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

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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
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chloro
phenyl
imidazol
ethyl
benzyl
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JP2009519967A5 (https=
JP2009519967A (ja
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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
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Bristol Myers Squibb Co
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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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

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JP2009519967A JP2009519967A (ja) 2009-05-21
JP2009519967A5 JP2009519967A5 (https=) 2009-12-03
JP5225098B2 true JP5225098B2 (ja) 2013-07-03

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

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
EP1966141A1 (en) * 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
WO2007070816A2 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Thiophene derivatives as factor xia inhibitors
EP2102189B1 (en) * 2006-12-15 2015-07-29 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
CN101784516B (zh) * 2007-06-13 2014-07-02 百时美施贵宝公司 作为凝血因子抑制剂的二肽类似物
US8324199B2 (en) 2008-03-13 2012-12-04 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
KR101678255B1 (ko) * 2009-09-25 2016-11-21 아스텔라스세이야쿠 가부시키가이샤 치환 아미드 화합물
NZ602266A (en) 2010-02-11 2014-05-30 Bristol Myers Squibb Co Macrocycles as factor xia inhibitors
LV14606B (lv) 2011-05-17 2013-01-20 Tetra, Sia Jauns XII faktora inhibitors
AU2012278976B2 (en) * 2011-07-06 2017-05-11 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
WO2013055984A1 (en) 2011-10-14 2013-04-18 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP6033319B2 (ja) 2011-10-14 2016-11-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第XIa因子阻害剤としての置換テトラヒドロイソキノリン化合物
GB2497806A (en) * 2011-12-21 2013-06-26 Ono Pharmaceutical Co Pyridinone and pyrimidinone derivatives as factor XIa inhibitors
US9732085B2 (en) 2011-12-21 2017-08-15 Ono Pharmaceutical Co., Ltd. Pyridinone and pyrimidinone derivatives as factor Xia
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
US9376444B2 (en) 2012-08-03 2016-06-28 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
AU2013296259A1 (en) 2012-08-03 2015-03-19 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
TR201807316T4 (tr) 2012-10-12 2018-06-21 Bristol Myers Squibb Co Bir faktör XIa inhibitörünün kristalli formları.
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906552B1 (en) 2012-10-12 2017-11-22 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
EP2970177A1 (en) 2013-03-15 2016-01-20 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 (https=) 2014-01-31 2018-03-10
WO2015123093A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Factor xia inhibitors
WO2015123091A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Factor xia inhibitors
US9732103B2 (en) * 2014-02-25 2017-08-15 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of complement mediated disorders
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
EP3134408B1 (en) 2014-04-22 2020-08-12 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
HUE040133T2 (hu) 2014-07-15 2019-02-28 Gruenenthal Gmbh Szubsztituált azaspiro(4.5)dekán származékok
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
WO2016015593A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2016020880A2 (en) 2014-08-07 2016-02-11 Novartis Ag Angiopoietin-like 4 antibodies and methods of use
WO2016020882A2 (en) 2014-08-07 2016-02-11 Novartis Ag Angiopoetin-like 4 (angptl4) antibodies and methods of use
ES2714283T3 (es) 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
EP3229801B1 (en) 2014-12-10 2020-04-01 Merck Sharp & Dohme Corp. Factor ixa inhibitors
BR112017012146B1 (pt) 2014-12-10 2023-11-21 Ono Pharmaceutical Co., Ltd Composto derivado de di-hidroindolizinona, seu uso, composição farmacêutica e inibidor de fxia
EP3662751B1 (en) * 2015-05-26 2021-10-13 Kaohsiung Medical University Pyrazolo[4,3-c]quinoline derivatives for inhibition of b-glucuronidase
ES2762987T3 (es) 2015-06-19 2020-05-26 Bristol Myers Squibb Co Macrociclos de diamida como inhibidores del factor XIA
UY36751A (es) 2015-06-26 2017-01-31 Novartis Ag Anticuerpos de factor xi y métodos de uso
JP6629958B2 (ja) 2015-07-29 2020-01-15 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company アルキルまたはシクロアルキルP2’基を担持する大員環の第XIa因子阻害剤
CN114874222B (zh) 2015-07-29 2025-06-06 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
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
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
CN119462611A (zh) 2016-08-19 2025-02-18 吉利德科学公司 用于预防性或治疗性治疗hiv病毒感染的治疗性化合物
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
AU2017383232B2 (en) 2016-12-23 2024-09-12 Novartis Ag Factor XI antibodies and methods of use
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
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
JP7083398B2 (ja) 2018-02-15 2022-06-10 ギリアード サイエンシーズ, インコーポレイテッド ピリジン誘導体およびhiv感染を処置するためのその使用
EP3752496B1 (en) 2018-02-16 2023-07-05 Gilead Sciences, Inc. Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection
KR20210033492A (ko) 2018-07-16 2021-03-26 길리애드 사이언시즈, 인코포레이티드 Hiv의 치료를 위한 캡시드 억제제
CA3157275C (en) 2019-11-26 2026-02-10 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
TWI858267B (zh) 2020-06-25 2024-10-11 美商基利科學股份有限公司 用於治療hiv之蛋白殼抑制劑
KR20230110544A (ko) * 2020-11-19 2023-07-24 머크 샤프 앤드 돔 엘엘씨 혈장 칼리크레인 억제제
US12404262B2 (en) 2021-12-03 2025-09-02 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
CR20240223A (es) 2021-12-03 2024-07-08 Gilead Sciences Inc Compuestos terapéuticos para la infección por el virus del vih

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0946587A2 (en) 1996-12-16 1999-10-06 Fujisawa Pharmaceutical Co., Ltd. New amide compounds
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.
DK1086086T3 (da) * 1998-06-12 2005-01-24 Sod Conseils Rech Applic Imidazolylderivater og anvendelse deraf som somatostatinreceptorligander
PL345037A1 (en) 1998-06-16 2001-11-19 Sod Conseils Rech Applic Cyclic somatostatin analogs
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
ATE360620T1 (de) * 2000-08-01 2007-05-15 Sod Conseils Rech Applic Imidazolderivate
KR20040096541A (ko) * 2002-01-31 2004-11-16 모르포켐 악티엥게셀샤프트 퓌르 콤비나토리셰 케미 인자 Xa 활성을 저해하는 화합물
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
AU2005224091B2 (en) 2004-03-15 2012-02-02 Janssen Pharmaceutica, N.V. Novel compounds as opioid receptor modulators
US7417063B2 (en) * 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
RU2361872C2 (ru) * 2004-05-26 2009-07-20 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Циннамидное соединение
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP1828171B1 (en) 2004-12-10 2014-03-12 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. 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
EP1966141A1 (en) * 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors

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