BR0013926A - Inibidores de serina protease de azacicloalcanona - Google Patents
Inibidores de serina protease de azacicloalcanonaInfo
- Publication number
- BR0013926A BR0013926A BR0013926-2A BR0013926A BR0013926A BR 0013926 A BR0013926 A BR 0013926A BR 0013926 A BR0013926 A BR 0013926A BR 0013926 A BR0013926 A BR 0013926A
- Authority
- BR
- Brazil
- Prior art keywords
- sup
- sub
- methylene
- ethylene
- alkyl
- Prior art date
Links
- 239000003001 serine protease inhibitor Substances 0.000 title 1
- -1 biphenylyl Chemical group 0.000 abstract 4
- 229940123583 Factor Xa inhibitor Drugs 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 1
- 239000005977 Ethylene Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 abstract 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 abstract 1
- 125000005518 carboxamido group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 230000001732 thrombotic effect Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
"INIBIDORES DE SERINA PROTEASE DE AZACICLOALCANONA". A presente invenção é voltada as inibidores não peptídicos do fator Xa que são úteis para o tratamento de distúrbios oclusivos trombóticos arteriais e venosos, inflamação, câncer e doenças neurodegenerativas. Os inibidores do fator Xa proporcionam compostos tendo a fórmula (I) ou sais seus aceitáveis do ponto de vista farmacêutico; sendo Q fenila, benzila, piridila, tienila, indolila, quinolinila, benzotienila, bifenilila, ou imidazolila; qualquer um dos quais pode incluir um ou mais substituintes opcionais independentemente selecionado dentre halo, trifluormetil, hidróxi, amino, nitro, ciano, alcóxi C~ 1-3~, alquila C~ 1-3~, metileno-dióxi, carboxamido, acetamido, ou amidino; X é metileno, carbonila ou sulfonila; Z é metileno, etileno, ou propileno; M é metileno ou etileno; e R^ 1^, R^ 2^ e R^ 3^ são independentemente hidrogênio ou alquila C~ 1-3~.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15323699P | 1999-09-13 | 1999-09-13 | |
| PCT/US2000/025006 WO2001019795A1 (en) | 1999-09-13 | 2000-09-13 | Azacycloalkanone serine protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0013926A true BR0013926A (pt) | 2002-07-23 |
Family
ID=22546339
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0013926-2A BR0013926A (pt) | 1999-09-13 | 2000-09-13 | Inibidores de serina protease de azacicloalcanona |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US6469029B1 (pt) |
| EP (1) | EP1212300B1 (pt) |
| JP (1) | JP2003509409A (pt) |
| KR (1) | KR20020027639A (pt) |
| CN (1) | CN1373755A (pt) |
| AT (1) | ATE253558T1 (pt) |
| AU (1) | AU7480800A (pt) |
| BR (1) | BR0013926A (pt) |
| CA (1) | CA2384247A1 (pt) |
| DE (1) | DE60006407T2 (pt) |
| DK (1) | DK1212300T3 (pt) |
| ES (1) | ES2209987T3 (pt) |
| HK (1) | HK1050005A1 (pt) |
| IL (1) | IL148358A0 (pt) |
| MX (1) | MXPA02002657A (pt) |
| NO (1) | NO322753B1 (pt) |
| NZ (1) | NZ517603A (pt) |
| PL (1) | PL354265A1 (pt) |
| PT (1) | PT1212300E (pt) |
| WO (1) | WO2001019795A1 (pt) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI290136B (en) | 2000-04-05 | 2007-11-21 | Daiichi Seiyaku Co | Ethylenediamine derivatives |
| HUP0304058A2 (hu) | 2001-01-30 | 2004-04-28 | Bristol-Myers Squibb Company | Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények |
| EP1395560A1 (en) | 2001-05-23 | 2004-03-10 | Ucb, S.A. | 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivativ es for the treatment of epilepsy and other neurological disorders |
| WO2003000657A1 (en) | 2001-06-20 | 2003-01-03 | Daiichi Pharmaceutical Co., Ltd. | Diamine derivatives |
| GB0127568D0 (en) * | 2001-11-16 | 2002-01-09 | Glaxo Group Ltd | Chemical compounds |
| EP1569912B1 (en) | 2002-12-03 | 2015-04-29 | Pharmacyclics, Inc. | 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors |
| US20070191306A1 (en) * | 2005-08-17 | 2007-08-16 | Bristol-Myers Squibb Company | FACTOR Xa INHIBITOR FORMULATION AND METHOD |
| WO2009096198A1 (ja) * | 2008-02-01 | 2009-08-06 | Pharma Ip Limited Liability Intermediary Corporations | 新規ビアリール誘導体 |
| CN103910688B (zh) * | 2013-01-04 | 2016-05-25 | 陈春麟 | 2-丙基-4-氯喹唑啉衍生物及其制备方法和应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4727064A (en) | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
| GB8506792D0 (en) | 1985-03-15 | 1985-04-17 | Janssen Pharmaceutica Nv | Derivatives of y-cyclodextrin |
| US5002935A (en) | 1987-12-30 | 1991-03-26 | University Of Florida | Improvements in redox systems for brain-targeted drug delivery |
| US5385885A (en) | 1988-01-15 | 1995-01-31 | Gasic; Gregory P. | Inhibition of smooth muscle cell proliferation by antistasin and tick anticoagulant peptide |
| DE4121947A1 (de) | 1991-07-03 | 1993-01-07 | Basf Ag | 2-(3-(4-amidino-phenyl))-propionsaeurederivate, ihre herstellung und verwendung |
| CA2075154A1 (en) * | 1991-08-06 | 1993-02-07 | Neelakantan Balasubramanian | Peptide aldehydes as antithrombotic agents |
| WO1994020535A1 (en) | 1992-12-11 | 1994-09-15 | Corvas International, Inc. | ECOTIN AS A FACTOR Xa, XIa, AND XIIa INHIBITOR |
| JPH10503176A (ja) * | 1994-06-17 | 1998-03-24 | コーバス インターナショナル， インコーポレイテッド | 酵素インヒビターとしての３−アミノ−２−オキソ−１−ピペリジン酢酸誘導体 |
| US5703208A (en) | 1994-06-17 | 1997-12-30 | Corvas International, Inc. | 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors |
| JPH11508558A (ja) * | 1995-06-27 | 1999-07-27 | メルク エンド カンパニー インコーポレーテッド | ピリジノン トロンビン阻害剤 |
| JPH09165370A (ja) * | 1995-10-13 | 1997-06-24 | Fuji Yakuhin Kogyo Kk | ラクタム誘導体およびその塩 |
| AU719216B2 (en) | 1996-02-13 | 2000-05-04 | Akzo Nobel N.V. | Serine protease inhibitors |
| EP0923372A4 (en) | 1996-02-22 | 2001-09-05 | Merck & Co Inc | INHIBITORS OF PYRIDINONE THROMBIN |
| CA2250426C (en) | 1996-03-29 | 2006-05-02 | 3-Dimensional Pharmaceuticals, Inc. | Amidinohydrazones as protease inhibitors |
| WO1998016523A2 (en) | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
| WO1999007732A1 (en) | 1997-08-11 | 1999-02-18 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
| WO1999007731A1 (en) | 1997-08-11 | 1999-02-18 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
| JP2001524467A (ja) | 1997-11-26 | 2001-12-04 | ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド | ヘテロアリールアミノグアニジンおよびアルコキシグアニジンおよびプロテアーゼインヒビターとしてのこれらの使用 |
-
2000
- 2000-09-13 HK HK03102217.0A patent/HK1050005A1/zh unknown
- 2000-09-13 AU AU74808/00A patent/AU7480800A/en not_active Abandoned
- 2000-09-13 JP JP2001523375A patent/JP2003509409A/ja active Pending
- 2000-09-13 AT AT00963388T patent/ATE253558T1/de not_active IP Right Cessation
- 2000-09-13 IL IL14835800A patent/IL148358A0/xx unknown
- 2000-09-13 DE DE60006407T patent/DE60006407T2/de not_active Expired - Fee Related
- 2000-09-13 ES ES00963388T patent/ES2209987T3/es not_active Expired - Lifetime
- 2000-09-13 US US09/661,327 patent/US6469029B1/en not_active Expired - Lifetime
- 2000-09-13 PT PT00963388T patent/PT1212300E/pt unknown
- 2000-09-13 MX MXPA02002657A patent/MXPA02002657A/es unknown
- 2000-09-13 WO PCT/US2000/025006 patent/WO2001019795A1/en not_active Ceased
- 2000-09-13 CN CN00812827A patent/CN1373755A/zh active Pending
- 2000-09-13 EP EP00963388A patent/EP1212300B1/en not_active Expired - Lifetime
- 2000-09-13 KR KR1020027003241A patent/KR20020027639A/ko not_active Withdrawn
- 2000-09-13 CA CA002384247A patent/CA2384247A1/en not_active Abandoned
- 2000-09-13 BR BR0013926-2A patent/BR0013926A/pt not_active Application Discontinuation
- 2000-09-13 NZ NZ517603A patent/NZ517603A/en unknown
- 2000-09-13 PL PL00354265A patent/PL354265A1/xx not_active Application Discontinuation
- 2000-09-13 DK DK00963388T patent/DK1212300T3/da active
-
2002
- 2002-03-12 NO NO20021224A patent/NO322753B1/no unknown
- 2002-09-16 US US10/243,938 patent/US6962942B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU7480800A (en) | 2001-04-17 |
| NO20021224L (no) | 2002-05-13 |
| PT1212300E (pt) | 2004-03-31 |
| WO2001019795A1 (en) | 2001-03-22 |
| PL354265A1 (en) | 2003-12-29 |
| JP2003509409A (ja) | 2003-03-11 |
| US20030109517A1 (en) | 2003-06-12 |
| ATE253558T1 (de) | 2003-11-15 |
| HK1050005A1 (zh) | 2003-06-06 |
| KR20020027639A (ko) | 2002-04-13 |
| DK1212300T3 (da) | 2004-03-15 |
| EP1212300A1 (en) | 2002-06-12 |
| NZ517603A (en) | 2003-09-26 |
| NO20021224D0 (no) | 2002-03-12 |
| DE60006407T2 (de) | 2004-09-09 |
| CN1373755A (zh) | 2002-10-09 |
| MXPA02002657A (es) | 2002-10-28 |
| CA2384247A1 (en) | 2001-03-22 |
| US6962942B2 (en) | 2005-11-08 |
| ES2209987T3 (es) | 2004-07-01 |
| US6469029B1 (en) | 2002-10-22 |
| IL148358A0 (en) | 2002-09-12 |
| NO322753B1 (no) | 2006-12-04 |
| EP1212300B1 (en) | 2003-11-05 |
| DE60006407D1 (de) | 2003-12-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |