CA2977539A1 - Sterol regulatory element-binding proteins (srebps) inhibitors - Google Patents

Sterol regulatory element-binding proteins (srebps) inhibitors Download PDF

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Publication number
CA2977539A1
CA2977539A1 CA2977539A CA2977539A CA2977539A1 CA 2977539 A1 CA2977539 A1 CA 2977539A1 CA 2977539 A CA2977539 A CA 2977539A CA 2977539 A CA2977539 A CA 2977539A CA 2977539 A1 CA2977539 A1 CA 2977539A1
Authority
CA
Canada
Prior art keywords
thiophen
piperidin
tert
methanone
butylpyridin
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.)
Abandoned
Application number
CA2977539A
Other languages
English (en)
French (fr)
Inventor
Brahmam PUJALA
Ramniwas JANGIR
Rambabu GUGULOTH
Bharat Uttam SHINDE
Roopa Rai
Son Minh Pham
Sebastian Bernales
Jeffrey Lindquist
Mausumee Guha
Satyanarayana KALLEM
Bhawana BHATT
Vikas Ramdas BHAGWAT
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.)
Medivation Technologies LLC
Original Assignee
Medivation Technologies LLC
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 Medivation Technologies LLC filed Critical Medivation Technologies LLC
Publication of CA2977539A1 publication Critical patent/CA2977539A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA2977539A 2015-03-04 2016-03-04 Sterol regulatory element-binding proteins (srebps) inhibitors Abandoned CA2977539A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN615/DEL/2015 2015-03-04
IN615DE2015 2015-03-04
IN640DE2015 2015-03-09
IN640/DEL/2015 2015-03-09
PCT/US2016/020802 WO2016141258A1 (en) 2015-03-04 2016-03-04 Sterol regulatory element-binding proteins (srebps) inhibitors

Publications (1)

Publication Number Publication Date
CA2977539A1 true CA2977539A1 (en) 2016-09-09

Family

ID=55586426

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2977539A Abandoned CA2977539A1 (en) 2015-03-04 2016-03-04 Sterol regulatory element-binding proteins (srebps) inhibitors

Country Status (5)

Country Link
US (1) US10189826B2 (enExample)
EP (1) EP3265457A1 (enExample)
JP (1) JP2018507235A (enExample)
CA (1) CA2977539A1 (enExample)
WO (1) WO2016141258A1 (enExample)

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US10328064B2 (en) 2014-12-23 2019-06-25 Fgh Biotech, Inc. Compositions of fatostatin based heterocyclic compounds and uses thereof
EP3265088A1 (en) 2015-03-04 2018-01-10 Medivation Technologies LLC Srebp blockers for use in treating liver fibrosis, elevated cholesterol and insulin resistance
ES2912921T3 (es) 2016-04-29 2022-05-30 Fgh Biotech Inc Compuestos de pirazol disustituidos para el tratamiento de enfermedades
US11339142B2 (en) 2016-09-07 2022-05-24 Fgh Biotech, Inc. Di-substituted pyrazole compounds for the treatment of diseases
JP2021512160A (ja) 2018-01-29 2021-05-13 カピュラス セラピューティクス リミテッド ライアビリティ カンパニー 6員の中央環を含むsrebp阻害剤
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
WO2020132700A1 (en) 2018-12-21 2020-06-25 Fgh Biotech Inc. Methods of using inhibitors of srebp in combination with niclosamide and analogs thereof
WO2020159889A1 (en) * 2019-01-28 2020-08-06 Capulus Therapeutics, Llc Srebp inhibitors comprising a thiophene central ring
WO2021097123A1 (en) * 2019-11-13 2021-05-20 Capulus Therapeutics, Llc Thiophene compounds with cyclic amides, and uses thereof
KR20220128335A (ko) * 2019-11-13 2022-09-20 카풀루스 테라퓨틱스, 엘엘씨 티오펜 중심 고리를 포함하는 srebp 저해제
WO2021154735A1 (en) * 2020-01-27 2021-08-05 Capulus Therapeutics, Llc Srebp inhibitors comprising a thiophene central ring
EP4185584A1 (en) * 2020-07-24 2023-05-31 Capulus Therapeutics, LLC Srebp inhibitors comprising a thiophene central ring
CN112225728A (zh) * 2020-08-18 2021-01-15 四川农业大学 一种多取代苯甲酰胺化合物及其制备方法和应用
CN117050074B (zh) * 2022-05-05 2025-08-12 中国药科大学 一类吡啶联咪唑并吡啶化合物及其制备方法与用途

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Also Published As

Publication number Publication date
WO2016141258A1 (en) 2016-09-09
JP2018507235A (ja) 2018-03-15
US20180051013A1 (en) 2018-02-22
EP3265457A1 (en) 2018-01-10
US10189826B2 (en) 2019-01-29

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20210907