CN104080777B - 用作mogat-2抑制剂的吗啉基衍生物 - Google Patents

用作mogat-2抑制剂的吗啉基衍生物 Download PDF

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Publication number
CN104080777B
CN104080777B CN201380007113.8A CN201380007113A CN104080777B CN 104080777 B CN104080777 B CN 104080777B CN 201380007113 A CN201380007113 A CN 201380007113A CN 104080777 B CN104080777 B CN 104080777B
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mixture
compound
mmol
reduced pressure
under reduced
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Expired - Fee Related
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CN201380007113.8A
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English (en)
Chinese (zh)
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CN104080777A (zh
Inventor
M.R.冈萨雷斯-加西亚
M.C.费尔南德斯
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Eli Lilly and Co
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Eli Lilly and Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201380007113.8A 2012-01-31 2013-01-24 用作mogat-2抑制剂的吗啉基衍生物 Expired - Fee Related CN104080777B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP12382037 2012-01-31
EP12382037.5 2012-01-31
US201261617093P 2012-03-29 2012-03-29
US61/617,093 2012-03-29
EP12382433.6 2012-11-06
EP12382433 2012-11-06
PCT/US2013/022828 WO2013116065A1 (en) 2012-01-31 2013-01-24 Novel morpholinyl derivatives useful as mogat-2 inhibitors

Publications (2)

Publication Number Publication Date
CN104080777A CN104080777A (zh) 2014-10-01
CN104080777B true CN104080777B (zh) 2015-12-09

Family

ID=48905712

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380007113.8A Expired - Fee Related CN104080777B (zh) 2012-01-31 2013-01-24 用作mogat-2抑制剂的吗啉基衍生物

Country Status (23)

Country Link
US (1) US8993568B2 (https=)
EP (1) EP2809661B1 (https=)
JP (1) JP5852269B2 (https=)
KR (1) KR20140107641A (https=)
CN (1) CN104080777B (https=)
AP (1) AP2014007793A0 (https=)
AU (1) AU2013215549B2 (https=)
BR (1) BR112014018712A8 (https=)
CA (1) CA2859992A1 (https=)
CL (1) CL2014001862A1 (https=)
CO (1) CO7020914A2 (https=)
CR (1) CR20140325A (https=)
DO (1) DOP2014000177A (https=)
EA (1) EA024182B1 (https=)
ES (1) ES2571577T3 (https=)
GT (1) GT201400169A (https=)
IL (1) IL233542A0 (https=)
MX (1) MX2014008604A (https=)
PE (1) PE20141789A1 (https=)
PH (1) PH12014501712B1 (https=)
SG (1) SG11201404508XA (https=)
WO (1) WO2013116065A1 (https=)
ZA (1) ZA201405227B (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073856B2 (en) 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
BR112014018712A8 (pt) 2012-01-31 2017-07-11 Lilly Co Eli Derivados de morfolinila úteis como inibidores de mogat-2
AR089771A1 (es) 2012-01-31 2014-09-17 Lilly Co Eli Derivados de bencil sulfonamida utiles como inhibidores de mogat-2
US9416138B2 (en) 2012-11-06 2016-08-16 Eli Lilly And Company Benzyl sulfonamide compounds useful as MoGAT-2 inhibitors
EP3395798A4 (en) 2015-12-21 2019-07-17 Shionogi & Co., Ltd NON-AROMATIC HETEROCYCLIC DERIVATIVE HAVING MGAT2 INHIBITORY ACTIVITY
TWI782056B (zh) 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有ｍｇａｔ２抑制活性的縮合環衍生物
MX2021008050A (es) 2019-01-11 2021-08-05 Shionogi & Co Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008075070A1 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Sulfonamide derivatives for therapeutic use as fatty acid synthase inhibitors
CN102026976A (zh) * 2007-12-05 2011-04-20 阿斯利康(瑞典)有限公司 作为抗肥胖药物的吗啉衍生物

