HK1246164A1 - 作為絲氨酸蛋白酶抑制劑的被取代的吡唑化合物 - Google Patents

作為絲氨酸蛋白酶抑制劑的被取代的吡唑化合物

Info

Publication number
HK1246164A1
HK1246164A1 HK18105646.7A HK18105646A HK1246164A1 HK 1246164 A1 HK1246164 A1 HK 1246164A1 HK 18105646 A HK18105646 A HK 18105646A HK 1246164 A1 HK1246164 A1 HK 1246164A1
Authority
HK
Hong Kong
Prior art keywords
protease inhibitors
serine protease
pyrazole compounds
substituted pyrazole
substituted
Prior art date
Application number
HK18105646.7A
Other languages
English (en)
Inventor
Kevin Michael Short
Maria De Los Angeles Estiarte-Martinez
David Ben Kita
Timothy Philip Shiau
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 HK1246164A1 publication Critical patent/HK1246164A1/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Detergent Compositions (AREA)
  • Cosmetics (AREA)
HK18105646.7A 2015-02-27 2018-05-02 作為絲氨酸蛋白酶抑制劑的被取代的吡唑化合物 HK1246164A1 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562126424P 2015-02-27 2015-02-27
PCT/US2016/020116 WO2016138532A1 (en) 2015-02-27 2016-02-29 Substituted pyrazole compounds as serine protease inhibitors

Publications (1)

Publication Number Publication Date
HK1246164A1 true HK1246164A1 (zh) 2018-09-07

Family

ID=56789853

Family Applications (1)

Application Number Title Priority Date Filing Date
HK18105646.7A HK1246164A1 (zh) 2015-02-27 2018-05-02 作為絲氨酸蛋白酶抑制劑的被取代的吡唑化合物

Country Status (22)

Country Link
US (2) US10532995B2 (zh)
EP (1) EP3261639B1 (zh)
JP (3) JP2018506563A (zh)
KR (1) KR20170122767A (zh)
CN (1) CN107405333A (zh)
AU (2) AU2016224974B2 (zh)
BR (1) BR112017018092A2 (zh)
CA (1) CA2977993A1 (zh)
DK (1) DK3261639T3 (zh)
ES (1) ES2931460T3 (zh)
HK (1) HK1246164A1 (zh)
HR (1) HRP20221287T1 (zh)
HU (1) HUE060104T2 (zh)
IL (1) IL253876A0 (zh)
LT (1) LT3261639T (zh)
MX (1) MX2017011000A (zh)
PL (1) PL3261639T3 (zh)
PT (1) PT3261639T (zh)
RU (1) RU2017131562A (zh)
SG (2) SG11201706411YA (zh)
SI (1) SI3261639T1 (zh)
WO (1) WO2016138532A1 (zh)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
RS62807B1 (sr) 2015-10-01 2022-02-28 Biocryst Pharm Inc Inhibitori humanog kalikreina plazme
JP6884801B2 (ja) 2016-05-31 2021-06-09 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
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
WO2019028362A1 (en) 2017-08-04 2019-02-07 Dyax Corp. INHIBITORS OF PLASMATIC KALLIKREIN AND USES THEREOF
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
IL274557B1 (en) 2017-11-29 2024-05-01 Kalvista Pharmaceuticals Ltd Dosage forms containing a plasma kallikrein inhibitor
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
EP3793990B1 (en) 2018-05-16 2023-07-19 Infex Therapeutics Limited Antibacterial compounds
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
WO2023137469A2 (en) * 2022-01-13 2023-07-20 Children's Hospital Medical Center Thrombin and fibrinogen as targets for atopic dermatitis diagnosis and treatment

