JP4791460B2 - セリンプロテアーゼ阻害剤として有用な5員複素環 - Google Patents

セリンプロテアーゼ阻害剤として有用な5員複素環 Download PDF

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JP4791460B2
JP4791460B2 JP2007516703A JP2007516703A JP4791460B2 JP 4791460 B2 JP4791460 B2 JP 4791460B2 JP 2007516703 A JP2007516703 A JP 2007516703A JP 2007516703 A JP2007516703 A JP 2007516703A JP 4791460 B2 JP4791460 B2 JP 4791460B2
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phenyl
substituted
imidazol
benzyl
alkyl
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Japanese (ja)
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JP2008502700A (ja
JP2008502700A5 (enExample
Inventor
ジョン・ジェイ・ハンジェランド
ミミ・エル・クワン
ジョアン・エム・スモールヒアー
グレゴリー・エス・ビサッチ
ジェイムズ・アール・コート
トッド・ジェイ・フレンズ
ゾン・サン
カレン・エイ・ロッシ
カレン・エル・カバラロ
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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Families Citing this family (99)

* 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
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US8143425B2 (en) * 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
CN101137412B (zh) * 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物
US20060183771A1 (en) * 2005-02-17 2006-08-17 Seiffert Dietmar A Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors
WO2007007588A1 (ja) * 2005-07-08 2007-01-18 Ono Pharmaceutical Co., Ltd. 平面性を有する環状基を母核とする化合物
US20070135499A1 (en) * 2005-07-11 2007-06-14 Aerie Pharmaceuticals, Inc. Hydrazide compounds
ES2580108T3 (es) * 2005-07-11 2016-08-19 Aerie Pharmaceuticals, Inc Compuestos de isoquinolina
JP5225098B2 (ja) 2005-12-14 2013-07-03 ブリストル−マイヤーズ スクイブ カンパニー 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
AU2006325746A1 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US8466295B2 (en) * 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
WO2007076161A2 (en) * 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
PL2051975T3 (pl) * 2006-05-16 2013-01-31 Boehringer Ingelheim Int Podstawione prolinamidy, ich wytwarzanie oraz ich zastosowanie jako środków leczniczych
EP2526948A1 (en) 2006-09-20 2012-11-28 Aerie Pharmaceuticals, Inc. RHO kinase inhibitors
ES2546815T3 (es) * 2006-12-15 2015-09-28 Bristol-Myers Squibb Company Análogos de arilpropilamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor XIa
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
AR066379A1 (es) * 2007-05-02 2009-08-12 Boehringer Ingelheim Int Amidas de acido carboxilico su preparacion y su uso como medicamentos
WO2008154441A1 (en) * 2007-06-07 2008-12-18 Joyant Pharmaceuticals, Inc. Methods for preparing diazonamides
KR20100037600A (ko) * 2007-06-13 2010-04-09 브리스톨-마이어스 스큅 컴퍼니 응고 인자 억제제로서의 디펩티드 유사체
US8193177B2 (en) * 2007-11-13 2012-06-05 Angion Biomedica Corp. Hepatocyte growth factor pathway activators in fibrotic connective tissue diseases
US8455514B2 (en) * 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
CN102026996B (zh) * 2008-03-13 2015-01-07 百时美施贵宝公司 作为凝血因子xia抑制剂的哒嗪衍生物
WO2009115572A2 (en) * 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
WO2010044441A1 (ja) * 2008-10-17 2010-04-22 塩野義製薬株式会社 血管内皮リパーゼ阻害活性を有する酢酸アミド誘導体
WO2010126626A2 (en) 2009-05-01 2010-11-04 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US8609866B2 (en) * 2009-12-18 2013-12-17 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US9206123B2 (en) 2009-12-18 2015-12-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
JP5844287B2 (ja) 2010-02-11 2016-01-13 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マクロ環
WO2012022487A1 (de) * 2010-08-20 2012-02-23 Grünenthal GmbH Substituierte cyclische carboxamid- und harnstoff-derivate als liganden des vanilloid-rezeptors
CN103221410B (zh) * 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
US8685966B2 (en) 2011-04-08 2014-04-01 University Of Kansas GRP94 inhibitors
EP2697196A1 (en) 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
CA2840095A1 (en) 2011-07-06 2013-01-10 Gilead Sciences, Inc. Compounds for the treatment of hiv
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
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
LT2766346T (lt) 2011-10-14 2017-06-12 Bristol-Myers Squibb Company Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai
IN2014CN02806A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
IN2014CN02805A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
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
CA2880898A1 (en) 2012-08-03 2014-02-06 Bristol-Myers Squibb Company Dihydropyridone p1 as factor xia inhibitors
KR20150038372A (ko) 2012-08-03 2015-04-08 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제제로서의 디히드로피리돈 P1
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
HRP20180465T1 (hr) 2012-10-12 2018-05-04 Bristol-Myers Squibb Company Kristalni oblici inhibitora faktora xia
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9220710B2 (en) 2013-01-09 2015-12-29 Gilead Sciences, Inc. Therapeutic compounds
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
ES2776199T3 (es) 2013-03-15 2020-07-29 Aerie Pharmaceuticals Inc Conjugados de compuestos de isoquinolina y prostaglandinas
JP6479763B2 (ja) 2013-03-25 2019-03-06 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アゾール含有のテトラヒドロイソキノリン
AR097279A1 (es) 2013-08-09 2016-03-02 Actelion Pharmaceuticals Ltd Derivados de benzimidazolil-metil urea como agonistas del receptor de alx
NO2760821T3 (enExample) 2014-01-31 2018-03-10
JP6505727B2 (ja) 2014-01-31 2019-04-24 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ヘテロ環式p2’基を有する第xia因子阻害剤としてのマクロ環
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
WO2015130964A1 (en) 2014-02-28 2015-09-03 Gilead Sciences, Inc. Therapeutic compounds
WO2015164308A1 (en) 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2015171527A1 (en) * 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
US9868727B2 (en) 2014-07-28 2018-01-16 Merck Sharp & Dohme Corp. Factor XIa inhibitors
JP6526796B2 (ja) 2014-09-04 2019-06-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Fxia阻害剤であるジアミドマクロ環
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10189819B2 (en) 2014-12-10 2019-01-29 Merck Sharp & Dohme, Corp. Factor IXa inhibitors
WO2016115282A1 (en) * 2015-01-13 2016-07-21 Vanderbilt University Benzoisoxazole-substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2016123629A1 (en) 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
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
ES2871111T3 (es) 2015-07-29 2021-10-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático
WO2017074833A1 (en) 2015-10-29 2017-05-04 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
BR112018008506B8 (pt) 2015-10-29 2023-12-05 Merck Sharp & Dohme Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos
WO2017086941A1 (en) 2015-11-17 2017-05-26 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
LT3347352T (lt) 2016-08-19 2019-08-12 Gilead Sciences, Inc. Terapiniai junginiai, naudotini živ viruso infekcijos profilaktikai arba terapiniam gydymui
US10143681B2 (en) 2016-08-22 2018-12-04 Merck Sharp & Dohme Corp. Factor XIa inhibitors
WO2018045091A1 (en) 2016-08-31 2018-03-08 Aerie Pharmaceuticals, Inc. Ophthalmic compositions
CN113912586B (zh) * 2016-08-31 2023-04-07 江苏恒瑞医药股份有限公司 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用
CN109715163B (zh) 2016-09-19 2022-11-22 诺华股份有限公司 包含raf抑制剂和erk抑制剂的治疗组合
CA3057872A1 (en) 2017-03-31 2018-10-04 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
WO2018203219A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
TW202024061A (zh) 2017-08-17 2020-07-01 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
WO2019161017A1 (en) 2018-02-15 2019-08-22 Gilead Sciences, Inc. Pyridine derivatives and their use for treating hiv infection
KR102847339B1 (ko) 2018-02-16 2025-08-19 길리애드 사이언시즈, 인코포레이티드 레트로비리다에 바이러스 감염의 치료에 유용한 치료 화합물을 제조하기 위한 방법 및 중간체
US11299462B2 (en) * 2018-02-27 2022-04-12 Jiangsu Hengrui Medicine Co., Ltd. Crystal form of oxopicolinamide derivative and preparation method therefor
DK3774796T3 (da) * 2018-04-10 2022-07-18 Bayer Pharma AG Et substitueret oxopyridinderivat
CA3103522C (en) 2018-07-16 2023-11-21 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
AU2019337703B2 (en) 2018-09-14 2023-02-02 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
EP4563150A3 (en) 2019-05-13 2025-07-23 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
CA3157275C (en) 2019-11-26 2026-02-10 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
CN113683598B (zh) * 2020-05-18 2022-10-14 成都先导药物开发股份有限公司 一种免疫调节剂
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
AU2022399845B2 (en) 2021-12-03 2026-03-26 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
FI4440702T3 (fi) 2021-12-03 2025-08-08 Gilead Sciences Inc Terapeuttisia yhdisteitä hiv-virusinfektiota varten
AU2022403012B2 (en) 2021-12-03 2026-02-12 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
JP7733916B2 (ja) * 2022-02-28 2025-09-04 学校法人東海大学 Clec-2および/またはgpviの拮抗剤
CN117143081B (zh) * 2022-05-24 2025-08-01 赣南医科大学 一种Sabizabulin的制备方法
CN116891472A (zh) * 2023-07-13 2023-10-17 延边大学 一种含咪唑结构的酰胺类衍生物及其制备方法和应用
WO2025122845A1 (en) * 2023-12-07 2025-06-12 Genep Inc. Imidazole compounds and their use as sodium channel inhibitors

