CN102239165A - 二酰甘油酰基转移酶抑制剂 - Google Patents

二酰甘油酰基转移酶抑制剂 Download PDF

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Publication number
CN102239165A
CN102239165A CN2009801482136A CN200980148213A CN102239165A CN 102239165 A CN102239165 A CN 102239165A CN 2009801482136 A CN2009801482136 A CN 2009801482136A CN 200980148213 A CN200980148213 A CN 200980148213A CN 102239165 A CN102239165 A CN 102239165A
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China
Prior art keywords
carboxylic acid
amino
ethyl
piperazine
acid
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CN2009801482136A
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Chinese (zh)
Inventor
戴维·罗伯特·博林
斯图尔特·海登
钱义民
员维亚
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VIA Pharmaceuticals Inc
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VIA Pharmaceuticals Inc
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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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • 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
    • 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
    • C07D417/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Indole Compounds (AREA)
CN2009801482136A 2008-12-03 2009-11-18 二酰甘油酰基转移酶抑制剂 Pending CN102239165A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11946708P 2008-12-03 2008-12-03
US61/119,467 2008-12-03
PCT/US2009/064971 WO2010065310A1 (en) 2008-12-03 2009-11-18 Inhibitors of diacylglycerol acyltransferase

Publications (1)

Publication Number Publication Date
CN102239165A true CN102239165A (zh) 2011-11-09

Family

ID=42231833

Family Applications (1)

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CN2009801482136A Pending CN102239165A (zh) 2008-12-03 2009-11-18 二酰甘油酰基转移酶抑制剂

Country Status (8)

Country Link
US (1) US8124766B2 (https=)
EP (1) EP2367817A4 (https=)
JP (1) JP2012510515A (https=)
CN (1) CN102239165A (https=)
AU (1) AU2009322774A1 (https=)
CA (1) CA2744152A1 (https=)
IL (1) IL212916A0 (https=)
WO (1) WO2010065310A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116457346A (zh) * 2020-10-08 2023-07-18 默沙东有限责任公司 作为新型二酰基甘油酯o-酰基转移酶2抑制剂的吲哚酮衍生物的制备
WO2024199387A1 (zh) * 2023-03-30 2024-10-03 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的化合物

Families Citing this family (20)

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US8115011B2 (en) 2007-05-22 2012-02-14 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
US8153644B2 (en) 2007-05-22 2012-04-10 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
US8211884B2 (en) * 2008-08-06 2012-07-03 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
JP4900361B2 (ja) * 2008-10-21 2012-03-21 ソニー株式会社 画像処理装置、画像処理方法およびプログラム
US8324385B2 (en) * 2008-10-30 2012-12-04 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
JP2012512252A (ja) * 2008-12-17 2012-05-31 ブイアイエイ・ファーマシューティカルズ・インコーポレーテッド ジアシルグリセロールアシルトランスフェラーゼの阻害剤
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
EA019685B1 (ru) 2009-02-06 2014-05-30 Янссен Фармасьютикалз, Инк. Новые замещенные бициклические гетероциклические соединения в качестве модуляторов гамма-секретазы
TWI461425B (zh) 2009-02-19 2014-11-21 Janssen Pharmaceuticals Inc 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類
BRPI1011190A8 (pt) 2009-05-07 2016-11-16 Janssen Pharmaceuticals Inc Derivados de indazol e aza-indazol substituídos como moduladores de gama secretase
ES2519565T3 (es) 2009-07-15 2014-11-07 Janssen Pharmaceuticals Inc. Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa
EP2477498A4 (en) * 2009-09-14 2013-02-27 Merck Sharp & Dohme INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
EP2523949B1 (en) 2010-01-15 2014-08-20 Janssen Pharmaceuticals Inc. Novel substituted triazole derivatives as gamma secretase modulators
CA2827969A1 (en) 2011-03-24 2012-09-27 Janssen Pharmaceuticals, Inc. Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
TWI567079B (zh) 2011-07-15 2017-01-21 健生醫藥公司 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物
NZ702611A (en) 2012-05-16 2016-10-28 Cellzome Ltd Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer’s disease
AU2013366668B2 (en) 2012-12-20 2017-07-20 Janssen Pharmaceutica Nv Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators
ES2612215T3 (es) 2013-01-17 2017-05-12 Janssen Pharmaceutica, N.V. Novedosos derivados de pirido-piperazinona sustituidos como moduladores de gamma secretasa
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
WO2021262484A1 (en) * 2020-06-24 2021-12-30 Pmv Pharmaceuticals, Inc. Combination therapy for treatment of cancer

