CN112165944B - 转录激活蛋白的咪唑并哌嗪抑制剂 - Google Patents

转录激活蛋白的咪唑并哌嗪抑制剂 Download PDF

Info

Publication number
CN112165944B
CN112165944B CN201980035368.2A CN201980035368A CN112165944B CN 112165944 B CN112165944 B CN 112165944B CN 201980035368 A CN201980035368 A CN 201980035368A CN 112165944 B CN112165944 B CN 112165944B
Authority
CN
China
Prior art keywords
mmol
methyl
compound
mixture
reduced pressure
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.)
Active
Application number
CN201980035368.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN112165944A (zh
Inventor
K·乐
M·J·索思
P·琼斯
J·克罗斯
C·L·卡罗尔
T·J·麦卡福斯
P·K·曼达尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Texas System
Original Assignee
University of Texas System
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by University of Texas System filed Critical University of Texas System
Publication of CN112165944A publication Critical patent/CN112165944A/zh
Application granted granted Critical
Publication of CN112165944B publication Critical patent/CN112165944B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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 two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201980035368.2A 2018-03-29 2019-03-29 转录激活蛋白的咪唑并哌嗪抑制剂 Active CN112165944B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862650151P 2018-03-29 2018-03-29
US62/650,151 2018-03-29
PCT/US2019/024976 WO2019191667A1 (en) 2018-03-29 2019-03-29 Imidazopiperazine inhibitors of transcription activating proteins

Publications (2)

Publication Number Publication Date
CN112165944A CN112165944A (zh) 2021-01-01
CN112165944B true CN112165944B (zh) 2024-04-09

Family

ID=68057632

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980035368.2A Active CN112165944B (zh) 2018-03-29 2019-03-29 转录激活蛋白的咪唑并哌嗪抑制剂

Country Status (12)

Country Link
US (3) US11058688B2 (https=)
EP (1) EP3773587A4 (https=)
JP (1) JP7387627B2 (https=)
KR (1) KR102815607B1 (https=)
CN (1) CN112165944B (https=)
AU (2) AU2019245403B2 (https=)
BR (1) BR112020019824A2 (https=)
CA (1) CA3095367A1 (https=)
IL (1) IL277628A (https=)
RU (1) RU2020131507A (https=)
WO (1) WO2019191667A1 (https=)
ZA (1) ZA202006092B (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019245403B2 (en) 2018-03-29 2025-02-06 Board Of Regents, The University Of Texas System Imidazopiperazine inhibitors of transcription activating proteins
WO2019195846A1 (en) 2018-04-06 2019-10-10 Board Of Regents, The University Of Texas System Imidazopiperazinone inhibitors of transcription activating proteins
AU2021259814B2 (en) * 2020-04-25 2023-09-28 Pharmablock Sciences (Nanjing), Inc. CBP/EP300 inhibitor and use thereof
JP7777131B2 (ja) * 2020-10-02 2025-11-27 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム 転写活性化タンパク質のイミダゾピペラジン阻害剤
WO2022072648A1 (en) * 2020-10-02 2022-04-07 Board Of Regents, The University Of Texas System Imidazopiperazine inhibitors of transcription activating proteins
US20240122941A1 (en) * 2020-12-25 2024-04-18 National Cancer Center Therapy based on synthetic lethality in swi/snf complex-dysfunction cancer
KR102910851B1 (ko) * 2021-04-21 2026-01-09 장춘 진사이언스 파마슈티컬 씨오., 엘티디. 이미다졸 함유 축합고리계 유도체, 이의 제조방법 및 이의 의약적 용도
CN113429427A (zh) * 2021-07-05 2021-09-24 湖南南新制药股份有限公司 杂环化合物及其制备方法和药物用途
CN115724857B (zh) * 2021-08-25 2024-06-21 杭州禹泓医药科技有限公司 一种芳杂环类化合物、含其的药物组合物及其应用
CN116410211A (zh) * 2021-12-29 2023-07-11 山东新时代药业有限公司 一种苯并呋喃类化合物
TW202340164A (zh) * 2022-01-21 2023-10-16 大陸商深圳默元生物科技有限公司 N-羥基喹啉甲醯胺化合物及其用途
WO2023235809A1 (en) * 2022-06-02 2023-12-07 Eli Lilly And Company Cgas inhibitors
WO2025111184A1 (en) 2023-11-21 2025-05-30 Fmc Corporation Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101686989A (zh) * 2007-06-21 2010-03-31 卡拉治疗学股份有限公司 取代的咪唑并杂环
CN102307581A (zh) * 2008-12-08 2012-01-04 吉利德康涅狄格股份有限公司 咪唑并哌嗪syk抑制剂
CN105518007A (zh) * 2013-06-28 2016-04-20 艾伯维公司 布罗莫结构域抑制剂
WO2016086200A1 (en) * 2014-11-27 2016-06-02 Genentech, Inc. 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors
WO2017205538A1 (en) * 2016-05-24 2017-11-30 Genentech, Inc. Pyrazolopyridine derivatives for the treatment of cancer

