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 PDFInfo
- 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
- Authority
- CN
- China
- Prior art keywords
- mixture
- compound
- mmol
- reduced pressure
- under reduced
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 C*=C(C*CCC(C(C(**)C1)N)=CCC1=*)N Chemical compound C*=C(C*CCC(C(C(**)C1)N)=CCC1=*)N 0.000 description 4
Classifications
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (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)
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 | 2012-11-06 | ||
| EP12382433.6 | 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)
| 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 |
| AR089771A1 (es) | 2012-01-31 | 2014-09-17 | Lilly Co Eli | Derivados de bencil sulfonamida utiles como inhibidores de mogat-2 |
| JP5852269B2 (ja) | 2012-01-31 | 2016-02-03 | イーライ リリー アンド カンパニー | Mogat−2阻害剤として有用な新規モルホリニル誘導体 |
| MX2015005739A (es) | 2012-11-06 | 2015-09-16 | Lilly Co Eli | Compuestos novedosos de bencil sulfonamida utiles como inhibidores de mogat-2. |
| 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 |
| CA3126334A1 (en) | 2019-01-11 | 2020-07-16 | Shionogi & Co., Ltd. | Dihydropyrazolopyrazinone derivative having mgat2 inhibitory activity |
Citations (2)
| 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)
| 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 |
| EP1659113A1 (en) | 2004-11-08 | 2006-05-24 | Evotec AG | Inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1) |
| EP1655283A1 (en) | 2004-11-08 | 2006-05-10 | Evotec OAI AG | 11beta-HSD1 Inhibitors |
| US8232282B2 (en) | 2006-09-28 | 2012-07-31 | Dainippon Sumitomo Pharma Co., Ltd. | Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the same |
| CA2709784A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| EP2272841A1 (en) | 2008-03-28 | 2011-01-12 | Banyu Pharmaceutical Co., Ltd. | Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor |
| JP2011522006A (ja) | 2008-06-04 | 2011-07-28 | アストラゼネカ アクチボラグ | 新規化合物v |
| US20110275647A1 (en) | 2009-02-23 | 2011-11-10 | 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 |
| JP5852269B2 (ja) | 2012-01-31 | 2016-02-03 | イーライ リリー アンド カンパニー | Mogat−2阻害剤として有用な新規モルホリニル誘導体 |
| AR089771A1 (es) | 2012-01-31 | 2014-09-17 | Lilly Co Eli | Derivados de bencil sulfonamida utiles como inhibidores de mogat-2 |
| MX2015005739A (es) | 2012-11-06 | 2015-09-16 | Lilly Co Eli | Compuestos novedosos de bencil sulfonamida utiles como inhibidores de mogat-2. |
-
2013
- 2013-01-24 JP JP2014554806A patent/JP5852269B2/ja not_active Expired - Fee Related
- 2013-01-24 CN CN201380007113.8A patent/CN104080777B/zh not_active Expired - Fee Related
- 2013-01-24 AP AP2014007793A patent/AP2014007793A0/xx unknown
- 2013-01-24 EP EP13702564.9A patent/EP2809661B1/en active Active
- 2013-01-24 SG SG11201404508XA patent/SG11201404508XA/en unknown
- 2013-01-24 CA CA2859992A patent/CA2859992A1/en not_active Abandoned
- 2013-01-24 KR KR1020147021129A patent/KR20140107641A/ko not_active Abandoned
- 2013-01-24 PE PE2014001194A patent/PE20141789A1/es not_active Application Discontinuation
- 2013-01-24 BR BR112014018712A patent/BR112014018712A8/pt not_active IP Right Cessation
- 2013-01-24 ES ES13702564T patent/ES2571577T3/es active Active
- 2013-01-24 WO PCT/US2013/022828 patent/WO2013116065A1/en not_active Ceased
- 2013-01-24 MX MX2014008604A patent/MX2014008604A/es unknown
- 2013-01-24 AU AU2013215549A patent/AU2013215549B2/en not_active Ceased
- 2013-01-24 US US14/372,833 patent/US8993568B2/en not_active Expired - Fee Related
- 2013-01-24 EA EA201491227A patent/EA024182B1/ru not_active IP Right Cessation
-
2014
- 2014-07-07 IL IL233542A patent/IL233542A0/en unknown
- 2014-07-08 CR CR20140325A patent/CR20140325A/es unknown
- 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
Patent Citations (2)
| 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 |
|---|---|
| EA024182B1 (ru) | 2016-08-31 |
| CR20140325A (es) | 2014-08-25 |
| JP2015504917A (ja) | 2015-02-16 |
| ZA201405227B (en) | 2016-05-25 |
| EP2809661A1 (en) | 2014-12-10 |
| HK1199024A1 (zh) | 2015-06-19 |
| AP2014007793A0 (en) | 2014-07-31 |
| US8993568B2 (en) | 2015-03-31 |
| PH12014501712A1 (en) | 2014-10-13 |
| AU2013215549A1 (en) | 2014-07-17 |
| CA2859992A1 (en) | 2013-08-08 |
| PE20141789A1 (es) | 2014-11-19 |
| MX2014008604A (es) | 2014-08-22 |
| PH12014501712B1 (en) | 2014-10-13 |
| EP2809661B1 (en) | 2016-04-06 |
| IL233542A0 (en) | 2014-08-31 |
| GT201400169A (es) | 2015-08-27 |
| BR112014018712A2 (https=) | 2017-06-20 |
| AU2013215549B2 (en) | 2015-09-03 |
| DOP2014000177A (es) | 2014-08-31 |
| WO2013116065A1 (en) | 2013-08-08 |
| JP5852269B2 (ja) | 2016-02-03 |
| CO7020914A2 (es) | 2014-08-11 |
| ES2571577T3 (es) | 2016-05-26 |
| KR20140107641A (ko) | 2014-09-04 |
| US20150005305A1 (en) | 2015-01-01 |
| BR112014018712A8 (pt) | 2017-07-11 |
| EA201491227A1 (ru) | 2015-01-30 |
| CN104080777A (zh) | 2014-10-01 |
| CL2014001862A1 (es) | 2014-11-14 |
| SG11201404508XA (en) | 2014-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20151209 Termination date: 20190124 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |