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1.发明公开
公开(公告)号：EP0698015A1
公开(公告)日：1996-02-28
申请号：EP94917338.0
申请日：1994-05-10
发明人： MARSTERS, James, C., Jr. , BROWN, Michael, S. , CROWLEY, Craig, W. , GOLDSTEIN, Joseph, L. , JAMES, Guy, L. , McDOWELL, Robert, S. , OARE, David , RAWSON, Thomas, E. , REYNOLDS, Mark , SOMERS, Todd, G.
IPC分类号： A61K31 , A61P31 , A61P35 , C07D223 , C07D243 , C07D401 , C07D403 , C07D405 , C07D409 , C07D417 , C07D487 , C07D498 , C07D513 , C07K5 , A61K38
CPC分类号： C07D223/16 , A61K38/00 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027
摘要： Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.
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公开(公告)号：EP1144373B1
公开(公告)日：2005-10-19
申请号：EP00911572.6
申请日：2000-01-11
申请人： GENENTECH, INC.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：EP1628954A2
公开(公告)日：2006-03-01
申请号：EP04752854.2
申请日：2004-05-19
申请人： GENENTECH, INC.
IPC分类号： C07C307/06 , C07D307/79 , A61K31/325 , A61K31/343 , A61P7/02
CPC分类号： C07D307/79 , C07C307/06 , C07C311/51 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/86
摘要： Compounds having the general formula (I) are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有通式（I）的化合物可用于抑制丝氨酸蛋白酶，例如组织因子VIIa，因子Xa，凝血酶和激肽释放酶，并具有改善的渗透性。 这些化合物可以用于预防和/或治疗凝血障碍的方法中。
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公开(公告)号：EP0792289B1
公开(公告)日：2000-07-12
申请号：EP95940028.4
申请日：1995-11-16
申请人： GENENTECH, INC.
发明人： SOMERS, Todd, C. , ELIAS, Kathleen, A. , CLARK, Ross, G. , McDOWELL, Robert, S. , STANLEY, Mark, S. , BURNIER, John, P. , RAWSON, Thomas, E.
CPC分类号： C07D401/12 , A61K38/00 , C07D209/20 , C07D211/62 , C07D403/12 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06078 , C07K5/0812 , C07K5/1016 , C07K5/1024 , C07K7/06 , C07K14/60
摘要： The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound (1) of this invention is provided above.
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公开(公告)号：EP1144373A2
公开(公告)日：2001-10-17
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C317/00
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having structure (A) are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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公开(公告)号：EP1919920A2
公开(公告)日：2008-05-14
申请号：EP06813425.3
申请日：2006-08-14
发明人： RAWSON, Thomas, E. , SAFINA, Brian , DOTSON, Jennafer , ALIAGAS-MARTIN, Ignacio , HALLADAY, Jason , LIANG, Jun , RUETH, Matthias , ZHU, Bing-Yan , BROOKFIELD, Frederick , PRIME, Michael , ZHANG, Birong , LI, Jun, M. , Zhou, Aihe.
IPC分类号： C07D487/04 , C07D491/04 , A61K31/4155 , A61P35/00
CPC分类号： C07D487/04 , C07D491/04
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula: (I) wherein A, X, Y, Z, Ra, Rb, Rc, R1 , R2, R3 and m are defined herein.
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公开(公告)号：EP1330430A2
公开(公告)日：2003-07-30
申请号：EP01965996.0
申请日：2001-08-16
申请人： GENENTECH, INC.
发明人： ARTIS, Dean, R. , JACKSON, David, Y. , RAWSON, Thomas, E. , REYNOLDS, Mark, E. , SUTHERLIN, Daniel, P. , STANLEY, Mark, S.
IPC分类号： C07C237/22 , C07C237/20 , C07C233/81 , C07C233/75 , C07C237/04 , A61K31/40 , A61K31/216 , A61K31/196 , C07D207/16 , C07D207/48 , A61P19/02
CPC分类号： C07D403/12 , C07C233/25 , C07C233/60 , C07C233/81 , C07C237/04 , C07C237/20 , C07C237/22 , C07C2601/08 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/48 , C07D209/88 , C07D405/12
摘要： Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.
摘要翻译： 提供式（I）的化合物，其中A，Q，W，X，Y，Z，R 1至R 4，m和n如本文所定义。 本发明的化合物结合α4H整联蛋白受体，从而抑制α4A整联蛋白的配体结合，其可用于预防和/或治疗与 α4整联蛋白或其配体。
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公开(公告)号：EP1919920B1
公开(公告)日：2011-05-18
申请号：EP06813425.3
申请日：2006-08-14
发明人： RAWSON, Thomas, E. , SAFINA, Brian , DOTSON, Jennafer , ALIAGAS-MARTIN, Ignacio , HALLADAY, Jason , LIANG, Jun , RUETH, Matthias , ZHU, Bing-Yan , BROOKFIELD, Frederick , PRIME, Michael , ZHANG, Birong , LI, Jun, M. , Zhou, Aihe
IPC分类号： C07D487/04 , C07D491/04 , A61K31/4155 , A61P35/00
CPC分类号： C07D487/04 , C07D491/04
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula: (I) wherein A, X, Y, Z, Ra, Rb, Rc, R1 , R2, R3 and m are defined herein.
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公开(公告)号：EP1144373A3
公开(公告)日：2002-01-02
申请号：EP00911572.6
申请日：2000-01-11
申请人： Genentech, Inc.
发明人： ALIAGAS-MARTIN, Ignacio , ARTIS, Dean, R. , DINA, Michael, S. , FLYGARE, John, A. , GOLDSMITH, Richard, A. , MUNROE, Regina, A. , OLIVERO, Alan, G. , PASTOR, Richard , RAWSON, Thomas, E. , ROBARGE, Kirk, D. , SUTHERLIN, Daniel, P. , WEESE, Kenneth, J. , ZHOU, Aihe , ZHU, Yan
IPC分类号： C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
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公开(公告)号：EP0792289A1
公开(公告)日：1997-09-03
申请号：EP95940028.0
申请日：1995-11-16
申请人： GENENTECH, INC.
发明人： SOMERS, Todd, C. , ELIAS, Kathleen, A. , CLARK, Ross, G. , McDOWELL, Robert, S. , STANLEY, Mark, S. , BURNIER, John, P. , RAWSON, Thomas, E.
IPC分类号： C07D295 , A61K31 , A61K38 , A61P3 , A61P5 , C07D209 , C07D211 , C07D401 , C07D403 , C07K5 , C07K7 , C07K14
CPC分类号： C07D401/12 , A61K38/00 , C07D209/20 , C07D211/62 , C07D403/12 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06078 , C07K5/0812 , C07K5/1016 , C07K5/1024 , C07K7/06 , C07K14/60
摘要： The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound (1) of this invention is provided above.
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