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MX2020004183A - Compuestos aromaticos multisustituidos como inhibidores de serina proteasa. - Google Patents

Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.

Info

Publication number
MX2020004183A
MX2020004183A MX2020004183A MX2020004183A MX2020004183A MX 2020004183 A MX2020004183 A MX 2020004183A MX 2020004183 A MX2020004183 A MX 2020004183A MX 2020004183 A MX2020004183 A MX 2020004183A MX 2020004183 A MX2020004183 A MX 2020004183A
Authority
MX
Mexico
Prior art keywords
aromatic compounds
protease inhibitors
serine protease
multisubstituted aromatic
kallikrein
Prior art date
Application number
MX2020004183A
Other languages
English (en)
Inventor
Son Minh Pham
Kevin Michael Short
David Charles Williams
David Ben Kita
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 MX2020004183A publication Critical patent/MX2020004183A/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Se proporcionan, entre otras cosas, compuestos aromáticos multisustituidos útiles para la inhibición de calicreína, los cuales incluyen pirazolilo sustituido o triazolilo sustituido; se proporcionan además composiciones farmacéuticas; se proporcionan además métodos para tratar y prevenir determinadas enfermedades o trastornos, los cuales son susceptibles al tratamiento o la prevención mediante la inhibición de calicreína.
MX2020004183A 2013-03-15 2015-09-14 Compuestos aromaticos multisustituidos como inhibidores de serina proteasa. MX2020004183A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361789358P 2013-03-15 2013-03-15

Publications (1)

Publication Number Publication Date
MX2020004183A true MX2020004183A (es) 2020-08-03

Family

ID=51538152

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2015012867A MX373964B (es) 2013-03-15 2014-03-17 Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.
MX2020004183A MX2020004183A (es) 2013-03-15 2015-09-14 Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2015012867A MX373964B (es) 2013-03-15 2014-03-17 Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.

Country Status (25)

Country Link
US (5) US9533970B2 (es)
EP (2) EP2968297B1 (es)
JP (3) JP6388634B2 (es)
KR (1) KR20150132148A (es)
CN (5) CN110101700A (es)
AU (5) AU2014232308B2 (es)
BR (1) BR112015022340A2 (es)
CA (2) CA2901637C (es)
DK (1) DK2968297T3 (es)
ES (2) ES2702182T3 (es)
HK (1) HK1257685A1 (es)
HR (1) HRP20182081T1 (es)
HU (1) HUE042393T2 (es)
IL (2) IL240691B (es)
LT (1) LT2968297T (es)
MX (2) MX373964B (es)
NZ (1) NZ711064A (es)
PL (2) PL3421036T3 (es)
PT (1) PT2968297T (es)
RU (2) RU2678830C2 (es)
SG (2) SG11201506449QA (es)
SI (1) SI2968297T1 (es)
TR (1) TR201819092T4 (es)
WO (1) WO2014145986A1 (es)
ZA (1) ZA201506295B (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101955691B1 (ko) * 2010-03-30 2019-03-07 베르선 코포레이션 트롬빈 억제제로서의 다중치환된 방향족 화합물
CA2901637C (en) * 2013-03-15 2019-09-24 Kevin Michael Short Multisubstituted aromatic compounds as serine protease inhibitors
SG10201707486XA (en) 2013-03-15 2017-10-30 Verseon Corp Halogenopyrazoles as inhibitors of thrombin
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
CN106659159A (zh) 2014-08-29 2017-05-10 杜邦公司 除草三唑
MX2017003624A (es) * 2014-09-17 2017-07-13 Verseon Corp Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.
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
AR103742A1 (es) * 2015-02-25 2017-05-31 Hoffmann La Roche Derivados de trifluorometilpropanamida
LT3261639T (lt) 2015-02-27 2022-11-25 Verseon International Corporation Pakaitiniai pirazolo junginiai kaip serino proteazės inhibitoriai
CN105218545A (zh) * 2015-11-04 2016-01-06 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法、用途
CN106518880B (zh) * 2015-11-04 2018-10-19 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法与用途
WO2017083433A1 (en) * 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
WO2017152842A1 (en) * 2016-03-10 2017-09-14 National Institute Of Biological Sciences, Beijing Kinase inhibitors
ME03794B (me) 2016-05-31 2021-04-20 Kalvista Pharmaceuticals Ltd Derivati pirazola kao inhibitori kalikreina plazme
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
DK3716952T3 (da) 2017-11-29 2022-03-14 Kalvista Pharmaceuticals Ltd Doseringsformer omfattende en plasmakallikrein-inhibitor
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
MX2021000472A (es) * 2018-07-13 2021-06-23 Verseon Int Corporation Inhibidores de trombina, formulaciones y usos de estos.
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CA3133803A1 (en) 2019-04-11 2020-10-15 Angion Biomedica Corp. Solid forms of (e)-3-[2-(2-thienyl)vinyl]-1h-pyrazole
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
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
US20250034112A1 (en) * 2021-10-13 2025-01-30 Yale University Improved selective jak2 inhibitors and methods of use

