AR105911A1 - Inhibidores de hdac8 bicíclicos fusionados [6,6] - Google Patents

Inhibidores de hdac8 bicíclicos fusionados [6,6]

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AR105911A1
AR105911A1 ARP160102695A ARP160102695A AR105911A1 AR 105911 A1 AR105911 A1 AR 105911A1 AR P160102695 A ARP160102695 A AR P160102695A AR P160102695 A ARP160102695 A AR P160102695A AR 105911 A1 AR105911 A1 AR 105911A1
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Argentina
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alkyl
heterocycle
cycloalkyl
heteroaryl
aryl
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ARP160102695A
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English (en)
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W Bair Kenneth
Barczak Nicholas
Lancia David Jr
Rudnitskaya Aleksandra
Liu Cuixian
Zablocki Mary
R Margaret - Thomason Jennifer
Han Bingsong
Yee Ng Pui
Zheng Xiaozhang
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Forma Therapeutics Inc
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Publication of AR105911A1 publication Critical patent/AR105911A1/es

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Abstract

Reivindicación 1: Un compuesto de la fórmula (1), y sus sales, profármacos, solvatos, hidratos, isómeros o tautómeros farmacéuticamente aceptables, en donde: Y¹, Y², Y³ e Y⁴ son cada uno, de modo independiente, N, C o CR³, siempre que, cuando unidos a -C(O)NHOH, cualquiera de Y¹, Y², Y³ o Y⁴ sea C; X se selecciona del grupo que consiste en S(O)₂, S(O), S, O, C(=O) y C(R⁴)(R⁵); W es C(R⁴)(R⁵) u O; R¹ es, de modo independiente, alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, arilo, heteroarilo, heterociclo de 3 a 8 miembros, -(CH₂)ₙ-Rᵃ, -(CH₂)ₙ-O-(CH₂)ₚ-Rᵃ, -S(O)₂Rᵃ, -C(O)Rᵃ, o -C(O)N(Rᵃ)(Rᵇ), en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo o heterociclo está opcionalmente sustituido con uno o más -OH, halógeno, oxo, -NO₂, -NH₂, -CN, -alquilo C₁₋₆, -alcoxi C₁₋₆, heterociclo, arilo, heteroarilo, o R⁴; Rᵃ es, en cada ocurrencia, hidrógeno, halógeno, OH, NH₂, alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, arilo, heteroarilo, heterociclo de 3 a 8 miembros, o -C(O)N(R¹⁰)(R¹¹), en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo, o heterociclo es opcionalmente sustituido con uno o más -OH, R⁴’, R⁵’, halógeno, oxo, (CH₂)ₙOR⁶, -NO₂, -OR⁶, -N(R⁶)(R⁷), C(O)OR⁶, -C(O)N(R⁶)(R⁷), -S(O)₂R⁶, -S(O)R⁶, -S(R⁶), -C(O)R⁶, S(O)₂N(R⁶)(R⁷), -CN, alquilo -C₁₋₆, haloalquilo -C₁₋₆, alcoxi -C₁₋₆, alquilamino C₁₋₆, dialquilamino C₁₋₆, hidroxialquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilalquilo C₃₋₈, arilalquilo, heterociclo, arilo, o heteroarilo; Rᵇ es, en cada ocurrencia, hidrógeno, halógeno, OH, NH₂, alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, arilo, heteroarilo, heterociclo de 3 a 8 miembros, o -C(O)N(R¹⁰)(R¹¹), en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo, o heterociclo es opcionalmente sustituido con uno o más -OH, R⁴’, R⁵’, halógeno, oxo, (CH₂)ₙOR⁶, -NO₂, -OR⁶, -N(R⁶)(R⁷), C(O)OR⁶, -C(O)N(R⁶)(R⁷), -S(O)₂R⁶, -S(O)R⁶, -S(R⁶), -C(O)R⁶, -S(O)₂N(R⁶)(R⁷), -CN, alquilo -C₁₋₆, haloalquilo -C₁₋₆, alcoxi -C₁₋₆, alquilamino C₁₋₆, dialquilamino C₁₋₆, hidroxialquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilalquilo C₃₋₈, arilalquilo, heterociclo, arilo, o heteroarilo; o Rᵃ y Rᵇ se pueden combinar con el carbono o nitrógeno al que están unidos para formar un cicloalquilo C₃₋₈ o heterociclo de 3 a 8 miembros opcionalmente sustituido con uno o más sustituyentes seleccionados de R⁴’ y R⁵’, en donde R⁴’ y R⁵’ de modo independiente en cada ocurrencia son H o alquilo -C₁₋₆; R² y R²’ son, de modo independiente, hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, -OH, halógeno, -NO₂, -NH₂, -CN, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, arilo, heteroarilo, heterociclo de 3 a 8 miembros, en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo o heterociclo está opcionalmente sustituido con uno o más -OH, halógeno, oxo, -NO₂, -NH₂, -CN, -alquilo C₁₋₆, -alcoxi C₁₋₆; o R² y R²’ se pueden combinar con el carbono al que están unidos para formar un grupo oxo, cicloalquilo C₃₋₈ o heterociclo de 3 a 8 miembros; R³ es, de modo independiente, en cada aparición, hidrógeno, halógeno, OH, CN, NO₂, NH₂, alquilo C₁₋₃ o alcoxi C₁₋₃; cada R⁴ o R⁵ es cada uno, de modo independiente, en cada aparición, hidrógeno, halógeno, OH, NH₂, alquilo C₁₋₆, alcoxi C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₄₋₈, arilo, heteroarilo, heterociclo de 3 a 8 miembros o -C(O)N(R¹⁰)(R¹¹), en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo o heterociclo está opcionalmente sustituido con uno o más -OH, R⁴’, R⁵’, halógeno, oxo, -(CH₂)ₙOR⁶, -NO₂, -OR⁶, -N(R⁶)(R⁷), C(O)OR⁶, -C(O)N(R⁶)(R⁷), -S(O)₂R⁶, -S(O)R⁶, -S(R⁶), -C(O)R⁶, -S(O)₂N(R⁶)(R⁷), -CN, -alquilo C₁₋₆, -haloalquilo C₁₋₆, -alcoxi C₁₋₆, alquil C₁₋₆-amino, dialquil C₁₋₆-amino, hidroxi C₁₋₆-alquilo, cicloalquilo C₃₋₈, cicloalquil C₃₋₈-alquilo, arilalquilo, heterociclo, arilo o heteroarilo; o R⁴ y R⁵ se pueden combinar con el carbono o nitrógeno al que están unidos para formar un grupo oxo, cicloalquilo C₃₋₈ o heterociclo de 3 a 8 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados de R⁴’ y R⁵’, en donde R⁴’ y R⁵’, de modo independiente, en cada ocurrencia, son H o alquilo -C₁₋₆; o R⁴’ y R⁵’ juntos cuando se unen al mismo átomo forman un anillo spirocicloalquilo C₃₋₈; o R⁴’ y R⁵’ juntos cuando se unen al mismo átomo forman un anillo spiroheterocicloalquilo C₃₋₈; o R⁴’ y R⁵’ juntos cuando se unen a átomos adyacentes forman un anillo arilo, un anillo heteroarilo, un anillo cicloalquilo C₃₋₈, o un heterociclo de 3 a 8 miembros, en donde el spirocicloalquilo, spiroheterocicloalquilo, heteroarilo, cicloalquilo o heterociclo son sustituidos opcionalmente con uno o más grupos seleccionados de OH, halógeno, alquilo -C₁₋₆ o C(O)OR⁶; R⁶ y R⁷ están seleccionados cada uno, de modo independiente, del grupo que consiste en hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, alcoxi C₁₋₆, amino, alquilamino C₁₋₆, dialquilamino C₁₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₃₋₈, arilo, heteroarilo, heterociclo, -S(O)₂NR⁸R⁹, -S(O)₂R⁸, -C(O)R⁸, -CO₂R⁸, -S(O)R⁸ o -S(O)NR⁸R⁹, en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, fenilo, heteroarilo o heterociclo está opcionalmente sustituido con uno o más -OH, halógeno, oxo, -NO₂, -NH₂, -CN, -alquilo C₁₋₆, -alcoxi C₁₋₆, alquil C₁₋₆-amino, dialquil C₁₋₆-amino, hidroxi C₁₋₆-alquilo, heterociclo, arilo, heteroarilo; o R⁶ y R⁷ junto con un átomo al que están unidos forman un cicloalquilo C₃₋₈ o un heterociclo de 3 a 8 miembros, en donde el cicloalquilo o el heterociclo es sustituido opcionalmente con uno o más grupos seleccionados de halógeno, oxo y alquilo C₁₋₆; R⁸ y R⁹ son cada uno, de modo independiente, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₃₋₈, heteroarilo o heterociclo de 3 a 8 miembros, en donde cada uno está opcionalmente sustituido con uno o más -OH, halógeno, oxo, -NO₂, -NH₂, -CN, -alquilo C₁₋₆, -alcoxi C₁₋₆, alquil C₁₋₆-amino, dialquil C₁₋₆-amino, hidroxi C₁₋₆-alquilo, heterociclo, arilo o heteroarilo; R¹⁰ y R¹¹ son cada uno, de modo independiente, hidrógeno, alquilo C₁₋₆, arilo, alquil C₁₋₆-arilo o heterociclo de 3 a 8 miembros; en donde arilo, arilalquilo y heterociclo son sustituidos opcionalmente con uno o más grupos seleccionados de halógeno, alquilo C₁₋₆, y alcoxi C₁₋₆; o R¹⁰ y R¹¹ se pueden combinar para formar un heterociclo de 3 a 8 miembros opcionalmente sustituido con uno o más R¹²; R¹² es H o alquilo C₁₋₆ o dos adyacentes R¹² se pueden combinar para formar un grupo arilo o heteroarilo; n es un número entero de 1 a 6; y p es un número entero de 0 a 2; siempre que el compuesto no sea N-hidroxi-1-((4-metoxifenil)sulfonil)-1,2,3,4-tetrahidroquinolin-6-carboxamida.
ARP160102695A 2015-09-03 2016-09-02 Inhibidores de hdac8 bicíclicos fusionados [6,6] AR105911A1 (es)

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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160083343A1 (en) 2013-03-15 2016-03-24 Global Blood Therapeutics, Inc Compounds and uses thereof for the modulation of hemoglobin
EA201992707A1 (ru) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
MX2017011778A (es) 2015-03-13 2017-12-04 Forma Therapeutics Inc Compuestos y composiciones de alfa-cinamida como inhibidores de histona desacetilasa 8 (hdac8).
TW201711999A (zh) 2015-09-03 2017-04-01 佛瑪治療公司 ﹝６，６﹞稠合雙環組蛋白脫乙醯基酶８（ｈｄａｃ８）抑制劑
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
UA125730C2 (uk) 2017-06-22 2022-05-25 Курадев Фарма Лімітед Низькомолекулярні модулятори sting людини
EP3642184A1 (en) * 2017-06-22 2020-04-29 Curadev Pharma Limited Small molecule modulators of human sting
JP2020530443A (ja) * 2017-07-24 2020-10-22 イソキュア バイオサイエンシーズ インク． 突然変異体イソクエン酸デヒドロゲナーゼの阻害剤、及びその組成物、並びに方法
GB2568549A (en) * 2017-11-21 2019-05-22 Univ Leicester New compounds and uses
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
CN109761968A (zh) * 2018-12-25 2019-05-17 河南师范大学 具有抗肿瘤活性的丹皮酚并苯并噁嗪类化合物及其制备方法和应用
CR20220363A (es) 2019-12-27 2022-09-23 Lupin Ltd Compuestos tricíclicos sustituidos
US20240051931A1 (en) * 2020-12-03 2024-02-15 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Hdac inhibitors

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5234923A (en) 1991-12-16 1993-08-10 E. R. Squibb & Sons, Inc. Substitute indole and benzimidazole derivatives
WO1993015066A1 (en) 1992-01-23 1993-08-05 Pfizer Inc. Benzopyran and related ltb4 antagonists
US5312820A (en) 1992-07-17 1994-05-17 Merck & Co., Inc. Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5393771A (en) 1993-05-12 1995-02-28 Brisol-Myers Squibb Company 4-substituted benzopyran and related compounds
AU704114B2 (en) 1993-11-18 1999-04-15 Siga Technologies, Inc. Compounds and pharmaceutical compositions for the treatment and prophylaxis of bacterial infections
KR0125117B1 (ko) 1994-06-15 1997-12-05 성재갑 항 에이즈(aids)효과를 갖는 신규한 인간 면역 결핍 바이러스(hiv)프로테아제 억제 화합물 및 그의 제조방법
MY113463A (en) 1994-01-04 2002-03-30 Novo Nordisk As Novel heterocyclic compounds
CA2201742A1 (en) 1994-10-13 1996-04-25 Anthony Daniel Piscopio Benzopyran and benzo-fused compounds, their preparation and their use as leukotriene b4 (ltb4) antagonists
EP0785935A1 (en) 1994-10-13 1997-07-30 Pfizer Inc. Benzopyran and benzo-fused compounds, their preparation and their use as leukotriene b4' (ltb4) antagonists
CA2217194A1 (en) 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
WO1996031473A1 (en) 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
WO1996031500A1 (en) 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
WO1996031470A1 (en) 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
WO1996031503A1 (en) 1995-04-07 1996-10-10 Novo Nordisk A/S Novel heterocyclic compounds
DE69622031T2 (de) 1995-04-10 2002-12-12 Fujisawa Pharmaceutical Co INDOLDERIVATE ALS cGMP-PDE INHIBITOREN
AU3166897A (en) 1996-06-24 1998-01-14 Novo Nordisk A/S Factor vii-binding reagent
