YU22400A - Supstituisana 4-amino-tiazol-2-i jedinjenja kao cdks inhibitori - Google Patents

Supstituisana 4-amino-tiazol-2-i jedinjenja kao cdks inhibitori

Info

Publication number
YU22400A
YU22400A YU22400A YU22400A YU22400A YU 22400 A YU22400 A YU 22400A YU 22400 A YU22400 A YU 22400A YU 22400 A YU22400 A YU 22400A YU 22400 A YU22400 A YU 22400A
Authority
YU
Yugoslavia
Prior art keywords
fused
carbocyclic
monocyclic
heterocyclic
alkyl
Prior art date
Application number
YU22400A
Other languages
English (en)
Inventor
Wesley Chong
Shao Song Chu
K. Rohit Duvadie
Lin Li
Wei Xiao
Yi Yang
Original Assignee
Agouron Pharmaceuticals Inc.
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 Agouron Pharmaceuticals Inc. filed Critical Agouron Pharmaceuticals Inc.
Publication of YU22400A publication Critical patent/YU22400A/sh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Ovaj pronalazak upucen je na jedinjenja aminotiazola sa formulom (I) u kojoj je R1 supstituisana ili nesupstituisana grupa koja je izabrana od: C1-6-alkil; C1-6-alkenil; C1-6-alkinil; C1-6-alkoksi; C1-6-alkohol; karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policiklicne, cikloalkil; karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policiklicne, aril; karbonil; etar; (C1-6-alkil)-karbonil; (C1-6-alkil)-aril; (C1-6-alkil)-cikloalkil; (C1-6-alkil)-(C1-6-alkoksi); aril-( C1-6-alkoksil); tioetar; tiol; i sulfonil; u kojoj kada je R1 supstituisan, svaki supstituent je svaki za sebe nezavisno, halgoen; haloalkil; C1-6-alkil; C1-6-alkenil; C1-6-alkinil; hidroksil; C1-6-alkoksil; amino; nitro; tiol; tioetar; imin; cijano; amido; fosfonato; fosfin; karboksil, tiokarbonil; sulfonil; sulfonamid; keton; aldehid; estar; kiseonik; karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policiklicne, cikloalkil; ili karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policiklicne; aril; i R72 je karbociklicna ili heterociklicna, monociklicna ili spojena ili nespojena policiklicna, prstenasta struktura koja ima supstituent u susednom polozaju od tacke spajanja; cija prstenasta struktura je po slobodnom izboru dalje supstituisana, gde je svaki supstituent po slobodnom izboru za R2, svaki za sebe nezavisno halogen; haloalkil; C1-6-alkil; C1-6-alkenil; C1-6-alkinil; hidroksil; C1-6-alkoksil; amino; nitro; tiol; tioetar; imin; cijano; amido;fosfonato; fosfin; karboksil; tiokarbonil; sulfonil; sulfonamid; keton; aldehid; estar; kiseonik; karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policiklicne, cikloalkil; ili karbociklicne ili heterociklicne, monociklicne ili spojene ili nespojene policikklicne; aril; ili farmaceutski prihvatljiva so od jedinjenja sa formulom (I), ili ciljni lek i farmaceutski aktivni metabolit od jedinjenja sa formulom (I) ili njegove farmaceutski prihvatljive soli, za inhibiciju ciklin zavisnih kinaza (CDKs), kao sto su CDK1, CDK2, CDK4, i CDK6. Pronalazak je takodje upucen i na terapeutsku i profilakticku upotrebufarmaceutskih kompozicija sa takvim jedinjenjima i postupcima za lecenje maligniteta i drugih poremecaja davanjem efikasne kolicine takvih jedinjenja.
YU22400A 1997-10-27 1998-10-27 Supstituisana 4-amino-tiazol-2-i jedinjenja kao cdks inhibitori YU22400A (sh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6363497P 1997-10-27 1997-10-27
US6366697P 1997-10-28 1997-10-28

Publications (1)

Publication Number Publication Date
YU22400A true YU22400A (sh) 2003-08-29

Family

ID=26743609

Family Applications (1)

Application Number Title Priority Date Filing Date
YU22400A YU22400A (sh) 1997-10-27 1998-10-27 Supstituisana 4-amino-tiazol-2-i jedinjenja kao cdks inhibitori

Country Status (34)