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1537114B8 (en) 2002-08-07 2007-10-03 Novartis AG Organic compounds as agents for the treatment of aldosterone mediated conditions
AU2003284596A1 (en) 2002-11-22 2004-06-18 Takeda Pharmaceutical Company Limited Imidazole derivative, process for producing the same, and use
MX2008015008A (es) 2006-05-26 2008-12-05 Novartis Ag INHIBIDORES DE SINTASA DE ALDOSTERONA Y/O DE 11ß-HIDROXILASA.
US7943617B2 (en) * 2006-11-27 2011-05-17 Bristol-Myers Squibb Company Heterobicyclic compounds useful as kinase inhibitors
ATE545647T1 (de) 2006-12-22 2012-03-15 Actelion Pharmaceuticals Ltd 5,6,7,8-tetrahydro-imidazoä1,5-aüpyrazinderivat
US8859538B2 (en) 2007-06-21 2014-10-14 Cara Therapeutics, Inc. Uses of substituted imidazoheterocycles
CN101417999A (zh) 2007-10-25 2009-04-29 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
CN101468988A (zh) * 2007-12-26 2009-07-01 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
KR20110036069A (ko) 2008-06-25 2011-04-06 액테리온 파마슈티칼 리미티드 5,6,7,8-테트라히드로-이미다조[1,5-a]피라진 화합물
EP2528918B1 (en) 2010-01-29 2014-09-10 Nerviano Medical Sciences S.r.l. 6,7-dihydroimidazo[1,5-a]pyrazin-8(5h)-one derivatives as protein kinase modulators
CN102372716A (zh) 2010-08-09 2012-03-14 江苏恒瑞医药股份有限公司 酞嗪酮类衍生物、其制备方法及其在医药上的应用
US9145418B2 (en) 2011-10-07 2015-09-29 Nerviano Medical Sciences S.R.L. Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
CN103087067A (zh) * 2012-08-02 2013-05-08 盛世泰科生物医药技术(苏州)有限公司 作为二肽基酶抑制剂的化合物及其组合物,以及它们的用途
EP2920173B1 (en) 2012-10-18 2016-11-23 Bristol-Myers Squibb Company Tetrahydroimdidazopyrazine derivatives as cgrp receptor antagonists
WO2014199171A1 (en) 2013-06-12 2014-12-18 Proximagen Limited New therapeutic uses of enzyme inhibitors
WO2016055028A1 (en) 2014-10-10 2016-04-14 Genentech, Inc. Therapeutic compounds and uses thereof
MA41338B1 (fr) 2015-01-16 2019-07-31 Hoffmann La Roche Composés de pyrazine pour le traitement de maladies infectieuses
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
AU2017252276A1 (en) 2016-04-18 2018-11-15 Celgene Quanticel Research, Inc. Therapeutic compounds
MA45122A (fr) 2016-05-24 2019-04-10 Constellation Pharmaceuticals Inc Inhibiteurs hétérocycliques de cbp/ep300 et leur utilisation dans le traitement du cancer
AU2019245403B2 (en) 2018-03-29 2025-02-06 Board Of Regents, The University Of Texas System Imidazopiperazine inhibitors of transcription activating proteins
WO2019195846A1 (en) 2018-04-06 2019-10-10 Board Of Regents, The University Of Texas System Imidazopiperazinone inhibitors of transcription activating proteins

