PE20061117A1 - DERIVADOS DE FENILGLICINAMIDA COMO INHIBIDORES DEL FACTOR VIIa - Google Patents
DERIVADOS DE FENILGLICINAMIDA COMO INHIBIDORES DEL FACTOR VIIaInfo
- Publication number
- PE20061117A1 PE20061117A1 PE2006000049A PE2006000049A PE20061117A1 PE 20061117 A1 PE20061117 A1 PE 20061117A1 PE 2006000049 A PE2006000049 A PE 2006000049A PE 2006000049 A PE2006000049 A PE 2006000049A PE 20061117 A1 PE20061117 A1 PE 20061117A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- inhibitors
- factor viia
- preferred
- phenylglycinamide
- Prior art date
Links
- 229940012414 factor viia Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- KIYRSYYOVDHSPG-UHFFFAOYSA-N 2-amino-2-phenylacetamide Chemical class NC(=O)C(N)C1=CC=CC=C1 KIYRSYYOVDHSPG-UHFFFAOYSA-N 0.000 title 1
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical class OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- LSBDFXRDZJMBSC-UHFFFAOYSA-N 2-phenylacetamide Chemical group NC(=O)CC1=CC=CC=C1 LSBDFXRDZJMBSC-UHFFFAOYSA-N 0.000 abstract 2
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 abstract 1
- 230000015271 coagulation Effects 0.000 abstract 1
- 238000005345 coagulation Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (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 UN COMPUESTO DE FORMULA I DONDE Y ES A, B, ENTRE OTROS; R1 ES H, F, Cl, ALQUILO C1-C5, ENTRE OTROS; R2 Y R3 SON CADA UNO H, F, Cl, OCF3, CN, ENTRE OTROS; R4 ES H, F, CN, NO2, ALQUILO C1-C6, ENTRE OTROS; W ES NH, O; Z ES DE PREFERENCIA 1-ISOQUINOLIN; A ES UN HETEROCICLO DE 4-8 MIEMBROS, DE PREFERENCIA N-PIRROLIDIN; R8 ES H, CN, TETRAZOLILO, ALQUILO C1-C4 SUSTITUIDO; R9 ES FENILACETAMIDA, 2-ISOPROPILTIOFENIL, 3-NITROFENIL, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: SAL ACIDO TRIFLUOROACETICO DE 2-(1-AMINOSIOQUINOLIN-6-ILAMINO)-2-(3-ETOXI-4-ISOPROPOXIFENIL)-1-(2-FENILPIRROLIDIN-1-IL)ETANONA; SAL ACIDO TRIFLUOROACETICO DE N-(3-((S)-1-((R)-2-(1-AMINOISOQUINOLIN-6-ILAMINO)-2-(3-ETOXI-4-ISOPROPOXIFENIL)ACETIL)PIRROLIDIN-2-IL)FENIL)ACETAMIDA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE LA SERINA PROTEASA DE LA CASCADA DE COAGULACION, EN PARTICULAR DEL FACTOR VIIa UTILES EN EL TRATAMIENTO DE TRASTORNOS TROMBOEMBOLICOS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64275105P | 2005-01-10 | 2005-01-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20061117A1 true PE20061117A1 (es) | 2006-10-13 |
Family
ID=36587246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000049A PE20061117A1 (es) | 2005-01-10 | 2006-01-09 | DERIVADOS DE FENILGLICINAMIDA COMO INHIBIDORES DEL FACTOR VIIa |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7622585B2 (es) |
| EP (1) | EP1856096B1 (es) |
| AR (1) | AR054321A1 (es) |
| AT (1) | ATE479676T1 (es) |
| DE (1) | DE602006016566D1 (es) |
| ES (1) | ES2349428T3 (es) |
| PE (1) | PE20061117A1 (es) |
| TW (1) | TW200637843A (es) |
| WO (1) | WO2006076246A2 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006062972A2 (en) * | 2004-12-08 | 2006-06-15 | Bristol-Myers Squibb Company | Heterocyclic compounds as inhibitors of factor viia |
| WO2007002313A2 (en) * | 2005-06-24 | 2007-01-04 | Bristol-Myers Squibb Company | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants |
| PE20071132A1 (es) * | 2005-12-23 | 2007-12-14 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| US20070161670A1 (en) * | 2006-01-09 | 2007-07-12 | Bristol-Myers Squibb Company | Process for the preparation of substituted heterocycles |