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5889006A (en) 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
WO2000006539A1 (en) 1998-07-31 2000-02-10 Eli Lilly And Company Alkenyl sulphonamide derivatives
AU5235699A (en) 1998-07-31 2000-02-21 Eli Lilly And Company Sulfonamide derivatives
GB0408777D0 (en) 2004-04-20 2004-05-26 Glaxo Group Ltd Compounds
EP1655283A1 (en) 2004-11-08 2006-05-10 Evotec OAI AG 11beta-HSD1 Inhibitors
EP1659113A1 (en) 2004-11-08 2006-05-24 Evotec AG Inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1)
EP2078719A4 (en) * 2006-09-28 2009-11-11 Dainippon Sumitomo Pharma Co COMPOUND WITH BICYCLIC PYRIMIDINE STRUCTURE AND THE COMPOUND CONTAINING PHARMACEUTICAL COMPOSITION
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009119726A1 (ja) 2008-03-28 2009-10-01 萬有製薬株式会社 メラニン凝集ホルモン受容体拮抗作用を有するジアリールメチルアミド誘導体
WO2009147211A1 (en) * 2008-06-04 2009-12-10 Biovitrum Ab (Publ) New compounds v
AU2010216633A1 (en) 2009-02-23 2011-09-08 Msd K.K. Pyrimidin-4(3H)-one derivatives
JP2014051434A (ja) 2010-12-28 2014-03-20 Dainippon Sumitomo Pharma Co Ltd 二環性ピリミジン誘導体
US9073856B2 (en) 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
AR089771A1 (es) 2012-01-31 2014-09-17 Lilly Co Eli Derivados de bencil sulfonamida utiles como inhibidores de mogat-2
BR112014018712A8 (pt) 2012-01-31 2017-07-11 Lilly Co Eli Derivados de morfolinila úteis como inibidores de mogat-2
US9416138B2 (en) 2012-11-06 2016-08-16 Eli Lilly And Company Benzyl sulfonamide compounds useful as MoGAT-2 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008075070A1 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Sulfonamide derivatives for therapeutic use as fatty acid synthase inhibitors
CN102026976A (zh) * 2007-12-05 2011-04-20 阿斯利康(瑞典)有限公司 作为抗肥胖药物的吗啉衍生物

Also Published As

Publication number Publication date
JP5852269B2 (ja) 2016-02-03
PE20141789A1 (es) 2014-11-19
EA024182B1 (ru) 2016-08-31
CN104080777A (zh) 2014-10-01
US8993568B2 (en) 2015-03-31
WO2013116065A1 (en) 2013-08-08
CA2859992A1 (en) 2013-08-08
KR20140107641A (ko) 2014-09-04
CL2014001862A1 (es) 2014-11-14
CO7020914A2 (es) 2014-08-11
PH12014501712A1 (en) 2014-10-13
ZA201405227B (en) 2016-05-25
GT201400169A (es) 2015-08-27
BR112014018712A2 (https=) 2017-06-20
PH12014501712B1 (en) 2014-10-13
AU2013215549B2 (en) 2015-09-03
ES2571577T3 (es) 2016-05-26
AP2014007793A0 (en) 2014-07-31
MX2014008604A (es) 2014-08-22
HK1199024A1 (zh) 2015-06-19
EP2809661B1 (en) 2016-04-06
JP2015504917A (ja) 2015-02-16
IL233542A0 (en) 2014-08-31
EP2809661A1 (en) 2014-12-10
US20150005305A1 (en) 2015-01-01
SG11201404508XA (en) 2014-10-30
CR20140325A (es) 2014-08-25
AU2013215549A1 (en) 2014-07-17
DOP2014000177A (es) 2014-08-31
BR112014018712A8 (pt) 2017-07-11
EA201491227A1 (ru) 2015-01-30

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Granted publication date: 20151209

Termination date: 20190124

CF01 Termination of patent right due to non-payment of annual fee