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.)
Active
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
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02—Seven-membered rings
    • C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/10—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—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
    • C07D487/02—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
    • C07D487/22—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 four or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (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 Active 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
CNPCT/CN2016/083124 2016-05-24
CN2016083124 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 Active 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 (https=)
EP (2) EP3464270B1 (https=)
JP (2) JP7160688B2 (https=)
CN (2) CN109476641B (https=)
MA (1) MA45122A (https=)
WO (1) WO2017205536A2 (https=)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109640959B (zh) 2016-04-29 2023-03-17 西奈山伊坎医学院 靶向先天免疫系统以诱导长期耐受性及解决动脉粥样硬化中的巨噬细胞累积
EP3464270B1 (en) 2016-05-24 2022-02-23 Genentech, Inc. Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
ES2928773T3 (es) 2017-01-17 2022-11-22 Heparegenix Gmbh Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
KR102563325B1 (ko) * 2017-06-30 2023-08-03 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Ｒｈｏ-관련 단백질 키나아제 억제제, Ｒｈｏ-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
CN110582491B (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
JP7311228B2 (ja) * 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
TWI795440B (zh) 2017-09-15 2023-03-11 美商佛瑪治療公司 作為ＣＢＰ／ｐ３００抑制劑之四氫─咪唑並喹啉化合物
WO2019161162A1 (en) * 2018-02-16 2019-08-22 Constellation Pharmaceuticals, Inc. P300/cbp hat inhibitors
US11414384B2 (en) 2018-02-16 2022-08-16 Constellation Pharmaceuticals, Inc. P300/CBP hat inhibitors
RU2020131507A (ru) * 2018-03-29 2022-05-04 Боард Оф Реджентс, Де Юниверсити Оф Техас Систем Имидазопиперазиновые ингибиторы белков-активаторов транскрипции
WO2019195846A1 (en) 2018-04-06 2019-10-10 Board Of Regents, The University Of Texas System Imidazopiperazinone inhibitors of transcription activating proteins
JP7197075B2 (ja) * 2018-04-20 2022-12-27 中国科学院上海薬物研究所 ヒストンアセチルトランスフェラーゼ（ｈａｔ）阻害剤及びその用途
EP3793521A4 (en) * 2018-05-18 2022-02-23 Janssen Biotech, Inc. SAFE AND EFFECTIVE METHOD OF TREATING LUPUS WITH AN ANTI-IL12/IL23 ANTIBODY
US10870648B2 (en) 2018-06-29 2020-12-22 Forma Therapeutics, Inc. Inhibiting CREB binding protein (CBP)
IL280539B2 (en) 2018-08-02 2024-08-01 Univ Boston Late sv40 factor (lsf) inhibitors
CN109336836A (zh) * 2018-11-23 2019-02-15 厦门大学 Carm1小分子抑制剂的化合物及用途
US20220135538A1 (en) * 2019-02-27 2022-05-05 Constellation Pharmaceuticals, Inc. P300/cbp hat inhibitors and methods for their use
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
WO2020190791A1 (en) 2019-03-15 2020-09-24 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
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
US11242353B2 (en) 2020-01-24 2022-02-08 Trustees Of Boston University Heterocyclic LSF inhibitors and their uses
KR102939417B1 (ko) * 2020-04-25 2026-03-17 파마블럭 사이언시스 (난징), 인코포레이티드 Cbp/ep 300 억제제 및 이의 용도
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
AU2021341879A1 (en) * 2020-09-09 2023-04-13 Aurigene Oncology Limited Heterocyclic compounds as CBP/EP300 bromodomain inhibitors
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)
EP4221708A4 (en) 2020-10-02 2024-11-06 Board of Regents, The University of Texas System IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION-ACTIVATING PROTEINS
CA3193745A1 (en) 2020-10-02 2022-04-07 Kang Le Imidazopiperazine inhibitors of transcription activating proteins
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
IL326766A (en) * 2023-08-30 2026-04-01 Oncopia Therapeutics Inc D/B/A Sk Life Science Labs Compounds and preparations as CBP/P300 compounds and their uses
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
EP0491007B1 (en) 1989-09-08 1996-03-13 The Johns Hopkins University 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
DE69428764T2 (de) 1993-12-24 2002-06-20 Merck Patent Gmbh Immunokonjugate
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
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
WO1996003397A1 (en) 1994-07-21 1996-02-08 Akzo Nobel N.V. Cyclic ketone peroxide formulations
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
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
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
EA001595B1 (ru) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
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
WO1998050038A1 (en) 1997-05-06 1998-11-12 American Cyanamid Company Use of quinazoline compounds for the treatment of polycystic kidney disease
ZA986729B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
BR9814116A (pt) 1997-11-06 2000-10-03 American Cyanamid Co Uso de derivados de quinazolina como inibidores de cinase de tirosina para tratamento de pólipo colÈnico
EA003786B1 (ru) 1998-11-19 2003-10-30 Варнер Ламберт Компани N-[4-(3-хлор-4-фторфениламино)-7-(3-морфолин-4-илпропокси)хиназолин-6-ил]акриламид - необратимый ингибитор тирозинкиназ
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
AU2007309708A1 (en) * 2006-03-13 2008-05-02 Merck Sharp & Dohme Corp. Somatostatin agonists
US7989472B2 (en) * 2006-03-23 2011-08-02 Merck Sharp & Dohme Corp. 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
US8324226B2 (en) * 2007-10-24 2012-12-04 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
WO2009071895A1 (en) * 2007-12-04 2009-06-11 Ucb Pharma S.A. Fused thiazole and thiophene derivatives as kinase inhibitors
GB0723747D0 (en) * 2007-12-04 2008-12-31 Ucb Pharma Sa Therapeutic agents
CN101970499B (zh) 2008-02-11 2014-12-31 治疗科技公司 用于肿瘤治疗的单克隆抗体
EP2262837A4 (en) 2008-03-12 2011-04-06 Merck Sharp & Dohme PD-1 BINDING PROTEINS
JP2012500855A (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 Ｐｄ−１アンタゴニストおよび感染性疾患を処置するための方法
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
WO2010075270A1 (en) * 2008-12-22 2010-07-01 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
CN102459248A (zh) * 2009-05-26 2012-05-16 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧杂环庚三烯以及它们使用与制造方法
GB0919431D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. 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
WO2012058671A1 (en) * 2010-10-31 2012-05-03 Endo Pharmaceuticals Inc. Substituted quinazoline and pyrido-pyrimidine derivatives
EA026115B1 (ru) * 2010-12-17 2017-03-31 Ф. Хоффманн-Ля Рош Аг Замещенные 6,6-конденсированные азотсодержащие гетероциклические соединения и их применение
BR112013021675A2 (pt) * 2011-02-25 2016-11-01 Array Biopharma Inc compostos de triazolopiridina como inibidores de pim cinase
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
HUE043568T2 (hu) * 2013-03-14 2019-08-28 Glaxosmithkline Ip No 2 Ltd 2,3-diszubsztituált 1-acil-4-amino-1,2,3,4-tetrahidrokinolin származékok és bromodomén inhibitorokkénti felhasználásuk
JP6820254B2 (ja) * 2014-10-10 2021-01-27 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
EP3632915A1 (en) * 2014-11-27 2020-04-08 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
EP3464270B1 (en) 2016-05-24 2022-02-23 Genentech, Inc. Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer

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

Similar Documents

Publication Publication Date Title
CN109476641B (zh) Cbp/ep300的杂环抑制剂及其在治疗癌症中的用途
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
HK40005957A (en) Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
HK40005957B (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