RU2020119415A - Соединения и их фармацевтические композиции для применения при лечении фиброзных заболеваний - Google Patents

Соединения и их фармацевтические композиции для применения при лечении фиброзных заболеваний Download PDF

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Publication number
RU2020119415A
RU2020119415A RU2020119415A RU2020119415A RU2020119415A RU 2020119415 A RU2020119415 A RU 2020119415A RU 2020119415 A RU2020119415 A RU 2020119415A RU 2020119415 A RU2020119415 A RU 2020119415A RU 2020119415 A RU2020119415 A RU 2020119415A
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RU
Russia
Prior art keywords
dihydro
isoquinolin
ylmethoxy
dioxan
pyrimido
Prior art date
Application number
RU2020119415A
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English (en)
Russian (ru)
Inventor
Режиналь Кристоф Ксавье БРИС
Филипп КЛЕМАН-ЛАКРУА
Стив Ирма Жоэль ДЕ ВОС
Лоран Раймон Морис САНЬЕР
Original Assignee
Галапагос Нв
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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 Галапагос Нв filed Critical Галапагос Нв
Publication of RU2020119415A publication Critical patent/RU2020119415A/ru

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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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/4375Heterocyclic 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2063Proteins, e.g. gelatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P43/00Drugs 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)
RU2020119415A 2017-11-15 2018-11-15 Соединения и их фармацевтические композиции для применения при лечении фиброзных заболеваний RU2020119415A (ru)

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
RU2020119415A true RU2020119415A (ru) 2021-12-16

Family

ID=64746511

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2020119415A RU2020119415A (ru) 2017-11-15 2018-11-15 Соединения и их фармацевтические композиции для применения при лечении фиброзных заболеваний

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=)

Families Citing this family (9)

* 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
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
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

Family Cites Families (7)

* 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
EP2935262B1 (en) 2012-12-20 2017-03-15 Galapagos NV Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
SI2970255T1 (sl) 2013-03-14 2017-12-29 Galapagos Nv Spojine in farmacevtski sestavki le-teh za zdravljenje vnetnih motenj
TWI742541B (zh) * 2013-03-15 2021-10-11 英商邊緣生物科技有限公司 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物
GB201411241D0 (en) * 2014-06-25 2014-08-06 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
GB201506894D0 (en) * 2015-04-23 2015-06-10 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
GB201603745D0 (en) 2016-03-04 2016-04-20 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Also Published As

Publication number Publication date
IL274578A (en) 2020-06-30
US20230241068A1 (en) 2023-08-03
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
CN111343986A (zh) 2020-06-26
KR20200088844A (ko) 2020-07-23

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