpha binding to its CCR1 receptor |
| AU2001252958A1 (en) * | 2000-03-23 | 2001-10-03 | Elan Pharmaceuticals, Inc. | Compounds and methods to treat alzheimer's disease |
| EP1453789A2 (en) * | 2001-11-08 | 2004-09-08 | 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 WO PCT/EP2002/013515 patent/WO2003045913A1/en not_active Ceased
- 2002-11-29 JP JP2003547365A patent/JP2005514373A/ja active Pending
- 2002-11-29 EP EP02790460A patent/EP1448520A1/en not_active Withdrawn
- 2002-11-29 US US10/496,269 patent/US6992103B2/en not_active Expired - Fee Related
- 2002-11-29 AU AU2002365516A patent/AU2002365516A1/en not_active Abandoned
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