Nothing Special   »   [go: up one dir, main page]

CA2474322A1 - (thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2 - Google Patents

(thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2 Download PDF

Info

Publication number
CA2474322A1
CA2474322A1 CA002474322A CA2474322A CA2474322A1 CA 2474322 A1 CA2474322 A1 CA 2474322A1 CA 002474322 A CA002474322 A CA 002474322A CA 2474322 A CA2474322 A CA 2474322A CA 2474322 A1 CA2474322 A1 CA 2474322A1
Authority
CA
Canada
Prior art keywords
mmol
hplc
group
general procedure
ethanol
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002474322A
Other languages
English (en)
Inventor
Frank Stieber
Klaus Hellmuth
Herbert Waldmann
Ralph Mazitschek
Athanassios Giannis
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
KYLIX PHARMACEUTICALS BV
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
Priority claimed from US10/057,747 external-priority patent/US20030158199A1/en
Application filed by KYLIX PHARMACEUTICALS BV filed Critical KYLIX PHARMACEUTICALS BV
Publication of CA2474322A1 publication Critical patent/CA2474322A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • C07D417/04—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 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D277/22—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • 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
    • C07D417/10—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 aromatic rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne un composé représenté par la formule (I), dans laquelle V est H ou, ou bien ; R¿1? peut être indépendamment H, alkyle, alcényle, cycloalkyle, hétéroalkyle, aryle, hétéroaryle, arylalkyle, alkylaryle, N-R¿6?R¿7?, N- (CO) R¿6?R¿7?, N-R¿6? (CO) R¿7 ?ou N- (CO) -O-R¿6?R¿7 ?; R¿8? peut être indépendamment H, alkyle, alcényle, cycloalkyle, hétéroalkyle, aryle, hétéroaryle, arylalkyle, alkylaryle, N-R¿3?R¿4?, N- (CO) R¿3?R¿4?, N-R¿3? (CO) R¿4?, N- (CO) -O-R¿3?R¿4?, O-R¿3?, CO-R¿3?, CO-OR¿3? ou O-CO-R¿3 ?; R¿2?, R¿5? peuvent être indépendamment H, alkyle, alcényle, cycloalkyle, hétéroalkyle, aryle, hétéroaryle, arylalkyle, alkylaryle, carboxyle, Br, C1, F, CF¿3 ?; R¿3?, R¿4?, R¿6?, R¿7 ?peuvent être indépendamment H, alkyle, alcényle, cycloalkyle, hétéroalkyle, aryle, hétéroaryle, arylalkyle, alkylaryle, COOR¿5? et CO-R¿5?, et peuvent former une structure en anneau ; X, Y, Z peuvent être indépendamment CH ou N ; et U peut être indépendamment S ou NH ;W peut être indépendamment NH, O ou S, et des mélanges racémiques-diastereomériques, des isomères optiques, et des sels de ce composé acceptables au plan pharmaceutique. L'invention concerne une méthode permettant d'inhiber l'activité d'une ou de plusieurs protéines kinases à l'aide de ces composés, in vitro ou en culture cellulaire, ainsi qu'une composition pharmaceutique comprenant un tel composé et son utilisation médicamenteuse.
CA002474322A 2002-01-25 2003-01-27 (thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2 Abandoned CA2474322A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP02075367 2002-01-25
US10/057,747 US20030158199A1 (en) 2002-01-25 2002-01-25 Novel compounds for inhibition of Tie-2
US10/057,747 2002-01-25
EP02075367.9 2002-01-25
PCT/EP2003/000810 WO2003062215A1 (fr) 2002-01-25 2003-01-27 (thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2

Publications (1)

Publication Number Publication Date
CA2474322A1 true CA2474322A1 (fr) 2003-07-31

Family

ID=27614618

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002474322A Abandoned CA2474322A1 (fr) 2002-01-25 2003-01-27 (thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2

Country Status (3)

Country Link
EP (1) EP1467981A1 (fr)
CA (1) CA2474322A1 (fr)
WO (1) WO2003062215A1 (fr)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004537537A (ja) 2001-06-29 2004-12-16 アブ サイエンス 炎症性疾患を治療するためのチロシンキナーゼ阻害剤の使用法
CA2452392A1 (fr) 2001-06-29 2003-01-16 Ab Science Utilisation d'inhibiteurs de tyrosine kinases pour traiter les maladies intestinales inflammatoires (mii)
JP2005500041A (ja) 2001-06-29 2005-01-06 アブ サイエンス 強力で選択的かつ非毒性のｃ−ｋｉｔ阻害剤
ATE345839T1 (de) 2001-06-29 2006-12-15 Ab Science Die verwendung von tyrosinkinasehemmer zur behandlung von allergischen erkrankungen
CA2494695C (fr) 2002-08-02 2011-04-05 Ab Science 2-(3-aminoaryl)amino-4-aryl-thiazoles et leur utilisation en tant que inhibiteurs de c-kit
US8450302B2 (en) 2002-08-02 2013-05-28 Ab Science 2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors
GB0326601D0 (en) * 2003-11-14 2003-12-17 Novartis Ag Organic compounds
WO2005063743A1 (fr) 2003-12-26 2005-07-14 Kyowa Hakko Kogyo Co., Ltd. Dérivé de thiazole
EP1555264A1 (fr) * 2004-01-15 2005-07-20 Sireen AG Hétérocycles à cinq chaínons comme inhibiteurs de la famille des SRC proteines kinases
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
WO2005073225A1 (fr) * 2004-01-30 2005-08-11 Ab Science 2-(3-substitues aryle)amino-4-aryle-thiazoles en tant qu'inhibiteurs de tyrosine kinase
US7678810B2 (en) 2004-03-05 2010-03-16 Taisho Pharmaceutical Co., Ltd Thiazole derivative
EP1781287A4 (fr) 2004-08-13 2008-02-27 Genentech Inc Composes a base de thiazole presentant une activite inhibitrice enzymatique utilisant de l'adenosine triphosphate (atp)
UA95071C2 (ru) * 2005-04-04 2011-07-11 Аб Сьянс Замещенные производные оксазола и их применение как ингибиторов тирозинкиназы
BRPI0608910A2 (pt) 2005-05-09 2010-02-17 Achillion Pharmaceuticals Inc uso de um composto da fórmula ou um sal ou hidrato farmaceuticamente aceitável desse, composto ou sal ou hidrato do mesmo, composição farmacêutica e composição farmacêutica embalada
EA015628B1 (ru) * 2005-05-24 2011-10-31 Мерк Сероно С.А. Производные тиазола и их применение
WO2006137527A1 (fr) 2005-06-23 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. Dérivé du thiazole
WO2007031440A2 (fr) * 2005-09-13 2007-03-22 Janssen Pharmaceutica N.V. Derives de thiazole substitues par 2-aniline-4-aryle
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
PT2402319T (pt) 2006-03-31 2017-12-11 Novartis Ag Inibidores de dgat
DE602007008723D1 (de) 2006-05-12 2010-10-07 Vertex Pharma Selektive rock-proteinkinasehemmer und ihre verwendung
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
JO2849B1 (en) 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
CA2682671C (fr) 2007-04-23 2015-11-17 Janssen Pharmaceutica N.V. Thia(dia)zoles en tant qu'antagonistes du recepteur de la dopamine a dissociation rapide
SI2148873T1 (sl) 2007-04-23 2013-01-31 Janssen Pharmaceutica, N.V. Derivati 4-alkoksipiridazina kot antagonisti receptorja dopamina 2 s hitro disociacijo
JP2010528019A (ja) 2007-05-22 2010-08-19 アキリオン ファーマシューティカルズ，インコーポレーテッド ヘテロアリール置換チアゾール
JO2784B1 (en) 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
RU2474579C2 (ru) 2007-10-18 2013-02-10 Янссен Фармацевтика Нв Тризамещенные 1,2,4-триазолы
KR101564303B1 (ko) 2008-03-19 2015-11-06 얀센 파마슈티카 엔.브이. 니코틴성 아세틸콜린 수용체 조절제로서의 삼치환된 1,2,4-트리아졸
EP2107054A1 (fr) * 2008-04-01 2009-10-07 Università Degli Studi Di Milano - Bicocca Composés antiprolifératives et ses utilisations thérapeutiques
EP2280945B1 (fr) 2008-05-09 2014-09-03 Janssen Pharmaceutica, N.V. Pyrazoles trisubstitués en tant que modulateurs des récepteurs de l'acétylcholine
US8106209B2 (en) 2008-06-06 2012-01-31 Achillion Pharmaceuticals, Inc. Substituted aminothiazole prodrugs of compounds with anti-HCV activity
EA019001B1 (ru) * 2008-06-24 2013-12-30 Айрм Ллк Соединения и способы модулирования рецепторов, связанных с белком g
BRPI0915834A2 (pt) 2008-07-03 2015-11-03 Janssen Pharmaceutica Nv 6-(1-piperazinil)-piridazinas substituídas como antagonistas do receptor de 5-ht6
SI2307374T1 (sl) 2008-07-31 2017-05-31 Janssen Pharmaceutica Nv Piperazin-1-il-trifluorometil-substituirani-piridini kot hitro disociirajoči antagonisti receptorja dopamin 2
EP2166006A1 (fr) * 2008-09-18 2010-03-24 Dompe' S.P.A. Acides 2-aryl-propioniques et dérivés et compositions pharmaceutiques les contenant
WO2012162461A1 (fr) * 2011-05-25 2012-11-29 Janssen Pharmaceutica Nv Inhibiteurs phényle-thiazolylés de l'activation de pro-métalloprotéinase de matrice
ES2633987T3 (es) 2013-07-02 2017-09-26 Bristol-Myers Squibb Company Derivados de pirido-carboxamidas tricíclicas como inhibidores de ROCK
ES2634628T3 (es) 2013-07-02 2017-09-28 Bristol-Myers Squibb Company Derivados tricíclicos de pirido-carboxamida como inhibidores ROCK
US9453002B2 (en) 2013-08-16 2016-09-27 Janssen Pharmaceutica Nv Substituted imidazoles as N-type calcium channel blockers
US9828351B2 (en) * 2014-06-26 2017-11-28 Monash University Enzyme interacting agents
JP6424068B2 (ja) * 2014-11-06 2018-11-14 東友ファインケム株式会社Ｄｏｎｇｗｏｏ Ｆｉｎｅ−Ｃｈｅｍ Ｃｏ．， Ｌｔｄ． 化合物
CN107635981B (zh) * 2015-02-17 2020-08-04 中国科学院广州生物医药与健康研究院 用于诱导白色脂肪组织褐变的化合物和方法
US10696638B2 (en) 2017-12-26 2020-06-30 Industrial Technology Research Institute Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same
US11472781B2 (en) 2018-02-21 2022-10-18 Southern Research Institute 2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases
UA128288C2 (uk) 2018-03-08 2024-05-29 Інсайт Корпорейшн СПОЛУКИ АМІНОПІРАЗИНДІОЛУ ЯК ІНГІБІТОРИ PI3K-<font face="Symbol">g</font>
US11718593B2 (en) * 2018-05-17 2023-08-08 Southern Research Institute 2,5-aryl-thiazole analogs for the treatment of neurodegenerative diseases
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
CN113164419A (zh) 2018-09-07 2021-07-23 皮克医疗公司 Eif4e抑制剂和其用途
MX2022010944A (es) * 2020-03-03 2022-11-09 Pic Therapeutics Inc Inhibidores del factor de iniciacion de traduccion eucariotica 4e (eif4e) y sus usos.

