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1. 发明申请

US20140315916A1 MACROCYCLES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF 有权
标题翻译：增加p53活性及其用途的MACROCYCLES
公开(公告)号：US20140315916A1
公开(公告)日：2014-10-23
申请号：US14354303
申请日：2012-10-23
申请人： Latha G. Nair , Stephane L. Bogen , Ronald J. Doll , Yao Ma , Yuan Tian
发明人： Latha G. Nair , Stephane L. Bogen , Ronald J. Doll , Yao Ma , Yuan Tian
IPC分类号： C07D498/14
CPC分类号： C07D498/14 , C07D409/14
摘要： The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译：本发明提供式（1）的化合物：如本文所述或其药学上可接受的盐或溶剂化物。该化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

2. 发明授权

US08859776B2 Substituted piperidines that increase p53 activity and the uses thereof 有权
标题翻译：增加p53活性的替代哌啶及其用途
公开(公告)号：US08859776B2
公开(公告)日：2014-10-14
申请号：US13501685
申请日：2010-10-05
申请人： Stephane L. Bogen , Yao Ma , Yaolin Wang , Brian Robert Lahue , Latha G. Nair , Manami Shizuka , Matthew Ernst Voss , Margarita Kirova-Snover , Weidong Pan , Yuan Tian , Bheemashankar A. Kulkarni , Craig R. Gibeau , Yuan Liu , Giovanna Scapin , Diane Rindgen , Ronald J. Doll , Timothy J. Guzi , Danny J. Hicklin , Amin Nomeir , Gerald W. Shipps, Jr. , Malcolm MacCoss
发明人： Stephane L. Bogen , Yao Ma , Yaolin Wang , Brian Robert Lahue , Latha G. Nair , Manami Shizuka , Matthew Ernst Voss , Margarita Kirova-Snover , Weidong Pan , Yuan Tian , Bheemashankar A. Kulkarni , Craig R. Gibeau , Yuan Liu , Giovanna Scapin , Diane Rindgen , Ronald J. Doll , Timothy J. Guzi , Danny J. Hicklin , Amin Nomeir , Gerald W. Shipps, Jr. , Malcolm MacCoss
IPC分类号： C07D401/00 , A01N43/40 , C07D401/14 , C07D409/14
CPC分类号： C07D401/14 , C07D409/14
摘要： The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译：本发明提供本文所述的式1的化合物或其药学上可接受的盐，溶剂合物或酯。该化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

3. 发明申请

US20120208844A1 SUBSTITUTED PIPERIDINES THAT INCREASE P53 ACTIVITY AND THE USES THEREOF 有权
标题翻译：增加P53活性的替代品PIPERIDIN及其用途
公开(公告)号：US20120208844A1
公开(公告)日：2012-08-16
申请号：US13501685
申请日：2010-10-05
申请人： Stephane L. Bogen , Yao Ma , Yaolin Wang , Brian Robert Lahue , Latha G. Nair , Manami Shizuka , Matthew Ernst Voss , Margarita Kirova-Snover , Weidong Pan , Yuan Tian , Bheemashankar A. Kulkarni , Craig R. Gibeau , Yuan Liu , Giovanna Scapin , Diane Rindgen , Ronald J. Doll , Timothy J. Guzi , Danny J. Hicklin , Amin Nomeir , Cynthia Seidel-Dugan , Gerald W. Shipps, JR. , Malcolm MacCoss
发明人： Stephane L. Bogen , Yao Ma , Yaolin Wang , Brian Robert Lahue , Latha G. Nair , Manami Shizuka , Matthew Ernst Voss , Margarita Kirova-Snover , Weidong Pan , Yuan Tian , Bheemashankar A. Kulkarni , Craig R. Gibeau , Yuan Liu , Giovanna Scapin , Diane Rindgen , Ronald J. Doll , Timothy J. Guzi , Danny J. Hicklin , Amin Nomeir , Cynthia Seidel-Dugan , Gerald W. Shipps, JR. , Malcolm MacCoss
IPC分类号： A61K31/4545 , A61P35/02 , A61P35/00 , C07D409/14 , C07D401/14
CPC分类号： C07D401/14 , C07D409/14
摘要： The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译：本发明提供本文所述的式（1）化合物或其药学上可接受的盐，溶剂合物或酯。该化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

4. 发明授权

US08987274B2 Macrocycles that increase p53 activity and the uses thereof 有权
标题翻译：增加p53活性的大环化合物及其用途
公开(公告)号：US08987274B2
公开(公告)日：2015-03-24
申请号：US14354303
申请日：2012-10-23
申请人： Latha G. Nair , Stephane L. Bogen , Ronald J. Doll , Yao Ma , Yuan Tian
发明人： Latha G. Nair , Stephane L. Bogen , Ronald J. Doll , Yao Ma , Yuan Tian
IPC分类号： A61K31/497 , C07D498/14 , C07D409/14
CPC分类号： C07D498/14 , C07D409/14
摘要： The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译：本发明提供式（1）的化合物：如本文所述或其药学上可接受的盐或溶剂化物。该化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

5. 发明授权

US07884107B2 Substituted piperidines that increase P53 activity and the uses thereof 有权
标题翻译：增加P53活性的替代哌啶及其用途
公开(公告)号：US07884107B2
公开(公告)日：2011-02-08
申请号：US11769030
申请日：2007-06-27
申请人： Yao Ma , Brian Robert Lahue , Gerald W. Shipps, Jr. , Yaolin Wang , Stephane L. Bogen , Matthew Ernst Voss , Latha G. Nair , Yuan Tian , Ronald J. Doll , Zhuyan Guo , Corey O. Strickland , Rumin Zhang , Mark A. McCoy , Weidong Pan , Elise M. Siegel , Craig R. Gibeau
发明人： Yao Ma , Brian Robert Lahue , Gerald W. Shipps, Jr. , Yaolin Wang , Stephane L. Bogen , Matthew Ernst Voss , Latha G. Nair , Yuan Tian , Ronald J. Doll , Zhuyan Guo , Corey O. Strickland , Rumin Zhang , Mark A. McCoy , Weidong Pan , Elise M. Siegel , Craig R. Gibeau
IPC分类号： A61K31/54 , C07D413/00 , C07D403/00 , C07D405/00
CPC分类号： C07D409/14 , C07D401/06 , C07D401/14
摘要： In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明公开了作为HDM2蛋白的制备方法的抑制剂的新型化合物，包括一种或多种这样的化合物的药物组合物，治疗，预防，抑制与HDM2蛋白相关的一种或多种疾病的方法或P53使用这些化合物或药物组合物。

6. 发明申请

US20150329548A1 SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS 有权
标题翻译：取代的吡咯烷酮作为HDM2抑制剂
公开(公告)号：US20150329548A1
公开(公告)日：2015-11-19
申请号：US14652466
申请日：2013-12-18
申请人： Michelle MACHACEK , B. Wesley TROTTER , Christopher DISNMORE , Francesc Xavier FRADERA LLINAS , Amit Ashokrao KUDALE , Michael Hale REUTERSHAN , Christopher Francis THOMPSON , Liping YANG , Michael D. ALTMAN , Stephane L. BOGEN , Ronald J. DOLL , Matthew E. VOSS , MERCH SHARP & DOHME CORP.
发明人： Christopher Dinsmore , Francesc Xavier Fradera Llinas , Amit Ashokro Kudale , Michelle Machacek , Michael Hale Reutershan , Christopher Francis Thompason , B. Wesley Trotter , Liping Yang , Michael D. Altman , Stephane L. Bogen , Ronald J. Doll , Matthew E. Voss
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译：本发明提供如本文所述的取代吡咯并嘧啶或其药学上可接受的盐或溶剂化物。代表性化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

7. 发明授权

US07452902B2 Imidazopyridines as cyclin dependent kinase inhibitors 有权
标题翻译：咪唑并吡啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07452902B2
公开(公告)日：2008-11-18
申请号：US11238597
申请日：2005-09-29
申请人： Michael P. Dwyer , Timothy J. Guzi , Kamil Paruch , Ronald J. Doll , Kartik M. Keertikar , Viyyoor M. Girijavallabhan
发明人： Michael P. Dwyer , Timothy J. Guzi , Kamil Paruch , Ronald J. Doll , Kartik M. Keertikar , Viyyoor M. Girijavallabhan
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compounds as inhibitors of cyclin dependent kinases, 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 CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

