AU2013286894B2 - Heterocyclic modulators of lipid synthesis - Google Patents

Heterocyclic modulators of lipid synthesis Download PDF

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Publication number
AU2013286894B2
AU2013286894B2 AU2013286894A AU2013286894A AU2013286894B2 AU 2013286894 B2 AU2013286894 B2 AU 2013286894B2 AU 2013286894 A AU2013286894 A AU 2013286894A AU 2013286894 A AU2013286894 A AU 2013286894A AU 2013286894 B2 AU2013286894 B2 AU 2013286894B2
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alkyl
compound
halogen
cycloalkyl
mmol
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AU2013286894A1 (en
Inventor
Haiying CAI
Marc EVANCHIK
Lily W. HU
Russell Johnson
Robert S. Mcdowell
Johan D. Oslob
Allan Wagman
Hanbiao Yang
Cristiana A. Zaharia
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Sagimet Biosciences Inc
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Sagimet Biosciences Inc
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Publication of AU2013286894A1 publication Critical patent/AU2013286894A1/en
Priority to AU2017265027A priority Critical patent/AU2017265027A1/en
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    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • 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
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2013286894A 2012-07-03 2013-07-01 Heterocyclic modulators of lipid synthesis Active AU2013286894B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2017265027A AU2017265027A1 (en) 2012-07-03 2017-11-21 Heterocyclic modulators of lipid synthesis

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201261667894P 2012-07-03 2012-07-03
US61/667,894 2012-07-03
US201261698511P 2012-09-07 2012-09-07
US61/698,511 2012-09-07
US201261699819P 2012-09-11 2012-09-11
US61/699,819 2012-09-11
US201361785933P 2013-03-14 2013-03-14
US61/785,933 2013-03-14
PCT/US2013/048950 WO2014008197A1 (en) 2012-07-03 2013-07-01 Heterocyclic modulators of lipid synthesis

Related Child Applications (1)

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AU2017265027A Division AU2017265027A1 (en) 2012-07-03 2017-11-21 Heterocyclic modulators of lipid synthesis

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AU2013286894A1 AU2013286894A1 (en) 2015-01-22
AU2013286894B2 true AU2013286894B2 (en) 2017-12-07

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AU2017265027A Abandoned AU2017265027A1 (en) 2012-07-03 2017-11-21 Heterocyclic modulators of lipid synthesis

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EP (1) EP2870150B1 (enExample)
JP (1) JP6109934B2 (enExample)
KR (1) KR102071095B1 (enExample)
CN (1) CN104507928B (enExample)
AU (2) AU2013286894B2 (enExample)
BR (1) BR112015000106B1 (enExample)
CA (1) CA2877999C (enExample)
ES (1) ES2738823T3 (enExample)
IL (1) IL236407A (enExample)
IN (1) IN2015DN00137A (enExample)
MX (1) MX364815B (enExample)
NZ (2) NZ703162A (enExample)
PL (1) PL2870150T3 (enExample)
SG (1) SG11201500024YA (enExample)
WO (1) WO2014008197A1 (enExample)
ZA (1) ZA201409477B (enExample)

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US9624173B2 (en) * 2011-03-08 2017-04-18 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
TWI522348B (zh) * 2011-03-08 2016-02-21 ３ Ｖ生物科技公司 脂質合成之雜環調節劑
CA2877999C (en) 2012-07-03 2021-02-23 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
EP3083583B1 (en) * 2013-12-20 2020-11-18 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis and combinations thereof
EP3092232B1 (en) 2014-01-07 2022-03-09 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
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JP7668509B2 (ja) * 2016-11-11 2025-04-25 サギメット バイオサイエンシーズ インコーポレイテッド 脂質合成の複素環式モジュレーター
CN107954852A (zh) * 2017-11-30 2018-04-24 贝利化学（张家港）有限公司 2，5-二卤代苯甲酸的制备方法
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US20220400732A1 (en) * 2019-03-21 2022-12-22 Cornell University Anti-fructose therapy for colorectal and small intestine cancers
CN111592495A (zh) * 2020-07-06 2020-08-28 上海启讯医药科技有限公司 一种2-正丁基-4-氯-5甲酰基咪唑的制备方法
CN114988975A (zh) * 2022-06-28 2022-09-02 江苏科技大学 一种基于有机染料催化的β-三氟甲基烯胺化合物的制备方法
CN116482278B (zh) * 2023-05-06 2024-02-09 广州清瑞生物科技有限责任公司 一种用于检测阿昔洛韦的对照品的制备方法
CN119080742A (zh) * 2023-06-05 2024-12-06 甘莱制药有限公司 脂质合成的杂环调节剂的工业化制备
WO2025086054A1 (zh) * 2023-10-23 2025-05-01 歌礼生物科技（杭州）有限公司 一种包含苯甲腈衍生物的药物组合物
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EP3083583B1 (en) * 2013-12-20 2020-11-18 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis and combinations thereof
EP3092232B1 (en) * 2014-01-07 2022-03-09 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
JP6691909B2 (ja) * 2014-08-15 2020-05-13 サギメット バイオサイエンシーズ インコーポレイテッド 薬物耐性癌の治療で用いるための脂肪酸シンターゼ阻害剤
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KR102071095B1 (ko) 2020-01-29
CN104507928A (zh) 2015-04-08
JP2015522036A (ja) 2015-08-03
IN2015DN00137A (enExample) 2015-06-12
MX2015000151A (es) 2015-04-10
US10118913B2 (en) 2018-11-06
AU2013286894A1 (en) 2015-01-22
SG11201500024YA (en) 2015-03-30
US10053450B2 (en) 2018-08-21
EP2870150A1 (en) 2015-05-13
PL2870150T3 (pl) 2019-12-31
ZA201409477B (en) 2021-05-26
BR112015000106A2 (pt) 2017-06-27
ES2738823T3 (es) 2020-01-27
MX364815B (es) 2019-05-08
US20160311803A1 (en) 2016-10-27
KR20150032571A (ko) 2015-03-26
BR112015000106B1 (pt) 2022-02-22
US9428502B2 (en) 2016-08-30
HK1208445A1 (en) 2016-03-04
CA2877999A1 (en) 2014-01-09
IL236407A0 (en) 2015-02-26
JP6109934B2 (ja) 2017-04-05
NZ703162A (en) 2017-05-26
RU2015103345A (ru) 2016-08-20
CN104507928B (zh) 2016-09-28
WO2014008197A1 (en) 2014-01-09
US20150210688A1 (en) 2015-07-30
AU2017265027A1 (en) 2017-12-14
NZ729443A (en) 2017-11-24
EP2870150B1 (en) 2019-06-19
CA2877999C (en) 2021-02-23
US20180222892A1 (en) 2018-08-09
IL236407A (en) 2017-10-31

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