BR0308875A - Composto ou um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, processo para prepará-lo, composição farmacêutica, uso do composto da fórmula de um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, e, métodos para produzir um efeito inibidor de hdac e para tratar o câncer em um animal de sangue quente, tal como o homem, em necessidade de tal tratamento - Google Patents

Composto ou um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, processo para prepará-lo, composição farmacêutica, uso do composto da fórmula de um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, e, métodos para produzir um efeito inibidor de hdac e para tratar o câncer em um animal de sangue quente, tal como o homem, em necessidade de tal tratamento

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Publication number
BR0308875A
BR0308875A BR0308875-8A BR0308875A BR0308875A BR 0308875 A BR0308875 A BR 0308875A BR 0308875 A BR0308875 A BR 0308875A BR 0308875 A BR0308875 A BR 0308875A
Authority
BR
Brazil
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
amide
ester
Prior art date
Application number
BR0308875-8A
Other languages
English (en)
Inventor
Elaine Sophie Elizabeth Stokes
Craig Anthony Roberts
Michael James Waring
Original Assignee
Astrazeneca Ab
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 GB0207863A external-priority patent/GB0207863D0/en
Priority claimed from GB0229930A external-priority patent/GB0229930D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of BR0308875A publication Critical patent/BR0308875A/pt

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    • C07ORGANIC CHEMISTRY
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
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    • C07D239/42One nitrogen atom
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    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
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    • C07D277/22Heterocyclic 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
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  • Chemical & Material Sciences (AREA)
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  • Pyridine Compounds (AREA)
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Abstract

"COMPOSTO OU UM SAL FARMACEUTICAMENTE ACEITáVEL OU AMIDA OU éSTER DESTE HIDROLISáVEL IN VIVO, PROCESSO PARA PREPARá-LO, COMPOSIçãO FARMACêUTICA, USO DO COMPOSTO DA FóRMULA DE UM SAL FARMACEUTICAMENTE ACEITáVEL OU AMIDA OU éSTER DESTE HIDROLISáVEL IN VIVO, E, MéTODOS PARA PRODUZIR UM EFEITO INIBIDOR DE HDAC E PARA TRATAR O CâNCER EM UM ANIMAL DE SANGUE QUENTE, TAL COMO O HOMEM, EM NECESSIDADE DE TAL TRATAMENTO". A invenção diz respeito a um composto da fórmula (I) em que o Anel A é heterociclila; m é de 0 a 4 e cada R^ 1^ é um grupo tal como hidróxi, halo, trifluorometila e ciano; R^ 2^ é halo e n é de 0 a 2 e cada R^ 4^ é um grupo tal como hidróxi, halo, trifluorometila e ciano; p é de 0 a 4 e R^ 3^ é amino ou hidróxi ou sais farmaceuticamente aceitáveis ou ésteres hidrolisáveis in vivo ou amida destes processos para a sua preparação, composições farmacêuticas que os contenham e a seu uso no tratamento de doenças ou de condições médicas mediadas por histona desacetilase.
