BR0115938A - Derivados de guanidina e amidina com inibidores do fator xa - Google Patents
Derivados de guanidina e amidina com inibidores do fator xaInfo
- Publication number
- BR0115938A BR0115938A BR0115938-0A BR0115938A BR0115938A BR 0115938 A BR0115938 A BR 0115938A BR 0115938 A BR0115938 A BR 0115938A BR 0115938 A BR0115938 A BR 0115938A
- Authority
- BR
- Brazil
- Prior art keywords
- factor
- compounds
- inhibitors
- formula
- guanidine
- Prior art date
Links
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical class NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 title abstract 4
- 229940123583 Factor Xa inhibitor Drugs 0.000 title abstract 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001409 amidines Chemical class 0.000 title abstract 2
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 title abstract 2
- 108010074860 Factor Xa Proteins 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
"DERIVADOS DE GUANIDINA E AMIDINA COMO INIBIDORES DO FATOR XA". A presente invenção refere-se a compostos da fórmula I, onde R~ 0~, Q, X, Q, D, R~ 10~ e V têm os significados indicados nas reivindicações. Os compostos da fórmula I são compostos farmacologicamente ativos valiosos. Eles apresentam um forte efeito antitrombótico e são adequados, por exemplo, para a terapia e a profilaxia de distúrbios cardiovasculares como doenças tromboembólicas ou restenoses. Eles são inibidores reversíveis das enzimas de coagulação do sangue fator Xa (FXa) e/ou fator Vlla (FVlla), e em geral podem ser aplicados em condições em que esteja presente uma atividade indesejada do fator Xa e/ou do fator Vlla ou para cuja cura ou prevenção se deseja uma inibição do fator Xa e/ou do fator Vlla. A invenção referese ainda a processos para a preparação de compostos da fórmula (I), seus uso, em particular como ingredientes ativos em farmacêuticos, e preparados farmacêuticos compreendendo os mesmos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00126750 | 2000-12-06 | ||
| PCT/EP2001/013874 WO2002046159A1 (en) | 2000-12-06 | 2001-11-28 | Guanidine and amidine derivatives as factor xa inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0115938A true BR0115938A (pt) | 2003-12-23 |
Family
ID=8170585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0115938-0A BR0115938A (pt) | 2000-12-06 | 2001-11-28 | Derivados de guanidina e amidina com inibidores do fator xa |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US20020173656A1 (pt) |
| EP (1) | EP1345900B1 (pt) |
| JP (1) | JP4274522B2 (pt) |
| KR (1) | KR20040015036A (pt) |
| CN (1) | CN1479722A (pt) |
| AR (1) | AR033684A1 (pt) |
| AU (2) | AU2002233206B2 (pt) |
| BR (1) | BR0115938A (pt) |
| CA (1) | CA2430518C (pt) |
| CZ (1) | CZ20031554A3 (pt) |
| DE (1) | DE60126143T2 (pt) |
| DK (1) | DK1345900T3 (pt) |
| EE (1) | EE200300192A (pt) |
| ES (1) | ES2278798T3 (pt) |
| HR (1) | HRP20030447A2 (pt) |
| HU (1) | HUP0302604A3 (pt) |
| IL (2) | IL156214A0 (pt) |
| MX (1) | MXPA03004848A (pt) |
| NO (1) | NO20032489L (pt) |
| NZ (1) | NZ526269A (pt) |
| PL (1) | PL362320A1 (pt) |
| PT (1) | PT1345900E (pt) |
| RU (1) | RU2003120070A (pt) |
| SK (1) | SK6862003A3 (pt) |
| WO (1) | WO2002046159A1 (pt) |
| ZA (1) | ZA200303847B (pt) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003265398A1 (en) * | 2002-08-09 | 2004-02-25 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds and methods to modulate coagulation |
| US7405210B2 (en) | 2003-05-21 | 2008-07-29 | Osi Pharmaceuticals, Inc. | Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase |
| US7544699B2 (en) * | 2003-08-08 | 2009-06-09 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions, and methods of use |
| US7208601B2 (en) * | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
| US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
| US8603481B2 (en) * | 2003-10-10 | 2013-12-10 | Chugai Seiyaku Kabushiki Kaisha | Therapeutic agents for solid tumors |
| DE602005023965D1 (de) | 2004-03-08 | 2010-11-18 | Prosidion Ltd | Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase |
| ATE424821T1 (de) | 2004-12-02 | 2009-03-15 | Prosidion Ltd | Pyrrolopyridin-2-karbonsäureamide |
| DE102006048300A1 (de) * | 2006-01-26 | 2007-08-02 | Hellstern, Peter, Prof. Dr.med. | Inhibitoren des Blutgerinnungsfaktors Xa zur Verwendung als Antikoagulans |
| WO2010098866A1 (en) | 2009-02-27 | 2010-09-02 | Supergen, Inc. | Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors |
| US8507640B2 (en) | 2010-08-19 | 2013-08-13 | International Business Machines Corporation | Methods of ring opening polymerization and catalysts therefor |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| AU2018346597B2 (en) | 2017-10-06 | 2023-07-13 | Forma Therapeutics, Inc. | Inhibiting Ubiquitin Specific Peptidase 30 |
| JP7449242B2 (ja) | 2018-05-17 | 2024-03-13 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的ペプチダーゼ３０（ｕｓｐ３０）阻害剤として有用な縮合二環化合物 |
| JP7530889B2 (ja) | 2018-10-05 | 2024-08-08 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ３０（ｕｓｐ３０）阻害剤として作用する縮合ピロリン |
| US12440481B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| US20250389737A1 (en) * | 2024-06-20 | 2025-12-25 | Instrumentation Laboratory Company | FACTOR Xa REAGENT |
| EP4667582A1 (en) * | 2024-06-20 | 2025-12-24 | Instrumentation Laboratory Company | Factor xa reagent |
| CN121608507B (zh) * | 2026-02-02 | 2026-04-17 | 肃宁县中原纺织有限责任公司 | 一种充气浮桥高压气肋外层材料及其制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201303B (pt) * | 1990-07-05 | 1993-03-01 | Hoffmann La Roche | |
| US5506134A (en) | 1990-10-22 | 1996-04-09 | Corvas International, Inc. | Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex |
| US5833982A (en) | 1991-02-28 | 1998-11-10 | Zymogenetics, Inc. | Modified factor VII |
| US5788965A (en) | 1991-02-28 | 1998-08-04 | Novo Nordisk A/S | Modified factor VII |
| ES2103181B1 (es) * | 1994-08-01 | 1998-04-01 | Menarini Lab | Amidas naftalenicas con accion antagonista de los leucotrienos. |
| EP1384725A3 (en) * | 1994-04-26 | 2007-02-21 | Aventis Pharmaceuticals Inc. | Factor Xa inhibitors |
| US5792769A (en) * | 1995-09-29 | 1998-08-11 | 3-Dimensional Pharmaceuticals, Inc. | Guanidino protease inhibitors |
| GB9602166D0 (en) * | 1996-02-02 | 1996-04-03 | Zeneca Ltd | Aminoheterocyclic derivatives |
| TW542822B (en) * | 1997-01-17 | 2003-07-21 | Ajinomoto Kk | Benzamidine derivatives |
| EP1007037A4 (en) * | 1997-06-26 | 2004-10-06 | Lilly Co Eli | ANTITHROMBOTIC AGENTS |
| EP1080075B1 (en) * | 1998-03-23 | 2004-08-11 | Aventis Pharmaceuticals Inc. | Piperididinyl and n-amidinopiperidinyl derivatives |
| US20020016339A1 (en) * | 1998-03-23 | 2002-02-07 | Klein Scott I. | Piperididinyl and N-amidinopiperidinyl derivatives |
| EP0987274A1 (en) | 1998-09-15 | 2000-03-22 | Hoechst Marion Roussel Deutschland GmbH | Factor VIIa Inhibitors |
| ES2316383T3 (es) * | 1999-09-17 | 2009-04-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
-
2001
- 2001-11-28 PL PL01362320A patent/PL362320A1/xx unknown
- 2001-11-28 DE DE60126143T patent/DE60126143T2/de not_active Expired - Lifetime
- 2001-11-28 PT PT01984775T patent/PT1345900E/pt unknown
- 2001-11-28 JP JP2002547898A patent/JP4274522B2/ja not_active Expired - Fee Related
- 2001-11-28 RU RU2003120070/04A patent/RU2003120070A/ru not_active Application Discontinuation
- 2001-11-28 HR HR20030447A patent/HRP20030447A2/hr not_active Application Discontinuation
- 2001-11-28 HU HU0302604A patent/HUP0302604A3/hu unknown
- 2001-11-28 NZ NZ526269A patent/NZ526269A/en unknown
- 2001-11-28 BR BR0115938-0A patent/BR0115938A/pt not_active Application Discontinuation
- 2001-11-28 CN CNA018201121A patent/CN1479722A/zh active Pending
- 2001-11-28 KR KR10-2003-7007612A patent/KR20040015036A/ko not_active Withdrawn
- 2001-11-28 EE EEP200300192A patent/EE200300192A/xx unknown
- 2001-11-28 CA CA2430518A patent/CA2430518C/en not_active Expired - Fee Related
- 2001-11-28 IL IL15621401A patent/IL156214A0/xx unknown
- 2001-11-28 AU AU2002233206A patent/AU2002233206B2/en not_active Ceased
- 2001-11-28 WO PCT/EP2001/013874 patent/WO2002046159A1/en not_active Ceased
- 2001-11-28 DK DK01984775T patent/DK1345900T3/da active
- 2001-11-28 SK SK686-2003A patent/SK6862003A3/sk unknown
- 2001-11-28 CZ CZ20031554A patent/CZ20031554A3/cs unknown
- 2001-11-28 AU AU3320602A patent/AU3320602A/xx active Pending
- 2001-11-28 EP EP01984775A patent/EP1345900B1/en not_active Expired - Lifetime
- 2001-11-28 MX MXPA03004848A patent/MXPA03004848A/es active IP Right Grant
- 2001-11-28 ES ES01984775T patent/ES2278798T3/es not_active Expired - Lifetime
- 2001-12-04 AR ARP010105642A patent/AR033684A1/es unknown
- 2001-12-06 US US10/004,422 patent/US20020173656A1/en not_active Abandoned
-
2003
- 2003-05-19 ZA ZA200303847A patent/ZA200303847B/en unknown
- 2003-05-29 IL IL156214A patent/IL156214A/en not_active IP Right Cessation
- 2003-06-02 NO NO20032489A patent/NO20032489L/no not_active Application Discontinuation
-
2004
- 2004-07-07 US US10/886,312 patent/US7435747B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25D | Requested change of name of applicant approved |
Owner name: SANOFI-AVENTIS DEUTSCHLAND GMBH (DE) Free format text: ALTERADO DE: AVENTIS PHARMA DEUTSCHLAND GMBH |
|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL. |