JP6293784B2 - 炎症性障害の治療のための新規ジヒドロピリミジノイソキノリノン及びその医薬組成物（ｇｐｒ８４アンタゴニスト） - Google Patents

炎症性障害の治療のための新規ジヒドロピリミジノイソキノリノン及びその医薬組成物（ｇｐｒ８４アンタゴニスト） Download PDF

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JP6293784B2
JP6293784B2 JP2015548428A JP2015548428A JP6293784B2 JP 6293784 B2 JP6293784 B2 JP 6293784B2 JP 2015548428 A JP2015548428 A JP 2015548428A JP 2015548428 A JP2015548428 A JP 2015548428A JP 6293784 B2 JP6293784 B2 JP 6293784B2
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dihydro
ylmethoxy
pyrimido
isoquinolin
pyridin
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JP2016503765A5 (enExample
JP2016503765A (ja
Inventor
ラベグエレ フレデリク
ラベグエレ フレデリク
アルベイ ルケ
アルベイ ルケ
ニュウサム グレゴリ
ニュウサム グレゴリ
サニエレ ラウレント
サニエレ ラウレント
フレッチャー スティーブン
フレッチャー スティーブン
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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)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2015548428A 2012-12-20 2013-12-17 炎症性障害の治療のための新規ジヒドロピリミジノイソキノリノン及びその医薬組成物（ｇｐｒ８４アンタゴニスト） Expired - Fee Related JP6293784B2 (ja)

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 (3)

Publication Number Publication Date
JP2016503765A JP2016503765A (ja) 2016-02-08
JP2016503765A5 JP2016503765A5 (enExample) 2017-01-26
JP6293784B2 true JP6293784B2 (ja) 2018-03-14

Family

ID=49841660

Family Applications (1)

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JP2015548428A Expired - Fee Related JP6293784B2 (ja) 2012-12-20 2013-12-17 炎症性障害の治療のための新規ジヒドロピリミジノイソキノリノン及びその医薬組成物（ｇｐｒ８４アンタゴニスト）

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 (21)

* 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
US20210106582A1 (en) 2017-11-15 2021-04-15 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
PH12022551509A1 (en) * 2019-12-19 2023-04-24 Bayer Ag Furoindazole derivatives
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
KR20230153387A (ko) 2021-02-02 2023-11-06 리미널 바이오사이언시스 리미티드 Gpr84 길항제 및 이의 용도
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
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
WO2022229061A1 (en) 2021-04-29 2022-11-03 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
WO2022263676A1 (en) 2021-06-18 2022-12-22 University Of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
JP7705966B2 (ja) * 2021-06-21 2025-07-10 武漢人福創新薬物研発中心有限公司 Ｇｐｒ８４アンタゴニストとしての三環式化合物
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
US20250171436A1 (en) 2022-01-21 2025-05-29 Xizang Haisco Pharmaceutical Co., Ltd. Tricyclic Fused Heterocyclic PDE3/4 Dual Inhibitor and Use Thereof
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain
WO2024140969A1 (zh) * 2022-12-30 2024-07-04 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
US20260091147A1 (en) * 2023-04-17 2026-04-02 The Board Of Trustees Of The Leland Standford Junior University Method for detecting innate immune action in vivo using gpr84-pet

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2720085A1 (de) * 1977-05-05 1978-11-16 Hoechst Ag Pyrimido(6,1-a)isochinolin-2-on- derivate
US7501512B2 (en) * 2003-07-08 2009-03-10 Smithkline Beecham Corporation Chemical compounds
CA2621144A1 (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
AR089284A1 (es) * 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios

Also Published As

Publication number Publication date
WO2014095798A1 (en) 2014-06-26
CN104870445A (zh) 2015-08-26
EP2935262B1 (en) 2017-03-15
US20180016275A1 (en) 2018-01-18
CN104870445B (zh) 2017-09-15
US20160039807A1 (en) 2016-02-11
JP2016503765A (ja) 2016-02-08
EP2935262A1 (en) 2015-10-28
US9708312B2 (en) 2017-07-18

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