AU2014244426B2 - Methods and compositions for inhibition of bromodomain-containing proteins - Google Patents

Methods and compositions for inhibition of bromodomain-containing proteins Download PDF

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AU2014244426B2
AU2014244426B2 AU2014244426A AU2014244426A AU2014244426B2 AU 2014244426 B2 AU2014244426 B2 AU 2014244426B2 AU 2014244426 A AU2014244426 A AU 2014244426A AU 2014244426 A AU2014244426 A AU 2014244426A AU 2014244426 B2 AU2014244426 B2 AU 2014244426B2
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substituted
unsubstituted
alkyl
compound
hydrogen
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AU2014244426A1 (en
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Janak Khimchand Padia
Jeffrey William STROVEL
Hariprasad Vankayalapati
Makoto Yoshioka
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ConverGene LLC
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ConverGene LLC
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C217/78—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C217/80—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
    • C07C217/82—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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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    • 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
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    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/20—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 4
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    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
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    • 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
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2014244426A 2013-03-14 2014-03-13 Methods and compositions for inhibition of bromodomain-containing proteins Ceased AU2014244426B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361781988P 2013-03-14 2013-03-14
US61/781,988 2013-03-14
PCT/US2014/025289 WO2014159837A1 (en) 2013-03-14 2014-03-13 Methods and compositions for inhibition of bromodomain-containing proteins

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AU2014244426A1 AU2014244426A1 (en) 2015-10-22
AU2014244426B2 true AU2014244426B2 (en) 2019-02-28

