PE20040925A1 - DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa - Google Patents
DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR XaInfo
- Publication number
- PE20040925A1 PE20040925A1 PE2004000015A PE2004000015A PE20040925A1 PE 20040925 A1 PE20040925 A1 PE 20040925A1 PE 2004000015 A PE2004000015 A PE 2004000015A PE 2004000015 A PE2004000015 A PE 2004000015A PE 20040925 A1 PE20040925 A1 PE 20040925A1
- Authority
- PE
- Peru
- Prior art keywords
- members
- thiofen
- mono
- alkylene
- compounds
- Prior art date
Links
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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
-
- 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
-
- 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
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Surgery (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE A COMPUESTOS DE FORMULA I, DONDE R0 ES UN HETEROCICLILO MONO O BICICLICO DE 4 A 15 MIEMBROS QUE CONTIENE DE 1 A 4 HETEROATOMOS DE N, S Y O, OPCIONALMENTE SUSTITUIDO; UN HETEROCICLILO SELECCIONADO DE BENZOIMIDAZOLILO, 1,3-BENZODIOXOLILO, BENZOFURANILO, BENZOXAZOLILO, ENTRE OTROS, UN ARILO MONO O BICICLICO DE 6 A 14 MIEMBROS, OPCIONALMENTE SUSTITUIDO POR R8; Q ES UN ENLACE DIRECTO, -ALQUILENO(C0-C2)-C(O)-NR10-, -NR10-C(O)-NR10-, -NR10-C(O)-, -SO2-, ENTRE OTROS; R1 ES H, ALQUILO(C1-C4), ALQUILENO(C1-C3)-C(O)-NH-R0, ENTRE OTROS; R2 ES UN ENLACE DIRECTO O ALQUILENO (C1-C4), O R1 Y R3 JUNTOS FORMARIAN UN GRUPO CICLICO DE 6 A 8 MIEMBROS CON 1 A 4 HETEROATOMOS DE N, S Y O; V ES UN RESTO CICLICO DE 3 A 7 MIEMBROS, ARILO DE 6 A 14 MIEMBROS O HETEROCICLILO MONO O BICICLICO DE 4 A 15 MIEMBROS OPCIONALMENTE SUSTITUIDO POR R14; G ES UN ENLACE DIRECTO, -(CH2)m-NR10-SO2-NR10-(CH2)n-, -(CH2)m-CH(OH)-(CH2)n, -(CH2)m, ENTRE OTROS; M ES H, -ALQUILO(C1-C8), -C(O)-N(R11)-R12-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 2-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-5-TIOFEN-2-IL-2H-PIRAZOL-3-CARBOXILICO, (1-ISOPROPIL-PIPERIDIN-4-IL)-AMIDA DEL ACIDO 1-[5-(5-CLORO-TIOFEN-2-IL)-ISOXAZOL-3-ILMETIL]-5-TIOFEN-2-IL-1H-PIRAZOL-3-CARBOXILICO, ENTRE OTROS. ESTOS COMPUESTOS SON INHIBIDORESS REVERSIBLES DE LAS ENZIMAS DE COAGULACION SANGUINEA FACTOR Xa(FXa) Y/O FACTOR VIIa Y SON ADECUADOS PARAEL TRATAMIENTO DE ENFERMEDADES TROMBOEMBOLICAS Y REESTENOSIS
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02028915A EP1433788A1 (en) | 2002-12-23 | 2002-12-23 | Pyrazole-derivatives as factor Xa inhibitors |
EP03011308A EP1479678A1 (en) | 2003-05-19 | 2003-05-19 | Pyrazole-derivatives as factor xa inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20040925A1 true PE20040925A1 (es) | 2004-12-24 |
Family
ID=32683809
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2004000015A PE20040925A1 (es) | 2002-12-23 | 2004-01-05 | DERIVADOS DE PIRAZOL COMO INHIBIDORES DEL FACTOR Xa |
Country Status (13)
Country | Link |
---|---|
EP (1) | EP1581523B1 (es) |
JP (1) | JP4585448B2 (es) |
AR (1) | AR042648A1 (es) |
AT (1) | ATE444292T1 (es) |
AU (1) | AU2003292218A1 (es) |
BR (1) | BR0317659A (es) |
CA (1) | CA2511321A1 (es) |
DE (1) | DE60329529D1 (es) |
IL (1) | IL169323A0 (es) |
MX (1) | MXPA05006200A (es) |
PE (1) | PE20040925A1 (es) |
TW (1) | TW200505914A (es) |
WO (1) | WO2004056815A1 (es) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
ITMI20041032A1 (it) | 2004-05-24 | 2004-08-24 | Neuroscienze S C A R L | Compositi farmaceutici |
DE102004047255A1 (de) * | 2004-09-29 | 2006-04-13 | Merck Patent Gmbh | Prolinderivate |
WO2006047415A2 (en) | 2004-10-26 | 2006-05-04 | Janssen Pharmaceutica, N.V. | Factor xa compounds |
US7381732B2 (en) | 2004-10-26 | 2008-06-03 | Bristol-Myers Squibb Company | Pyrazolobenzamides and derivatives as factor Xa inhibitors |
WO2006050034A1 (en) * | 2004-10-29 | 2006-05-11 | Schering Corporation | Substituted 5-carboxyamide pyrazoles and [1,2,4]triazoles as antiviral agents |
US8110573B2 (en) | 2004-12-30 | 2012-02-07 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases |
EP1724269A1 (en) * | 2005-05-20 | 2006-11-22 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors |
WO2007002563A1 (en) * | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Imidazole based lxr modulators |
EP1968579A1 (en) | 2005-12-30 | 2008-09-17 | Astex Therapeutics Limited | Pharmaceutical compounds |
US8435970B2 (en) | 2006-06-29 | 2013-05-07 | Astex Therapeutics Limited | Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea |
EP2238127B1 (en) * | 2007-12-26 | 2012-08-15 | Sanofi | Pyrazole-carboxamide derivatives as p2y12 antagonists |
EP2238128B1 (en) * | 2007-12-26 | 2012-08-22 | Sanofi | Heterocyclic pyrazole-carboxamides as p2y12 antagonists |
EP2264017A4 (en) | 2008-04-04 | 2011-07-27 | Takeda Pharmaceutical | Heterocyclic derivative and its use |
JP5658138B2 (ja) * | 2008-04-23 | 2015-01-21 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 代謝障害の処置のためのカルボキサミド化合物 |
AR079967A1 (es) | 2010-01-26 | 2012-02-29 | Sanofi Aventis | Derivados de acido 3-heteroaroilamino-propionico sustituidos con oxigeno y su uso como productos farmaceuticos |
CN104940200B (zh) | 2010-03-30 | 2019-06-28 | 维颂公司 | 多取代芳族化合物作为凝血酶的抑制剂 |
TWI523844B (zh) | 2011-01-26 | 2016-03-01 | 賽諾菲公司 | 經胺基取代之3-雜芳醯基胺基-丙酸衍生物及其作為藥物之用途 |
UY33874A (es) | 2011-01-26 | 2012-08-31 | Sanofi Aventis | Derivados de ácido 3-heteroaroilamino-propiónico sustituidos y su uso como sustancias farmacéuticas |
CA2841905A1 (en) | 2011-07-26 | 2013-01-31 | Sanofi | 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals |
BR112014001587A2 (pt) | 2011-07-26 | 2017-02-14 | Sanofi Sa | derivados de ácido 3-(tiazol-4-carbonil)- ou 3-(tiazol-2-carbonil) amino-propiônico substituídos e seu uso como produtos farmacêuticos |
US20130123325A1 (en) | 2011-11-14 | 2013-05-16 | Sven Ruf | Use of boceprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases |
WO2013072328A1 (en) | 2011-11-14 | 2013-05-23 | Sanofi | Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases |
CN105209440B (zh) | 2013-03-15 | 2019-07-23 | 维颂公司 | 作为凝血酶抑制剂的卤代吡唑 |
SG10201707480PA (en) * | 2013-03-15 | 2017-10-30 | Verseon Corp | Multisubstituted aromatic compounds as serine protease inhibitors |
CN105073720B (zh) | 2013-03-28 | 2017-10-13 | 赛诺菲 | 联芳基‑丙酸衍生物及其作为药物的用途 |
AU2014243069B2 (en) | 2013-03-28 | 2017-12-21 | Sanofi | Biaryl-propionic acid derivatives and their use as pharmaceuticals |
EP3184095A1 (en) | 2013-05-23 | 2017-06-28 | IP Gesellschaft für Management mbH | Administration units comprising polymorph 1 of 2-(2-methylamino-pyrimidin-4-yl]-1h-indole-5-carboxylic acid [(s)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide |
CN106687445A (zh) | 2014-09-17 | 2017-05-17 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物 |
DK3261639T3 (da) | 2015-02-27 | 2022-10-31 | Verseon Int Corporation | Substituerede pyrazolforbindelser som serinproteaseinhibitorer |
WO2016202756A1 (en) | 2015-06-18 | 2016-12-22 | Bayer Pharma Aktiengesellschaft | Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds |
JOP20190192A1 (ar) * | 2017-03-01 | 2019-08-08 | Glaxosmithkline Ip No 2 Ltd | مشتقات بيرازول بوصفها مثبطات برومودومين |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
US5998424A (en) * | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
US6339099B1 (en) * | 1997-06-20 | 2002-01-15 | Dupont Pharmaceuticals Company | Guanidine mimics as factor Xa inhibitors |
EP1045846B1 (en) * | 1997-11-28 | 2003-05-02 | Lg Chemical Limited | Imidazole derivatives having an inhibitory activity for farnesyl transferase and process for preparation thereof |
JP2001526268A (ja) * | 1997-12-22 | 2001-12-18 | デュポン ファーマシューティカルズ カンパニー | Xa因子阻害剤としての、オルト−置換P1を有する、窒素含有複素環式芳香族化合物 |
CN100340559C (zh) * | 1998-12-23 | 2007-10-03 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为凝血因子xa抑制剂的含氮杂双环 |
BR0013200A (pt) * | 1999-07-16 | 2002-05-07 | Bristol Myers Squibb Pharma Co | Compostos derivados de heterobiciclos contendo nitrogênio, composições farmacêuticas, método de tratamento ou prevenção de uma disfunção tromboembólica e uso dos compostos |
US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
CN1390206A (zh) * | 1999-09-17 | 2003-01-08 | 千嬉药品公司 | 因子Xa的抑制剂 |
EP1226123A1 (en) * | 1999-11-03 | 2002-07-31 | Du Pont Pharmaceuticals Company | Cyano compounds as factor xa inhibitors |
WO2002000647A1 (en) * | 2000-06-23 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Heteroaryl-phenyl substituted factor xa inhibitors |
WO2002000651A2 (en) * | 2000-06-27 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Factor xa inhibitors |
WO2002085356A1 (en) * | 2001-04-18 | 2002-10-31 | Bristol-Myers Squibb Company | 1, 4, 5, 6-tetrahydropyrazolo-[3, 4-c]-pyrid in-7-ones as factor xa inhibitors |
-
2003
- 2003-12-10 EP EP03767776A patent/EP1581523B1/en not_active Expired - Lifetime
- 2003-12-10 BR BR0317659-2A patent/BR0317659A/pt not_active IP Right Cessation
- 2003-12-10 MX MXPA05006200A patent/MXPA05006200A/es unknown
- 2003-12-10 CA CA002511321A patent/CA2511321A1/en not_active Abandoned
- 2003-12-10 WO PCT/EP2003/013979 patent/WO2004056815A1/en active Application Filing
- 2003-12-10 JP JP2005502535A patent/JP4585448B2/ja not_active Expired - Fee Related
- 2003-12-10 DE DE60329529T patent/DE60329529D1/de not_active Expired - Lifetime
- 2003-12-10 AU AU2003292218A patent/AU2003292218A1/en not_active Abandoned
- 2003-12-10 AT AT03767776T patent/ATE444292T1/de not_active IP Right Cessation
- 2003-12-19 TW TW092136068A patent/TW200505914A/zh unknown
- 2003-12-22 AR ARP030104773A patent/AR042648A1/es unknown
-
2004
- 2004-01-05 PE PE2004000015A patent/PE20040925A1/es not_active Application Discontinuation
-
2005
- 2005-06-21 IL IL169323A patent/IL169323A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO2004056815A1 (en) | 2004-07-08 |
JP2006511608A (ja) | 2006-04-06 |
AU2003292218A1 (en) | 2004-07-14 |
MXPA05006200A (es) | 2005-08-19 |
IL169323A0 (en) | 2007-07-04 |
JP4585448B2 (ja) | 2010-11-24 |
ATE444292T1 (de) | 2009-10-15 |
AR042648A1 (es) | 2005-06-29 |
BR0317659A (pt) | 2005-12-06 |
DE60329529D1 (de) | 2009-11-12 |
TW200505914A (en) | 2005-02-16 |
EP1581523B1 (en) | 2009-09-30 |
EP1581523A1 (en) | 2005-10-05 |
CA2511321A1 (en) | 2004-07-08 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FD | Application declared void or lapsed |