Country Link
US (2) US6569878B1 (sh)
EP (1) EP1056732B1 (sh)
JP (1) JP2004500304A (sh)
KR (1) KR20010082501A (sh)
CN (1) CN1158269C (sh)
AP (1) AP1445A (sh)
AT (2) ATE332896T1 (sh)
AU (1) AU738792B2 (sh)
BG (1) BG64195B1 (sh)
BR (1) BR9815200A (sh)
CA (1) CA2306082A1 (sh)
DE (2) DE69833223T2 (sh)
EA (1) EA003527B1 (sh)
EE (1) EE200000289A (sh)
ES (2) ES2267873T3 (sh)
GE (1) GEP20032896B (sh)
HR (1) HRP20000222A2 (sh)
HU (1) HUP0004512A3 (sh)
ID (1) ID24372A (sh)
IL (1) IL135574A0 (sh)
IS (1) IS5462A (sh)
LT (1) LT4855B (sh)
LV (1) LV12592B (sh)
NO (1) NO20001955L (sh)
NZ (1) NZ503788A (sh)
OA (1) OA11352A (sh)
PL (1) PL342447A1 (sh)
RO (1) RO119463B1 (sh)
SI (1) SI20324A (sh)
SK (1) SK5212000A3 (sh)
TR (1) TR200001081T2 (sh)
UA (1) UA66810C2 (sh)
WO (1) WO1999021845A2 (sh)
YU (1) YU22400A (sh)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010082501A (ko) * 1997-10-27 2001-08-30 개리 이. 프라이드만 4-아미노티아졸 유도체, 그 제조방법 및 싸이클린-의존성키나아제의 억제제로서의 이용방법
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
CN1129581C (zh) * 1998-09-22 2003-12-03 山之内制药株式会社 氰基苯基衍生物
US6414156B2 (en) 1998-10-21 2002-07-02 Bristol-Myers Squibb Company Process for preparing azacycloalkanoylaminothiazoles
US6214852B1 (en) 1998-10-21 2001-04-10 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
EP3222619A1 (en) 1999-04-15 2017-09-27 Bristol-Myers Squibb Holdings Ireland Cyclic protein tyrosine kinase inhibitors
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
PE20010306A1 (es) * 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
US7141581B2 (en) 1999-07-02 2006-11-28 Agouron Pharmaceuticals, Inc. Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
US6114365A (en) * 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
US6392053B2 (en) 1999-12-15 2002-05-21 Bristol-Myers Squibb Company Process for preparing arylacetylaminothiazoles
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
WO2001056567A1 (en) * 2000-02-04 2001-08-09 Novo Nordisk A/S 2,4-diaminothiazole derivatives and their use as glycogen synthase kinase-3 (gsk-3) inhibitors
EP1274706A1 (en) 2000-04-18 2003-01-15 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinases
KR100423899B1 (ko) * 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
WO2002012250A2 (en) * 2000-08-09 2002-02-14 Agouron Pharmaceuticals, Inc. Pyrazole-thiazole compounds, pharmaceutical compositions containing them, and methods of their use for inhibiting cyclin-dependent kinases
ES2238463T3 (es) 2000-08-18 2005-09-01 Agouron Pharmaceuticals, Inc. Hidroxiimino-fluorenos heterociclicos y uso para inhibir proteina-quinasas.
EP1712550A3 (en) * 2000-12-22 2009-07-15 Ortho-McNeil Pharmaceutical, Inc. Substituted triazole diamine derivatives as kinase inhibitors
CZ20031941A3 (cs) 2000-12-22 2004-08-18 Orthoámcneilápharmaceuticalźáinc Substituované triazol diaminové deriváty jako inhibitory kináz
US6756374B2 (en) * 2001-01-22 2004-06-29 Hoffmann-La Roche Inc. Diaminothiazoles having antiproliferative activity
ES2255621T3 (es) * 2001-06-22 2006-07-01 MERCK & CO., INC. Inhibidores de tirosina quinasa.
