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MX2017003624A - Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas. - Google Patents

Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.

Info

Publication number
MX2017003624A
MX2017003624A MX2017003624A MX2017003624A MX2017003624A MX 2017003624 A MX2017003624 A MX 2017003624A MX 2017003624 A MX2017003624 A MX 2017003624A MX 2017003624 A MX2017003624 A MX 2017003624A MX 2017003624 A MX2017003624 A MX 2017003624A
Authority
MX
Mexico
Prior art keywords
pyrazolyl
pyridone compounds
protease inhibitors
serine protease
substituted pyridone
Prior art date
Application number
MX2017003624A
Other languages
English (en)
Inventor
Kevin Michael Short
Son Minh Pham
David Ben Kita
De Los Angeles Estiarte-Martinez Maria
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 MX2017003624A publication Critical patent/MX2017003624A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)

Abstract

Se proporcionan, entre otros, compuestos de piridona sustituida con pirazolilo, que exhiben actividad biológica, por ejemplo, acción inhibidora, contra serina proteasas, que incluyen trombina y diversas calicreínas; adicionalmente, se proporcionan composiciones farmacéuticas; además, se proporcionan métodos para tratar y prevenir algunas enfermedades y trastornos, en donde la enfermedad o el trastorno pueden responder al tratamiento o a la prevención mediante la inhibición de serina proteasas, que incluyen trombina y diversas calicreínas.
MX2017003624A 2014-09-17 2015-09-17 Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas. MX2017003624A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462051511P 2014-09-17 2014-09-17
US201462051585P 2014-09-17 2014-09-17
PCT/US2015/050809 WO2016044662A1 (en) 2014-09-17 2015-09-17 Pyrazolyl-substituted pyridone compounds as serine protease inhibitors

Publications (1)

Publication Number Publication Date
MX2017003624A true MX2017003624A (es) 2017-07-13

Family

ID=55533876

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017003624A MX2017003624A (es) 2014-09-17 2015-09-17 Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.

Country Status (14)

Country Link
US (2) US10189810B2 (es)
EP (1) EP3194369A4 (es)
JP (2) JP2017528486A (es)
KR (1) KR20170048410A (es)
CN (1) CN106687445A (es)
AU (2) AU2015317522A1 (es)
BR (1) BR112017004704A2 (es)
CA (1) CA2960790A1 (es)
IL (1) IL250965A0 (es)
MX (1) MX2017003624A (es)
RU (1) RU2017112739A (es)
SG (1) SG11201701940UA (es)
WO (1) WO2016044662A1 (es)
ZA (1) ZA201701799B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2702182T3 (es) * 2013-03-15 2019-02-27 Verseon Corp Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa
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
BR112017004704A2 (pt) * 2014-09-17 2018-01-23 Verseon Corp composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio em um indivíduo
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
US11179399B2 (en) 2016-02-19 2021-11-23 Sprint Bioscience Ab 6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes
CA3015045A1 (en) 2016-02-19 2017-08-24 Sprint Bioscience Ab 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
CN106008362B (zh) * 2016-05-24 2018-08-10 杰达维（上海）医药科技发展有限公司 一种嘧啶衍生物的制备方法
HRP20201131T1 (hr) 2016-05-31 2020-10-30 Kalvista Pharmaceuticals Limited Derivati pirazola kao inhibitori kalikreina plazme
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
EP3575286B1 (en) * 2017-01-26 2022-05-11 Mitsui Chemicals Agro, Inc. Pyridone compound and bactericide for agricultural and horticultural use, which uses said compound as active ingredient
US10617680B2 (en) * 2017-04-18 2020-04-14 Celgene Quanticel Research, Inc. Therapeutic compounds
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
CN110386932A (zh) 2018-04-20 2019-10-29 艾科思莱德制药公司 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂
CN113164765A (zh) 2018-07-13 2021-07-23 维颂国际公司 凝血酶抑制剂、制剂及其用途
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN110467601B (zh) * 2019-08-29 2021-07-02 杭州市西溪医院 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität
BR102020009679A2 (pt) 2020-05-14 2021-11-23 Fundação Universidade Federal Do Abc - Ufabc Anticorpos recombinantes humanos para inibição da calicreína tecidual humana 7 (klk7) e uso em doenças relacionadas ao processo de descamação da pele
WO2022115562A1 (en) 2020-11-25 2022-06-02 Deciphera Pharmaceuticals, Llc Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE627394A (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
IL82542A0 (en) 1986-05-23 1987-11-30 Smithkline Beckman Corp Triazole derivatives,their preparation and pharmaceutical compositions containing them
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
EP0495421B1 (en) 1991-01-15 1996-08-21 Alcon Laboratories, 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 (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
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
ATE233245T1 (de) 1993-11-30 2003-03-15 Searle & Co Substituierte pyrazolyl-benzolsulfonamide und ihre verwendung als cyclooxygenaseii inhibitoren
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
JPH10509708A (ja) 1994-11-10 1998-09-22 コア セラピューティクス，インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
US5733955A (en) 1995-02-10 1998-03-31 The Goodyear Tire & Rubber Company Asphalt cement modification
JP3663522B2 (ja) 1995-08-12 2005-06-22 日本農薬株式会社 植物生育調節用組成物及びその使用方法
US5756529A (en) 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
US5739083A (en) 1995-10-13 1998-04-14 Otsuka Kagaku Kabushiki Kaisha Pyrazole derivatives and insecticidal compositions containing the derivative as active component
US5792761A (en) 1996-08-12 1998-08-11 Merck & Co., Inc. Thrombin inhibitors
DE19632773A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
GB9622370D0 (en) 1996-10-28 1997-01-08 Merck Sharp & Dohme Therapeutic agents
US5869500A (en) 1996-12-13 1999-02-09 Hoffmann-La Roche Inc. Pyridone compounds useful in treating Alzheimer's disease
EP0946508B1 (en) 1996-12-23 2009-09-23 Bristol-Myers Squibb Pharma Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
AR012117A1 (es) * 1997-03-21 2000-09-27 Novartis Ag Compuestos herbicidas, proceso para su preparacion, compuestos intermediarios para su exclusivo uso en dicho proceso, composicion herbicidae inhibidora del crecimiento de las plantas, metodo para controlar el crecimiento indeseado de plantas y uso de dicha composicion en el control de
JP2003519081A (ja) 1998-08-11 2003-06-17 バイエルクロップサイエンス株式会社 殺線虫性及び駆虫性ピラゾール類
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.
WO2000071536A1 (en) 1999-05-20 2000-11-30 E.I. Du Pont De Nemours And Company Heteroaryloxypyrimidine insecticides and acaricides
BR0013143A (pt) 1999-08-12 2002-06-11 Pharmacia Italia Spa Derivados de 3 (5) amino pirazol, processo para sua preparação e uso dos mesmos como agentes antitumorais
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
NZ517828A (en) 1999-09-17 2003-10-31 Millennium Pharm Inc Inhibitors having activity against mammalian factor Xa
CA2390113A1 (en) 1999-12-02 2001-06-07 Maurizio Schwarzenbach Aminoheterocyclylamides as pesticides and antiparasitic agents
