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
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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

ID=52706277

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
JP6401773B2 (ja) 2013-03-11 2018-10-10 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔブロモドメイン阻害剤およびこれを用いる治療方法
EP3110818B1 (en) * 2014-02-28 2019-10-23 The Regents of The University of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
US10307407B2 (en) 2015-02-27 2019-06-04 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
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
US20190040063A1 (en) * 2016-02-05 2019-02-07 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tricyclic compound for bromodomain-containing protein inhibitor and preparation pharmaceutical composition, and application thereof
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
CN113788818A (zh) * 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
AU2017246453A1 (en) 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
UA123168C2 (uk) 2016-04-12 2021-02-24 Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган Деструктори білка вет
JOP20180113B1 (ar) 2016-06-16 2022-03-14 Denali Therapeutics Inc مركبات بيريميدين -2-يل امينو -h1- بيرازول كمثبطات lrrk2 للاستخدام في علاج اضطرابات تنكسية عصبية
WO2018052945A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
ES2857743T3 (es) 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
JP2020527593A (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． １，８−ナフチリジノン化合物およびその使用
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
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
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
WO2020020288A1 (zh) 2018-07-25 2020-01-30 正大天晴药业集团股份有限公司 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途
JP2022509534A (ja) 2018-10-30 2022-01-20 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
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
SG11202107810WA (en) 2019-01-18 2021-08-30 Nuvation Bio Inc Heterocyclic compounds as adenosine antagonists
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
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
JP2022535743A (ja) * 2019-05-29 2022-08-10 アイエフエム デュー インコーポレイテッド Ｓｔｉｎｇ活性に関連する状態を治療するための化合物および組成物
US11584756B2 (en) 2019-07-02 2023-02-21 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
JP7340100B2 (ja) 2019-10-28 2023-09-06 メルク・シャープ・アンド・ドーム・エルエルシー Ｋｒａｓ ｇ１２ｃ変異型の小分子阻害薬
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
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
WO2021106230A1 (ja) 2019-11-29 2021-06-03 大鵬薬品工業株式会社 新規なフェノール化合物又はその塩
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
US12466840B2 (en) 2023-10-20 2025-11-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS proteins
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
US8044042B2 (en) 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
NZ579355A (en) 2007-02-01 2012-03-30 Resverlogix Corp 2-(Aryl)-4-oxo-quinazoline derivatives
US8431569B2 (en) * 2007-12-13 2013-04-30 Merck Sharp & Dohme Corp. 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
SI2346837T1 (sl) 2008-06-26 2015-05-29 Resverlogix Corporation Postopki pripravljanja kinazolinonskih derivatov
JP5813626B2 (ja) 2009-04-22 2015-11-17 レスバーロジックス コーポレイション 新規抗炎症剤
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011054845A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (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
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
BR112012029005A2 (pt) 2010-05-14 2016-07-26 Dana Farber Cancer Inst Inc composições e métodos de tratamento de neoplasia, doença inflamatória e outros distúrbios
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
EP2590972B1 (en) 2010-07-09 2015-01-21 Pfizer Limited N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US20140066410A1 (en) 2011-02-23 2014-03-06 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
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
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
US9409906B2 (en) * 2012-01-27 2016-08-09 Universite De Montreal Pyrimido[4,5-B]indole derivatives and use thereof in the expansion of hematopoietic stem cells
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
MX2014012635A (es) 2012-04-20 2015-05-15 Abbvie Inc Derivados de isoindolona.
BR112014031068A2 (pt) 2012-06-12 2017-06-27 Abbvie Inc derivados piridinona e piridazinona
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines 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
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
JP6401773B2 (ja) 2013-03-11 2018-10-10 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔブロモドメイン阻害剤およびこれを用いる治療方法
SI3466949T1 (sl) * 2013-12-24 2021-03-31 Bristol-Myers Squibb Company Triciklična spojina kot sredstvo proti raku
EP3110818B1 (en) * 2014-02-28 2019-10-23 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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US20170210761A1 (en) 2017-07-27
CN107074861A (zh) 2017-08-18
JP2017511801A (ja) 2017-04-27
US10253044B2 (en) 2019-04-09
US9580430B2 (en) 2017-02-28
AU2015222887A1 (en) 2016-09-08
WO2015131005A1 (en) 2015-09-03
AU2015222887B2 (en) 2019-06-27
EP3110818A1 (en) 2017-01-04
US20150246923A1 (en) 2015-09-03
EP3110818B1 (en) 2019-10-23

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