CA3112411A1 - Farnesoid x receptor agonists and uses thereof - Google Patents

Farnesoid x receptor agonists and uses thereof Download PDF

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Publication number
CA3112411A1
CA3112411A1 CA3112411A CA3112411A CA3112411A1 CA 3112411 A1 CA3112411 A1 CA 3112411A1 CA 3112411 A CA3112411 A CA 3112411A CA 3112411 A CA3112411 A CA 3112411A CA 3112411 A1 CA3112411 A1 CA 3112411A1
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CA
Canada
Prior art keywords
c4alkyl
compound
solvate
pharmaceutically acceptable
acceptable salt
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.)
Pending
Application number
CA3112411A
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English (en)
French (fr)
Inventor
Nicholas D. Smith
Steven P. Govek
Karensa L. Douglas
Andiliy G. Lai
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organovo Inc
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 CA3112411A1 publication Critical patent/CA3112411A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • 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
    • C07D401/14—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/14—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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Virology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Biotechnology (AREA)
CA3112411A 2018-09-18 2019-09-17 Farnesoid x receptor agonists and uses thereof Pending CA3112411A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862733004P 2018-09-18 2018-09-18
US201862733006P 2018-09-18 2018-09-18
US62/733,006 2018-09-18
US62/733,004 2018-09-18
US201962881560P 2019-08-01 2019-08-01
US62/881,560 2019-08-01
PCT/US2019/051603 WO2020061113A1 (en) 2018-09-18 2019-09-17 Farnesoid x receptor agonists and uses thereof

Publications (1)

Publication Number Publication Date
CA3112411A1 true CA3112411A1 (en) 2020-03-26

Family

ID=69887982

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3112411A Pending CA3112411A1 (en) 2018-09-18 2019-09-17 Farnesoid x receptor agonists and uses thereof

Country Status (27)

Country Link
US (4) US11084817B2 (https=)
EP (2) EP4596543A3 (https=)
JP (1) JP7554739B2 (https=)
KR (2) KR102810978B1 (https=)
CN (1) CN113056271B (https=)
AU (2) AU2019344903B2 (https=)
BR (1) BR112021004919A2 (https=)
CA (1) CA3112411A1 (https=)
CL (1) CL2021000632A1 (https=)
DK (1) DK3852748T3 (https=)
ES (1) ES3051007T3 (https=)
FI (1) FI3852748T3 (https=)
HR (1) HRP20251321T1 (https=)
IL (1) IL281475B2 (https=)
LT (1) LT3852748T (https=)
MA (1) MA53665B1 (https=)
MD (1) MD3852748T2 (https=)
MX (1) MX2021003110A (https=)
PH (1) PH12021550605A1 (https=)
PL (1) PL3852748T3 (https=)
PT (1) PT3852748T (https=)
RS (1) RS67371B1 (https=)
SG (1) SG11202102651SA (https=)
SI (1) SI3852748T1 (https=)
SM (1) SMT202600076T1 (https=)
TW (1) TWI833805B (https=)
WO (1) WO2020061113A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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AU2019344903B2 (en) 2018-09-18 2025-02-27 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof
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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
WO2021188695A1 (en) 2020-03-18 2021-09-23 Metacrine, Inc. Formulations of a farnesoid x receptor agonist
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
CN116554121A (zh) * 2023-05-05 2023-08-08 济南悟通生物科技有限公司 一种2-异丁基噻唑的合成方法

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KR20220155356A (ko) 2020-03-18 2022-11-22 메타크린, 인크. 파르네소이드 x 수용체 효능제의 결정형

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HRP20251321T1 (hr) 2025-12-05
US20200102308A1 (en) 2020-04-02
AU2019344903B2 (en) 2025-02-27
SI3852748T1 (sl) 2025-11-28
MD3852748T2 (ro) 2026-01-31
PT3852748T (pt) 2025-10-24
KR102810978B1 (ko) 2025-05-23
BR112021004919A2 (pt) 2021-06-01
CL2021000632A1 (es) 2021-07-23
IL281475A (en) 2021-04-29
US20230382913A1 (en) 2023-11-30
EP3852748B1 (en) 2025-09-03
US11773094B2 (en) 2023-10-03
DK3852748T3 (da) 2025-10-06
MA53665A (fr) 2021-07-28
JP2022500392A (ja) 2022-01-04
CN113056271B (zh) 2024-10-29
EP4596543A2 (en) 2025-08-06
SG11202102651SA (en) 2021-04-29
KR20250073553A (ko) 2025-05-27
PL3852748T3 (pl) 2025-12-01
IL281475B1 (en) 2024-12-01
AU2019344903A1 (en) 2021-05-13
MX2021003110A (es) 2021-05-13
EP3852748A4 (en) 2022-05-18
TW202024052A (zh) 2020-07-01
LT3852748T (lt) 2025-11-25
US11084817B2 (en) 2021-08-10
MA53665B1 (fr) 2025-09-30
KR20210076910A (ko) 2021-06-24
FI3852748T3 (fi) 2025-10-22
SMT202600076T1 (it) 2026-03-09
EP3852748A1 (en) 2021-07-28
PH12021550605A1 (en) 2021-10-04
EP4596543A3 (en) 2025-10-15
CN113056271A (zh) 2021-06-29
IL281475B2 (en) 2025-04-01
US20210395253A1 (en) 2021-12-23
TWI833805B (zh) 2024-03-01
US20250289821A1 (en) 2025-09-18
JP7554739B2 (ja) 2024-09-20
RS67371B1 (sr) 2025-11-28
AU2025203804A1 (en) 2025-06-12
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