| EP2061756B1 (en) | 2006-06-08 | 2013-09-25 | Bristol-Myers Squibb Company | 2-aminocarbonylphenylamino-2-phenilacetamides as factor viia inhibitors useful as anticoagulants |
| JP2010513562A (ja) * | 2006-12-20 | 2010-04-30 | ブリストル−マイヤーズ スクイブ カンパニー | 抗凝血剤として有用な二環状ラクタム第ｖｉｉａ因子阻害剤 |
| PE20081775A1 (es) * | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| WO2009046448A1 (en) * | 2007-10-04 | 2009-04-09 | Intellikine, Inc. | Chemical entities and therapeutic uses thereof |
| WO2009114874A2 (en) * | 2008-03-14 | 2009-09-17 | Intellikine, Inc. | Benzothiazole kinase inhibitors and methods of use |
| WO2009114870A2 (en) | 2008-03-14 | 2009-09-17 | Intellikine, Inc. | Kinase inhibitors and methods of use |
| JP5788316B2 (ja) | 2008-07-08 | 2015-09-30 | インテリカイン， エルエルシー | キナーゼインヒビターおよび使用方法 |
| EP2149565A1 (de) | 2008-07-24 | 2010-02-03 | Bayer Schering Pharma AG | Sulfonsubstituierte Chinazolinderivate als Immunmodulatoren zur Behandlung von enzündlichen und allergischen Erkrankungen |
| JP5417860B2 (ja) * | 2008-08-26 | 2014-02-19 | 住友化学株式会社 | α−ヒドロキシエステル類の製造方法 |
| US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
| PT2624696T (pt) | 2010-10-06 | 2017-03-21 | Glaxosmithkline Llc | Derivados de benzimidazole como inibidores da cinase pi3 |
| TWI592411B (zh) | 2011-02-23 | 2017-07-21 | 英特爾立秦有限責任公司 | 激酶抑制劑之組合及其用途 |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| EP3180317B1 (en) | 2014-07-28 | 2021-04-14 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| MA43128A (fr) | 2015-10-29 | 2018-09-05 | Merck Sharp & Dohme | Inhibiteurs du facteur xia |
| EP3371162B1 (en) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| WO2017158147A1 (en) | 2016-03-18 | 2017-09-21 | Savira Pharmaceuticals Gmbh | Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease |
| US10143681B2 (en) | 2016-08-22 | 2018-12-04 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| CN112225647A (zh) * | 2020-10-14 | 2021-01-15 | 河南中医药大学 | 一种合成5-溴-2-甲氧基苯酚的方法 |
| CN117466714A (zh) * | 2023-10-30 | 2024-01-30 | 中国科学技术大学 | 一种2,4-二氯-5-卤代苯酚的制备方法 |
| CN118344240A (zh) * | 2024-04-16 | 2024-07-16 | 中国科学技术大学 | 一种2,4-二氯-5-溴苯酚的制备方法 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023236A (en) | 1988-04-07 | 1991-06-11 | Corvas, Inc. | Factor VII/VIIA active site inhibitors |
| FR2667864B2 (fr) | 1990-03-07 | 1994-08-05 | Rhone Poulenc Sante | Derives de n-phenyl glycinamides, leur preparation et les medicaments les contenant. |
| US5843442A (en) | 1990-10-22 | 1998-12-01 | Corvas International, Inc. | Blood coagulation protein antagonists and uses therefor |
| US5563127A (en) | 1993-03-24 | 1996-10-08 | The Dupont Merck Pharmaceutical Company | Boronic acid and ester inhibitors of thrombin |
| US5602101A (en) * | 1994-03-04 | 1997-02-11 | Eli Lilly And Company | Antithrombotic agents |
| US5866542A (en) | 1994-10-18 | 1999-02-02 | Corvas International, Inc. | Nematode-extracted anticoagulant protein |
| WO1997010214A1 (en) | 1995-09-14 | 1997-03-20 | Shionogi & Co., Ltd. | Novel phenylacetic acid derivatives and medicinal composition containing the same |
| IL123986A (en) | 1997-04-24 | 2011-10-31 | Organon Nv | Medicinal compounds |
| PT921116E (pt) | 1997-12-04 | 2003-11-28 | Hoffmann La Roche | Derivados de n-(4-carbamimido-fenil)-glicinamida |
| EP1078917A4 (en) | 1998-02-17 | 2002-11-06 | Ono Pharmaceutical Co | AMIDINO DERIVATIVES FOR USE AS ACTIVE INGREDIENTS AND MEDICINES CONTAINING THEM |
| US6335324B1 (en) | 1998-06-25 | 2002-01-01 | Bristol-Myers Squibb Co. | Beta lactam compounds and their use as inhibitors of tryptase |
