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1. 发明申请

WO2012069948A1 4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS 审中-公开
标题翻译： 4-（5-氰基 - 吡咯-1-基） - 哌啶衍生物作为GPR 119调节剂
公开(公告)号：WO2012069948A1
公开(公告)日：2012-05-31
申请号：PCT/IB2011/054996
申请日：2011-11-09
申请人： PFIZER INC. , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
发明人： MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
IPC分类号： C07D401/04 , C07D401/14 , C07D403/14 , A61K31/454 , A61K31/506 , A61P3/10
CPC分类号： C07D401/04 , C07D401/14 , C07D403/14
摘要： Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPR119的活性的化合物及其用于治疗与动物中G-蛋白偶联受体GPR119的调节相关的疾病的用途。

2. 发明申请

WO2011114271A1 2,3 DIHYDRO-1H-INDEN-1-YL- 2,7-DIAZASPIRO [3.6] NONANE DERIVATIVES AND THEIR USE AS ANTAGONISTS OR INVERSE AGONISTS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译： 2,3-二氢-1H-茚-1-基-2,7-二氮杂萘[3.6]壬烷衍生物及其作为GHRELIN受体的拮抗剂或逆反应物的用途
公开(公告)号：WO2011114271A1
公开(公告)日：2011-09-22
申请号：PCT/IB2011/051035
申请日：2011-03-11
申请人： PFIZER INC. , BHATTACHARYA, Samit Kumar , CAMERON, Kimberly O'Keefe , FERNANDO, Dilinie Prasadhini , KUNG, Daniel Wei-Shung , LONDREGAN, Allyn Timothy , MCCLURE, Kim Francis , SIMILA, Suvi Tuula Marjukka
发明人： BHATTACHARYA, Samit Kumar , CAMERON, Kimberly O'Keefe , FERNANDO, Dilinie Prasadhini , KUNG, Daniel Wei-Shung , LONDREGAN, Allyn Timothy , MCCLURE, Kim Francis , SIMILA, Suvi Tuula Marjukka
IPC分类号： C07D471/10 , C07D519/00 , A61K31/4747 , A61P3/04 , A61P3/10
CPC分类号： C07D471/10 , A61K31/435 , A61K31/497 , A61K31/506 , A61K31/53 , A61K45/06 , C07D491/056 , C07D513/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R 1 , R 2 , Ra, L, Z, Z 1 and Z 2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
摘要翻译：本发明提供了作为Ghrelin拮抗剂或反向激动剂的式（I）化合物或其药学上可接受的盐，其中R1，R2，Ra，L，Z，Z1和Z2如本文所定义。其药物组合物; 以及治疗由Ghrelin受体的拮抗作用介导的疾病，病症或病症的方法。

3. 发明申请

WO2011061679A1 IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS 审中-公开
标题翻译：作为GPR119抑制剂的咪唑并吡唑
公开(公告)号：WO2011061679A1
公开(公告)日：2011-05-26
申请号：PCT/IB2010/055194
申请日：2010-11-16
申请人： PFIZER INC. , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton
发明人： MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton
IPC分类号： C07D487/04 , A61K31/506
CPC分类号： C07D487/04
摘要： Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R 1 is -C(O)-O-R 3 or R 2 is hydrogen, cyano, C 1 -C 6 alkyl, or C 3 -C 6 cycloalkyl; R 5 is hydrogen, cyano, nitro, C 1 -C 6 fluoroalkyl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 fluoroalkoxy, or C 3 -C 6 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, -C(O)-NH 2 , or C 1 -C 6 alkyl substituted with hydroxy or C 1 - C 6 alkoxy; m is 1 or 2, wherein when m is 1 then R 8 is hydrogen, C 1 -C 6 alkyl, -CH 2 -(C 1 - C 5 )haloalkyl, C 3 -C 6 cycloalkyl, or C 1 -C 6 alkyl substituted with hydroxy; and when m is 2 then each R 8 is independently C 1 -C 3 alkyl or -CH 2 -(C 1 -C 2 )haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G- protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：式（I）化合物，其中：X为（A）或（B）; Y是O或键; R 1是-C（O）-O-R 3或R 2是氢，氰基，C 1 -C 6烷基或C 3 -C 6环烷基; R5是氢，氰基，硝基，C1-C6氟代烷基，C1-C6烷基，C1-C6烷氧基，C1-C6氟烷氧基或C3-C6环烷基; R 6是氢，C 1 -C 6烷基，C 3 -C 6环烷基，-C（O）-NH 2或被羟基或C 1 -C 6烷氧基取代的C 1 -C 6烷基; m为1或2，其中当m为1时，R 8为氢，C 1 -C 6烷基，-CH 2 - （C 1 -C 5）卤代烷基，C 3 -C 6环烷基或被羟基取代的C 1 -C 6烷基; 当m为2时，各R 8独立地为C 1 -C 3烷基或-CH 2 - （C 1 -C 2）卤代烷基; 调节G蛋白偶联受体GPR119的活性及其用于治疗与动物中G-蛋白偶联受体GPR119的调节相关的疾病。

4. 发明申请

WO2010106457A3 3-OXA-7-AZABICYCLO[3.3.1]NONANES 审中-公开
标题翻译： 3-氧杂-7-氮杂双环[3.3.1]壬烷
公开(公告)号：WO2010106457A3
公开(公告)日：2010-11-18
申请号：PCT/IB2010050945
申请日：2010-03-04
申请人： PFIZER , DENINNO MICHAEL PAUL , FUTATSUGI KENTARO , LEFKER BRUCE ALLEN , MASCITTI VINCENT , MCCLURE KIM FRANCIS , MUNCHHOF MICHAEL JOHN
发明人： DENINNO MICHAEL PAUL , FUTATSUGI KENTARO , LEFKER BRUCE ALLEN , MASCITTI VINCENT , MCCLURE KIM FRANCIS , MUNCHHOF MICHAEL JOHN
IPC分类号： C07D491/08 , A61K31/407
CPC分类号： C07D491/08 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G蛋白偶联受体GPR119的活性的式（I）化合物及其在治疗与动物中G蛋白偶联受体GPR119的调节有关的疾病中的用途。

5. 发明申请

WO2004020440A1 DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS 审中-公开
标题翻译： DI和三氟乙酸吡啶类抗炎化合物
公开(公告)号：WO2004020440A1
公开(公告)日：2004-03-11
申请号：PCT/IB2003/003847
申请日：2003-08-19
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
发明人： DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula (I) wherein R 1 is fluoro; s is an integer from two to three; R 2 is (C 3 -C 6 )cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C l -C 4 )alkyl, hydroxy, (C l -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C=O)-0-; or R 2 is (C l -C 6 )alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, hydroxy, (C 1 -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式（I）的新的三唑并 - 吡啶，其中R 1是氟; s是从2到3的整数; R 2是任选被一个或两个独立地选自卤素，（C 1 -C 4）烷基，羟基，（C 1 -C 4）烷基的部分取代的（C 3 -C 6）环烷基（C 1 -C 6）烷基 - （C = O）-O-;（C 1 -C 6）烷基 - （C = O）或R 2是任选被一个或两个独立地选自以下的部分取代的（C 1 -C 6）烷基：卤素，（C 1 -C 6）烷基，羟基，（C 1 -C 6）（C 1 -C 6）烷基 - （C = O）-O-;（C 1 -C 6）烷基 - （C = O）条件是所述式（I）化合物不能是6- [4-（2,4-二氟 - 苯基） - 恶唑-5-基] -3-异丙基 - [1,2,4]三唑并[4,5- 3-a]吡啶; 或6- [4-（3,4-二氟 - 苯基） - 恶唑-5-基] -3-异丙基 - [1,2,4]三唑并[4,3-a]吡啶; 制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

6. 发明申请

WO2004099129A3 INTERMEDIATES USEFUL IN THE SYNTHESIS OF HIV-PROTEASE INHIBITORS AND METHODS FOR PREPARING THE SAME 审中-公开
标题翻译：用于合成HIV-蛋白酶抑制剂的中间体及其制备方法
公开(公告)号：WO2004099129A3
公开(公告)日：2005-01-13
申请号：PCT/IB2004001380
申请日：2004-04-28
申请人： PFIZER , ALBIZATI KIM FRANCIS , BABU SRINIVASAN
发明人： ALBIZATI KIM FRANCIS , BABU SRINIVASAN
IPC分类号： C07C319/20 , C07C323/20 , C07C323/25 , C07C323/43 , C07D209/48 , C07D217/26 , C07D303/36 , C07C323/31 , C07C323/32 , C07D217/00 , C07D317/46
CPC分类号： C07D209/48 , C07B2200/07 , C07C319/20 , C07C323/25 , C07C323/43 , C07D217/26 , C07D303/36
摘要： Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed (Formula I).
摘要翻译：公开了用于合成HIV-蛋白酶抑制剂的光学活性3-氨基 - 丁烯和1,2-二羟基-3-氨基 - 丁烷中间体化合物和制备这些中间体化合物的方法（式I）。

7. 发明申请

WO2011036576A1 GPR 119 MODULATORS 审中-公开
标题翻译： GPR 119调制器
公开(公告)号：WO2011036576A1
公开(公告)日：2011-03-31
申请号：PCT/IB2010/053347
申请日：2010-07-22
申请人： PFIZER INC. , GUIMARAES, Cristiano Ruch Werneck , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
发明人： GUIMARAES, Cristiano Ruch Werneck , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
IPC分类号： C07D487/04 , C07D519/00 , A61K31/439 , A61P3/10
CPC分类号： C07D487/04 , A61K31/4965 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/55 , A61K31/566 , A61K31/7036 , A61K31/706 , A61K38/164 , A61K38/17 , A61K38/2264 , A61K38/26 , A61K45/06 , C07D491/08 , C07D519/00
摘要： Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPR119的活性的式（I）化合物及其在治疗与动物中G蛋白偶联受体GPR119的调节相关的疾病中的用途。

8. 发明申请

WO2010128425A1 GPR 119 MODULATORS 审中-公开
标题翻译： GPR 119调制器
公开(公告)号：WO2010128425A1
公开(公告)日：2010-11-11
申请号：PCT/IB2010/051834
申请日：2010-04-27
申请人： PFIZER INC. , DAROUT, Etzer , DENINNO, Michael Paul , FUTATSUGI, Kentaro , GUIMARAES, Cristiano Ruch Werneck , LEFKER, Bruce Allen , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
发明人： DAROUT, Etzer , DENINNO, Michael Paul , FUTATSUGI, Kentaro , GUIMARAES, Cristiano Ruch Werneck , LEFKER, Bruce Allen , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John , ROBINSON, Ralph Pelton, Jr.
IPC分类号： C07D401/14 , C07D471/04 , C07D491/08 , A61K31/497 , A61P3/10
CPC分类号： C07D401/14 , C07D471/04 , C07D491/08
摘要： Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR1 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPR119的活性的式（I）化合物及其用于治疗与动物中G-蛋白偶联受体GPR119的调节相关的疾病的用途。

9. 发明申请

WO2010128414A1 GPR 119 MODULATORS 审中-公开
标题翻译： GPR 119调制器
公开(公告)号：WO2010128414A1
公开(公告)日：2010-11-11
申请号：PCT/IB2010/051567
申请日：2010-04-12
申请人： PFIZER INC. , DAROUT, Etzer , DENINNO, Michael, Paul , FUTATSUGI, Kentaro , GUIMARAES, Cristiano, Ruch, Werneck , LEFKER, Bruce, Allen , MASCITTI, Vincent , MCCLURE, Kim, Francis , MUNCHHOF, Michael, John , ROBINSON, Ralph, Pelton, Jr.
发明人： DAROUT, Etzer , DENINNO, Michael, Paul , FUTATSUGI, Kentaro , GUIMARAES, Cristiano, Ruch, Werneck , LEFKER, Bruce, Allen , MASCITTI, Vincent , MCCLURE, Kim, Francis , MUNCHHOF, Michael, John , ROBINSON, Ralph, Pelton, Jr.
IPC分类号： C07D401/14 , C07D471/04 , C07D491/08 , A61K31/497 , A61P3/10
CPC分类号： C07D471/04 , C07D401/14 , C07D491/08
摘要： Compounds of Formula (I) that modulate the activity of the G -protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPFM 19的活性的式（I）化合物及其在治疗与动物中G-蛋白偶联受体GPR119的调节相关的疾病中的用途。

10. 发明申请

WO2010106457A2 3-OXA-7-AZABICYCLO[3.3.1]NONANES 审中-公开
标题翻译： 3-氧杂-7-氮杂双环[3.3.1]壬烷
公开(公告)号：WO2010106457A2
公开(公告)日：2010-09-23
申请号：PCT/IB2010/050945
申请日：2010-03-04
申请人： PFIZER INC. , DENINNO, Michael Paul , FUTATSUGI, Kentaro , LEFKER, Bruce Allen , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John
发明人： DENINNO, Michael Paul , FUTATSUGI, Kentaro , LEFKER, Bruce Allen , MASCITTI, Vincent , MCCLURE, Kim Francis , MUNCHHOF, Michael John
IPC分类号： C07D491/08
CPC分类号： C07D491/08 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
摘要翻译：本文描述了调节G-蛋白偶联受体GPR119的活性的式（I）化合物及其在治疗与动物中G蛋白偶联受体GPR119的调节相关的疾病中的用途。

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