JP2016512243A5 - - Google Patents

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JP2016512243A5
JP2016512243A5 JP2016500154A JP2016500154A JP2016512243A5 JP 2016512243 A5 JP2016512243 A5 JP 2016512243A5 JP 2016500154 A JP2016500154 A JP 2016500154A JP 2016500154 A JP2016500154 A JP 2016500154A JP 2016512243 A5 JP2016512243 A5 JP 2016512243A5
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JP6479749B2 (ja
JP2016512243A (ja
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Priority claimed from PCT/US2014/000058 external-priority patent/WO2014149139A2/en
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JP2016500154A 2013-03-15 2014-03-17 トロンビン阻害剤としてのハロゲノピラゾール Active JP6479749B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361789358P 2013-03-15 2013-03-15
US61/789,358 2013-03-15
US201361899588P 2013-11-04 2013-11-04
US61/899,588 2013-11-04
PCT/US2014/000058 WO2014149139A2 (en) 2013-03-15 2014-03-17 Halogenopyrazoles as inhibitors of thrombin

Related Child Applications (1)

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JP2019019308A Division JP2019081782A (ja) 2013-03-15 2019-02-06 トロンビン阻害剤としてのハロゲノピラゾール

Publications (3)

Publication Number Publication Date
JP2016512243A JP2016512243A (ja) 2016-04-25
JP2016512243A5 true JP2016512243A5 (enExample) 2017-04-20
JP6479749B2 JP6479749B2 (ja) 2019-03-06

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JP2016500154A Active JP6479749B2 (ja) 2013-03-15 2014-03-17 トロンビン阻害剤としてのハロゲノピラゾール
JP2019019308A Pending JP2019081782A (ja) 2013-03-15 2019-02-06 トロンビン阻害剤としてのハロゲノピラゾール
JP2020103499A Pending JP2020158522A (ja) 2013-03-15 2020-06-16 トロンビン阻害剤としてのハロゲノピラゾール

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JP2019019308A Pending JP2019081782A (ja) 2013-03-15 2019-02-06 トロンビン阻害剤としてのハロゲノピラゾール
JP2020103499A Pending JP2020158522A (ja) 2013-03-15 2020-06-16 トロンビン阻害剤としてのハロゲノピラゾール

Country Status (16)

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US (2) US9951025B2 (enExample)
EP (1) EP2970141B1 (enExample)
JP (3) JP6479749B2 (enExample)
KR (1) KR20150130405A (enExample)
CN (2) CN110423221A (enExample)
AU (2) AU2014238478B2 (enExample)
BR (1) BR112015023214A8 (enExample)
CA (1) CA2902431A1 (enExample)
ES (1) ES2791749T3 (enExample)
HK (1) HK1214252A1 (enExample)
IL (1) IL240763B (enExample)
MX (1) MX373646B (enExample)
RU (1) RU2015144193A (enExample)
SG (2) SG10201707486XA (enExample)
WO (2) WO2014149139A2 (enExample)
ZA (1) ZA201506440B (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2853483T3 (es) 2013-03-15 2021-09-16 Verseon Int Corporation Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa
ES2791749T3 (es) 2013-03-15 2020-11-05 Verseon Corp Halogenopirazoles como inhibidores de la trombina
HK1246164A1 (zh) * 2015-02-27 2018-09-07 Verseon Corporation 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物
SG11202110406SA (en) 2019-04-11 2021-10-28 Angion Biomedica Corp Solid forms of (e)-3-[2-(2-thienyl)vinyl]-1h-pyrazole
CN112062692A (zh) * 2019-06-11 2020-12-11 太仓市茜泾化工有限公司 一种乙氧甲叉氰基乙酸乙酯的制备方法
CN112986065B (zh) * 2021-02-08 2021-08-31 杭州同创医学检验实验室有限公司 一种用于血细胞分析仪的全血质控品及其制备方法