HN2002000156A (es) * 2001-07-06 2003-11-27 Inc Agouron Pharmaceuticals Derivados de benzamida tiazol y composiciones farmaceuticas para inhibir la proliferacion de celulas y metodos para su utilización.
EP1724270A3 (en) 2001-07-19 2007-01-03 Pfizer Italia S.r.l. Phenylacetamido-thiazole derivatives, process for their preparation and their use as antitumor agents
EP1417188A1 (en) * 2001-08-03 2004-05-12 Novo Nordisk A/S Novel 2,4-diaminothiazole derivatives
EA007395B3 (ru) 2002-01-22 2018-02-28 Уорнер-Ламберт Компани Ллс 2-(ПИРИДИН-2-ИЛАМИНО)ПИРИДО[2,3-d]ПИРИМИДИН-7-ОНЫ
US6818663B2 (en) * 2002-05-17 2004-11-16 Hoffmann-La Roches Diaminothiazoles
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
US6872724B2 (en) 2002-07-24 2005-03-29 Merck & Co., Inc. Polymorphs with tyrosine kinase activity
MXPA05000950A (es) 2002-07-25 2005-05-16 Pfizer Prod Inc Derivados de isotiazol utiles como agentes anticancerosos.
CN100381429C (zh) * 2002-08-07 2008-04-16 霍夫曼-拉罗奇有限公司 噻唑衍生物
US7157455B2 (en) 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
EP1594866A1 (en) * 2003-02-12 2005-11-16 Pfizer Inc. Antiproliferative 2-(sulfo-phenyl)-aminothiazole derivatives
WO2004074283A1 (en) * 2003-02-21 2004-09-02 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
DE602004022668D1 (de) 2003-06-03 2009-10-01 Novartis Ag 5-gliedrige heterocyclische p-38 inhibitoren
DK1641764T3 (da) 2003-06-26 2011-11-21 Novartis Ag P38-kinasehæmmere på grundlag af 5-leddede heterocykliske forbindelser
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
WO2005012256A1 (en) 2003-07-22 2005-02-10 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
PL1651615T3 (pl) 2003-07-29 2010-08-31 High Point Pharmaceuticals Llc Pirydazynylo-piperazyny oraz ich zastosowanie jako ligandów receptora histaminowego H3
WO2005047504A1 (en) * 2003-11-07 2005-05-26 The Board Of Trustees Of The University Of Illinois Induction of cellular senescence by cdk4 disruption for tumor suppression and regression
EP1699477A2 (en) * 2003-12-11 2006-09-13 Theravance, Inc. Compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases
EP1550372A1 (en) * 2003-12-24 2005-07-06 Bayer CropScience GmbH Plant growth regulation
CN1934107A (zh) * 2004-01-30 2007-03-21 Ab科学公司 作为酪氨酸激酶抑制剂的2－(3－取代芳基)氨基－4－芳基－噻唑
EP1732905A1 (en) 2004-03-31 2006-12-20 Lexicon Genetics Incorporated 2-aminomethylthiazole-5-carboxamides as protein kinase modulators
US7211576B2 (en) * 2004-04-20 2007-05-01 Hoffmann-La Roche Inc. Diaminothiazoles
JP2008503446A (ja) 2004-05-06 2008-02-07 プレキシコン，インコーポレーテッド Ｐｄｅ４ｂ阻害剤及びその使用
US7405220B2 (en) 2004-06-09 2008-07-29 Hoffmann-La Roche Inc. Pyrazolopyrimidines
US7423053B2 (en) * 2004-07-15 2008-09-09 Hoffmann-La Roche Inc. 4-Aminothiazole derivatives
US7423051B2 (en) * 2004-07-15 2008-09-09 Hoffmann-La Roche Inc. 2,6-diaminopyridine derivatives
CA2583428A1 (en) 2004-09-03 2006-03-09 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
US7241893B2 (en) * 2004-09-17 2007-07-10 Hoffman-La Roche Inc. Thiazolinone 2-substituted quinolines
US7253285B2 (en) * 2004-09-17 2007-08-07 Hoffmann-La Roche Inc. Thiazolinone 4-monosubstituted quinolines
EP1805175B1 (en) 2004-10-14 2008-03-05 F. Hoffmann-Roche AG Novel azaindole thiazolinones as anti-cancer agents
EP1836199A1 (en) 2004-12-30 2007-09-26 Astex Therapeutics Limited Thiazole and isothiazole derivatives that modulate the activity of cdk, gsk and aurora kinases
CA2593993C (en) 2004-12-30 2014-07-29 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
BRPI0606455A (pt) 2005-01-21 2008-03-11 Astex Therapeutics Ltd compostos farmacêuticos
US20080161251A1 (en) 2005-01-21 2008-07-03 Astex Therapeutics Limited Pharmaceutical Compounds
US7304074B2 (en) 2005-04-05 2007-12-04 Hoffmann-La Roche Inc. Substituted 1,5-naphthyridine azolinones
US8501739B2 (en) 2005-07-04 2013-08-06 High Point Pharmaceuticals, Llc Medicaments
KR20080033450A (ko) 2005-07-30 2008-04-16 아스트라제네카 아베 증식성 질환의 치료에 사용하기 위한 이미다졸릴-피리미딘화합물
US7705009B2 (en) * 2005-11-22 2010-04-27 Hoffman-La Roche Inc. 4-aminopyrimidine-5-thione derivatives
CN101410385B (zh) 2006-03-28 2011-08-24 高点制药有限责任公司 具有组胺h3受体活性的苯并噻唑类
JP2009537596A (ja) 2006-05-23 2009-10-29 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー ６−（４−シクロプロピルピペリジン−１−イル）−２’−メチル−［３，４’］−ビピリジン及びその医薬としての使用
JP5694661B2 (ja) 2006-05-29 2015-04-01 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー ３−（１，３−ベンゾジオキソル−５−イル）−６−（４−シクロプロピルピペラジン−１−イル）−ピリダジンと、その塩と、その溶媒和物と、そのヒスタミンｈ３受容体アンタゴニストとしての利用法
MX2009008665A (es) * 2007-02-13 2009-08-21 Ab Science Procedimiento para la sintesis de compuestos de 2-aminotiazol como inhibidores de quinasa.
AU2008250436B2 (en) * 2007-05-11 2013-03-28 F. Hoffmann-La Roche Ag Hetarylanilines as modulators for amyloid beta
EP2014656A3 (en) 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists
ES2685171T3 (es) 2010-06-14 2018-10-05 The Scripps Research Institute Reprogramación de células a un nuevo destino
US9321737B2 (en) * 2012-02-02 2016-04-26 Senex Biotechnology Inc CDK8-CDK19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer
CN102977049A (zh) * 2012-11-26 2013-03-20 盛世泰科生物医药技术(苏州)有限公司 一种2-氨基-4-环丙基-5-羧酸乙酯噻唑的合成方法
SG11201509194SA (en) 2013-05-07 2015-12-30 Univ California Radiomitigating pharmaceutical formulations
CN104628627A (zh) * 2014-12-23 2015-05-20 安徽德信佳生物医药有限公司 一种1-boc-4-氨基哌啶的合成方法
CN106854200B (zh) * 2015-12-08 2019-05-21 上海复星星泰医药科技有限公司 色瑞替尼及其中间体的制备方法
WO2018089902A1 (en) * 2016-11-13 2018-05-17 Apogee Biotechnology Corporation Diaminothiazole compounds, compositions and methods of use
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Ｂｍｐシグナル阻害化合物
US10941126B2 (en) 2017-01-19 2021-03-09 Temple University-Of The Commonwealth System Of Higher Education Bridged bicycloalkyl-substituted aminothiazoles and their methods of use
CN115569137A (zh) 2018-06-15 2023-01-06 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物
CN109897014A (zh) * 2019-04-17 2019-06-18 成都睿智化学研究有限公司 一种1-（取代苯基）-4-甲基哌嗪的工艺制备方法
CN114099503A (zh) * 2020-09-01 2022-03-01 乔海灵 化合物作为cyp2e1抑制剂的应用
CN114805432A (zh) * 2022-03-03 2022-07-29 西北工业大学 新型可光催化剪切的羧酸保护基及其氨基酸衍生物的制备方法

