JP2005534614A - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP2005534614A JP2005534614A JP2003558035A JP2003558035A JP2005534614A JP 2005534614 A JP2005534614 A JP 2005534614A JP 2003558035 A JP2003558035 A JP 2003558035A JP 2003558035 A JP2003558035 A JP 2003558035A JP 2005534614 A JP2005534614 A JP 2005534614A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- aryl
- groups
- heteroaryl
- 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
- 0 *C(C(*)N(*)C(*)=O)N(*)C(*)C(N(*)*1CC1)=O Chemical compound *C(C(*)N(*)C(*)=O)N(*)C(*)C(N(*)*1CC1)=O 0.000 description 2
- FNLPKWQHJBUPFC-HOFKKMOUSA-N CCCN(CCC)C(c1cccc(C(N[C@@H](Cc2ccccc2)CN[C@@H](C)C(NCC(C)C)=O)=O)c1)=O Chemical compound CCCN(CCC)C(c1cccc(C(N[C@@H](Cc2ccccc2)CN[C@@H](C)C(NCC(C)C)=O)=O)c1)=O FNLPKWQHJBUPFC-HOFKKMOUSA-N 0.000 description 2
- MNQYEBRKYOEJFD-HSQYWUDLSA-N CC(C)CNC([C@H](C(C)C)NC([C@H](C)NC[C@H](Cc1cc(F)cc(F)c1)NC(OC(C)(C)C)=O)=O)=O Chemical compound CC(C)CNC([C@H](C(C)C)NC([C@H](C)NC[C@H](Cc1cc(F)cc(F)c1)NC(OC(C)(C)C)=O)=O)=O MNQYEBRKYOEJFD-HSQYWUDLSA-N 0.000 description 1
- JGSCFJILJJUXOV-OATBXSGESA-N CCCN(CCC)C(c1cc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(N[C@@H](C(C)C)C(NCC(C)C)=O)=O)=O)cc(C)c1)=O Chemical compound CCCN(CCC)C(c1cc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(N[C@@H](C(C)C)C(NCC(C)C)=O)=O)=O)cc(C)c1)=O JGSCFJILJJUXOV-OATBXSGESA-N 0.000 description 1
- BITMBOFCMBJDIZ-HIWYQFENSA-N CCCN(CCC)C(c1cc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(N[C@@H](C(C)C)C(NCC(C)C)=O)=O)=O)ccc1)O Chemical compound CCCN(CCC)C(c1cc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(N[C@@H](C(C)C)C(NCC(C)C)=O)=O)=O)ccc1)O BITMBOFCMBJDIZ-HIWYQFENSA-N 0.000 description 1
- WAERKZLNIDDODN-UUOWRZLLSA-N CCCNC(c1cccc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(NCC(C)C)=O)=O)c1)=O Chemical compound CCCNC(c1cccc(C(N[C@@H](Cc2cc(F)cc(F)c2)CN[C@@H](C)C(NCC(C)C)=O)=O)c1)=O WAERKZLNIDDODN-UUOWRZLLSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
- C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 true JP2005534614A (ja) | 2005-11-17 |
| JP2005534614A5 JP2005534614A5 (https=) | 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 (https=) |
| EP (1) | EP1458745A2 (https=) |
| JP (1) | JP2005534614A (https=) |
| AU (1) | AU2003206413A1 (https=) |
| BR (1) | BR0306724A (https=) |
| CA (1) | CA2472617A1 (https=) |
| MX (1) | MXPA04006575A (https=) |
| WO (1) | WO2003057721A2 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007509988A (ja) * | 2003-10-30 | 2007-04-19 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病治療のためのヒドロキシプロピルアミド |
| JP2007516207A (ja) * | 2003-06-30 | 2007-06-21 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療のためのN−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤 |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7045551B2 (en) * | 2002-11-22 | 2006-05-16 | 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 |
| US7550481B2 (en) | 2003-12-19 | 2009-06-23 | Merck & Co., Inc. | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease |
| WO2005070407A1 (en) * | 2004-01-21 | 2005-08-04 | Elan Pharmaceuticals, Inc. | Methods of treatment of amyloidosis using aspartyl-protease inihibitors |
| CA2563639A1 (en) | 2004-04-20 | 2005-11-03 | Merck & Co., Inc. | 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 |
| US7714021B2 (en) * | 2004-06-15 | 2010-05-11 | Merck & Co., Inc. | Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease |
| JP2008534541A (ja) * | 2005-03-30 | 2008-08-28 | 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 | 置換1,2−エチレンジアミン、前記化合物を含む薬物、それらの使用及びそれらの製造方法 |
| NZ562314A (en) | 2005-04-08 | 2010-02-26 | Comentis Inc | Compounds which inhibit beta-secretase activity and methods of use thereof |