JPH10259176A (ja) * 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
US6461610B1 (en) 1997-07-18 2002-10-08 Novo Nordisk A/S Methods for modifying cell motility using factor VIIa or inactivated factor VIIa
EP1005361B1 (en) 1997-07-18 2010-01-06 Novo Nordisk Health Care AG USE OF FVIIa OR FVIIai FOR THE TREATMENT OF ENDOTHELIAL DYSFUNKTION AND FOR THE INHIBITION OF ANGIOGENESIS RESPECTIVELY
IL128731A0 (en) 1998-03-12 2000-01-31 Pfizer Prod Inc Method of preventing allograft rejection
EP0963755A3 (en) 1998-04-16 2001-03-14 Pfizer Products Inc. Use of benzopyranes for preventing allograft rejection
US6277885B1 (en) 1999-01-27 2001-08-21 American Cyanamid Company Acetylenic aryl sulfonamide and phosphinic acid amide hydroxamic acid TACE inhibitors
WO2000068230A1 (en) 1999-05-05 2000-11-16 Darwin Discovery Limited 9-(1,2,3,4-tetrahydronaphthalen-1-yl)-1,9-dihydropurin-6-one derivatives as pde7 inhibitors
EP1255743A1 (en) 2000-02-01 2002-11-13 Millenium Pharmaceuticals, Inc. 3,4-DIHYDRO-2H-BENZO[1,4]OXAZINE INHIBITORS OF FACTOR Xa
EP1255741A2 (en) 2000-02-01 2002-11-13 Cor Therapeutics, Inc. 2- 1H]-QUINOLONE AND 2- 1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
CA2399791A1 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
ATE309996T1 (de) 2000-09-11 2005-12-15 Chiron Corp Chinolinonderivate als tyrosin-kinase inhibitoren
AU2001293835A1 (en) 2000-09-25 2002-04-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives
AU2002306687A1 (en) 2001-03-13 2002-09-24 Glenmark Pharmaceuticals Limited Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them
US7615640B2 (en) 2002-07-29 2009-11-10 Mitsubishi PaperMillsLtd. Organic dye, photoelectric conversion material, semiconductor electrode and photoelectric conversion device
EP2374455A3 (en) 2004-08-19 2012-03-28 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
ITRM20050390A1 (it) 2005-07-22 2007-01-23 Giuliani Spa Composti e loro sali specifici per i recettori ppar ed i recettori per l'egf e loro uso in campo medico.
US7700592B2 (en) 2005-08-25 2010-04-20 Schering Corporation α2C adrenoreceptor agonists
WO2007024944A1 (en) 2005-08-25 2007-03-01 Schering Corporation Imidazole derivatives as functionally selective alpha2c adrenoreceptor agonists
US8003624B2 (en) 2005-08-25 2011-08-23 Schering Corporation Functionally selective ALPHA2C adrenoreceptor agonists
EP1940805A4 (en) 2005-08-26 2009-11-11 Methylgene Inc BENZODIAZEPIN AND BENZOPIPERAZINANALOGA AS INHIBITORS OF HISTONDEACETYLASE
US7858635B2 (en) 2005-12-22 2010-12-28 Vertex Pharmaceuticals Incorporated Spiro compounds as modulators of muscarinic receptors
WO2008030120A1 (en) 2006-09-07 2008-03-13 Auckland Uniservices Limited A method for the fluorescent detection of nitroreductase activity using nitro-substituted aromatic compounds
JP5583406B2 (ja) 2006-10-28 2014-09-03 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の阻害剤
WO2008059339A2 (en) 2006-11-13 2008-05-22 Glenmark Pharmaceuticals S.A. Isoquinoline derivatives as vanilloid receptor modulators
WO2008124300A1 (en) 2007-04-10 2008-10-16 National Health Research Institutes Hepatitis c virus inhibitors
WO2008141980A1 (en) 2007-05-24 2008-11-27 Basf Se Substituted amino-thiourea compounds for combating animal pests
