[go: up one dir, main page]

PE20061153A1 - Compuestos heterociclicos como inhibidores del factor viia - Google Patents

Compuestos heterociclicos como inhibidores del factor viia

Info

Publication number
PE20061153A1
PE20061153A1 PE2005001422A PE2005001422A PE20061153A1 PE 20061153 A1 PE20061153 A1 PE 20061153A1 PE 2005001422 A PE2005001422 A PE 2005001422A PE 2005001422 A PE2005001422 A PE 2005001422A PE 20061153 A1 PE20061153 A1 PE 20061153A1
Authority
PE
Peru
Prior art keywords
etoxy
benzamidine
fluoro
ring
trifluoroacetic acid
Prior art date
Application number
PE2005001422A
Other languages
English (en)
Inventor
Peter W Glunz
Xuhong Cheng
Nicholas Wurtz
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20061153A1 publication Critical patent/PE20061153A1/es

Links

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA (I), DONDE X ES UN COMPUESTO DE FORMULA (II) O (III), DONDE X1, X2, X3, X4, X5, X6, X7, X8 Y X9 SON CR6 O N CON LA CONDICION DE QUE X NO TENGA MAS DE 3 ATOMOS DE NITROGENO EN EL ANILLO; R6 ES H, F, OCF3, CN, ENTRE OTROS; R8 ES FENILO SUSTITUIDO CON 0 A 5 R8b O HETEROARILO DE 5 A 6 MIEMBROS QUE COMPRENDE 1 A 4 HETEROATOMOS SELECCIONADOS DE N, O Y S, SUSTITUIDO CON 0 A 5 R8b, DONDE R8b ES H, F, CN, NO2, OCF3, ENTRE OTROS; R8a ES H O ALQUILO C1-C4; EL ANILLO Z ES UN HETEROARILO DE 5 A 6 MIEMBROS QUE INCLUYE EL ATOMO DE N QUE SE MUESTRA EN EL ANILLO QUE TIENE ATOMOS DE CARBONO Y 0 A 3 HETEROATOMOS ADICIONALES SELECCIONADOS DE N, O, S, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: SAL DEL ACIDO BIS-TRIFLUOROACETICO DE 4-((1H-BENZO[d]IMIDAZOL-2-IL)(5-ETOXI-2-FLUORO-3-ISOPROPOXIFENIL)METILAMINO)BENZAMIDINA, SAL DEL ACIDO TRIFLUOROACETICO DE 4-((5-ETOXI-2-FLUORO-3-ISOPROPOXIFENIL)(1H-TETRAZOL-5-IL)METILAMINO)BENZAMIDINA, SAL DEL ACIDO BIS-TRIFLUOROACETICO DE 4-((5-ETOXI-2-FLUORO-3-ISOPROPOXIFENIL)(1-METIL-4-FENIL-1H-IMIDAZOL-2-IL)METILAMINO)BENZAMIDINA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DE LAS ENZIMAS SERINA PROTEASA DE LA CASCADA DE COAGULACION, PARTICULARMENTE, DEL FACTOR VIIa Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS TROMBOEMBOLICOS TALES COMO ANGINA INESTABLE, SINDROME CORONARIO AGUDO, FIBRILACION ATRIAL, INFARTO DE MIOCARDIO, ENTRE OTROS
PE2005001422A 2004-12-08 2005-12-09 Compuestos heterociclicos como inhibidores del factor viia PE20061153A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US63429004P 2004-12-08 2004-12-08
US73292605P 2005-11-02 2005-11-02

Publications (1)

Publication Number Publication Date
PE20061153A1 true PE20061153A1 (es) 2006-10-27

Family

ID=36578487

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001422A PE20061153A1 (es) 2004-12-08 2005-12-09 Compuestos heterociclicos como inhibidores del factor viia

Country Status (9)

Country Link
US (1) US7576098B2 (es)
EP (1) EP1828152B1 (es)
AR (1) AR051984A1 (es)
AT (1) ATE405553T1 (es)
DE (1) DE602005009252D1 (es)
ES (1) ES2310861T3 (es)
PE (1) PE20061153A1 (es)
TW (1) TW200621229A (es)
WO (1) WO2006062972A2 (es)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006041119A1 (ja) * 2004-10-13 2006-04-20 Eisai R & D Management Co., Ltd. ヒドラジド誘導体
WO2006076246A2 (en) 2005-01-10 2006-07-20 Bristol-Myers Squibb Company Phenylglycinamide derivatives useful as anticoagulants
ATE455103T1 (de) * 2005-06-24 2010-01-15 Bristol Myers Squibb Co Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate
MX2008012031A (es) 2006-03-24 2008-10-02 Eisai R&D Man Co Ltd Derivado de triazolona.
US8222453B2 (en) 2006-06-08 2012-07-17 Bristol-Myers Squibb Company Benzamide factor VIIa inhibitors useful as anticoagulants
JP2010514672A (ja) 2006-12-29 2010-05-06 武田薬品工業株式会社 Ｃｒｆアンタゴニスト活性を有する縮合複素環化合物
WO2008136428A1 (ja) 2007-04-27 2008-11-13 Takeda Pharmaceutical Company Limited 含窒素５員複素環化合物
US8212047B2 (en) * 2007-09-20 2012-07-03 Exxonmobil Chemical Patents Inc. Methods for preparation of pyridylamines
JPWO2009038157A1 (ja) 2007-09-21 2011-01-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 ２，３−ジヒドロ−イミノイソインドール誘導体
CA2745121A1 (en) 2008-12-05 2010-06-10 Mochida Pharmaceutical Co., Ltd. Morpholinone compounds as factor ixa inhibitors
JP2010150200A (ja) * 2008-12-25 2010-07-08 Tosoh Corp イミダゾール化合物およびその製造方法
ES2547124T3 (es) 2009-04-02 2015-10-01 Merck Patent Gmbh Inhibidores de autotaxina
WO2015054087A1 (en) * 2013-10-07 2015-04-16 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US9944643B2 (en) 2014-02-11 2018-04-17 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
US10093683B2 (en) 2014-04-22 2018-10-09 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9695166B2 (en) 2014-05-05 2017-07-04 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
WO2016015593A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
CN104496926B (zh) * 2015-01-13 2016-06-01 佛山市赛维斯医药科技有限公司 一类含二烯四氮唑结构的化合物、其制备方法和用途
CA2995457A1 (en) 2015-08-13 2017-02-16 Dyax Corp. Evacuated blood collection tubes containing protease inhibitors for the assessment of contact system activation
EP3368036B1 (en) 2015-10-29 2022-07-20 Merck Sharp & Dohme LLC Macrocyclic pyridine-n-oxide derivatives as factor xia inhibitors
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
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
CN111557899B (zh) * 2020-04-30 2023-02-21 北华大学 一种治疗角膜炎的药物及其制备方法
CN114621096A (zh) * 2020-12-11 2022-06-14 余购粮 一种3,5-二甲基-1,2-苯二胺二盐酸盐的合成方法
CN114621101A (zh) * 2020-12-11 2022-06-14 李冰坚 一种3,5-二甲基-1,2-苯二胺二盐酸盐的精制方法

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5023236A (en) * 1988-04-07 1991-06-11 Corvas, Inc. Factor VII/VIIA active site inhibitors
US5843442A (en) * 1990-10-22 1998-12-01 Corvas International, Inc. Blood coagulation protein antagonists and uses therefor
US5866542A (en) * 1994-10-18 1999-02-02 Corvas International, Inc. Nematode-extracted anticoagulant protein
DE59808751D1 (de) * 1997-12-04 2003-07-24 Hoffmann La Roche N-(4-carbamimido-phenyl)-glycinamidderivate
US6271237B1 (en) * 1997-12-22 2001-08-07 Dupont Pharmaceuticals Company Nitrogen containing heteromatics with ortho-substituted P1s as factor Xa inhabitors
US6596747B2 (en) * 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
HK1043106A1 (zh) * 1998-12-14 2002-09-06 F. Hoffmann-La Roche Ag 苯基甘氨酸衍生物
US6632815B2 (en) * 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
PE20020384A1 (es) * 2000-07-21 2002-05-28 Schering Corp PEPTIDOS COMO INHIBIDORES DE LA PROTEASA SERINA NS3/NS4a DEL VIRUS DE LA HEPATITIS C
US6642252B2 (en) * 2000-11-07 2003-11-04 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
AU2002231235A1 (en) * 2000-11-07 2002-05-21 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
CA2435492A1 (en) 2001-02-02 2002-08-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Antithrombotic compounds, the preparation thereof and their use as pharmaceutical compositions
US20020151534A1 (en) * 2001-02-02 2002-10-17 Ries Uwe Joerg Antithrombotic compounds
BR0207216A (pt) 2001-02-14 2004-03-09 Warner Lambert Co Derivados de tieno 2,3-d-pirimidindiona como inibidores de metaloproteinase matriz
ATE280164T1 (de) 2001-02-14 2004-11-15 Warner Lambert Co Benzothiadiazine als matrix metallproteinase inhibitoren
DOP2002000334A (es) 2001-02-14 2002-08-30 Warner Lambert Co Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz
CN100343238C (zh) * 2001-11-03 2007-10-17 阿斯特拉曾尼卡有限公司 用作抗肿瘤药物的喹唑啉衍生物
GB0126433D0 (en) * 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
EP1314733A1 (en) * 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
WO2004000214A2 (en) 2002-06-19 2003-12-31 Bristol-Myers Squibb Company Use of compounds having an amine nucleus in manufacture of a medicament useful for treating factor viia-associated conditions
AU2003243657A1 (en) * 2002-06-26 2004-01-19 Bristol-Myers Squibb Company Amino-bicyclic pyrazinones and pyridinones
EP1539762A2 (en) * 2002-06-26 2005-06-15 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade inhibitors
EP1594505A4 (en) * 2003-02-11 2008-08-13 Bristol Myers Squibb Co PHENYLGLYCIN DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS
WO2004072102A2 (en) * 2003-02-11 2004-08-26 Bristol-Myers Squibb Company Benzene acetamide compounds useful as serine protease inhibitors
US7247654B2 (en) * 2003-06-04 2007-07-24 Bristol-Myers Squibb Company 3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors
WO2006076246A2 (en) * 2005-01-10 2006-07-20 Bristol-Myers Squibb Company Phenylglycinamide derivatives useful as anticoagulants
ATE455103T1 (de) * 2005-06-24 2010-01-15 Bristol Myers Squibb Co Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate

Also Published As

Publication number Publication date
DE602005009252D1 (de) 2008-10-02
ES2310861T3 (es) 2009-01-16
EP1828152A2 (en) 2007-09-05
EP1828152B1 (en) 2008-08-20
TW200621229A (en) 2006-07-01
WO2006062972A3 (en) 2006-08-24
ATE405553T1 (de) 2008-09-15
WO2006062972A2 (en) 2006-06-15
US7576098B2 (en) 2009-08-18
AR051984A1 (es) 2007-02-21
US20060211720A1 (en) 2006-09-21

Similar Documents

Publication Publication Date Title
PE20061153A1 (es) Compuestos heterociclicos como inhibidores del factor viia
NO20043098L (no) Alfa-(N-sulfonamido) acetamidderivater som beta-amyloidinhibitorer
NO20083684L (no) Laktam-inneholdende forbindelser og derivater derav som faktor XA-inhibitorer
NO20081467L (no) Inhibitorer av sennproteaser
DK1569901T3 (da) Aryl-, aryloxy- og alkoxysubstituerede 1H-indol-3-yl-glyoxylsyrederivater som inhibitorer af plasminogenaktivatorinhibitor-1 (PAI-1)
PE20011314A1 (es) DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA
NO20070201L (no) Seksleddede heterocykler anvendelige som serinproteaseinhibitorer
HUP0401740A2 (hu) N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
NO20053460L (no) Nye forbindelser med selektiv inhibiterende effekt ved GSK3
JO2282B1 (en) Oxazole derivatives
JO2646B1 (en) New differentiated cyclic compounds as beta - lactam inhibitors
NO20066055L (no) Pyridinderivater
NO20044731L (no) Kinolin- og isokinolinderivater fremgangsmate for fremstilling derav og anvendelse derav som betennelseshemmere
NO20052311L (no) Mandelsyrederivater.
DE502004005033D1 (de) Substituierte 2-aminotetraline zur behandlung von depressionen
NO20056010L (no) Biaryloksymetylaren-karboksylsyrer
NO20082629L (no) Macrocyklisk factor VIIa-inhibitorer anvendbare som antikoagulanter
DK1569900T3 (da) Substituerede 3-carbonyl-1-yl-eddikesyrederivater som inhibitorer af plasminogenaktivator-inhibitor-1 (PAI-1)
SV2003001099A (es) Nuevos derivados de acido sulfonico ref.pc23084
NO20062021L (no) Omleirede pentanoler, fremgangsmpte for fremstilling av dette, og deres anvendelse som antiflogistika
NO20052487L (no) 1-(4-benzyl-piperazin-1-yl)-3-fenyl-propenonderivater.
NO20050612L (no) Pyrrolidinderivater som oksytocinantagonister
DE60316436D1 (de) Amidderivate als inhibitoren der enzymatischen aktivität von renin
NO20060383L (no) Substituerte diketopiperaziner og deres anvendelse som oksytocinantagonister
ATE284882T1 (de) Chromenylmethylpyrimidindiamine als antibakterielle wirkstoffe

Legal Events

Date Code Title Description
FC Refusal