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000511173A (ja) * 1996-05-27 2000-08-29 藤沢薬品工業株式会社 一酸化窒素産生阻害剤としての新規なインドリルおよびベンゾフラニルカルボキサミド
JP2001505585A (ja) * 1996-12-16 2001-04-24 藤沢薬品工業株式会社 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途
WO2002010140A2 (en) * 2000-08-01 2002-02-07 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Imidazolyl derivatives
JP2003523921A (ja) * 1998-06-12 2003-08-12 ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス イミダゾリル誘導体
WO2004011445A1 (ja) * 2002-07-31 2004-02-05 Nippon Soda Co.,Ltd. アミノサリチル酸アミド誘導体、製造法及び農園芸用殺菌剤
WO2004017908A2 (en) * 2002-08-26 2004-03-04 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
JP2004323516A (ja) * 2003-04-11 2004-11-18 Nippon Soda Co Ltd 3−アシルアミノサリチル酸アミド誘導体、製造法及び農園芸用殺菌剤

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3255202A (en) * 1963-08-23 1966-06-07 Union Carbide Corp Process for the preparation of 2-(acylamidoalkyl)benzimidazoles
US5618792A (en) 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
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
US6740682B2 (en) * 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
JP3676677B2 (ja) 1998-06-30 2005-07-27 ファイザー・プロダクツ・インク 炎症性疾患、自己免疫疾患および呼吸疾患の治療において有用なvla−4依存性細胞結合の非ペプチジル阻害薬
EP1126833A4 (en) 1998-10-29 2004-09-08 Trega Biosciences Inc OXADIAZOLE, THIADIAZOLE AND TRIAZOLE DERIVATIVES AND COMBINATORIAL LIBRARIES CONTAINING THESE DERIVATIVES
US6518292B1 (en) 1999-03-12 2003-02-11 Bristol-Myers Squibb Co. Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
TWI283577B (en) 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
WO2001032628A1 (en) 1999-11-03 2001-05-10 Bristol-Myers Squibb Pharma Company Cyano compounds as factor xa inhibitors
YU41202A (sh) 1999-12-28 2005-03-15 Pfizer Products Inc. Ne-peptidni inhibitori vezivanja za ćeliju zavisnog od vla-4 korisni pri tretiranju inflamatornih, autoimunih i respiratornih bolesti
WO2001052867A1 (en) 2000-01-19 2001-07-26 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Use of pentosan polysulfate to treat certain conditions of the prostate
AR029803A1 (es) * 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
EP1263753B1 (en) * 2000-03-06 2004-05-06 SmithKline Beecham plc Imidazol derivatives as raf kinase inhibitors
US6414013B1 (en) * 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
GB0021831D0 (en) 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
KR100673265B1 (ko) * 2000-10-04 2007-01-22 엘지.필립스 엘시디 주식회사 액정표시장치
CN100581544C (zh) 2001-03-05 2010-01-20 美国医疗产品公司 用于勃起机能障碍治疗和逆转的可注射药物组合物
CN1235583C (zh) 2001-03-05 2006-01-11 特兰斯泰克制药公司 用作治疗剂的苯并咪唑衍生物
AU2002344820B2 (en) 2001-06-20 2006-12-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
AU2002348394A1 (en) 2001-10-25 2003-05-06 Merck And Co., Inc. Tyrosine kinase inhibitors
DE10211770A1 (de) 2002-03-14 2003-10-02 Boehringer Ingelheim Pharma Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
PE20040804A1 (es) * 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
EP1613629A1 (en) 2003-03-27 2006-01-11 Pfizer Products Inc. Substituted 4-amino 1,2,4 triazolo 4,3-a quinoxalines
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
EP1479679A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
EP1670798A1 (en) 2003-10-01 2006-06-21 Altana Pharma AG Aminopyridine-derivatives as inductible no-synthase inhibitors
US7128412B2 (en) * 2003-10-03 2006-10-31 Xerox Corporation Printing processes employing intermediate transfer with molten intermediate transfer materials
TW200524601A (en) 2003-12-05 2005-08-01 Bristol Myers Squibb Co Heterocyclic anti-migraine agents
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
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
CN101137412B (zh) 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物
JP5225098B2 (ja) 2005-12-14 2013-07-03 ブリストル−マイヤーズ スクイブ カンパニー 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

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000511173A (ja) * 1996-05-27 2000-08-29 藤沢薬品工業株式会社 一酸化窒素産生阻害剤としての新規なインドリルおよびベンゾフラニルカルボキサミド
JP2001505585A (ja) * 1996-12-16 2001-04-24 藤沢薬品工業株式会社 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途
JP2003523921A (ja) * 1998-06-12 2003-08-12 ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス イミダゾリル誘導体
WO2002010140A2 (en) * 2000-08-01 2002-02-07 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Imidazolyl derivatives
WO2004011445A1 (ja) * 2002-07-31 2004-02-05 Nippon Soda Co.,Ltd. アミノサリチル酸アミド誘導体、製造法及び農園芸用殺菌剤
WO2004017908A2 (en) * 2002-08-26 2004-03-04 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
JP2004323516A (ja) * 2003-04-11 2004-11-18 Nippon Soda Co Ltd 3−アシルアミノサリチル酸アミド誘導体、製造法及び農園芸用殺菌剤

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