Family Cites Families (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1323438A (en) * 1919-12-02 of niagara falls
US188918A (en) * 1877-03-27 Improvement in towel-racks
BE627393A (enExample) 1962-01-23
BE793955A (fr) 1972-01-15 1973-07-12 Merck Patent Gmbh Arylpiperazines et leur procede de preparation
DE2409753A1 (de) 1974-03-01 1975-09-11 Basf Ag Substituierte pyrazole
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
PH23506A (en) 1986-05-23 1989-08-16 Smithkline Beckman Corp 1-aralkyl-substituted-1,2,4,-triazole-5-thiols as dopamine- -hydroxylase inhibitors
JPH089541B2 (ja) 1988-03-07 1996-01-31 三井東圧化学株式会社 ピラゾール類を主成分とする脳浮腫抑制剤
JP2784925B2 (ja) * 1988-09-07 1998-08-13 日本農薬株式会社 3又は5−フェニルピラゾール類又はその塩及び除草剤
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
JP3810097B2 (ja) 1993-01-15 2006-08-16 明治製菓株式会社 ピロリジン−2−イルカルボニル複素環式化合物誘導体
ES2172959T3 (es) * 1993-11-30 2002-10-01 Searle & Co Pirazolil-bencenosulfonamidas triciclicas, sustituidas y su uso como inhibidores de ciclooxigenasa ii.
US5466823A (en) * 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
ATE262902T1 (de) 1994-11-10 2004-04-15 Millennium Pharm Inc Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
US5733955A (en) 1995-02-10 1998-03-31 The Goodyear Tire & Rubber Company Asphalt cement modification
JP3663522B2 (ja) * 1995-08-12 2005-06-22 日本農薬株式会社 植物生育調節用組成物及びその使用方法
US5756529A (en) 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
WO1997013756A1 (en) 1995-10-13 1997-04-17 Otsuka Kagaku Kabushiki Kaisha Pyrazole derivatives and insecticidal compositions containing the same as active ingredient
US5792761A (en) * 1996-08-12 1998-08-11 Merck & Co., Inc. Thrombin inhibitors
ES2185042T3 (es) * 1996-08-12 2003-04-16 Merck & Co Inc Inhibidores de la trombina.
DE19632773A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
GB9622370D0 (en) 1996-10-28 1997-01-08 Merck Sharp & Dohme Therapeutic agents
US5869500A (en) 1996-12-13 1999-02-09 Hoffmann-La Roche Inc. Pyridone compounds useful in treating Alzheimer's disease
HUP0000735A3 (en) * 1996-12-23 2002-03-28 Bristol Myers Squibb Pharma Co Nitrogen containing heteroaromatics as factor xa inhibitors
CN1250446A (zh) 1997-03-21 2000-04-12 诺瓦提斯公司 作为除草剂的吡唑衍生物
KR20010071975A (ko) 1998-08-11 2001-07-31 해슬러 요세 살선충성 피라졸
KR20000047461A (ko) 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
SE9900070D0 (sv) 1999-01-13 1999-01-13 Astra Ab New use
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
AU5020400A (en) * 1999-05-20 2000-12-12 E.I. Du Pont De Nemours And Company Heteroaryloxypyrimidine insecticides and acaricides
PL353455A1 (en) 1999-08-12 2003-11-17 Pharmacia Italia S.P.A. 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
WO2001019798A2 (en) 1999-09-17 2001-03-22 Cor Therapeutics Inc. INHIBITORS OF FACTOR Xa
PT1254135E (pt) 1999-12-02 2005-03-31 Novartis Ag Compostos organicos
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
EP1404669A2 (en) 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
US6589997B2 (en) 2001-06-29 2003-07-08 North Shore-Long Island Jewish Health System Small-molecule modulators of hepatocyte growth factor/scatter factor activities
SI21097A (sl) 2001-12-04 2003-06-30 Univerza V Ljubljani Inhibitorji trombina
EP1509505A2 (en) 2002-01-23 2005-03-02 Arena Pharmaceuticals, Inc. SMALL MOLECULE MODULATORS OF THE 5−HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
JP2003313103A (ja) * 2002-02-20 2003-11-06 Sankyo Agro Kk 4−アシルアミノピラゾール誘導体を有効成分として含有する農薬
GB0214139D0 (en) 2002-06-19 2002-07-31 Glaxo Group Ltd Chemical compounds
DE10229070A1 (de) 2002-06-28 2004-01-15 Merck Patent Gmbh Phenylderivate 5
AU2003268064A1 (en) 2002-08-09 2004-02-25 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
AU2003274025A1 (en) 2002-10-17 2004-05-04 Syngenta Participations Ag Pyridine derivatives useful as herbicides
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
DE60329529D1 (de) 2002-12-23 2009-11-12 Sanofi Aventis Deutschland Pyrazolderivate als faktor-xa-inhibitoren
WO2004058722A1 (en) 2002-12-24 2004-07-15 Arena Pharmaceuticals, Inc. Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
JP2004231528A (ja) * 2003-01-28 2004-08-19 Sankyo Agro Kk アミド誘導体
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
ES2370463T3 (es) * 2003-05-01 2011-12-16 Bristol-Myers Squibb Company Compuestos de pirazol - amida sustituidos con arilo útiles como inhibidores de quinasa.
ATE410161T1 (de) * 2003-05-02 2008-10-15 Elan Pharm Inc 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3- carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen
US7223780B2 (en) 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
EP1479679A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
JP2007513058A (ja) 2003-09-08 2007-05-24 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
US7749999B2 (en) 2003-09-11 2010-07-06 Itherx Pharmaceuticals, Inc. Alpha-ketoamides and derivatives thereof
EP1667983A4 (en) 2003-09-23 2010-07-21 Merck Sharp & Dohme PYRAZOL MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
US20080188527A1 (en) 2003-12-23 2008-08-07 Cashman John R Synthetic Compounds and Derivatives as Modulators of Smoking or Nicotine Ingestion and Lung Cancer
WO2005092899A1 (en) * 2004-03-26 2005-10-06 Methylgene Inc. Inhibitors of histone deacetylase
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
EP1845972A4 (en) 2005-01-10 2010-12-22 Univ Connecticut CANNAPINOID RECEPTORS APPLYING NOVEL HETEROPYRROL ANALOGS
WO2006109846A1 (ja) 2005-04-06 2006-10-19 Takeda Pharmaceutical Company Limited トリアゾール誘導体およびその用途
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CN100427481C (zh) 2005-05-26 2008-10-22 沈阳化工研究院 一种芳基醚类化合物及其制备与应用
CA2630233A1 (en) 2005-12-05 2007-06-14 Boehringer Ingelheim International Gmbh Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
DE102006032824A1 (de) * 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
WO2008009638A2 (en) 2006-07-17 2008-01-24 Boehringer Ingelheim International Gmbh New indications for direct thrombin inhibitors in the cardiovascular field
JP5322935B2 (ja) 2006-07-31 2013-10-23 アクティベサイト ファーマシューティカルズ インコーポレイティッド 血漿カリクレインの阻害薬
WO2008023235A1 (en) * 2006-08-25 2008-02-28 Pfizer Products Inc. Pyrazole derivatives as anti-platelet and anti-thrombotic agents
EP2096111A1 (en) 2006-11-20 2009-09-02 Japan Tobacco Inc. Pyrazoles and use thereof as drugs
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
EP2121619A2 (en) * 2006-11-24 2009-11-25 AC Immune S.A. Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
JP2010513519A (ja) 2006-12-22 2010-04-30 ミレニアム・ファーマシューティカルズ・インコーポレイテッド キナーゼインヒビター活性を有するある種のピラゾリン誘導体
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2008105383A1 (ja) 2007-02-26 2008-09-04 Toray Industries, Inc. ピラゾール誘導体およびその医薬用途
GB0714129D0 (en) 2007-07-19 2007-08-29 Smithkline Beecham Corp compounds
MX2010001566A (es) * 2007-08-06 2010-03-15 Dainippon Sumitomo Pharma Co Derivado de aminopirazolamida.
US8334301B2 (en) 2007-09-28 2012-12-18 Takeda Pharmaceutical Company Limited 5-Membered heterocyclic compound
EP2219646A4 (en) 2007-12-21 2010-12-22 Univ Rochester PROCESS FOR EXTENDING THE LIFE OF EUKARYOTIC ORGANISMS
EP2259679A4 (en) 2008-01-31 2011-09-14 Joslin Diabetes Ct METHODS OF TREATING KALLIKREIN RELATED DISORDERS
AU2009212135B2 (en) 2008-02-07 2014-08-21 Massachusetts Eye & Ear Infirmary Compounds that enhance Atoh-1 expression
WO2009140621A2 (en) 2008-05-15 2009-11-19 Duke University Compositions and methods relating to heat shock transcription factor activating compounds and targets thereof
WO2009143039A2 (en) 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
CN102149379A (zh) 2008-07-10 2011-08-10 安吉翁生物医药有限公司 调节肝细胞生长因子(分散因子)活性的方法和肝细胞生长因子(分散因子)活性的小分子调节剂组合物
US8273900B2 (en) * 2008-08-07 2012-09-25 Novartis Ag Organic compounds
CA2733958A1 (en) * 2008-08-14 2010-02-18 Bayer Cropscience Ag Insecticidal 4-phenyl-1h-pyrazoles
CA2734809A1 (en) 2008-08-19 2010-02-25 Boehringer Ingelheim International Gmbh Dabigatran in tumour therapy
JP2012500243A (ja) 2008-08-19 2012-01-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 肺高血圧症患者の治療のためのダビガトランエテキシラートの使用
CA2734794A1 (en) 2008-08-19 2010-02-25 Boehringer Ingelheim International Gmbh Dabigatran for percutaneous interventional cardiac catheterisation
MX2011011800A (es) 2009-05-07 2012-01-27 Gruenenthal Gmbh Derivados de carboxamida y urea aromaticas sustituidas como ligandos del receptor de vanilloides.
CA2829790C (en) 2010-03-30 2018-06-05 Verseon Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
CN101851207B (zh) 2010-06-11 2012-01-25 扬州康伊尔医药科技有限公司 抗病毒化合物中间体1-酰基-吡唑-3-羧酸及其制备方法
EP2604602A4 (en) * 2010-08-11 2013-12-18 Taisho Pharmaceutical Co Ltd HETEROARYL PYRAZOLE DERIVATIVE
JP6072695B2 (ja) * 2010-11-03 2017-02-01 ダウ アグロサイエンシィズ エルエルシー 殺有害生物剤組成物およびこれに関連した方法
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
EP2697196A1 (en) 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2012154880A1 (en) * 2011-05-09 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases
SG194847A1 (en) 2011-05-17 2013-12-30 Plexxikon Inc Kinase modulation and indications therefor
US9371307B2 (en) 2011-09-12 2016-06-21 The Johns Hopkins University Serine protease inhibitors
WO2013049591A2 (en) 2011-09-29 2013-04-04 Verseon Corporation Dual inhibitor compounds and methods of use thereof
EP3112363A1 (en) 2011-12-27 2017-01-04 Ironwood Pharmaceuticals, Inc. 2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1h-pyrazol-3-yl]-pyrimidine derivatives and related compounds as soluble guanylate cyclase (sgc) stimulators for the treatment of pulmonary hypertension
US20140378474A1 (en) 2012-01-27 2014-12-25 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
ES2791749T3 (es) * 2013-03-15 2020-11-05 Verseon Corp Halogenopirazoles como inhibidores de la trombina
ES2853483T3 (es) 2013-03-15 2021-09-16 Verseon Int Corporation Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa

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