EA201791002A1 - Новые соединения, модулирующие fxr (nr1h4) - Google Patents

Новые соединения, модулирующие fxr (nr1h4)

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Publication number
EA201791002A1
EA201791002A1 EA201791002A EA201791002A EA201791002A1 EA 201791002 A1 EA201791002 A1 EA 201791002A1 EA 201791002 A EA201791002 A EA 201791002A EA 201791002 A EA201791002 A EA 201791002A EA 201791002 A1 EA201791002 A1 EA 201791002A1
Authority
EA
Eurasian Patent Office
Prior art keywords
nr1h4
compounds
new connections
modulating fxr
frx
Prior art date
Application number
EA201791002A
Other languages
English (en)
Other versions
EA033642B1 (ru
Inventor
Олаф Кинцель
Клаус Кремозер
Питер А. Бломгрен
Кевин С. Карри
Джеффри И. Кропф
Аарон Шмитт
Уильям Дж. Уоткинс
Цзяньцзюнь Сюй
Кристиан Геге
Original Assignee
Джилид Сайэнс, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Джилид Сайэнс, Инк. filed Critical Джилид Сайэнс, Инк.
Publication of EA201791002A1 publication Critical patent/EA201791002A1/ru
Publication of EA033642B1 publication Critical patent/EA033642B1/ru

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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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
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    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • 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
    • C07D471/08—Bridged systems

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  • Gastroenterology & Hepatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (1)которые связываются с рецептором NR1H4 (FRX) и действуют в качестве агонистов FRX. Изобретение дополнительно относится к применению соединений для получения лекарственного средства для лечения заболеваний и/или состояний за счет связывания указанного ядерного рецептора указанными соединениями, а также к способу синтеза указанных соединений.
EA201791002A 2014-12-17 2015-12-14 Соединения, модулирующие fxr (nr1h4) EA033642B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14004260.7A EP3034499A1 (en) 2014-12-17 2014-12-17 Novel FXR (NR1H4) modulating compounds
PCT/EP2015/002512 WO2016096116A1 (en) 2014-12-17 2015-12-14 Novel fxr (nr1h4) modulating compounds

Publications (2)

Publication Number Publication Date
EA201791002A1 true EA201791002A1 (ru) 2018-06-29
EA033642B1 EA033642B1 (ru) 2019-11-12

Family

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EA201791002A EA033642B1 (ru) 2014-12-17 2015-12-14 Соединения, модулирующие fxr (nr1h4)

Country Status (23)

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US (1) US9938278B2 (ru)
EP (2) EP3034499A1 (ru)
JP (2) JP6452821B2 (ru)
KR (1) KR101955840B1 (ru)
CN (1) CN107108595B (ru)
AR (1) AR103064A1 (ru)
AU (1) AU2015365945B2 (ru)
BR (1) BR102015031497A2 (ru)
CA (1) CA2971241C (ru)
EA (1) EA033642B1 (ru)
ES (1) ES2719902T3 (ru)
HK (1) HK1245786B (ru)
IL (1) IL252496A0 (ru)
MX (1) MX2017007522A (ru)
NZ (1) NZ732210A (ru)
PL (1) PL3233831T3 (ru)
PT (1) PT3233831T (ru)
SG (1) SG11201704539TA (ru)
SI (1) SI3233831T1 (ru)
TR (1) TR201906401T4 (ru)
TW (1) TWI598345B (ru)
UY (1) UY36452A (ru)
WO (1) WO2016096116A1 (ru)

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