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101686989A (zh) * 2007-06-21 2010-03-31 卡拉治疗学股份有限公司 取代的咪唑并杂环
CN102307581A (zh) * 2008-12-08 2012-01-04 吉利德康涅狄格股份有限公司 咪唑并哌嗪syk抑制剂
CN105518007A (zh) * 2013-06-28 2016-04-20 艾伯维公司 布罗莫结构域抑制剂
WO2016086200A1 (en) * 2014-11-27 2016-06-02 Genentech, Inc. 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors
WO2017205538A1 (en) * 2016-05-24 2017-11-30 Genentech, Inc. Pyrazolopyridine derivatives for the treatment of cancer

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Bromodomains:表观遗传医学新靶点及其抑制剂;周啸峰;焦宇;张智敏;唐伟方;;药学进展(08);全文 *
组蛋白乙酰转移酶/组蛋白去乙酰基酶在慢性阻塞性肺疾病发病机制和治疗中的研究进展;窦丽阳;徐治波;冯玉麟;;国际呼吸杂志(19);全文 *
转录辅激活子p300/CBP的结构、功能及其在白细胞介素基因表达调控中的作用;邵阳光, 张国平, 陆军, 黄百渠;科学通报(23);全文 *

Also Published As

Publication number Publication date
BR112020019824A2 (pt) 2021-01-05
EP3773587A4 (en) 2021-09-29
KR20210003764A (ko) 2021-01-12
JP7387627B2 (ja) 2023-11-28
US20190298729A1 (en) 2019-10-03
CN112165944A (zh) 2021-01-01
US20230008047A1 (en) 2023-01-12
RU2020131507A (ru) 2022-05-04
AU2019245403A1 (en) 2020-10-22
ZA202006092B (en) 2022-11-30
US20250127792A1 (en) 2025-04-24
US11058688B2 (en) 2021-07-13
CA3095367A1 (en) 2019-10-03
AU2025202971A1 (en) 2025-05-15
US12186324B2 (en) 2025-01-07
JP2021519308A (ja) 2021-08-10
IL277628A (en) 2020-11-30
AU2019245403B2 (en) 2025-02-06
KR102815607B1 (ko) 2025-05-30
EP3773587A1 (en) 2021-02-17
WO2019191667A1 (en) 2019-10-03

Similar Documents

Publication Publication Date Title
CN112165944B (zh) 转录激活蛋白的咪唑并哌嗪抑制剂
CN109475531B (zh) Ptpn11的杂环抑制剂
CN102015705B (zh) 稠合的杂环衍生物及其用途
US10899769B2 (en) Imidazopiperazinone inhibitors of transcription activating proteins
CN114026083B (zh) 酪氨酸激酶的杂环抑制剂
CN111867590A (zh) Atr激酶的杂环抑制剂
AU2015209189A1 (en) Substituted pyroolopyridines and pyrrolopyrazines for treating cancer or inflammatory diseases
US12559497B2 (en) Imidazopiperazine inhibitors of transcription activating proteins
CN107921044A (zh) 用于治疗疾病的gls1抑制剂
US12540139B2 (en) Imidazopiperazine inhibitors of transcription activating proteins
WO2018213777A1 (en) Heterocyclic inhibitors of kdm5 for the treatment of disease
WO2020219906A1 (en) Heterocyclic inhibitors of tyrosine kinase

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant