JP5225098B2 - 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ - Google Patents

第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ Download PDF

Info

Publication number
JP5225098B2
JP5225098B2 JP2008545955A JP2008545955A JP5225098B2 JP 5225098 B2 JP5225098 B2 JP 5225098B2 JP 2008545955 A JP2008545955 A JP 2008545955A JP 2008545955 A JP2008545955 A JP 2008545955A JP 5225098 B2 JP5225098 B2 JP 5225098B2
Authority
JP
Japan
Prior art keywords
chloro
phenyl
imidazol
ethyl
benzyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2008545955A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009519967A5 (OSRAM
JP2009519967A (ja
Inventor
ドナルド・ジェイ・ピー・ピント
ジョアン・エム・スモールヒーア
ジェイムズ・アール・コート
フ・チルン
カレン・エル・カバラロ
ポール・ジェイ・ギリガン
ミミ・エル・クワン
レオン・エム・スミス・ザ・セカンド
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
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 JP2009519967A publication Critical patent/JP2009519967A/ja
Publication of JP2009519967A5 publication Critical patent/JP2009519967A5/ja
Application granted granted Critical
Publication of JP5225098B2 publication Critical patent/JP5225098B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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
    • C07D233/66—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 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
    • C07D233/68—Halogen atoms
    • 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
    • C07D401/02—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
    • 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
    • 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
    • C07D403/14—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 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
    • C07D405/14—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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2008545955A 2005-12-14 2006-12-13 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ Expired - Fee Related JP5225098B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US75013005P 2005-12-14 2005-12-14
US60/750,130 2005-12-14
US82116306P 2006-08-02 2006-08-02
US60/821,163 2006-08-02
US86521106P 2006-11-10 2006-11-10
US60/865,211 2006-11-10
PCT/US2006/062005 WO2007070826A1 (en) 2005-12-14 2006-12-13 Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors

Publications (3)

Publication Number Publication Date
JP2009519967A JP2009519967A (ja) 2009-05-21
JP2009519967A5 JP2009519967A5 (OSRAM) 2009-12-03
JP5225098B2 true JP5225098B2 (ja) 2013-07-03

Family

ID=37944011

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008545955A Expired - Fee Related JP5225098B2 (ja) 2005-12-14 2006-12-13 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ

Country Status (16)

Country Link
US (4) US7626039B2 (OSRAM)
EP (1) EP1981854B1 (OSRAM)
JP (1) JP5225098B2 (OSRAM)
KR (1) KR20080087817A (OSRAM)
AR (1) AR058379A1 (OSRAM)
AT (1) ATE511502T1 (OSRAM)
AU (1) AU2006325754B2 (OSRAM)
BR (1) BRPI0620010A2 (OSRAM)
CA (1) CA2633252A1 (OSRAM)
EA (1) EA014245B1 (OSRAM)
IL (1) IL192033A0 (OSRAM)
NO (1) NO20082444L (OSRAM)
NZ (1) NZ568595A (OSRAM)
PE (1) PE20070811A1 (OSRAM)
TW (1) TW200730477A (OSRAM)
WO (1) WO2007070826A1 (OSRAM)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
EP1841504B1 (en) * 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors
WO2007070816A2 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Thiophene derivatives as factor xia inhibitors
JP2009519966A (ja) * 2005-12-14 2009-05-21 ブリストル−マイヤーズ スクイブ カンパニー セリンプロテアーゼ阻害剤として有用な６員ヘテロ環
ES2546815T3 (es) * 2006-12-15 2015-09-28 Bristol-Myers Squibb Company Análogos de arilpropilamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor XIa
PE20091002A1 (es) * 2007-06-13 2009-07-15 Bristol Myers Squibb Co Analogos dipeptidos como inhibidores del factor de coagulacion
WO2009114677A1 (en) * 2008-03-13 2009-09-17 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
US8513415B2 (en) * 2009-04-20 2013-08-20 OSI Pharmaceuticals, LLC Preparation of C-pyrazine-methylamines
WO2011037192A1 (ja) * 2009-09-25 2011-03-31 アステラス製薬株式会社 置換アミド化合物
WO2011100401A1 (en) 2010-02-11 2011-08-18 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
LV14606B (lv) 2011-05-17 2013-01-20 Tetra, Sia Jauns XII faktora inhibitors
US9540343B2 (en) * 2011-07-06 2017-01-10 Gilead Sciences, Inc. Compounds for the treatment of HIV
TW201319068A (zh) 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
CN103987697B (zh) 2011-10-14 2017-04-26 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
PH12014500625B1 (en) 2011-10-14 2018-12-12 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
CN103987696B (zh) 2011-10-14 2016-12-21 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
IN2014CN04676A (OSRAM) * 2011-12-21 2015-09-18 Ono Pharmaceutical Co
GB2497806A (en) * 2011-12-21 2013-06-26 Ono Pharmaceutical Co Pyridinone and pyrimidinone derivatives as factor XIa inhibitors
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
GB201209138D0 (en) * 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds
GB201212081D0 (en) * 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
HRP20161378T1 (hr) 2012-08-03 2016-12-02 Bristol-Myers Squibb Company Dihidropiridon kao faktor xia inhibitora
HUE032622T2 (en) 2012-08-03 2017-10-30 Bristol Myers Squibb Co Dihydropyridone p1 as factor xia inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
MX351848B (es) 2012-10-12 2017-10-31 Bristol Myers Squibb Co Formas cristalinas de inhibidor del factor xia.
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
GB201300304D0 (en) * 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
CA2905242C (en) 2013-03-15 2016-11-29 Pfizer Inc. Indole compounds that activate ampk
WO2014160668A1 (en) 2013-03-25 2014-10-02 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
EA201300843A1 (ru) * 2013-08-01 2015-04-30 Арсений Валерьевич Айбушев Карбамоилфенильные производные для остановки, предотвращения и профилактики кровотечений или усиления системы гемостаза
GB2517908A (en) * 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
WO2015054087A1 (en) * 2013-10-07 2015-04-16 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (OSRAM) 2014-01-31 2018-03-10
WO2015123093A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Factor xia inhibitors
US9676723B2 (en) * 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
CN106456604B (zh) * 2014-02-25 2020-11-06 艾其林医药公司 用于治疗补体介导疾病的芳基、杂芳基和杂环化合物
EP3131897B8 (en) 2014-04-16 2022-08-03 Merck Sharp & Dohme LLC Factor ixa inhibitors
US10093683B2 (en) 2014-04-22 2018-10-09 Merck Sharp & Dohme Corp. Factor XIa inhibitors
TW201607923A (zh) 2014-07-15 2016-03-01 歌林達有限公司 被取代之氮螺環（４．５）癸烷衍生物
CN106660954A (zh) 2014-07-15 2017-05-10 格吕伦塔尔有限公司 取代氮杂螺(4.5)癸烷衍生物
US9868727B2 (en) 2014-07-28 2018-01-16 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9988443B2 (en) 2014-08-07 2018-06-05 Novartis Ag Angiopoetin-like 4 (ANGPTL4) antibodies and methods of use
DK3177642T3 (da) 2014-08-07 2022-02-21 Novartis Ag Angiopoietin-lignende 4-antistoffer og fremgangsmåder til anvendelse deraf
WO2016036893A1 (en) 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
WO2016094260A1 (en) * 2014-12-10 2016-06-16 Merck Sharp & Dohme Corp. Factor ixa inhibitors
DK3231803T3 (da) 2014-12-10 2020-08-24 Ono Pharmaceutical Co Dihydroindolizinonderivat
EP3662751B1 (en) * 2015-05-26 2021-10-13 Kaohsiung Medical University Pyrazolo[4,3-c]quinoline derivatives for inhibition of b-glucuronidase
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
JOP20200312A1 (ar) 2015-06-26 2017-06-16 Novartis Ag الأجسام المضادة للعامل xi وطرق الاستخدام
KR102729666B1 (ko) 2015-07-29 2024-11-12 브리스톨-마이어스 스큅 컴퍼니 비-방향족 P2' 기를 갖는 인자 XIa 신규 마크로사이클
CN107849026B (zh) 2015-07-29 2021-01-01 百时美施贵宝公司 携带烷基或环烷基p2′部分的因子xia大环抑制剂
US10214512B2 (en) 2015-10-29 2019-02-26 Merck Sharp & Dohme Corp. 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
US10472344B2 (en) 2015-12-02 2019-11-12 Merck Sharp & Dohme Corp. Factor XIa inhibitors
WO2017123518A1 (en) * 2016-01-11 2017-07-20 The Rockefeller University Aminotriazole immunomodulators for treating autoimmune diseases
TW201802121A (zh) 2016-05-25 2018-01-16 諾華公司 抗因子XI/XIa抗體之逆轉結合劑及其用途
BR112018071678B1 (pt) 2016-08-19 2021-01-26 Gilead Sciences, Inc. compostos terapêuticos úteis para o tratamento profilático ou terapêutico de uma infecção por vírus hiv e suas composições farmacêuticas
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
BR112019012667A2 (pt) 2016-12-23 2020-02-11 Novartis Ag Anticorpos do fator xi e métodos de uso
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
TWI687415B (zh) 2017-08-17 2020-03-11 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
PL3752495T3 (pl) 2018-02-15 2024-01-15 Gilead Sciences, Inc. Pochodne pirydynowe i ich zastosowanie do leczenia infekcji hiv
TWI823164B (zh) 2018-02-16 2023-11-21 美商基利科學股份有限公司 用於製備有療效化合物之方法及中間物
CA3216031A1 (en) 2018-07-16 2020-01-23 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
TWI854067B (zh) 2019-11-26 2024-09-01 美商基利科學股份有限公司 預防hiv之蛋白殼抑制劑
TW202502766A (zh) 2020-06-25 2025-01-16 美商基利科學股份有限公司 用於治療hiv之蛋白殼抑制劑
WO2022109161A1 (en) * 2020-11-19 2022-05-27 Merck Sharp & Dohme Corp. Plasma kallikrein inhibitors
EP4440701A1 (en) 2021-12-03 2024-10-09 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
TW202342448A (zh) 2021-12-03 2023-11-01 美商基利科學股份有限公司 用於ｈｉｖ病毒感染之治療性化合物
EP4440702B1 (en) 2021-12-03 2025-05-21 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998027108A2 (en) 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. New amide compounds and their use as nitric oxide synthase inhibitors
US6593291B1 (en) 1997-02-06 2003-07-15 Entremed, Inc. Compositions and methods of use of ligands that bind components of the blood coagulation/clotting pathway for the treatment of cancer and angiogenic-based disease
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
WO1999064401A2 (en) 1998-06-12 1999-12-16 Societe De Conseils De Recherches Et D'applications Scientifiques Sas Imidazolyl derivatives and their use as somatostatin receptor ligands
HUP0102902A3 (en) * 1998-06-16 2002-02-28 Sod Conseils Rech Applic Cyclic somatostatin analogs, process for production thereof and their use
AUPQ142599A0 (en) * 1999-07-05 1999-07-29 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
US20040132788A1 (en) * 1999-10-11 2004-07-08 Chabrier De Lassauniere Pierre-Etienne Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
NZ523774A (en) 2000-08-01 2004-09-24 Sod Conseils Rech Applic Imidazolyl derivatives
BR0307266A (pt) 2002-01-31 2004-12-07 Morphochem Ag Komb Chemie Compostos que inibem a atividade do fator xa
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
US20040180855A1 (en) 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7371743B2 (en) * 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
RS54199B1 (sr) 2004-03-15 2015-12-31 Janssen Pharmaceutica Nv Postupak za dobijanje intermedijera jedinjenja korisnih kao modulatori opioidnih receptora
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
BRPI0511504A (pt) * 2004-05-26 2008-01-22 Eisai R&D Man Co Ltd composto ou um sal farmaceuticamente aceitável do mesmo, e, agente preventivo ou terapêutico para uma doença resultante de beta-amilóides
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
WO2006061638A2 (en) 2004-12-10 2006-06-15 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Heterocycle derivatives as histone deacetylase (hdac) inhibitors
EP1841504B1 (en) 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors
WO2007070816A2 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Thiophene derivatives as factor xia inhibitors
JP2009519966A (ja) 2005-12-14 2009-05-21 ブリストル−マイヤーズ スクイブ カンパニー セリンプロテアーゼ阻害剤として有用な６員ヘテロ環

