CN109476641B - Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途 - Google Patents

Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途 Download PDF

Info

Publication number
CN109476641B
CN109476641B CN201780045651.4A CN201780045651A CN109476641B CN 109476641 B CN109476641 B CN 109476641B CN 201780045651 A CN201780045651 A CN 201780045651A CN 109476641 B CN109476641 B CN 109476641B
Authority
CN
China
Prior art keywords
cancer
compound
methyl
formula
salt
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.)
Expired - Fee Related
Application number
CN201780045651.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN109476641A (zh
Inventor
P·西尔
S·布朗纳
F·A·罗梅罗
S·马格努森
V·H-W·徐
J·瓦伊
K·W·赖
F·王
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.)
Genentech Inc
Constellation Pharmaceuticals Inc
Original Assignee
Genentech Inc
Constellation Pharmaceuticals Inc
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 Genentech Inc, Constellation Pharmaceuticals Inc filed Critical Genentech Inc
Priority to CN202210701205.7A priority Critical patent/CN115028617A/zh
Publication of CN109476641A publication Critical patent/CN109476641A/zh
Application granted granted Critical
Publication of CN109476641B publication Critical patent/CN109476641B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D281/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02Seven-membered rings
    • C07D281/04Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/10Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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
    • 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
    • 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
    • C07D487/22Heterocyclic 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 four or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
CN201780045651.4A 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途 Expired - Fee Related CN109476641B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210701205.7A CN115028617A (zh) 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016083124 2016-05-24
CNPCT/CN2016/083124 2016-05-24
PCT/US2017/034320 WO2017205536A2 (en) 2016-05-24 2017-05-24 Therapeutic compounds and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202210701205.7A Division CN115028617A (zh) 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途

Publications (2)

Publication Number Publication Date
CN109476641A CN109476641A (zh) 2019-03-15
CN109476641B true CN109476641B (zh) 2022-07-05

Family

ID=59014798

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201780045651.4A Expired - Fee Related CN109476641B (zh) 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途
CN202210701205.7A Pending CN115028617A (zh) 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202210701205.7A Pending CN115028617A (zh) 2016-05-24 2017-05-24 Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途

Country Status (6)

Country Link
US (2) US10696655B2 (enExample)
EP (2) EP3464270B1 (enExample)
JP (2) JP7160688B2 (enExample)
CN (2) CN109476641B (enExample)
MA (1) MA45122A (enExample)
WO (1) WO2017205536A2 (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3021645A1 (en) 2016-04-29 2017-11-02 Icahn School Of Medicine At Mount Sinai Targeting the innate immune system to induce long-term tolerance and to resolve macrophage accumulation in atherosclerosis
WO2017205536A2 (en) 2016-05-24 2017-11-30 Genentech, Inc. Therapeutic compounds and uses thereof
CN110291089B (zh) 2017-01-17 2022-05-27 海帕瑞吉尼克斯股份有限公司 用于促进肝再生或者减少或预防肝细胞死亡的蛋白激酶抑制剂
CN110573501B (zh) * 2017-06-30 2023-09-29 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
WO2019000683A1 (zh) 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
AU2018294054B2 (en) * 2017-06-30 2022-05-26 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
WO2019055877A1 (en) 2017-09-15 2019-03-21 Forma Therapeutics, Inc. TETRAHYDROIMIDAZO QUINOLINE COMPOSITIONS AS INHIBITORS OF CBP / P300
US11414384B2 (en) 2018-02-16 2022-08-16 Constellation Pharmaceuticals, Inc. P300/CBP hat inhibitors
RS65966B1 (sr) 2018-02-16 2024-10-31 Constellation Pharmaceuticals Inc Inhibitori p300/cbp hat
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
WO2019201291A1 (zh) * 2018-04-20 2019-10-24 中国科学院上海药物研究所 组蛋白乙酰转移酶(hat)抑制剂及其用途
US11578124B2 (en) 2018-05-18 2023-02-14 Janssen Biotech, Inc. Safe and effective method of treating lupus with anti-IL12/IL23 antibody
KR20250067962A (ko) 2018-06-29 2025-05-15 포르마 세라퓨틱스 인크. Creb 결합 단백질(cbp)의 저해
CN112770752A (zh) 2018-08-02 2021-05-07 波士顿大学董事会 晚期sv40因子(lsf)抑制剂
CN111635356A (zh) * 2018-11-23 2020-09-08 厦门大学 Carm1小分子抑制剂的化合物、可药用盐、药物组合及用途
TWI850342B (zh) * 2019-02-27 2024-08-01 美商星座製藥公司 P300/cbp hat抑制劑及其使用方法
WO2020173440A1 (en) * 2019-02-27 2020-09-03 Cullgen (Shanghai), Inc. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use
US12351577B2 (en) 2019-03-15 2025-07-08 Forma Therapeutics, Inc. Inhibiting cyclic AMP-responsive element-binding protein (CREB)
CN111763180B (zh) * 2019-04-02 2023-06-09 中国医学科学院药物研究所 苯并氮杂环类化合物及其制法和药物用途
TW202120095A (zh) * 2019-08-05 2021-06-01 美商美國禮來大藥廠 7,8-二氫-4H-吡唑并[4,3-c]氮呯-6-酮化合物
CN112574189B (zh) 2019-09-27 2024-05-31 海创药业股份有限公司 一种ep300/cbp抑制剂
JP2022549506A (ja) 2019-09-27 2022-11-25 ディスク・メディシン・インコーポレイテッド 骨髄線維症および関連状態を処置するための方法
WO2021150835A1 (en) * 2020-01-24 2021-07-29 Trustees Of Boston University Heterocyclic lsf inhibitors and their uses
WO2021213521A1 (zh) * 2020-04-25 2021-10-28 南京药石科技股份有限公司 Cbp/ep300抑制剂及其用途
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
US11458132B2 (en) 2020-09-01 2022-10-04 Trustees Of Boston University Quinolin-2(1H)-one inhibitors of Late SV40 Factor
JP2023539931A (ja) * 2020-09-09 2023-09-20 オーリジーン オンコロジー リミテッド Cbp/ep300ブロモドメイン阻害剤としての複素環式化合物
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
CN116348112A (zh) * 2020-10-02 2023-06-27 德州大学系统董事会 转录激活蛋白的咪唑并哌嗪抑制剂
JP2023544173A (ja) 2020-10-02 2023-10-20 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
AU2022239614A1 (en) * 2021-03-19 2023-10-12 Icahn School Of Medicine At Mount Sinai Compounds for regulating trained immunity, and their methods of use
CN113087683B (zh) * 2021-03-22 2022-04-22 华南理工大学 氮取代苯并噻唑啉酮类xor/urat1双重抑制剂及其制备方法与应用
TW202409023A (zh) 2022-07-14 2024-03-01 美商富曼西公司 除草苯并𠯤
CN117843618A (zh) * 2022-08-29 2024-04-09 北京沐华生物科技有限责任公司 一种ep300/cbp调节剂及其制备方法和用途
AU2024333590A1 (en) * 2023-08-30 2026-03-12 Oncopia Therapeutics, Inc. D/B/A Sk Life Science Labs Compounds and compositions as cbp/p300 degraders and uses thereof
WO2025111184A1 (en) 2023-11-21 2025-05-30 Fmc Corporation Substituted tetrahydroquinoline and tetrahydroquinoxaline herbicides

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6011029A (en) * 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
WO2010118208A1 (en) * 2009-04-09 2010-10-14 Exelixis, Inc. Benzoxazepin-4- (5h) -yl derivatives and their use to treat cancer
WO2010138490A1 (en) * 2009-05-26 2010-12-02 Exelixis, Inc. Benzoxazepines as inhibitors of mtor and methods of their use and manufacture
CN103857659A (zh) * 2011-07-01 2014-06-11 吉利德科学公司 作为离子通道调节剂的稠合杂环化合物
WO2014133414A2 (ru) * 2013-02-26 2014-09-04 Алла Хем Ллс Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения
WO2016044694A1 (en) * 2014-09-19 2016-03-24 Genentech, Inc. Use of cbp/ep300 and bet inhibitors for treatment of cancer

