JP7258763B2 - ファルネソイドｘ受容体アゴニストおよびその使用 - Google Patents

ファルネソイドｘ受容体アゴニストおよびその使用 Download PDF

Info

Publication number
JP7258763B2
JP7258763B2 JP2019547663A JP2019547663A JP7258763B2 JP 7258763 B2 JP7258763 B2 JP 7258763B2 JP 2019547663 A JP2019547663 A JP 2019547663A JP 2019547663 A JP2019547663 A JP 2019547663A JP 7258763 B2 JP7258763 B2 JP 7258763B2
Authority
JP
Japan
Prior art keywords
trans
cyclohexyl
methyl
phenyl
methoxy
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2019547663A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020514334A (ja
JP2020514334A5 (https=
Inventor
ディー． スミス，ニコラス
ピー． ゴベク，スティーブン
ワイ． ナガサワ，ジョニー
エル． ダグラス，カレンサ
ジー． ライ，アンディリー
Original Assignee
メタクリン，インク．
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 メタクリン，インク． filed Critical メタクリン，インク．
Publication of JP2020514334A publication Critical patent/JP2020514334A/ja
Publication of JP2020514334A5 publication Critical patent/JP2020514334A5/ja
Application granted granted Critical
Publication of JP7258763B2 publication Critical patent/JP7258763B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not 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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/444—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
    • 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
    • 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
    • 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
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • 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
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • 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
    • 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
    • C07D401/12—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
    • 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
    • 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
    • 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
    • C07D417/14—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (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)
JP2019547663A 2017-03-15 2018-03-14 ファルネソイドｘ受容体アゴニストおよびその使用 Active JP7258763B2 (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201762471511P 2017-03-15 2017-03-15
US201762471525P 2017-03-15 2017-03-15
US201762471517P 2017-03-15 2017-03-15
US62/471,517 2017-03-15
US62/471,511 2017-03-15
US62/471,525 2017-03-15
US201762563488P 2017-09-26 2017-09-26
US201762563502P 2017-09-26 2017-09-26
US62/563,502 2017-09-26
US62/563,488 2017-09-26
PCT/US2018/022513 WO2018170182A1 (en) 2017-03-15 2018-03-14 Farnesoid x receptor agonists and uses thereof

Publications (3)

Publication Number Publication Date
JP2020514334A JP2020514334A (ja) 2020-05-21
JP2020514334A5 JP2020514334A5 (https=) 2021-04-15
JP7258763B2 true JP7258763B2 (ja) 2023-04-17

Family

ID=63523880

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019547663A Active JP7258763B2 (ja) 2017-03-15 2018-03-14 ファルネソイドｘ受容体アゴニストおよびその使用

Country Status (23)

Country Link
US (2) US11236071B1 (https=)
EP (2) EP3609888B1 (https=)
JP (1) JP7258763B2 (https=)
KR (1) KR102588982B1 (https=)
CN (1) CN110637015B (https=)
AU (1) AU2018236275B2 (https=)
BR (1) BR112019019154A2 (https=)
CA (1) CA3056019A1 (https=)
DK (1) DK3609888T3 (https=)
ES (1) ES3049520T3 (https=)
FI (1) FI3609888T3 (https=)
HR (1) HRP20251322T1 (https=)
IL (1) IL269065B (https=)
LT (1) LT3609888T (https=)
MX (1) MX2019010907A (https=)
PH (1) PH12019502058A1 (https=)
PL (1) PL3609888T3 (https=)
PT (1) PT3609888T (https=)
RS (1) RS67372B1 (https=)
SG (1) SG11201908330PA (https=)
SI (1) SI3609888T1 (https=)
SM (1) SMT202600045T1 (https=)
WO (1) WO2018170182A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022500392A (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

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017049177A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
US10703712B2 (en) 2015-09-16 2020-07-07 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
CA3055990A1 (en) * 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
JP7258763B2 (ja) 2017-03-15 2023-04-17 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
CN111278817B (zh) 2017-11-01 2023-05-16 百时美施贵宝公司 作为法尼醇x受体调节剂的多环化合物
AU2018360575A1 (en) 2017-11-01 2020-06-18 Bristol-Myers Squibb Company Alkene spirocyclic compounds as farnesoid X receptor modulators
EP3852749A4 (en) * 2018-09-18 2022-08-24 Metacrine, Inc. CRYSTALLINE FORMS OF A FARNESOID X RECEPTOR AGONIST
WO2020061116A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN113056264A (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
JP2022500393A (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
AU2019365213A1 (en) * 2018-10-24 2021-06-03 Metacrine, Inc. SSAO inhibitors and uses thereof
CN113727973B (zh) 2019-02-15 2025-08-29 百时美施贵宝公司 可用作类法尼醇x受体调节剂的取代酰胺化合物
JP7465883B2 (ja) * 2019-02-15 2024-04-11 ブリストル－マイヤーズ スクイブ カンパニー ファルネソイドｘ受容体モジュレータとしての置換二環式化合物
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
AU2020221371A1 (en) 2019-02-15 2021-10-07 Bristol-Myers Squibb Company Substituted amide compounds useful as farnesoid x receptor modulators
CA3129533A1 (en) * 2019-02-15 2020-08-20 Bristol-Myers Squibb Company Substituted bicyclic compounds as farnesoid x receptor modulators
KR20220035365A (ko) 2019-07-18 2022-03-22 엔요 파마 인터페론의 부작용을 감소시키는 방법
IL293892A (en) 2020-01-15 2022-08-01 Inserm Institut National De La Sant? Et De La Rech M?Dicale 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
CN120732855A (zh) * 2020-03-18 2025-10-03 伊莱利利公司 用于治疗疾病的法尼醇x受体激动剂
KR20220155356A (ko) * 2020-03-18 2022-11-22 메타크린, 인크. 파르네소이드 x 수용체 효능제의 결정형
JP2024502673A (ja) 2021-01-14 2024-01-22 ウエヌイグレックオ・ファーマ Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果
JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強
CN118178662B (zh) * 2022-12-14 2026-03-20 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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004046162A2 (en) 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
WO2004045511A2 (en) 2002-11-15 2004-06-03 The Salk Institute For Biological Studies Non-steroidal farnesoid x receptor modulators
WO2015138969A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
WO2018170166A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
JP6905530B2 (ja) 2015-09-16 2021-07-21 メタクリン，インク． ファルネソイドｘ受容体アゴニストとその使用

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000069810A1 (en) 1999-05-17 2000-11-23 Novo Nordisk A/S Glucagon antagonists/inverse agonists
JP2003500392A (ja) 1999-05-25 2003-01-07 セプラコール， インク． 複素環式鎮痛性化合物およびその使用方法
US6645980B1 (en) 2000-05-25 2003-11-11 Sepracor Inc. Heterocyclic analgesic compounds and methods of use thereof
US6511980B2 (en) 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
IL154363A0 (en) 2000-09-25 2003-09-17 Actelion Pharmaceuticals Ltd Substituted amino-aza-cycloalkanes useful against malaria
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
AU2003249983A1 (en) 2002-07-18 2004-02-09 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
BR0314126A (pt) 2002-09-20 2005-06-28 Pfizer Prod Inc Ligandos de amida acìclica e sulfonamida para o receptor de estrogênio
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
US7759348B2 (en) 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
EP1648874B1 (en) 2003-07-30 2011-10-05 Xenon Pharmaceuticals Inc. Piperazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
WO2005058822A1 (en) 2003-12-17 2005-06-30 Actelion Pharmaceuticals Ltd Substituted amino-cycloalkanes
WO2005097760A1 (en) 2004-03-26 2005-10-20 Rigel Pharmaceuticals, Inc. Heterocyclic anti-viral compounds comprising metabolizable moieties and their uses
WO2005113522A1 (en) 2004-05-07 2005-12-01 Janssen Pharmaceutica, N.V. Azole carboxamide 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
EP2001851A2 (en) 2006-03-28 2008-12-17 Novartis AG Amide derivatives and their application for the treament 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
EP2234977A4 (en) 2007-12-19 2011-04-13 Boehringer Ingelheim Int VIRAL POLYMERASE INHIBITORS
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
CA2767089A1 (en) 2009-07-15 2011-01-20 Abbott Laboratories Pyrrolopyridine inhibitors of kinases
EP2454243A2 (en) 2009-07-15 2012-05-23 Merck Serono SA 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
ME02754B (me) 2011-03-23 2018-01-20 Trevena Inc Ligandi opioidnih receptora i postupci njihove upotrebe i pripreme
EP2732871A4 (en) 2011-07-13 2015-03-04 M Tech Co Ltd PROCESS FOR PRODUCING MICROPARTICLES WITH CONTROLLED CRYSTALLITE DIAMETER
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
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
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
US20180116993A1 (en) 2015-01-22 2018-05-03 Xiamen University Modulators of farnesoid x receptor and methods for the use thereof
AU2016233579A1 (en) * 2015-03-13 2017-10-12 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid X receptor agonists to activate intestinal receptors
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
EP3350164A4 (en) 2015-09-16 2019-03-27 Metacrine, Inc. FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF
WO2017049177A1 (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
WO2017170182A1 (ja) 2016-03-31 2017-10-05 株式会社Adeka 感光性組成物及び新規化合物
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
US20200131129A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
JP7258763B2 (ja) 2017-03-15 2023-04-17 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
WO2018170167A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018170165A1 (en) 2017-03-15 2018-09-20 Metacrine, 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
JP2022500393A (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
WO2020061116A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EA202190661A1 (ru) 2018-09-18 2021-08-13 Метакрайн, Инк. Агонисты фарнезоидного х-рецептора для лечения заболевания
WO2020061118A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN113056264A (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
AU2019344903B2 (en) 2018-09-18 2025-02-27 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004046162A2 (en) 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
WO2004045511A2 (en) 2002-11-15 2004-06-03 The Salk Institute For Biological Studies Non-steroidal farnesoid x receptor modulators
WO2015138969A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
JP6905530B2 (ja) 2015-09-16 2021-07-21 メタクリン，インク． ファルネソイドｘ受容体アゴニストとその使用
WO2018170166A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022500392A (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

