PE20050554A1 - DERIVADOS DE AZAINZOL COMO INHIBIDORES DEL FACTOR Xa - Google Patents
DERIVADOS DE AZAINZOL COMO INHIBIDORES DEL FACTOR XaInfo
- Publication number
- PE20050554A1 PE20050554A1 PE2004000481A PE2004000481A PE20050554A1 PE 20050554 A1 PE20050554 A1 PE 20050554A1 PE 2004000481 A PE2004000481 A PE 2004000481A PE 2004000481 A PE2004000481 A PE 2004000481A PE 20050554 A1 PE20050554 A1 PE 20050554A1
- Authority
- PE
- Peru
- Prior art keywords
- alkylene
- azetidine
- alkyl
- direct link
- factor
- Prior art date
Links
- 108010074860 Factor Xa Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- -1 INDOLYL Chemical class 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 abstract 1
- 241000282693 Cercopithecidae Species 0.000 abstract 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 1
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical class [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical compound O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 229940012414 factor viia Drugs 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A DERIVADOS DE AZAINZOL DE FORMULA (I), EN DONDE R0 ES UN ARILO(6 A 14 MIEMBROS) MONO O BICICLO COMO FENILO, HETEROCICLILO DEL GRUPO BENCIMIDAZOLILO, INDOLILO, BENZOTIOFURANILO, BENZOTIAZOLILO, DEL GRUPO PIRIDILO, FURILO, ENTRE OTROS OPCIONALMENTE SUSTITUIDOS POR R8; D ES UN RESTO DE AZETIDINA, PIRIDILO, PIRIDIL-N-OXIDO, PIRROLILO, TIENILO, IMIDAZOLILO, ENTRE OTROS OPCIONALMENTE SUSTITUIDOS CON R3 O =O; Q ES UN ENLACE DIRECTO, -C(O)-, -SO2-, ALQUILENO(C1-C6) O ALQUILENO(C0-C2)-C(O)-NR10-; R1 ES H, ALQUILO(C1-C2), ENTRE OTROS; R2 ES UN ENLACE DIRECTO O ALQUILENO(C1-C2); O R1-N-R2-V PUEDE FORMAR UN CICLICO DE 4 A 7 MIEMBROS DEL GRUPO AZETIDINA, AZETIDINONA, PIRROLIDINA, PIPERIDINA, ENTRE OTROS; V ES DERIVADO DE AZAINDOLILO(1H-PIRROLOPIRIDILO), AZETIDINA, 1,4-DIAZEPANO, ENTRE OTROS; O ES FENILO; G ES UN ENLACE DIRECTO, -(CH2)m, -C(O)- O -(CH2)mNR10-; M ES H, ALQUILO(C2-C4), AZEPANILO, CICLOPROPILO, ENTRE OTROS; R3 ES H, F, Cl, ALQUILO(C1-C4), ALQUILENO(C0-C2)-OR19, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ESTER METILICO DE ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-2-(1-ISOPROPIL-PIPERIDIN-4-ILCARBAMOIL)-1H-PIRROLO[2,3-b]PIRIDINA-5-CARBOXILICO, (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DE ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-5-OXO-4,5-DIHIDRO-1H-PIRROLO[3,2-b]PIRIDINA-2-CARBOXILICO, ENTRE OTROS. ESTOS COMPUESTOS SON INHIBIDORES REVERSIBLES DE LAS ENZIMAS DE COAGULACION SANGUINEA FACTOR Xa (FXa) Y/O FACTOR VIIa
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03011304A EP1479680A1 (en) | 2003-05-19 | 2003-05-19 | Azaindole derivatives as Factor Xa inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20050554A1 true PE20050554A1 (es) | 2005-08-04 |
Family
ID=33040951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2004000481A PE20050554A1 (es) | 2003-05-19 | 2004-05-11 | DERIVADOS DE AZAINZOL COMO INHIBIDORES DEL FACTOR Xa |
Country Status (24)
| Country | Link |
|---|---|
| EP (2) | EP1479680A1 (es) |
| JP (1) | JP4733642B2 (es) |
| KR (1) | KR20060012636A (es) |
| CN (1) | CN100347172C (es) |
