JP2005534614A5 - - Google Patents
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- Publication number
- JP2005534614A5 JP2005534614A5 JP2003558035A JP2003558035A JP2005534614A5 JP 2005534614 A5 JP2005534614 A5 JP 2005534614A5 JP 2003558035 A JP2003558035 A JP 2003558035A JP 2003558035 A JP2003558035 A JP 2003558035A JP 2005534614 A5 JP2005534614 A5 JP 2005534614A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- aryl
- heteroaryl
- groups
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 72
- 229910052736 halogen Inorganic materials 0.000 claims 55
- 150000002367 halogens Chemical class 0.000 claims 55
- 125000000753 cycloalkyl group Chemical group 0.000 claims 42
- 125000004663 dialkyl amino group Chemical group 0.000 claims 36
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 34
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 125000000623 heterocyclic group Chemical group 0.000 claims 28
- 125000003118 aryl group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 21
- -1 cyano, nitro, amino Chemical group 0.000 claims 17
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 15
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 229960004295 valine Drugs 0.000 claims 12
- 206010012289 Dementia Diseases 0.000 claims 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 5
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000003412 degenerative effect Effects 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 2
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 206010033799 Paralysis Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 206010044688 Trisomy 21 Diseases 0.000 claims 2
- 125000005025 alkynylaryl group Chemical group 0.000 claims 2
- 210000004227 basal ganglia Anatomy 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 230000001054 cortical effect Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 210000004558 lewy body Anatomy 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- NCQYGBKQXRQAAG-JVPBZIDWSA-N (2s)-2-[[(2s)-2-[[(2s)-2-amino-3-(3,5-difluorophenyl)propyl]amino]propanoyl]amino]-3-methyl-n-(2-methylpropyl)butanamide Chemical compound CC(C)CNC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC[C@@H](N)CC1=CC(F)=CC(F)=C1 NCQYGBKQXRQAAG-JVPBZIDWSA-N 0.000 claims 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000036536 dutch type ABeta amyloidosis Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- NLFBCYMMUAKCPC-KQQUZDAGSA-N ethyl (e)-3-[3-amino-2-cyano-1-[(e)-3-ethoxy-3-oxoprop-1-enyl]sulfanyl-3-oxoprop-1-enyl]sulfanylprop-2-enoate Chemical compound CCOC(=O)\C=C\SC(=C(C#N)C(N)=O)S\C=C\C(=O)OCC NLFBCYMMUAKCPC-KQQUZDAGSA-N 0.000 claims 1
- 235000019256 formaldehyde Nutrition 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 0 *C(C(*=C)N(*)C(C(C1)C1N(*)*)N)N(*)C(I)=O Chemical compound *C(C(*=C)N(*)C(C(C1)C1N(*)*)N)N(*)C(I)=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34531602P | 2002-01-04 | 2002-01-04 | |
| US35041902P | 2002-01-18 | 2002-01-18 | |
| PCT/US2003/000326 WO2003057721A2 (en) | 2002-01-04 | 2003-01-06 | Substituted amino carboxamides for the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005534614A JP2005534614A (ja) | 2005-11-17 |
| JP2005534614A5 true JP2005534614A5 (enExample) | 2006-03-16 |
Family
ID=26994342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003558035A Pending JP2005534614A (ja) | 2002-01-04 | 2003-01-06 | アルツハイマー病治療のための置換アミノカルボキサミド |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6962934B2 (enExample) |
| EP (1) | EP1458745A2 (enExample) |
| JP (1) | JP2005534614A (enExample) |
| AU (1) | AU2003206413A1 (enExample) |
| BR (1) | BR0306724A (enExample) |
| CA (1) | CA2472617A1 (enExample) |
| MX (1) | MXPA04006575A (enExample) |
| WO (1) | WO2003057721A2 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003294441A1 (en) * | 2002-11-22 | 2004-06-18 | Bristol-Myers Squibb Company | 1-aryl-2-hydroxyethyl amides as potassium channel openers |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| EP1641748B1 (en) | 2003-06-30 | 2013-08-28 | Merck Sharp & Dohme Corp. | N-alkyl phenylcarboxamide 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 |
| AU2004311749A1 (en) | 2003-12-19 | 2005-07-21 | Merck & Co., Inc. | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