Family Cites Families (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE627393A (zh) 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
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
DE69212850T2 (de) 1991-01-15 1997-03-06 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
CN1061036C (zh) 1993-11-30 2001-01-24 G·D·瑟尔公司 用于治疗炎症的取代的吡唑基苯磺酰胺类化合物
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
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 (fr) 1995-10-13 1997-04-17 Otsuka Kagaku Kabushiki Kaisha Derives de pyrazole et compositions insecticides contenant de tels derives comme ingredients actifs
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
SK86699A3 (en) 1996-12-23 2000-11-07 Du Pont Pharm Co Nitrogen containing heteroaromatics as factor xa inhibitors
AU718048B2 (en) 1997-03-21 2000-04-06 Novartis Ag Pyrazole derivatives as herbicides
TR200100426T2 (tr) 1998-08-11 2001-06-21 Nihon Bayer Agrochem K.K. Nematisit pirazoller
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
CN1390206A (zh) 1999-09-17 2003-01-08 千嬉药品公司 因子Xa的抑制剂
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
EP1254135B1 (en) 1999-12-02 2004-09-15 Novartis AG Aminoheterocyclylamides as pesticides and antiparasitic agents
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
WO2002092573A2 (en) 2001-05-16 2002-11-21 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
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
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
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
EP1536790A2 (en) 2002-08-09 2005-06-08 AstraZeneca AB Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004035564A1 (en) 2002-10-17 2004-04-29 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
CA2511321A1 (en) 2002-12-23 2004-07-08 Aventis Pharma Deutschland Gmbh Pyrazole-derivatives as factor xa inhibitors
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
ES2350837T3 (es) 2003-05-01 2011-01-27 Bristol-Myers Squibb Company Compuestos de pirazol-amida sustituidos con arilo útiles como inhibidores de quinasas.
WO2004098589A1 (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
US20050065144A1 (en) 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
BRPI0414313A (pt) 2003-09-11 2006-11-07 Kemia Inc inibidores de citocinas
JP2007506741A (ja) 2003-09-23 2007-03-22 メルク　エンド　カムパニー　インコーポレーテッド 向代謝性グルタミン酸受容体のピラゾール系調節剤
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
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
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
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
MX2008016523A (es) * 2006-06-30 2009-01-19 Astrazeneca Ab Derivados de pirimidina utiles en el tratamiento de cancer.
DE102006032824A1 (de) 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
EA200900091A1 (ru) 2006-07-17 2009-06-30 Бёрингер Ингельхайм Интернациональ Гмбх Новые показания к применению прямых ингибиторов тромбина в лечении сердечно-сосудистых заболеваний
WO2008016883A2 (en) 2006-07-31 2008-02-07 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 (fr) 2006-11-20 2008-05-29 Japan Tobacco Inc. Pyrazoles et leur utilisation en tant que médicaments
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
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
US20090011833A1 (en) * 2007-07-03 2009-01-08 Seelig Jerald C Descending Qualification Community Game
GB0714129D0 (en) 2007-07-19 2007-08-29 Smithkline Beecham Corp compounds
EP2189449A4 (en) 2007-08-06 2011-10-19 Dainippon Sumitomo Pharma Co AMINOPYRAZOLE AMIDE DERIVATIVE
KR101559597B1 (ko) 2007-09-28 2015-10-12 다케다 야쿠힌 고교 가부시키가이샤 ５―원 헤테로시클릭 화합물
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2259679A4 (en) 2008-01-31 2011-09-14 Joslin Diabetes Ct METHOD FOR THE TREATMENT OF CALLIQUE CLEANING 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
CA2724413C (en) 2008-05-15 2016-10-18 Duke University Compositions and methods relating to heat shock transcription factor activating compounds and targets thereof
CN102099340A (zh) 2008-05-19 2011-06-15 先灵公司 作为因子ixa抑制剂的杂环化合物
CA2767331A1 (en) 2008-07-10 2010-01-14 Angion Biomedica Corp. Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity
TW201004941A (en) 2008-07-16 2010-02-01 Wyeth Corp Alpha7 nicotinic acetylcholine receptor inhibitors
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
JP2012500245A (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 経皮的インターベンション心臓カテーテル法のためのダビガトラン
WO2010020600A1 (en) 2008-08-19 2010-02-25 Boehringer Ingelheim International Gmbh Use of dabigatranetexilate for treating patients with pulmonary hypertension
JP2012500244A (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 腫瘍療法におけるダビガトラン
CA2758289A1 (en) 2009-05-07 2010-11-11 Gruenenthal Gmbh Substituted aromatic carboxamide and urea derivatives as vanilloid receptor ligands
WO2011126903A2 (en) 2010-03-30 2011-10-13 Verseon, Inc. 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
EP3012258B1 (en) 2010-06-24 2018-09-19 Gilead Sciences, Inc. Pharmaceutical composition comprising a pyrazolo[1,5-a]pyrimidine derivative as an antiviral agent
WO2012020820A1 (ja) 2010-08-11 2012-02-16 大正製薬株式会社 ヘテロアリール－ピラゾール誘導体
CA2816076C (en) 2010-11-03 2020-07-14 Dow Agrosciences Llc Pyridyl-pyrazolyl molecules
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
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
KR20140062079A (ko) * 2011-08-25 2014-05-22 에프. 호프만-라 로슈 아게 세린/트레오닌 pak1 억제제
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
CN104066731B (zh) 2011-12-27 2016-06-15 铁木医药有限公司 可用作sgc刺激剂的2-苄基、3-(嘧啶-2-基)取代的吡唑类
EP2807157A1 (en) 2012-01-27 2014-12-03 Novartis AG 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
CA2876382A1 (en) * 2012-06-14 2013-12-19 Daiichi Sankyo Company, Limited Piperidinylpyrazolopyridine derivative
WO2014111496A1 (en) * 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag 3-substituted pyrazoles and use as dlk inhibitors
CN110423221A (zh) * 2013-03-15 2019-11-08 维颂公司 作为凝血酶抑制剂的卤代吡唑
NZ711064A (en) 2013-03-15 2019-06-28 Verseon Corp Pyridone-substituted pyrazolyl compounds as serine protease inhibitors
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
RS57843B1 (sr) 2014-02-06 2018-12-31 Heptares Therapeutics Ltd Biciklična aza jedinjenja kao agonisti muskarinskog receptora m1
JP6917988B2 (ja) 2015-10-27 2021-08-11 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 血漿カリクレイン阻害薬としてのヘテロアリールカルボキサミド誘導体