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US533A (en) 1837-12-26 Truss for hermta
US4943A (en) 1847-01-26 Harness-buckle
CU22545A1 (es) 1994-11-18 1999-03-31 Centro Inmunologia Molecular Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico
US4943533A (en) 1984-03-01 1990-07-24 The Regents Of The University Of California Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor
CA2066428C (en) 1989-09-08 2000-11-28 Bert Vogelstein Structural alterations of the egf receptor gene in human gliomas
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
DK0659439T3 (da) 1993-12-24 2002-01-14 Merck Patent Gmbh Immunkonjugater
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
HU216142B (hu) 1994-07-21 1999-04-28 Akzo Nobel N.V. Ciklusos keton-peroxidokat tartalmazó kompozíciók, és azok alkalmazása (ko)polimerek módosítására
US5804396A (en) 1994-10-12 1998-09-08 Sugen, Inc. Assay for agents active in proliferative disorders
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
GB9508565D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
JPH11507535A (ja) 1995-06-07 1999-07-06 イムクローン システムズ インコーポレイテッド 腫瘍の成長を抑制する抗体および抗体フラグメント類
EP0836605B1 (en) 1995-07-06 2002-02-06 Novartis AG Pyrrolopyrimidines and processes for the preparation thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd., Greenford Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
ES2201484T3 (es) 1997-05-06 2004-03-16 Wyeth Holdings Corporation Utilizacion de compuestos de quinazolina para el tratamiento de la enfermedad de la poliquistosis renal.
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ZA986729B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
NZ503991A (en) 1997-11-06 2001-11-30 American Cyanamid Co Use of quinazoline derivatives as tyrosine kinase inhibitors for treating colonic polyps
ES2188254T3 (es) 1998-11-19 2003-06-16 Warner Lambert Co N-(4-(3-chloro-4-fluoro-fenilamino)-7-(3-morfolin-4-il-propoxi)-quin azolin-6-il)-acrilamada, un inhibidor irreversible de tirosina quinasas.
PL2161336T5 (pl) 2005-05-09 2017-10-31 Ono Pharmaceutical Co Ludzkie przeciwciała monoklonalne przeciwko białku Programmed Death 1 (PD-1) oraz sposoby leczenia raka z zastosowaniem samych przeciwciał anty-PD-1 lub w połączeniu z innymi środkami immunoterapeutycznymi
CA2612241C (en) 2005-07-01 2018-11-06 Medarex, Inc. Human monoclonal antibodies to programmed death ligand 1 (pd-l1)
US20090258853A1 (en) * 2006-03-13 2009-10-15 Brian Eastman Somatostatin Agonists
EP2001472A2 (en) * 2006-03-23 2008-12-17 Merck and Co., Inc. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
CA2651072A1 (en) * 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
GB0620059D0 (en) * 2006-10-10 2006-11-22 Ucb Sa Therapeutic agents
WO2009053694A1 (en) * 2007-10-24 2009-04-30 Cancer Research Technology Limited Therapeutic oxy-phenyl-aryl compounds and their use
WO2009071890A1 (en) * 2007-12-04 2009-06-11 Ucb Pharma S.A. Tricyclic kinase inhibitors
GB0723747D0 (en) * 2007-12-04 2008-12-31 Ucb Pharma Sa Therapeutic agents
WO2009071895A1 (en) * 2007-12-04 2009-06-11 Ucb Pharma S.A. Fused thiazole and thiophene derivatives as kinase inhibitors
RU2531758C2 (ru) 2008-02-11 2014-10-27 Куретек Лтд. Моноклональные антитела для лечения опухолей
US8168757B2 (en) 2008-03-12 2012-05-01 Merck Sharp & Dohme Corp. PD-1 binding proteins
JP2012500652A (ja) 2008-08-25 2012-01-12 アンプリミューン、インコーポレーテッド 標的化共刺激ポリペプチドおよび癌を処置するための使用方法
EP4209510B1 (en) 2008-12-09 2024-01-31 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
EP2379523A1 (en) * 2008-12-22 2011-10-26 Incyte Corporation 4, 6-disubstituted 2-amino-pyrimidines as histamine h4 receptor modulators
EP2241557A1 (de) * 2009-04-02 2010-10-20 Æterna Zentaris GmbH Chinoxalin-Derivate und deren Anwendung zur Behandlung gutartiger und bösartiger Tumorerkrankungen
CA2763008A1 (en) 2009-05-26 2010-12-02 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
GB0919431D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US20130017199A1 (en) 2009-11-24 2013-01-17 AMPLIMMUNE ,Inc. a corporation Simultaneous inhibition of pd-l1/pd-l2
AR079814A1 (es) * 2009-12-31 2012-02-22 Otsuka Pharma Co Ltd Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos
US8440662B2 (en) * 2010-10-31 2013-05-14 Endo Pharmaceuticals, Inc. Substituted quinazoline and pyrido-pyrimidine derivatives
TW201307292A (zh) * 2010-12-17 2013-02-16 Hoffmann La Roche 經取代之6,6-稠合含氮雜環化合物及其用途
UA111075C2 (uk) * 2011-02-25 2016-03-25 Еррей Біофарма Інк. Триазолопіридинові сполуки як інгібітори кінази рім
JP6121658B2 (ja) * 2011-06-29 2017-04-26 大塚製薬株式会社 治療用化合物、及び関連する使用の方法
US9145411B2 (en) * 2012-08-02 2015-09-29 Asana Biosciences, Llc Substituted amino-pyrimidine derivatives
ES2704048T3 (es) * 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
CN107108512B (zh) * 2014-10-10 2021-05-04 基因泰克公司 治疗性化合物及其用途
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
EP3317278B1 (en) * 2015-07-01 2021-04-14 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
CN105039258B (zh) 2015-07-03 2018-04-17 北京大学 将非神经元细胞重编程为神经元样细胞的方法和组合物
AR108326A1 (es) * 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
AR108325A1 (es) * 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
WO2017205536A2 (en) 2016-05-24 2017-11-30 Genentech, Inc. Therapeutic compounds and uses thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6011029A (en) * 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
WO2010118208A1 (en) * 2009-04-09 2010-10-14 Exelixis, Inc. Benzoxazepin-4- (5h) -yl derivatives and their use to treat cancer
WO2010138490A1 (en) * 2009-05-26 2010-12-02 Exelixis, Inc. Benzoxazepines as inhibitors of mtor and methods of their use and manufacture
CN103857659A (zh) * 2011-07-01 2014-06-11 吉利德科学公司 作为离子通道调节剂的稠合杂环化合物
WO2014133414A2 (ru) * 2013-02-26 2014-09-04 Алла Хем Ллс Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения
WO2016044694A1 (en) * 2014-09-19 2016-03-24 Genentech, Inc. Use of cbp/ep300 and bet inhibitors for treatment of cancer

