CN101421265A - 作为蛋白激酶b(pkb)抑制剂的噻唑化合物 - Google Patents

作为蛋白激酶b(pkb)抑制剂的噻唑化合物 Download PDF

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Publication number
CN101421265A
CN101421265A CNA2007800097081A CN200780009708A CN101421265A CN 101421265 A CN101421265 A CN 101421265A CN A2007800097081 A CNA2007800097081 A CN A2007800097081A CN 200780009708 A CN200780009708 A CN 200780009708A CN 101421265 A CN101421265 A CN 101421265A
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CN
China
Prior art keywords
amino
thiazole
phenyl
alkyl
propyl group
Prior art date
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Pending
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CNA2007800097081A
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English (en)
Chinese (zh)
Inventor
曾庆平
J·G·艾伦
M·P·布尔博
C·多明格斯
C·H·富特施
韩念和
洪凡超
黄昕
M·R·李
李爱文
刘庆艳
J·T·赖德
S·塔德斯
A·S·塔斯克
V·N·维斯瓦纳汉
王向红
K·E·维勒
G·E·沃尔希特
姚国民
原晨光
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Amgen Inc
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Amgen Inc
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Publication of CN101421265A publication Critical patent/CN101421265A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
CNA2007800097081A 2006-01-18 2007-01-11 作为蛋白激酶b(pkb)抑制剂的噻唑化合物 Pending CN101421265A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75954606P 2006-01-18 2006-01-18
US60/759,546 2006-01-18

Publications (1)

Publication Number Publication Date
CN101421265A true CN101421265A (zh) 2009-04-29

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KR (1) KR20080091369A (US08084479-20111227-C00115.png)
CN (1) CN101421265A (US08084479-20111227-C00115.png)
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AU (1) AU2007207743B2 (US08084479-20111227-C00115.png)
BR (1) BRPI0706621A2 (US08084479-20111227-C00115.png)
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Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102548990A (zh) * 2009-06-10 2012-07-04 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶抑制剂
CN102647908A (zh) * 2009-10-08 2012-08-22 葛兰素史密斯克莱有限责任公司 组合
CN102665418A (zh) * 2009-10-08 2012-09-12 葛兰素史密斯克莱有限责任公司 组合
CN102665720A (zh) * 2009-10-12 2012-09-12 葛兰素史密斯克莱有限责任公司 组合
CN103304468A (zh) * 2012-03-13 2013-09-18 华东师范大学 一种氧化吲哚的一锅法串联合成方法
CN114014787A (zh) * 2022-01-10 2022-02-08 苏州开元民生科技股份有限公司 一种制备(2s,3r)-对甲砜基苯丝氨酸乙酯的不对称合成方法
CN114391012A (zh) * 2019-08-02 2022-04-22 美国安进公司 作为kif18a抑制剂的吡啶衍生物
CN116813608A (zh) * 2023-06-08 2023-09-29 英矽智能科技(上海)有限公司 噻唑类化合物及其应用

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA012181B1 (ru) 2004-10-18 2009-08-28 Амген, Инк. Соединения тиадиазола и их применение
BRPI0706621A2 (pt) 2006-01-18 2011-04-05 Amgen Inc composto, composição farmacêutica, métodos para tratar um distúrbio mediado por quinase em um mamìfero e para tratar um distúrbio relacionado com a proliferação em um mamìfero, e , uso do composto
RU2009134059A (ru) 2007-02-13 2011-03-20 Шеринг Корпорейшн (US) Функционально селективные агонисты альфа2с адренорецептора
WO2009011871A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
CA2692713A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
UA103319C2 (en) * 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
US20110092423A1 (en) * 2008-06-26 2011-04-21 GlaxoSmithKline, LLC INHIBITORS OF Akt ACTIVITY
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
PE20110368A1 (es) * 2008-08-18 2011-06-13 Univ Yale Moduladores de mif
DK2356109T3 (en) * 2008-10-10 2017-03-13 Vm Discovery Inc COMPOSITIONS AND PROCEDURES FOR TREATING DISEASES IN CONNECTION WITH ALCOHOL CONSUMPTION, Pain and OTHER DISEASES
JP5770102B2 (ja) * 2008-12-19 2015-08-26 ジェネンテック, インコーポレイテッド 複素環化合物と使用方法
WO2010083246A1 (en) * 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
RS56352B2 (sr) 2009-06-25 2023-02-28 Alkermes Pharma Ireland Ltd Heterociklična jedinjenja za lečenje neuroloških i psiholoških poremećaja
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
MY173795A (en) 2009-11-05 2020-02-24 Incozen Therapeutics Pvt Ltd Novel benzopyran kinase modulators
WO2011115071A1 (ja) * 2010-03-15 2011-09-22 国立大学法人広島大学 チエノピリジン誘導体及びその製造方法、並びにそれを用いた有機半導体デバイス
JP5578705B2 (ja) * 2010-03-29 2014-08-27 公益財団法人相模中央化学研究所 (アリール)ジフルオロ酢酸エステル誘導体及びその製造方法
US8383623B2 (en) * 2010-04-16 2013-02-26 Abbott Laboratories Phthalazin-(2H)-one inhibitors of kinases
WO2011130921A1 (en) * 2010-04-23 2011-10-27 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US20130102605A1 (en) * 2010-04-23 2013-04-25 Peng Liang Inhibitors of akt activity
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
SI2705029T1 (sl) 2011-05-04 2019-03-29 Rhizen Pharmaceuticals S.A. Nove spojine kot modulatori protein-kinaz
JP6093770B2 (ja) 2011-09-27 2017-03-08 アムジエン・インコーポレーテツド 癌の治療のためのmdm2阻害剤としての複素環化合物
US9499533B2 (en) 2012-03-27 2016-11-22 Shionogi & Co., Ltd. Aromatic 5-membered heterocyclic derivative having TRPV4-Inhibiting activity
WO2013173382A1 (en) 2012-05-15 2013-11-21 Amgen Inc. Benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein
MY169987A (en) 2012-07-04 2019-06-19 Rhizen Pharmaceuticals Sa Selective pi3k delta inhibitors
WO2014130470A1 (en) 2013-02-19 2014-08-28 Amgen Inc. Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer
EP2970206A1 (en) * 2013-03-13 2016-01-20 Boston Biomedical, Inc. 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer
CA2906538C (en) 2013-03-14 2021-02-02 Ana Gonzalez Buenrostro Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
SG10201902429PA (en) 2013-11-11 2019-04-29 Amgen Inc Combination therapy including an mdm2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers
TN2017000374A1 (en) * 2015-03-02 2019-01-16 Bristol Myers Squibb Co TGF-β INHIBITORS
WO2017151409A1 (en) 2016-02-29 2017-09-08 University Of Florida Research Foundation, Incorporated Chemotherapeutic methods
EP3426652B1 (en) * 2016-03-10 2021-12-01 Astrazeneca AB Novel inhibitors of phosphatidylinositol 3-kinase gamma
MA48994A (fr) 2017-03-30 2020-02-05 Hoffmann La Roche Isoquinoléines utilisées en tant qu'inhibiteurs de hpk1
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
US11479770B2 (en) 2017-10-05 2022-10-25 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of DUX4
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
EP3761983A1 (en) 2018-03-05 2021-01-13 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
EP3788038B1 (en) 2018-05-04 2023-10-11 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11612606B2 (en) 2018-10-03 2023-03-28 Genentech, Inc. 8-aminoisoquinoline compounds and uses thereof
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CN114144414A (zh) 2019-05-21 2022-03-04 美国安进公司 固态形式
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor
CN111603466B (zh) * 2020-06-29 2022-07-22 江南大学 一种乙酮类化合物在制备治疗肿瘤药物中的应用

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3591600A (en) 1969-07-07 1971-07-06 Stauffer Chemical Co 2-aminothiazole phosphates and phosphonates
GB1435139A (en) 1972-08-17 1976-05-12 Sumitomo Chemical Co Thiazole derivatives
JPS5239827B2 (US08084479-20111227-C00115.png) 1973-11-08 1977-10-07
US4086239A (en) 1977-07-01 1978-04-25 Stauffer Chemical Company Thiazole bis-phosphates and phosphonates, intermediates, and insecticidal compositions and methods
DK150068C (da) 1978-06-02 1987-06-29 Pfizer Analogifremgangsmaade til fremstilling af aminothiazoler
US4297365A (en) * 1978-08-04 1981-10-27 Ciba-Geigy Corporation Benzimidazoles and pharmaceutical preparations containing such compounds
US4451471A (en) 1981-03-18 1984-05-29 Ciba-Geigy Corporation Certain 2,4,5-tri-substituted thiazoles, pharmaceutical compositions containing same and methods of using same
FR2511375A1 (fr) 1981-08-17 1983-02-18 Rhone Poulenc Sante Nouveaux derives de la cephalosporine, leur preparation et les medicaments qui les contiennent
DE3630732A1 (de) 1986-09-10 1988-03-17 Bayer Ag 2-cyano-2-alkoximino-acetamide
US5232921A (en) 1987-03-12 1993-08-03 Sanofi Thiazole derivatives active on the cholinergic system, process for obtention and pharmaceutical compositions
JPH0753666B2 (ja) 1987-09-14 1995-06-07 久光製薬株式会社 置換ジフェニルチアゾール誘導体からなる抗炎症剤
FR2636628B1 (fr) 1988-08-25 1990-12-28 Sanofi Sa Derives du thiadiazole-1,3,4, leur procede d'obtention et compositions pharmaceutiques en contenant
US5302608A (en) 1988-11-18 1994-04-12 Takeda Chemical Industries, Ltd. Age formation inhibitors
US5145860A (en) 1989-01-05 1992-09-08 Fujisawa Pharmaceutical Co., Ltd. Thiazole compounds and pharmaceutical composition comprising the same
US5550138A (en) 1992-03-25 1996-08-27 Takeda Chemical Industries, Ltd. Condensed thiadiazole derivative, method of its production, and use thereof
WO1996016650A1 (fr) 1994-11-29 1996-06-06 Hisamitsu Pharmaceutical Co., Inc. Antibacterien et bactericide comprenant un derive de 2-aminothiazole et sels de ce derive
FR2735777B1 (fr) * 1995-06-21 1997-09-12 Sanofi Sa Derives de 4-phenylaminothiazole, leur procede de preparation et les compositions pharmaceutiques les contenant
ES2237919T4 (es) 1998-06-18 2007-05-01 Bristol-Myers Squibb Company Inhibidores aminotiazol sustituidos con carbono de quinasas dependientes de ciclina.
US6407124B1 (en) * 1998-06-18 2002-06-18 Bristol-Myers Squibb Company Carbon substituted aminothiazole inhibitors of cyclin dependent kinases
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
AU3487500A (en) 1999-02-08 2000-08-25 Lion Bioscience Ag Thiazole derivatives and combinatorial libraries thereof
AUPP873799A0 (en) 1999-02-17 1999-03-11 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
AU6471300A (en) 1999-08-06 2001-03-05 Takeda Chemical Industries Ltd. P38map kinase inhibitors
JP2001114690A (ja) * 1999-08-06 2001-04-24 Takeda Chem Ind Ltd p38MAPキナーゼ阻害剤
EP1268474A2 (en) 2000-03-30 2003-01-02 Takeda Chemical Industries, Ltd. Substituted 1,3-thiazole compounds, their production and use
WO2001074793A2 (en) 2000-04-03 2001-10-11 3-Dimensional Pharmaceuticals, Inc. Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
US7074934B2 (en) 2000-06-13 2006-07-11 Tularik Limited Serine protease inhibitors
GT200100147A (es) 2000-07-31 2002-06-25 Derivados de imidazol
JP4689801B2 (ja) 2000-08-09 2011-05-25 ケミプロ化成株式会社 アミノチアゾール誘導体の製造方法
JP2002053566A (ja) 2000-08-11 2002-02-19 Japan Tobacco Inc チアゾール化合物及びその医薬用途
GB0114185D0 (en) 2001-06-12 2001-08-01 Protherics Molecular Design Lt Compounds
US20040097555A1 (en) 2000-12-26 2004-05-20 Shinegori Ohkawa Concomitant drugs
AR032653A1 (es) 2001-02-09 2003-11-19 Telik Inc Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos.
ATE315555T1 (de) 2001-05-11 2006-02-15 Pfizer Prod Inc Thiazolderivate und ihre verwendung als cdk- inhibitoren
CA2450400A1 (en) 2001-06-11 2002-12-19 Takeda Chemical Industries, Ltd. Medicinal compositions
AR039059A1 (es) 2001-08-06 2005-02-09 Sanofi Aventis Compuesto derivado de acilaminotiazol, su utilizacion, procedimientos para prepararlo, composicion farmaceutica que lo comprende, y compuestos intermediarios
JP4495963B2 (ja) * 2001-09-28 2010-07-07 サイクラセル リミテッド 抗増殖性化合物としてのn−(4−(4−メチルチアゾール−5−イル)ピリミジン−2−イル)−n−フェニルアミン類
GB0123589D0 (en) 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
JP2005510508A (ja) 2001-11-08 2005-04-21 藤沢薬品工業株式会社 アデノシンアンタゴニストとしてのチアゾールピリダジノン類
EP1474141A1 (en) 2002-02-13 2004-11-10 Pharmagene Laboratories Ltd 5-ht2b receptor antagonists
PE20030968A1 (es) 2002-02-28 2004-01-12 Novartis Ag Derivados de 5-feniltiazol como inhibidores de cinasas
ES2292992T3 (es) * 2002-02-28 2008-03-16 F. Hoffmann-La Roche Ag Derivados de tiazol como antagonistas del receptor npy.
US20040053948A1 (en) 2002-05-10 2004-03-18 Cytokinetics, Inc. Compounds, compositions and methods
FR2842523A1 (fr) 2002-07-17 2004-01-23 Sanofi Synthelabo Derives d'acylaminothiazole, leur preparation et leur application en therapeutique
AU2003265068A1 (en) 2002-10-09 2004-05-04 Pfizer Products Inc. Thiazole compounds for the treatment of neurodegenerative disorders
EP1558607B1 (en) * 2002-10-30 2010-05-05 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
US20050004186A1 (en) 2002-12-20 2005-01-06 Pfizer Inc MEK inhibiting compounds
FR2850380B1 (fr) 2003-01-23 2006-07-07 Sanofi Synthelabo Derives d'acylaminothiazole, leur preparation et leur utilisation en therapeutique
JP2006182648A (ja) 2003-04-08 2006-07-13 Dai Ichi Seiyaku Co Ltd 7員複素環誘導体
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
JP2007512230A (ja) * 2003-08-20 2007-05-17 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 プロテインキナーゼ阻害剤として有用な(4−アミノ−1,2,5−オキサジアゾール−4−イル)−ヘテロ芳香族化合物
CN1898221A (zh) 2003-09-06 2007-01-17 沃泰克斯药物股份有限公司 Atp-结合弹夹转运蛋白的调控剂
GB0327380D0 (en) 2003-11-25 2003-12-31 Cyclacel Ltd Method
GB0329275D0 (en) 2003-12-18 2004-01-21 Merck Sharp & Dohme Therapeutic treatment
EP1709019B1 (en) 2004-01-12 2007-08-08 Applied Research Systems ARS Holding N.V. Thiazole derivatives and use thereof
WO2005073202A1 (fr) 2004-01-16 2005-08-11 Sanofi-Aventis Derives d’acylaminothiazole et leur application comme inhibiteurs de beta-amyloide
WO2005073226A1 (fr) 2004-01-16 2005-08-11 Sanofi-Aventis Derives d’acylaminothiazole, leur preparation et leur application en therapeutique
JP2007526324A (ja) * 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Akt活性のある阻害剤
AP2379A (en) 2004-03-23 2012-03-08 Pfizer Prod Inc Imidazole compounds for the treatment of neurodegenerative disorders.
JP2007531757A (ja) 2004-03-30 2007-11-08 カイロン コーポレイション 抗癌剤としての置換チオフェン誘導体
WO2005116052A2 (en) * 2004-04-27 2005-12-08 Research Development Foundation ANTAGONISM OF TGF-β SUPERFAMILY RECEPTOR SIGNALING
AU2005245962A1 (en) 2004-05-21 2005-12-01 Mpex Pharmaceuticals, Inc. Bacterial efflux pump inhibitors and methods of treating bacterial infections
GB0411791D0 (en) 2004-05-26 2004-06-30 Cyclacel Ltd Compounds
AR050917A1 (es) 2004-08-13 2006-12-06 Amphora Discovery Corp Compuestos basados en 2-amido-tiazol que presentan actividad inhibidora de enzimas que utilizan atp, y composiciones y usos de los mismos
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
EA012181B1 (ru) 2004-10-18 2009-08-28 Амген, Инк. Соединения тиадиазола и их применение
SE0402735D0 (sv) 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
KR100917511B1 (ko) 2005-02-28 2009-09-16 니뽄 다바코 산교 가부시키가이샤 Syk 저해 활성을 갖는 신규한 아미노피리딘 화합물
CN101248041B (zh) 2005-06-17 2013-11-20 艾宝奇生物工艺有限公司 鞘氨醇激酶抑制剂
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
DE102005048072A1 (de) 2005-09-24 2007-04-05 Bayer Cropscience Ag Thiazole als Fungizide
EP1970377A4 (en) 2005-12-09 2013-02-27 Meiji Seika Kaisha LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THIS AS AN ACTIVE SUBSTANCE
BRPI0619730A2 (pt) 2005-12-12 2011-10-11 Genelabs Tech Inc compostos antivirais de n-(anel aromático de 5 membros)-amido
BRPI0706621A2 (pt) * 2006-01-18 2011-04-05 Amgen Inc composto, composição farmacêutica, métodos para tratar um distúrbio mediado por quinase em um mamìfero e para tratar um distúrbio relacionado com a proliferação em um mamìfero, e , uso do composto
CA2637565A1 (en) 2006-01-18 2007-07-26 Schering Corporation Cannibinoid receptor modulators
KR101015073B1 (ko) 2006-01-18 2011-02-16 에프. 호프만-라 로슈 아게 Mdm2 억제제로서의시스-4,5-비아릴-2-헤테로시클릭-이미다졸린
US20080242694A1 (en) 2006-09-18 2008-10-02 D Sidocky Neil R Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith

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CN116813608A (zh) * 2023-06-08 2023-09-29 英矽智能科技(上海)有限公司 噻唑类化合物及其应用
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