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
US6589997B2 (en) 2001-06-29 2003-07-08 North Shore-Long Island Jewish Health System Small-molecule modulators of hepatocyte growth factor/scatter factor activities
SI21097A (sl) 2001-12-04 2003-06-30 Univerza V Ljubljani Inhibitorji trombina
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
TW200812986A (en) 2002-08-09 2008-03-16 Nps Pharma Inc New compounds
AU2003274025A1 (en) * 2002-10-17 2004-05-04 Syngenta Participations Ag Pyridine derivatives useful as herbicides
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
JP4585448B2 (ja) 2002-12-23 2010-11-24 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 第Ｘａ因子阻害剤としてのピラゾール−誘導体
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
BRPI0409949A (pt) 2003-05-01 2006-04-25 Bristol Myers Squibb Co compostos de pirazol amida aril-substituìda úteis como inibidores de cinase
DE602004016992D1 (de) 2003-05-02 2008-11-20 Elan Pharm Inc 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3-carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen
EP1479679A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
US7223780B2 (en) 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
US20050065144A1 (en) * 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
US20060281803A1 (en) 2003-09-23 2006-12-14 Lindsley Craig W 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
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
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
EP1960367A2 (en) 2005-12-05 2008-08-27 Boehringer Ingelheim International GmbH Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
CN101484438A (zh) 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 吡唑衍生物及其作为p13k抑制剂的用途
EP2035005A4 (en) 2006-06-09 2011-07-06 Kemia Inc THERAPY BASED ON 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
US7625944B2 (en) 2006-07-31 2009-12-01 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
US20100144793A1 (en) 2006-11-24 2010-06-10 Ac Immune Sa Novel 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
RU2010108325A (ru) 2007-08-06 2011-09-20 Дайниппон Сумитомо Фарма Ко., Лтд. (Jp) Амидное производное аминопиразола
WO2009041447A1 (ja) 2007-09-28 2009-04-02 Takeda Pharmaceutical Company Limited 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
EP2732819B1 (en) 2008-02-07 2019-10-16 Massachusetts Eye & Ear Infirmary Compounds that enhance Atoh-1 expression
CA2724413C (en) 2008-05-15 2016-10-18 Duke University 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
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
CN102186809A (zh) 2008-08-14 2011-09-14 拜尔农作物科学股份公司 杀虫性的4-苯基-1h-吡唑
BRPI0917507A2 (pt) 2008-08-19 2015-11-17 Boehring Ingelheim Internat Gmbh dabigatrana para a caterização cardíaca percutânea intervencionista
US20110306640A1 (en) 2008-08-19 2011-12-15 Boehringer Ingelheim International Gmbh Dabigatran in tumour therapy
US20110190352A1 (en) 2008-08-19 2011-08-04 Boehringer Ingelheim International Gmbh Use of dabigatranetexilate for treating patients with pulmonary hypertension
BRPI1011192A2 (pt) 2009-05-07 2016-03-15 Gruenenthal Gmbh derivados de carboxamida e ureia aromáticas substituídas como ligantes de receptor de vaniloide, composição farmacêutica, uso e processo para preparação dos referidos derivados
SG10201502484SA (en) * 2010-03-30 2015-05-28 Verseon Corp 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
DK2585467T3 (en) 2010-06-24 2016-06-13 Gilead Sciences Inc PYRAZOLO [1,5-A] PYRIMIDINES AND TRIAZINES AS ANTIVIRAL AGENTS
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
UA113501C2 (xx) 2010-11-03 2017-02-10 Пестицидні композиції і пов'язані з ними способи
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
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2012154880A1 (en) 2011-05-09 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases
CA2836474A1 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
WO2013039985A2 (en) 2011-09-12 2013-03-21 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
US9139564B2 (en) * 2011-12-27 2015-09-22 Ironwood Pharmaceuticals, Inc. 2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators
EP2807157A1 (en) 2012-01-27 2014-12-03 Novartis AG 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
CN104781257A (zh) 2012-06-14 2015-07-15 第一三共株式会社 哌啶基吡唑并吡啶衍生物
CN104918934B (zh) 2013-01-18 2017-12-22 霍夫曼-拉罗奇有限公司 3‑取代的吡唑及其作为dlk抑制剂的用途
ES2702182T3 (es) * 2013-03-15 2019-02-27 Verseon Corp Compuestos aromáticos multisustituidos como inhibidores de la serina proteasa
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
SMT202400446T1 (it) 2014-02-06 2024-11-15 Nxera Pharma Uk Ltd Composti aza biciclici come agonisti del recettore muscarinico
BR112017004704A2 (pt) * 2014-09-17 2018-01-23 Verseon Corp composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio em um indivíduo

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