JP5852269B2 - Ｍｏｇａｔ−２阻害剤として有用な新規モルホリニル誘導体 - Google Patents
Ｍｏｇａｔ−２阻害剤として有用な新規モルホリニル誘導体 Download PDFInfo
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- JP5852269B2 JP5852269B2 JP2014554806A JP2014554806A JP5852269B2 JP 5852269 B2 JP5852269 B2 JP 5852269B2 JP 2014554806 A JP2014554806 A JP 2014554806A JP 2014554806 A JP2014554806 A JP 2014554806A JP 5852269 B2 JP5852269 B2 JP 5852269B2
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- MWKJTNBSKNUMFN-UHFFFAOYSA-N trifluoromethyltrimethylsilane Chemical compound C[Si](C)(C)C(F)(F)F MWKJTNBSKNUMFN-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000001262 western blot Methods 0.000 description 1
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
Landscapes
- 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)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12382037.5 | 2012-01-31 | ||
| EP12382037 | 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 (3)
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|---|---|
| JP2015504917A JP2015504917A (ja) | 2015-02-16 |
| JP2015504917A5 JP2015504917A5 (enExample) | 2015-03-26 |
| JP5852269B2 true JP5852269B2 (ja) | 2016-02-03 |
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| JP2014554806A Expired - Fee Related JP5852269B2 (ja) | 2012-01-31 | 2013-01-24 | Ｍｏｇａｔ−２阻害剤として有用な新規モルホリニル誘導体 |
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| EP (1) | EP2809661B1 (enExample) |
| JP (1) | JP5852269B2 (enExample) |
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| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
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| 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) |
| US8232282B2 (en) | 2006-09-28 | 2012-07-31 | Dainippon Sumitomo Pharma Co., Ltd. | Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the same |
| 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 |
| AU2009254547A1 (en) * | 2008-06-04 | 2009-12-10 | Astrazeneca Ab (Publ) | New compounds V |
| 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 |
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2013
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- 2013-01-24 MX MX2014008604A patent/MX2014008604A/es unknown
- 2013-01-24 PE PE2014001194A patent/PE20141789A1/es not_active Application Discontinuation
- 2013-01-24 CN CN201380007113.8A patent/CN104080777B/zh not_active Expired - Fee Related
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- 2013-01-24 BR BR112014018712A patent/BR112014018712A8/pt not_active IP Right Cessation
- 2013-01-24 AU AU2013215549A patent/AU2013215549B2/en not_active Ceased
- 2013-01-24 AP AP2014007793A patent/AP2014007793A0/xx unknown
- 2013-01-24 ES ES13702564T patent/ES2571577T3/es active Active
- 2013-01-24 CA CA2859992A patent/CA2859992A1/en not_active Abandoned
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- 2013-01-24 JP JP2014554806A patent/JP5852269B2/ja not_active Expired - Fee Related
- 2013-01-24 US US14/372,833 patent/US8993568B2/en not_active Expired - Fee Related
- 2013-01-24 KR KR1020147021129A patent/KR20140107641A/ko not_active Abandoned
- 2013-01-24 WO PCT/US2013/022828 patent/WO2013116065A1/en not_active Ceased
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2014
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- 2014-07-15 CL CL2014001862A patent/CL2014001862A1/es unknown
- 2014-07-16 ZA ZA2014/05227A patent/ZA201405227B/en unknown
- 2014-07-24 CO CO14161421A patent/CO7020914A2/es unknown
- 2014-07-29 GT GT201400169A patent/GT201400169A/es unknown
- 2014-07-30 PH PH12014501712A patent/PH12014501712B1/en unknown
- 2014-07-30 DO DO2014000177A patent/DOP2014000177A/es unknown
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 |
| 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 |
| EA024182B1 (ru) | 2016-08-31 |
| 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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