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公开(公告)号：EP2473491A1
公开(公告)日：2012-07-11
申请号：EP10722268.9
申请日：2010-06-01
发明人： NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan , NEELAMKAVIL, Santhosh , SHAH, Unmesh, G.
IPC分类号： C07D265/32 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/12 , C07D265/32 , C07D413/04 , C07D413/14
摘要： The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译： 本发明提供具有式（I）的化合物或其药学上可接受的盐或溶剂化物，包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝血或纤维化改变的方法。
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公开(公告)号：EP2373634A1
公开(公告)日：2011-10-12
申请号：EP09768572.1
申请日：2009-12-03
发明人： NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan
IPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/04 , A61K31/4725 , A61K31/54 , A61K31/553 , A61K31/5355 , A61P7/00
CPC分类号： C07D401/12 , C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译： 本发明提供如本文所述的式（I）化合物或其药学上可接受的盐或溶剂合物。 本发明还提供了包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。
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公开(公告)号：EP2373634B1
公开(公告)日：2015-11-11
申请号：EP09768572.1
申请日：2009-12-03
发明人： NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan
IPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/04 , A61K31/4725 , A61K31/54 , A61K31/553 , A61K31/5355 , A61P7/00
CPC分类号： C07D401/12 , C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D413/12 , C07D413/14 , C07D417/04
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公开(公告)号：EP2473491B1
公开(公告)日：2013-07-17
申请号：EP10722268.9
申请日：2010-06-01
发明人： NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan , NEELAMKAVIL, Santhosh , SHAH, Unmesh, G.
IPC分类号： C07D265/32 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/12 , C07D265/32 , C07D413/04 , C07D413/14
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5.发明公开NOVEL PYRROLIDINES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权吡咯烷ALS胰高血糖素受体拮抗剂，其组合物及使用方法
公开(公告)号：EP2480077A1
公开(公告)日：2012-08-01
申请号：EP10819272.5
申请日：2010-09-16
申请人： Schering Corporation
发明人： GILBERT, Eric, J. , MILLER, Michael, W. , DEMONG, Duane Eugene , STAMFORD, Andrew, W. , GREENLEE, William, J.
CPC分类号： A61K31/40 , C07D207/08 , C07D207/09 , C07D207/48 , C07D207/50
摘要： The present invention relates to compounds of the general formula: (I) wherein ring B, R
1, R
2 , R
3 , Z, and L
1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.-
公开(公告)号：EP2352731A1
公开(公告)日：2011-08-10
申请号：EP09753287.3
申请日：2009-11-05
申请人： Schering Corporation
发明人： ZHU, Zhaoning , GREENLEE, William, J. , GALLO, Gioconda, V. , LI, Hongmei , MANDAL, Mihirbaran , MCCRACKEN, Troy , BENNETT, Chad, E. , BURNETT, Duane, A
IPC分类号： C07D403/10 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/20 , C07D498/04 , C07D498/20 , C07D513/04 , C07F7/10 , A61K31/53 , A61P25/28
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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7.发明公开SPIRO-IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS 有权SPIRO-IMIDAZOLONDERIVATE ALS GLUCAGONREZEPTORANTAGONISTEN
公开(公告)号：EP2350020A1
公开(公告)日：2011-08-03
申请号：EP09741076.5
申请日：2009-09-30
申请人： Schering Corporation
发明人： STAMFORD, Andrew , MILLER, Michael, W. , DEMONG, Duane, Eugene , GREENLEE, William, J. , KOZLOWSKI, Joseph, A. , LAVEY, Brian, J. , WONG, Michael, K.C. , YU, Wensheng , DAI, Xing , YANG, De-Yi , ZHOU, Guowei
IPC分类号： C07D235/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K31/4184 , A61K31/4188 , A61K31/4439 , A61K31/4453 , A61K31/47
CPC分类号： C07D235/02 , A61K31/4184 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/12 , C07D491/10 , A61K2300/00
摘要： The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R
1 , R
3 , Z, L
1 , and L
2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.-
8.发明公开GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权葛兰素史克公司，ZUSAMMENSETZUNGEN UND VERFAHREN ZU IHRER VERWENDUNG
公开(公告)号：EP2291358A1
公开(公告)日：2011-03-09
申请号：EP09747426.6
申请日：2009-05-13
申请人： Schering Corporation
IPC分类号： C07D231/22 , C07D231/38 , A61K31/415
CPC分类号： C07D231/22 , C07D231/38
摘要： The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译： 本发明涉及通式（I）的化合物，其中环A，环B，R 1，R 2，R 3，Z和L 1彼此独立地并且如本文所定义，与包含该化合物的组合物和方法 使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之相关的病症。
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公开(公告)号：EP2155737A1
公开(公告)日：2010-02-24
申请号：EP08767575.7
申请日：2008-05-05
申请人： Schering Corporation
发明人： ZHU, Zhaoning , GREENLEE, William, J. , SUN, Zhong-yue , GALLO, Gioconda , ASBEROM, Theodros , HUANG, Xianhai , ZHU, Xiaohong , MCBRIAR, Mark, D. , PISSARNITSKI, Dmitri, A. , ZHAO, Zhiqiang , XU, Ruo , LI, Hongmei , PALANI, Anandan , MAZZOLA, Robert, D., Jr. , CLADER, John , JOSIEN, Hubert , QIN, Jun , VOIGT, Johannes, H.
IPC分类号： C07D413/10 , C07D413/14 , C07D498/04 , C07D498/10 , C07D498/20 , A61K31/4245 , A61P25/00 , A61P25/28
CPC分类号： C07D413/10 , C07D413/14 , C07D498/04 , C07D498/10 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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公开(公告)号：EP2097387A2
公开(公告)日：2009-09-09
申请号：EP08714220.4
申请日：2008-02-20
发明人： ZHU, Zhaoning , MCKITTRICK, Brian , SUN, Zhong-Yue , YE, Yuanzan, C. , VOIGT, Johannes, H. , STRICKLAND, Corey , SMITH, Elizabeth, M. , STAMFORD, Andrew , GREENLEE, William, J. , MAZZOLA, JR., Robert, D. , CALDWELL, John , CUMMING, Jared, N. , WANG, Lingyan , WU, Yusheng , ISERLOH, Ulrich , LIU, Xiaoxiang , HUANG, Ying , LI, Guoqing , PAN, Jianping , MISIASZEK, Jeffrey, A. , GUO, Tao , LE, Thuy X. H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C. , MORRIS, Michelle, L. , GU, Huizhong , QIAN, Gang , TADESSE, Dawit , LAI, Gaifa , DUO, Jingqi , QU, Chuanxing , SHAO, Yuefei
IPC分类号： C07D233/88 , C07D239/22 , C07D401/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14 , C07D495/10 , C07D401/10 , C07D417/10 , A61K31/513 , A61P25/28
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- or -C(=N(R5))-; X is -O-, -N(R5)- or -C(R6)(R7)-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O)2-, -C(=O)- or -C(=NR5)-; U is a bond, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, U is not -S(O)-, -S(O)2-, -O-, or -N(R5)-; provided that when X is -N(R5)- and W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
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