PE20030661A1 - N-[4-(1H-IMIDAZOL-1IL)-2-FLUOROFENIL]-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa - Google Patents
N-[4-(1H-IMIDAZOL-1IL)-2-FLUOROFENIL]-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR XaInfo
- Publication number
- PE20030661A1 PE20030661A1 PE2002001167A PE2002001167A PE20030661A1 PE 20030661 A1 PE20030661 A1 PE 20030661A1 PE 2002001167 A PE2002001167 A PE 2002001167A PE 2002001167 A PE2002001167 A PE 2002001167A PE 20030661 A1 PE20030661 A1 PE 20030661A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- imidazol
- fluorophenyl
- trifluoromethyl
- carboxamides
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 title 1
- -1 1H-IMIDAZOL-1YL Chemical class 0.000 abstract 4
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 abstract 3
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- AQIAIZBHFAKICS-UHFFFAOYSA-N methylaminomethyl Chemical compound [CH2]NC AQIAIZBHFAKICS-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
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
- 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
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A N-[4-(1H-IMIDAZOL-1IL)-2-FLUOROFENIL]-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDAS DE FORMULA I DONDE R ES H, ALQUILO; R1 ES H, ALQUENILENO-CO-ALQUILO, CO-ALQUILO, CO-ALQUILO-NRaRa; Ra ES H, ALQUILO, CO(CH2)2CH(NRaRa)COORa, ENTRE OTROS; R2 ES Cl, F, Br, I, OH, ALQUILO, ALCOXI, ALQUILENO-OCO-ALQUILO; R3 ES ALQUILO, FENILO. SON COMPUESTOS PREFERIDOS N-[4-(2-[DIMETILAMINOMETIL]-1H-IMIDAZOL-1-IL)-2-FLUOROFENIL]-1-(3-AMIDINO-4-HIDROXIFENIL)-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDA; SAL DEL BIS(ACIDO TRIFLUOROACETICO) DE N-{4-(2-[METILAMINO]METIL}-1H-IMIDAZOL-1-IL)-2-FLUOROFENIL]-1-(3-AMINO-1,2-BENCISOXAZOL-5-IL)-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDA; SAL DE BIS(ACIDO TRIFLUOROACETICO) DE N-[4-(2-[METILAMINOMETIL]-1H-IMIDAZOL-1-IL)-2-FLUOROFENIL]-1-(3-AMIDINO-4-HIDROXIFENIL)-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDA, ENTRE OTROS. LOS COMPUESTOS SON INHIBIDORES DEL FACTOR Xa Y PUEDEN SER UTILES COMO ANTICOAGULANTES Y PARA EL TRATAMIENTO DE TRASTORNOS TROMBOEMBOLICOS CARDIOVASCULARES, ARTERIALES, VENOSOS O EN LAS CAVIDADES DEL CORAZON
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33697201P | 2001-12-04 | 2001-12-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030661A1 true PE20030661A1 (es) | 2003-08-08 |
Family
ID=23318529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002001167A PE20030661A1 (es) | 2001-12-04 | 2002-12-04 | N-[4-(1H-IMIDAZOL-1IL)-2-FLUOROFENIL]-3-(TRIFLUOROMETIL)-1H-PIRAZOL-5-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6730689B2 (es) |
| EP (1) | EP1460996A4 (es) |
| JP (1) | JP2005527485A (es) |
| AR (1) | AR037698A1 (es) |
| AU (1) | AU2002352962A1 (es) |
| HU (1) | HUP0402515A2 (es) |
| PE (1) | PE20030661A1 (es) |
| PL (1) | PL373907A1 (es) |
| TW (1) | TW200303309A (es) |
| WO (1) | WO2003047517A2 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6339099B1 (en) * | 1997-06-20 | 2002-01-15 | Dupont Pharmaceuticals Company | Guanidine mimics as factor Xa inhibitors |
| GB0128996D0 (en) | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
| US20030220383A1 (en) * | 2002-02-14 | 2003-11-27 | Aventis Pharma Deutschland Gmbh | Use of inhibitors of the sodium-dependent chloride/bicarbonate exchanger for the treatment of thrombotic and inflammatory disorders |
| WO2004031143A2 (en) * | 2002-10-02 | 2004-04-15 | Bristol-Myers Squibb Company | Novel combination of a factor xa inhibitor and clopidogrel |
| US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
| PL1750862T3 (pl) | 2004-06-04 | 2011-06-30 | Teva Pharma | Kompozycja farmaceutyczna zawierająca irbesartan |
| WO2006034270A2 (en) * | 2004-09-20 | 2006-03-30 | Therapyzone, Inc. | Exercise handle and methods of use |
| EP2196461A1 (de) | 2008-12-15 | 2010-06-16 | Bayer CropScience AG | 4-Amino-1,2,3-benzoxathiazin-Derivate als Pestizide |
| WO2012027331A1 (en) | 2010-08-27 | 2012-03-01 | Ironwood Pharmaceuticals, Inc. | Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders |
| CA2941380C (en) | 2014-03-07 | 2022-09-06 | Biocryst Pharmaceuticals, Inc. | Human plasma kallikrein inhibitors |
| WO2017168174A1 (en) | 2016-04-02 | 2017-10-05 | N4 Pharma Uk Limited | New pharmaceutical forms of sildenafil |
| WO2018002673A1 (en) | 2016-07-01 | 2018-01-04 | N4 Pharma Uk Limited | Novel formulations of angiotensin ii receptor antagonists |
| EP3661500A1 (en) | 2017-07-31 | 2020-06-10 | Novartis AG | Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5342851A (en) | 1992-10-07 | 1994-08-30 | Mcneil-Ppc, Inc. | Substituted thiazole derivatives useful as platelet aggregation inhibitors |
| US5925635A (en) * | 1996-04-17 | 1999-07-20 | Dupont Pharmaceuticals Company | N-(amidinophenyl) cyclourea analogs as factor XA inhibitors |
| DE69739593D1 (de) | 1996-12-23 | 2009-11-05 | Bristol Myers Squibb Pharma Co | Stickstoffhaltige heterocyclen als faktor xa-hemmer |
| US6020357A (en) | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| ZA985247B (en) * | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| US6339099B1 (en) * | 1997-06-20 | 2002-01-15 | Dupont Pharmaceuticals Company | Guanidine mimics as factor Xa inhibitors |
| US6271237B1 (en) | 1997-12-22 | 2001-08-07 | Dupont Pharmaceuticals Company | Nitrogen containing heteromatics with ortho-substituted P1s as factor Xa inhabitors |
| TW200302225A (en) * | 2001-12-04 | 2003-08-01 | Bristol Myers Squibb Co | Substituted amino methyl factor Xa inhibitors |
-
2002
- 2002-11-20 TW TW091133819A patent/TW200303309A/zh unknown
- 2002-11-22 US US10/302,184 patent/US6730689B2/en not_active Expired - Lifetime
- 2002-11-26 PL PL02373907A patent/PL373907A1/xx not_active Application Discontinuation
- 2002-11-26 JP JP2003548778A patent/JP2005527485A/ja not_active Withdrawn
- 2002-11-26 WO PCT/US2002/038168 patent/WO2003047517A2/en not_active Ceased
- 2002-11-26 EP EP02789922A patent/EP1460996A4/en not_active Withdrawn
- 2002-11-26 AU AU2002352962A patent/AU2002352962A1/en not_active Abandoned
- 2002-11-26 HU HU0402515A patent/HUP0402515A2/hu unknown
- 2002-12-04 AR ARP020104702A patent/AR037698A1/es not_active Application Discontinuation
- 2002-12-04 PE PE2002001167A patent/PE20030661A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1460996A4 (en) | 2005-11-16 |
| WO2003047517A3 (en) | 2004-02-26 |
| TW200303309A (en) | 2003-09-01 |
| WO2003047517A2 (en) | 2003-06-12 |
| AU2002352962A1 (en) | 2003-06-17 |
| AU2002352962A8 (en) | 2003-06-17 |
| AR037698A1 (es) | 2004-12-01 |
| JP2005527485A (ja) | 2005-09-15 |
| US6730689B2 (en) | 2004-05-04 |
| HUP0402515A2 (hu) | 2005-03-29 |
| EP1460996A2 (en) | 2004-09-29 |
| US20030144287A1 (en) | 2003-07-31 |
| PL373907A1 (en) | 2005-09-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |