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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  • 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)
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) PH12014501712A1 (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
US9073856B2 (en) 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
MX2014008604A (es) 2012-01-31 2014-08-22 Lilly Co Eli Nuevos derivados de morofolinilo utiles como inhibidores de mogat-2.
AR089771A1 (es) 2012-01-31 2014-09-17 Lilly Co Eli Derivados de bencil sulfonamida utiles como inhibidores de mogat-2
CA2886831A1 (en) 2012-11-06 2014-05-15 Eli Lilly And Company Novel benzyl sulfonamide compounds useful as mogat-2 inhibitors
JPWO2017110841A1 (ja) 2015-12-21 2018-10-11 塩野義製薬株式会社 Ｍｇａｔ２阻害活性を有する非芳香族複素環誘導体
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
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
US6387954B1 (en) 1998-07-31 2002-05-14 Eli Lilly And Company Alkenyl sulphonamide derivatives
US6500865B1 (en) 1998-07-31 2002-12-31 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)
TW200831092A (en) * 2006-12-21 2008-08-01 Astrazeneca Ab Therapeutic agents
KR20100097701A (ko) * 2007-12-05 2010-09-03 아스트라제네카 아베 비만 치료제로서의 모르폴린 유도체
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
CA2717384A1 (en) 2008-03-28 2009-10-01 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
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
MX2014008604A (es) 2012-01-31 2014-08-22 Lilly Co Eli Nuevos derivados de morofolinilo utiles como inhibidores de mogat-2.
CA2886831A1 (en) 2012-11-06 2014-05-15 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
CN104080777B (zh) 2015-12-09
ES2571577T3 (es) 2016-05-26
CA2859992A1 (en) 2013-08-08
EP2809661A1 (en) 2014-12-10
CL2014001862A1 (es) 2014-11-14
PH12014501712B1 (en) 2014-10-13
PH12014501712A1 (en) 2014-10-13
GT201400169A (es) 2015-08-27
PE20141789A1 (es) 2014-11-19
CN104080777A (zh) 2014-10-01
SG11201404508XA (en) 2014-10-30
KR20140107641A (ko) 2014-09-04
WO2013116065A1 (en) 2013-08-08
BR112014018712A8 (pt) 2017-07-11
BR112014018712A2 (enExample) 2017-06-20
AU2013215549B2 (en) 2015-09-03
HK1199024A1 (zh) 2015-06-19
AP2014007793A0 (en) 2014-07-31
CO7020914A2 (es) 2014-08-11
AU2013215549A1 (en) 2014-07-17
JP2015504917A (ja) 2015-02-16
JP5852269B2 (ja) 2016-02-03
CR20140325A (es) 2014-08-25
DOP2014000177A (es) 2014-08-31
US8993568B2 (en) 2015-03-31
EP2809661B1 (en) 2016-04-06
EA201491227A1 (ru) 2015-01-30
ZA201405227B (en) 2016-05-25
IL233542A0 (en) 2014-08-31
MX2014008604A (es) 2014-08-22
US20150005305A1 (en) 2015-01-01

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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