| JP2007522129A (ja) * | 2004-01-21 | 2007-08-09 | エラン ファーマシューティカルズ，インコーポレイテッド | アスパラギン酸プロテアーゼ阻害薬を用いるアミロイドーシスの処置方法 |
| EP1740581B1 (en) | 2004-04-20 | 2012-08-22 | Merck Sharp & Dohme Corp. | 2, 4, 6-substituted pyridyl derivative compounds useful as 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 |
| WO2005113582A1 (en) * | 2004-05-22 | 2005-12-01 | Boehringer Ingelheim International Gmbh | Substituted ethane-1,2-diamines for the treatment of alzheimer's disease |
| EP1758854B1 (en) * | 2004-06-15 | 2014-07-16 | Merck Sharp & Dohme Corp. | Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| EP1866034A1 (en) * | 2005-03-30 | 2007-12-19 | Boehringer Ingelheim International GmbH | Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture |
| CA2604291A1 (en) | 2005-04-08 | 2006-10-19 | Comentis, Inc. | Compounds which inhibit beta-secretase activity and methods of use thereof |
| US20100298278A1 (en) * | 2005-08-11 | 2010-11-25 | Christian Eickmeier | Inhibitors of beta-secretase for the treatment of alzheimer's disease |
| JP2009504613A (ja) * | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用化合物 |
| EP1919861A2 (de) * | 2005-08-11 | 2008-05-14 | Boehringer Ingelheim International GmbH | Verbindungen zur behandlung der alzheimer erkrankung |
| JP2009504612A (ja) * | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用化合物 |
| 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 |
| WO2007061670A1 (en) | 2005-11-21 | 2007-05-31 | 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 |
| AU2008257145B2 (en) | 2007-05-25 | 2011-11-10 | 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. |
| US8222264B2 (en) | 2007-07-06 | 2012-07-17 | Boehringer Ingelheim International Gmbh | Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture |
| 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 |
| CN102209721A (zh) * | 2008-09-11 | 2011-10-05 | 安姆根有限公司 | 作为β-分泌酶调节剂的螺四环化合物及其使用方法 |
| US8822485B2 (en) | 2009-11-23 | 2014-09-02 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| WO2011063233A1 (en) | 2009-11-23 | 2011-05-26 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| WO2011090911A1 (en) | 2010-01-19 | 2011-07-28 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| EP2547686B1 (en) | 2010-03-15 | 2014-01-22 | Amgen Inc. | Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use |
| US8883782B2 (en) | 2010-03-15 | 2014-11-11 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
| EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | 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 |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5552558A (en) * | 1989-05-23 | 1996-09-03 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5362912A (en) * | 1989-05-23 | 1994-11-08 | Abbott Laboratories | Process for the preparation of a substituted diaminodiol |
| US5352705A (en) * | 1992-06-26 | 1994-10-04 | Merck & Co., Inc. | Inhibitors of farnesyl protein transferase |
| KR100187613B1 (ko) * | 1992-12-29 | 1999-06-01 | 스티븐 에프. 웨인스톡 | 레트로바이러스성 프로테이제 억제 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
| AU6383396A (en) * | 1995-06-07 | 1996-12-30 | Athena Neurosciences, Inc. | Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition |
| US6316440B1 (en) * | 1998-07-30 | 2001-11-13 | Warner-Lambert Company | Reduced dipeptide analogues as calcium channel antagonists |
| CA2376420A1 (en) * | 1999-06-15 | 2000-12-21 | Elan Pharmaceuticals, Inc. | Statine-derived tetrapeptide inhibitors of beta-secretase |
-
2003
- 2003-01-06 EP EP03703711A patent/EP1458745A2/en not_active Withdrawn
- 2003-01-06 CA CA002472617A patent/CA2472617A1/en not_active Abandoned
- 2003-01-06 BR BRPI0306724-6A patent/BR0306724A/pt not_active IP Right Cessation
- 2003-01-06 JP JP2003558035A patent/JP2005534614A/ja active Pending
- 2003-01-06 US US10/337,075 patent/US6962934B2/en not_active Expired - Fee Related
- 2003-01-06 AU AU2003206413A patent/AU2003206413A1/en not_active Abandoned
- 2003-01-06 WO PCT/US2003/000326 patent/WO2003057721A2/en not_active Ceased
-
2004
- 2004-07-02 MX MXPA04006575A patent/MXPA04006575A/es active IP Right Grant
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