CN104870445B - 用于治疗炎性疾病的新二氢嘧啶并异喹啉酮类及其药物组合物(gpr84拮抗剂) - Google Patents

用于治疗炎性疾病的新二氢嘧啶并异喹啉酮类及其药物组合物(gpr84拮抗剂) Download PDF

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Publication number
CN104870445B
CN104870445B CN201380067345.2A CN201380067345A CN104870445B CN 104870445 B CN104870445 B CN 104870445B CN 201380067345 A CN201380067345 A CN 201380067345A CN 104870445 B CN104870445 B CN 104870445B
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dihydro
ylmethoxy
pyrimido
isoquinolin
pyridin
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Chinese (zh)
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CN104870445A (zh
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F·拉贝古尔
L·阿尔维
G·纽瑟姆
L·萨尼尔
S·弗莱彻
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Galapagos NV
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Galapagos NV
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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201380067345.2A 2012-12-20 2013-12-17 用于治疗炎性疾病的新二氢嘧啶并异喹啉酮类及其药物组合物(gpr84拮抗剂) Expired - Fee Related CN104870445B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261740028P 2012-12-20 2012-12-20
US61/740,028 2012-12-20
PCT/EP2013/076818 WO2014095798A1 (en) 2012-12-20 2013-12-17 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)

Publications (2)

Publication Number Publication Date
CN104870445A CN104870445A (zh) 2015-08-26
CN104870445B true CN104870445B (zh) 2017-09-15

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CN201380067345.2A Expired - Fee Related CN104870445B (zh) 2012-12-20 2013-12-17 用于治疗炎性疾病的新二氢嘧啶并异喹啉酮类及其药物组合物(gpr84拮抗剂)

Country Status (5)

Country Link
US (2) US9708312B2 (enExample)
EP (1) EP2935262B1 (enExample)
JP (1) JP6293784B2 (enExample)
CN (1) CN104870445B (enExample)
WO (1) WO2014095798A1 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
GB201506894D0 (en) 2015-04-23 2015-06-10 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
JP6918957B2 (ja) * 2017-03-06 2021-08-11 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズＳｈａｎｇｈａｉ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｍａｔｅｒｉａ Ｍｅｄｉｃａ， Ｃｈｉｎｅｓｅ Ａｃａｄｅｍｙ Ｏｆ Ｓｃｉｅｎｃｅｓ Ｇｐｒ８４受容体拮抗剤およびその使用
EP3403649A1 (en) 2017-05-16 2018-11-21 Bayer Pharma Aktiengesellschaft Inhibitors and antagonists of gpr84 for the treatment of endometriosis
WO2019096944A1 (en) 2017-11-15 2019-05-23 Galapagos Nv Compounds and pharmaceutical compositions thereof for use in the treatment of fibrotic diseases
WO2020007342A1 (zh) * 2018-07-06 2020-01-09 中国科学院上海药物研究所 联苯磷酸酯类化合物作为gpr84拮抗剂的应用
JOP20220156A1 (ar) 2019-12-19 2023-01-30 Bayer Ag مشتقات فوروإندازول
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
CA3206499A1 (en) 2021-02-02 2022-08-11 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
WO2022179940A1 (en) 2021-02-23 2022-09-01 Bayer Aktiengesellschaft Furoindazole derivatives as gpr84 antagonists
CN115109072A (zh) * 2021-03-18 2022-09-27 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
CA3218018A1 (en) 2021-04-29 2022-11-03 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
US20250066335A1 (en) 2021-06-18 2025-02-27 University Of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
EP4361151A4 (en) * 2021-06-21 2025-06-11 Wuhan Humanwell Innovative Drug Research and Development Center Limited Company Tricyclic compound as a GPR84 antagonist
CN115611944A (zh) * 2021-07-15 2023-01-17 中国科学院上海药物研究所 不对称gpr84拮抗剂及其用途
EP4467543A4 (en) 2022-01-21 2025-12-17 Xizang Haisco Pharmaceutical Co Ltd TRICYCLICAL CONDENSED HETEROCYCLICAL PDE3/4 DOUBLE INTHIBITOR AND USE OF THEREBY
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain
CN120569392A (zh) * 2022-12-30 2025-08-29 广州市联瑞制药有限公司 三环类化合物及其制备方法和应用
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2801289A1 (de) * 1977-05-05 1979-05-03 Hoechst Ag Pyrimido(6,1-a)isochinolin-2-on- derivate
WO2005007092A2 (en) * 2003-07-08 2005-01-27 Smithkline Beecham Corporation Novel chemical compounds
WO2007027661A2 (en) * 2005-09-02 2007-03-08 Arena Pharmaceuticals, Inc. Human g protein-coupled receptor and modulators thereof for the treatment of atherosclerosis and atherosclerotic disease and for the treatment of conditions related to mcp-1 expression
JP2011088847A (ja) * 2009-10-21 2011-05-06 Takeda Chem Ind Ltd 三環性化合物およびその用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR089284A1 (es) * 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2801289A1 (de) * 1977-05-05 1979-05-03 Hoechst Ag Pyrimido(6,1-a)isochinolin-2-on- derivate
WO2005007092A2 (en) * 2003-07-08 2005-01-27 Smithkline Beecham Corporation Novel chemical compounds
WO2007027661A2 (en) * 2005-09-02 2007-03-08 Arena Pharmaceuticals, Inc. Human g protein-coupled receptor and modulators thereof for the treatment of atherosclerosis and atherosclerotic disease and for the treatment of conditions related to mcp-1 expression
JP2011088847A (ja) * 2009-10-21 2011-05-06 Takeda Chem Ind Ltd 三環性化合物およびその用途

Also Published As

Publication number Publication date
US20160039807A1 (en) 2016-02-11
US9708312B2 (en) 2017-07-18
WO2014095798A1 (en) 2014-06-26
JP2016503765A (ja) 2016-02-08
EP2935262A1 (en) 2015-10-28
EP2935262B1 (en) 2017-03-15
CN104870445A (zh) 2015-08-26
US20180016275A1 (en) 2018-01-18
JP6293784B2 (ja) 2018-03-14

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