SG10201907699YA - Substituted pyrazole compounds as serine protease inhibitors - Google Patents
Substituted pyrazole compounds as serine protease inhibitorsInfo
- Publication number
- SG10201907699YA SG10201907699YA SG10201907699YA SG10201907699YA SG10201907699YA SG 10201907699Y A SG10201907699Y A SG 10201907699YA SG 10201907699Y A SG10201907699Y A SG 10201907699YA SG 10201907699Y A SG10201907699Y A SG 10201907699YA SG 10201907699Y A SG10201907699Y A SG 10201907699YA
- Authority
- SG
- Singapore
- Prior art keywords
- protease inhibitors
- serine protease
- substituted pyrazole
- compounds
- pyrazole compounds
- Prior art date
Links
Classifications
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Detergent Compositions (AREA)
- Cosmetics (AREA)
Abstract
OF THE DISCLOSURE SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS 5 There provided alia ultisubstituted compounds for inhibition thrombin kallikrein, compounds de pyrazolyl. are provided compositions. are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition 10 of thrombin and/or kallikrein.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562126424P | 2015-02-27 | 2015-02-27 |
Publications (1)
Publication Number | Publication Date |
---|---|
SG10201907699YA true SG10201907699YA (en) | 2019-09-27 |
Family
ID=56789853
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG10201907699YA SG10201907699YA (en) | 2015-02-27 | 2016-02-29 | Substituted pyrazole compounds as serine protease inhibitors |
SG11201706411YA SG11201706411YA (en) | 2015-02-27 | 2016-02-29 | Substituted pyrazole compounds as serine protease inhibitors |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG11201706411YA SG11201706411YA (en) | 2015-02-27 | 2016-02-29 | Substituted pyrazole compounds as serine protease inhibitors |
Country Status (22)
Country | Link |
---|---|
US (2) | US10532995B2 (en) |
EP (1) | EP3261639B1 (en) |
JP (3) | JP2018506563A (en) |
KR (1) | KR20170122767A (en) |
CN (1) | CN107405333A (en) |
AU (2) | AU2016224974B2 (en) |
BR (1) | BR112017018092A2 (en) |
CA (1) | CA2977993A1 (en) |
DK (1) | DK3261639T3 (en) |
ES (1) | ES2931460T3 (en) |
HK (1) | HK1246164A1 (en) |
HR (1) | HRP20221287T1 (en) |
HU (1) | HUE060104T2 (en) |
IL (1) | IL253876A0 (en) |
LT (1) | LT3261639T (en) |
MX (1) | MX2017011000A (en) |
PL (1) | PL3261639T3 (en) |
PT (1) | PT3261639T (en) |
RU (1) | RU2017131562A (en) |
SG (2) | SG10201907699YA (en) |
SI (1) | SI3261639T1 (en) |
WO (1) | WO2016138532A1 (en) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI636047B (en) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | Heterocyclic derivatives |
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 |
EP3355890B1 (en) | 2015-10-01 | 2021-11-10 | Biocryst Pharmaceuticals, Inc. | Human plasma kallikrein inhibitors |
US11180484B2 (en) | 2016-05-31 | 2021-11-23 | Kalvista Pharmaceuticals Limited | Pyrazole derivatives as plasma kallikrein inhibitors |
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 |
WO2019028362A1 (en) * | 2017-08-04 | 2019-02-07 | Dyax Corp. | Inhibitors of plasma kallikrein and uses thereof |
GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
RS63069B1 (en) | 2017-11-29 | 2022-04-29 | Kalvista Pharmaceuticals Ltd | Dosage forms comprising a plasma kallikrein inhibitor |
HU231206B1 (en) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepines |
IL278571B2 (en) * | 2018-05-16 | 2023-12-01 | Infex Therapeutics Ltd | Antibacterial compounds |
US11034669B2 (en) | 2018-11-30 | 2021-06-15 | 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BE627393A (en) | 1962-01-23 | |||
BE793955A (en) | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | ARYLPIPERAZINES AND THEIR PREPARATION PROCESS |