| AR (1) | AR045682A1 (es) |
| AU (1) | AU2004238500B2 (es) |
| BR (1) | BRPI0410429A (es) |
| CA (1) | CA2526084A1 (es) |
| CL (1) | CL2004001079A1 (es) |
| CR (1) | CR8088A (es) |
| EC (1) | ECSP056179A (es) |
| MA (1) | MA27799A1 (es) |
| MX (1) | MXPA05012156A (es) |
| NO (1) | NO20055911L (es) |
| NZ (1) | NZ543669A (es) |
| OA (1) | OA13169A (es) |
| PE (1) | PE20050554A1 (es) |
| RS (1) | RS20050857A (es) |
| RU (1) | RU2330853C2 (es) |
| TN (1) | TNSN05296A1 (es) |
| TW (1) | TW200510411A (es) |
| UA (1) | UA86767C2 (es) |
| WO (1) | WO2004101563A1 (es) |
| ZA (1) | ZA200508150B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2417226C2 (ru) * | 2005-11-18 | 2011-04-27 | Ф.Хоффманн-Ля Рош Аг | Производные азаиндол-2-карбоксамида |
| US8883819B2 (en) | 2011-09-01 | 2014-11-11 | Irm Llc | Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension |
| IN2015DN01061A (es) | 2012-08-17 | 2015-06-26 | Bayer Cropscience Ag | |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| CN111834531B (zh) * | 2019-04-15 | 2022-04-19 | 天津大学 | 一种有机半导体材料、制备方法及应用 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1241472B (it) | 1990-07-06 | 1994-01-17 | Olivier Linda | Dispositivo elettromeccanico per la cattura continua in particolare di topi e ratti. |
| 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 |
| JP3655632B2 (ja) | 1994-04-26 | 2005-06-02 | アベンティス・ファーマスーティカルズ・インコーポレイテッド | 第Ｘａ因子インヒビター |
| ZA964008B (en) * | 1995-06-02 | 1997-07-11 | Akzo Nobel Nv | Imidazo[1,5a]pyridine derived serine protease inhibitors |
| CA2315070A1 (en) * | 1997-12-17 | 1999-07-01 | Schering Aktiengesellschaft | Ortho-anthranilamide derivatives as anti-coagulants |
| ES2241194T3 (es) * | 1997-12-24 | 2005-10-16 | Aventis Pharma Deutschland Gmbh | Derivados de indol en calidad de inhibidores de factor xa. |
| EP0987274A1 (en) | 1998-09-15 | 2000-03-22 | Hoechst Marion Roussel Deutschland GmbH | Factor VIIa Inhibitors |
| JP4241970B2 (ja) * | 1998-10-30 | 2009-03-18 | 中外製薬株式会社 | アミド結合を有するインドール誘導体、及びモノ又はジアザインドール誘導体 |
| CZ2002961A3 (cs) * | 1999-09-17 | 2002-08-14 | Millennium Pharmaceuticals, Inc. | Benzamidy a příbuzné sloučeniny pro inhibici faktoru Xa |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| JP2001294572A (ja) * | 2000-02-09 | 2001-10-23 | Dai Ichi Seiyaku Co Ltd | 新規スルホニル誘導体 |
| US6436965B1 (en) * | 2000-03-02 | 2002-08-20 | Merck Frosst Canada & Co. | PDE IV inhibiting amides, compositions and methods of treatment |
| AU2001273040A1 (en) * | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| CA2440803A1 (en) * | 2001-03-07 | 2002-09-12 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| US6790845B2 (en) * | 2001-04-09 | 2004-09-14 | Bristol-Myers Squibb Pharma Company | Fused heterocyclic inhibitors of factor Xa |
| EP1314733A1 (en) * | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
| WO2003053361A2 (en) * | 2001-12-20 | 2003-07-03 | Osi Pharmaceuticals, Inc. | PYRROLOPYRIMIDINE A2b SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE |
| DE10214832A1 (de) * | 2002-04-04 | 2003-10-16 | Merck Patent Gmbh | Phenylderivate 4 |
| JP2004203791A (ja) * | 2002-12-25 | 2004-07-22 | Dai Ichi Seiyaku Co Ltd | 芳香族化合物 |
| JP2004210716A (ja) * | 2002-12-27 | 2004-07-29 | Dai Ichi Seiyaku Co Ltd | ジアミド誘導体 |
| US7135469B2 (en) * | 2003-03-18 | 2006-11-14 | Bristol Myers Squibb, Co. | Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors |
-
2003
- 2003-05-19 EP EP03011304A patent/EP1479680A1/en not_active Withdrawn
-
2004
- 2004-05-05 AU AU2004238500A patent/AU2004238500B2/en not_active Expired - Fee Related
- 2004-05-05 RS YUP-2005/0857A patent/RS20050857A/sr unknown
- 2004-05-05 MX MXPA05012156A patent/MXPA05012156A/es active IP Right Grant
- 2004-05-05 CA CA002526084A patent/CA2526084A1/en not_active Abandoned
- 2004-05-05 RU RU2005139557/04A patent/RU2330853C2/ru not_active IP Right Cessation
- 2004-05-05 EP EP04731161.8A patent/EP1636226B1/en not_active Expired - Lifetime
- 2004-05-05 WO PCT/EP2004/004754 patent/WO2004101563A1/en active Application Filing
- 2004-05-05 JP JP2006529743A patent/JP4733642B2/ja not_active Expired - Fee Related
- 2004-05-05 NZ NZ543669A patent/NZ543669A/en unknown
- 2004-05-05 CN CNB2004800139362A patent/CN100347172C/zh not_active Expired - Fee Related
- 2004-05-05 KR KR1020057022131A patent/KR20060012636A/ko not_active Ceased
- 2004-05-05 OA OA1200500323A patent/OA13169A/en unknown
- 2004-05-05 UA UAA200512133A patent/UA86767C2/ru unknown
- 2004-05-05 BR BRPI0410429-3A patent/BRPI0410429A/pt not_active IP Right Cessation
- 2004-05-11 PE PE2004000481A patent/PE20050554A1/es not_active Application Discontinuation
- 2004-05-17 TW TW093113797A patent/TW200510411A/zh unknown
- 2004-05-17 CL CL200401079A patent/CL2004001079A1/es unknown
- 2004-05-17 AR ARP040101694A patent/AR045682A1/es unknown
-
2005
- 2005-10-10 ZA ZA200508150A patent/ZA200508150B/en unknown
- 2005-11-08 MA MA28588A patent/MA27799A1/fr unknown
- 2005-11-11 CR CR8088A patent/CR8088A/es not_active Application Discontinuation
- 2005-11-18 EC EC2005006179A patent/ECSP056179A/es unknown
- 2005-11-18 TN TNP2005000296A patent/TNSN05296A1/en unknown
- 2005-12-13 NO NO20055911A patent/NO20055911L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006528214A (ja) | 2006-12-14 |
| WO2004101563A1 (en) | 2004-11-25 |
| CR8088A (es) | 2006-09-22 |
| NO20055911L (no) | 2006-02-10 |
| AU2004238500B2 (en) | 2010-07-22 |
| MA27799A1 (fr) | 2006-03-01 |
| KR20060012636A (ko) | 2006-02-08 |
| CA2526084A1 (en) | 2004-11-25 |
| EP1479680A1 (en) | 2004-11-24 |
| EP1636226B1 (en) | 2014-10-15 |
| HK1089175A1 (zh) | 2006-11-24 |
| BRPI0410429A (pt) | 2006-06-06 |
| NZ543669A (en) | 2008-12-24 |
| RU2330853C2 (ru) | 2008-08-10 |
| CL2004001079A1 (es) | 2005-04-08 |
| AR045682A1 (es) | 2005-11-09 |
| RS20050857A (en) | 2007-11-15 |
| CN100347172C (zh) | 2007-11-07 |
| CN1791601A (zh) | 2006-06-21 |
| RU2005139557A (ru) | 2007-06-27 |
| UA86767C2 (ru) | 2009-05-25 |
| AU2004238500A1 (en) | 2004-11-25 |
| MXPA05012156A (es) | 2006-08-18 |
| TNSN05296A1 (en) | 2007-07-10 |
| JP4733642B2 (ja) | 2011-07-27 |
| TW200510411A (en) | 2005-03-16 |
| OA13169A (en) | 2006-12-13 |
| ZA200508150B (en) | 2007-02-28 |
| ECSP056179A (es) | 2006-08-30 |
| EP1636226A1 (en) | 2006-03-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |