CN111343986A - 用于治疗纤维化疾病的化合物及其药物组合物 - Google Patents

用于治疗纤维化疾病的化合物及其药物组合物 Download PDF

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Publication number
CN111343986A
CN111343986A CN201880074060.4A CN201880074060A CN111343986A CN 111343986 A CN111343986 A CN 111343986A CN 201880074060 A CN201880074060 A CN 201880074060A CN 111343986 A CN111343986 A CN 111343986A
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CN
China
Prior art keywords
dihydro
ylmethoxy
isoquinolin
dioxan
pyrimido
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.)
Pending
Application number
CN201880074060.4A
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English (en)
Chinese (zh)
Inventor
R·C·X·布莱斯
P·克莱门特-拉克鲁瓦
S·I·J·德沃斯
L·R·M·萨尼莱
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Galapagos NV
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Galapagos NV
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Publication date
Priority claimed from GBGB1718838.4A external-priority patent/GB201718838D0/en
Priority claimed from GBGB1817346.8A external-priority patent/GB201817346D0/en
Application filed by Galapagos NV filed Critical Galapagos NV
Publication of CN111343986A publication Critical patent/CN111343986A/zh
Pending legal-status Critical Current

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    • 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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2063—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
CN201880074060.4A 2017-11-15 2018-11-15 用于治疗纤维化疾病的化合物及其药物组合物 Pending CN111343986A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB1718838.4 2017-11-15
GBGB1718838.4A GB201718838D0 (en) 2017-11-15 2017-11-15 Compounds and pharmaceutical compositions thereof for use in the treatment of fibrotic diseases
GBGB1817346.8A GB201817346D0 (en) 2018-10-25 2018-10-25 Compounds and pharmaceutical compositions thereof for use in the treatment of diseases
GB1817346.8 2018-10-25
PCT/EP2018/081457 WO2019096944A1 (en) 2017-11-15 2018-11-15 Compounds and pharmaceutical compositions thereof for use in the treatment of fibrotic diseases

Publications (1)

Publication Number Publication Date
CN111343986A true CN111343986A (zh) 2020-06-26

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ID=64746511

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880074060.4A Pending CN111343986A (zh) 2017-11-15 2018-11-15 用于治疗纤维化疾病的化合物及其药物组合物

Country Status (16)

Country Link
US (2) US20210106582A1 (https=)
EP (2) EP4186507A1 (https=)
JP (1) JP2021502987A (https=)
KR (1) KR20200088844A (https=)
CN (1) CN111343986A (https=)
AU (1) AU2018367193A1 (https=)
BR (1) BR112020008425A2 (https=)
CA (1) CA3082742A1 (https=)
CO (1) CO2020005919A2 (https=)
IL (1) IL274578A (https=)
MA (1) MA50905A (https=)
MX (1) MX2020004810A (https=)
PH (1) PH12020550616A1 (https=)
RU (1) RU2020119415A (https=)
SG (1) SG11202004408YA (https=)
WO (1) WO2019096944A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022194267A1 (zh) * 2021-03-18 2022-09-22 武汉人福创新药物研发中心有限公司 一种gpr84拮抗剂及其制备方法和用途
WO2022218372A1 (zh) * 2021-04-14 2022-10-20 武汉人福创新药物研发中心有限公司 一种二氢嘧啶并异喹啉酮类衍生物及用途
WO2022268088A1 (zh) * 2021-06-21 2022-12-29 武汉人福创新药物研发中心有限公司 用于gpr84拮抗剂的三环化合物
CN119591596A (zh) * 2024-12-04 2025-03-11 沈阳药科大学 4,5-二氢-3H-吡咯并[2,3-c]喹啉-4-酮衍生物及其应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
WO2022112186A1 (en) 2020-11-24 2022-06-02 Galapagos Nv Compound for use in and methods of treatment of fibrotic diseases
JP2024506858A (ja) 2021-02-02 2024-02-15 リミナル・バイオサイエンシーズ・リミテッド Ｇｐｒ８４アンタゴニストおよびその使用
US20250066335A1 (en) 2021-06-18 2025-02-27 University Of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
WO2024220480A2 (en) * 2023-04-17 2024-10-24 The Board Of Trustees Of The Leland Stanford Junior University Method for detecting innate immune action in vivo using gpr84-pet

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013092791A1 (en) * 2011-12-22 2013-06-27 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2014095798A1 (en) * 2012-12-20 2014-06-26 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
WO2014138907A1 (en) * 2013-03-15 2014-09-18 Prometic Biosciences Inc. Substituted aromatic compounds for the treatment of pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis
WO2015197550A1 (en) * 2014-06-25 2015-12-30 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2016169911A1 (en) * 2015-04-23 2016-10-27 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2970255T1 (sl) 2013-03-14 2017-12-29 Galapagos Nv Spojine in farmacevtski sestavki le-teh za zdravljenje vnetnih motenj
GB201603745D0 (en) 2016-03-04 2016-04-20 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013092791A1 (en) * 2011-12-22 2013-06-27 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2014095798A1 (en) * 2012-12-20 2014-06-26 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
WO2014138907A1 (en) * 2013-03-15 2014-09-18 Prometic Biosciences Inc. Substituted aromatic compounds for the treatment of pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis
WO2015197550A1 (en) * 2014-06-25 2015-12-30 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2016169911A1 (en) * 2015-04-23 2016-10-27 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022194267A1 (zh) * 2021-03-18 2022-09-22 武汉人福创新药物研发中心有限公司 一种gpr84拮抗剂及其制备方法和用途
WO2022218372A1 (zh) * 2021-04-14 2022-10-20 武汉人福创新药物研发中心有限公司 一种二氢嘧啶并异喹啉酮类衍生物及用途
WO2022268088A1 (zh) * 2021-06-21 2022-12-29 武汉人福创新药物研发中心有限公司 用于gpr84拮抗剂的三环化合物
CN119591596A (zh) * 2024-12-04 2025-03-11 沈阳药科大学 4,5-二氢-3H-吡咯并[2,3-c]喹啉-4-酮衍生物及其应用

Also Published As

Publication number Publication date
IL274578A (en) 2020-06-30
US20230241068A1 (en) 2023-08-03
RU2020119415A (ru) 2021-12-16
BR112020008425A2 (pt) 2020-11-17
EP3710004A1 (en) 2020-09-23
US20210106582A1 (en) 2021-04-15
SG11202004408YA (en) 2020-06-29
EP4186507A1 (en) 2023-05-31
PH12020550616A1 (en) 2021-03-01
MA50905A (fr) 2020-09-23
MX2020004810A (es) 2020-08-13
JP2021502987A (ja) 2021-02-04
AU2018367193A1 (en) 2020-07-02
CO2020005919A2 (es) 2020-05-29
CA3082742A1 (en) 2019-05-23
WO2019096944A1 (en) 2019-05-23
KR20200088844A (ko) 2020-07-23

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Application publication date: 20200626