WO2020177729A1 - Dérivé cyclique aromatique fusionné, procédé de préparation correspondant et utilisation pharmaceutique associée - Google Patents

Dérivé cyclique aromatique fusionné, procédé de préparation correspondant et utilisation pharmaceutique associée Download PDF

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Publication number
WO2020177729A1
WO2020177729A1 PCT/CN2020/077890 CN2020077890W WO2020177729A1 WO 2020177729 A1 WO2020177729 A1 WO 2020177729A1 CN 2020077890 W CN2020077890 W CN 2020077890W WO 2020177729 A1 WO2020177729 A1 WO 2020177729A1
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WIPO (PCT)
Prior art keywords
group
cycloalkyl
alkyl
general formula
amino
Prior art date
Application number
PCT/CN2020/077890
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English (en)
Chinese (zh)
Inventor
张晓敏
张睿
王珏
贺峰
陶维康
Original Assignee
江苏恒瑞医药股份有限公司
上海恒瑞医药有限公司
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.)
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Publication date
Application filed by 江苏恒瑞医药股份有限公司, 上海恒瑞医药有限公司 filed Critical 江苏恒瑞医药股份有限公司
Priority to CN202080005992.0A priority Critical patent/CN112955432B/zh
Publication of WO2020177729A1 publication Critical patent/WO2020177729A1/fr

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    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4741Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un dérivé cyclique aromatique fusionné, un procédé de préparation correspondant et une utilisation pharmaceutique associée. En particulier, la présente invention concerne un dérivé cyclique aromatique fusionné représenté par la formule générale (I), un procédé de préparation correspondant, une composition pharmaceutique contenant le dérivé, une utilisation de celui-ci en tant qu'inhibiteur d'ATX, et une utilisation de celui-ci dans la préparation d'un médicament pour le traitement d'un cancer ou d'une maladie ou d'un trouble de dégénérescence fibreuse. Chaque substituant dans la formule générale (I) est tel que défini dans la description.
PCT/CN2020/077890 2019-03-06 2020-03-05 Dérivé cyclique aromatique fusionné, procédé de préparation correspondant et utilisation pharmaceutique associée WO2020177729A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202080005992.0A CN112955432B (zh) 2019-03-06 2020-03-05 稠合芳香环类衍生物、其制备方法及其在医药上的应用

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201910169283 2019-03-06
CN201910169283.5 2019-03-06
CN201911374834.8 2019-12-27
CN201911374834 2019-12-27

Publications (1)

Publication Number Publication Date
WO2020177729A1 true WO2020177729A1 (fr) 2020-09-10

Family

ID=72337609

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2020/077890 WO2020177729A1 (fr) 2019-03-06 2020-03-05 Dérivé cyclique aromatique fusionné, procédé de préparation correspondant et utilisation pharmaceutique associée

Country Status (3)

Country Link
CN (1) CN112955432B (fr)
TW (1) TW202100512A (fr)
WO (1) WO2020177729A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113493453A (zh) * 2020-04-07 2021-10-12 江苏恒瑞医药股份有限公司 稠合芳香环类衍生物、其制备方法及其在医药上的应用
WO2022007882A1 (fr) * 2020-07-09 2022-01-13 苏州爱科百发生物医药技术有限公司 Inhibiteur d'atx, son procédé de préparation et son utilisation
WO2022135590A1 (fr) * 2020-12-27 2022-06-30 上海凌达生物医药有限公司 Composés pyrimido-hétérocycliques, et leur procédé de préparation et leur utilisation
WO2023093832A1 (fr) * 2021-11-25 2023-06-01 上海济煜医药科技有限公司 Dérivé tricyclique et procédé de préparation s'y rapportant et application associée
US11820747B2 (en) 2021-11-02 2023-11-21 Flare Therapeutics Inc. PPARG inverse agonists and uses thereof
US11912668B2 (en) 2020-11-18 2024-02-27 Deciphera Pharmaceuticals, Llc GCN2 and perk kinase inhibitors and methods of use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996036633A1 (fr) * 1995-05-17 1996-11-21 E.I. Du Pont De Nemours And Company Amides cycliques fongiques
WO1997000612A1 (fr) * 1995-06-20 1997-01-09 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides
WO1998005652A2 (fr) * 1996-08-01 1998-02-12 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides
WO1998023155A1 (fr) * 1996-11-26 1998-06-04 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996036633A1 (fr) * 1995-05-17 1996-11-21 E.I. Du Pont De Nemours And Company Amides cycliques fongiques
WO1997000612A1 (fr) * 1995-06-20 1997-01-09 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides
WO1998005652A2 (fr) * 1996-08-01 1998-02-12 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides
WO1998023155A1 (fr) * 1996-11-26 1998-06-04 E.I. Du Pont De Nemours And Company Amides cycliques arthropodicides et fongicides

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113493453A (zh) * 2020-04-07 2021-10-12 江苏恒瑞医药股份有限公司 稠合芳香环类衍生物、其制备方法及其在医药上的应用
CN113493453B (zh) * 2020-04-07 2023-06-16 江苏恒瑞医药股份有限公司 稠合芳香环类衍生物、其制备方法及其在医药上的应用
WO2022007882A1 (fr) * 2020-07-09 2022-01-13 苏州爱科百发生物医药技术有限公司 Inhibiteur d'atx, son procédé de préparation et son utilisation
US11912668B2 (en) 2020-11-18 2024-02-27 Deciphera Pharmaceuticals, Llc GCN2 and perk kinase inhibitors and methods of use thereof
WO2022135590A1 (fr) * 2020-12-27 2022-06-30 上海凌达生物医药有限公司 Composés pyrimido-hétérocycliques, et leur procédé de préparation et leur utilisation
US11820747B2 (en) 2021-11-02 2023-11-21 Flare Therapeutics Inc. PPARG inverse agonists and uses thereof
WO2023093832A1 (fr) * 2021-11-25 2023-06-01 上海济煜医药科技有限公司 Dérivé tricyclique et procédé de préparation s'y rapportant et application associée

Also Published As

Publication number Publication date
TW202100512A (zh) 2021-01-01
CN112955432A (zh) 2021-06-11
CN112955432B (zh) 2022-11-22

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