CN115667236B - 1,5-二氢-2,4-苯二氮䓬-3-酮衍生物及其应用 - Google Patents

1,5-二氢-2,4-苯二氮䓬-3-酮衍生物及其应用 Download PDF

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CN115667236B
CN115667236B CN202180029971.7A CN202180029971A CN115667236B CN 115667236 B CN115667236 B CN 115667236B CN 202180029971 A CN202180029971 A CN 202180029971A CN 115667236 B CN115667236 B CN 115667236B
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methyl
hydrogen
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CN115667236A (zh
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徐祥清
邱印利
郭强
于民权
赵松
李曲祥
靖鹏
侯媛媛
董莹莹
吴国胜
张双
陆爱军
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Nhwa Pharmaceutical Corp
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • 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
    • C07D471/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202180029971.7A 2020-04-26 2021-04-25 1,5-二氢-2,4-苯二氮䓬-3-酮衍生物及其应用 Active CN115667236B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN202010330893 2020-04-26
CN2020103308931 2020-04-26
CN2021102881418 2021-03-17
CN202110288141 2021-03-17
PCT/CN2021/089660 WO2021218863A1 (zh) 2020-04-26 2021-04-25 1,5-二氢-2,4-苯二氮䓬-3-酮衍生物及其应用

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CN115667236A CN115667236A (zh) 2023-01-31
CN115667236B true CN115667236B (zh) 2024-04-26

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US (1) US12559471B2 (https=)
EP (1) EP4144725B1 (https=)
JP (1) JP7693709B2 (https=)
KR (1) KR102832951B1 (https=)
CN (1) CN115667236B (https=)
AU (1) AU2021262281B2 (https=)
BR (1) BR112022021228A2 (https=)
CA (1) CA3172692C (https=)
WO (1) WO2021218863A1 (https=)

Families Citing this family (4)

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Publication number Priority date Publication date Assignee Title
CN115605202B (zh) 2020-03-26 2025-10-28 盐野义制药株式会社 具有血清素受体结合活性的芳香族杂环衍生物
CN121039114A (zh) 2023-04-21 2025-11-28 江苏恩华药业股份有限公司 1,5-二氢-2,4-苯二氮䓬-3-酮衍生物枸橼酸盐的晶型、制备方法及其应用
WO2025044768A1 (zh) * 2023-08-29 2025-03-06 江苏恩华药业股份有限公司 1,5-二氢-2,4-苯二氮䓬-3-酮衍生物的制备方法和其中间体及其制备方法
CN120329280A (zh) * 2024-01-17 2025-07-18 江苏恩华药业股份有限公司 取代的1,2,4-四氢-3h-苯并二氮䓬-3-酮衍生物及其应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1985002843A1 (fr) * 1983-12-24 1985-07-04 Nippon Soda Co., Ltd. DERIVES D'IMIDAZO AD1,5-a BD PYRIDIN-3-ONE ET LEUR PROCEDE DE PREPARATION
WO1997038984A1 (en) * 1996-04-17 1997-10-23 Du Pont Pharmaceuticals Company N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-one derivatives as factor xa inhibitors
CN1238689A (zh) * 1996-10-02 1999-12-15 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
WO2001002358A2 (en) * 1999-07-06 2001-01-11 Vertex Pharmaceuticals Incorporated Cyclized amide derivatives for treating or preventing neuronal damage
CN1215054C (zh) * 1997-08-06 2005-08-17 辛根塔参与股份公司 杀微生物的n－磺酰基甘氨酸炔氧基苯乙基酰胺衍生物
WO2008132139A2 (en) * 2007-04-27 2008-11-06 Ucb Pharma S.A. New heterocyclic derivatives useful for the treatment of cns disorders
CN101304980A (zh) * 2005-12-24 2008-11-12 贝林格尔·英格海姆国际有限公司 3－(4－哌啶基)－2,3,4,5,－四氢－1,3－苯并二氮杂䓬－2(1h)－酮
CN103702983A (zh) * 2011-05-12 2014-04-02 艾伯维德国有限责任两合公司 苯并氮杂环庚烯衍生物、含有它们的药物组合物及其在治疗中的用途

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ES2197160T3 (es) * 1992-12-21 2004-01-01 Smithkline Beecham Corp Antagonistas fibronogeno bicicliclos.
SI1720836T1 (sl) * 2004-02-25 2014-06-30 Eli Lilly And Company 6-substituirani 2,3,4,5-tetrahidro-1h-benzo (d)azepini kot agonisti 5-ht2c receptorja
KR101594898B1 (ko) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로벤자제핀, 및 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
JP5502733B2 (ja) * 2007-07-26 2014-05-28 エフ．ホフマン−ラ ロシュ アーゲー ５−ｈｔ２ａ及びｄ３受容体の二重のモジュレーター
EP3409658B9 (en) * 2016-01-29 2024-07-17 ONO Pharmaceutical Co., Ltd. Tetrahydronaphthalene derivative

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1985002843A1 (fr) * 1983-12-24 1985-07-04 Nippon Soda Co., Ltd. DERIVES D'IMIDAZO AD1,5-a BD PYRIDIN-3-ONE ET LEUR PROCEDE DE PREPARATION
WO1997038984A1 (en) * 1996-04-17 1997-10-23 Du Pont Pharmaceuticals Company N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-one derivatives as factor xa inhibitors
CN1238689A (zh) * 1996-10-02 1999-12-15 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
CN1215054C (zh) * 1997-08-06 2005-08-17 辛根塔参与股份公司 杀微生物的n－磺酰基甘氨酸炔氧基苯乙基酰胺衍生物
WO2001002358A2 (en) * 1999-07-06 2001-01-11 Vertex Pharmaceuticals Incorporated Cyclized amide derivatives for treating or preventing neuronal damage
CN101304980A (zh) * 2005-12-24 2008-11-12 贝林格尔·英格海姆国际有限公司 3－(4－哌啶基)－2,3,4,5,－四氢－1,3－苯并二氮杂䓬－2(1h)－酮
WO2008132139A2 (en) * 2007-04-27 2008-11-06 Ucb Pharma S.A. New heterocyclic derivatives useful for the treatment of cns disorders
CN103702983A (zh) * 2011-05-12 2014-04-02 艾伯维德国有限责任两合公司 苯并氮杂环庚烯衍生物、含有它们的药物组合物及其在治疗中的用途

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Title
选择性5-HT2A 受体反向激动剂哌马色林的药理作用与临床评价;田超 等;《临床药物治疗杂志》;15-19 *

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JP7693709B2 (ja) 2025-06-17
BR112022021228A2 (pt) 2022-12-06
JP2023522078A (ja) 2023-05-26
EP4144725B1 (en) 2025-11-26
KR102832951B1 (ko) 2025-07-10
AU2021262281A1 (en) 2022-11-24
US12559471B2 (en) 2026-02-24
EP4144725A1 (en) 2023-03-08
WO2021218863A1 (zh) 2021-11-04
CN115667236A (zh) 2023-01-31
CA3172692C (en) 2024-05-14
AU2021262281B2 (en) 2024-11-28
US20230132621A1 (en) 2023-05-04
CA3172692A1 (en) 2021-11-04
EP4144725C0 (en) 2025-11-26
KR20230004662A (ko) 2023-01-06
EP4144725A4 (en) 2023-10-25

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