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE627393A (es) 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
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
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
ES2180233T3 (es) 1993-11-30 2003-02-01 Searle & Co Pirazolil bencenosulfonamidas sustituidas para uso en el tratamiento de la inflamacion.
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
US5916908A (en) 1994-11-10 1999-06-29 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
JPH1023173A (ja) 1996-07-02 1998-01-23 Nippon Telegr & Teleph Corp <Ntt> 移動体の遠隔制御システム及び遠隔制御方法
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
KR20000062284A (ko) 1996-12-23 2000-10-25 블레어 큐. 퍼거슨 인자 Xa 억제제로서의 질소 함유 헤테로방향족 화합물
JP2001518110A (ja) 1997-03-21 2001-10-09 ノバルティス アクチェンゲゼルシャフト 除草剤としてのピラゾール誘導体
KR20010071975A (ko) 1998-08-11 2001-07-31 해슬러 요세 살선충성 피라졸
KR20000047461A (ko) 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
SE9900070D0 (sv) 1999-01-13 1999-01-13 Astra Ab New use
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
AU5020400A (en) 1999-05-20 2000-12-12 E.I. Du Pont De Nemours And Company Heteroaryloxypyrimidine insecticides and acaricides
US7034049B1 (en) 1999-08-12 2006-04-25 Pharmacia Italia S.P.A. 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
HUP0203954A2 (hu) 1999-09-17 2003-03-28 Millennium Pharmaceuticals, Inc. Xa faktor inhibitorok
MXPA02005428A (es) 1999-12-02 2002-11-29 Novartis Ag Aminoheterociclilamidas como plaguicidas y agentes antiparasiticos.
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals 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
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
EP1509505A2 (en) 2002-01-23 2005-03-02 Arena Pharmaceuticals, Inc. SMALL MOLECULE MODULATORS OF THE 5&minus;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
US20040132726A1 (en) 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
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
AU2003292218A1 (en) * 2002-12-23 2004-07-14 Sanofi-Aventis 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
RU2342365C2 (ru) 2003-05-01 2008-12-27 Бристол-Маерс Сквибб Компани Арилзамещенные пиразоламиды в качестве ингибиторов киназ
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
MXPA06002853A (es) 2003-09-11 2006-06-14 Kemia Inc Inhibidores citoquina.
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
US20080188527A1 (en) * 2003-12-23 2008-08-07 Cashman John R Synthetic Compounds and Derivatives as Modulators of Smoking or Nicotine Ingestion and Lung Cancer
CA2559733C (en) 2004-03-26 2014-05-13 Methylgene Inc. Inhibitors of histone deacetylase
US7235530B2 (en) * 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
CA2594488C (en) 2005-01-10 2015-04-28 University Of Connecticut Novel heteropyrrole analogs acting on cannabinoid receptors
WO2006109846A1 (ja) 2005-04-06 2006-10-19 Takeda Pharmaceutical Company Limited トリアゾール誘導体およびその用途
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CN100427481C (zh) 2005-05-26 2008-10-22 沈阳化工研究院 一种芳基醚类化合物及其制备与应用
WO2007067836A2 (en) 2005-12-05 2007-06-14 Boehringer Ingelheim International Gmbh Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
