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1. 发明申请

WO2004004652A2 MITOTIC KINESIN BINDING SITE 审中-公开
公开(公告)号：WO2004004652A2
公开(公告)日：2004-01-15
申请号：PCT/US2003/021145
申请日：2003-07-03
申请人： MERCK & CO., INC. , BUSER-DOEPNER, Carolyn, A. , COLEMAN, Paul, J. , COX, Christopher, D. , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HARTMAN, George, D. , HEIMBROOK, David, C. , KUO, Lawrence, C. , HUBER, Hans, E. , SARDANA, Vinod, V. , TORRENT, Maricel , YAN, Youwei
发明人： BUSER-DOEPNER, Carolyn, A. , COLEMAN, Paul, J. , COX, Christopher, D. , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HARTMAN, George, D. , HEIMBROOK, David, C. , KUO, Lawrence, C. , HUBER, Hans, E. , SARDANA, Vinod, V. , TORRENT, Maricel , YAN, Youwei
IPC分类号： A61K
CPC分类号： C07K14/47 , C07K2299/00 , C12N9/14 , G01N33/6803 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention is directed to the identification, characterization and three-dimensional structure of a novel ligand binding site of KSP. Binding of ligands to the novel binding site result in a conformational change in the three-dimensional structure of the protein and a modulation of the activity of KSP. This conformational change in turn results in the formation of a novel binding pocket in the KSP protein, which comprises the novel binding site of the instant invention.
摘要翻译：本发明涉及KSP新型配体结合位点的鉴定，表征和三维结构。配体与新结合位点的结合导致蛋白质三维结构的构象变化和KSP活性的调节。这种构象变化又导致在KSP蛋白质中形成新的结合口袋，其包含本发明的新结合位点。

2. 发明公开

EP0906099A1 A METHOD OF TREATING CANCER 失效
标题翻译：一种治疗癌症的方法
公开(公告)号：EP0906099A1
公开(公告)日：1999-04-07
申请号：EP97921085.0
申请日：1997-03-31
申请人： MERCK & CO., INC.
发明人： HEIMBROOK, David, C. , OLIFF, Allen, I. , STIRDIVANT, Steven, M.
IPC分类号： A61K45 , A61K31 , A61K38 , A61P35
CPC分类号： A61K38/05 , A61K31/4439 , A61K31/496
摘要： The present invention relates to a method of treating cancer which comprises administering to a mammalian patient a compound which inhibits Raf and a compound which inhibits farnesyl protein transferase.
摘要翻译：本发明涉及治疗癌症的方法，其包括向哺乳动物患者施用抑制Raf的化合物和抑制法尼基蛋白转移酶的化合物。

3. 发明公开

EP1019529A1 A METHOD OF TREATING CANCER 审中-公开
标题翻译：一种治疗癌症的方法
公开(公告)号：EP1019529A1
公开(公告)日：2000-07-19
申请号：EP98941069.1
申请日：1998-08-26
申请人： MERCK & CO., INC.
发明人： HEIMBROOK, David, C. , DeFEO-JONES, Deborah , OLIFF, Allen, I. , STIRDIVANT, Steven, M.
IPC分类号： C12Q1/48 , C12N9/10 , A01N43/00 , A01N43/40 , A01N43/50 , A61K31/55 , A61K31/415 , A61K31/445
CPC分类号： A61K31/00 , C12Q1/48 , G01N33/5011
摘要： The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is an inhibitor of cellular processing of the H-Ras and K4B-Ras proteins. The invention in particular provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The instant invention als provides for a method of identifying such a compound, the method comprising an assay whose readout is a consequence of the biological activity or inhibition of that activity of the Ras protein, thus providing convenient identification of compounds that inhibit cellular processing of the H-Ras and K4B-Ras proteins.
摘要翻译：本发明提供了一种抑制异戊二烯基蛋白转移酶并治疗癌症的方法，该方法包括给予哺乳动物异戊二烯基 - 蛋白转移酶抑制剂，该抑制剂是H-Ras和K4B-Ras蛋白细胞加工的抑制剂。本发明特别提供了通过施用作为那些异戊二烯基蛋白转移酶的双重抑制剂的化合物来抑制法尼基蛋白转移酶和香叶基香叶基蛋白转移酶I型的方法。本发明还提供了一种鉴定这种化合物的方法，该方法包括一种检测方法，该方法的读数是Ras蛋白质的该活性的生物活性或抑制作用的结果，因此提供了方便鉴定抑制细胞加工 H-Ras和K4B-Ras蛋白。

