CN112368281A - 作为pde3/pde4双重抑制剂的三并环类化合物 - Google Patents

作为pde3/pde4双重抑制剂的三并环类化合物 Download PDF

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CN112368281A
CN112368281A CN201980045308.9A CN201980045308A CN112368281A CN 112368281 A CN112368281 A CN 112368281A CN 201980045308 A CN201980045308 A CN 201980045308A CN 112368281 A CN112368281 A CN 112368281A
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alkyl
hydroxy
optionally
amino
compound
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CN112368281B (zh
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罗云富
潘建峰
张国利
苏胜
王勇
陈曙辉
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55—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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

公开了一类作为PDE3/PDE4双重抑制剂的三并环类化合物，及其在制备PDE3/PDE4相关疾病方面的药物的应用，尤其是在如慢性阻塞性肺病(COPD)等方面的药用功能。具体公开了式(Ⅰ)所示化合物及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201980045308.9A 2018-07-13 2019-07-12 作为pde3/pde4双重抑制剂的三并环类化合物 Active CN112368281B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210301047.6A CN114644630A (zh) 2018-07-13 2019-07-12 作为pde3/pde4双重抑制剂的三并环类化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018107723743 2018-07-13
CN201810772374 2018-07-13
PCT/CN2019/095826 WO2020011254A1 (zh) 2018-07-13 2019-07-12 作为pde3/pde4双重抑制剂的三并环类化合物

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CN112368281B CN112368281B (zh) 2022-02-18

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CN201980045308.9A Active CN112368281B (zh) 2018-07-13 2019-07-12 作为pde3/pde4双重抑制剂的三并环类化合物

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EP (1) EP3822272A4 (zh)
KR (1) KR20210031727A (zh)
CN (2) CN114644630A (zh)
AU (2) AU2019302610B2 (zh)
CA (1) CA3106052A1 (zh)
IL (1) IL280075B1 (zh)
MX (1) MX2021000456A (zh)
WO (1) WO2020011254A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114929700A (zh) * 2020-01-15 2022-08-19 正大天晴药业集团股份有限公司 三并环类pde3/pde4双重抑制剂化合物的药物组合物

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023512471A (ja) * 2020-01-15 2023-03-27 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド Ｐｄｅ３／ｐｄｅ４二重阻害剤の結晶及びその使用
KR20240004495A (ko) 2021-04-29 2024-01-11 쑤저우 선카디아 바이오파마수티컬즈 컴퍼니 리미티드 이소퀴놀론 화합물과 이의 용도
TW202325301A (zh) * 2021-12-14 2023-07-01 大陸商海思科醫藥集團股份有限公司 三環稠雜環類pde3/4雙重抑制及其用途
WO2023138676A1 (zh) * 2022-01-21 2023-07-27 四川海思科制药有限公司 三环稠杂环类pde3/4双重抑制及其用途
WO2024088402A1 (zh) * 2022-10-28 2024-05-02 江苏恒瑞医药股份有限公司 一种异喹啉酮类化合物的晶型及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4482556A (en) * 1977-05-05 1984-11-13 Hoechst Aktiengesellschaft Pyrimido (6,1-a)isoquinolin-4-one derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ185900A (en) 1976-12-10 1981-04-24 Hoechst Ag Pyrimido (6,1-a) isoquinolin-4-ones medicaments intermediate isoquinolines
CA1237429A (en) * 1983-05-05 1988-05-31 Frank Kienzle Pyrimidone derivatives
US6473627B1 (en) 1998-07-22 2002-10-29 Mitsubishi Denki Kabushiki Kaisha Mobile communication system and mobile communication method
NZ514158A (en) 1999-03-31 2000-03-29 Vernalis Ltd Derivatives of pyrimido[6,1-a]isoquinolin-4-one

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4482556A (en) * 1977-05-05 1984-11-13 Hoechst Aktiengesellschaft Pyrimido (6,1-a)isoquinolin-4-one derivatives

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114929700A (zh) * 2020-01-15 2022-08-19 正大天晴药业集团股份有限公司 三并环类pde3/pde4双重抑制剂化合物的药物组合物

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MX2021000456A (es) 2021-07-21
WO2020011254A1 (zh) 2020-01-16
JP2021532088A (ja) 2021-11-25
EP3822272A4 (en) 2022-04-06
AU2019302610B2 (en) 2023-11-23
EP3822272A1 (en) 2021-05-19
CA3106052A1 (en) 2020-01-16
US20210323960A1 (en) 2021-10-21
KR20210031727A (ko) 2021-03-22
CN112368281B (zh) 2022-02-18
AU2019302610A1 (en) 2021-03-04
AU2024201135A1 (en) 2024-03-14
IL280075A (en) 2021-03-01
CN114644630A (zh) 2022-06-21
IL280075B1 (en) 2024-02-01

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