JP2017528486A - セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 - Google Patents

セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 Download PDF

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JP2017528486A
JP2017528486A JP2017514899A JP2017514899A JP2017528486A JP 2017528486 A JP2017528486 A JP 2017528486A JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017514899 A JP2017514899 A JP 2017514899A JP 2017528486 A JP2017528486 A JP 2017528486A
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substituted
unsubstituted
compound
mmol
aryl
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JP2017528486A5 (enExample
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マイケル ショート，ケヴィン
マイケル ショート，ケヴィン
ベン キタ，デイヴィッド
ベン キタ，デイヴィッド
デ ロサンゼルス エスティアーテ−マーティネズ，マリア
デ ロサンゼルス エスティアーテ−マーティネズ，マリア
ミン ファム，サン
ミン ファム，サン
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ヴァーセオン コーポレイション
ヴァーセオン コーポレイション
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Publication of JP2017528486A5 publication Critical patent/JP2017528486A5/ja
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    • 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

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  • 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)
JP2017514899A 2014-09-17 2015-09-17 セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物 Pending JP2017528486A (ja)

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

Related Child Applications (1)

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JP2020087253A Division JP2020143112A (ja) 2014-09-17 2020-05-19 セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物

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JP2017528486A true JP2017528486A (ja) 2017-09-28
JP2017528486A5 JP2017528486A5 (enExample) 2018-11-01

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JP2017514899A Pending JP2017528486A (ja) 2014-09-17 2015-09-17 セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
JP2020087253A Pending JP2020143112A (ja) 2014-09-17 2020-05-19 セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物

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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)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020143112A (ja) * 2014-09-17 2020-09-10 ヴァーセオン コーポレイション セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
JP2021531338A (ja) * 2018-07-13 2021-11-18 ヴァーセオン インターナショナル コーポレイション トロンビン阻害薬、製剤、及びそれらの使用

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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
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
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

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