DK2680694T3 - Histondeacetylasehæmmere - Google Patents

Histondeacetylasehæmmere Download PDF

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Publication number
DK2680694T3
DK2680694T3 DK12751918.9T DK12751918T DK2680694T3 DK 2680694 T3 DK2680694 T3 DK 2680694T3 DK 12751918 T DK12751918 T DK 12751918T DK 2680694 T3 DK2680694 T3 DK 2680694T3
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Prior art keywords
compound
alkyl
mmol
pyrazol
pharmaceutically acceptable
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DK12751918.9T
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English (en)
Inventor
Vincent Jacques
James R Rusche
Norton P Peet
Jasbir Singh
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Biomarin Pharm Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/18—Heterocyclic 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
    • C07D211/34—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • 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
    • C07D233/64—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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • 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
    • C07D277/30—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Claims (14)

1. Forbindelse med formlen (I):
hvor: Ar/Het er en 5-leddet heteroaryl valgt fra gruppen bestående af pyrazolyl, thiazolyl, oxazolyl, imidazolyl, isoxazolyl, 3,5-dimethylpyrazolyl og isothiazolyl; X er-Y-[C(Ra)2]a[C(Rb)2]b; hvor: Y er CRc=CRd; a er 1-3; b er 0-3; hver forekomst af Ra og Rb er uafhængigt valgt fra H, F og Cl-C6-alkyl: hver af Rc og Rd er H; hver af R4 og R5 er uafhængigt valgt fra H, Cl-C6-alkyl og F; RI er: (i) C6-C10-aryl, der eventuelt er substitueret med fra 1-3 R°; eller (ii) monocyklisk eller bicyklisk heteroaryl, der indbefatter fra 5-10 ringatomer, der eventuelt er substitueret med fra 1-3 R°; hvor fra 1-4 af ringatomerne et heteroatom er uafhængigt valgt fra O, N, N-H, N-R° og S; eller (iii) heterocyclyl, der indbefatter fra 4-10 ringatomer, der eventuelt er substitueret med fra 1-3 R°; hvor fra 1-4 af ringatomeme et heteroatom er uafhængigt valgt fra O, N, N-H, N-R° og S; hver forekomst af R° uafhængigt er valgt fra gruppen bestående af: • halogen; • Cl-C6-alkyl; fhior(Cl-C6)alkyl; • hydroxyl; • hydroxy(Cl-C4)alkyl; • Cl-C6-alkoxy; fluor(Cl-C6)alkoxy; • (Cl-C6-alkyl)C(O)-; • (Cl-C6-alkyl)NH-; (Cl-C6alkyl)2N-; • formyl; formyl(Cl-C4)alkyl; cyano; cyano(Cl-C4)alkyl;
• SO2-(Cl-C6)alkyl; S0-(Cl-C6)alkyl og • nitro; R2 er H og R3 er H, F eller Cl; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse eller salt ifølge krav 1, hvor hver forekomst af Ra og Rb (når de er til stede) er H.
3. Forbindelse eller salt ifølge et hvilket som helst af de foregående krav, hvor hver af R4 og R5 er H.
4. Forbindelsen eller salt ifølge et hvilket som helst af de foregående krav, hvor R3 er H.
5. Forbindelsen eller salt ifølge et hvilket som helst af kravene 1 til 3, hvor R3 er F eller Cl.
6. Forbindelse eller salt ifølge et hvilket som helst af de foregående krav, hvor Ar/Het er valgt fra pyrazolyl og imidazolyl.
7. Forbindelse eller salt ifølge krav 6, hvor Ar/Het er pyrazolyl.
8. Forbindelse eller salt ifølge et hvilket som helst af de foregående krav, hvor X er -CH=CH-CH2- eller -CH=CHCH2CH2.
9. Forbindelse eller salt ifølge et hvilket som helst af de foregående krav, hvor RI er phenyl, der eventuelt er substitueret med fra 1-3 R°.
10. Forbindelse eller salt ifølge krav 1, der har en struktur valgt fra
11. Farmaceutisk sammensætning, der omfatter en forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1 til 10 og en farmaceutisk acceptabel bærer.
12. Forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1 til 10, til anvendelse i medicin.
13. Forbindelse, eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1 til 10, til anvendelse i behandling af en neurologisk forstyrrelse, såsom Friedreichs ataksi, myotonisk dystrofi, spinal muskelatrofi, fragilt X-syndrom, Huntingtons sygdom, spinocerebellar ataksi, Kennedys sygdom, amyotrofisk lateral sklerose, spinal og bulbær muskelatrofi og Alzheimers sygdom; en cancer; en inflammatorisk sygdom; en tilstand med svækket hukommelse eller lægemiddelafhængighed.
14. Forbindelse ifølge krav 13, hvor forstyrrelsen er Friedreichs ataksi.
DK12751918.9T 2011-02-28 2012-02-28 Histondeacetylasehæmmere DK2680694T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161447416P 2011-02-28 2011-02-28
PCT/US2012/026874 WO2012118782A1 (en) 2011-02-28 2012-02-28 Histone deacetylase inhibitors

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DK2680694T3 true DK2680694T3 (da) 2019-03-25

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US (1) US9540395B2 (da)
EP (2) EP2680694B1 (da)
JP (3) JP6250403B2 (da)
AU (2) AU2012223509B2 (da)
CA (2) CA2828524C (da)
DK (1) DK2680694T3 (da)
ES (1) ES2712803T3 (da)
PT (1) PT2680694T (da)
WO (1) WO2012118782A1 (da)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9265734B2 (en) 2008-09-03 2016-02-23 Biomarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
CA2828524C (en) 2011-02-28 2020-01-07 Repligen Corporation Histone deacetylase inhibitors
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
WO2012149540A1 (en) 2011-04-28 2012-11-01 The Broad Institute Inc Inhibitors of histone deacetylase
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
WO2014100438A1 (en) 2012-12-20 2014-06-26 The Broad Institute, Inc. Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors
NZ711585A (en) * 2013-03-15 2020-05-29 Biomarin Pharm Inc Hdac inhibitors
WO2015058106A1 (en) * 2013-10-18 2015-04-23 The General Hospital Corporation Imaging histone deacetylases with a radiotracer using positron emission tomography
WO2016109549A1 (en) 2014-12-30 2016-07-07 University Of Utah Research Foundation Hdac1,2 inhibitors and methods of using the same
US11149062B2 (en) 2015-08-28 2021-10-19 Uwm Research Foundation, Inc. HDAC inhibitors and methods of treatment using the same
CN105920604B (zh) * 2016-06-08 2019-09-03 上海荻硕贝肯生物科技有限公司 用于治疗白血病的联合用药物及其在治疗白血病中的应用
CN106977474B (zh) * 2017-05-10 2020-04-07 四川大学 一种取代2-氰基-3-苯基呋喃-丙烯酰胺衍生物及其制备方法和用途
CN112135610A (zh) * 2018-01-12 2020-12-25 KDAc治疗股份有限公司 用于治疗癌症的选择性组蛋白去乙酰酶3(hdac3)抑制剂及免疫治疗剂的组合
GB201901559D0 (en) * 2019-02-05 2019-03-27 Syngenta Crop Protection Ag Herbicidal compositions
AR120040A1 (es) 2019-09-27 2022-01-26 Takeda Pharmaceuticals Co Compuesto heterocíclico
CN110981868B (zh) * 2019-11-05 2021-08-31 中山大学 咪唑并吡啶类化合物、包含该化合物的药物组合物及其制备方法和用途
CN113248499A (zh) * 2021-06-07 2021-08-13 中国科学院广州生物医药与健康研究院 一种吲嗪类化合物的制备及应用
WO2023034440A1 (en) 2021-09-01 2023-03-09 Case Western Reserve University Treatment of neurodegenerative diseases with hdac inhibitors

Family Cites Families (141)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4855442A (en) 1988-04-13 1989-08-08 Monsanto Company Substituted 3-hydroxy pyrazoles
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US6794392B1 (en) 1996-09-30 2004-09-21 Schering Aktiengesellschaft 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
AU2056800A (en) 1998-12-18 2000-07-03 Du Pont Pharmaceuticals Company Heterocyclic piperidines as modulators of chemokine receptor activity
