JP2016512243A5 - - Google Patents

Download PDF

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
substituted
unsubstituted
group
compound according
compound
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.)
Granted
Application number
JP2016500154A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016512243A (ja
JP6479749B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2014/000058 external-priority patent/WO2014149139A2/en
Publication of JP2016512243A publication Critical patent/JP2016512243A/ja
Publication of JP2016512243A5 publication Critical patent/JP2016512243A5/ja
Application granted granted Critical
Publication of JP6479749B2 publication Critical patent/JP6479749B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)

Application Number Title Priority Date Filing Date
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

Family

ID=51538179

Family Applications (3)

Application Number Title Priority Date Filing Date
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

Family Applications After (2)

Application Number Title Priority Date Filing Date
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)

Country Link
US (2) US9951025B2 (enExample)
EP (1) EP2970141B1 (enExample)
JP (3) JP6479749B2 (enExample)
KR (1) KR20150130405A (enExample)
CN (2) CN105209440B (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
HK1214252A1 (zh) * 2013-03-15 2016-07-22 Verseon Corporation 作為凝血酶抑制劑的鹵代吡唑
CN110101699A (zh) 2013-03-15 2019-08-09 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物
PL3261639T3 (pl) * 2015-02-27 2022-12-19 Verseon International Corporation Podstawione związki pirazolowe jako inhibitory proteazy serynowej
MX2021012250A (es) 2019-04-11 2022-01-18 Angion Biomedica Corp Formas solidas de (e)-3-[2-(2-tienil)vinil]-1h-pirazol.
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
US188918A (en) * 1877-03-27 Improvement in towel-racks
US1323438A (en) * 1919-12-02 of niagara falls
BE627394A (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
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
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
IL82542A0 (en) 1986-05-23 1987-11-30 Smithkline Beckman Corp Triazole derivatives,their preparation and pharmaceutical compositions containing them
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
EP0495421B1 (en) 1991-01-15 1996-08-21 Alcon Laboratories, Inc. Use of carrageenans in topical ophthalmic compositions
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
US5466823A (en) * 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
CZ294630B6 (cs) 1993-11-30 2005-02-16 G. D. Searle & Co. Substituované pyrazolylbenzensulfonamidy pro léčení zánětů
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
ES2219670T3 (es) 1994-11-10 2004-12-01 Millennium Pharmaceuticals, Inc. Utilizacion de compuestos de pirazola para el tratamiento de la glomerulonefritis, cancer, ateroesclerosis o restenosis.
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
DE69717147T2 (de) * 1996-08-12 2003-07-24 Merck & Co., Inc. Thrombin inhibitoren
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
ATE443698T1 (de) 1996-12-23 2009-10-15 Bristol Myers Squibb Pharma Co Stickstoffhaltige heterocyclen als faktor xa- hemmer
ID22380A (id) 1997-03-21 1999-10-07 Novartis Ag Turunan-turunan pirazol sebagai herbisida
WO2000009500A2 (en) 1998-08-11 2000-02-24 Nihon Bayer Agrochem K.K. Nematicidal pyrazoles
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
EE200200065A (et) 1999-08-12 2003-04-15 Pharmacia Italia S.P.A. 3-aminopürasooli derivaadid, nende valmistamine ja kasutamine vähivastaste toimeainetena ning neid sisaldav farmatseutiline kompositsioon
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
RU2002110295A (ru) 1999-09-17 2003-12-10 Милленниум Фармасьютикалс, Инк. (Us) Ингибиторы фактора Ха
CA2390113A1 (en) 1999-12-02 2001-06-07 Maurizio Schwarzenbach Aminoheterocyclylamides as pesticides and antiparasitic agents
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
JP4316893B2 (ja) 2001-05-16 2009-08-19 バーテックス ファーマシューティカルズ インコーポレイテッド Srcおよび他のプロテインキナーゼのインヒビター
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
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
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
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
AR041508A1 (es) 2002-08-09 2005-05-18 Astra Ab Compuestos con actividad en los receptores de glutamato metabotropicos
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
JP4585448B2 (ja) 2002-12-23 2010-11-24 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 第Xa因子阻害剤としてのピラゾール−誘導体
US20060229335A1 (en) * 2002-12-24 2006-10-12 Bradley Teegarden 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
ATE482200T1 (de) * 2003-05-01 2010-10-15 Bristol Myers Squibb Co Als kinaseinhibitoren geeignete arylsubstituierte pyrazolamidverbindungen
EP1633348B1 (en) * 2003-05-02 2008-10-08 Elan Pharmaceuticals, Inc. 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B sb 1 /sb RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES
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
EP1697342A2 (en) 2003-09-08 2006-09-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
BRPI0414313A (pt) 2003-09-11 2006-11-07 Kemia Inc inibidores de citocinas
WO2005030128A2 (en) 2003-09-23 2005-04-07 Merck & Co., Inc. Pyrazole modulators of metabotropic glutamate receptors
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
WO2005066162A1 (en) 2003-12-23 2005-07-21 Human Biomolecular Research Institute Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer
KR101258504B1 (ko) * 2004-03-26 2013-04-26 메틸진 인코포레이티드 히스톤 데아세틸라제의 억제제
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
EP2368881A1 (en) 2005-01-10 2011-09-28 University of Connecticut Heteropyrazole analogs acting on cannabinoid receptors
JPWO2006109846A1 (ja) 2005-04-06 2008-11-20 武田薬品工業株式会社 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
JP2009518442A (ja) 2005-12-05 2009-05-07 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 可溶性エポキシド加水分解酵素インヒビターとして有益な置換ピラゾール化合物
DE102006032824A1 (de) * 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
MX2009000602A (es) 2006-07-17 2009-01-28 Boehringer Ingelheim Int Nuevas indicaciones para los inhibidores directos de la trombina en el campo cardiovascular.
EP2051707B1 (en) 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
WO2008023235A1 (en) * 2006-08-25 2008-02-28 Pfizer Products Inc. Pyrazole derivatives as anti-platelet and anti-thrombotic agents
WO2008062739A1 (en) 2006-11-20 2008-05-29 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
US20100144793A1 (en) * 2006-11-24 2010-06-10 Ac Immune Sa Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
US7795249B2 (en) 2006-12-22 2010-09-14 Millennium Pharmaceuticals, Inc. Certain pyrazoline derivatives with kinase inhibitory activity
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
WO2009020137A1 (ja) * 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. アミノピラゾールアミド誘導体
US8334301B2 (en) 2007-09-28 2012-12-18 Takeda Pharmaceutical Company Limited 5-Membered heterocyclic compound
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009097141A1 (en) 2008-01-31 2009-08-06 Joslin Diabetes Center Methods for treatment of kallikrein-related disorders
EP2732819B1 (en) 2008-02-07 2019-10-16 Massachusetts Eye & Ear Infirmary Compounds that enhance Atoh-1 expression
CN102088973A (zh) 2008-05-15 2011-06-08 杜克大学 与热休克转录因子激活化合物及其靶标有关的组合物和方法
EP2300435A2 (en) 2008-05-19 2011-03-30 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
EP2374791A1 (de) * 2008-08-14 2011-10-12 Bayer CropScience Aktiengesellschaft Insektizide 4-Phenyl-1H-pyrazole
MX2011001612A (es) 2008-08-19 2011-03-04 Boehringer Ingelheim Int Dabigatran para cateterismo cardiaco con intervencion percutanea.
EP2328581A1 (en) 2008-08-19 2011-06-08 Boehringer Ingelheim International GmbH Use of dabigatranetexilate for treating patients with pulmonary hypertension
EP2331096A1 (en) 2008-08-19 2011-06-15 Boehringer Ingelheim International GmbH Dabigatran in tumour therapy
SI2427436T1 (sl) 2009-05-07 2013-04-30 Grunenthal Gmbh Substituirani aromatski karboksamidni in sečninski derivati kot ligandi vaniloidnega receptorja
SG10201502484SA (en) * 2010-03-30 2015-05-28 Verseon Corp 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
CN105360132A (zh) * 2010-11-03 2016-03-02 陶氏益农公司 杀虫组合物和与其相关的方法
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
JP6113151B2 (ja) 2011-05-17 2017-04-12 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼ調節およびその適応症
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
US9139564B2 (en) 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators
EP2807157A1 (en) 2012-01-27 2014-12-03 Novartis AG 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
CN110101699A (zh) 2013-03-15 2019-08-09 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物
HK1214252A1 (zh) 2013-03-15 2016-07-22 Verseon Corporation 作為凝血酶抑制劑的鹵代吡唑

Similar Documents

Publication Publication Date Title
JP2016512243A5 (enExample)
JP2016513714A5 (enExample)
JP2016530259A5 (enExample)
JP2018507238A5 (enExample)
JP2016516699A5 (enExample)
JP2019524883A5 (enExample)
JP2011520967A5 (enExample)
JP2017528486A5 (enExample)
JP2016539180A5 (enExample)
AU2018250514A1 (en) Halogenopyrazoles as inhibitors of thrombin
JP2019527215A5 (enExample)
JP2013537203A5 (enExample)
JP2017517512A5 (enExample)
JP2009536218A5 (enExample)
JP2014193925A5 (enExample)
HRP20171950T1 (hr) Pirimidinoni kao inhibitori faktora xia
JP2017504642A5 (enExample)
JP2018500360A5 (enExample)
JP2015524443A5 (enExample)
JP2013509431A5 (enExample)
JP2013510125A5 (enExample)
JP2015529235A5 (enExample)
JP2015514806A5 (enExample)
GEAP201914608A (en) Fused bicyclic heteroaryl derivatives having activity as phd inhibitors
JP2013544860A5 (enExample)