DE2409753A1 (en) | 1974-03-01 | 1975-09-11 | Basf Ag | SUBSTITUTED PYRAZOLES |
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 (en) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | LIQUID-GEL PHASE TRANSITION PHARMACEUTICAL COMPOSITION |
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 (en) | 1988-03-07 | 1996-01-31 | 三井東圧化学株式会社 | Brain edema inhibitor containing pyrazoles as the main component |
JP2784925B2 (en) | 1988-09-07 | 1998-08-13 | 日本農薬株式会社 | 3 or 5-phenylpyrazoles or salts thereof and herbicides |
DK0495421T3 (en) | 1991-01-15 | 1996-12-09 | Alcon Lab Inc | Use of carrageenans in topical ophthalmic compositions |
US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
JP3810097B2 (en) | 1993-01-15 | 2006-08-16 | 明治製菓株式会社 | Pyrrolidin-2-ylcarbonyl heterocyclic compound derivative |
US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
DK0923933T3 (en) | 1993-11-30 | 2002-10-21 | Searle & Co | Substituted pyrazolylbenzenesulfonamides for use in the treatment of inflammation |
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 |
AU700964B2 (en) | 1994-11-10 | 1999-01-14 | 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 (en) | 1995-08-12 | 2005-06-22 | 日本農薬株式会社 | Composition for controlling plant growth and method of using the same |
US5756529A (en) | 1995-09-29 | 1998-05-26 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies |
EP0802191A4 (en) | 1995-10-13 | 2001-08-01 | Otsuka Kagaku Kk | 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 (en) | 1996-08-14 | 1998-02-19 | Basf Ag | New thrombin inhibitors |
GB9622370D0 (en) | 1996-10-28 | 1997-01-08 | Merck Sharp & Dohme | Therapeutic agents |
US5869500A (en) | 1996-12-13 | 1999-02-09 | Hoffmann-La Roche Inc. | Pyridone compounds useful in treating Alzheimer's disease |
ATE443698T1 (en) | 1996-12-23 | 2009-10-15 | Bristol Myers Squibb Pharma Co | NITROGEN-CONTAINING HETEROCYCLES AS FACTOR XA INHIBITORS |
AU718048B2 (en) | 1997-03-21 | 2000-04-06 | Novartis Ag | Pyrazole derivatives as herbicides |
US6310049B1 (en) | 1998-08-11 | 2001-10-30 | Nihon Bayer Agrochem K.K. | Nematicidal pyrazoles |
KR20000047461A (en) | 1998-12-29 | 2000-07-25 | 성재갑 | Thrombin inhibitors |
SE9900070D0 (en) | 1999-01-13 | 1999-01-13 | Astra Ab | New use |
AR023510A1 (en) | 1999-04-21 | 2002-09-04 | Astrazeneca Ab | A TEAM OF PARTS, PHARMACEUTICAL FORMULATION AND USE OF A THROMBIN INHIBITOR. |
AU5020400A (en) | 1999-05-20 | 2000-12-12 | E.I. Du Pont De Nemours And Company | Heteroaryloxypyrimidine insecticides and acaricides |
AP2002002442A0 (en) | 1999-08-12 | 2002-03-31 | Pharmacia Italia Spa | 3(5)-Amino-pyrazole derivatives, process for their preparation and their preparation and their use as antitumor agents. |
US6632815B2 (en) | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
IL148698A0 (en) | 1999-09-17 | 2002-09-12 | Cor Therapeutics Inc | INHIBITORS OF FACTOR Xa |
NZ518931A (en) | 1999-12-02 | 2004-02-27 | Novartis Ag | Aminoheterocyclyamides as Pesticides and Antiparasitic Agents |
WO2002000651A2 (en) | 2000-06-27 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Factor xa inhibitors |
CA2446864C (en) | 2001-05-16 | 2011-02-15 | Vertex Pharmaceuticals Incorporated | 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 (en) | 2001-12-04 | 2003-06-30 | Univerza V Ljubljani | Thrombine inhibitors |
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 |
SE0200198D0 (en) | 2002-01-23 | 2002-01-23 | Astrazeneca Ab | New use |
JP2003313103A (en) | 2002-02-20 | 2003-11-06 | Sankyo Agro Kk | Agrochemical comprising 4-acylaminopyrazole derivative as active ingredient |
GB0214139D0 (en) | 2002-06-19 | 2002-07-31 | Glaxo Group Ltd | Chemical compounds |
