JP2017511801A5 - - Google Patents

Download PDF

Info

Publication number
JP2017511801A5
JP2017511801A5 JP2016554607A JP2016554607A JP2017511801A5 JP 2017511801 A5 JP2017511801 A5 JP 2017511801A5 JP 2016554607 A JP2016554607 A JP 2016554607A JP 2016554607 A JP2016554607 A JP 2016554607A JP 2017511801 A5 JP2017511801 A5 JP 2017511801A5
Authority
JP
Japan
Prior art keywords
methyl
methoxy
dimethylisoxazol
pyrimido
amine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2016554607A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017511801A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2015/017908 external-priority patent/WO2015131005A1/en
Publication of JP2017511801A publication Critical patent/JP2017511801A/ja
Publication of JP2017511801A5 publication Critical patent/JP2017511801A5/ja
Pending legal-status Critical Current

Links

JP2016554607A 2014-02-28 2015-02-27 BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体 Pending JP2017511801A (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201461946501P 2014-02-28 2014-02-28
US61/946,501 2014-02-28
US201461950406P 2014-03-10 2014-03-10
US61/950,406 2014-03-10
US201462031640P 2014-07-31 2014-07-31
US62/031,640 2014-07-31
US201462048388P 2014-09-10 2014-09-10
US62/048,388 2014-09-10
PCT/US2015/017908 WO2015131005A1 (en) 2014-02-28 2015-02-27 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors

Publications (2)

Publication Number Publication Date
JP2017511801A JP2017511801A (ja) 2017-04-27
JP2017511801A5 true JP2017511801A5 (enExample) 2018-04-05

Family

ID=52706277

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016554607A Pending JP2017511801A (ja) 2014-02-28 2015-02-27 BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体

Country Status (7)