JP2000256194A (ja) 1999-01-06 2000-09-19 Mitsui Chemicals Inc 核内レセプタ作動薬およびその効果増強剤
EP1182192A4 (en) 1999-04-09 2002-06-05 Mochida Pharm Co Ltd 4-HYDROXYPIPERIDINE DERIVATIVES WITH ANTI-ARRHYTHMIC EFFECT
EP1233958B1 (en) * 1999-11-23 2011-06-29 MethylGene Inc. Inhibitors of histone deacetylase
WO2002018335A1 (fr) 2000-08-28 2002-03-07 Yamanouchi Pharmaceutical Co., Ltd. Derives d'amine cyclique
ATE401395T1 (de) 2001-05-02 2008-08-15 Univ California Verfahren zur behandlung neurodegenerativer, psychiatrischer und anderer störungen mit deacetylaseinhibitoren
US20040142859A1 (en) 2002-05-02 2004-07-22 Steffan Joan S. Method for treating neurodegenerative, psychiatric, and other disorders with deacetylase inhibitors
US6784173B2 (en) 2001-06-15 2004-08-31 Hoffmann-La Roche Inc. Aromatic dicarboxylic acid derivatives
AR034897A1 (es) * 2001-08-07 2004-03-24 Hoffmann La Roche Derivados n-monoacilados de o-fenilendiaminas, sus analogos heterociclicos de seis miembros y su uso como agentes farmaceuticos
US6806272B2 (en) 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
CN1578663B (zh) * 2001-09-14 2011-05-25 梅特希尔基因公司 组蛋白脱乙酰化酶抑制剂
JP2003137866A (ja) 2001-11-01 2003-05-14 Sankyo Co Ltd フェニレンジアミン誘導体
PL220783B1 (pl) 2002-03-13 2016-01-29 Janssen Pharmaceutica Nv Pochodna sulfonylowa, jej zastosowanie i sposób wytwarzania oraz kompozycja farmaceutyczna
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
US20040072770A1 (en) 2002-07-03 2004-04-15 Besterman Jeffrey M. Methods for specifically inhibiting histone deacetylase-7 and 8
JP2004035485A (ja) 2002-07-04 2004-02-05 Mitsui Chemicals Inc テロメラーゼ阻害剤
US20050215601A1 (en) 2002-09-25 2005-09-29 Santen Pharmaceutical Co., Ltd. Therapeutic agent for rheumatic disease comprising benzamide derivative as active ingredient
CN100448844C (zh) 2002-10-17 2009-01-07 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
CA2503119A1 (en) 2002-10-25 2004-05-13 Genesoft Pharmaceuticals, Inc. Anti-infective biaryl compounds
US6852748B1 (en) 2002-10-30 2005-02-08 Boehringer Ingelheim Pharmaceuticals, Inc. Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
TW200426138A (en) 2002-12-10 2004-12-01 Hoffmann La Roche Novel arylene-carboxylic acid (2-amino-phenyl)-amide derivatives, their manufacture and use as pharmaceutical agents
AU2003292888A1 (en) 2002-12-27 2004-07-22 Schering Aktiengesellschaft Pharmaceutical combinations of phthalazine vegf inhibitors and benzamide hdac inhibitors
US7208491B2 (en) 2003-02-07 2007-04-24 Hoffmann-La Roche Inc. N-monoacylated o-phenylenediamines
PL379553A1 (pl) 2003-02-10 2006-10-16 Amgen Inc. Ligandy receptora waniloidowego oraz ich zastosowanie w leczeniu
US7244751B2 (en) 2003-02-14 2007-07-17 Shenzhen Chipscreen Biosciences Ltd. Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity
US7030112B2 (en) 2003-03-25 2006-04-18 Bristol-Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
TW200424187A (en) 2003-04-04 2004-11-16 Hoffmann La Roche New oxime derivatives and their use as pharmaceutically active agents
GB0315203D0 (en) 2003-06-28 2003-08-06 Celltech R&D Ltd Chemical compounds
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
RU2396250C2 (ru) 2003-07-24 2010-08-10 Лео Фарма А/С Новые производные аминобензофенона
AU2004276337B2 (en) * 2003-09-24 2009-11-12 Methylgene Inc. Inhibitors of histone deacetylase
US7141596B2 (en) 2003-10-08 2006-11-28 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
ES2562778T3 (es) 2003-12-02 2016-03-08 The Ohio State University Research Foundation Ácidos grasos de cadena corta unidos a motivos quelantes de Zn2+ como una clase novedosa de inhibidores de histona deacetilasa