DE10229070A1 (en) * | 2002-06-28 | 2004-01-15 | Merck Patent Gmbh | Phenyl derivatives 5 |
AR041508A1 (en) | 2002-08-09 | 2005-05-18 | Astra Ab | COMPOUNDS WITH ACTIVITY IN METABOTROPIC GLUTAMATE RECEPTORS |
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 |
BR0317659A (en) | 2002-12-23 | 2005-12-06 | Aventis Pharma 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 (en) | 2003-01-28 | 2004-08-19 | Sankyo Agro Kk | Amide derivative |
GB0308318D0 (en) | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
EP2385041B1 (en) | 2003-05-01 | 2013-09-18 | Bristol-Myers Squibb Company | Pyrazole-amine compounds useful as kinase inhibitors |
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 |
WO2005030751A2 (en) | 2003-09-08 | 2005-04-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
MXPA06002853A (en) | 2003-09-11 | 2006-06-14 | Kemia Inc | Cytokine inhibitors. |
WO2005030128A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
TW200526588A (en) | 2003-11-17 | 2005-08-16 | Smithkline Beecham Corp | Chemical compounds |
WO2005066162A1 (en) | 2003-12-23 | 2005-07-21 | Human Biomolecular Research Institute | Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer |
JP5319113B2 (en) | 2004-03-26 | 2013-10-16 | メチルジーン インコーポレイテッド | 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 |
JP2008526887A (en) | 2005-01-10 | 2008-07-24 | ユニバーシティ オブ コネチカット | Novel heteropyrrole analogs that act on cannabinoid receptors |
EP1867331A4 (en) | 2005-04-06 | 2009-04-08 | Takeda Pharmaceutical | Triazole derivative and the use thereof |
GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
CN100427481C (en) | 2005-05-26 | 2008-10-22 | 沈阳化工研究院 | An arylether kind compound and its preparation and application |
EP1960367A2 (en) | 2005-12-05 | 2008-08-27 | Boehringer Ingelheim International GmbH | Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors |
WO2007129052A1 (en) | 2006-05-03 | 2007-11-15 | Astrazeneca Ab | Pyrazole derivatives and their use as pi3k inhibitors |
AU2007257959A1 (en) | 2006-06-09 | 2007-12-21 | Kemia, Inc. | Therapy using cytokine inhibitors |
MX2008016523A (en) * | 2006-06-30 | 2009-01-19 | Astrazeneca Ab | Pyrimidine derivatives useful in the treatment of cancer. |
DE102006032824A1 (en) | 2006-07-14 | 2008-01-17 | Bayer Healthcare Ag | Substituted indazoles |
CA2657266A1 (en) | 2006-07-17 | 2008-01-24 | Boehringer Ingelheim International Gmbh | New indications for direct thrombin inhibitors in the cardiovascular field |
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 |
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 |
EP2125778A1 (en) | 2006-12-22 | 2009-12-02 | Millennium Pharmaceuticals, Inc. | Certain pyrazoline derivatives with kinase inhibitory activity |
UY30892A1 (en) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | AKT ACTIVITY INHIBITORS |
WO2008105383A1 (en) | 2007-02-26 | 2008-09-04 | Toray Industries, Inc. | Pyrazole derivative and use thereof for medical purposes |
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 |
JPWO2009020137A1 (en) | 2007-08-06 | 2010-11-04 | 大日本住友製薬株式会社 | Aminopyrazole amide derivatives |
KR101559597B1 (en) | 2007-09-28 | 2015-10-12 | 다케다 야쿠힌 고교 가부시키가이샤 | 5-membered heterocyclic compound |
CA2709784A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
US8658685B2 (en) | 2008-01-31 | 2014-02-25 | Activesite Pharmaceuticals, Inc. | Methods for treatment of kallikrein-related disorders |
EP2254572B1 (en) | 2008-02-07 | 2013-10-16 | Massachusetts Eye & Ear Infirmary | Compounds that enhance atoh-1 expression |
CN102088973A (en) | 2008-05-15 | 2011-06-08 | 杜克大学 | 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 (en) | 2008-07-10 | 2011-08-10 | 安吉翁生物医药有限公司 | 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 |