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3250771A (en) * 1962-12-17 1966-05-10 Geigy Chem Corp 5-monocarbocyclic aryl-n-lower alkyl-2-pyrrolidine carboxylic acid, esters, amides and derivatives thereof
US3929793A (en) * 1973-07-24 1975-12-30 Boehringer Mannheim Gmbh Certain piperazine-containing indole compounds
US4066654A (en) * 1975-04-16 1978-01-03 G. D. Searle & Co. 1-triarylalkyl-4-phenyl-4-piperidine carboxylic acids and derivatives
US20040019067A1 (en) * 1999-01-22 2004-01-29 Amgen Inc. Kinase inhibitors
US7094896B2 (en) * 2001-01-22 2006-08-22 Hoffmann-La Roche Inc. Diaminothiazoles having antiproliferative activity
WO2008099221A1 (en) * 2007-02-15 2008-08-21 Prosidion Limited Amide and urea derivatives for the treatment of metabolic diseases
WO2008141976A1 (en) * 2007-05-22 2008-11-27 Via Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors

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AU2002333456B2 (en) 2001-08-31 2008-07-17 Sanofi-Aventis Deutschland Gmbh Diaryl cycloalkyl derivatives, method for producing the same and the use thereof as PPAR activators
AU2003261935A1 (en) 2002-09-06 2004-03-29 Takeda Pharmaceutical Company Limited Furan or thiophene derivative and medicinal use thereof
RU2342388C2 (ru) * 2002-11-22 2008-12-27 Джапан Тобакко Инк. Конденсированные бициклические азотсодержащие гетероциклы, обладающие dgat ингибирующим действием
AU2006258917A1 (en) 2005-06-11 2006-12-21 Astrazeneca Ab Oxadiazole derivatives as DGAT inhibitors
KR20080063865A (ko) 2005-11-28 2008-07-07 에프. 호프만-라 로슈 아게 다이아실글리세롤 아실전이효소(dgat)의 저해제

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3250771A (en) * 1962-12-17 1966-05-10 Geigy Chem Corp 5-monocarbocyclic aryl-n-lower alkyl-2-pyrrolidine carboxylic acid, esters, amides and derivatives thereof
US3929793A (en) * 1973-07-24 1975-12-30 Boehringer Mannheim Gmbh Certain piperazine-containing indole compounds
US4066654A (en) * 1975-04-16 1978-01-03 G. D. Searle & Co. 1-triarylalkyl-4-phenyl-4-piperidine carboxylic acids and derivatives
US20040019067A1 (en) * 1999-01-22 2004-01-29 Amgen Inc. Kinase inhibitors
US7094896B2 (en) * 2001-01-22 2006-08-22 Hoffmann-La Roche Inc. Diaminothiazoles having antiproliferative activity
WO2008099221A1 (en) * 2007-02-15 2008-08-21 Prosidion Limited Amide and urea derivatives for the treatment of metabolic diseases
WO2008141976A1 (en) * 2007-05-22 2008-11-27 Via Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116457346A (zh) * 2020-10-08 2023-07-18 默沙东有限责任公司 作为新型二酰基甘油酯o-酰基转移酶2抑制剂的吲哚酮衍生物的制备
WO2024199387A1 (zh) * 2023-03-30 2024-10-03 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的化合物

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Publication number Publication date
CA2744152A1 (en) 2010-06-10
EP2367817A4 (en) 2012-05-09
WO2010065310A1 (en) 2010-06-10
US8124766B2 (en) 2012-02-28
US20100145047A1 (en) 2010-06-10
IL212916A0 (en) 2011-07-31
EP2367817A1 (en) 2011-09-28
AU2009322774A1 (en) 2011-06-30
JP2012510515A (ja) 2012-05-10

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