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
3D-QSAR, molecular dynamics simulations and molecular docking studies of benzoxazepine moiety as mTOR inhibitor for the treatment of lung cancer;Udit Chaube等;《Bioorganic & Medicinal Chemistry Letters》;20151223;第26卷;第866页 Table1 *
A new approach to monoprotected 1,4-benzodiazepines via a one-pot N-deprotection/reductive cyclization procedure;Tobias Alexander Popp 等;《Tetrahedron》;20160209;第72卷;第1670页 Scheme 3 *
Discovery and Structure-Activity Relationships of Imidazole- Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase;Charles Z. Ding 等;《J. Med. Chem.》;19991030;第42卷;第5244页表5,第5251页右栏第2、4段 *
Discovery of a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR);《J. Med. Chem. 》;《J. Med. Chem. 》;20130208;第56卷;第2219页 Figure2,第2221页Table1、Table2 *
Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy;Sarah Picaud 等;《Cancer Research》;20151109;第75卷(第23期);摘要,Figure 1 *

Also Published As

Publication number Publication date
EP3464270B1 (en) 2022-02-23
US10696655B2 (en) 2020-06-30
MA45122A (fr) 2019-04-10
EP4067347B1 (en) 2024-06-19
US20200399244A1 (en) 2020-12-24
US20190152949A1 (en) 2019-05-23
CN109476641A (zh) 2019-03-15
CN115028617A (zh) 2022-09-09
EP3464270A2 (en) 2019-04-10
EP4067347A1 (en) 2022-10-05
US11168070B2 (en) 2021-11-09
WO2017205536A3 (en) 2018-01-04
JP2019516757A (ja) 2019-06-20
WO2017205536A2 (en) 2017-11-30
JP7160688B2 (ja) 2022-10-25
EP4067347C0 (en) 2024-06-19
JP2023002643A (ja) 2023-01-10

Similar Documents

Publication Publication Date Title
US11168070B2 (en) Therapeutic compounds and uses thereof
CN107108512B (zh) 治疗性化合物及其用途
CN109476663B (zh) 用于治疗癌症的吡唑并吡啶衍生物
CN107531668B (zh) 治疗性哒嗪化合物及其用途
CN107108614B (zh) 作为布罗莫结构域抑制剂的取代的吡咯并吡啶
CN107531690B (zh) 用作CBP和/或EP300抑制剂的4,5,6,7-四氢-1H-吡唑并[4,3-c]吡啶-3-胺化合物
CN107074824B (zh) 作为用于治疗癌症的pcaf和gcn5抑制剂的式(i)的酞嗪衍生物
CN116003409A (zh) 作为布罗莫结构域抑制剂的经取代的吡咯并吡啶
CN107531692B (zh) 治疗化合物及其用途
CN107406429B (zh) 哒嗪酮衍生物及其在治疗癌症中的用途
HK40079501A (en) Heterocyclic inhibitors of cbp/ep300 and their use in treatment of cancer
HK40005957B (en) Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
HK40005957A (en) Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
HK40079390A (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK40005958A (en) Pyrazolopyridine derivatives for the treatment of cancer
HK1243073B (zh) 治療性化合物及其用途
HK40005958B (zh) 用於治疗癌症的吡唑并吡啶衍生物
HK1242695A1 (en) Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer
HK1248695B (zh) 用作cbp和/或ep300抑制劑的4,5,6,7-四氫-1h-吡唑並[4,3-c]吡啶-3-胺化合物
HK1243072A1 (zh) 布罗莫结构域抑制剂及其用途
HK1248696B (zh) 治療性噠嗪化合物及其用途
HK1244282A1 (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK1244282B (en) Substituted pyrrolopyrdines as inhibitors of bromodomain
HK1248697B (zh) 治療化合物及其用途

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
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40005957

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20220705