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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Canada
Prior art keywords
methyl
methoxy
dimethylisoxazol
pyrimido
amine
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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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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

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)

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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

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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
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
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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
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CA3036834A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
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MD4051678T2 (en) 2019-10-28 2026-07-31 Merck Sharp & Dohme Llc Small molecule inhibitors of the KRAS G12C mutant
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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
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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
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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
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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
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US20150246923A1 (en) 2015-09-03
EP3110818B1 (en) 2019-10-23
US9580430B2 (en) 2017-02-28
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AU2015222887B2 (en) 2019-06-27

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