JP2005510559A5 - - Google Patents
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- Publication number
- JP2005510559A5 JP2005510559A5 JP2003547355A JP2003547355A JP2005510559A5 JP 2005510559 A5 JP2005510559 A5 JP 2005510559A5 JP 2003547355 A JP2003547355 A JP 2003547355A JP 2003547355 A JP2003547355 A JP 2003547355A JP 2005510559 A5 JP2005510559 A5 JP 2005510559A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- alkyl
- compound
- benzyl
- protected
- 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 17
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 239000012453 solvate Substances 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
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 2
- -1 bicyclo [2.2.1] hept-2-ylcarbamoyl Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 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
- FSANQGKLVRTEFH-ZUVGRRGESA-N N-[(2S,3S,5R)-5-(2-bicyclo[2.2.1]heptanylcarbamoyl)-3-hydroxy-8-methyl-1-phenylnonan-2-yl]-3-methylsulfonyl-5-propoxybenzamide Chemical compound CS(=O)(=O)C1=CC(OCCC)=CC(C(=O)N[C@@H](CC=2C=CC=CC=2)[C@@H](O)C[C@@H](CCC(C)C)C(=O)NC2C3CCC(C3)C2)=C1 FSANQGKLVRTEFH-ZUVGRRGESA-N 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
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- YSHQWXMZPYKBEO-YGOYIFOWSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-methylsulfonylbenzamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1C=C(C=CC=1)S(C)(=O)=O)C1=CC=CC=C1 YSHQWXMZPYKBEO-YGOYIFOWSA-N 0.000 claims 1
- LUKQYLFCEYZVOF-HOJAQTOUSA-N n-[(2s,3s,5r)-6-(3,3-dimethylbutylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-5-methylsulfonylthiophene-2-carboxamide Chemical compound C([C@@H]([C@@H](O)C[C@@H](C)C(=O)NCCC(C)(C)C)NC(=O)C=1SC(=CC=1)S(C)(=O)=O)C1=CC=CC=C1 LUKQYLFCEYZVOF-HOJAQTOUSA-N 0.000 claims 1
- KZKSCWDMDRSEKJ-OOEPTKCWSA-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-methylsulfonylbenzamide Chemical compound CS(=O)(=O)C1=CC(OC)=CC(C(=O)N[C@@H](CC=2C=CC=CC=2)[C@@H](O)C[C@@H](C)C(=O)NC2C3CCC(C3)C2)=C1 KZKSCWDMDRSEKJ-OOEPTKCWSA-N 0.000 claims 1
- GTHIDBYCDWSTCL-XGMAVGGMSA-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-methylsulfonylpyridine-4-carboxamide Chemical compound COC1=CN=CC(S(C)(=O)=O)=C1C(=O)N[C@H]([C@@H](O)C[C@@H](C)C(=O)NC1C2CCC(C2)C1)CC1=CC=CC=C1 GTHIDBYCDWSTCL-XGMAVGGMSA-N 0.000 claims 1
- YOWQAGWJEGZZAD-HUMIOPDMSA-N n-[(2s,3s,5r)-6-(3-bicyclo[2.2.1]heptanylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-methylsulfonyl-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(C=1)N1C(CCC1)=O)S(C)(=O)=O)C1=CC=CC=C1 YOWQAGWJEGZZAD-HUMIOPDMSA-N 0.000 claims 1
- NQQNEJOPZMESIV-COPCDDAFSA-N n-[(2s,3s,5r)-6-(cyclohexylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]-3-methoxy-5-methylsulfonylpyridine-4-carboxamide Chemical compound COC1=CN=CC(S(C)(=O)=O)=C1C(=O)N[C@H]([C@@H](O)C[C@@H](C)C(=O)NC1CCCCC1)CC1=CC=CC=C1 NQQNEJOPZMESIV-COPCDDAFSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 238000001556 precipitation Methods 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 *C(C(CC1*)OC1=O)NI Chemical compound *C(C(CC1*)OC1=O)NI 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0128746A GB0128746D0 (en) | 2001-11-30 | 2001-11-30 | Novel compounds |
| GB0128747A GB0128747D0 (en) | 2001-11-30 | 2001-11-30 | Novel compounds |
| GB0214088A GB0214088D0 (en) | 2002-06-18 | 2002-06-18 | Novel compounds |
| PCT/EP2002/013517 WO2003045903A1 (en) | 2001-11-30 | 2002-11-29 | Hydroxyethylene compounds with asp2 inhibitory activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005510559A JP2005510559A (ja) | 2005-04-21 |
| JP2005510559A5 true JP2005510559A5 (https=) | 2006-01-05 |
Family
ID=27256340
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003547355A Pending JP2005510559A (ja) | 2001-11-30 | 2002-11-29 | Ａｓｐ２阻害剤活性を有するヒドロキシエチレン化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7160905B2 (https=) |
| EP (1) | EP1448516A1 (https=) |
| JP (1) | JP2005510559A (https=) |
| AU (1) | AU2002352189A1 (https=) |
| WO (1) | WO2003045903A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0314302D0 (en) * | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Novel compounds |
| CA2548849A1 (en) * | 2003-12-19 | 2005-07-21 | Merck & Co., Inc. | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| CA2558036A1 (en) * | 2004-03-09 | 2005-09-22 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamine aspartyl protease inhibitors |
| KR20070107062A (ko) * | 2005-02-01 | 2007-11-06 | 와이어쓰 | β-세크리타제의 억제제로서의 아미노-피리딘 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60124080T2 (de) * | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
-
2002
- 2002-11-29 US US10/496,334 patent/US7160905B2/en not_active Expired - Fee Related
- 2002-11-29 AU AU2002352189A patent/AU2002352189A1/en not_active Abandoned
- 2002-11-29 EP EP02787874A patent/EP1448516A1/en not_active Withdrawn
- 2002-11-29 JP JP2003547355A patent/JP2005510559A/ja active Pending
- 2002-11-29 WO PCT/EP2002/013517 patent/WO2003045903A1/en not_active Ceased
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