AU2013215549B2 - Novel morpholinyl derivatives useful as MOGAT-2 inhibitors - Google Patents
Novel morpholinyl derivatives useful as MOGAT-2 inhibitors Download PDFInfo
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- AU2013215549B2 AU2013215549B2 AU2013215549A AU2013215549A AU2013215549B2 AU 2013215549 B2 AU2013215549 B2 AU 2013215549B2 AU 2013215549 A AU2013215549 A AU 2013215549A AU 2013215549 A AU2013215549 A AU 2013215549A AU 2013215549 B2 AU2013215549 B2 AU 2013215549B2
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- 125000002757 morpholinyl group Chemical group 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 98
- 150000003839 salts Chemical class 0.000 claims abstract description 28
- 238000000034 method Methods 0.000 claims abstract description 16
- 208000006575 hypertriglyceridemia Diseases 0.000 claims abstract description 10
- 238000004519 manufacturing process Methods 0.000 claims abstract description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 23
- 229910052731 fluorine Inorganic materials 0.000 claims description 21
- 229910052801 chlorine Inorganic materials 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 15
- 238000011282 treatment Methods 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- USJUUYYGHABIBU-UHFFFAOYSA-N methanesulfonamide;hydrochloride Chemical compound Cl.CS(N)(=O)=O USJUUYYGHABIBU-UHFFFAOYSA-N 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 5
- 239000003085 diluting agent Substances 0.000 claims description 5
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Classifications
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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
- C07D295/02—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)
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- 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 (2)
| Publication Number | Publication Date |
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| AU2013215549A1 AU2013215549A1 (en) | 2014-07-17 |
| AU2013215549B2 true AU2013215549B2 (en) | 2015-09-03 |
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| AU2013215549A Ceased AU2013215549B2 (en) | 2012-01-31 | 2013-01-24 | Novel morpholinyl derivatives useful as MOGAT-2 inhibitors |
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| SG (1) | SG11201404508XA (enExample) |
| WO (1) | WO2013116065A1 (enExample) |
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| 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 |
Citations (1)
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| EP2078719A1 (en) * | 2006-09-28 | 2009-07-15 | Dainippon Sumitomo Pharma Co., Ltd. | Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the compound |
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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) |
| 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 CN CN201380007113.8A patent/CN104080777B/zh not_active Expired - Fee Related
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- 2013-01-24 AU AU2013215549A patent/AU2013215549B2/en not_active Ceased
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- 2013-01-24 ES ES13702564T patent/ES2571577T3/es active Active
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2014
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- 2014-07-30 PH PH12014501712A patent/PH12014501712B1/en unknown
- 2014-07-30 DO DO2014000177A patent/DOP2014000177A/es unknown
Patent Citations (1)
| 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 |
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| 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 |
| 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 |
| 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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