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
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- 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
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- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 238000011895 specific detection Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 229950000244 sulfanilic acid Drugs 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 238000011820 transgenic animal model Methods 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 108010082372 valspodar Proteins 0.000 description 1
- 229950010938 valspodar Drugs 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229960001722 verapamil Drugs 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 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)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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 (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) |
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 |
|---|---|---|---|---|
| WO2004047743A2 (en) * | 2002-11-22 | 2004-06-10 | 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 |
| 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 |
| 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 |
| CN1942457A (zh) | 2004-04-20 | 2007-04-04 | 默克公司 | 作为β－促分泌酶抑制剂用于阿尔茨海默氏病的治疗中的1,3,5－取代的苯基衍生化合物 |
| WO2005113582A1 (en) * | 2004-05-22 | 2005-12-01 | Boehringer Ingelheim International Gmbh | Substituted ethane-1,2-diamines for the treatment of alzheimer's disease |
| AU2005257904A1 (en) * | 2004-06-15 | 2006-01-05 | 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 |
| AU2006235344B2 (en) | 2005-04-08 | 2012-07-26 | Comentis, Inc. | Compounds which inhibit beta-secretase activity and methods of use thereof |
| EP1915353A2 (de) * | 2005-08-11 | 2008-04-30 | Boehringer Ingelheim International GmbH | Isophthalsäurediamide zur behandlung der alzheimer erkrankung |
| JP2009504614A (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 |
| WO2007017509A1 (de) * | 2005-08-11 | 2007-02-15 | Boehringer Ingelheim International Gmbh | Verbindungen zur behandlung der alzheimer erkrankung |
| EP1915339A1 (de) * | 2005-08-11 | 2008-04-30 | Boehringer Ingelheim International GmbH | Inhibitoren der beta-sekretase zur behandlung der alzheimer- erkrankung |
| EP1971598A1 (en) | 2005-11-21 | 2008-09-24 | 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 |
| US7872009B2 (en) | 2005-11-21 | 2011-01-18 | Amgen Inc. | Beta-Secretase modulators and methods of use |
| US8163909B2 (en) | 2007-05-25 | 2012-04-24 | Amgen Inc. | Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use |
| JP5440984B2 (ja) | 2007-05-25 | 2014-03-12 | アムジエン・インコーポレーテツド | β−セクレターゼ修飾剤としての置換ヒドロキシエチルアミン化合物および使用方法 |
| CA2687750C (en) | 2007-07-06 | 2016-10-18 | 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 |
| KR20110073511A (ko) * | 2008-09-11 | 2011-06-29 | 암젠 인크 | 베타세크레타제 조절제로서의 스피로-테트라사이클릭 고리 화합물 및 사용 방법 |
| EP2504330A1 (en) | 2009-11-23 | 2012-10-03 | 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 |
| CA2788363A1 (en) | 2010-01-19 | 2011-07-28 | Amgen Inc. | Amino heteroaryl compounds as beta-secretase modulators and methods of use |
| JP5584352B2 (ja) | 2010-03-15 | 2014-09-03 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途 |
| CA2791281A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators |
| 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 |
| EP2758406A1 (en) | 2011-09-21 | 2014-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | 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 |
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| 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 |
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| 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 |
| US5696270A (en) | 1989-05-23 | 1997-12-09 | Abbott Laboratories | Intermediate for making retroviral protease inhibiting compounds |
| EP1090914B1 (en) | 1992-12-29 | 2003-01-02 | Abbott Laboratories | 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 |
| EP1192177A1 (en) | 1999-06-15 | 2002-04-03 | Elan Pharmaceuticals, Inc. | Statine-derived tetrapeptide inhibitors of beta-secretase |
-
2003
- 2003-01-06 CA CA002472617A patent/CA2472617A1/en not_active Abandoned
- 2003-01-06 WO PCT/US2003/000326 patent/WO2003057721A2/en not_active Ceased
- 2003-01-06 US US10/337,075 patent/US6962934B2/en not_active Expired - Fee Related
- 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 EP EP03703711A patent/EP1458745A2/en not_active Withdrawn
-
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 |
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| 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 |
| WO2003057721A2 (en) | 2003-07-17 |
| AU2003206413A1 (en) | 2003-07-24 |
| AU2003206413A8 (en) | 2003-07-24 |
| CA2472617A1 (en) | 2003-07-17 |
| MXPA04006575A (es) | 2004-10-04 |
| WO2003057721A3 (en) | 2004-03-25 |
| US6962934B2 (en) | 2005-11-08 |
| BR0306724A (pt) | 2006-04-11 |
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