ECSP055640A - Composiciones de pirazol útiles como inhibidores de gsk-3 - Google Patents

Composiciones de pirazol útiles como inhibidores de gsk-3

Info

Publication number
ECSP055640A
ECSP055640A EC2005005640A ECSP055640A ECSP055640A EC SP055640 A ECSP055640 A EC SP055640A EC 2005005640 A EC2005005640 A EC 2005005640A EC SP055640 A ECSP055640 A EC SP055640A EC SP055640 A ECSP055640 A EC SP055640A
Authority
EC
Ecuador
Prior art keywords
inhibitors
pirazol
gsk
compositions useful
compounds
Prior art date
Application number
EC2005005640A
Other languages
English (en)
Inventor
Cornelia Jutta Forster
Larry C Park
Marion W Wannamaker
Young-Mae Yao
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of ECSP055640A publication Critical patent/ECSP055640A/es

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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)

Abstract

La presente invención proporciona un compuesto de fórmula (I) o un derivado farmacéuticamente aceptable del mismo. Estos compuestos son inhibidores de las proteínas quinasas, particularmente inhibidores proteína quinasa de mamífero GSK3. La invención también proporciona composiciones farmacéuticamente aceptables que comprenden los compuestos de la invención y los métodos de utilizar esos compuestos y composiciones en el tratamiento de los varios desórdenes mediados por proteínas quinasas.
EC2005005640A 2002-08-02 2005-03-02 Composiciones de pirazol útiles como inhibidores de gsk-3 ECSP055640A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40096702P 2002-08-02 2002-08-02

Publications (1)

Publication Number Publication Date
ECSP055640A true ECSP055640A (es) 2005-07-06

Family

ID=31495907

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005005640A ECSP055640A (es) 2002-08-02 2005-03-02 Composiciones de pirazol útiles como inhibidores de gsk-3

Country Status (25)

