JP2019536820A - Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法 - Google Patents

Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法 Download PDF

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JP2019536820A
JP2019536820A JP2019549613A JP2019549613A JP2019536820A JP 2019536820 A JP2019536820 A JP 2019536820A JP 2019549613 A JP2019549613 A JP 2019549613A JP 2019549613 A JP2019549613 A JP 2019549613A JP 2019536820 A JP2019536820 A JP 2019536820A
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cancer
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halogen
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シャンカー ウパダヤヤ，ラム
シャンカー ウパダヤヤ，ラム
ケシリ，ラグハヴァ
マダン，サチン
クマール コツリ ラジャイア，サントシュ
クマール コツリ ラジャイア，サントシュ
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アプトセ バイオサイエンシーズ インコーポレイテッド
アプトセ バイオサイエンシーズ インコーポレイテッド
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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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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    • C07D471/12—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 three hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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  • Chemical & Material Sciences (AREA)
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  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2019549613A 2016-12-01 2017-12-01 Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法 Pending JP2019536820A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662428756P 2016-12-01 2016-12-01
US62/428,756 2016-12-01
PCT/CA2017/000258 WO2018098561A1 (en) 2016-12-01 2017-12-01 Fused pyrimidine compounds as brd4 and jak2 dual inhibitors and methods for use thereof

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JP2019536820A true JP2019536820A (ja) 2019-12-19
JP2019536820A5 JP2019536820A5 (enExample) 2021-01-14

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US (1) US11279703B2 (enExample)
EP (1) EP3548496A4 (enExample)
JP (1) JP2019536820A (enExample)
KR (1) KR20190135464A (enExample)
CN (1) CN110691782A (enExample)
AU (1) AU2017369753A1 (enExample)
WO (1) WO2018098561A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
JP2021510153A (ja) 2018-01-05 2021-04-15 アイカーン スクール オブ メディシン アット マウント サイナイ 膵臓ベータ細胞の増殖を増加させる方法、治療方法、および組成物
WO2019183245A1 (en) 2018-03-20 2019-09-26 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
US12391676B2 (en) * 2018-09-07 2025-08-19 H. Lee Moffitt Cancer Center And Research Institute, Inc. BRD4-JAK2 inhibitors
KR102377007B1 (ko) * 2018-09-20 2022-03-22 한미약품 주식회사 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체
EP3842435A4 (en) * 2018-09-20 2022-05-11 Hanmi Pharm. Co., Ltd. NEW SULFONAMIDE DERIVATIVE PRESENTING A FUSED PYRIMIDINE SKELETON, HAVING AN INHIBITOR EFFECT OF EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION
EP3906028A4 (en) * 2018-12-31 2022-10-12 Icahn School of Medicine at Mount Sinai KINA INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
CN110305140B (zh) * 2019-07-30 2020-08-04 上海勋和医药科技有限公司 二氢吡咯并嘧啶类选择性jak2抑制剂
US20220315594A1 (en) * 2019-08-09 2022-10-06 Ohm Oncology Method of synthesis of compound for dual inhibition of jak2 and bet
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
GB201914910D0 (en) * 2019-10-15 2019-11-27 Sentinel Oncology Ltd Pharmaceutical compounds
BR112022008685A2 (pt) * 2019-11-08 2022-07-26 Heptares Therapeutics Ltd Compostos moduladores de gpr52
CN114728978A (zh) * 2019-11-22 2022-07-08 南京明德新药研发有限公司 作为dna-pk抑制剂的嘧啶并吡咯类螺环化合物及其衍生物
WO2022083560A1 (zh) * 2020-10-19 2022-04-28 南京药石科技股份有限公司 Tyk2选择性抑制剂及其用途
CN117295743A (zh) * 2021-04-30 2023-12-26 微境生物医药科技(上海)有限公司 作为Wee-1抑制剂的吡咯并嘧啶衍生物
GB202113079D0 (en) * 2021-09-14 2021-10-27 Ucl Business Ltd New therapy
US20240409538A1 (en) * 2021-10-19 2024-12-12 Impact Therapeutics (Shanghai), Inc. Substituted triazoloheteroaryl compounds as usp1 inhibitors and the use thereof
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2023137634A1 (zh) * 2022-01-19 2023-07-27 上海奕拓医药科技有限责任公司 三并环化合物、其制备、药物组合物及应用
WO2023169461A1 (zh) * 2022-03-08 2023-09-14 广州再极医药科技有限公司 一种噻吩并嘧啶类化合物、中间体、其制备方法、组合物和应用
CN114957248B (zh) * 2022-05-09 2023-12-29 南开大学 一种吡咯并嘧啶化合物及其制备方法、药物组合物和应用
CN116813624B (zh) * 2023-06-29 2025-10-03 成都金瑞基业生物科技有限公司 一种jak2抑制剂的晶型及制备方法

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010071885A1 (en) * 2008-12-19 2010-06-24 Cephalon, Inc. Pyrrolotriazines as alk and jak2 inhibitors
JP2011503115A (ja) * 2007-11-15 2011-01-27 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド Ｎ含有複素環式化合物
WO2011062372A2 (en) * 2009-11-19 2011-05-26 Korea Institute Of Science And Technology 2, 4, 7 -substituted thieno [3, 2 -d] pyrimidine compounds as protein kinase inhibitors
JP2011518219A (ja) * 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼの阻害剤
JP2013508354A (ja) * 2009-10-22 2013-03-07 コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー 蛋白質キナーゼ阻害活性を有する２，７−置換されたチエノ［３，２−ｄ］ピリミジン化合物
KR20150001967A (ko) * 2013-06-28 2015-01-07 한국과학기술연구원 티에노[3,2-ｄ]피리미딘 유도체의 Ｔ315Ｉ-Ｂｃｒ-Ａｂｌ 점돌연변이종의 저해 활성
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
WO2015151006A1 (en) * 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
WO2016022460A1 (en) * 2014-08-03 2016-02-11 H. Lee Moffitt Cancer Center And Research Institute, Inc. Potent dual brd4-kinase inhibitors as cancer therapeutics
WO2016133935A1 (en) * 2015-02-17 2016-08-25 Neupharma, Inc. Certain chemical entities, compositions, and methods

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9903762D0 (en) * 1999-02-18 1999-04-14 Novartis Ag Organic compounds
TW201100429A (en) * 2009-05-22 2011-01-01 Incyte Corp 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
US9745320B2 (en) * 2013-01-18 2017-08-29 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof
CN107698603B (zh) * 2016-08-09 2022-04-08 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011503115A (ja) * 2007-11-15 2011-01-27 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド Ｎ含有複素環式化合物
JP2011518219A (ja) * 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼの阻害剤
WO2010071885A1 (en) * 2008-12-19 2010-06-24 Cephalon, Inc. Pyrrolotriazines as alk and jak2 inhibitors
JP2013508354A (ja) * 2009-10-22 2013-03-07 コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー 蛋白質キナーゼ阻害活性を有する２，７−置換されたチエノ［３，２−ｄ］ピリミジン化合物
WO2011062372A2 (en) * 2009-11-19 2011-05-26 Korea Institute Of Science And Technology 2, 4, 7 -substituted thieno [3, 2 -d] pyrimidine compounds as protein kinase inhibitors
KR20150001967A (ko) * 2013-06-28 2015-01-07 한국과학기술연구원 티에노[3,2-ｄ]피리미딘 유도체의 Ｔ315Ｉ-Ｂｃｒ-Ａｂｌ 점돌연변이종의 저해 활성
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
WO2015151006A1 (en) * 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
WO2016022460A1 (en) * 2014-08-03 2016-02-11 H. Lee Moffitt Cancer Center And Research Institute, Inc. Potent dual brd4-kinase inhibitors as cancer therapeutics
WO2016133935A1 (en) * 2015-02-17 2016-08-25 Neupharma, Inc. Certain chemical entities, compositions, and methods

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZIFICSAK, CRAIG A. 他: "Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 22(1), JPN6021042854, 2012, pages 133 - 137, ISSN: 0004812247 *

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US11279703B2 (en) 2022-03-22
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EP3548496A1 (en) 2019-10-09
CN110691782A (zh) 2020-01-14
US20200095252A1 (en) 2020-03-26
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