IL269065B - Paranoid x receptor agonists and uses thereof - Google Patents

Paranoid x receptor agonists and uses thereof

Info

Publication number
IL269065B
IL269065B IL269065A IL26906519A IL269065B IL 269065 B IL269065 B IL 269065B IL 269065 A IL269065 A IL 269065A IL 26906519 A IL26906519 A IL 26906519A IL 269065 B IL269065 B IL 269065B
Authority
IL
Israel
Prior art keywords
cyclohexyl
substituted
unsubstituted
methyl
carbamoyl
Prior art date
Application number
IL269065A
Other languages
English (en)
Hebrew (he)
Other versions
IL269065A (en
Original Assignee
Metacrine Inc
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.)
Filing date
Publication date
Application filed by Metacrine Inc filed Critical Metacrine Inc
Publication of IL269065A publication Critical patent/IL269065A/en
Publication of IL269065B publication Critical patent/IL269065B/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
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    • A61K31/425—Thiazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • 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
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4545—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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    • 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
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    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
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    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/28—Radicals substituted by nitrogen atoms
    • 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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
    • C07D413/02—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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
IL269065A 2017-03-15 2018-03-14 Paranoid x receptor agonists and uses thereof IL269065B (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201762471517P 2017-03-15 2017-03-15
US201762471525P 2017-03-15 2017-03-15
US201762471511P 2017-03-15 2017-03-15
US201762563488P 2017-09-26 2017-09-26
US201762563502P 2017-09-26 2017-09-26
PCT/US2018/022513 WO2018170182A1 (en) 2017-03-15 2018-03-14 Farnesoid x receptor agonists and uses thereof

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IL269065A IL269065A (en) 2019-11-28
IL269065B true IL269065B (en) 2022-09-01

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JP (1) JP7258763B2 (enExample)
KR (1) KR102588982B1 (enExample)
CN (1) CN110637015B (enExample)
AU (1) AU2018236275B2 (enExample)
BR (1) BR112019019154A2 (enExample)
CA (1) CA3056019A1 (enExample)
DK (1) DK3609888T3 (enExample)
ES (1) ES3049520T3 (enExample)
FI (1) FI3609888T3 (enExample)
HR (1) HRP20251322T1 (enExample)
IL (1) IL269065B (enExample)
LT (1) LT3609888T (enExample)
MX (1) MX2019010907A (enExample)
PH (1) PH12019502058A1 (enExample)
PL (1) PL3609888T3 (enExample)
PT (1) PT3609888T (enExample)
RS (1) RS67372B1 (enExample)
SG (1) SG11201908330PA (enExample)
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Families Citing this family (26)

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Publication number Priority date Publication date Assignee Title
US10377717B2 (en) 2015-09-16 2019-08-13 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
CA2998493A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
US10626081B2 (en) 2015-09-16 2020-04-21 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
PT3609888T (pt) 2017-03-15 2025-10-23 Lilly Co Eli Agonistas do recetor farnesoide x e suas utilizações
EP3596053B1 (en) 2017-03-15 2023-08-16 Organovo, Inc. Farnesoid x receptor agonists and uses thereof
SG11202003830SA (en) 2017-11-01 2020-05-28 Bristol Myers Squibb Co Alkene spirocyclic compounds as farnesoid x receptor modulators
ES2944601T3 (es) 2017-11-01 2023-06-22 Bristol Myers Squibb Co Compuestos multicíclicos como moduladores del receptor farnesoide X
JP2022500391A (ja) * 2018-09-18 2022-01-04 メタクリン，インク． ファルネソイドｘ受容体アゴニストおよびその使用
CN113056270A (zh) * 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂的结晶形式
WO2020061116A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP4596543A3 (en) * 2018-09-18 2025-10-15 Organovo, Inc. Farnesoid x receptor agonists and uses thereof
CN113056265A (zh) * 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途
EP3870162A4 (en) * 2018-10-24 2022-08-24 Metacrine, Inc. SSAO INHIBITORS AND USES THEREOF
EA202192275A1 (ru) * 2019-02-15 2021-11-03 Бристол-Маерс Сквибб Компани Замещенные амидные соединения, полезные в качестве модуляторов фарнезоидного x-рецептора
US12227496B2 (en) 2019-02-15 2025-02-18 Bristol-Myers Squibb Company Substituted bicyclic compounds as farnesoid X receptor modulators
MX2021009564A (es) * 2019-02-15 2021-09-08 Bristol Myers Squibb Co Compuestos de amida sustituida utiles como moduladores del receptor de farnesoide x.
MX2021009570A (es) * 2019-02-15 2021-09-08 Bristol Myers Squibb Co Compuestos biciclicos sustituidos como moduladores del receptor de farnesoide x.
AR118050A1 (es) * 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
US20220241376A1 (en) 2019-07-18 2022-08-04 Enyo Pharma Method for decreasing adverse-effects of interferon
CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
WO2021188695A1 (en) * 2020-03-18 2021-09-23 Metacrine, Inc. Formulations of a farnesoid x receptor agonist
CN115666521A (zh) * 2020-03-18 2023-01-31 梅塔科林公司 法尼醇x受体激动剂的结晶形式
AU2021240001A1 (en) * 2020-03-18 2022-10-13 Eli Lilly And Company Farnesoid X receptor agonists for the treatment of disease
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
CN118178662A (zh) * 2022-12-14 2024-06-14 深圳奥萨制药有限公司 含有法尼醇x受体激动剂的药物组合物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015138969A1 (en) * 2014-03-13 2015-09-17 Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
WO2016149111A1 (en) * 2015-03-13 2016-09-22 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid x receptor agonists to activate intestinal receptors

