EA024182B1 - Новые производные морфолинила, подходящие для применения в качестве ингибиторов mogat-2 - Google Patents

Новые производные морфолинила, подходящие для применения в качестве ингибиторов mogat-2 Download PDF

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Publication number
EA024182B1
EA024182B1 EA201491227A EA201491227A EA024182B1 EA 024182 B1 EA024182 B1 EA 024182B1 EA 201491227 A EA201491227 A EA 201491227A EA 201491227 A EA201491227 A EA 201491227A EA 024182 B1 EA024182 B1 EA 024182B1
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EA
Eurasian Patent Office
Prior art keywords
mixture
mmol
added
ethyl
reduced pressure
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EA201491227A
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English (en)
Russian (ru)
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EA201491227A1 (ru
Inventor
Мария Росарио Гонсалес-Гарсиа
Мария Кармен Фернандес
Original Assignee
Эли Лилли Энд Компани
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Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201491227A1 publication Critical patent/EA201491227A1/ru
Publication of EA024182B1 publication Critical patent/EA024182B1/ru

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Classifications

    • 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
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
  • Hematology (AREA)
  • Diabetes (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)
EA201491227A 2012-01-31 2013-01-24 Новые производные морфолинила, подходящие для применения в качестве ингибиторов mogat-2 EA024182B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP12382037 2012-01-31
US201261617093P 2012-03-29 2012-03-29
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
EA201491227A1 EA201491227A1 (ru) 2015-01-30
EA024182B1 true EA024182B1 (ru) 2016-08-31

Family

ID=48905712

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201491227A EA024182B1 (ru) 2012-01-31 2013-01-24 Новые производные морфолинила, подходящие для применения в качестве ингибиторов mogat-2

Country Status (23)

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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2807147A1 (en) 2012-01-23 2014-12-03 Eli Lilly and Company Phenyl methanesulfonamide derivatives useful as mgat - 2 inhibitors
SG11201404508XA (en) 2012-01-31 2014-10-30 Lilly Co Eli Novel morpholinyl derivatives useful as mogat-2 inhibitors
AR089771A1 (es) 2012-01-31 2014-09-17 Lilly Co Eli Derivados de bencil sulfonamida utiles como inhibidores de mogat-2
EP2917194B1 (en) 2012-11-06 2017-09-27 Eli Lilly and Company Novel benzyl sulfonamide compounds useful as mogat-2 inhibitors
US10335401B2 (en) 2015-12-21 2019-07-02 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
KR20210114001A (ko) 2019-01-11 2021-09-17 시오노기 앤드 컴파니, 리미티드 Mgat2 저해 활성을 갖는 다이하이드로피라졸로피라지논 유도체

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2078719A1 (en) * 2006-09-28 2009-07-15 Dainippon Sumitomo Pharma Co., Ltd. Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the compound
WO2009147211A1 (en) * 2008-06-04 2009-12-10 Biovitrum Ab (Publ) New compounds v

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
WO2000006083A2 (en) 1998-07-31 2000-02-10 Eli Lilly And Company Sulfonamide derivatives
CA2338862A1 (en) 1998-07-31 2000-02-10 Dennis Michael Zimmerman Alkenyl sulphonamide 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)
TW200831092A (en) * 2006-12-21 2008-08-01 Astrazeneca Ab Therapeutic agents
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
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
CA2751244A1 (en) 2009-02-23 2010-08-26 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
EP2807147A1 (en) 2012-01-23 2014-12-03 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
SG11201404508XA (en) 2012-01-31 2014-10-30 Lilly Co Eli Novel morpholinyl derivatives useful as mogat-2 inhibitors
EP2917194B1 (en) 2012-11-06 2017-09-27 Eli Lilly and Company Novel 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
EP2078719A1 (en) * 2006-09-28 2009-07-15 Dainippon Sumitomo Pharma Co., Ltd. Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the compound
WO2009147211A1 (en) * 2008-06-04 2009-12-10 Biovitrum Ab (Publ) New compounds v

Also Published As

Publication number Publication date
BR112014018712A2 (enExample) 2017-06-20
AU2013215549A1 (en) 2014-07-17
US20150005305A1 (en) 2015-01-01
JP2015504917A (ja) 2015-02-16
HK1199024A1 (zh) 2015-06-19
PH12014501712A1 (en) 2014-10-13
ZA201405227B (en) 2016-05-25
CR20140325A (es) 2014-08-25
DOP2014000177A (es) 2014-08-31
AU2013215549B2 (en) 2015-09-03
IL233542A0 (en) 2014-08-31
JP5852269B2 (ja) 2016-02-03
EA201491227A1 (ru) 2015-01-30
PH12014501712B1 (en) 2014-10-13
CL2014001862A1 (es) 2014-11-14
ES2571577T3 (es) 2016-05-26
US8993568B2 (en) 2015-03-31
GT201400169A (es) 2015-08-27
KR20140107641A (ko) 2014-09-04
EP2809661A1 (en) 2014-12-10
WO2013116065A1 (en) 2013-08-08
BR112014018712A8 (pt) 2017-07-11
CA2859992A1 (en) 2013-08-08
AP2014007793A0 (en) 2014-07-31
CO7020914A2 (es) 2014-08-11
SG11201404508XA (en) 2014-10-30
EP2809661B1 (en) 2016-04-06
PE20141789A1 (es) 2014-11-19
CN104080777A (zh) 2014-10-01
MX2014008604A (es) 2014-08-22
CN104080777B (zh) 2015-12-09

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU