EA201691468A1 - Производные бензимидазола и их фармацевтические композиции для лечения воспалительных заболеваний - Google Patents

Производные бензимидазола и их фармацевтические композиции для лечения воспалительных заболеваний

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Publication number
EA201691468A1
EA201691468A1 EA201691468A EA201691468A EA201691468A1 EA 201691468 A1 EA201691468 A1 EA 201691468A1 EA 201691468 A EA201691468 A EA 201691468A EA 201691468 A EA201691468 A EA 201691468A EA 201691468 A1 EA201691468 A1 EA 201691468A1
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EA
Eurasian Patent Office
Prior art keywords
diseases
inflammatory diseases
benzimidazole
derivatives
treatment
Prior art date
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EA201691468A
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English (en)
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EA029827B1 (ru
Inventor
Кристель Жанн Мари Мене
Оскар Маммолити
Хавьер Блан
Мислав Оршулиц
Майя Рошциц
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Галапагос Нв
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Application filed by Галапагос Нв filed Critical Галапагос Нв
Publication of EA201691468A1 publication Critical patent/EA201691468A1/ru
Publication of EA029827B1 publication Critical patent/EA029827B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06—Antipsoriatics
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    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение раскрывает соединения формулы Iгде Су, R, L, R, R, R, Lи Rтакие, как определено в описании изобретения. Раскрыты новые бензимидазолы формулы I, способные ингибировать JAK, эти соединения могут быть получены в виде фармацевтической композиции, и могут быть использованы для профилактики и лечения различных состояний у млекопитающих, включая человека, включая в качестве неограничивающего примера, аллергические заболевания, воспалительные заболевания, аутоиммунные заболевания, пролиферативные заболевания, отторжение трансплантата, заболевания, связанные с ухудшением обновления хряща, врожденные дефекты развития хряща, и/или заболевания, связанные с гиперсекрецией IL6 или гиперсекрецией интерферонов.
EA201691468A 2014-01-23 2015-01-19 Производные бензимидазола и их фармацевтические композиции для лечения воспалительных заболеваний EA029827B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1401086.2A GB201401086D0 (en) 2014-01-23 2014-01-23 Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
PCT/EP2015/050850 WO2015110378A1 (en) 2014-01-23 2015-01-19 Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Publications (2)

Publication Number Publication Date
EA201691468A1 true EA201691468A1 (ru) 2016-12-30
EA029827B1 EA029827B1 (ru) 2018-05-31

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EA201691468A EA029827B1 (ru) 2014-01-23 2015-01-19 Производные бензимидазола и их фармацевтические композиции для лечения воспалительных заболеваний

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US (3) US9440929B2 (ru)
EP (2) EP3395802A1 (ru)
JP (1) JP6472454B2 (ru)
CN (1) CN106132934B (ru)
AR (1) AR099160A1 (ru)
AU (1) AU2015208269B2 (ru)
BR (1) BR112016016732B1 (ru)
CA (1) CA2941474A1 (ru)
CY (1) CY1120679T1 (ru)
DK (1) DK3097083T3 (ru)
EA (1) EA029827B1 (ru)
ES (1) ES2693019T3 (ru)
GB (1) GB201401086D0 (ru)
HR (1) HRP20181332T1 (ru)
HU (1) HUE039450T2 (ru)
IL (1) IL246823B (ru)
LT (1) LT3097083T (ru)
MX (1) MX370546B (ru)
MY (1) MY180363A (ru)
NZ (1) NZ723313A (ru)
PH (1) PH12016501677B1 (ru)
PL (1) PL3097083T3 (ru)
PT (1) PT3097083T (ru)
SG (1) SG11201606971XA (ru)
SI (1) SI3097083T1 (ru)
TW (1) TWI689496B (ru)
WO (1) WO2015110378A1 (ru)

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Publication number Priority date Publication date Assignee Title
AR105400A1 (es) * 2015-08-04 2017-09-27 Lilly Co Eli Inhibidores de jak1
CA3030697C (en) 2016-07-14 2021-02-23 Eli Lilly And Company Pyrazolylaminobenzimidazole derivatives as jak inhibitors
GB201717260D0 (en) * 2017-10-20 2017-12-06 Galapagos Nv Novel compounds and pharma ceutical compositions thereof for the treatment of inflammatory disorders
CN108355618B (zh) * 2018-02-27 2020-09-08 江南大学 牛来源透明质酸酶亲和介质及其吸附方法
CN108776121B (zh) * 2018-04-08 2021-07-30 广州卡马生物科技有限公司 一种基于荧光猝灭原理对药材中抗氧剂的高通量筛选方法
TWI826525B (zh) * 2018-09-18 2023-12-21 美商拓臻股份有限公司 用於治療特定白血病之化合物
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
GB201904373D0 (en) * 2019-03-29 2019-05-15 Galapagos Nv Novel compounds and pharamaceutical compositions thereof for the treatment of inflammatory disorders
CN114671858B (zh) * 2022-03-07 2023-08-08 华中师范大学 一种苯并咪唑系化合物及其制备方法与应用

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US20070004658A1 (en) 2004-06-21 2007-01-04 Nick Vandeghinste Method and means for treatment of osteoarthritis
WO2009084695A1 (ja) * 2007-12-28 2009-07-09 Carna Biosciences Inc. ２－アミノキナゾリン誘導体
AU2009238590A1 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
KR20130141500A (ko) * 2010-09-29 2013-12-26 크리스탈지노믹스(주) 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물
UY34615A (es) * 2012-02-10 2013-09-30 Galapagos Nv Nuevos compuestos útiles para el tratamiento de enfermedades degenerativas e inflamatorias.

Also Published As

Publication number Publication date
US10179771B2 (en) 2019-01-15
TW201613873A (en) 2016-04-16
DK3097083T3 (en) 2018-10-01
US20190152922A1 (en) 2019-05-23
PL3097083T3 (pl) 2018-11-30
CN106132934A (zh) 2016-11-16
NZ723313A (en) 2019-11-29
TWI689496B (zh) 2020-04-01
IL246823A0 (en) 2016-08-31
SG11201606971XA (en) 2016-10-28
CA2941474A1 (en) 2015-07-30
LT3097083T (lt) 2018-11-26
JP2017503834A (ja) 2017-02-02
MX2016009442A (es) 2016-10-13
PH12016501677A1 (en) 2016-11-07
AU2015208269A1 (en) 2016-09-01
US9440929B2 (en) 2016-09-13
JP6472454B2 (ja) 2019-02-20
CY1120679T1 (el) 2019-12-11
US20170057928A1 (en) 2017-03-02
EA029827B1 (ru) 2018-05-31
HRP20181332T1 (hr) 2018-10-19
CN106132934B (zh) 2019-04-02
US20150203455A1 (en) 2015-07-23
SI3097083T1 (sl) 2018-10-30
EP3097083B1 (en) 2018-08-08
PH12016501677B1 (en) 2016-11-07
PT3097083T (pt) 2018-10-26
ES2693019T3 (es) 2018-12-07
GB201401086D0 (en) 2014-03-12
EP3097083A1 (en) 2016-11-30
WO2015110378A1 (en) 2015-07-30
MY180363A (en) 2020-11-28
AU2015208269B2 (en) 2018-08-30
HUE039450T2 (hu) 2018-12-28
BR112016016732A8 (pt) 2020-06-16
BR112016016732B1 (pt) 2023-04-18
MX370546B (es) 2019-12-17
IL246823B (en) 2020-02-27
AR099160A1 (es) 2016-07-06
EP3395802A1 (en) 2018-10-31

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