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1356977A (zh) 1999-05-17 2002-07-03 诺沃挪第克公司 胰高血糖素拮抗剂/反向激动剂
WO2000071518A2 (en) 1999-05-25 2000-11-30 Sepracor, Inc. Heterocyclic analgesic compounds and their use
US6511980B2 (en) 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
WO2001092226A1 (en) 2000-05-25 2001-12-06 Sepracor, Inc. Heterocyclic analgesic compounds and method of use thereof
HUP0303360A2 (hu) 2000-09-25 2004-01-28 Actelion Pharmaceuticals Ltd. Maláriaellenes hatású szubsztituált amino-aza-cikloalkánok és ezeket tartalmazó gyógyszerkészítmények
FR2815032B1 (fr) 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
FR2825706B1 (fr) 2001-06-06 2003-12-12 Pf Medicament Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase
FR2839974B1 (fr) 2002-05-24 2004-07-16 Pf Medicament Derives de phenyl-furane ou de phenyl-thiophene,leur preparation et leur application a titre de medicament
WO2004009549A2 (en) 2002-07-18 2004-01-29 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
MXPA05003054A (es) 2002-09-20 2005-05-27 Pfizer Prod Inc Ligandos de amida y sulfonamida para el receptor de estrogenos.
WO2004046162A2 (en) * 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
US20050143449A1 (en) * 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
US7647217B2 (en) 2002-11-15 2010-01-12 The Salk Institute For Biological Studies Structure of the farnesoid X receptor ligand binding domain and methods of use therefor
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7759348B2 (en) 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
AR047557A1 (es) 2003-07-30 2006-01-25 Xenon Pharmaceuticals Inc Compuestos derivados de piridazina y su uso como agentes terapeuticos
WO2005058822A1 (en) 2003-12-17 2005-06-30 Actelion Pharmaceuticals Ltd Substituted amino-cycloalkanes
US20050239751A1 (en) 2004-03-26 2005-10-27 Rigel Pharmaceuticals, Inc. Heterocyclic anti-viral compounds comprising metabolizable moieties and their uses
US20050272784A1 (en) 2004-05-07 2005-12-08 Xiaobing Li Inhibitors of bacterial Type III protein secretion systems
JP2006199656A (ja) 2005-01-24 2006-08-03 Kowa Co アミド基を有する環状アミン化合物
MY144229A (en) 2006-01-26 2011-08-15 Xenon Pharmaceuticals Inc Pyridazine derivatives and their use as therapeutic agents
CA2644369A1 (en) 2006-03-28 2007-10-04 Novartis Ag Amide derivatives and their application for the treatment of g protein related diseases
US20080081824A1 (en) 2006-09-29 2008-04-03 Bristol-Myers Squibb Company Substituted piperidines as modulators of chemokine receptor activity
WO2008065500A2 (en) 2006-11-30 2008-06-05 Pfizer Products Inc. Heteroaryl amides as type i glycine transport inhibitors
CN103483251A (zh) 2007-12-19 2014-01-01 贝林格尔.英格海姆国际有限公司 病毒聚合酶抑制剂
WO2010001869A1 (ja) 2008-06-30 2010-01-07 武田薬品工業株式会社 ４置換ベンゼン化合物およびその用途
JP2010077109A (ja) 2008-08-28 2010-04-08 Takeda Chem Ind Ltd 複素環化合物およびその用途
CN102471339A (zh) 2009-07-15 2012-05-23 雅培制药有限公司 激酶的吡咯并吡啶抑制剂
US20120115869A1 (en) 2009-07-15 2012-05-10 Merck Serono S.A. Tetrazole derivatives
FR2963005B1 (fr) 2010-07-23 2012-08-17 Sanofi Aventis Derives d'oxadiazoles et de pyridazines, leur preparation et leur application en therapeutique
HUE032948T2 (en) 2011-03-23 2017-11-28 Trevena Inc Opioid receptor ligands and methods of using and making same
KR20140038467A (ko) 2011-07-13 2014-03-28 엠. 테크닉 가부시키가이샤 결정자 지름이 제어된 미립자의 제조 방법
RU2543485C2 (ru) 2013-02-26 2015-03-10 Андрей Александрович Иващенко Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения
GB201316824D0 (en) 2013-09-23 2013-11-06 R & D Vernalis Ltd New Chemical Entities
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
US20150258052A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Methods of using fexaramine and agents that increase sympathetic nervous system activity to promote browning of white adipose tissue
WO2016116054A1 (en) 2015-01-22 2016-07-28 Xiamen University Modulators of farnesoid x receptor and methods for the use thereof
WO2017018751A1 (ko) 2015-07-24 2017-02-02 동국대학교 산학협력단 Blt 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 염증성 질환 예방 또는 치료용 조성물
CA2998493A1 (en) * 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2017049176A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
US10626081B2 (en) * 2015-09-16 2020-04-21 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
US10377717B2 (en) * 2015-09-16 2019-08-13 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
KR102316645B1 (ko) 2016-03-31 2021-10-25 가부시키가이샤 아데카 감광성 조성물 및 신규 화합물
DE102016210851A1 (de) 2016-06-17 2017-12-21 Hamilton Bonaduz Ag Fluidversorgungsschnittstelle mit Sicherheitsventil für eine Zellkulturanlage, Verwendung einer solchen Fluidversorgungsschnittstelle zur Bewirtschaftung von Zellkulturbehältern und Zellkultur-Bewirtschaftungsanlage
PT3609888T (pt) 2017-03-15 2025-10-23 Lilly Co Eli Agonistas do recetor farnesoide x e suas utilizações
US20200131132A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
US20200131142A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018170173A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP3596053B1 (en) 2017-03-15 2023-08-16 Organovo, Inc. Farnesoid x receptor agonists and uses thereof
WO2020060007A1 (ko) 2018-09-17 2020-03-26 엘지전자 주식회사 5g 이동통신에서 pdu 세션을 핸들링하는 방법 및 무선 기기
EA202190661A1 (ru) 2018-09-18 2021-08-13 Метакрайн, Инк. Агонисты фарнезоидного х-рецептора для лечения заболевания
WO2020061116A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
JP2022500391A (ja) 2018-09-18 2022-01-04 メタクリン，インク． ファルネソイドｘ受容体アゴニストおよびその使用
WO2020061118A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP4596543A3 (en) 2018-09-18 2025-10-15 Organovo, Inc. Farnesoid x receptor agonists and uses thereof
CN113056265A (zh) 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015138969A1 (en) * 2014-03-13 2015-09-17 Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
WO2016149111A1 (en) * 2015-03-13 2016-09-22 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid x receptor agonists to activate intestinal receptors

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