Also Published As

Publication number Publication date
US20200109132A1 (en) 2020-04-09
EP3261639B1 (en) 2022-08-24
SI3261639T1 (sl) 2023-01-31
AU2016224974A1 (en) 2017-08-31
KR20170122767A (ko) 2017-11-06
IL253876A0 (en) 2017-10-31
JP2021020939A (ja) 2021-02-18
AU2020200016A1 (en) 2020-02-06
MX2017011000A (es) 2017-10-20
LT3261639T (lt) 2022-11-25
RU2017131562A3 (zh) 2019-07-24
WO2016138532A1 (en) 2016-09-01
US20180237421A1 (en) 2018-08-23
US10532995B2 (en) 2020-01-14
HRP20221287T1 (hr) 2023-02-03
PT3261639T (pt) 2022-11-25
HUE060104T2 (hu) 2023-01-28
EP3261639A1 (en) 2018-01-03
SG10201907699YA (en) 2019-09-27
AU2016224974B2 (en) 2019-09-26
RU2017131562A (ru) 2019-03-27
DK3261639T3 (da) 2022-10-31
CA2977993A1 (en) 2016-09-01
SG11201706411YA (en) 2017-09-28
PL3261639T3 (pl) 2022-12-19
BR112017018092A2 (pt) 2018-04-10
ES2931460T3 (es) 2022-12-29
CN107405333A (zh) 2017-11-28
JP2023040150A (ja) 2023-03-22
EP3261639A4 (en) 2018-07-04
JP2018506563A (ja) 2018-03-08

Similar Documents

Publication Publication Date Title
HK1246164A1 (zh) 作為絲氨酸蛋白酶抑制劑的被取代的吡唑化合物
IL282103B1 (en) Furinones as ubiquitin-specific protease 1 inhibitors
HK1249905A1 (zh) 作為lsd1抑制劑的雜環化合物
ZA201808639B (en) Pyrazole derivatives as plasma kallikrein inhibitors
HK1244268A1 (zh) 作爲血漿激肽釋放酶抑制劑的n-((雜)芳基甲基)雜芳基甲酰胺化合物
ZA201701799B (en) Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
HK1231411A1 (zh) 作為 抑制劑的取代的吲唑化合物
HK1231480A1 (zh) 作為 抑制劑的吲唑化合物
HK1248222A1 (zh) 噻吩並嘧啶酮作為泛素特異性蛋白酶7抑制劑
PT3371190T (pt) Compostos heterocíclicos como inibidores de pi3k-gamma
GB201513481D0 (en) Inhibitor compounds
GB201505658D0 (en) Inhibitor compounds
GB201522453D0 (en) Inhibitor compounds
GB201500644D0 (en) Inhibitor compounds