8. 发明授权

US07275995B2 Adjustable guard for protecting coupling connection between rotating shafts 有权
标题翻译：可调节防护罩，用于保护旋转轴之间的联接连接
公开(公告)号：US07275995B2
公开(公告)日：2007-10-02
申请号：US10430963
申请日：2003-05-06
申请人： Ronald J. Doll
发明人： Ronald J. Doll
IPC分类号： F16D3/84
CPC分类号： F16P1/02
摘要： An injection molded plastic guard is used to enclose a coupling connection between a prime mover input shaft and a driven output shaft. The guard is comprised of two halves that are hinged together with a stainless steel pin at one end. The coupling is centered within the guard with the hinge being positioned above the coupling. The halves extend from the hinge to distal ends that are pivoted about the pin to surround and enclose the coupling. The distal ends meet underneath the coupling area and are mounted to a non-rotating base. Sleeves extend outwardly from opposing ends of the guard to surround the input and output shafts and abut against the prime mover and output device equipment. The sleeves have a vertically, elongated opening so that one guard can be used to cover many different base-to-shaft heights. Further, the length of the sleeves can be adjusted to accommodate different centerline-of-guard to equipment face distances. End caps are used when these distances are too great or if the equipment face is such that it does not abut appropriately against the respective sleeve. A shaft opening is cut into the end caps at the appropriate base-to-shaft height.
摘要翻译：使用注射成型的塑料防护罩封装原动机输入轴和从动输出轴之间的联接连接。防护罩由两端铰接在一起的不锈钢销钉组成。联轴器在防护罩内居中，铰链位于联轴器上方。一半从铰链延伸到远端，围绕销枢转以围绕并包围联接器。远端在耦合区域下方相遇，并安装在非旋转底座上。套管从护罩的相对端向外延伸，以围绕输入和输出轴并抵靠原动机和输出装置设备。袖子有一个垂直细长的开口，所以一个防护罩可以用来覆盖许多不同的底座到轴的高度。此外，袖子的长度可以被调节以适应不同的中心线到设备面距离。当这些距离太大或者设备面不能适当地抵靠相应的套筒时，使用端盖。在适当的基轴至轴高度处，将轴孔切割成端盖。

9. 发明授权

US06919341B2 Imidazopyrazines as cyclin dependent kinase inhibitors 有权
标题翻译：咪唑吡嗪作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US06919341B2
公开(公告)日：2005-07-19
申请号：US10665005
申请日：2003-09-19
申请人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams
发明人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams
IPC分类号： A61P35/00 , C07D487/04 , A61K31/495
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, 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 CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡嗪化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

10. 发明授权

US06426352B1 Sulfonamide inhibitors of farnesyl-protein transferase 失效
标题翻译：法呢基蛋白转移酶的磺酰胺抑制剂
公开(公告)号：US06426352B1
公开(公告)日：2002-07-30
申请号：US09374390
申请日：1999-08-13
申请人： F. George Njoroge , Bancha Vibulbhan , Arthur G. Taveras , Ronald J. Doll , Viyyoor M. Girijavallabhan
发明人： F. George Njoroge , Bancha Vibulbhan , Arthur G. Taveras , Ronald J. Doll , Viyyoor M. Girijavallabhan
IPC分类号： A61K31435
CPC分类号： C07D401/04 , C07D221/16 , C07D401/14 , C07D413/14
摘要： Novel tricyclic sulfonamide compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel sulfonamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.
摘要翻译：公开了新的三环磺酰胺化合物和药物组合物，其是酶的抑制剂，法呢基蛋白转移酶。还公开了抑制Ras功能并因此抑制细胞异常生长的方法。该方法包括将新的磺酰胺化合物施用于生物系统。特别地，该方法抑制哺乳动物如人的细胞的异常生长。

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