Country Link
US (2) US7491730B2 (es)
EP (1) EP1532145B1 (es)
JP (3) JP4733388B2 (es)
KR (1) KR20050032105A (es)
CN (2) CN1319968C (es)
AR (1) AR040773A1 (es)
AT (1) ATE339419T1 (es)
AU (2) AU2003257078B2 (es)
BR (1) BR0313176A (es)
CA (1) CA2494100C (es)
CO (1) CO5700772A2 (es)
DE (1) DE60308387T2 (es)
DK (1) DK1532145T3 (es)
EA (1) EA200500299A1 (es)
EC (1) ECSP055640A (es)
ES (1) ES2273043T3 (es)
IL (1) IL166620A (es)
MX (1) MXPA05001367A (es)
NO (1) NO20051100L (es)
NZ (2) NZ538426A (es)
PL (1) PL374967A1 (es)
PT (1) PT1532145E (es)
TW (1) TWI324157B (es)
WO (1) WO2004013140A1 (es)
ZA (1) ZA200501124B (es)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
DK1318997T3 (da) 2000-09-15 2006-09-25 Vertex Pharma Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
ATE468336T1 (de) 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
DE60308387T2 (de) 2002-08-02 2007-09-20 Vertex Pharmaceuticals Inc., Cambridge Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
WO2004072029A2 (en) 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
WO2006007864A1 (en) * 2004-07-17 2006-01-26 Max Planck Geselllschaft Zur Förderung Der Wissenschaft Treating neurodegenerative conditions
CA2579143A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2006034207A2 (en) * 2004-09-17 2006-03-30 Vanderbilt University Use of gsk3 inhibitors in combination with radiation therapies
AU2006279376B2 (en) 2005-08-18 2011-04-14 Vertex Pharmaceuticals Incoporated Pyrazine kinase inhibitors
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス，インコーポレイティド Ｐｄｅ阻害による神経新生の調節
EP2314289A1 (en) 2005-10-31 2011-04-27 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
TW200734327A (en) 2005-11-03 2007-09-16 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
KR101107800B1 (ko) 2006-10-31 2012-01-25 화이자 프로덕츠 인코포레이티드 무기질코르티코이드 수용체 길항제로서의 피라졸린 화합물
WO2008057940A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
WO2008077086A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
US8247421B2 (en) 2006-12-21 2012-08-21 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
US8802638B1 (en) 2007-01-25 2014-08-12 University Of South Florida Flavonoid treatment of glycogen synthase kinase-based disease
JP2010518014A (ja) * 2007-01-31 2010-05-27 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用な２−アミノピリジン誘導体
EP2137183B1 (en) 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
WO2008112642A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
JP2010523700A (ja) 2007-04-13 2010-07-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリミジン
CN101801959A (zh) 2007-05-02 2010-08-11 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
CN101679378A (zh) 2007-05-02 2010-03-24 沃泰克斯药物股份有限公司 用作激酶抑制剂的噻唑和吡唑
SG182187A1 (en) * 2007-06-08 2012-07-30 Abbott Gmbh & Co Kg 5-heteroaryl substituted indazoles as kinase inhibitors
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
AR067762A1 (es) * 2007-07-31 2009-10-21 Vertex Pharma Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma
KR20090031122A (ko) * 2007-09-21 2009-03-25 주식회사 중외제약 인다졸 골격을 함유하는 화합물, 이의 제조방법 및 상기화합물을 함유하는 약제학적 조성물
CN101932583A (zh) 2007-12-19 2010-12-29 沃泰克斯药物股份有限公司 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
EP2262498A2 (en) * 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
US8263547B2 (en) 2008-05-28 2012-09-11 Massachusetts Institute Of Technology DISC-1 pathway activators in the control of neurogenesis
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US9265764B2 (en) * 2009-02-27 2016-02-23 Massachusetts Institute Of Technology Uses of chemicals to modulate GSK-3 signaling for treatment of bipolar disorder and other brain disorders
KR20100101055A (ko) * 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 ｇｓｋ３ 이동 관련 질환의 치료 또는 예방용 약학적 조성물
GEAP202213376A (en) 2009-06-17 2022-02-25 Vertex Pharmaceuticals Incorporated Us Inhibitors of influenza viruses replication
WO2011059388A1 (en) * 2009-11-13 2011-05-19 Astrazeneca Ab Oxazolo[4,5-c]pyridine substituted pyrazine
US8592485B2 (en) 2010-06-17 2013-11-26 Healthpartners Research Foundation Methods and pharmaceutical compositions for treating the animal central nervous system for psychiatric disorders
KR20120063283A (ko) * 2010-12-07 2012-06-15 제일약품주식회사 신규한 피라졸로 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물
CN103492381A (zh) 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
EP2671885A1 (en) 2012-06-05 2013-12-11 Ares Trading S.A. Imidazo-oxadiazole and Imidazo-thiadiazole derivatives
US8992951B2 (en) 2013-01-09 2015-03-31 Sapna Life Sciences Corporation Formulations, procedures, methods and combinations thereof for reducing or preventing the development, or the risk of development, of neuropathology as a result of trauma
WO2014159356A1 (en) 2013-03-14 2014-10-02 The Brigham And Women's Hospital, Inc. Compositions and methods for epithelial stem cell expansion and culture
HUE052178T2 (hu) 2013-11-13 2021-04-28 Vertex Pharma Eljárások influenzavírus-replikáció inhibitorainak elõállítására
LT3068776T (lt) 2013-11-13 2019-08-12 Vertex Pharmaceuticals Incorporated Gripo virusų replikacijos inhibitoriai
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
KR101731624B1 (ko) 2014-07-01 2017-05-04 광주과학기술원 세포 리프로그래밍 유도용 조성물
IL299964A (en) 2014-09-03 2023-03-01 Massachusetts Inst Technology Preparations, systems and methods for producing hair cells in the inner ear to treat hearing loss
JP6857617B2 (ja) 2015-05-13 2021-04-14 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
JP2019506153A (ja) 2016-01-08 2019-03-07 マサチューセッツ インスティテュート オブ テクノロジー 分化した腸内分泌細胞およびインスリン産生細胞の作製
CN107151235B (zh) * 2016-03-04 2019-12-13 上海市计划生育科学研究所 噻二唑烷二酮基gsk3抑制剂在调节精子运动能力中的用途
WO2018217766A1 (en) 2017-05-22 2018-11-29 Whitehead Institute For Biomedical Research Kcc2 expression enhancing compounds and uses thereof
CN112334473B (zh) * 2018-09-14 2022-05-27 江苏恒瑞医药股份有限公司 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的晶型及制备方法
US20220133740A1 (en) 2019-02-08 2022-05-05 Frequency Therapeutics, Inc. Valproic acid compounds and wnt agonists for treating ear disorders