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3530161A (en) 1968-08-19 1970-09-22 Shell Oil Co Aromatic isothiocyanate production
BE792402A (fr) 1971-12-07 1973-06-07 Ciba Geigy Composes heterocycliques azotes et medicaments anthelminthiqueset antimicrobiens qui en contiennent
CH593806A5 (sh) 1974-11-14 1977-12-15 Ciba Geigy Ag
US4086239A (en) 1977-07-01 1978-04-25 Stauffer Chemical Company Thiazole bis-phosphates and phosphonates, intermediates, and insecticidal compositions and methods
US4649146A (en) 1983-01-31 1987-03-10 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives and pharmaceutical composition comprising the same
DE3804531A1 (de) 1988-02-13 1989-08-24 Bayer Ag 5-cyano-2,4-diamino-thiazol-derivate
IE68593B1 (en) 1989-12-06 1996-06-26 Sanofi Sa Heterocyclic substituted acylaminothiazoles their preparation and pharmaceutical compositions containing them
US5620963A (en) 1991-10-15 1997-04-15 Isis Pharmaceuticals, Inc. Oligonucleotides for modulating protein kinase C having phosphorothioate linkages of high chiral purity
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
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
ES2108120T3 (es) * 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
DE69233399T2 (de) 1991-09-20 2005-08-04 Fred Hutchinson Cancer Research Center, Seattle Menschliches cyclin e
US5262409A (en) 1991-10-11 1993-11-16 Fred Hutchinson Cancer Research Center Binary tumor therapy
US5441880A (en) 1991-11-18 1995-08-15 Cold Spring Harbor Laboratory Human cdc25 genes, encoded products and uses thereof
US5302706A (en) 1991-12-16 1994-04-12 Baylor College Of Medicine Senescent cell derived inhibitors of DNA synthesis
US5596079A (en) 1991-12-16 1997-01-21 Smith; James R. Mimetics of senescent cell derived inhibitors of DNA synthesis
CA2117913C (en) 1992-04-10 2006-05-09 Richard J. Epstein Activation-state-specific phosphoprotein immunodetection
WO1994007522A1 (en) 1992-09-30 1994-04-14 Yale University Therapeutic and diagnostic methods and compositions based on transducin-like enhancer of split proteins and nucleic acids
US5543291A (en) 1993-01-29 1996-08-06 Dana Farber Cancer Institute Method of detecting carcinoma
JPH08510451A (ja) 1993-05-13 1996-11-05 ネオルックス コーポレイション 異常増殖性平滑筋細胞に関連した病因の予防及び治療
US5443962A (en) 1993-06-04 1995-08-22 Mitotix, Inc. Methods of identifying inhibitors of cdc25 phosphatase
US5514571A (en) 1993-08-05 1996-05-07 University Technologies International Inc. Cyclin D1 negative regulatory activity
US5473056A (en) 1993-10-13 1995-12-05 Merck & Co., Inc. E2F-2, a novel mammalian transcription factor
US5532167A (en) 1994-01-07 1996-07-02 Beth Israel Hospital Substrate specificity of protein kinases
US5484710A (en) 1994-01-14 1996-01-16 La Jolla Cancer Research Foundation Method of down-regulating a gene linked to a P-53 responsive element
US5625031A (en) 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
WO1995025813A1 (en) 1994-03-18 1995-09-28 University Of Utah Research Foundation Germline mutations in the mts gene and method for detecting predisposition to cancer at the mts gene
US5496831A (en) 1994-05-13 1996-03-05 The General Hospital Corporation Inhibition of insulin-induced adiposis
US5631156A (en) 1994-06-21 1997-05-20 The University Of Michigan DNA encoding and 18 KD CDK6 inhibiting protein
US5571523A (en) 1995-03-09 1996-11-05 President And Fellows Of Harvard College Antioxidant-induced apoptosis in vascular smooth muscle cells
US5733920A (en) 1995-10-31 1998-03-31 Mitotix, Inc. Inhibitors of cyclin dependent kinases
DE69627195T2 (de) 1995-11-01 2004-01-29 Novartis Ag Purinderivate und verfahren zu ihrer herstellung
US5849733A (en) 1996-05-10 1998-12-15 Bristol-Myers Squibb Co. 2-thio or 2-oxo flavopiridol analogs
TW513418B (en) 1996-07-31 2002-12-11 Otsuka Pharma Co Ltd Thiazole derivatives, their production and use
DZ2285A1 (fr) 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
EP0964864B1 (en) * 1997-02-05 2008-04-09 Warner-Lambert Company LLC Pyrido 2,3-d pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
KR20010082501A (ko) * 1997-10-27 2001-08-30 개리 이. 프라이드만 4-아미노티아졸 유도체, 그 제조방법 및 싸이클린-의존성키나아제의 억제제로서의 이용방법
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