EP1541549A1 (en) 2003-12-12 2005-06-15 Exonhit Therapeutics S.A. Tricyclic hydroxamate and benzaminde derivatives, compositions and methods
EP2272827A1 (en) 2004-03-11 2011-01-12 4Sc Ag Sulphonylpyrroles as hdac inhibitors
KR101156406B1 (ko) 2004-03-25 2012-06-13 아스텔라스세이야쿠 가부시키가이샤 솔리페나신 또는 그의 염의 고형 제제용 조성물
AU2005225471B2 (en) * 2004-03-26 2011-05-12 Methylgene Inc. Inhibitors of histone deacetylase
JP2008502719A (ja) 2004-05-21 2008-01-31 メルク　エンド　カムパニー　インコーポレーテッド アミノシクロペンチル複素環および炭素環系ケモカイン受容体活性調節剤
EP1758847A1 (en) 2004-06-10 2007-03-07 Cancer Research Technology Limited Inhibitors of histone deacetylase
WO2006005955A1 (en) 2004-07-12 2006-01-19 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Amide derivatives as inhibitors of histone deacetylase
ATE468853T1 (de) 2004-07-22 2010-06-15 Merck Sharp & Dohme Substituierte pyrazole, derartige verbindungen enthaltende zusammensetzungen und verfahren zu ihrer verwendung
US8710038B2 (en) 2004-09-17 2014-04-29 Exelixis, Inc. Pyrazole kinase modulators and methods of use
CN101080389A (zh) 2004-10-15 2007-11-28 拜尔药品公司 具有抗增殖活性的茚满酰胺
CN100349070C (zh) 2004-11-25 2007-11-14 同济大学 一种偶氮/酞菁复合单层有机光电导体及其制备方法
CA2590294A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
EP1824831A2 (en) 2004-12-16 2007-08-29 Takeda San Diego, Inc. Histone deacetylase inhibitors
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
EA201100689A1 (ru) 2005-03-15 2011-10-31 4Сц Аг N-сульфонилпирролы и их применение в качестве ингибиторов гистондезацетилазы
US20060223807A1 (en) 2005-03-29 2006-10-05 University Of Massachusetts Medical School, A Massachusetts Corporation Therapeutic methods for type I diabetes
US20060264415A1 (en) 2005-04-01 2006-11-23 Methylgene Inc. Inhibitors of histone deacetylase
EP1868994B1 (en) * 2005-04-07 2011-05-25 4Sc Ag Sulfonylpyrroles as histone deacetylase inhibitors
US7834034B2 (en) * 2005-04-20 2010-11-16 Merck Sharp & Dohme Corp. Benzothiophene derivatives
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP4528918B2 (ja) 2005-06-21 2010-08-25 学校法人 関西大学 カルボキサミド誘導体
EP1896395B1 (en) 2005-06-24 2015-07-15 Merck Sharp & Dohme Corp. Modified malonate derivatives
EP1904452A2 (en) 2005-07-14 2008-04-02 Takeda San Diego, Inc. Histone deacetylase inhibitors
CA2620414A1 (en) 2005-08-26 2007-03-01 Methylgene Inc. Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase
KR20080052630A (ko) 2005-09-01 2008-06-11 어레이 바이오파마 인크. Ｒａｆ 억제제 화합물 및 그의 사용 방법
EP1928872B1 (en) 2005-09-21 2012-03-14 4Sc Ag Novel sulphonylpyrroles as inhibitors of hdac
NZ566073A (en) 2005-09-21 2011-08-26 4Sc Ag Sulphonylpyrrole hydrochloride salts as histone deacetylases inhibitors
WO2007044565A2 (en) 2005-10-06 2007-04-19 University Of Massachusetts Composition and synthesis of new reagents for inhibition of hiv replication
GB0521244D0 (en) 2005-10-19 2005-11-30 Astrazeneca Ab Benzamide compounds
US20090105264A1 (en) 2005-11-03 2009-04-23 Christopher Hamblett Substituted Nicotinamide Compounds
US20070219244A1 (en) 2005-11-11 2007-09-20 The Scripps Research Institute Histone deacetylase inhibitors as therapeutics for neurological diseases
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
WO2007087130A2 (en) 2006-01-12 2007-08-02 Merck & Co., Inc. Hydroxyalkylarylamide derivatives
AU2007208494A1 (en) 2006-01-12 2007-08-02 Merck Sharp & Dohme Corp. Fluorinated arylamide derivatives
JP2009525955A (ja) 2006-01-13 2009-07-16 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
