CN104507928B - 脂质合成的杂环调节剂 - Google Patents

脂质合成的杂环调节剂 Download PDF

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CN104507928B
CN104507928B CN201380035602.4A CN201380035602A CN104507928B CN 104507928 B CN104507928 B CN 104507928B CN 201380035602 A CN201380035602 A CN 201380035602A CN 104507928 B CN104507928 B CN 104507928B
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compound
compound according
halogen
cycloalkyl
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CN104507928A (zh
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J·D·奥斯洛布
R·S·麦克道尔
R·约翰逊
H·杨
M·伊万奇克
C·A·扎哈里亚
H·蔡
L·W·胡
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Ganglai Pharmaceutical Co ltd
Sagimit Biosciences
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3V Biosciences Inc
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    • 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
    • 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
    • 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
    • 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
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (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)
CN201380035602.4A 2012-07-03 2013-07-01 脂质合成的杂环调节剂 Active CN104507928B (zh)

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

Publications (2)

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CN104507928A CN104507928A (zh) 2015-04-08
CN104507928B true CN104507928B (zh) 2016-09-28

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US (3) US9428502B2 (enExample)
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) NZ729443A (enExample)
PL (1) PL2870150T3 (enExample)
SG (1) SG11201500024YA (enExample)
WO (1) WO2014008197A1 (enExample)
ZA (1) ZA201409477B (enExample)

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CA2934251C (en) * 2013-12-20 2024-01-02 3-V Biosciences, Inc. A combination of heterocyclic modulators of lipid synthesis and chemotherapeutic drugs in treatment of cancer
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RS60981B1 (sr) 2015-12-18 2020-11-30 Janssen Pharmaceutica Nv Radiooznačeni mglur2/3 pet ligandi
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KR102644934B1 (ko) * 2016-11-11 2024-03-08 새지메트 바이오사이언시스, 인코포레이티드 지질 합성의 헤테로사이클릭 조절인자
US20220340556A1 (en) * 2016-11-11 2022-10-27 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis
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
US12398155B2 (en) 2018-12-26 2025-08-26 Janssen Pharmaceutica Nv Thienopyridinone compounds
US12628858B2 (en) * 2019-03-21 2026-05-19 Cornell University 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
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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KR102071095B1 (ko) * 2012-07-03 2020-01-29 3-브이 바이오사이언시스, 인코포레이티드 지질 합성의 헤테로사이클릭 조절인자
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JP6522007B2 (ja) * 2014-01-07 2019-05-29 3−ブイ・バイオサイエンシーズ・インコーポレイテッド3−V Biosciences,Inc. 癌及びウイルス感染症に対する使用のための脂質合成の複素環式モジュレータ
ES2833454T3 (es) * 2014-08-15 2021-06-15 Sagimet Biosciences Inc Inhibidor de la ácido graso sintasa para su uso en el tratamiento de un cáncer farmacorresistente
JP6758314B2 (ja) * 2015-03-19 2020-09-23 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調節因子

Patent Citations (4)

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WO2008059214A1 (en) * 2006-11-13 2008-05-22 Astrazeneca Ab Bisamlde derivatives and use thereof as fatty acid synthase inhibitors
WO2008075077A1 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Piperidine derivatives for the treatment of obesity
US20090105305A1 (en) * 2006-12-21 2009-04-23 Astrazeneca Ab Therapeutic Agents - 550
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PL2870150T3 (pl) 2019-12-31
IN2015DN00137A (enExample) 2015-06-12
US20180222892A1 (en) 2018-08-09
AU2013286894B2 (en) 2017-12-07
KR20150032571A (ko) 2015-03-26
JP6109934B2 (ja) 2017-04-05
SG11201500024YA (en) 2015-03-30
AU2013286894A1 (en) 2015-01-22
JP2015522036A (ja) 2015-08-03
US9428502B2 (en) 2016-08-30
CA2877999A1 (en) 2014-01-09
US20160311803A1 (en) 2016-10-27
US10053450B2 (en) 2018-08-21
EP2870150B1 (en) 2019-06-19
CN104507928A (zh) 2015-04-08
NZ729443A (en) 2017-11-24
US20150210688A1 (en) 2015-07-30
AU2017265027A1 (en) 2017-12-14
US10118913B2 (en) 2018-11-06
ES2738823T3 (es) 2020-01-27
MX364815B (es) 2019-05-08
CA2877999C (en) 2021-02-23
KR102071095B1 (ko) 2020-01-29
EP2870150A1 (en) 2015-05-13
IL236407A (en) 2017-10-31
BR112015000106B1 (pt) 2022-02-22
ZA201409477B (en) 2021-05-26
RU2015103345A (ru) 2016-08-20
IL236407A0 (en) 2015-02-26
HK1208445A1 (en) 2016-03-04
WO2014008197A1 (en) 2014-01-09
BR112015000106A2 (pt) 2017-06-27
NZ703162A (en) 2017-05-26
MX2015000151A (es) 2015-04-10

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