JP2009535388A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのpi3k阻害薬としての使用
WO2007146712A2 (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
AU2007276205A1 (en) 2006-07-17 2008-01-24 Boehringer Ingelheim International Gmbh New indications for direct thrombin inhibitors in the cardiovascular field
EP2051707B1 (en) 2006-07-31 2013-07-17 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
CN101495468A (zh) * 2006-07-31 2009-07-29 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂
WO2008023235A1 (en) 2006-08-25 2008-02-28 Pfizer Products Inc. Pyrazole derivatives as anti-platelet and anti-thrombotic agents
WO2008062739A1 (en) 2006-11-20 2008-05-29 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
WO2008079277A1 (en) 2006-12-22 2008-07-03 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
US20110071289A1 (en) 2007-08-06 2011-03-24 Dainippon Sumitomo Pharma Co., Ltd. Aminopyrazole amide derivative
JP5379690B2 (ja) 2007-09-28 2013-12-25 武田薬品工業株式会社 5員複素環化合物
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
JP2011511806A (ja) 2008-02-07 2011-04-14 マサチューセッツ・アイ・アンド・イア・インファーマリー Atoh1発現を増強する化合物
CN102088973A (zh) 2008-05-15 2011-06-08 杜克大学 与热休克转录因子激活化合物及其靶标有关的组合物和方法
US8148363B2 (en) * 2008-05-19 2012-04-03 Schering Corporation Heterocyclic compounds as factor IXA inhibitors
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
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
US20110190365A1 (en) 2008-08-14 2011-08-04 Bayer Crop Science Ag Insecticidal 4-phenyl-1H-pyrazoles
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
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
DK2427436T3 (da) 2009-05-07 2013-04-02 Gruenenthal Gmbh Substituerede aromatiske carboxamid og urea derivater som vanilloidreceptorligander.
KR101955691B1 (ko) 2010-03-30 2019-03-07 베르선 코포레이션 트롬빈 억제제로서의 다중치환된 방향족 화합물
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
ES2571334T3 (es) 2010-06-24 2016-05-24 Gilead Sciences Inc Pirazolo[1,5-a]pirimidinas y -triazinas como agentes antivirales
EP2604602A4 (en) 2010-08-11 2013-12-18 Taisho Pharmaceutical Co Ltd HETEROARYL PYRAZOLE DERIVATIVE
BR122014017503B8 (pt) 2010-11-03 2022-10-11 Dow Agrosciences Llc Moléculas pesticidas
WO2012065019A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
EP2688872A4 (en) 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES
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
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
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
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
WO2013187462A1 (ja) 2012-06-14 2013-12-19 第一三共株式会社 ピペリジニルピラゾロピリジン誘導体
TWI498325B (zh) 2013-01-18 2015-09-01 Hoffmann La Roche 3-取代吡唑及其用途
SG10201707486XA (en) 2013-03-15 2017-10-30 Verseon Corp Halogenopyrazoles as inhibitors of thrombin
CA2901637C (en) 2013-03-15 2019-09-24 Kevin Michael Short Multisubstituted aromatic compounds as serine protease inhibitors
SMT202400446T1 (it) 2014-02-06 2024-11-15 Nxera Pharma Uk Ltd Composti aza biciclici come agonisti del recettore muscarinico
MX2017003624A (es) * 2014-09-17 2017-07-13 Verseon Corp Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.

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