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EP (1) EP2968360B1 (cg-RX-API-DMAC10.html)
JP (1) JP6464139B2 (cg-RX-API-DMAC10.html)
KR (1) KR20150135359A (cg-RX-API-DMAC10.html)
CN (1) CN105407894A (cg-RX-API-DMAC10.html)
AU (1) AU2014244426B2 (cg-RX-API-DMAC10.html)
BR (1) BR112015022417A2 (cg-RX-API-DMAC10.html)
CA (1) CA2905451A1 (cg-RX-API-DMAC10.html)
EA (1) EA201591746A1 (cg-RX-API-DMAC10.html)
HK (1) HK1222793A1 (cg-RX-API-DMAC10.html)
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Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2118074E (pt) 2007-02-01 2014-03-20 Resverlogix Corp Compostos para a prevenção e tratamento de doenças cardiovasculares
NZ617779A (en) 2009-03-18 2015-08-28 Resverlogix Corp Novel anti-inflammatory agents
PT2773354T (pt) 2011-11-01 2019-07-17 Resverlogix Corp Formulações orais de libertação imediata para quinazolinonas substituídas
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
JP2016507496A (ja) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションZenith Epigenetics Corp. ブロモドメイン阻害剤としての新規複素環式化合物
US9353122B2 (en) 2013-02-15 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
US9353123B2 (en) 2013-02-20 2016-05-31 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
EA201591746A1 (ru) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
EA027139B1 (ru) * 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
CN105473581B (zh) 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
KR20160099084A (ko) 2013-11-01 2016-08-19 칼라 파마슈티컬스, 인크. 치료 화합물의 결정질 형태 및 그의 용도
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
ES2750452T3 (es) * 2013-11-26 2020-03-25 Gilead Sciences Inc Derivados de quinolina como inhibidores del bromodominio
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
KR102394518B1 (ko) 2014-01-09 2022-05-06 오리온 코포레이션 브로모도메인 억제제로서의 비사이클릭 헤테로사이클릭 유도체
SMT202000133T1 (it) 2014-04-23 2020-05-08 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
JP2017534653A (ja) * 2014-11-13 2017-11-24 コンバージーン・リミテッド・ライアビリティ・カンパニーConvergene Llc ブロモドメイン及びエキストラ末端タンパク質の阻害のための方法及び組成物
HK1245246A1 (zh) 2014-12-01 2018-08-24 恒翼生物医药科技(上海)有限公司 作为溴域抑制剂的取代吡啶酮
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
CA2968884A1 (en) * 2014-12-10 2016-06-16 Massachusetts Institute Of Technology Fused 1,3-azole derivatives useful for the treatment of proliferative diseases
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US10577349B2 (en) 2015-03-02 2020-03-03 Sanford Burnham Prebys Medical Discovery Institute Quinolinones as inhibitors of translation initiation complex
CN114984016A (zh) 2015-03-13 2022-09-02 雷斯韦洛吉克斯公司 用于治疗补体相关疾病之组合物及治疗方法
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AU2016245864C1 (en) 2015-04-10 2021-09-09 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
JP2018522871A (ja) * 2015-07-02 2018-08-16 オリオン コーポレーション ブロモドメイン阻害剤としての二環式複素環誘導体
HK1249105A1 (zh) 2015-07-17 2018-10-26 富士胶片富山化学株式会社 含氮杂环化合物
CN108026046B (zh) * 2015-07-22 2021-12-21 亚瑞克西斯制药公司 取代的喹唑啉化合物及其作为g12c突变体kras、hras和/或nras蛋白质的抑制剂的用途
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
JP6869947B2 (ja) * 2015-07-22 2021-05-12 アラクセス ファーマ エルエルシー 置換キナゾリン化合物ならびにそのg12c変異kras、hrasおよび/またはnrasタンパク質の阻害剤としての使用
CN108137547B (zh) 2015-08-03 2021-11-12 百时美施贵宝公司 可用作TNFα调节剂的杂环化合物
HK1256753A1 (zh) 2015-08-11 2019-10-04 Neomed Institute 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CN114605387A (zh) 2015-08-12 2022-06-10 埃皮吉纳提克斯股份有限公司 取代的苯并咪唑、它们的制备和它们作为药物的用途
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Rasの阻害剤をスクリーニングするための方法
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
KR102932353B1 (ko) 2015-11-16 2026-02-27 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
EP3380469B1 (en) * 2015-11-25 2022-03-16 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
RU2018132559A (ru) 2016-02-16 2020-03-17 Массачусетс Инститьют Оф Текнолоджи Связывающие молекулы для max в качестве модуляторов myc и их применения
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3509421A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
WO2018048750A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
US10253036B2 (en) 2016-09-08 2019-04-09 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
CA3047098A1 (en) * 2016-12-16 2018-06-21 Jia Zhou Inhibitors of bromodomain-containing protein 4 (brd4)
EP3563851B1 (en) 2016-12-27 2021-04-21 FUJIFILM Corporation Antitumor agent and bromodomain inhibitor
CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
CN108658972A (zh) * 2017-03-28 2018-10-16 中国海洋大学 一种取代内酰胺类化合物及其制备方法和用途
CN108658855A (zh) * 2017-03-28 2018-10-16 中国海洋大学 一种含氮双环化合物及其制备方法和用途
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
US11389433B2 (en) 2018-06-18 2022-07-19 Board Of Regents, The University Of Texas System BRD4 inhibitor treatment of IgE-mediated diseases
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
US12503467B2 (en) 2018-12-10 2025-12-23 Ideaya Biosciences, Inc. 2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors
WO2020219168A1 (en) * 2019-04-24 2020-10-29 Convergene, Llc Small molecule bromodomain inhibitors and uses thereof
US11535621B2 (en) 2019-07-31 2022-12-27 Ribon Therapeutics, Inc. Heterobicyclic amides as inhibitors of CD38
JP7677976B2 (ja) * 2019-12-23 2025-05-15 ブリストル-マイヤーズ スクイブ カンパニー T細胞アクティベーターとして有用な置換ヘテロアリール化合物
MX2022007369A (es) * 2019-12-23 2022-07-12 Bristol Myers Squibb Co Compuestos de quinolinonilo piperazina sustituidos utiles como activadores de celulas t.
WO2021142252A1 (en) * 2020-01-10 2021-07-15 Incyte Corporation Tricyclic compounds as inhibitors of kras
CN113549010B (zh) * 2020-04-26 2023-10-20 中国科学院上海药物研究所 一种具有ampk激动活性的化合物及其前药的制备和应用
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US20230227409A1 (en) * 2020-06-10 2023-07-20 Ideaya Biosciences, Inc. Quinolinone derivatives as methionine adenosyltransferase 2a inhibitors
EP4210683A4 (en) * 2020-09-09 2024-10-09 Aurigene Oncology Limited Heterocyclic compounds as cbp/ep300 bromodomain inhibitors
AR124718A1 (es) * 2021-01-29 2023-04-26 Ribon Therapeutics Inc Quinolinas y azaquinolinas como inhibidores de cd38