4. 发明公开

EP1009854A1 A METHOD OF TREATING CANCER 审中-公开
标题翻译：用于癌症的治疗方法
公开(公告)号：EP1009854A1
公开(公告)日：2000-06-21
申请号：EP98944537.4
申请日：1998-08-26
申请人： MERCK & CO., INC.
发明人： BARNETT, Stanley, F. , HEIMBROOK, David, C. , HUBER, Hans, E. , PATRICK, Denis, R.
IPC分类号： C12Q1/48 , C12N9/10 , A01N43/40 , A01N43/50 , A01N43/62 , A61K31/55 , A61K31/415 , A61K31/445
CPC分类号： G01N33/5011 , A61K31/00 , A61K31/4174 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/5513 , A61K38/005 , A61K38/05 , C12N9/99 , C12Q1/48
摘要： The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-protein transferase type I (GGTase-I). The invention also provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The invention also provides for a method of identifying such a compound, the method comprising a modified inhibitory assay that incorporates a modulator anion that alters the in vitro potency of prenyl-protein transferase inhibitors in a way that predicts their potency in vivo, thus providing convenient identification of compounds that possess such in vivo activity.

5. 发明公开

EP0973396A1 A METHOD OF TREATING CANCER 失效
标题翻译：方法治疗癌症的
公开(公告)号：EP0973396A1
公开(公告)日：2000-01-26
申请号：EP98915318.4
申请日：1998-04-06
申请人： MERCK & CO., INC.
发明人： DUGGAN, Mark, E. , HARTMAN, George, D. , HEIMBROOK, David, C. , OLIFF, Allen, I.
IPC分类号： A01N43/42 , A01N43/60 , A61K31/445 , A61K31/495
CPC分类号： A61K31/472 , A61K31/195 , A61K31/223 , A61K31/365 , A61K31/4164 , A61K31/4184 , A61K31/425 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505
摘要： The present invention relates to methods of treating cancer using a combination of a compound which is an integrin antagonist and a compound which is an inhibitor of farnesyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is an integrin antagonist and a compound which is an inhibitor of farnesyl-protein transferase. The invention also relates to methods of preparing such compositions.

6. 发明公开

EP1551962A2 MITOTIC KINESIN BINDING SITE 审中-公开
标题翻译：丝分裂驱动蛋白结合位点
公开(公告)号：EP1551962A2
公开(公告)日：2005-07-13
申请号：EP03763258.5
申请日：2003-07-03
申请人： Merck & Co., Inc.
发明人： BUSER-DOEPNER, Carolyn, A. , COLEMAN, Paul, J. , COX, Christopher, D. , FRALEY, Mark, E. , GARBACCIO, Robert, M. , HARTMAN, George, D. , HEIMBROOK, David, C. , KUO, Lawrence, C. , HUBER, Hans, E. , SARDANA, Vinod, V. , TORRENT, Maricel , YAN, Youwei
IPC分类号： C12N9/00
CPC分类号： C07K14/47 , C07K2299/00 , C12N9/14 , G01N33/6803 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention is directed to the identification, characterization and three-dimensional structure of a novel ligand binding site of KSP. Binding of ligands to the novel binding site result in a conformational change in the three-dimensional structure of the protein and a modulation of the activity of KSP. This conformational change in turn results in the formation of a novel binding pocket in the KSP protein, which comprises the novel binding site of the instant invention.

7. 发明公开

EP0934270A1 A METHOD OF TREATING CANCER 失效
标题翻译：用于癌症的治疗方法
公开(公告)号：EP0934270A1
公开(公告)日：1999-08-11
申请号：EP97927776.0
申请日：1997-05-27
申请人： MERCK & CO., INC.
发明人： HEIMBROOK, David, C. , OLIFF, Allen, I. , STIRDIVANT, Steven, M.
IPC分类号： A61K31 , A61K38 , A61K45 , A61P35 , C07D207 , C07D233 , C07D311 , C07D401 , C07D403
CPC分类号： C07D233/64 , A61K31/00 , A61K31/216 , A61K31/352 , A61K31/40 , A61K31/4025 , A61K31/4174 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/495 , A61K31/496 , C07D207/09 , C07D207/28 , C07D311/30 , C07D401/12 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to a method of treating cancer which comprises administering to a mammalian patient a compound which inhibits MEK and a compound which inhibits farnesyl protein transferase.

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