JP5225104B2 (ja) 2006-01-19 2013-07-03 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 新しい、ヒストンデアセチラーゼのインヒビターとしてのアミノフェニル誘導体
AU2007206950B2 (en) 2006-01-19 2012-02-02 Janssen Pharmaceutica N.V. Substituted indolyl-alkyl-amino-derivatives as inhibitors of histone deacetylase
JP5137848B2 (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ピリジン及びピリミジン誘導体
CN101374828B (zh) 2006-01-19 2012-09-19 詹森药业有限公司 作为组蛋白脱乙酰酶抑制剂的杂环烷基衍生物
EP1979326B1 (en) 2006-01-19 2012-10-03 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
AU2007221207A1 (en) 2006-02-28 2007-09-07 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase
GB0606876D0 (en) 2006-04-05 2006-05-17 Glaxo Group Ltd Compounds
US8598168B2 (en) 2006-04-07 2013-12-03 Methylgene Inc. Inhibitors of histone deacetylase
JP2009537529A (ja) 2006-05-18 2009-10-29 メルク エンド カムパニー インコーポレーテッド アリール縮合スピロ環化合物
GB0614070D0 (en) 2006-07-14 2006-08-23 Glaxo Group Ltd Compounds
JP2009544611A (ja) 2006-07-20 2009-12-17 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阻害剤としてのリン誘導体
US8653278B2 (en) 2006-08-03 2014-02-18 Georgetown University Isoform selective HDAC inhibitors
CA2663147A1 (en) 2006-09-11 2008-03-20 Curis, Inc. Substituted 2-indolinone as ptk inhibitors containing a zinc binding moiety
CA2662937A1 (en) 2006-09-11 2008-03-20 Curis, Inc. Multi-functional small molecules as anti-proliferative agents
CA2672192A1 (en) 2006-12-19 2008-06-26 Methylgene Inc. Inhibitors of histone deacetylase and prodrugs thereof
US8076332B2 (en) 2006-12-26 2011-12-13 Santen Pharmaceutical Co., Ltd. N- (2-aminophenyl) benzamide derivative having urea structure
WO2008084218A1 (en) 2007-01-12 2008-07-17 Boehringer Ingelheim International Gmbh Benzazole derivatives for the treatment of inflammations
TW200911757A (en) 2007-01-18 2009-03-16 Takeda San Diego Inc Crystalline forms of histone deacetylase inhibitors
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
NZ598251A (en) 2007-03-14 2013-06-28 Exelixis Patent Co Llc 2-Arylamino-pyridopyrimidines and their uses, particularly in the treatment of cancer
CN101730703B (zh) 2007-03-16 2012-12-26 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
CA2680517A1 (en) 2007-03-28 2008-10-02 Santen Pharmaceutical Co., Ltd. Novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having urea structure
CA2680838A1 (en) 2007-03-28 2008-10-16 Santen Pharmaceutical Co., Ltd. Intraocular pressure-lowering agent comprising compound having histone deacetylase inhibitory effect as active ingredient
JP5746860B2 (ja) 2007-04-09 2015-07-08 メチルジーン インコーポレイテッド ヒストンデアセチラーゼ阻害剤
CA2690192A1 (en) 2007-06-26 2008-12-31 Gilead Colorado, Inc. Imidazopyridinyl thiazolyl histone deacetylase inhibitors
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
JP4567099B2 (ja) 2007-06-29 2010-10-20 ファイザー・インク ベンズイミダゾール誘導体
US20100267779A1 (en) 2007-07-23 2010-10-21 Syndax Pharmaceuticals, Inc. Novel Compounds and Methods of Using Them
US20110130361A1 (en) 2007-08-09 2011-06-02 Jonathan Grimm Silicon derivatives as histone deacetylase inhibitors
US20120004222A1 (en) 2007-08-21 2012-01-05 Zhicai Wu Cb2 receptor ligands for the treatment of pain
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
TW200918521A (en) 2007-08-31 2009-05-01 Astrazeneca Ab Heterocyclic amides and methods of use thereof
WO2009036057A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Antiproliferative agents containing a zinc binding moiety
WO2009033281A1 (en) 2007-09-14 2009-03-19 Methylgene Inc. Cancer combination therapy with a selective inhibitor of histone deacetylase hdac1, hdac2 and/or hdac3 and a microtubule stabilizer