JP2011530548A (en) | 2008-08-14 | 2011-12-22 | バイエル・クロップサイエンス・アーゲー | Insecticidal 4-phenyl-1H-pyrazoles |
CA2734809A1 (en) | 2008-08-19 | 2010-02-25 | Boehringer Ingelheim International Gmbh | Dabigatran in tumour therapy |
WO2010020600A1 (en) | 2008-08-19 | 2010-02-25 | Boehringer Ingelheim International Gmbh | Use of dabigatranetexilate for treating patients with pulmonary hypertension |
MX2011001612A (en) | 2008-08-19 | 2011-03-04 | Boehringer Ingelheim Int | Dabigatran for percutaneous interventional cardiac catheterisation. |
US8334315B2 (en) | 2009-05-07 | 2012-12-18 | Gruenenthal Gmbh | Substituted aromatic carboxamide and urea derivatives as vanilloid receptor ligands |
CA2829790C (en) | 2010-03-30 | 2018-06-05 | Verseon Corporation | Multisubstituted aromatic compounds as inhibitors of thrombin |
CN101851207B (en) | 2010-06-11 | 2012-01-25 | 扬州康伊尔医药科技有限公司 | Antiviral compound intermediate 1-acyl-pyrazol-3-carboxylic acid and preparation method thereof |
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 |
US20130137865A1 (en) | 2010-08-11 | 2013-05-30 | Taisho Pharmaceutical Co., Ltd. | Heteroaryl-pyrazole derivative |
CN103619171B (en) | 2010-11-03 | 2015-11-25 | 陶氏益农公司 | Insect-killing composition and relative method |
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 | Amidopyrazole inhibitors of interleukin receptor-associated kinases |
US8691861B2 (en) | 2011-04-13 | 2014-04-08 | 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 |
CA2836474A1 (en) | 2011-05-17 | 2012-11-22 | Plexxikon Inc. | Kinase modulation and indications therefor |
JP2014524456A (en) * | 2011-08-25 | 2014-09-22 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | Serine / threonine PAK1 inhibitor |
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 |
EP2797915B1 (en) | 2011-12-27 | 2016-07-13 | Ironwood Pharmaceuticals, Inc. | 2-benzyl-3-(oxazole/thiazole)-5-(pyrimidin-2-yl)-1(H)-pyrazole derivatives as stimulators of the soluble guanylate cyclase (sGC) for the treatment of e.g. hypertension or heart failure |
US20140378474A1 (en) | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
ES2563861T3 (en) | 2012-06-14 | 2016-03-16 | Daiichi Sankyo Company, Limited | Piperidinylpyrazolopyridine derivative |
CN104918934B (en) * | 2013-01-18 | 2017-12-22 | 霍夫曼-拉罗奇有限公司 | The pyrazoles of 3 substitutions and its purposes as DLK inhibitor |
MX2015012867A (en) | 2013-03-15 | 2016-06-10 | Verseon Corp | Multisubstituted aromatic compounds as serine protease inhibitors. |
AU2014238478B2 (en) * | 2013-03-15 | 2018-07-19 | Verseon Corporation | Halogenopyrazoles as inhibitors of thrombin |
WO2015087995A1 (en) | 2013-12-13 | 2015-06-18 | 第一三共株式会社 | Cycloalkyl or heterocyclyl pyrazolopyridine derivative |
EP3102568B1 (en) | 2014-02-06 | 2018-06-27 | Heptares Therapeutics Limited | Bicyclic aza compounds as muscarinic m1 receptor agonists. |
EP3368529B1 (en) | 2015-10-27 | 2022-04-06 | Boehringer Ingelheim International GmbH | Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
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CN107405333A (en) | 2017-11-28 |
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SI3261639T1 (en) | 2023-01-31 |
IL253876A0 (en) | 2017-10-31 |
PL3261639T3 (en) | 2022-12-19 |
HK1246164A1 (en) | 2018-09-07 |
AU2020200016A1 (en) | 2020-02-06 |
EP3261639A4 (en) | 2018-07-04 |
US10532995B2 (en) | 2020-01-14 |
SG11201706411YA (en) | 2017-09-28 |
JP2023040150A (en) | 2023-03-22 |
JP2021020939A (en) | 2021-02-18 |
MX2017011000A (en) | 2017-10-20 |
HRP20221287T1 (en) | 2023-02-03 |
EP3261639B1 (en) | 2022-08-24 |
AU2016224974B2 (en) | 2019-09-26 |
RU2017131562A (en) | 2019-03-27 |
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