CN106687445A - 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物 - Google Patents

作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物 Download PDF

Info

Publication number
CN106687445A
CN106687445A CN201580050088.0A CN201580050088A CN106687445A CN 106687445 A CN106687445 A CN 106687445A CN 201580050088 A CN201580050088 A CN 201580050088A CN 106687445 A CN106687445 A CN 106687445A
Authority
CN
China
Prior art keywords
substituted
unsubstituted
compound
equiv
aryl
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.)
Pending
Application number
CN201580050088.0A
Other languages
English (en)
Chinese (zh)
Inventor
K·M·肖特
D·B·奇塔
M·D·L·A·埃斯绨阿特-马缇内斯
S·M·帕姆
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 CN106687445A publication Critical patent/CN106687445A/zh
Pending 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
CN201580050088.0A 2014-09-17 2015-09-17 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物 Pending CN106687445A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462051585P 2014-09-17 2014-09-17
US201462051511P 2014-09-17 2014-09-17
US62/051,585 2014-09-17
US62/051,511 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
CN106687445A true CN106687445A (zh) 2017-05-17

Family

ID=55533876

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580050088.0A Pending CN106687445A (zh) 2014-09-17 2015-09-17 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物

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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110467601A (zh) * 2019-08-29 2019-11-19 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

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2678830C2 (ru) * 2013-03-15 2019-02-04 Версеон Корпорейшн Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз
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
JP2017528486A (ja) * 2014-09-17 2017-09-28 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
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
HRP20201400T1 (hr) 2016-02-19 2020-11-27 Sprint Bioscience Ab Spojevi 6-aril-4-(morfolin-4-il)-1h-piridin-2-ona korisni za liječenje karcinoma i dijabetesa
CN108884067B (zh) 2016-02-19 2021-01-08 思普瑞特生物科学公司 可用于治疗癌症和糖尿病的6-杂环基-4-吗啉-4-基吡啶-2-酮化合物
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
HUE049918T2 (hu) 2016-05-31 2020-11-30 Kalvista Pharmaceuticals Ltd Pirazol-származékok mint plazma kallikrein inhibitorok
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
US11051513B2 (en) 2017-01-26 2021-07-06 Mitsui Chemicals Agro, Inc. Pyridone compounds and agricultural and horticultural fungicides containing the same as active ingredients
TW202332436A (zh) 2017-04-18 2023-08-16 美商塞爾基因定量細胞研究公司 治療用化合物
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
LT3716952T (lt) 2017-11-29 2022-04-11 Kalvista Pharmaceuticals Limited Vaisto formos, apimančios plazmos kalikreino inhibitorių
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
IL280078B2 (en) * 2018-07-13 2024-04-01 Verseon Int 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
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007067836A2 (en) * 2005-12-05 2007-06-14 Boehringer Ingelheim International Gmbh Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
CN102918034A (zh) * 2010-03-30 2013-02-06 维颂公司 多取代芳族化合物作为凝血酶的抑制剂
WO2013101830A1 (en) * 2011-12-27 2013-07-04 Ironwood Pharmaceuticals, Inc. 2 - benzyl, 3 - (pyrimidin- 2 -yl) substituted pyrazoles useful as sgc stimulators
WO2014145986A1 (en) * 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors

Family Cites Families (114)

* 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
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
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
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
RO118291B1 (ro) 1993-11-30 2003-04-30 Searle & Co Derivati de pirazol 1,3,4,5 - tetrasubstituiti si compozitie farmaceutica care ii contine
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
WO1996014843A2 (en) 1994-11-10 1996-05-23 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
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
US5739083A (en) 1995-10-13 1998-04-14 Otsuka Kagaku Kabushiki Kaisha Pyrazole derivatives and insecticidal compositions containing the derivative as active component
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
CZ225699A3 (cs) 1996-12-23 2000-09-13 Du Pont Pharmaceuticals Company Dusíkaté heteroaromatické sloučeniny jako inhibitory faktoru Xa
US6274536B1 (en) * 1997-03-21 2001-08-14 Syngenta Crop Protection, Inc. Pyrazole derivatives as herbicides
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
HUP0203542A3 (en) 1999-08-12 2003-07-28 Upjohn Co 3(5)-amino-pyrazole derivatives, process for their preparation, their use and pharmaceutical compositions containing the same
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
HUP0203954A2 (hu) 1999-09-17 2003-03-28 Millennium Pharmaceuticals, Inc. Xa faktor inhibitorok
RU2002117428A (ru) 1999-12-02 2003-12-20 Новартис АГ (CH) Аминогетероцикламиды в качестве пестицидов и антипаразитарных агентов
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
AU2002308748A1 (en) 2001-05-16 2002-11-25 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
WO2003062206A2 (en) 2002-01-23 2003-07-31 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
JP2006506340A (ja) * 2002-08-09 2006-02-23 アストラゼネカ アクチボラグ 代謝調節型グルタミン酸受容体５のモジュレーターとしてのオキサジアゾール
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
ATE444292T1 (de) 2002-12-23 2009-10-15 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
WO2004098518A2 (en) 2003-05-01 2004-11-18 Bristol-Myers Squibb Company Pyrazole-amide compounds useful as kinase inhibitors
CA2524269A1 (en) 2003-05-02 2004-11-18 Elan Pharmaceuticals, Inc. 4- bromo - 5 - (2- chloro - benzoylamino) - 1h - pyrazole - 3 - carboxylic acid amide derivatives and related compounds as bradykinin b1 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
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
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
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
US8084451B2 (en) 2005-01-10 2011-12-27 University Of Connecticut Heteropyrrole 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
US20090118336A1 (en) 2006-05-03 2009-05-07 Laurent David Pyrazole derivatives and their use as pi3k inhibitors
AU2007257959A1 (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
BRPI0715492A2 (pt) 2006-07-17 2013-03-19 Boehringer Ingelheim Int uso de inibidores diretos de trombina
CA2658523C (en) 2006-07-31 2012-06-12 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
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
WO2008061796A2 (en) 2006-11-24 2008-05-29 Ac Immune Sa Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
EP2125778A1 (en) 2006-12-22 2009-12-02 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
EP2196459B1 (en) 2007-09-28 2016-11-02 Takeda Pharmaceutical Company Limited 5-membered heterocyclic compound
AU2008345225A1 (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
CN101990433B (zh) 2008-02-07 2014-11-05 马萨诸塞眼科耳科诊所 提高Atoh1表达的化合物
EP2300004A4 (en) 2008-05-15 2012-05-30 Univ Duke COMPOSITIONS AND METHODS RELATED TO HEAT SHOCK TRANSCRIPTION FACTOR ACTIVATING CONNECTIONS AND OBJECTS THEREFOR
CA2724430A1 (en) 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
EP2313093A4 (en) 2008-07-10 2012-03-28 Angion Biomedica Corp METHOD AND COMPOSITIONS FOR LOW-MOLECULAR MODULATORS OF THE HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
CN102186809A (zh) 2008-08-14 2011-09-14 拜尔农作物科学股份公司 杀虫性的4-苯基-1h-吡唑
BRPI0917507A2 (pt) 2008-08-19 2015-11-17 Boehring Ingelheim Internat Gmbh dabigatrana para a caterização cardíaca percutânea intervencionista
US20110306640A1 (en) 2008-08-19 2011-12-15 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
AR076753A1 (es) 2009-05-07 2011-07-06 Gruenenthal Chemie Derivados de carboxamida y urea aromaticas sustituidas como ligandos del receptor de vanilloides.
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
HUE029174T2 (hu) 2010-06-24 2017-02-28 Gilead Sciences Inc Pirazolo[1,5-A]pirimidinek és -triazinok mint antivirális szerek
JPWO2012020820A1 (ja) 2010-08-11 2013-10-28 大正製薬株式会社 ヘテロアリール−ピラゾール誘導体
BR112013010320B8 (pt) 2010-11-03 2022-10-11 Dow Agrosciences Llc Composições pesticidas.
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2012142308A1 (en) 2011-04-13 2012-10-18 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
AU2012255275B2 (en) 2011-05-17 2016-01-28 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
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
CN104781257A (zh) 2012-06-14 2015-07-15 第一三共株式会社 哌啶基吡唑并吡啶衍生物
TWI498325B (zh) 2013-01-18 2015-09-01 Hoffmann La Roche ３－取代吡唑及其用途
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
MX393637B (es) 2014-02-06 2025-03-11 Heptares Therapeutics Ltd Compuestos aza biciclicos como agonistas del receptor muscarinico m1.
JP2017528486A (ja) * 2014-09-17 2017-09-28 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007067836A2 (en) * 2005-12-05 2007-06-14 Boehringer Ingelheim International Gmbh Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
CN102918034A (zh) * 2010-03-30 2013-02-06 维颂公司 多取代芳族化合物作为凝血酶的抑制剂
WO2013101830A1 (en) * 2011-12-27 2013-07-04 Ironwood Pharmaceuticals, Inc. 2 - benzyl, 3 - (pyrimidin- 2 -yl) substituted pyrazoles useful as sgc stimulators
WO2014145986A1 (en) * 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110467601A (zh) * 2019-08-29 2019-11-19 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

Also Published As

Publication number Publication date
US20170267656A1 (en) 2017-09-21
BR112017004704A2 (pt) 2018-01-23
JP2017528486A (ja) 2017-09-28
RU2017112739A (ru) 2018-10-17
CA2960790A1 (en) 2016-03-24
AU2020202167A1 (en) 2020-04-30
KR20170048410A (ko) 2017-05-08
EP3194369A4 (en) 2018-02-28
US10189810B2 (en) 2019-01-29
MX2017003624A (es) 2017-07-13
SG11201701940UA (en) 2017-04-27
US20190359586A1 (en) 2019-11-28
WO2016044662A1 (en) 2016-03-24
RU2017112739A3 (enExample) 2019-04-01
IL250965A0 (en) 2017-04-30
ZA201701799B (en) 2019-06-26
EP3194369A1 (en) 2017-07-26
AU2015317522A1 (en) 2017-03-23
JP2020143112A (ja) 2020-09-10

Similar Documents

Publication Publication Date Title
CN106687445A (zh) 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物
JP6694458B2 (ja) セリンプロテアーゼ阻害剤としての多置換芳香族化合物
CN102918034B (zh) 多取代芳族化合物作为凝血酶的抑制剂
KR102730753B1 (ko) 피리딘아민-피리돈 및 피리미딘아민-피리돈 화합물
CN107405333A (zh) 作为丝氨酸蛋白酶抑制剂的被取代的吡唑化合物
KR20160132470A (ko) 피페리딘-다이온 유도체
HU228195B1 (hu) Pirazolo-piridin gyûrût tartalmazó laktámok és származékaik, valamint az ezeket tartalmazó Xa faktor gátlására szolgáló gyógyszerkészítmények
JP2024056742A (ja) キノリン誘導体から調製される新規な阻害剤
KR20240004634A (ko) 삼환식 유비퀴틴 특이적 프로테아제 1 억제제 및 이의 용도
CN105209440B (zh) 作为凝血酶抑制剂的卤代吡唑
EP2755952B1 (en) 5-cycloalkyl- or 5-heterocyclyl-nicotinamides
KR20010102072A (ko) 인자 ｘａ의 저해제로서의 복소환 유도체
HK40030344B (en) Pyridinamine-pyridone and pyrimidinamine-pyridone compounds
HK40030344A (en) Pyridinamine-pyridone and pyrimidinamine-pyridone compounds

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20170517