| EP1915339A1 (de) * | 2005-08-11 | 2008-04-30 | Boehringer Ingelheim International GmbH | Inhibitoren der beta-sekretase zur behandlung der alzheimer- erkrankung |
| US20100168070A1 (en) * | 2005-08-11 | 2010-07-01 | Niklas Heine | Compounds for the treatment of alzheimer's disease |
| US20100144681A1 (en) * | 2005-08-11 | 2010-06-10 | Klaus Fuchs | Compounds for the treatment of alzheimer's disease |
| US20090042867A1 (en) * | 2005-08-11 | 2009-02-12 | Klaus Fuchs | Compounds for the treatment of alzheimer's disease |
| US7872009B2 (en) | 2005-11-21 | 2011-01-18 | 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 |
| US7745484B2 (en) | 2005-11-21 | 2010-06-29 | Amgen Inc. | Beta-secretase modulators and methods of use |
| 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. |
| 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 |
| MY148558A (en) * | 2008-09-11 | 2013-04-30 | Amgen Inc | Spiro-tetracyclic ring compounds as betasecretase 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 |
| 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 |
| EP2547685A1 (en) | 2010-03-15 | 2013-01-23 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta - secretase modulators |
| US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08500081A (ja) * | 1992-06-26 | 1996-01-09 | メルク エンド カンパニー インコーポレーテッド | ファルネシル蛋白質トランスフェラーゼの阻害剤 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5362912A (en) | 1989-05-23 | 1994-11-08 | Abbott Laboratories | Process for the preparation of a substituted diaminodiol |
| US5539122A (en) | 1989-05-23 | 1996-07-23 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| CA2170020C (en) | 1992-12-29 | 2005-08-02 | Dale J. Kempf | Retroviral protease inhibiting compounds |
| JPH11507538A (ja) | 1995-06-07 | 1999-07-06 | アテナ ニューロサイエンシズ インコーポレイティド | β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ |
| US6316440B1 (en) * | 1998-07-30 | 2001-11-13 | Warner-Lambert Company | Reduced dipeptide analogues as calcium channel antagonists |
| JP2003502342A (ja) * | 1999-06-15 | 2003-01-21 | エラン ファーマスーティカルズ インコーポレイテッド | ベータ−セクレターゼのスタチン誘導テトラペプチド阻害剤 |
-
2003
- 2003-01-06 US US10/337,075 patent/US6962934B2/en not_active Expired - Fee Related
- 2003-01-06 CA CA002472617A patent/CA2472617A1/en not_active Abandoned
- 2003-01-06 EP EP03703711A patent/EP1458745A2/en not_active Withdrawn
- 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 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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08500081A (ja) * | 1992-06-26 | 1996-01-09 | メルク エンド カンパニー インコーポレーテッド | ファルネシル蛋白質トランスフェラーゼの阻害剤 |
Non-Patent Citations (2)
| Title |
|---|
| JPN6009054971, Nizal S. Chandrakumar et al., "Preparation and Opioid Activity of Analogs of the Analgesic Dipeptide 2,6−Dimethyl−L−tyrosyl−N−(3−ph", J. Med. Chem., 1992, Vol.35, No.2, p.223−233 * |
| JPN6009054972, Yaeko Konda et al., "Alkaloid from Thermoactinomyces Species", Chem. Pharm. Bull., 1976, Vol.24, No.1, p.92−96 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007516207A (ja) * | 2003-06-30 | 2007-06-21 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療のためのN−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤 |
| JP2007509988A (ja) * | 2003-10-30 | 2007-04-19 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病治療のためのヒドロキシプロピルアミド |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1458745A2 (en) | 2004-09-22 |
| US20030166580A1 (en) | 2003-09-04 |
| AU2003206413A8 (en) | 2003-07-24 |
| WO2003057721A3 (en) | 2004-03-25 |
| WO2003057721A2 (en) | 2003-07-17 |
| BR0306724A (pt) | 2006-04-11 |
| MXPA04006575A (es) | 2004-10-04 |
| CA2472617A1 (en) | 2003-07-17 |
| AU2003206413A1 (en) | 2003-07-24 |
| US6962934B2 (en) | 2005-11-08 |
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