AR063977A1 - Enantiomero [r] puro de 5-{[2-fluoro-4-(2-oxo-2h-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido [r]-5-metil-4, 5-dihidro-pirazol-1, 5-dicarboxilico, un metodo para la preparacion del mencionado compuesto, una composicion farmaceutica que lo comprende, formas cristalinas del mismo y - Google Patents
Enantiomero [r] puro de 5-{[2-fluoro-4-(2-oxo-2h-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido [r]-5-metil-4, 5-dihidro-pirazol-1, 5-dicarboxilico, un metodo para la preparacion del mencionado compuesto, una composicion farmaceutica que lo comprende, formas cristalinas del mismo yInfo
- Publication number
- AR063977A1 AR063977A1 ARP070105244A ARP070105244A AR063977A1 AR 063977 A1 AR063977 A1 AR 063977A1 AR P070105244 A ARP070105244 A AR P070105244A AR P070105244 A ARP070105244 A AR P070105244A AR 063977 A1 AR063977 A1 AR 063977A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- amide
- phenyl
- formula
- acid
- Prior art date
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
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- 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
- A61P9/06—Antiarrhythmics
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- 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
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- 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
- A61P9/12—Antihypertensives
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Composiciones farmacéuticas de 5-{[2-Fluoro-4-(2-oxo-2H-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido (R)-5-metil-4,5-dihidro-pirazol-1,5-dicarboxílico, procedimientos y uso del compuesto o de las composiciones farmacéuticas del mismo para tratar enfermedades caracterizadas por trombosis anomala en mamíferos. Forma cristalina de 5-{[2-fluoro-4-(2-oxo-2H-piridin-1-iI)-fenil]-amida} 1-[(4-cloro-fenil)-amida} del ácido (R)-5-metil-4,5-dihidro- pirazol-1,5-dicarboxílico, se provee además un método para la preparacion del mismo. Reivindicacion 1: El compuesto 5-{[2-Fluoro-4-(2-oxo-2H-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido (R)-5-metil-4,5-dihidro-pirazol-1,5-dicarboxílico, en el que el enantiomero (R) es sustancialmente puro. Reivindicacion 20: Un procedimiento para preparar 5-{[2-fluoro-4-(2-oxo-2H-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido (R)-5-metil-4,5-dihidro-pirazol-1,5-dicarboxílico que comprende: Etapa (a) (1) hacer reaccionar el compuesto de formula (11) con cloruro de metacriloílo en presencia de un disolvente y una base; o (2) hacer reaccionar un compuesto de formula (11)con cloruro de litio, trietilamina y anhídrido 2-metilacrílico; para dar un compuesto de formula (12); Etapa (b) hacer reaccionar el compuesto de formula (12) con trimetilsilil diazometano, tratamiento con un ácido diluido y aislamiento para producir un compuesto de formula (13); Etapa (c) tratamiento del compuesto de formula (13) con un isocianato y una base suave en un disolvente para dar un compuesto de formula (14); Etapa (d) retirada del auxiliar quiral para dar un compuesto de formula (15) y Etapa (e) acoplamiento del compuesto de formula (15) con un compuesto de formula (3) para producir el compuesto deseado.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US86771406P | 2006-11-29 | 2006-11-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR063977A1 true AR063977A1 (es) | 2009-03-04 |
Family
ID=39032289
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070105244A AR063977A1 (es) | 2006-11-29 | 2007-11-27 | Enantiomero [r] puro de 5-{[2-fluoro-4-(2-oxo-2h-piridin-1-il)-fenil]-amida} 1-[(4-cloro-fenil)-amida] del ácido [r]-5-metil-4, 5-dihidro-pirazol-1, 5-dicarboxilico, un metodo para la preparacion del mencionado compuesto, una composicion farmaceutica que lo comprende, formas cristalinas del mismo y |
Country Status (11)
Country | Link |
---|---|
US (1) | US20080171773A1 (es) |
EP (1) | EP2086962A1 (es) |
JP (1) | JP2010511034A (es) |
AR (1) | AR063977A1 (es) |
CA (1) | CA2670595A1 (es) |
CL (1) | CL2007003349A1 (es) |
GT (1) | GT200700105A (es) |
PE (1) | PE20081498A1 (es) |
TW (1) | TW200831090A (es) |
UY (1) | UY30745A1 (es) |
WO (1) | WO2008065503A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2138178A1 (en) * | 2008-06-28 | 2009-12-30 | Bayer Schering Pharma Aktiengesellschaft | Oxazolidninones for the treatment fo chronic obstructive pulmonary disease (COPD) and/or asthma |
JP5605029B2 (ja) * | 2010-07-06 | 2014-10-15 | 住友化学株式会社 | 化合物、樹脂及びレジスト組成物 |
CN104610259B (zh) * | 2015-02-14 | 2016-06-01 | 佛山市赛维斯医药科技有限公司 | 含酰胺和氮杂环结构的FXa抑制剂、制备方法及其用途 |
CN104860942B (zh) * | 2015-02-14 | 2016-08-24 | 佛山市赛维斯医药科技有限公司 | 一种含双酰胺基和硝基苯基结构的FXa抑制剂及其用途 |
CN104725374B (zh) * | 2015-02-14 | 2016-08-24 | 佛山市赛维斯医药科技有限公司 | 一种含双酰胺基和腈基苯结构的FXa抑制剂及其用途 |
CN104610257B (zh) * | 2015-02-14 | 2016-06-01 | 佛山市赛维斯医药科技有限公司 | 一类含酰胺结构的FXa抑制剂、制备方法及其用途 |
EP3078378B1 (en) | 2015-04-08 | 2020-06-24 | Vaiomer | Use of factor xa inhibitors for regulating glycemia |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4559157A (en) * | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
LU84979A1 (fr) * | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
US4820508A (en) * | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
US4992478A (en) * | 1988-04-04 | 1991-02-12 | Warner-Lambert Company | Antiinflammatory skin moisturizing composition and method of preparing same |
US4938949A (en) * | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
DE4326465A1 (de) * | 1993-01-20 | 1995-02-09 | Thomae Gmbh Dr K | Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
US7030141B2 (en) * | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
-
2007
- 2007-11-16 WO PCT/IB2007/003609 patent/WO2008065503A1/en active Application Filing
- 2007-11-16 EP EP07825722A patent/EP2086962A1/en not_active Withdrawn
- 2007-11-16 CA CA002670595A patent/CA2670595A1/en not_active Abandoned
- 2007-11-16 JP JP2009538802A patent/JP2010511034A/ja not_active Withdrawn
- 2007-11-23 PE PE2007001636A patent/PE20081498A1/es not_active Application Discontinuation
- 2007-11-23 CL CL200703349A patent/CL2007003349A1/es unknown
- 2007-11-27 AR ARP070105244A patent/AR063977A1/es not_active Application Discontinuation
- 2007-11-27 UY UY30745A patent/UY30745A1/es not_active Application Discontinuation
- 2007-11-28 GT GT200700105A patent/GT200700105A/es unknown
- 2007-11-28 TW TW096145206A patent/TW200831090A/zh unknown
- 2007-11-29 US US11/947,713 patent/US20080171773A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US20080171773A1 (en) | 2008-07-17 |
UY30745A1 (es) | 2008-07-03 |
GT200700105A (es) | 2008-11-04 |
JP2010511034A (ja) | 2010-04-08 |
CA2670595A1 (en) | 2008-06-05 |
WO2008065503A1 (en) | 2008-06-05 |
EP2086962A1 (en) | 2009-08-12 |
CL2007003349A1 (es) | 2008-06-06 |
PE20081498A1 (es) | 2008-11-08 |
TW200831090A (en) | 2008-08-01 |
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