Also Published As

Publication number Publication date
HRP20000222A2 (en) 2001-02-28
DE69833223T2 (de) 2006-09-14
CA2306082A1 (en) 1999-05-06
ID24372A (id) 2000-07-13
BR9815200A (pt) 2001-10-16
OA11352A (en) 2003-12-23
EA003527B1 (ru) 2003-06-26
LT2000033A (en) 2001-06-25
DE69835241T2 (de) 2007-05-31
ES2267873T3 (es) 2007-03-16
ATE332896T1 (de) 2006-08-15
ES2256968T3 (es) 2006-07-16
AP1445A (en) 2005-07-10
NO20001955L (no) 2000-06-16
LV12592B (en) 2001-07-20
US20030220326A1 (en) 2003-11-27
EA200000464A1 (ru) 2000-12-25
SI20324A (sl) 2001-02-28
DE69833223D1 (de) 2006-04-06
ATE315553T1 (de) 2006-02-15
DE69835241D1 (de) 2006-08-24
IS5462A (is) 2000-04-19
NZ503788A (en) 2002-11-26
TR200001081T2 (tr) 2000-10-23
HUP0004512A2 (hu) 2002-03-28
US6569878B1 (en) 2003-05-27
LV12592A (en) 2000-12-20
CN1276789A (zh) 2000-12-13
JP2004500304A (ja) 2004-01-08
SK5212000A3 (en) 2001-04-09
CN1158269C (zh) 2004-07-21
AU738792B2 (en) 2001-09-27
PL342447A1 (en) 2001-06-04
GEP20032896B (en) 2003-02-25
IL135574A0 (en) 2001-05-20
EE200000289A (et) 2001-06-15
WO1999021845A3 (en) 1999-08-19
RO119463B1 (ro) 2004-11-30
AU1366499A (en) 1999-05-17
WO1999021845A2 (en) 1999-05-06
HUP0004512A3 (en) 2003-01-28
BG104478A (en) 2001-02-28
BG64195B1 (bg) 2004-04-30
LT4855B (lt) 2001-11-26
EP1056732B1 (en) 2006-01-11
EP1056732A2 (en) 2000-12-06
NO20001955D0 (no) 2000-04-14
AP2000001795A0 (en) 2000-06-30
KR20010082501A (ko) 2001-08-30
UA66810C2 (uk) 2004-06-15

Similar Documents

Publication Publication Date Title
YU22400A (sh) Supstituisana 4-amino-tiazol-2-i jedinjenja kao cdks inhibitori
BRPI0407618A (pt) derivados de tiazole amino substituidos com cicloalquilo contendo n e composições farmacêuticas para inibição da proliferação celular e métodos para a sua utilização
EP1079826B1 (en) Use of indigoid bisindole derivatives for the manufacture of a medicament to inhibit cyclin dependent kinases
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
BR0010520A (pt) Novos compostos farmaceuticamente ativos
WO2004041162A3 (en) Inhibitors of akt activity
MX2007010721A (es) Nuevo uso de inhibidores de fosfodiesterasa 7 para el tratamiento de dolor neuropatico.
HUP0202490A2 (hu) Indazolszármazékok és ezeket tartalmazó protein-kináz gátló hatású gyógyszerkészítmények
BRPI0407834A (pt) composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase
BRPI0616574A2 (pt) derivado de sulfonamida tendo atividade antagonìstica de receptor de pgd2
DE60237145D1 (de) Chinazolinderivate
TNSN05176A1 (fr) Derives de diazepino-indole servant d'inhibiteurs de kinases
BR9909256A (pt) 2- trans- (4-aminociclohexil)amino]purinas 6,9-di-substituìdas
BR0210874A (pt) Derivados de tiazol-benzamida e composições farmacêuticas para a inibição da proliferação celular e métodos para o seu uso
BR9807132A (pt) Derivados de pirrolidina tendo atividade inibitória de fosfolipase a2
EP1215208A3 (en) 4-Aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases
BR0314182A (pt) Formulações compreendendo um composto de indolinona
ATE279933T1 (de) Arzneimittel zur hemmung des nf-kb transkriptionsfaktors
BR0110211A (pt) Derivados de oxadiazol tendo efeitos anticâncer
NO20014864D0 (no) Substituerte 1,4-dihydro-inden [1,2-C] pyrazoler som inhibitorer av tyrosin kinase
BRPI0413384A (pt) inibidores da proteìna farnesil transferase como agentes antitumores
CA2294399C (en) Farnesyl transferase inhibitors in combination with hmg coa reductase inhibitors for the treatment of cancer
PT652874E (pt) 2-heterociclico-5-hidroxi-1,3-pirimidinas uteis como agentes anti-inflamatorios
JP2018525447A (ja) Ａｐｐ選択的ｂａｃｅ阻害のための組成物およびそのための使用
DE69917005D1 (de) Substituierte pyrrolobenzimidazolderivate zur entzündungshemmung