CA2940554A1 - 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors - Google Patents

9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors Download PDF

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Publication number
CA2940554A1
CA2940554A1 CA2940554A CA2940554A CA2940554A1 CA 2940554 A1 CA2940554 A1 CA 2940554A1 CA 2940554 A CA2940554 A CA 2940554A CA 2940554 A CA2940554 A CA 2940554A CA 2940554 A1 CA2940554 A1 CA 2940554A1
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CA
Canada
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.)
Abandoned
Application number
CA2940554A
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English (en)
French (fr)
Inventor
Shaomeng Wang
Yujun Zhao
Bing Zhou
Angelo AGUILAR
Liu Liu
Longchuan Bai
Donna Mceachern
Duxin Sun
Bo WEN
Ruijuan LUO
Ting ZHAO
Arul Chinnaiyan
Irfan A. Asangani
Jeanne STUCKEY
Jennifer Lynn Meagher
Xu RAN
Yang Hu
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University of Michigan System
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University of Michigan System
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Filing date
Publication date
Application filed by University of Michigan System filed Critical University of Michigan System
Publication of CA2940554A1 publication Critical patent/CA2940554A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2940554A 2014-02-28 2015-02-27 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors Abandoned CA2940554A1 (en)

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 (1)

Publication Number Publication Date
CA2940554A1 true CA2940554A1 (en) 2015-09-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2940554A Abandoned CA2940554A1 (en) 2014-02-28 2015-02-27 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors

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)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10618910B2 (en) 2014-09-15 2020-04-14 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US10626114B2 (en) 2016-06-20 2020-04-21 Incyte Corporation Crystalline solid forms of a BET inhibitor
US10781209B2 (en) 2014-04-23 2020-09-22 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
US10858372B2 (en) 2015-10-29 2020-12-08 Incyte Corporation Amorphous solid form of a BET protein inhibitor
US10919912B2 (en) 2013-03-15 2021-02-16 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2021119834A1 (en) * 2019-12-18 2021-06-24 Universite De Montreal Modulators of cullin 3 adaptor kbtbd4 as anti-cancer compounds
US11091484B2 (en) 2013-12-19 2021-08-17 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
CN105377851B (zh) * 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
WO2015131005A1 (en) * 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
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
WO2017087905A1 (en) 2015-11-20 2017-05-26 Denali Therapeutics Inc. Compound, compositions, and methods
EP3412669A4 (en) * 2016-02-05 2019-09-04 Chia Tai Tianqing Pharmaceutical Group Co.,Ltd TRICYCLIC COMPOUND FOR PROTEIN INHIBITOR CONTAINING BROMODOMAINE AND PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF
KR102387316B1 (ko) 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
WO2017176958A1 (en) 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
RU2752677C2 (ru) 2016-04-12 2021-07-29 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Деструкторы белка вет
PE20190395A1 (es) 2016-06-16 2019-03-13 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
JP6961684B2 (ja) 2016-09-13 2021-11-05 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔタンパク質分解物質としての縮合１，４−オキサゼピン
ES2857743T3 (es) 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
AU2018302178A1 (en) 2017-07-18 2020-02-13 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
WO2019018584A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
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
KR20210038921A (ko) 2018-07-25 2021-04-08 치아타이 티안큉 파마수티컬 그룹 주식회사 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도
WO2020092638A1 (en) 2018-10-30 2020-05-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
US20220002816A1 (en) * 2018-11-13 2022-01-06 Center For Cancer Research & Therapeutic Development, Clark Atlanta University Identification of jund target genes for inhibition of prostate cancer cell growth
WO2020106059A1 (ko) * 2018-11-21 2020-05-28 한국화학연구원 Irak4 저해제로서 신규의 삼중고리 화합물
KR102329235B1 (ko) 2018-11-21 2021-11-22 한국화학연구원 Irak4 저해제로서 신규의 삼중고리 화합물
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
KR20210116550A (ko) 2019-01-18 2021-09-27 누베이션 바이오 인크. 아데노신 길항제로서의 헤테로시클릭 화합물
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
WO2020243519A1 (en) * 2019-05-29 2020-12-03 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
CA3145827A1 (en) 2019-07-02 2021-01-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
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
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol 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
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
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
WO2024233776A1 (en) * 2023-05-09 2024-11-14 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12d mutant
TW202535891A (zh) 2023-10-20 2025-09-16 美商默沙東有限責任公司 Ｋｒａｓ蛋白之小分子抑制劑
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
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
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
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
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
ES2532402T3 (es) 2008-06-26 2015-03-26 Resverlogix Corporation Métodos de preparación de derivados de quinazolinona
CN107252429B (zh) 2009-04-22 2023-06-16 雷斯韦洛吉克斯公司 新抗炎剂
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP3050885B1 (en) 2009-11-05 2017-10-18 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
DE102009053235A1 (de) 2009-11-06 2011-05-19 Gottwald Port Technology Gmbh Umschlagsystem für ISO-Container mit einer Containerbrücke
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
US9145407B2 (en) 2010-07-09 2015-09-29 Pfizer Limited Sulfonamide compounds
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
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 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
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, 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
HK1206744A1 (en) 2012-04-20 2016-01-15 Abbvie Inc. Isoindolone derivatives
MX2014015156A (es) 2012-06-12 2015-08-06 Abbvie Inc Derivados de piridinona y piridazinona.
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
US9492460B2 (en) * 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
CN105189488B (zh) * 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
MA39211B1 (fr) * 2013-12-24 2019-01-31 Bristol Myers Squibb Co Composés tricycliques comme agents anti-cancers
WO2015131005A1 (en) * 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors

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US10919912B2 (en) 2013-03-15 2021-02-16 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
US11498926B2 (en) 2013-03-15 2022-11-15 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US11091484B2 (en) 2013-12-19 2021-08-17 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US10781209B2 (en) 2014-04-23 2020-09-22 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
US12227502B2 (en) 2014-04-23 2025-02-18 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c] pyridin-7(6H)-ones as inhibitors of BET proteins
US11059821B2 (en) 2014-04-23 2021-07-13 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
US11702416B2 (en) 2014-04-23 2023-07-18 Incyte Corporation 1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
US10618910B2 (en) 2014-09-15 2020-04-14 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US10858372B2 (en) 2015-10-29 2020-12-08 Incyte Corporation Amorphous solid form of a BET protein inhibitor
US11377446B2 (en) 2016-06-20 2022-07-05 Incyte Corporation Crystalline solid forms of a BET inhibitor
US10626114B2 (en) 2016-06-20 2020-04-21 Incyte Corporation Crystalline solid forms of a BET inhibitor
US11091480B2 (en) 2016-06-20 2021-08-17 Incyte Corporation Crystalline solid forms of a BET inhibitor
US12030882B2 (en) 2016-06-20 2024-07-09 Incyte Corporation Crystalline solid forms of a bet inhibitor
US12459943B2 (en) 2016-06-20 2025-11-04 Incyte Corporation Crystalline solid forms of a BET inhibitor
WO2021119834A1 (en) * 2019-12-18 2021-06-24 Universite De Montreal Modulators of cullin 3 adaptor kbtbd4 as anti-cancer compounds
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US12440495B2 (en) 2020-06-03 2025-10-14 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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EP3110818B1 (en) 2019-10-23
US10253044B2 (en) 2019-04-09
US20170210761A1 (en) 2017-07-27
US9580430B2 (en) 2017-02-28
AU2015222887B2 (en) 2019-06-27
CN107074861A (zh) 2017-08-18
AU2015222887A1 (en) 2016-09-08
EP3110818A1 (en) 2017-01-04
JP2017511801A (ja) 2017-04-27
US20150246923A1 (en) 2015-09-03
WO2015131005A1 (en) 2015-09-03

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