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6228871B1 (en) * 1995-07-10 2001-05-08 Merck & Co., Inc. Angiogenesis 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
EE200200123A (et) * 1999-09-10 2003-08-15 Merck & Co., Inc. Türosiinkinaasi pärssiv ühend, seda sisaldav farmatseutiline kompositsioon ning raviotstarbeline kasutamine

Also Published As

Publication number Publication date
EP1467981A1 (fr) 2004-10-20
WO2003062215A1 (fr) 2003-07-31

Similar Documents

Publication Publication Date Title
CA2474322A1 (fr) (thia-/oxa-/pyra) zoles substitues 4(hetero-) aryle pour inhibition de tie-2
RU2456285C2 (ru) Способ получения соединений 2-аминотиазола в качестве ингибиторов киназы
US20030158199A1 (en) Novel compounds for inhibition of Tie-2
ES2315566T3 (es) Tiazolidin-4-onas para inhibir proteinas hyak3.
TWI473792B (zh) New quinoline compounds and their use
JP3785397B2 (ja) ５員環化合物
JP6713928B2 (ja) Ｕｒａｔ１阻害剤
JP5463592B2 (ja) アデノシンａ１レセプターアンタゴニストとしての新規化合物
CA2395564A1 (fr) Nouveaux composes
WO2011085128A1 (fr) Inhibiteurs de la voie hedgehog
WO2003105842A1 (fr) Derives de chromen-2-one utilises comme inhibiteurs de la production des vegf dans les cellules mammaliennes
US6391894B1 (en) Myt1 kinase inhibitors
US6448272B1 (en) Myt1 kinase inhibitors
AU2003236875A1 (en) 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2
CA3026252A1 (fr) Inhibiteurs de l&#39;autotaxine
JP2006169257A (ja) ５員環化合物
AU2766100A (en) Myt1 kinase inhibitors
NZ503917A (en) Bis thiazole amine derivatives useful as Myt1 kinase inhibitors

Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead