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1. 发明公开

EP2190827A1 N-BENZYL, N' -ARYLCARBONYLPIPERAZINE DERIVATIVES AS LXR MODULATORS 失效转让
标题翻译：作为LXR调节剂的N-苄基，N'-二月桂基哌嗪衍生物
公开(公告)号：EP2190827A1
公开(公告)日：2010-06-02
申请号：EP08787281.8
申请日：2008-08-18
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： HO, Koc-Kan , ROUGHTON, Andrew Laird , NEAGU, Irina , CHAN, Jui-Hsiang , ANSARI, Nasrin , MORRIS, Michelle Lee , RONG, Yajing , OHLMEYER, Michael , COOKE, Andrew John , EDWARDS, Andrew Stanley , BENNETT, David, Jonathan
IPC分类号： C07D241/04 , C07D243/08 , C07D261/14 , C07D307/14 , C07D307/52 , C07D307/66 , C07D309/14 , C07D317/58 , C07D333/20 , C07D333/48 , C07D295/192 , A61K31/4965 , A61K31/497 , A61P9/10
CPC分类号： C07D295/192 , C07D207/09 , C07D207/27 , C07D213/40 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/36 , C07D241/26 , C07D241/28 , C07D243/08 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/28 , C07D277/48 , C07D285/135 , C07D295/155 , C07D295/205 , C07D295/215 , C07D307/14 , C07D307/52 , C07D307/66 , C07D307/79 , C07D309/14 , C07D333/20 , C07D333/48
摘要： The present invention relates to N-benzyl,N' -arylcarbonylpiperazine derivatives having the general Formula (I) to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N' -arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
摘要翻译：本发明涉及具有通式（I）的N-苄基，N'-芳基羰基哌嗪衍生物和包含其的药物组合物，并涉及这些N-苄基，N'-芳基羰基哌嗪衍生物在制备药物中的用途用于治疗或预防与胆固醇和胆汁酸转运和代谢有关的动脉粥样硬化和相关疾病。

2. 发明授权

EP2185530B1 5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS 有权
标题翻译： 5-苯基 - 异恶唑-3-甲酰胺衍生物作为TRPV1调节剂
公开(公告)号：EP2185530B1
公开(公告)日：2011-09-14
申请号：EP08786712.3
申请日：2008-07-31
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
IPC分类号： C07D261/14 , A61K31/4155 , A61P25/00 , A61P29/00
CPC分类号： C07D413/12 , C07D261/18
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

3. 发明公开

EP2185530A1 5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS 有权
标题翻译： 5-苯基 - 异恶唑-3-甲酰胺衍生物作为TRPV1调节剂
公开(公告)号：EP2185530A1
公开(公告)日：2010-05-19
申请号：EP08786712.3
申请日：2008-07-31
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
IPC分类号： C07D261/14 , A61K31/4155 , A61P25/00 , A61P29/00
CPC分类号： C07D413/12 , C07D261/18
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

4. 发明公开

EP2152708A1 PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：嘌呤和1H-咪唑并吡啶酮作为PKC-THETA抑制剂
公开(公告)号：EP2152708A1
公开(公告)日：2010-02-17
申请号：EP07797679.3
申请日：2007-05-23
申请人： Pharmacopeia, LLC
发明人： ROUGHTEN, Andrew , RONG, Yajing , HO, Koc Kan , OHLMEYER, Michael , DILLER, David
IPC分类号： C07D471/04 , C07D473/00 , C07D487/04 , A61K31/522 , A61P37/06
CPC分类号： C07D471/04 , C07D473/00 , C07D473/32 , C07D487/04
摘要： A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCΘ inhibitors, and their methods of use are disclosed. The genus is represented by the formula (I). A representative example is: (II).
摘要翻译：公开了可用作PKCθ抑制剂的嘌呤酮和1H-咪唑并吡啶酮的化学属及其使用方法。该属由式（I）表示。一个代表性的例子是：（II）。

5. 发明公开

EP2318368A1 1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES 有权转让
标题翻译： 1-（4-脲基苯甲酰基）哌嗪衍生物
公开(公告)号：EP2318368A1
公开(公告)日：2011-05-11
申请号：EP09791938.5
申请日：2009-08-26
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： COOKE, Andrew, John , BENNETT, David, Jonathan , EDWARDS, Andrew Stanley , ROUGHTON, Andrew Laird , NEAGU, Irina , CHAN, Jui-Hsiang , HO, Koc-Kan , ANSARI, Nasrin , MORRIS, Michelle Lee , RONG, Yajing , OHLMEYER, Michael
IPC分类号： C07D213/56 , C07D263/34 , C07D307/68 , C07D333/38 , A61P9/10 , A61K31/496
CPC分类号： C07D263/34 , C07D213/56 , C07D277/56 , C07D307/68 , C07D333/38
摘要： The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R
1 is (C
1-8 )alkyl, (C
3-8 )cycloalkyl or (C
3-8 )cycloalkyl(C
1-3 )alkyl, each of which may be substituted by hydroxy, cyano or halogen; R
2 represents 1 or 2 optional halogens; R
3 is (C
1-6 )alkyl, (C
3-6 )cycloalkyl or (C
3-6 )cycloalkyl(C
1-3 )alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5-or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
摘要翻译：本发明涉及具有通式I的1-（4-脲基苯甲酰基）哌嗪衍生物（我们引起您的注意，在该电子版中没有提供式I，因为它在该论文摘要中提供）其中R 1 是各自可被羟基，氰基或卤素取代的（C 1-8）烷基，（C 3-8）环烷基或（C 3-8）环烷基（C 1-3）烷基; R 2代表1或2个任选的卤素; R 3是可以被一个或多个卤素取代的（C 1-6）烷基，（C 3-6）环烷基或（C 3-6）环烷基（C 1-3）烷基; A表示包含1-3个选自N，O和S的杂原子的杂芳基环系统，当X是C时，该环系统是5-或6-元，并且当X是N时是5-元; n是1或2; 或其药学上可接受的盐; 涉及包含它们的药物组合物，并涉及这些1-（4-脲基苯甲酰基）哌嗪衍生物在制备用于治疗或预防与胆固醇和胆汁酸转运和代谢相关的动脉粥样硬化和相关病症的药物中的用途。

6. 发明授权

EP2318368B1 1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES 有权转让
标题翻译： 1-（4-脲基苯甲酰基）哌嗪衍生物
公开(公告)号：EP2318368B1
公开(公告)日：2013-10-16
申请号：EP09791938.5
申请日：2009-08-26
申请人： Merck Sharp & Dohme B.V. , Pharmacopeia, LLC
发明人： COOKE, Andrew, John , BENNETT, David, Jonathan , EDWARDS, Andrew Stanley , ROUGHTON, Andrew Laird , NEAGU, Irina , CHAN, Jui-Hsiang , HO, Koc-Kan , ANSARI, Nasrin , MORRIS, Michelle Lee , RONG, Yajing , OHLMEYER, Michael
IPC分类号： C07D213/56 , C07D263/34 , C07D307/68 , C07D333/38 , A61P9/10 , A61K31/496
CPC分类号： C07D263/34 , C07D213/56 , C07D277/56 , C07D307/68 , C07D333/38

7. 发明授权

EP2190827B1 N-BENZYL-N'-ARYLCARBONYLPIPERAZINE DERIVATIVES AS LXR MODULATORS 失效转让
标题翻译：作为LXR调节剂的N-苄基-N'-芳基羰基哌嗪衍生物
公开(公告)号：EP2190827B1
公开(公告)日：2011-01-12
申请号：EP08787281.8
申请日：2008-08-18
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： HO, Koc-Kan , ROUGHTON, Andrew Laird , NEAGU, Irina , CHAN, Jui-Hsiang , ANSARI, Nasrin , MORRIS, Michelle Lee , RONG, Yajing , OHLMEYER, Michael , COOKE, Andrew John , EDWARDS, Andrew Stanley , BENNETT, David, Jonathan
IPC分类号： C07D241/04 , C07D243/08 , C07D261/14 , C07D307/14 , C07D307/52 , C07D307/66 , C07D309/14 , C07D317/58 , C07D333/20 , C07D333/48 , C07D295/192 , A61K31/4965 , A61K31/497 , A61P9/10
CPC分类号： C07D295/192 , C07D207/09 , C07D207/27 , C07D213/40 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/36 , C07D241/26 , C07D241/28 , C07D243/08 , C07D261/08 , C07D261/14 , C07D261/18 , C07D277/28 , C07D277/48 , C07D285/135 , C07D295/155 , C07D295/205 , C07D295/215 , C07D307/14 , C07D307/52 , C07D307/66 , C07D307/79 , C07D309/14 , C07D333/20 , C07D333/48
摘要： The present invention relates to N-benzyl,N' -arylcarbonylpiperazine derivatives having the general Formula (I) to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N' -arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
摘要翻译：本发明涉及具有通式（I）的N-苄基，N'-芳基羰基哌嗪衍生物和包含其的药物组合物，并涉及这些N-苄基，N'-芳基羰基哌嗪衍生物在制备药物中的用途用于治疗或预防与胆固醇和胆汁酸转运和代谢有关的动脉粥样硬化和相关疾病。

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