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1369627A (fr) * 1963-08-30 1964-08-14 Geigy Ag J R Dérivés du carbostyrile et leur préparation
WO2003106452A2 (en) * 2002-06-12 2003-12-24 Millennium Pharmaceuticals, Inc. Antagonists of melanin concentrating hormone receptor
WO2007109251A2 (en) * 2006-03-21 2007-09-27 Avanir Pharmaceuticals Tumor necrosis factor alpha inhibitors and their use in the treatment of human diseases
US20100286127A1 (en) * 2007-12-28 2010-11-11 Mitsubishi Tanabe Pharma Corporation Antitumor agent
WO2011054848A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Thetrahydroquinolines derivatives as bromodomain inhibitors
WO2011054844A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Condensed azepine derivatives as bromodomain inhibitors
WO2011054846A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Imidazo [4, 5-c] quinoline derivates as bromodomain inhibitors
US20120157428A1 (en) * 2010-12-02 2012-06-21 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US20120220573A1 (en) * 2009-11-05 2012-08-30 Romain Luc Marie Gosmini Benzodiazepine Bromodomain Inhibitor
US20120252781A1 (en) * 2009-11-05 2012-10-04 James Bailey Benzodiazepine Bromodomain Inhibitor
WO2013027168A1 (en) * 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3755332A (en) 1971-07-01 1973-08-28 Ciba Geigy Corp Substituted 4 indazolaminoquinolines
GB8908229D0 (en) 1989-04-12 1989-05-24 Smithkline Beckman Intercredit Compounds
WO1992017452A1 (en) 1991-04-03 1992-10-15 Korea Research Institute Of Chemical Technology 2-quinolinone derivatives
CA2114727C (en) 1991-08-02 1996-12-10 Mikel P. Moyer Quinoline derivatives as immunostimulants
WO1999011658A1 (en) 1997-08-29 1999-03-11 Proteus Molecular Design Ltd. Meta-benzamidine derivatives as serin protease inhibitors
SE0102858D0 (sv) 2001-08-27 2001-08-27 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
CA2557433C (en) 2004-02-19 2013-05-14 Rexahn Corporation Quinazoline derivatives and therapeutic use thereof
AU2006216266C1 (en) 2005-02-23 2010-08-26 Shionogi & Co., Ltd. Quinazoline derivative having tyrosine kinase inhibitory activity
CR9465A (es) 2005-03-25 2008-06-19 Surface Logix Inc Compuestos mejorados farmacocineticamente
US20090221624A1 (en) 2005-05-06 2009-09-03 Olivo Paul D 4-aminoquinoline compounds for treating virus-related conditions
CA2700988A1 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
GB0705915D0 (en) 2007-03-28 2007-05-09 Helperby Therapeutics Ltd New use
US8003787B2 (en) 2007-05-24 2011-08-23 Bayer Schering Pharma Ag Sulphoximine-substituted quinoline and quinazoline derivatives as kinase inhibitors
AU2008321959B2 (en) 2007-11-12 2014-02-13 Msd K.K. Heteroaryloxy quinazoline derivative
EP2072502A1 (de) 2007-12-20 2009-06-24 Bayer Schering Pharma Aktiengesellschaft Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
AR079814A1 (es) 2009-12-31 2012-02-22 Otsuka Pharma Co Ltd Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos
JP2013526484A (ja) 2010-05-07 2013-06-24 グラクソ グループ リミテッド キナーゼ阻害剤としてのアミノ‐キノリン
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
WO2012040499A2 (en) 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
CN103648500B (zh) 2011-03-17 2016-05-04 宾夕法尼亚大学理事会 双功能酶制钳型分子的方法和用途
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
BR112013033417A2 (pt) 2011-06-29 2016-08-16 Otsuka Pharma Co Ltd compostos terapêuticos e métodos relacionados de uso
US9977024B2 (en) 2012-12-09 2018-05-22 The Scripps Research Institute Targeted covalent probes and inhibitors of proteins containing redox-sensitive cysteines
EA201591746A1 (ru) * 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
JP2017534653A (ja) 2014-11-13 2017-11-24 コンバージーン・リミテッド・ライアビリティ・カンパニーConvergene Llc ブロモドメイン及びエキストラ末端タンパク質の阻害のための方法及び組成物
WO2016120808A1 (en) 2015-01-28 2016-08-04 Minoryx Therapeutics S.L. Heteroarylaminoisoquinolines, methods for their preparation and therapeutic uses thereof