BR0308875-8A 2002-04-05 2003-04-02 Composto ou um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, processo para prepará-lo, composição farmacêutica, uso do composto da fórmula de um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, e, métodos para produzir um efeito inibidor de hdac e para tratar o câncer em um animal de sangue quente, tal como o homem, em necessidade de tal tratamento BR0308875A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0207863A GB0207863D0 (en) 2002-04-05 2002-04-05 Benzamide derivatives
GB0229930A GB0229930D0 (en) 2002-12-21 2002-12-21 Benzamide derivatives
PCT/GB2003/001442 WO2003087057A1 (en) 2002-04-05 2003-04-02 Benzamide derivatives useful as histone deacetylase inhibitors

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BR0308875A true BR0308875A (pt) 2005-01-04

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BR0308875-8A BR0308875A (pt) 2002-04-05 2003-04-02 Composto ou um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, processo para prepará-lo, composição farmacêutica, uso do composto da fórmula de um sal farmaceuticamente aceitável ou amida ou éster deste hidrolisável in vivo, e, métodos para produzir um efeito inibidor de hdac e para tratar o câncer em um animal de sangue quente, tal como o homem, em necessidade de tal tratamento

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US (3) US20050171103A1 (pt)
EP (1) EP1495002B1 (pt)
JP (1) JP4471665B2 (pt)
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Families Citing this family (157)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7868204B2 (en) 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
EP1429765A2 (en) 2001-09-14 2004-06-23 Methylgene, Inc. Inhibitors of histone deacetylase
AU2003216322A1 (en) 2002-02-15 2003-09-09 Rigel Pharmaceuticals, Inc. Inhibitors of tubulin polymerization
KR20040093692A (ko) 2002-03-13 2004-11-08 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 피페라지닐-,피페리디닐- 및 모르폴리닐-유도체
DE60326436D1 (en) 2002-03-13 2009-04-16 Janssen Pharmaceutica Nv Aminoderivate als histone-deacetylase-inhibitoren
US20050272647A1 (en) * 2002-08-20 2005-12-08 Noboru Yamaji Arthrodial cartilage extracellular matrix degradation inhibitor
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7250514B1 (en) 2002-10-21 2007-07-31 Takeda San Diego, Inc. Histone deacetylase inhibitors
CA2518318A1 (en) 2003-03-17 2004-09-30 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1664041B1 (en) * 2003-09-22 2008-07-02 Euro-Celtique S.A. Phenyl-carboxamide compounds useful for treating pain
KR101153335B1 (ko) * 2003-09-24 2012-07-05 메틸진 인코포레이티드 히스톤 데아세틸라제의 억제제
TW200533357A (en) * 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
WO2005074643A2 (en) * 2004-01-30 2005-08-18 Smithkline Beecham Corporation Benzamide compounds useful as rock inhibitors
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
AU2005225471B2 (en) * 2004-03-26 2011-05-12 Methylgene Inc. Inhibitors of histone deacetylase
RS51189B (sr) 2004-07-28 2010-10-31 Janssen Pharmaceutica N.V. Supstituisani derivati propenil piperazina kao novi inhibitori histonske deacetilaze
US8193205B2 (en) 2004-07-28 2012-06-05 Janssen Pharmaceutica N.V. Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
AR050926A1 (es) * 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
AU2005314601A1 (en) * 2004-10-15 2006-06-15 Bayer Pharmaceuticals Corporation Indane amides with antiproliferative activity
ATE502025T1 (de) * 2004-10-19 2011-04-15 Compass Pharmaceuticals Llc Arylcarboxamide und ihre verwendung als antitumormittel
JP2008524246A (ja) 2004-12-16 2008-07-10 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
GB0427758D0 (en) * 2004-12-18 2005-01-19 Astrazeneca Ab Novel benzamide compounds
US7968574B2 (en) 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
GB0500828D0 (en) * 2005-01-15 2005-02-23 Astrazeneca Ab Benzamide derivatives
GB0501146D0 (en) * 2005-01-20 2005-02-23 Astrazeneca Ab Novel benzamide derivatives
NZ589276A (en) 2005-02-03 2012-06-29 Topotarget Uk Ltd Combination therapies using hdac inhibitors and erlotinib (tarceva)
AU2006240246A1 (en) 2005-04-20 2006-11-02 Merck Sharp & Dohme Corp. Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
CA2605110A1 (en) 2005-04-20 2006-11-02 Merck & Co., Inc. Benzothiophene derivatives
AU2006240248A1 (en) 2005-04-20 2006-11-02 Merck Sharp & Dohme Corp. Benzothiophene hydroxamic acid derivatives
GB0509225D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of enzymatic activity
GB0509223D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Enzyme inhibitors
EP1719508A1 (en) * 2005-05-06 2006-11-08 Yih-Lin Chung Use of histone deacetylase inhibitors for the prevention or treatment of joint destruction
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
CN101189003B (zh) 2005-05-13 2012-02-08 托波塔吉特英国有限公司 Hdac抑制剂的药物制剂
AU2006248938B2 (en) 2005-05-18 2011-09-29 Janssen Pharmaceutica N.V. Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase
EP1731911A1 (fr) 2005-06-07 2006-12-13 Institut National De La Sante Et De La Recherche Medicale (Inserm) Procédé utile pour la détection d'encéphalopathies
JP2008546793A (ja) 2005-06-24 2008-12-25 メルク エンド カムパニー インコーポレーテッド 修飾マロン酸誘導体
US20090176837A1 (en) * 2005-07-12 2009-07-09 Sony Corporation Compounds with activity at retinoic acid receptors
EA200800321A1 (ru) 2005-07-14 2008-06-30 Такеда Сан Диего, Инк. Ингибиторы гистондеацетилазы
GB0521244D0 (en) 2005-10-19 2005-11-30 Astrazeneca Ab Benzamide compounds
ES2366132T3 (es) 2005-10-27 2011-10-17 Janssen Pharmaceutica Nv Derivados del ácido escuárico como inhibidores de la histona desacetilasa.
CA2626897A1 (en) 2005-11-03 2007-05-18 Joshua Close Histone deacetylase inhibitors with aryl-pyrazolyl motifs
JP5377968B2 (ja) 2005-11-10 2013-12-25 トポターゲット ユーケー リミテッド 癌治療のために単独で用いるまたは化学療法薬と併用するヒストンデアセチラーゼ(hdac)阻害剤
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
GB0526351D0 (en) * 2005-12-23 2006-02-01 Astrazeneca Ab Novel benzamide derivatives
GB0526352D0 (en) * 2005-12-23 2006-02-01 Astrazeneca Ab Benzamide derivatives
SI1981874T1 (sl) 2006-01-19 2009-10-31 Janssen Pharmaceutica Nv Aminofenilni derivati kot novi inhibitorji histon deacetilaze
AU2007206944B2 (en) 2006-01-19 2012-08-23 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
US7834011B2 (en) 2006-01-19 2010-11-16 Janssen Pharmaceutica N.V. Heterocyclylalkyl derivatives as novel inhibitors of histone deacetylase
AU2007206942B2 (en) 2006-01-19 2012-08-23 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
JP5137849B2 (ja) 2006-01-19 2013-02-06 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒストンデアセチラーゼのインヒビターとしての置換インドリル−アルキル−アミノ−誘導体
WO2007082880A1 (en) 2006-01-19 2007-07-26 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
WO2007087443A2 (en) 2006-01-25 2007-08-02 Synta Pharmaceuticals Corp. Vinyl-phenyl derivatives for inflammation and immune-related uses
JP2009528354A (ja) 2006-02-28 2009-08-06 メルク エンド カムパニー インコーポレーテッド ヒストン脱アセチル化酵素のインヒビター
TW200740769A (en) 2006-03-16 2007-11-01 Astrazeneca Ab Novel process
KR101495611B1 (ko) 2006-04-07 2015-02-25 메틸진 인코포레이티드 히스톤 데아세틸라아제의 억제제
CA2649861A1 (en) 2006-04-26 2007-11-08 Merck & Co., Inc. Disubstituted aniline compounds
CA2651681A1 (en) 2006-05-18 2007-11-29 Merck & Co., Inc. Aryl-fused spirocyclic compounds
EP2041071B1 (en) 2006-06-29 2014-06-18 Kinex Pharmaceuticals, LLC Biaryl compositions and methods for modulating a kinase cascade
EP1889830A1 (en) * 2006-07-10 2008-02-20 Pharmeste S.r.l. Biarylcarboxyarylamides as vanilloid-1 receptor modulators
EP2049124A4 (en) 2006-07-20 2010-02-10 Merck & Co Inc PHOSPHOR DERIVATIVES AS HISTONDEACETYLASE HEMMER
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
US8962825B2 (en) 2006-10-30 2015-02-24 Glaxosmithkline Intellectual Property Development Limited Hydroxamates as inhibitors of histone deacetylase
TWI457336B (zh) 2006-12-28 2014-10-21 Kinex Pharmaceuticals Llc 調節激酶級聯之組成物及方法
US7939529B2 (en) 2007-05-17 2011-05-10 Kinex Pharmaceuticals, Llc Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
US7935697B2 (en) 2006-12-28 2011-05-03 Kinex Pharmaceuticals, Llc Compositions for modulating a kinase cascade and methods of use thereof
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
EP2135620A4 (en) 2007-03-28 2010-12-29 Santen Pharmaceutical Co Ltd AGAINST OKULAR HYPOTONIA CONNECTED TO HISTONE DEACETYLASE INHIBITION AS AN ACTIVE SUBSTANCE
ES2536406T3 (es) 2007-06-08 2015-05-25 Janssen Pharmaceutica, N.V. Derivados de piperidina/piperazina
ES2558152T3 (es) 2007-06-08 2016-02-02 Janssen Pharmaceutica, N.V. Derivados de piperidina/piperazina
JO2972B1 (en) 2007-06-08 2016-03-15 جانسين فارماسوتيكا ان. في Piperidine / piperazine derivatives
WO2009005638A2 (en) 2007-06-27 2009-01-08 Merck & Co., Inc. Pyridyl and pyrimidinyl derivatives as histone deacetylase inhibitors
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8124605B2 (en) 2007-07-06 2012-02-28 Kinex Pharmaceuticals, Llc Compositions and methods for modulating a kinase cascade
CA2695071A1 (en) * 2007-08-02 2009-02-05 F. Hoffmann-La Roche Ag The use of benzamide derivatives for the treatment of cns disorders
JP2010540426A (ja) 2007-09-25 2010-12-24 トポターゲット ユーケー リミテッド 特定のヒドロキサム酸化合物の合成方法
EP2231596A4 (en) * 2007-12-14 2012-06-06 Univ Georgetown INHIBITORS OF HISTONATE ACETYLASE
AU2009228931B2 (en) 2008-03-27 2013-05-23 Janssen Pharmaceutica Nv Aza-bicyclohexyl substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
ES2617619T3 (es) 2008-06-05 2017-06-19 Janssen Pharmaceutica, N.V. Combinaciones de fármacos que comprenden un inhibidor de DGAT y un agonista de PPAR
EP2330894B8 (en) 2008-09-03 2017-04-19 BioMarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors
KR20170015566A (ko) 2008-11-10 2017-02-08 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
ES2663222T3 (es) 2008-12-19 2018-04-11 Vertex Pharmaceuticals Incorporated Derivados de pirazina útiles como inhibidores de la quinasa ATR
EP2221053A1 (de) * 2009-02-20 2010-08-25 Albert-Ludwigs-Universität Freiburg Pharmazeutische Zusammensetzung enthaltend Hemmstoffe der Proteinmethyltransferase I und deren Verwendung zur Behandlung von Tumorerkrankungen
GB0903480D0 (en) 2009-02-27 2009-04-08 Chroma Therapeutics Ltd Enzyme Inhibitors
EP2421368A4 (en) * 2009-04-20 2013-01-09 Inst Oneworld Health COMPOUNDS, COMPOSITIONS AND METHODS FOR PYRIDAZINE SULFONAMIDE DERIVATIVES
CN101906076B (zh) * 2009-06-04 2013-03-13 深圳微芯生物科技有限责任公司 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
IN2012DN02493A (pt) * 2009-09-03 2015-08-28 Allergan Inc
JP2013517281A (ja) 2010-01-13 2013-05-16 テンペロ、ファーマシューティカルズ、インコーポレイテッド 化合物及び方法
CN103221047B (zh) 2010-01-13 2014-12-17 坦颇罗制药股份有限公司 化合物和方法
EP2558085B1 (en) 2010-04-16 2017-08-30 Athenex, Inc. Compositions and methods for the prevention and treatment of cancer
JP5856151B2 (ja) 2010-05-12 2016-02-09 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 Atrキナーゼ阻害剤として有用な2−アミノピリジン誘導体
JP2013526540A (ja) 2010-05-12 2013-06-24 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 Atrキナーゼ阻害剤として有用な化合物
US9630956B2 (en) 2010-05-12 2017-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526539A (ja) 2010-05-12 2013-06-24 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 Atrキナーゼ阻害剤として有用なピラジン
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013529200A (ja) 2010-05-12 2013-07-18 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 Atrキナーゼ阻害剤として有用な化合物
CA2803802A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
US20130310379A1 (en) * 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US9540395B2 (en) 2011-02-28 2017-01-10 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
JP2014510151A (ja) 2011-04-05 2014-04-24 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 Atrキナーゼ(trakinase)阻害剤として有用なアミノピラジン化合物
EP2701699B1 (en) 2011-04-28 2019-10-16 The Broad Institute, Inc. Inhibitors of histone deacetylase
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
GB201111630D0 (en) * 2011-07-07 2011-08-24 Cancer Rec Tech Ltd Novel compounds and their use
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013049859A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
KR20140084112A (ko) 2011-09-30 2014-07-04 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071085A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
WO2013078320A1 (en) * 2011-11-21 2013-05-30 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
HRP20161578T1 (hr) * 2012-02-09 2016-12-30 Merck Patent Gmbh Derivati furo[3, 2-b]piridina kao inhibitori tbk1 i ikk
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
CA2869309C (en) 2012-04-05 2021-02-09 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
JP6337255B2 (ja) * 2012-07-27 2018-06-06 ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. ヒストンデアセチラーゼの阻害剤
ITRM20120405A1 (it) 2012-08-09 2014-02-10 C N C C S Scarl Collezione Naziona Le Dei Compost Compounds for use in the treatment of disorders that are ameliorated by inhibition of hdac
US9926273B2 (en) 2012-08-30 2018-03-27 Athenex, Inc. Composition and methods for modulating a kinase cascade
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
WO2014143666A1 (en) * 2013-03-15 2014-09-18 Biomarin Pharmaceutical Inc. Hdac inhibitors
JP2016512815A (ja) 2013-03-15 2016-05-09 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 Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003360A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2015054474A1 (en) * 2013-10-10 2015-04-16 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
DK3077397T3 (da) 2013-12-06 2019-12-16 Vertex Pharma 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf
PL3152212T3 (pl) 2014-06-05 2020-06-15 Vertex Pharmaceuticals Inc. Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych
LT3157566T (lt) 2014-06-17 2019-08-12 Vertex Pharmaceuticals Incorporated Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį
SG11201700094TA (en) 2014-07-07 2017-02-27 Acetylon Pharmaceuticals Inc Treatment of leukemia with histone deacetylase inhibitors
WO2016028971A1 (en) * 2014-08-21 2016-02-25 Bristol-Myers Squibb Company Tied-back benzamide derivatives as potent rock inhibitors
JP6697809B2 (ja) 2015-03-06 2020-05-27 ファーマケア,インク. フッ素化リシルオキシダーゼ様2阻害剤とその使用
WO2016144702A1 (en) 2015-03-06 2016-09-15 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
RU2720678C2 (ru) 2015-07-02 2020-05-12 Байомарин Фармасьютикал Инк. Ингибиторы гистондеацетилазы
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
KR102615565B1 (ko) 2016-09-07 2023-12-18 파마케아, 인크. 리실 옥시다제 유사 2 억제제의 용도
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
TWI741040B (zh) * 2016-10-20 2021-10-01 德商拜耳作物科學公司 製備3-烷基硫基-2-氯-n-(1-烷基-1h-四唑-5-基)-4-三氟甲基苯甲醯胺之方法
EP3736266A4 (en) * 2018-01-04 2021-01-06 Peking University Shenzhen Graduate School COMPOUND SIMULTANEOUSLY INHIBITING THE LSD1 AND HDAC TARGETS AND ITS APPLICATION
CA3125731A1 (en) 2018-01-12 2019-07-18 KDAc Therapeutics, Inc. Combination of a selective histone deacetylase 3 (hdac3) inhibitor and an immunotherapy agent for the treatment of cancer
EA202092328A1 (ru) 2018-05-11 2021-04-08 Темпл Юниверсити-Оф Зэ Коммонвелс Систем Оф Хаер Эдьюкейшн Новые функционализированные лактамы в качестве модуляторов 5-гидрокситриптаминового рецептора 7 и способ их применения
CN113368114B (zh) * 2020-03-10 2022-04-22 四川大学 一种吗啉嘧啶类化合物的抗肿瘤应用

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH117273A4 (pt) * 1973-01-26 1976-07-15
CH187973A4 (de) * 1973-02-09 1977-03-31 Hoechst Ag Verfahren zum optischen Aufhellen von Textilmaterialien
DE2918965A1 (de) * 1979-05-11 1980-11-20 Bayer Ag Benzofuranverbindungen sowie deren verwendung als optische aufheller
IT1232252B (it) * 1989-02-22 1992-01-28 Rotta Research Lab Derivati della n fenil benzamide ad attivita' antiulcera ed antiallerica e procedimento per la loro preparazione
JPH05239069A (ja) * 1992-02-28 1993-09-17 Canon Inc 液晶性化合物、これを含む液晶組成物、それを有する液晶素子、それらを用いた表示方法および表示装置
JP3354090B2 (ja) 1996-09-30 2002-12-09 シエーリング アクチエンゲゼルシャフト 分化誘導剤
US6174905B1 (en) 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
JPH11269140A (ja) 1998-03-23 1999-10-05 Mitsui Chem Inc 分化誘導剤
JPH11269146A (ja) 1998-03-24 1999-10-05 Mitsui Chem Inc 分化誘導剤
JP4405602B2 (ja) 1998-04-16 2010-01-27 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト ヒストン脱アセチル化酵素阻害剤
JPH11335375A (ja) 1998-05-20 1999-12-07 Mitsui Chem Inc ヒストン脱アセチル化酵素阻害作用を有するベンズアミド誘導体
JP4390024B2 (ja) * 1999-04-23 2009-12-24 アステラス製薬株式会社 新規なジアゼパン誘導体又はその塩
KR20020070285A (ko) * 1999-11-23 2002-09-05 메틸진, 인크. 히스톤 디아세틸라제의 억제제
AU776053B2 (en) * 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
JP2002161084A (ja) 2000-11-28 2002-06-04 Sumitomo Pharmaceut Co Ltd 複素環誘導体
EP1429765A2 (en) * 2001-09-14 2004-06-23 Methylgene, Inc. Inhibitors of histone deacetylase
DE10204115A1 (de) * 2002-02-01 2003-08-07 Bayer Cropscience Ag DELTA·1·-Pyrroline
US7148257B2 (en) * 2002-03-04 2006-12-12 Merck Hdac Research, Llc Methods of treating mesothelioma with suberoylanilide hydroxamic acid
WO2003075839A2 (en) 2002-03-04 2003-09-18 Aton Pharma, Inc. Methods of inducing terminal differentiation
ATE458047T1 (de) 2002-03-07 2010-03-15 Univ Delaware Verfahren zur verstärkung der oligonucleotid- vermittelten nucleinsäuresequenzänderung unter verwendung von zusammensetzungen mit einem hydroxyharnstoff
DE60326436D1 (en) 2002-03-13 2009-04-16 Janssen Pharmaceutica Nv Aminoderivate als histone-deacetylase-inhibitoren
OA12793A (en) 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv Sulfonylamino-derivatives as novel inhibitors of histone deacetylase.
KR20040093692A (ko) 2002-03-13 2004-11-08 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 피페라지닐-,피페리디닐- 및 모르폴리닐-유도체
MXPA04008796A (es) 2002-03-13 2004-11-26 Janssen Pharmaceutica Nv Derivados de carbonilamino como novedosos inhibidores de desacetilasa de histona.
ES2306859T3 (es) 2002-03-13 2008-11-16 Janssen Pharmaceutica Nv Derivados de sulfonil como nuevos inhibidores de histona deacetilasa.
US20050123397A1 (en) * 2003-12-03 2005-06-09 Mcardle Nathan J. Compressor diffuser

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