CN103703009B - 作为二酰基甘油酰基转移酶抑制剂的新化合物 - Google Patents
作为二酰基甘油酰基转移酶抑制剂的新化合物 Download PDFInfo
- Publication number
- CN103703009B CN103703009B CN201280035792.5A CN201280035792A CN103703009B CN 103703009 B CN103703009 B CN 103703009B CN 201280035792 A CN201280035792 A CN 201280035792A CN 103703009 B CN103703009 B CN 103703009B
- Authority
- CN
- China
- Prior art keywords
- amino
- pyrimido
- oxazepine
- alkyl
- indol
- 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 CC(COc1c2c(Cl)nc(C3=*C3)n1)(*=*)N(C(C=C)=CC1=C(*)CCCC1)C2=O Chemical compound CC(COc1c2c(Cl)nc(C3=*C3)n1)(*=*)N(C(C=C)=CC1=C(*)CCCC1)C2=O 0.000 description 14
- SANWNNBJJJRVKJ-UHFFFAOYSA-N Brc(cc1cc2)ccc1[n]2-c1ncc[s]1 Chemical compound Brc(cc1cc2)ccc1[n]2-c1ncc[s]1 SANWNNBJJJRVKJ-UHFFFAOYSA-N 0.000 description 1
- SYGFTZXDDPYORE-UHFFFAOYSA-N Brc1cnc2[n](C3CC3)ccc2c1 Chemical compound Brc1cnc2[n](C3CC3)ccc2c1 SYGFTZXDDPYORE-UHFFFAOYSA-N 0.000 description 1
- UYGOQOHDWQNQFP-UHFFFAOYSA-N CC(C)c(c1cc(Br)ccc11)c[n]1-c1ccccc1 Chemical compound CC(C)c(c1cc(Br)ccc11)c[n]1-c1ccccc1 UYGOQOHDWQNQFP-UHFFFAOYSA-N 0.000 description 1
- FBNRLQRIMLEPOY-UHFFFAOYSA-N CC(C)c1c[nH]c(cc2)c1cc2Br Chemical compound CC(C)c1c[nH]c(cc2)c1cc2Br FBNRLQRIMLEPOY-UHFFFAOYSA-N 0.000 description 1
- QDZBZNGFEAVJAL-UHFFFAOYSA-N CCC[n](ccc1n2)c1ccc2Cl Chemical compound CCC[n](ccc1n2)c1ccc2Cl QDZBZNGFEAVJAL-UHFFFAOYSA-N 0.000 description 1
- PFDALSPZOMRWFR-UHFFFAOYSA-N CCN(c(c1c2)ccc2[N+]([O-])=O)N/C1=[O]\C Chemical compound CCN(c(c1c2)ccc2[N+]([O-])=O)N/C1=[O]\C PFDALSPZOMRWFR-UHFFFAOYSA-N 0.000 description 1
- OHMVKTPDRSFWBF-UHFFFAOYSA-N CCOC(CN(CCc1c2ccc(Br)c1)C2=O)=O Chemical compound CCOC(CN(CCc1c2ccc(Br)c1)C2=O)=O OHMVKTPDRSFWBF-UHFFFAOYSA-N 0.000 description 1
- MDDZVMLRPJFVMF-UHFFFAOYSA-N CCc(cc1)ccs1OC Chemical compound CCc(cc1)ccs1OC MDDZVMLRPJFVMF-UHFFFAOYSA-N 0.000 description 1
- YPXTURNKDCGSJZ-WUXMJOGZSA-N CNC(C(C/C(/C=C1)=N/OC)=C1N)=O Chemical compound CNC(C(C/C(/C=C1)=N/OC)=C1N)=O YPXTURNKDCGSJZ-WUXMJOGZSA-N 0.000 description 1
- LWPPASWKWXDDFK-UHFFFAOYSA-N Clc1ncc2[nH]ccc2n1 Chemical compound Clc1ncc2[nH]ccc2n1 LWPPASWKWXDDFK-UHFFFAOYSA-N 0.000 description 1
- ABZLJEWBOGWLPQ-UHFFFAOYSA-N OCCN(C(c(c(Cl)ncn1)c1Cl)=O)c(cc1cc2)cnc1[n]2-c1ccc(C(F)(F)F)cc1 Chemical compound OCCN(C(c(c(Cl)ncn1)c1Cl)=O)c(cc1cc2)cnc1[n]2-c1ccc(C(F)(F)F)cc1 ABZLJEWBOGWLPQ-UHFFFAOYSA-N 0.000 description 1
- WTLMLWLPQFFATI-UHFFFAOYSA-N OCCN(C(c(c(Cl)ncn1)c1Cl)O)c(cc(cc[n]1-c2ccccc2)c1c1)c1F Chemical compound OCCN(C(c(c(Cl)ncn1)c1Cl)O)c(cc(cc[n]1-c2ccccc2)c1c1)c1F WTLMLWLPQFFATI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Child & Adolescent Psychology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN1452DE2011 | 2011-05-20 | ||
| IN1452/DEL/2011 | 2011-05-20 | ||
| US201161503728P | 2011-07-01 | 2011-07-01 | |
| US61/503,728 | 2011-07-01 | ||
| PCT/US2012/038523 WO2012162129A1 (en) | 2011-05-20 | 2012-05-18 | Novel compounds as diacylglycerol acyltransferase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103703009A CN103703009A (zh) | 2014-04-02 |
| CN103703009B true CN103703009B (zh) | 2016-08-17 |
Family
ID=47217645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280035792.5A Expired - Fee Related CN103703009B (zh) | 2011-05-20 | 2012-05-18 | 作为二酰基甘油酰基转移酶抑制剂的新化合物 |
Country Status (34)
| Country | Link |
|---|---|
| US (4) | US8859536B2 (https=) |
| EP (1) | EP2710013B1 (https=) |
| JP (1) | JP5844456B2 (https=) |
| KR (1) | KR101919080B1 (https=) |
| CN (1) | CN103703009B (https=) |
| AU (1) | AU2012259044B2 (https=) |
| BR (1) | BR112013029935B1 (https=) |
| CA (1) | CA2836669C (https=) |
| CO (1) | CO6811855A2 (https=) |
| CR (1) | CR20130602A (https=) |
| CY (1) | CY1118188T1 (https=) |
| DK (1) | DK2710013T3 (https=) |
| DO (1) | DOP2013000272A (https=) |
| EA (1) | EA023030B1 (https=) |
| ES (1) | ES2588748T3 (https=) |
| HR (1) | HRP20161089T1 (https=) |
| HU (1) | HUE028870T2 (https=) |
| IL (1) | IL229488A (https=) |
| LT (1) | LT2710013T (https=) |
| MA (1) | MA35185B1 (https=) |
| ME (1) | ME02479B (https=) |
| MX (1) | MX346494B (https=) |
| MY (1) | MY184553A (https=) |
| PE (1) | PE20141204A1 (https=) |
| PH (1) | PH12013502401A1 (https=) |
| PL (1) | PL2710013T3 (https=) |
| PT (1) | PT2710013T (https=) |
| RS (1) | RS55006B1 (https=) |
| SG (1) | SG195044A1 (https=) |
| SI (1) | SI2710013T1 (https=) |
| SM (1) | SMT201600328B (https=) |
| UA (1) | UA111360C2 (https=) |
| WO (1) | WO2012162129A1 (https=) |
| ZA (1) | ZA201308664B (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2836669C (en) | 2011-05-20 | 2019-03-19 | Glaxosmithkline Intellectual Property (No.2) Limited | Compounds as diacylglycerol acyltransferase inhibitors |
| WO2014081996A1 (en) * | 2012-11-23 | 2014-05-30 | Glaxosmithkline Llc | Novel compounds as diacylglycerol acyltransferase inhibitors |
| US9796729B2 (en) | 2012-11-23 | 2017-10-24 | Glaxosmithkline Llc | Compounds as diacylglycerol acyltransferase inhibitors |
| EA031114B1 (ru) | 2012-11-23 | 2018-11-30 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | ПРОИЗВОДНЫЕ ДИГИДРОПИРИМИДО[5,4-f]ОКСАЗЕПИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ДИАЦИЛГЛИЦЕРИН АЦИЛТРАНСФЕРАЗЫ |
| CN103524431B (zh) * | 2013-09-24 | 2016-01-13 | 西安交通大学 | 3-苄基-4-喹唑啉酮类化合物及其合成方法和应用 |
| WO2015049667A1 (en) | 2013-10-03 | 2015-04-09 | Glaxosmithkline Intellectual Property (No.2) Limited | Novel compound as a diacylglycerol acyltransferase inhibitor |
| WO2015049668A1 (en) | 2013-10-03 | 2015-04-09 | Glaxosmithkline Intellectual Property (No.2) Limited | Novel compound as a diacylglycerol acyltransferase inhibitor |
| CN103880757B (zh) * | 2014-04-15 | 2016-02-24 | 上海毕得医药科技有限公司 | 一种5-羟基嘧啶-2-羧酸的合成方法 |
| WO2016181409A1 (en) | 2015-05-11 | 2016-11-17 | Cadila Healthcare Limited | Saroglitazar magnesium for the treatment of chylomicronemia syndrome - |
| US10385017B2 (en) | 2015-10-14 | 2019-08-20 | Cadila Healthcare Limited | Pyrrole compound, compositions and process for preparation thereof |
| CN105732461A (zh) * | 2016-02-03 | 2016-07-06 | 常州工程职业技术学院 | 5-甲氧基-6-卤代吲哚的制备方法 |
| CN106083707B (zh) * | 2016-06-01 | 2018-10-26 | 温州大学 | 一种非对称杂芳基硫醚的合成方法 |
| CN107619928B (zh) * | 2016-07-15 | 2020-08-07 | 中国科学院上海有机化学研究所 | 一种萃取组合物、萃取体系及其应用 |
| CN107619932B (zh) * | 2016-07-15 | 2020-08-07 | 中国科学院上海有机化学研究所 | 一种萃取组合物、萃取体系及其应用 |
| RU2706655C1 (ru) * | 2019-01-28 | 2019-11-19 | Акционерное общество "Гознак" (АО "Гознак") | Полимерсодержащее композиционное защищенное изделие |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090036425A1 (en) * | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| US20100204119A1 (en) * | 2009-02-02 | 2010-08-12 | Pfizer Inc | 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5h)-yl phenyl derivatives |
| US20100210622A1 (en) * | 2008-12-19 | 2010-08-19 | Jonathan Bayldon Baell | Heterocyclic compounds and methods of use |
| WO2010107765A1 (en) * | 2009-03-18 | 2010-09-23 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| US20100273768A1 (en) * | 2009-04-24 | 2010-10-28 | Nolan James Dewdney | Inhibitors of Bruton's Tyrosine Kinase |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2836669C (en) | 2011-05-20 | 2019-03-19 | Glaxosmithkline Intellectual Property (No.2) Limited | Compounds as diacylglycerol acyltransferase inhibitors |
| US9796729B2 (en) | 2012-11-23 | 2017-10-24 | Glaxosmithkline Llc | Compounds as diacylglycerol acyltransferase inhibitors |
-
2012
- 2012-05-18 CA CA2836669A patent/CA2836669C/en not_active Expired - Fee Related
- 2012-05-18 EA EA201391737A patent/EA023030B1/ru unknown
- 2012-05-18 EP EP12789931.8A patent/EP2710013B1/en active Active
- 2012-05-18 ES ES12789931.8T patent/ES2588748T3/es active Active
- 2012-05-18 MX MX2013013566A patent/MX346494B/es active IP Right Grant
- 2012-05-18 UA UAA201314878A patent/UA111360C2/uk unknown
- 2012-05-18 HR HRP20161089TT patent/HRP20161089T1/hr unknown
- 2012-05-18 PT PT127899318T patent/PT2710013T/pt unknown
- 2012-05-18 JP JP2014511575A patent/JP5844456B2/ja not_active Expired - Fee Related
- 2012-05-18 KR KR1020137033509A patent/KR101919080B1/ko not_active Expired - Fee Related
- 2012-05-18 ME MEP-2016-159A patent/ME02479B/me unknown
- 2012-05-18 HU HUE12789931A patent/HUE028870T2/en unknown
- 2012-05-18 MY MYPI2013702195A patent/MY184553A/en unknown
- 2012-05-18 PL PL12789931T patent/PL2710013T3/pl unknown
- 2012-05-18 DK DK12789931.8T patent/DK2710013T3/en active
- 2012-05-18 SG SG2013085501A patent/SG195044A1/en unknown
- 2012-05-18 US US14/118,976 patent/US8859536B2/en not_active Expired - Fee Related
- 2012-05-18 SI SI201230689A patent/SI2710013T1/sl unknown
- 2012-05-18 WO PCT/US2012/038523 patent/WO2012162129A1/en not_active Ceased
- 2012-05-18 PH PH1/2013/502401A patent/PH12013502401A1/en unknown
- 2012-05-18 RS RS20160648A patent/RS55006B1/sr unknown
- 2012-05-18 CN CN201280035792.5A patent/CN103703009B/zh not_active Expired - Fee Related
- 2012-05-18 AU AU2012259044A patent/AU2012259044B2/en not_active Ceased
- 2012-05-18 LT LTEP12789931.8T patent/LT2710013T/lt unknown
- 2012-05-18 BR BR112013029935-5A patent/BR112013029935B1/pt not_active IP Right Cessation
- 2012-05-18 PE PE2013002531A patent/PE20141204A1/es active IP Right Grant
-
2013
- 2013-11-18 IL IL229488A patent/IL229488A/en active IP Right Grant
- 2013-11-19 ZA ZA2013/08664A patent/ZA201308664B/en unknown
- 2013-11-20 CR CR20130602A patent/CR20130602A/es unknown
- 2013-11-20 CO CO13273126A patent/CO6811855A2/es active IP Right Grant
- 2013-11-20 DO DO2013000272A patent/DOP2013000272A/es unknown
- 2013-12-13 MA MA36566A patent/MA35185B1/fr unknown
-
2014
- 2014-09-05 US US14/478,309 patent/US9040517B2/en not_active Expired - Fee Related
-
2015
- 2015-04-24 US US14/695,206 patent/US9273069B2/en not_active Expired - Fee Related
-
2016
- 2016-01-15 US US14/996,318 patent/US9540400B2/en not_active Expired - Fee Related
- 2016-09-19 CY CY20161100926T patent/CY1118188T1/el unknown
- 2016-09-20 SM SM201600328T patent/SMT201600328B/it unknown
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090036425A1 (en) * | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| CN101772504A (zh) * | 2007-08-02 | 2010-07-07 | 辉瑞产品公司 | 经取代的双环内酰胺化合物 |
| US20100210622A1 (en) * | 2008-12-19 | 2010-08-19 | Jonathan Bayldon Baell | Heterocyclic compounds and methods of use |
| US20100204119A1 (en) * | 2009-02-02 | 2010-08-12 | Pfizer Inc | 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5h)-yl phenyl derivatives |
| WO2010107765A1 (en) * | 2009-03-18 | 2010-09-23 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| US20100273768A1 (en) * | 2009-04-24 | 2010-10-28 | Nolan James Dewdney | Inhibitors of Bruton's Tyrosine Kinase |
Non-Patent Citations (1)
| Title |
|---|
| Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1;Robert L. Dow,等;《ACS Medicinal Chemistry Letters》;20110518;第2卷(第5期);第407-412页，参见全文 * |
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| C14 | Grant of patent or utility model | ||
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| CF01 | Termination of patent right due to non-payment of annual fee |
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