Also Published As

Publication number Publication date
US20220089575A1 (en) 2022-03-24
CA3056019A1 (en) 2018-09-20
CN110637015A (zh) 2019-12-31
BR112019019154A2 (pt) 2020-04-14
AU2018236275B2 (en) 2022-05-12
LT3609888T (lt) 2025-11-10
RS67372B1 (sr) 2025-11-28
MX2019010907A (es) 2019-11-07
CN110637015B (zh) 2024-04-02
AU2018236275A1 (en) 2019-09-26
SI3609888T1 (sl) 2025-11-28
SG11201908330PA (en) 2019-10-30
HRP20251322T1 (hr) 2025-12-05
IL269065A (en) 2019-11-28
KR102588982B1 (ko) 2023-10-12
SMT202600045T1 (it) 2026-03-09
FI3609888T3 (fi) 2025-10-15
DK3609888T3 (da) 2025-10-06
US11236071B1 (en) 2022-02-01
ES3049520T3 (en) 2025-12-17
WO2018170182A1 (en) 2018-09-20
JP2020514334A (ja) 2020-05-21
EP4596041A3 (en) 2025-12-10
EP3609888A4 (en) 2020-09-02
EP3609888A1 (en) 2020-02-19
EP3609888B1 (en) 2025-08-27
IL269065B (en) 2022-09-01
PH12019502058A1 (en) 2020-07-06
PL3609888T3 (pl) 2025-12-01
PT3609888T (pt) 2025-10-23
KR20190121399A (ko) 2019-10-25
EP4596041A2 (en) 2025-08-06

Similar Documents

Publication Publication Date Title
JP7258763B2 (ja) ファルネソイドｘ受容体アゴニストおよびその使用
JP7174709B2 (ja) ファルネソイドｘ受容体アゴニストおよびその使用
JP7554739B2 (ja) ファルネソイドｘ受容体アゴニストおよびその使用
WO2018170173A1 (en) Farnesoid x receptor agonists and uses thereof
US20200131142A1 (en) Farnesoid x receptor agonists and uses thereof
JP2022500391A (ja) ファルネソイドｘ受容体アゴニストおよびその使用
JP2018536015A (ja) ファルネソイドｘ受容体アゴニストとその使用
JP2018532772A (ja) ファルネソイドｘ受容体アゴニストおよびそれらの使用
JP2022500393A (ja) ファルネソイドｘ受容体アゴニストおよびその使用
HK40019860B (zh) 法尼醇x受体激动剂及其用途
EA040704B1 (ru) Агонисты фарнезоидного x-рецептора и их применение
HK40019860A (en) Farnesoid x receptor agonists and uses thereof
HK40048018A (en) Farnesoid x receptor agonists and uses thereof
HK40048018B (en) Farnesoid x receptor agonists and uses thereof
HK40019851B (zh) 法尼醇x受体激动剂及其用途
HK40019851A (en) Farnesoid x receptor agonists and uses thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20191217

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210304

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210305

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220113

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220207

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220506

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220627

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220921

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221215

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20230313

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230405

R150 Certificate of patent or registration of utility model

Ref document number: 7258763

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: R3D02