| ATE274491T1 (de) | 1998-12-14 | 2004-09-15 | Hoffmann La Roche | Phenylglycin-derivate |
| CN100488947C (zh) | 1999-01-13 | 2009-05-20 | 杰南技术公司 | 丝氨酸蛋白酶抑制剂 |
| CA2394639A1 (en) | 1999-12-15 | 2001-06-21 | Danny Peter Claude Mcgee | Salicylamides as serine protease and factor xa inhibitors |
| KR20020067702A (ko) | 2000-01-26 | 2002-08-23 | 오노 야꾸힝 고교 가부시키가이샤 | 질소 함유 5원환 화합물 및 이러한 화합물을 유효성분으로서 함유하는 약제 |
| US6548694B2 (en) | 2000-05-23 | 2003-04-15 | Hoffman-La Roche Inc. | N-(4-carbamimidoyl-phenyl)-glycine derivatives |
| DE10027025A1 (de) * | 2000-05-31 | 2001-12-06 | Merck Patent Gmbh | Clycinamide |
| JP2004505038A (ja) | 2000-08-02 | 2004-02-19 | スミスクライン・ビーチャム・コーポレイション | 脂肪酸シンターゼ阻害剤 |
| NZ526003A (en) | 2000-10-20 | 2005-09-30 | Biocryst Pharm Inc | Biaryl compounds as serine protease inhibitors |
| US6642252B2 (en) | 2000-11-07 | 2003-11-04 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| ES2332090T3 (es) | 2001-04-06 | 2010-01-26 | Biocryst Pharmaceuticals, Inc. | Compuestos biarilicos como inhibidores de serina proteasa. |
| DE10139060A1 (de) | 2001-08-08 | 2003-02-20 | Merck Patent Gmbh | Phenylderivate |
| US6642386B2 (en) | 2002-02-06 | 2003-11-04 | Hoffmann-La Roche Inc. | N-(4-carbamimidoyl-phenyl)-glycine derivatives |
| DE10214832A1 (de) | 2002-04-04 | 2003-10-16 | Merck Patent Gmbh | Phenylderivate 4 |
| WO2004072101A2 (en) | 2003-02-11 | 2004-08-26 | Bristol-Myers Squibb Company | Phenylglycine derivatives useful as serine protease inhibitors |
| EP1594845A4 (en) | 2003-02-11 | 2008-05-21 | Bristol Myers Squibb Co | BENZENE ACETAMIDE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS |
| DE10310278A1 (de) * | 2003-03-10 | 2004-09-23 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue aromatische Bicyclen, deren Herstellung und deren Verwendung als Arzneimittel |
| US20050107409A1 (en) | 2003-03-10 | 2005-05-19 | Boehringer Ingelheim International Gmbh | Aromatic bicyclic compounds, preparation thereof and their use as pharmaceutical compositions |
| US7309708B2 (en) | 2003-11-20 | 2007-12-18 | Birstol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2006062972A2 (en) | 2004-12-08 | 2006-06-15 | Bristol-Myers Squibb Company | Heterocyclic compounds as inhibitors of factor viia |
| WO2007002313A2 (en) | 2005-06-24 | 2007-01-04 | Bristol-Myers Squibb Company | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants |
-
2006
- 2006-01-09 WO PCT/US2006/000571 patent/WO2006076246A2/en not_active Ceased
- 2006-01-09 DE DE602006016566T patent/DE602006016566D1/de active Active
- 2006-01-09 AT AT06717735T patent/ATE479676T1/de not_active IP Right Cessation
- 2006-01-09 US US11/328,479 patent/US7622585B2/en active Active
- 2006-01-09 AR ARP060100077A patent/AR054321A1/es unknown
- 2006-01-09 ES ES06717735T patent/ES2349428T3/es active Active
- 2006-01-09 PE PE2006000049A patent/PE20061117A1/es not_active Application Discontinuation
- 2006-01-09 TW TW095100708A patent/TW200637843A/zh unknown
- 2006-01-09 EP EP06717735A patent/EP1856096B1/en not_active Not-in-force
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006076246A2 (en) | 2006-07-20 |
| ATE479676T1 (de) | 2010-09-15 |
| AR054321A1 (es) | 2007-06-20 |
| DE602006016566D1 (de) | 2010-10-14 |
| ES2349428T3 (es) | 2011-01-03 |
| US7622585B2 (en) | 2009-11-24 |
| EP1856096B1 (en) | 2010-09-01 |
| TW200637843A (en) | 2006-11-01 |
| WO2006076246A3 (en) | 2006-09-28 |
| EP1856096A2 (en) | 2007-11-21 |
| US20060166997A1 (en) | 2006-07-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |