ZA201701799B - Pyrazolyl-substituted pyridone compounds as serine protease inhibitors - Google Patents

Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Info

Publication number
ZA201701799B
ZA201701799B ZA2017/01799A ZA201701799A ZA201701799B ZA 201701799 B ZA201701799 B ZA 201701799B ZA 2017/01799 A ZA2017/01799 A ZA 2017/01799A ZA 201701799 A ZA201701799 A ZA 201701799A ZA 201701799 B ZA201701799 B ZA 201701799B
Authority
ZA
South Africa
Prior art keywords
pyrazolyl
protease inhibitors
serine protease
pyridone compounds
substituted pyridone
Prior art date
Application number
ZA2017/01799A
Other languages
English (en)
Inventor
Michael Short Kevin
Ben Kita David
De Los Angeles Estiarte-Martinez Maria
Minh Pham Son
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 ZA201701799B publication Critical patent/ZA201701799B/en

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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
ZA2017/01799A 2014-09-17 2017-03-13 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors ZA201701799B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462051511P 2014-09-17 2014-09-17
US201462051585P 2014-09-17 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
ZA201701799B true ZA201701799B (en) 2019-06-26

Family

ID=55533876

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2017/01799A ZA201701799B (en) 2014-09-17 2017-03-13 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
ES2853483T3 (es) * 2013-03-15 2021-09-16 Verseon Int Corporation Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa
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
SG11201701940UA (en) * 2014-09-17 2017-04-27 Verseon Corp Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
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
SI3416945T1 (sl) 2016-02-19 2020-11-30 Sprint Bioscience Ab Spojine 6-aril-4-(morfolin-4-IL)-1H-piridin-2-ona, uporabne za zdravljenje raka in diabetesa
SMT202000529T1 (it) 2016-02-19 2020-11-10 Sprint Bioscience Ab Composti di 6-eterociclil-4-morfolina-4-ilpiridin-2-one utili per il trattamento di cancro e diabete
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
RS60600B1 (sr) 2016-05-31 2020-08-31 Kalvista Pharmaceuticals Ltd Derivati pirazola kao inhibitori kalikreina plazme
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
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
JP7037507B2 (ja) * 2017-01-26 2022-03-16 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
WO2018195155A1 (en) * 2017-04-18 2018-10-25 Celgene Quanticel Research, Inc. Therapeutic compounds
PL3716952T3 (pl) 2017-11-29 2022-05-02 Kalvista Pharmaceuticals Limited Postacie dawkowania zawierające inhibitor kalikreiny osoczowej
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
AU2019300161B2 (en) * 2018-07-13 2025-05-22 Verseon International Corporation Thrombin inhibitors, formulations, and uses thereof
CN114206852A (zh) 2019-08-09 2022-03-18 卡尔维斯塔制药有限公司 血浆激肽释放酶抑制剂
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
EP4251166A1 (en) 2020-11-25 2023-10-04 Deciphera Pharmaceuticals, LLC Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
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
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
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
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
EP2016068A1 (en) 2006-05-03 2009-01-21 AstraZeneca AB Pyrazole derivatives and their use as pi3k inhibitors
CA2691214A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine 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
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
CA2734809A1 (en) 2008-08-19 2010-02-25 Boehringer Ingelheim International Gmbh Dabigatran in tumour therapy
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
US8486938B2 (en) 2010-06-24 2013-07-16 Gilead Sciences, Inc. Pyrazolo[1,5-a]pyrimidines for antiviral treatment
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
EP2688872A4 (en) 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED 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
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
JPWO2013187462A1 (ja) 2012-06-14 2016-02-08 第一三共株式会社 ピペリジニルピラゾロピリジン誘導体
MX2015009270A (es) 2013-01-18 2015-10-30 Hoffmann La Roche Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk).
ES2853483T3 (es) * 2013-03-15 2021-09-16 Verseon Int Corporation Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa
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
RU2685230C2 (ru) 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
SG11201701940UA (en) * 2014-09-17 2017-04-27 Verseon Corp Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Also Published As

Publication number Publication date
BR112017004704A2 (pt) 2018-01-23
KR20170048410A (ko) 2017-05-08
SG11201701940UA (en) 2017-04-27
AU2020202167A1 (en) 2020-04-30
AU2015317522A1 (en) 2017-03-23
US20190359586A1 (en) 2019-11-28
JP2017528486A (ja) 2017-09-28
CA2960790A1 (en) 2016-03-24
EP3194369A4 (en) 2018-02-28
MX2017003624A (es) 2017-07-13
IL250965A0 (en) 2017-04-30
WO2016044662A1 (en) 2016-03-24
JP2020143112A (ja) 2020-09-10
US10189810B2 (en) 2019-01-29
CN106687445A (zh) 2017-05-17
RU2017112739A (ru) 2018-10-17
RU2017112739A3 (enExample) 2019-04-01
EP3194369A1 (en) 2017-07-26
US20170267656A1 (en) 2017-09-21

Similar Documents

Publication Publication Date Title
IL282103B1 (en) Furinones as ubiquitin-specific protease 1 inhibitors
ZA201701799B (en) Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
IL250709A0 (en) Aminopyrimidines and their use to inhibit jak
ZA201608847B (en) Beta-lactamase inhibitors
IL246555A0 (en) Indazole compounds as irak4 inhibitors
DK3212780T3 (da) Serinprotease
IL246785A0 (en) Benzimidazole-2-amines as midh1 inhibitors
GB201421083D0 (en) Enzyme inhibitors
IL253876A0 (en) Converted pyrazole compounds as serine protease inhibitors
GB201421088D0 (en) New enzyme inhibitors
DK3212662T3 (da) Serinproteaser
DK3212781T3 (da) Serinproteaser
GB201416446D0 (en) New enzyme inhibitor compounds
IL251780A0 (en) New compounds as nik inhibitors
GB201421085D0 (en) New enzyme inhibitors
GB201403536D0 (en) Inhibitor compounds
PL3097084T3 (pl) Nowe inhibitory kalikreiny 7
ZA201702755B (en) Heterocyclic amphoteric compounds as surfactants
EP3113780A4 (en) Hiv protease inhibitors
EP3186271A4 (en) Azaindoline compounds as granzyme b inhibitors
HK1235061A1 (en) Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
GB201401792D0 (en) Beta-lactam compounds