Family Cites Families (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) 1964-05-12 J-aminoindazole derivatives
US3935183A (en) 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
JPS58124773A (ja) * 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc ５−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
JPS59173249U (ja) 1983-05-07 1984-11-19 日本碍子株式会社 避雷器素子を内蔵したオ−プンヒユ−ズカツトアウト
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
JPH0532662A (ja) 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
DE69434721T2 (de) 1993-10-01 2006-11-09 Novartis Ag Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
KR970706813A (ko) 1994-11-10 1997-12-01 찰스 홈시 단백질 키나아제의 억제물질로서 유용한 제약용 피라졸 조성물(pharmaceutical pyrazole compositions useful as inhibitors of protein kinases)
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
CA2230896A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
JP4386967B2 (ja) 1996-07-13 2009-12-16 グラクソ、グループ、リミテッド プロテインチロシンキナーゼ阻害剤としての縮合複素環式化合物
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
WO1998014450A1 (en) 1996-10-02 1998-04-09 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
BR9712530A (pt) 1996-10-11 1999-10-19 Warner Lambert Co Inibidores de ésteres de asparato de enzima de conversão de interleucina-1beta
BR9814817A (pt) 1997-10-10 2002-01-08 Cytovia Inc Inibidores de apoptose de dipeptìdio e o uso dos mesmos
US6267952B1 (en) 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
BR9908004A (pt) 1998-02-17 2001-12-18 Tularik Inc Composto, composição e método para prevençãoou supressão de uma infecção viral
EP1076563B1 (en) 1998-03-16 2005-05-11 Cytovia, Inc. Dipeptide caspase inhibitors and the use thereof
NZ508314A (en) 1998-06-02 2004-03-26 Osi Pharm Inc Pyrrolo[2,3d]pyrimidine compositions and their use
CN1312807A (zh) * 1998-06-19 2001-09-12 希龙公司 糖元合成酶激酶3的抑制剂
CA2339188A1 (en) 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
DK1119567T3 (da) 1998-10-08 2005-07-25 Astrazeneca Ab Quinazolinderivater
WO2000021927A2 (en) * 1998-10-08 2000-04-20 Smithkline Beecham Plc Pyrrole-2,5-diones as gsk-3 inhibitors
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
AU2482700A (en) 1999-01-13 2000-08-01 Warner-Lambert Company 1-heterocycle substituted diarylamines
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
EP1185528A4 (en) 1999-06-17 2003-03-26 Shionogi Biores Corp INHIBITORS OF IL-12 PRODUCTION
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
JP2003531103A (ja) 1999-08-12 2003-10-21 バーテックス ファーマシューティカルズ インコーポレイテッド ｃ−ＪＵＮＮ−末端キナーゼ（ＪＮＫ）および他のタンパク質キナーゼの阻害剤
ATE396978T1 (de) 1999-10-07 2008-06-15 Amgen Inc Triazin-kinase-hemmer
IL149103A0 (en) 1999-11-30 2002-11-10 Pfizer Prod Inc 2,4-diaminopyrimidine compounds useful as immunosuppressants
KR100840727B1 (ko) 1999-12-02 2008-06-23 오에스아이 파마슈티컬스, 인코포레이티드 아데노신 ａ1, ａ2ａ 및 ａ3 수용체 특이 화합물 및 그의 사용방법
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
EP1200422A2 (en) 2000-02-05 2002-05-02 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
MXPA02007957A (es) 2000-02-17 2002-11-29 Amgen Inc Inhibidores de cinasas.
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
JP2004501083A (ja) * 2000-04-18 2004-01-15 アゴーロン・ファーマシューティカルズ・インコーポレイテッド プロテインキナーゼを阻害するためのピラゾール
EE200200715A (et) 2000-06-28 2004-08-16 Astrazeneca Ab Asendatud kinasoliini derivaadid ja nende kasutamine inhibiitoritena
SK2002003A3 (en) 2000-08-31 2004-04-06 Pfizer Prod Inc Pyrazole derivatives and their use as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2001290940A1 (en) 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Isoxazoles and their use as inhibitors of erk
DK1318997T3 (da) 2000-09-15 2006-09-25 Vertex Pharma Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7547702B2 (en) 2000-09-20 2009-06-16 Ortho-Mcneil Pharmaceutical, Inc. 4-amino-quinazolines
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
WO2002047690A1 (en) 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
US7105532B2 (en) * 2000-12-19 2006-09-12 Smithkline Beecham Corporation Pyrazolo[3,4-c]pyridines as gsk-3 inhibitors
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
EP1373257B9 (en) 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2002083667A2 (en) 2001-04-13 2002-10-24 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2002085909A1 (en) * 2001-04-20 2002-10-31 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
JP4316893B2 (ja) * 2001-05-16 2009-08-19 バーテックス ファーマシューティカルズ インコーポレイテッド Ｓｒｃおよび他のプロテインキナーゼのインヒビター
US6825190B2 (en) * 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
WO2003004492A1 (en) * 2001-07-03 2003-01-16 Vertex Pharmaceuticals Incorporated Isoxazolyl-pyrimidines as inhibitors of src and lck protein kinases
JP2005516005A (ja) * 2001-12-07 2005-06-02 バーテクス ファーマスーティカルズ インコーポレイテッド Ｇｓｋ−３阻害剤として有用なピリミジンベースの化合物
ATE468336T1 (de) 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
ES2289279T3 (es) 2002-03-15 2008-02-01 Vertex Pharmaceuticals Incorporated Composiciones utiles como inhibidores de proteinquinasas.
EP1485100B1 (en) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles as inhibitors of protein kinases
ATE433973T1 (de) 2002-03-15 2009-07-15 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004005283A1 (en) * 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
DE60308387T2 (de) * 2002-08-02 2007-09-20 Vertex Pharmaceuticals Inc., Cambridge Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren

Also Published As

Publication number Publication date
AU2003257078A1 (en) 2004-02-23
ES2273043T3 (es) 2007-05-01
JP2010280729A (ja) 2010-12-16
JP4733388B2 (ja) 2011-07-27
EP1532145A1 (en) 2005-05-25
CN101037438A (zh) 2007-09-19
JP2006273872A (ja) 2006-10-12
CA2494100C (en) 2011-10-11
TW200409774A (en) 2004-06-16
AU2003257078B2 (en) 2010-04-01
JP2005539012A (ja) 2005-12-22
TWI324157B (en) 2010-05-01
IL166620A0 (en) 2006-01-15
PL374967A1 (en) 2005-11-14
BR0313176A (pt) 2005-06-14
KR20050032105A (ko) 2005-04-06
MXPA05001367A (es) 2005-04-28
US20040039007A1 (en) 2004-02-26
HK1081186A1 (en) 2006-05-12
NO20051100L (no) 2005-05-02
AU2010202787A1 (en) 2010-07-22
NZ538426A (en) 2007-05-31
WO2004013140A1 (en) 2004-02-12
AR040773A1 (es) 2005-04-20
EA200500299A1 (ru) 2005-08-25
PT1532145E (pt) 2007-01-31
ATE339419T1 (de) 2006-10-15
ZA200501124B (en) 2006-10-25
IL166620A (en) 2011-04-28
US7872129B2 (en) 2011-01-18
CA2494100A1 (en) 2004-02-12
CO5700772A2 (es) 2006-11-30
DK1532145T3 (da) 2007-01-15
NZ550883A (en) 2008-06-30
DE60308387T2 (de) 2007-09-20
US7491730B2 (en) 2009-02-17
CN1681815A (zh) 2005-10-12
US20090118278A1 (en) 2009-05-07
EP1532145B1 (en) 2006-09-13
CN1319968C (zh) 2007-06-06
DE60308387D1 (de) 2006-10-26

Similar Documents

Publication Publication Date Title
ECSP055640A (es) Composiciones de pirazol útiles como inhibidores de gsk-3
NO20053470L (no) Triazolopyridaziner som proteinkinase-inhibitorer
UY29246A1 (es) Nuevos compuestos
ATE346070T1 (de) Purinderivate als kinaseinhibitoren
UY27234A1 (es) Inhibidores novedosos de tirosina cinasa
UA87153C2 (ru) Энантиомерно чистые аминогетероарильные соединения как ингибиторы протеинкиназы
BRPI0616630B8 (pt) compostos de pirazol substituídos
DE60214703D1 (de) Thiazolverbindungen, die sich als inhibitoren von proteinkinasen eignen
SE0303180D0 (sv) Novel compounds
ATE384061T1 (de) Imidazo- und thiazolopyridine als jak3-kinase- inhibitoren
NO20082026L (no) Deazapuriner som er nyttige som inhibitorer for Janus-kinaser
SE0302232D0 (sv) Novel Compounds
NO20076502L (no) Pyrrolopyridiner nyttige som inhibitorer av proteinkinase
ECSP077985A (es) Inhibidores de proteina cinasa derivados de pirrol (2,3-b) piridina
NO20075113L (no) Proteinkinaseinhibitorer
BRPI0509369A (pt) azaindóis úteis como inibidores de jak e outras proteìna cinases
SE0301372D0 (sv) Novel compounds
SV2005001973A (es) Quinolinas utiles en el tratamiento de enfermedades cardiovasculares ref. wyth0090-504 (am101500)
NO20064976L (no) Azanidoler som er nyttige som inhibitorer av rock og andre proteinkinaser
EA200501928A1 (ru) Пирролодигидроизохинолины как ингибиторы pde10
NO20072567L (no) Triazoler nyttige som proteinkinase-inhibitorer
CY1109808T1 (el) Αρυλινδενο-πυριδινες και αρυλινδενο-πυριμιδινες και η χρηση τους ως ανταγωνιστων των υποδοχεων αδενοσινης α2α
EA200601391A1 (ru) Производные хинолина для применения в качестве микобактериальных ингибиторов
UY26564A1 (es) Inhibidores del factor xa con aril - amidinas y sus derivados, y composiciones farmacéuticas que contienen los mismos
ATE419242T1 (de) Pyrrolidinylharnstoffderivate als angiogeneseinhibitoren