US9493419B2 (en) 2007-08-21 2016-11-15 The Hong Kong Polytechnic University Quinoline derivatives as anti-cancer agents
US20090136461A1 (en) 2007-11-28 2009-05-28 Moon Suk Kim Neuronal differentiation method of adult stem cells using small molecules
MY155517A (en) 2008-03-31 2015-10-30 C&C Res Lab Heterocyclic derivatives
GB0818366D0 (en) 2008-10-07 2008-11-12 Argenta Discovery Ltd Quinolin-2-one-compounds
KR101051057B1 (ko) 2008-11-11 2011-07-21 한국화학연구원 신경전구세포 또는 줄기세포의 신경세포로의 분화 유도용 조성물 및 방법
TW201022279A (en) 2008-11-14 2010-06-16 Astrazeneca Ab Chemical compounds
US8791090B2 (en) 2009-03-31 2014-07-29 Kowa Company, Ltd. Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient
WO2011002520A2 (en) 2009-07-02 2011-01-06 Angion Biomedica Corp. Small molecule inhibitors of parp activity
JP2011148714A (ja) 2010-01-19 2011-08-04 Nippon Soda Co Ltd 病害防除方法
JP2013525400A (ja) 2010-04-28 2013-06-20 バイエル・クロップサイエンス・アーゲー 殺菌剤ヒドロキシモイル−複素環誘導体
WO2012001040A1 (en) 2010-07-02 2012-01-05 Syngenta Participations Ag Novel microbiocidal dioxime ether derivatives
WO2012009258A2 (en) 2010-07-13 2012-01-19 Edward Roberts Peptidomimetic galanin receptor modulators
RU2577861C2 (ru) 2010-09-09 2016-03-20 Ф. Хоффманн-Ля Рош Аг N-гидрокси-бензамиды для лечения рака
US8765773B2 (en) 2010-10-18 2014-07-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2012117421A1 (en) 2011-03-02 2012-09-07 Orchid Research Laboratories Ltd Histone deacetylase inhibitors
WO2012117021A2 (en) 2011-03-03 2012-09-07 Syngenta Participations Ag Novel microbiocidal oxime ethers
WO2012137224A1 (en) 2011-04-05 2012-10-11 University Of Delhi Coumarin compounds for the treatment of mycobacterial infections
KR102036199B1 (ko) 2011-08-17 2019-10-24 메르크 앤드 씨에 알부민-결합 개체들의 폴레이트 공액체들
WO2013026842A1 (en) 2011-08-22 2013-02-28 Merck & Cie 18f-saccharide-folates
WO2013059582A2 (en) * 2011-10-20 2013-04-25 Nupotential, Inc. Small molecule inhibitors of histone deacteylases
WO2013059852A1 (en) 2011-10-25 2013-05-02 Kernaghan Gregory Lawrence Method of improving the acoustic response of musical instruments
WO2013092460A1 (en) 2011-12-20 2013-06-27 Syngenta Participations Ag Cyclic bisoxime microbicides
CA2876370A1 (en) 2012-07-12 2014-01-16 Viiv Healthcare Uk Limited Compounds and methods for treating hiv
EP2970127B1 (en) 2013-03-14 2018-10-24 Glaxosmithkline Intellectual Property (No. 2) Limited 2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
JP2016147807A (ja) 2013-06-04 2016-08-18 日本理化学工業株式会社 ヒドロキサム酸誘導体またはその塩
TW201636329A (zh) 2015-02-02 2016-10-16 佛瑪治療公司 作為ｈｄａｃ抑制劑之雙環［４，６，０］異羥肟酸
CA2975605C (en) 2015-02-02 2023-12-12 Forma Therapeutics, Inc. 3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors
MX2017011778A (es) 2015-03-13 2017-12-04 Forma Therapeutics Inc Compuestos y composiciones de alfa-cinamida como inhibidores de histona desacetilasa 8 (hdac8).
TW201643139A (zh) 2015-04-17 2016-12-16 佛瑪治療公司 作為組蛋白脫乙醯基酶抑制劑之３－螺環－６－異羥肟酸萘滿
TW201711999A (zh) 2015-09-03 2017-04-01 佛瑪治療公司 ﹝６，６﹞稠合雙環組蛋白脫乙醯基酶８（ｈｄａｃ８）抑制劑
EP3472131B1 (en) 2016-06-17 2020-02-19 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors

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