Patent Citations (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1369627A (fr) * 1963-08-30 1964-08-14 Geigy Ag J R Dérivés du carbostyrile et leur préparation
WO2003106452A2 (en) * 2002-06-12 2003-12-24 Millennium Pharmaceuticals, Inc. Antagonists of melanin concentrating hormone receptor
WO2007109251A2 (en) * 2006-03-21 2007-09-27 Avanir Pharmaceuticals Tumor necrosis factor alpha inhibitors and their use in the treatment of human diseases
US20100286127A1 (en) * 2007-12-28 2010-11-11 Mitsubishi Tanabe Pharma Corporation Antitumor agent
CN101910182A (zh) * 2007-12-28 2010-12-08 田边三菱制药株式会社 抗癌剂
WO2011054844A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Condensed azepine derivatives as bromodomain inhibitors
WO2011054848A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Thetrahydroquinolines derivatives as bromodomain inhibitors
WO2011054846A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Imidazo [4, 5-c] quinoline derivates as bromodomain inhibitors
US20120220573A1 (en) * 2009-11-05 2012-08-30 Romain Luc Marie Gosmini Benzodiazepine Bromodomain Inhibitor
US20120252781A1 (en) * 2009-11-05 2012-10-04 James Bailey Benzodiazepine Bromodomain Inhibitor
CN102762569A (zh) * 2009-11-05 2012-10-31 葛兰素史克有限责任公司 苯并二氮杂*溴区结构域抑制剂
CN102781943A (zh) * 2009-11-05 2012-11-14 葛兰素史密丝克莱恩有限责任公司 苯并二氮杂*溴结构域抑制剂
US20120157428A1 (en) * 2010-12-02 2012-06-21 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013027168A1 (en) * 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Database CAPLUS in STN, Acc. No. 1964:16656, FR M1580 (12/17/1962) (abstract). *
Database CAPLUS in STN, Acc. No. 1964:16656, FR M1580 (Dec. 17, 1962) (abstract). *
Jonathan Seal¿, "Identification of a novel series of BET family bromodomain inhibitors: Binding more and profile of I-BET151(GSK1210151A)", Bioorganic & Medicinal Chemistry Letters *
S ANDREAE ET AL, "Electrophile Aminierung von C-H-aciden Verbindungen mit l-Oxa-2-azaspiro[ 2.51 octan", EUROPEAN JOOURNAL OF EUROPEAN CHEMISTRY, (1992-03-12), vol. 1992, no. 3, doi:10.1002/jlac.199219920143, pages 239 - 256 *

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