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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    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (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)

Application Number Title Priority Date Filing Date
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8153644B2 (en) * 2007-05-22 2012-04-10 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
US8115011B2 (en) * 2007-05-22 2012-02-14 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
AU2009333333A1 (en) * 2008-12-17 2011-06-30 Via Pharmaceuticals, Inc Inhibitors of diacylglycerol aclytransferase
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
WO2010089292A1 (en) 2009-02-06 2010-08-12 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators
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
AU2010262036B2 (en) 2009-05-07 2014-10-30 Cellzome Limited Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators
JP2012532912A (ja) 2009-07-15 2012-12-20 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド ガンマセクレターゼモジュレーターとしての置換されたトリアゾールおよびイミダゾール誘導体
US20120172369A1 (en) * 2009-09-14 2012-07-05 Ting Pauline C Inhibitors of diacylglycerol acyltransferase
BR112012017310A2 (pt) 2010-01-15 2016-04-19 Janssen Pharmaceuticals Inc derivados de triazol substituídos como moduladores de gama secretase
AU2012230348A1 (en) 2011-03-24 2013-08-29 Cellzome Limited Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators
KR101913135B1 (ko) 2011-07-15 2018-10-30 얀센 파마슈티칼즈, 인코포레이티드 감마 세크레타제 조절 인자로서의 신규의 치환 인돌 유도체
US9181245B2 (en) 2012-05-16 2015-11-10 Janssen Pharmaceuticals, Inc. Substituted pyrido[1,2-a]pyrazines and substituted pyrido[1,2-a][1,4]diazepines for the treatment of (inter alia) Alzheimer's disease
CA2889249C (en) 2012-12-20 2021-02-16 Francois Paul Bischoff Tricyclic 3,4-dihydro-2h-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators
CA2891755C (en) 2013-01-17 2021-10-26 Janssen Pharmaceutica Nv Substituted pyrido-piperazinone derivatives as gamma secretase modulators
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
US11938124B2 (en) 2020-06-24 2024-03-26 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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20040199A2 (en) 2001-08-31 2005-04-30 Aventis Pharma 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
KR100772297B1 (ko) 2002-11-22 2007-11-02 니뽄 다바코 산교 가부시키가이샤 융합 비시클릭 질소-함유 헤테로사이클
KR20080015113A (ko) 2005-06-11 2008-02-18 아스트라제네카 아베 Dgat 억제제로서의 옥사디아졸 유도체
CA2630269C (en) 2005-11-28 2011-07-05 F. Hoffmann-La Roche Ag Inhibitors of diacyglycerol acyltransferase (dgat)

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

Also Published As

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

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