BR0317659A - Derivados de pirazol como inibidores de fator xa - Google Patents
Derivados de pirazol como inibidores de fator xaInfo
- Publication number
- BR0317659A BR0317659A BR0317659-2A BR0317659A BR0317659A BR 0317659 A BR0317659 A BR 0317659A BR 0317659 A BR0317659 A BR 0317659A BR 0317659 A BR0317659 A BR 0317659A
- Authority
- BR
- Brazil
- Prior art keywords
- factor
- compounds
- formula
- inhibitors
- vila
- Prior art date
Links
Classifications
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- 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
Abstract
"DERIVADOS DE PIRAZOL COMO INIBIDORES DE FATOR XA". A presente invenção refere-se a compostos da fórmula I, em que R¬ 0¬; R¬ 1¬; R¬ 2¬; R¬ 3¬; R¬ 4¬; Q; V, G e M tem os significados indicados nas reivindicações. Os compostos da fórmula I são compostos farmacologicamente ativos valiosos. Eles demonstram um forte efeito antibrombótico e são apropriados, por exemplo, para a terapia e profilaxia de distúrbios cardiovasculares como doenças tromboembolíticas ou restenoses. Eles são inibidores reversíveis das enzimas de coagulação do sangue fator Xa (FXa) e/ou fator VIIa (FVIIa), e podem geralmente ser aplicados em condições em que uma atividade indesejada de fator Xa e/ou fator Vila está presente ou para a cura ou prevenção da qual uma inibição de fator Xa e/ou fator Vila é pretendida. A invenção além disso refere-se a processos para a preparação de compostos da fórmula I, seu uso, particularmente como ingredientes ativos em fármacos, e preparações farmacêuticas compreendendo os mesmos.
Applications Claiming Priority (3)
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 |
PCT/EP2003/013979 WO2004056815A1 (en) | 2002-12-23 | 2003-12-10 | PYRAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS |
Publications (1)
Publication Number | Publication Date |
---|---|
BR0317659A true BR0317659A (pt) | 2005-12-06 |
Family
ID=32683809
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR0317659-2A BR0317659A (pt) | 2002-12-23 | 2003-12-10 | Derivados de pirazol como inibidores de fator xa |
Country Status (13)
Country | Link |
---|---|
EP (1) | EP1581523B1 (pt) |
JP (1) | JP4585448B2 (pt) |
AR (1) | AR042648A1 (pt) |
AT (1) | ATE444292T1 (pt) |
AU (1) | AU2003292218A1 (pt) |
BR (1) | BR0317659A (pt) |
CA (1) | CA2511321A1 (pt) |
DE (1) | DE60329529D1 (pt) |
IL (1) | IL169323A0 (pt) |
MX (1) | MXPA05006200A (pt) |
PE (1) | PE20040925A1 (pt) |
TW (1) | TW200505914A (pt) |
WO (1) | WO2004056815A1 (pt) |
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 |
US7446210B2 (en) | 2004-10-26 | 2008-11-04 | 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 |
EP1814860B1 (en) * | 2004-10-29 | 2009-06-03 | Schering Corporation | Substituted 5-carboxyamide pyrazoles and [1,2,4]triazoles as antiviral agents |
EP2395000A1 (en) | 2004-12-30 | 2011-12-14 | Astex Therapeutics Limited | Benzimidazole 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 |
CA2613522A1 (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 |
WO2009080226A2 (en) * | 2007-12-26 | 2009-07-02 | Sanofis-Aventis | Heterocyclic pyrazole-carboxamides as p2y12 antagonists |
JP5560202B2 (ja) * | 2007-12-26 | 2014-07-23 | サノフイ | P2y12拮抗薬としてのピラゾール−カルボキサミド誘導体 |
JP5432890B2 (ja) | 2008-04-04 | 2014-03-05 | 武田薬品工業株式会社 | 複素環誘導体及びその用途 |
ES2552549T3 (es) * | 2008-04-23 | 2015-11-30 | Rigel Pharmaceuticals, Inc. | Compuestos de carboxamida para el tratamiento de trastornos metabólicos |
UY33200A (es) | 2010-01-26 | 2011-08-31 | Sanofi Aventis | Derivados de ácido 3-heteroaroilamino-propiónico sustituidos con oxígeno y su uso como productos farmacéuticos |
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 |
UY33874A (es) | 2011-01-26 | 2012-08-31 | Sanofi Aventis | Derivados de ácido 3-heteroaroilamino-propiónico sustituidos y su uso como sustancias farmacéuticas |
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 |
PT2736888E (pt) | 2011-07-26 | 2016-02-17 | Sanofi Sa | Derivados do ácido 3-heteroaroilamino-propiónico e o seu uso como produtos farmacêuticos |
WO2013014205A1 (en) | 2011-07-26 | 2013-01-31 | Sanofi | Substituted 3 - (thiazole - 4 - carbonyl) - or 3 - (thiazole - 2 - carbonyl) aminopropionic acid derivatives and their use as pharmaceuticals |
WO2013072327A1 (en) | 2011-11-14 | 2013-05-23 | Sanofi | Use of boceprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases |
US20130123276A1 (en) | 2011-11-14 | 2013-05-16 | Sven Ruf | Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases |
CN110423221A (zh) | 2013-03-15 | 2019-11-08 | 维颂公司 | 作为凝血酶抑制剂的卤代吡唑 |
MX2015012867A (es) | 2013-03-15 | 2016-06-10 | Verseon Corp | Compuestos aromaticos multisustituidos como inhibidores de serina proteasa. |
WO2014154727A1 (en) | 2013-03-28 | 2014-10-02 | Sanofi | Biaryl-propionic acid derivatives and their use as pharmaceuticals |
CA2907903A1 (en) | 2013-03-28 | 2014-10-02 | 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 |
CN107405333A (zh) | 2015-02-27 | 2017-11-28 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物 |
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 |
PT1140941E (pt) * | 1998-12-23 | 2005-02-28 | Bristol Myers Squibb Pharma Co | Heterociclicos que contem azoto como inibidores do factor xa |
CN1454211A (zh) * | 1999-07-16 | 2003-11-05 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为Xa因子抑制剂的含氮杂双环化合物 |
MX228790B (es) * | 1999-09-17 | 2005-06-30 | Millennium Pharm Inc | Inhibidores del factor xa. |
US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
WO2001032628A1 (en) * | 1999-11-03 | 2001-05-10 | Bristol-Myers Squibb Pharma Company | Cyano compounds as factor xa inhibitors |
US6599926B2 (en) * | 2000-06-23 | 2003-07-29 | Bristol-Myers Squibb 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 CA CA002511321A patent/CA2511321A1/en not_active Abandoned
- 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 EP EP03767776A patent/EP1581523B1/en not_active Expired - Lifetime
- 2003-12-10 DE DE60329529T patent/DE60329529D1/de not_active Expired - Lifetime
- 2003-12-10 AT AT03767776T patent/ATE444292T1/de not_active IP Right Cessation
- 2003-12-10 WO PCT/EP2003/013979 patent/WO2004056815A1/en active Application Filing
- 2003-12-10 AU AU2003292218A patent/AU2003292218A1/en not_active Abandoned
- 2003-12-10 JP JP2005502535A patent/JP4585448B2/ja not_active Expired - Fee Related
- 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 |
---|---|
AU2003292218A1 (en) | 2004-07-14 |
ATE444292T1 (de) | 2009-10-15 |
WO2004056815A1 (en) | 2004-07-08 |
JP4585448B2 (ja) | 2010-11-24 |
TW200505914A (en) | 2005-02-16 |
EP1581523B1 (en) | 2009-09-30 |
PE20040925A1 (es) | 2004-12-24 |
EP1581523A1 (en) | 2005-10-05 |
AR042648A1 (es) | 2005-06-29 |
MXPA05006200A (es) | 2005-08-19 |
DE60329529D1 (de) | 2009-11-12 |
JP2006511608A (ja) | 2006-04-06 |
CA2511321A1 (en) | 2004-07-08 |
IL169323A0 (en) | 2007-07-04 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 7A E 8A ANUIDADES. |
|
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2160 DE 29/05/2012. |