JP2021502987A - 線維性疾患の治療における使用のための化合物及びその医薬組成物 - Google Patents

線維性疾患の治療における使用のための化合物及びその医薬組成物 Download PDF

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JP2021502987A
JP2021502987A JP2020526530A JP2020526530A JP2021502987A JP 2021502987 A JP2021502987 A JP 2021502987A JP 2020526530 A JP2020526530 A JP 2020526530A JP 2020526530 A JP2020526530 A JP 2020526530A JP 2021502987 A JP2021502987 A JP 2021502987A
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dihydro
ylmethoxy
isoquinoline
dioxane
pyrimid
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JP2021502987A5 (https=
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クリストフェ クサビエル ブリス レジナルド
クリストフェ クサビエル ブリス レジナルド
クレメント‐ラクロイックス フィリッペ
クレメント‐ラクロイックス フィリッペ
イルマ ジョエル デ ヴォス スティーブ
イルマ ジョエル デ ヴォス スティーブ
レイモンド モーリス サニエレ ローラン
レイモンド モーリス サニエレ ローラン
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Galapagos NV
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Galapagos NV
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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 JP2021502987A publication Critical patent/JP2021502987A/ja
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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
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    • 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
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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)
JP2020526530A 2017-11-15 2018-11-15 線維性疾患の治療における使用のための化合物及びその医薬組成物 Pending JP2021502987A (ja)

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

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Publication Number Publication Date
JP2021502987A true JP2021502987A (ja) 2021-02-04
JP2021502987A5 JP2021502987A5 (https=) 2021-12-16

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JP2020526530A Pending JP2021502987A (ja) 2017-11-15 2018-11-15 線維性疾患の治療における使用のための化合物及びその医薬組成物

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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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024523460A (ja) * 2021-06-21 2024-06-28 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

Families Citing this family (8)

* 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
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
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
CN119591596B (zh) * 2024-12-04 2025-10-17 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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015500861A (ja) * 2011-12-22 2015-01-08 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 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
WO2015197550A1 (en) * 2014-06-25 2015-12-30 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
JP2016503765A (ja) * 2012-12-20 2016-02-08 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 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）
JP2016510769A (ja) * 2013-03-15 2016-04-11 プロメティック・バイオサイエンシーズ・インコーポレイテッドＰｒｏＭｅｔｉｃ ＢｉｏＳｃｉｅｎｃｅｓ Ｉｎｃ． 肺線維症、肝線維症、皮膚線維症、及び心線維症の治療のための置換芳香族化合物
JP2018513180A (ja) * 2015-04-23 2018-05-24 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 炎症性障害の治療のための新規ジヒドロピリドイソキノリノン及びその医薬組成物

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
JP2015500861A (ja) * 2011-12-22 2015-01-08 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 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
JP2016503765A (ja) * 2012-12-20 2016-02-08 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 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）
JP2016510769A (ja) * 2013-03-15 2016-04-11 プロメティック・バイオサイエンシーズ・インコーポレイテッドＰｒｏＭｅｔｉｃ ＢｉｏＳｃｉｅｎｃｅｓ Ｉｎｃ． 肺線維症、肝線維症、皮膚線維症、及び心線維症の治療のための置換芳香族化合物
WO2015197550A1 (en) * 2014-06-25 2015-12-30 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
JP2018513180A (ja) * 2015-04-23 2018-05-24 ガラパゴス・ナムローゼ・フェンノートシャップＧａｌａｐａｇｏｓ Ｎ．Ｖ． 炎症性障害の治療のための新規ジヒドロピリドイソキノリノン及びその医薬組成物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024523460A (ja) * 2021-06-21 2024-06-28 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
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

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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
AU2018367193A1 (en) 2020-07-02
CO2020005919A2 (es) 2020-05-29
CA3082742A1 (en) 2019-05-23
WO2019096944A1 (en) 2019-05-23
CN111343986A (zh) 2020-06-26
KR20200088844A (ko) 2020-07-23

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