CA2304117A1 - Integrin receptor antagonists - Google Patents
Integrin receptor antagonists Download PDFInfo
- Publication number
- CA2304117A1 CA2304117A1 CA002304117A CA2304117A CA2304117A1 CA 2304117 A1 CA2304117 A1 CA 2304117A1 CA 002304117 A CA002304117 A CA 002304117A CA 2304117 A CA2304117 A CA 2304117A CA 2304117 A1 CA2304117 A1 CA 2304117A1
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- CA
- Canada
- Prior art keywords
- 6alkyl
- compound according
- 4alkyl
- compound
- compounds
- 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.)
- Abandoned
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- IHQKEDIOMGYHEB-UHFFFAOYSA-M sodium dimethylarsinate Chemical compound [Na+].C[As](C)([O-])=O IHQKEDIOMGYHEB-UHFFFAOYSA-M 0.000 description 1
- 238000002415 sodium dodecyl sulfate polyacrylamide gel electrophoresis Methods 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 229960005202 streptokinase Drugs 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- OGBMKVWORPGQRR-UMXFMPSGSA-N teriparatide Chemical compound C([C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CNC=N1 OGBMKVWORPGQRR-UMXFMPSGSA-N 0.000 description 1
- ROKMMRDVGWRMKJ-UHFFFAOYSA-N tert-butyl 2-amino-3-(3-hydroxypropyl)-2h-pyridine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1C=CC=C(CCCO)C1N ROKMMRDVGWRMKJ-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 230000009424 thromboembolic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 description 1
- 210000001364 upper extremity Anatomy 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 108010047303 von Willebrand Factor Proteins 0.000 description 1
- 102100036537 von Willebrand factor Human genes 0.000 description 1
- 229960001134 von willebrand factor Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5752997P | 1997-09-04 | 1997-09-04 | |
| US6352097P | 1997-10-29 | 1997-10-29 | |
| US60/057,529 | 1997-10-29 | ||
| US60/063,520 | 1997-10-29 | ||
| PCT/US1998/018379 WO1999011626A1 (en) | 1997-09-04 | 1998-09-03 | Integrin receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2304117A1 true CA2304117A1 (en) | 1999-03-11 |
Family
ID=26736601
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002304117A Abandoned CA2304117A1 (en) | 1997-09-04 | 1998-09-03 | Integrin receptor antagonists |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1027337A4 (de) |
| JP (1) | JP2001514253A (de) |
| CA (1) | CA2304117A1 (de) |
| WO (1) | WO1999011626A1 (de) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU747503B2 (en) | 1999-02-03 | 2002-05-16 | Merck & Co., Inc. | Benzazepine derivatives as alpha-V integrin receptor antagonists |
| JP2002537260A (ja) * | 1999-02-17 | 2002-11-05 | メルク エンド カムパニー インコーポレーテッド | αVインテグリン受容体拮抗薬としてのジベンゾ−アゼピン誘導体 |
| JP2003506452A (ja) * | 1999-08-06 | 2003-02-18 | スミスクライン・ビーチャム・コーポレイション | 発作の治療に有用なビトロネクチン受容体アンタゴニスト |
| DE19936780A1 (de) | 1999-08-09 | 2001-02-15 | Basf Ag | Neue Antagonisten von Integrinrezeptoren |
| US6514964B1 (en) | 1999-09-27 | 2003-02-04 | Amgen Inc. | Fused cycloheptane and fused azacycloheptane compounds and their methods of use |
| DE10039998A1 (de) * | 2000-08-11 | 2002-02-21 | Basf Ag | Neue substituierte Diareno-azepin-Derivate als Integrin Liganden |
| CA2386457A1 (en) * | 1999-10-06 | 2001-04-12 | Basf Aktiengesellschaft | Inhibitors of the endothelin signalling pathway and .alpha.v.beta.3 integrin receptor antagonists for combination therapy |
| DE10028575A1 (de) | 2000-06-14 | 2002-03-14 | Basf Ag | Integrinliganden |
| EP1381384B1 (de) | 2001-04-24 | 2011-05-25 | Merck Patent GmbH | KOMBINATIONSTHERAPIE MIT ANTIANGIOGENEN MITTELN UND TNFalpha |
| DE102004004928A1 (de) * | 2004-01-31 | 2005-08-18 | Bayer Healthcare Ag | Dibenzoxazepine II |
| UA87854C2 (en) | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
| EP1973569B1 (de) | 2006-01-18 | 2013-05-22 | Merck Patent GmbH | Spezifische therapie mit integrin-liganden zur krebsbehandlung |
| JP2010516645A (ja) | 2007-01-18 | 2010-05-20 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌を治療するためのインテグリンリガンドを用いる特異的療法および薬剤 |
| US20120130146A1 (en) | 2009-05-25 | 2012-05-24 | Merck Patent Gmbh | Continuous administration of cilengitide in cancer treatments |
| ES2864079T3 (es) | 2014-05-30 | 2021-10-13 | Pfizer | Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos |
| WO2023275715A1 (en) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Metabolites of selective androgen receptor modulators |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE632563A (de) * | 1963-03-26 | |||
| NL127795C (de) * | 1966-01-28 | |||
| US3905977A (en) * | 1974-12-06 | 1975-09-16 | Carter Wallace | Octahydromorphanthridines |
| IT1207417B (it) * | 1982-03-15 | 1989-05-17 | Menarini Sas | Azepina-6-one ad attivita'composti triciclici derivati dalla farmacologica, e procedimenti di 5,6-diidro-11h-dibenzo (b,e)fabbricazione relativi |
| EP0419861B1 (de) * | 1989-08-29 | 1995-11-02 | Boehringer Ingelheim Pharmaceuticals Inc. | Verwendung von Dibenzo[b,f][1,4]oxazepin (und thiazepin)-11(10H)-one und -thione zur Herstellung eines Arzneimittels zur Prävention und Behandlung von AIDS |
| US5493020A (en) * | 1993-07-29 | 1996-02-20 | Genentech, Inc. | Tricyclic inhibitors of the GPIIb IIIa receptor |
| US5512563A (en) * | 1993-07-29 | 1996-04-30 | American Cyanamid Company | Tricyclic benzazepine vasopressin antagonists |
| EP0910563B1 (de) * | 1995-06-29 | 2003-05-02 | Smithkline Beecham Corporation | Integrin-rezeptor-antagonisten |
| CO4920232A1 (es) * | 1997-01-08 | 2000-05-29 | Smithkline Beecham Corp | Acidos aceticos dibenzo [a,d] cicloheptano con actividad antagonista del receptor de vitronectin |
-
1998
- 1998-09-03 WO PCT/US1998/018379 patent/WO1999011626A1/en not_active Ceased
- 1998-09-03 JP JP2000508666A patent/JP2001514253A/ja not_active Withdrawn
- 1998-09-03 CA CA002304117A patent/CA2304117A1/en not_active Abandoned
- 1998-09-03 EP EP98944735A patent/EP1027337A4/de not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999011626A1 (en) | 1999-03-11 |
| EP1027337A4 (de) | 2002-04-03 |
| JP2001514253A (ja) | 2001-09-11 |
| EP1027337A1 (de) | 2000-08-16 |
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Legal Events
| Date | Code | Title | Description |
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| FZDE | Dead |