AU2008300827B2 (en) 2007-09-19 2013-04-04 4Sc Ag Novel tetrahydrofusedpyridines as histone deacetylase inhibitors
WO2009045440A1 (en) 2007-10-01 2009-04-09 Lixte Biotechnology Holdings, Inc. Hdac inhibitors
NZ584845A (en) 2007-10-22 2011-09-30 Orchid Res Lab Ltd Histone deacetylase inhibitors
EP2060565A1 (en) 2007-11-16 2009-05-20 4Sc Ag Novel bifunctional compounds which inhibit protein kinases and histone deacetylases
EP2220066A1 (en) 2007-12-14 2010-08-25 Gilead Colorado, Inc. Benzofuran anilide histone deacetylase inhibitors
WO2009086012A1 (en) 2007-12-20 2009-07-09 Curis, Inc. Aurora inhibitors containing a zinc binding moiety
EP2100882A1 (en) 2008-03-12 2009-09-16 4Sc Ag (E) -N -(2-Amino-phenyl) -3-{1-[4-(1-methyl-1H-pyrazol-4-yl)- benzenesulfonyl]-1H-pyrrol-3-yl} -acrylamide salts
AU2009264242A1 (en) 2008-06-27 2009-12-30 Novartis Ag Organic compounds
US8134000B2 (en) 2008-07-14 2012-03-13 Gilead Sciences, Inc. Imidazolyl pyrimidine inhibitor compounds
US8344018B2 (en) 2008-07-14 2013-01-01 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
JP5640006B2 (ja) 2008-07-14 2014-12-10 ギリアード サイエンシーズ， インコーポレイテッド ヒストン脱アセチル化酵素および／またはサイクリン依存性キナーゼの縮合複素環式阻害剤
JP2011529504A (ja) 2008-07-28 2011-12-08 ギリアード サイエンシーズ， インコーポレイテッド シクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物およびヘテロシクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物
US9265734B2 (en) 2008-09-03 2016-02-23 Biomarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
KR20110055715A (ko) 2008-09-05 2011-05-25 엘란 파마슈티칼스, 인크. Ｎ-설폰아미도 폴리사이클릭 피라졸릴 화합물
US8202866B2 (en) 2008-09-17 2012-06-19 Hoffmann-La Roche Inc. Ortho-aminoanilides for the treatment of cancer
UY32158A (es) 2008-10-03 2010-04-30 Astrazeneca Ab Derivados heterociclicos y metodos de uso de los mismos
US20110212943A1 (en) 2008-10-15 2011-09-01 Orchid Research Laboratories Limited Novel bridged cyclic compounds as histone deacetylase inhibitors
EP2349245B1 (en) 2008-10-29 2016-08-03 Istituto Superiore di Sanità Treatment of latent hiv-1 infections using auranofin or arsenic trioxide
AU2010215524A1 (en) 2009-02-23 2011-06-30 F. Hoffmann-La Roche Ag Novel ortho-aminoamides for the treatment of cancer
KR101145345B1 (ko) 2009-04-24 2012-07-09 계명대학교 산학협력단 세포증식 억제제로서 유용한 2-싸이오-4-아미노 피리미딘 유도체 및 그 제조방법
JP5807971B2 (ja) 2009-04-27 2015-11-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｘｃｒ３受容体アンタゴニスト
US8362249B2 (en) 2009-04-27 2013-01-29 Boehringer Ingelheim International Gmbh CXCR3 receptor antagonists
WO2010127152A2 (en) 2009-04-29 2010-11-04 Irm Llc Compounds and compositions as microsomal prostaglandin e synthase-1 inhibitors
US8716326B2 (en) 2009-05-15 2014-05-06 Korea Research Institute Of Chemical Technology Isoindolinone derivatives, preparation method thereof and a pharmaceutical composition comprising same
US8211901B2 (en) 2009-05-22 2012-07-03 Shenzhen Chipscreen Biosciences Ltd. Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
AU2010259042A1 (en) 2009-06-08 2011-12-15 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
KR20120031170A (ko) 2009-06-08 2012-03-30 길리애드 사이언시즈, 인코포레이티드 알카노일아미노 벤즈아미드 아닐린 ｈｄａｃ 저해제 화합물
CN101648922B (zh) 2009-08-20 2011-08-31 苏州东南药物研发有限责任公司 苯甲酰胺类组蛋白去乙酰酶抑制剂及其用途
WO2012016081A2 (en) * 2010-07-30 2012-02-02 The Regents Of The University Of California Method and therapeutic for the treatment and regulation of memory formation
CA2828524C (en) 2011-02-28 2020-01-07 Repligen Corporation Histone deacetylase inhibitors
US8957066B2 (en) * 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors

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