Also Published As

Publication number Publication date
NO20082444L (no) 2008-09-12
KR20080087817A (ko) 2008-10-01
US7842708B2 (en) 2010-11-30
WO2007070826A1 (en) 2007-06-21
EP1981854B1 (en) 2011-06-01
AR058379A1 (es) 2008-01-30
BRPI0620010A2 (pt) 2011-11-22
EA200801530A1 (ru) 2008-12-30
AU2006325754A1 (en) 2007-06-21
IL192033A0 (en) 2008-12-29
JP2009519967A (ja) 2009-05-21
US20110028446A1 (en) 2011-02-03
US8252830B2 (en) 2012-08-28
US8604056B2 (en) 2013-12-10
ATE511502T1 (de) 2011-06-15
US20100022506A1 (en) 2010-01-28
US20080161373A1 (en) 2008-07-03
US7626039B2 (en) 2009-12-01
AU2006325754B2 (en) 2012-04-12
EP1981854A1 (en) 2008-10-22
NZ568595A (en) 2010-04-30
EA014245B1 (ru) 2010-10-29
TW200730477A (en) 2007-08-16
PE20070811A1 (es) 2007-08-13
US20120270853A1 (en) 2012-10-25
WO2007070826B1 (en) 2007-08-16
CA2633252A1 (en) 2007-06-21

Similar Documents

Publication Publication Date Title
JP5225098B2 (ja) 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ
JP5318094B2 (ja) 凝固因子阻害剤としてのジペプチド類似体
CN101010299B (zh) 用作丝氨酸蛋白酶抑制剂的6元杂环
JP5342450B2 (ja) 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ
US8466295B2 (en) Thiophene derivatives as factor XIa inhibitors
US8163749B2 (en) Six-membered heterocycles useful as serine protease inhibitors
CN108137549A (zh) 新颖的取代的甘氨酸衍生的fxia抑制剂
TW201410667A (zh) 二氫吡啶酮ｐ１作爲凝血因子ｘｉａ抑制劑
CN101341129B (zh) 作为因子xia抑制剂的芳基丙酰胺，芳基丙烯酰胺，芳基丙炔酰胺，或芳基甲基脲类似物
EP3191486B1 (en) Thioether triazolopyridine and triazolopyrmidine inhibitors of myeloperoxidase
EP3191485A1 (en) Triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase
MX2008007313A (en) Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
MX2008007296A (en) Six-membered heterocycles useful as serine protease inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20091014

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20091014

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120522

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20120522

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120822

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20121016

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130110

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20130212

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20130312

R150 Certificate of patent or registration of utility model

Ref document number: 5225098

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20160322

Year of fee payment: 3

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees