CA2960790A1 - Pyrazolyl-substituted pyridone compounds as serine protease inhibitors - Google Patents

Pyrazolyl-substituted pyridone compounds as serine protease inhibitors Download PDF

Info

Publication number
CA2960790A1
CA2960790A1 CA2960790A CA2960790A CA2960790A1 CA 2960790 A1 CA2960790 A1 CA 2960790A1 CA 2960790 A CA2960790 A CA 2960790A CA 2960790 A CA2960790 A CA 2960790A CA 2960790 A1 CA2960790 A1 CA 2960790A1
Authority
CA
Canada
Prior art keywords
substituted
unsubstituted
compound
aryl
compound according
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.)
Abandoned
Application number
CA2960790A
Other languages
English (en)
French (fr)
Inventor
Kevin Michael Short
David Ben Kita
Maria De Los Angeles Estiarte-Martinez
Son Minh Pham
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.)
Verseon Corp
Original Assignee
Verseon Corp
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 Verseon Corp filed Critical Verseon Corp
Publication of CA2960790A1 publication Critical patent/CA2960790A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
CA2960790A 2014-09-17 2015-09-17 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors Abandoned CA2960790A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462051511P 2014-09-17 2014-09-17
US201462051585P 2014-09-17 2014-09-17
US62/051,511 2014-09-17
US62/051,585 2014-09-17
PCT/US2015/050809 WO2016044662A1 (en) 2014-09-17 2015-09-17 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Publications (1)

Publication Number Publication Date
CA2960790A1 true CA2960790A1 (en) 2016-03-24

Family

ID=55533876

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2960790A Abandoned CA2960790A1 (en) 2014-09-17 2015-09-17 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Country Status (14)

Country Link
US (2) US10189810B2 (enExample)
EP (1) EP3194369A4 (enExample)
JP (2) JP2017528486A (enExample)
KR (1) KR20170048410A (enExample)
CN (1) CN106687445A (enExample)
AU (2) AU2015317522A1 (enExample)
BR (1) BR112017004704A2 (enExample)
CA (1) CA2960790A1 (enExample)
IL (1) IL250965A0 (enExample)
MX (1) MX2017003624A (enExample)
RU (1) RU2017112739A (enExample)
SG (1) SG11201701940UA (enExample)
WO (1) WO2016044662A1 (enExample)
ZA (1) ZA201701799B (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
BR112017004704A2 (pt) * 2014-09-17 2018-01-23 Verseon Corp composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio em um indivíduo
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
RS60900B1 (sr) 2016-02-19 2020-11-30 Sprint Bioscience Ab Jedinjenja 6-heterociklil-4-morfolin-4-ilpiridin-2-ona korisna za lečenje kancera i dijabetesa
US11077113B2 (en) 2016-02-19 2021-08-03 Sprint Bioscience Ab 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
CN106008362B (zh) * 2016-05-24 2018-08-10 杰达维（上海）医药科技发展有限公司 一种嘧啶衍生物的制备方法
CA3025718A1 (en) 2016-05-31 2017-12-07 Kalvista Pharmaceuticals Limited Pyrazole derivatives as plasma kallikrein inhibitors
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
WO2018139560A1 (ja) * 2017-01-26 2018-08-02 三井化学アグロ株式会社 ピリドン化合物およびそれを有効成分とする農園芸用殺菌剤
TWI788343B (zh) 2017-04-18 2023-01-01 美商塞爾基因定量細胞研究公司 治療用化合物
SI3716952T1 (sl) 2017-11-29 2022-04-29 Kalvista Pharmaceuticals Limited Farmacevtske oblike, ki obsegajo zaviralec plazemskega kalikreina
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
CN110386932A (zh) 2018-04-20 2019-10-29 艾科思莱德制药公司 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂
SG11202100247WA (en) * 2018-07-13 2021-02-25 Verseon Int Corporation Thrombin inhibitors, formulations, and uses thereof
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN110467601B (zh) * 2019-08-29 2021-07-02 杭州市西溪医院 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität
BR102020009679A2 (pt) 2020-05-14 2021-11-23 Fundação Universidade Federal Do Abc - Ufabc Anticorpos recombinantes humanos para inibição da calicreína tecidual humana 7 (klk7) e uso em doenças relacionadas ao processo de descamação da pele
US12414955B2 (en) 2020-11-25 2025-09-16 Deciphera Pharmaceuticals, Llc Anti-viral activity of VPS34 inhibitors

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
RU2002110295A (ru) 1999-09-17 2003-12-10 Милленниум Фармасьютикалс, Инк. (Us) Ингибиторы фактора Ха
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
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
US20040147561A1 (en) 2002-12-27 2004-07-29 Wenge Zhong Pyrid-2-one derivatives and methods of use
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
US7429604B2 (en) * 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
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
CN101484438A (zh) 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 吡唑衍生物及其作为p13k抑制剂的用途
EP2035005A4 (en) 2006-06-09 2011-07-06 Kemia Inc THERAPY BASED ON CYTOKINE INHIBITORS
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
EP2331096A1 (en) 2008-08-19 2011-06-15 Boehringer Ingelheim International GmbH Dabigatran in tumour therapy
EP2328581A1 (en) 2008-08-19 2011-06-08 Boehringer Ingelheim International GmbH Use of dabigatranetexilate for treating patients with pulmonary hypertension
MX2011001612A (es) 2008-08-19 2011-03-04 Boehringer Ingelheim Int Dabigatran para cateterismo cardiaco con intervencion percutanea.
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
ES2700542T3 (es) 2010-06-24 2019-02-18 Gilead Sciences Inc Composición farmacéutica que comprende un derivado de pirazolo[1,5-A]pirimidina como un agente antiviral
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
WO2012129258A1 (en) 2011-03-22 2012-09-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
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
KR20150021036A (ko) 2012-06-14 2015-02-27 다이이찌 산쿄 가부시키가이샤 피페리디닐피라졸로피리딘 유도체
CN104918934B (zh) 2013-01-18 2017-12-22 霍夫曼-拉罗奇有限公司 3‑取代的吡唑及其作为dlk抑制剂的用途
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
WO2015087995A1 (ja) 2013-12-13 2015-06-18 第一三共株式会社 シクロアルキル又はヘテロシクリルピラゾロピリジン誘導体
SI3406609T1 (sl) 2014-02-06 2024-10-30 Nxera Pharma Uk Limited Biciklične aza spojine kot agonisti muskarinskega receptorja
BR112017004704A2 (pt) * 2014-09-17 2018-01-23 Verseon Corp composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio em um indivíduo

Also Published As

Publication number Publication date
AU2015317522A1 (en) 2017-03-23
RU2017112739A3 (enExample) 2019-04-01
SG11201701940UA (en) 2017-04-27
BR112017004704A2 (pt) 2018-01-23
JP2020143112A (ja) 2020-09-10
IL250965A0 (en) 2017-04-30
US20190359586A1 (en) 2019-11-28
EP3194369A1 (en) 2017-07-26
US20170267656A1 (en) 2017-09-21
JP2017528486A (ja) 2017-09-28
EP3194369A4 (en) 2018-02-28
AU2020202167A1 (en) 2020-04-30
MX2017003624A (es) 2017-07-13
WO2016044662A1 (en) 2016-03-24
US10189810B2 (en) 2019-01-29
KR20170048410A (ko) 2017-05-08
RU2017112739A (ru) 2018-10-17
CN106687445A (zh) 2017-05-17
ZA201701799B (en) 2019-06-26

Similar Documents

Publication Publication Date Title
CA2960790A1 (en) Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
AU2018200736B2 (en) Multisubstituted aromatic compounds as serine protease inhibitors
CA2977993A1 (en) Substituted pyrazole compounds as serine protease inhibitors
AU2014238478A1 (en) Halogenopyrazoles as inhibitors of thrombin
HK1214142B (en) Multisubstituted aromatic compounds as serine protease inhibitors

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20211208

FZDE Discontinued

Effective date: 20211208