Country Link
US (2) US9580430B2 (enExample)
EP (1) EP3110818B1 (enExample)
JP (1) JP2017511801A (enExample)
CN (1) CN107074861A (enExample)
AU (1) AU2015222887B2 (enExample)
CA (1) CA2940554A1 (enExample)
WO (1) WO2015131005A1 (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US9580430B2 (en) * 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
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
EP3262045A1 (en) * 2015-02-27 2018-01-03 The Regents of The University of Michigan 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors
US9725449B2 (en) * 2015-05-12 2017-08-08 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
WO2017133681A1 (zh) * 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
EP3440082A1 (en) 2016-04-06 2019-02-13 The Regents of The University of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
AU2017246452C1 (en) 2016-04-06 2021-06-03 The Regents Of The University Of Michigan MDM2 protein degraders
AU2017250076B2 (en) * 2016-04-12 2021-07-22 The Regents Of The University Of Michigan Bet protein degraders
PT3472153T (pt) 2016-06-16 2021-12-31 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazóis como inibidores de lrrk2 para uso no tratamento de distúrbios neurodegenerativos
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
ES2857743T3 (es) 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
CA3036834A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドNuvation Bio Inc. アデノシンアンタゴニストとしてのヘテロ環式化合物
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
CN109223792A (zh) * 2018-04-24 2019-01-18 李明霞 一种治疗骨关节炎的药物组合物及其制备方法
US12030880B2 (en) 2018-07-25 2024-07-09 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Iminosulfanone compound as bromodomain protein inhibitor and pharmaceutical composition and medical use thereof
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS
WO2020101909A2 (en) * 2018-11-13 2020-05-22 Center For Cancer Research & Therapeutic Development, Clark Atlanta University Identification of jund target genes for inhibition of prostate cancer cell growth
KR102329235B1 (ko) * 2018-11-21 2021-11-22 한국화학연구원 Irak4 저해제로서 신규의 삼중고리 화합물
WO2020106059A1 (ko) * 2018-11-21 2020-05-28 한국화학연구원 Irak4 저해제로서 신규의 삼중고리 화합물
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
WO2020150674A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
CN110003204B (zh) * 2019-04-30 2020-08-11 上海勋和医药科技有限公司 一种bet蛋白抑制剂、其制备方法及用途
US20220227760A1 (en) * 2019-05-29 2022-07-21 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
JP7465945B2 (ja) 2019-07-02 2024-04-11 ニューベイション・バイオ・インコーポレイテッド Bet阻害剤としてのヘテロ環式化合物
MD4051678T2 (en) 2019-10-28 2026-07-31 Merck Sharp & Dohme Llc Small molecule inhibitors of the KRAS G12C mutant
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
CN112851678B (zh) * 2019-11-28 2022-04-19 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤转移作用
CN112851679B (zh) * 2019-11-28 2022-03-25 广东医科大学 2,4,7-三取代嘧啶并吲哚化合物抗肿瘤作用
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
CN113018301A (zh) * 2019-12-09 2021-06-25 中国科学院大连化学物理研究所 JQ1与Erlotinib组合物在制备治疗肝癌药物中应用和治疗肝癌药物
EP4076466B1 (en) * 2019-12-18 2026-03-11 Universite De Montreal Modulators of cullin 3 adaptor kbtbd4 as anti-cancer compounds
WO2021215544A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
US12702658B2 (en) 2020-04-24 2026-08-11 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11814388B1 (en) 2020-08-28 2023-11-14 Ferris State University Substituted pyrrolo[2,3-d]pyrimidines and pyrazolo[3,4-d]pyrimidines as inhibitors for multi-resistant cancers
WO2022109487A1 (en) 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant
US12016847B2 (en) * 2021-03-12 2024-06-25 Bristol-Myers Squibb Company Methods of treating prostate cancer
CN114044754A (zh) * 2021-11-23 2022-02-15 贵州大学 一类5-三氟甲基-4-吡唑衍生物的制备方法及其在抑制肿瘤细胞上的应用
CN115057859B (zh) * 2022-05-10 2023-07-21 中国人民解放军海军军医大学 一类具有抗肿瘤抗真菌活性的化合物及其应用
WO2024099441A1 (en) * 2022-11-11 2024-05-16 Jingrui Biopharma (Shandong) Co., Ltd. Bromodomain and extra-terminal (bet) protein degrader
EP4709371A1 (en) * 2023-05-09 2026-03-18 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12d mutant
KR20260096846A (ko) 2023-10-20 2026-06-24 머크 샤프 앤드 돔 엘엘씨 Kras 단백질의 소분자 억제제
WO2025230961A1 (en) * 2024-04-29 2025-11-06 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
WO1998011111A1 (en) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and medicinal uses thereof
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
PT2118074E (pt) 2007-02-01 2014-03-20 Resverlogix Corp Compostos para a prevenção e tratamento de doenças cardiovasculares
EP2231143B1 (en) * 2007-12-13 2013-07-03 Merck Sharp & Dohme Corp. 5H-pyrido[4,3-b]indoles as INHIBITORS OF JANUS KINASES
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
US8114995B2 (en) 2008-06-26 2012-02-14 Resverlogix Corp. Methods of preparing quinazolinone derivatives
US9757368B2 (en) 2009-04-22 2017-09-12 Resverlogix Corp. Anti-inflammatory agents
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AU2010317096B2 (en) 2009-11-05 2015-03-26 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
DE102009053235A1 (de) * 2009-11-06 2011-05-19 Gottwald Port Technology Gmbh Umschlagsystem für ISO-Container mit einer Containerbrücke
CN103154246B (zh) 2010-05-14 2015-11-25 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
JP5872552B2 (ja) 2010-07-09 2016-03-01 ファイザー・リミテッドPfizer Limited 化学化合物
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
EP2677865A4 (en) 2011-02-23 2015-04-22 Icahn School Med Mount Sinai BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
SI2807165T1 (sl) * 2012-01-27 2019-08-30 Universite De Montreal Pirimido(4,5-B)indol derivati in njihova uporaba pri ekspanziji hematopoetskih matičnih celic
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
HK1208681A1 (en) 2012-06-12 2016-03-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2961747B1 (en) * 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
EA201990240A1 (ru) * 2013-12-24 2019-06-28 Бристол-Маерс Сквибб Компани Новые трициклические соединения в качестве противораковых средств
US9580430B2 (en) * 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors

Similar Documents

Publication Publication Date Title
JP7460593B2 (ja) サイクリン依存性キナーゼ7(cdk7)の阻害剤
AU2017221802B2 (en) Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
US9969694B2 (en) N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9546156B2 (en) N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
JP2023011899A (ja) ユビキチン特異的プロテアーゼ1阻害剤としてのプリノン
US9790210B2 (en) N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
AU2010249380B2 (en) N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as Janus kinase inhibitors
US9981959B2 (en) Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9809578B2 (en) Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
AU2015222887B2 (en) 9H-pyrimido[4,5-b]indoles and related analogs as BET bromodomain inhibitors
TWI878423B (zh) 環狀化合物及其使用方法
JP2018505880A (ja) がんの治療のための化合物
JP2020514267A5 (enExample)
EP3356345A1 (en) Heteroaryl derivatives as sepiapterin reductase inhibitors
AU2017201418A1 (en) Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
TW202210482A (zh) 含氮稠合二環化合物及其作為泛素特異性加工蛋白酶1(usp1)抑制劑之用途
KR20210068479A (ko) Map4k1 억제제로서의 사용을 위한 인돌리논 화합물
WO2013178572A1 (en) Triazolo compounds as pde10 inhibitors
WO2024046512A2 (zh) 含氮大环类化合物及其制备方法和医药用途
EA043920B1 (ru) Индолиноновые соединения для применения в качестве ингибиторов map4k1