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91. 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。

92. 发明授权

US07271174B2 Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases 失效
标题翻译：用于抑制G蛋白功能的三环酰胺的代谢物和治疗增殖性疾病的方法
公开(公告)号：US07271174B2
公开(公告)日：2007-09-18
申请号：US10874556
申请日：2004-06-23
申请人： Swapan K. Chowdhury , Anima Ghosal , Robert M. Iannucci , Wenqing Feng , Tze-Ming Chan , Shmuel Zbaida , Kevin B. Alton , Ronald J. Doll , Keith P. Minor
发明人： Swapan K. Chowdhury , Anima Ghosal , Robert M. Iannucci , Wenqing Feng , Tze-Ming Chan , Shmuel Zbaida , Kevin B. Alton , Ronald J. Doll , Keith P. Minor
IPC分类号： C07D221/06 , A61K31/435
CPC分类号： C07D401/14
摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.
摘要翻译：本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶使用新型化合物。

93. 发明授权

US06241618B1 Adjustable rotating shaft guard 有权
标题翻译：可调式转轴防护罩
公开(公告)号：US06241618B1
公开(公告)日：2001-06-05
申请号：US09439513
申请日：1999-11-12
申请人： Ronald J. Doll
发明人： Ronald J. Doll
IPC分类号： F16C126
CPC分类号： F16P1/02 , Y10T74/2191
摘要： An adjustable rotating shaft guard includes a base, a first guard half, and a second guard half. A bottom of the first and second guard halves are retained by the base such that they contact each other to fully cover a rotating shaft or coupler. A half sleeve preferably extends outward from at least one end of the first and second guard halves. Preferably, the top of each guard half is fastened to each other. The first and second guard halves are preferably fabricated from a high impact plastic. The bottom area of the first and second guard halves preferably have a plurality of cutting lines which provide a reference for sawing to a specific height. The half sleeves also have a plurality of cutting lines which provide a reference for sawing to a specific length. In a second embodiment, an adjustable rotating shaft guard includes a first sleeve guard half, a second sleeve guard half and two sets of two end cap halves. Each pair of end cap halves are attached to each end of the first and second sleeve guard halves. One or both ends of the first and second sleeve halves may be supported by an adjustable leg set. One or both ends of the first and second sleeve guard halves may be supported by a mounting plate.
摘要翻译：可调节的转轴防护罩包括底座，第一护罩半部和第二护罩半部。第一和第二保护半部的底部由基座保持，使得它们彼此接触以完全覆盖旋转轴或联接器。半套管优选地从第一和第二保护半部的至少一端向外延伸。优选地，每个护罩半部的顶部彼此紧固。第一和第二保护半部优选地由高冲击塑料制成。第一和第二保护半部的底部区域优选地具有多个切割线，其提供用于锯切到特定高度的参考。半套还具有多条切割线，其提供用于锯切到特定长度的参考。在第二实施例中，可调节的旋转轴防护件包括第一套筒保护罩半部，第二套筒防护件半部和两组两个端盖半部。每对端帽半部分连接到第一和第二套筒保护半部的每个端部。第一和第二套筒半部的一端或两端可以由可调腿部支撑。第一和第二套筒保护半部的一端或两端可由安装板支撑。

94. 发明授权

US4879309A Mercapto-acylamino acids as antihypertensives 失效
标题翻译：巯基 - 酰氨基酸作为抗高血压药
公开(公告)号：US4879309A
公开(公告)日：1989-11-07
申请号：US304881
申请日：1989-01-30
申请人： Ronald J. Doll , Bernard R. Neustadt
发明人： Ronald J. Doll , Bernard R. Neustadt
IPC分类号： C07C323/60 , C07C327/22 , C07C327/26 , C07D213/82
CPC分类号： C07D213/82 , C07C323/60 , C07C327/22 , C07C327/26
摘要： Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.

95. 发明授权

US07608643B2 Compounds for inhibiting KSP kinesin activity 失效
标题翻译：用于抑制KSP驱动蛋白活性的化合物
公开(公告)号：US07608643B2
公开(公告)日：2009-10-27
申请号：US11370005
申请日：2006-03-07
申请人： Ronald J. Doll , Ronald Herbst , Wolfgang Seghezzi , Emma M. Lees , William F. Estacio
发明人： Ronald J. Doll , Ronald Herbst , Wolfgang Seghezzi , Emma M. Lees , William F. Estacio
IPC分类号： A01N35/04 , A61K31/541 , A01N43/90 , A61K31/519 , A61K31/12 , C07D419/04 , C07D417/00
CPC分类号： A61K31/4743 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂合物：本发明提供了包含这些化合物的组合物，其可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病或病症并抑制KSP驱动蛋白活性。

96. 发明授权

US06440974B2 Compounds useful for inhibition of farnesyl protein transferase 失效
标题翻译：可用于抑制法呢基蛋白转移酶的化合物
公开(公告)号：US06440974B2
公开(公告)日：2002-08-27
申请号：US09788947
申请日：2001-02-20
申请人： Ronald J. Doll , Carmen Alvarez , Tarik Lalwani , Yi-Tsung Liu
发明人： Ronald J. Doll , Carmen Alvarez , Tarik Lalwani , Yi-Tsung Liu
IPC分类号： A61K31496
CPC分类号： C07D401/04 , C07D221/16 , C07D405/14 , C07D409/14
摘要： Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译：公开了新的式的化合物。在式1.0中，a表示N或NO，R 1和R 3是卤素，R 2和R 4独立地是H或卤素，条件是至少一个是H，X是C，CH或N，T代表五或六元杂环烷基环，其具有选自S或O的一个或两个杂原子。还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。

97. 发明授权

US06277854B1 Tricyclic antitumor farnesyl protein transferase inhibitors 失效
标题翻译：三环抗肿瘤法尼基蛋白转移酶抑制剂
公开(公告)号：US06277854B1
公开(公告)日：2001-08-21
申请号：US09352895
申请日：1999-07-13
申请人： F. George Njoroge , Ronald J. Doll , Stacy W. Remiszewski
发明人： F. George Njoroge , Ronald J. Doll , Stacy W. Remiszewski
IPC分类号： A61K31496
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, R8, Y, A, B, X, a, b, c, d, v, and w are as described herein. The compounds of formula (1.0) are useful for inhibiting tumor growth.
摘要翻译：本发明涉及式R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，Y，A，B，X，a，b，c，d，v和w如本文所述的化合物。式（1.0）的化合物可用于抑制肿瘤生长。

98. 发明授权

US06211193B1 Compounds useful for inhibition of farnesyl protein transferase 失效
标题翻译：可用于抑制法呢基蛋白转移酶的化合物
公开(公告)号：US06211193B1
公开(公告)日：2001-04-03
申请号：US09094720
申请日：1998-06-15
申请人： Stacy W. Remiszewski , Ronald J. Doll , Carmen Alvarez , Tarik Lalwani
发明人： Stacy W. Remiszewski , Ronald J. Doll , Carmen Alvarez , Tarik Lalwani
IPC分类号： A61K314545
CPC分类号： C07D401/04 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D491/10 , C07D495/10
摘要： Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and R represents a cycloalkyl or a heterocycloalkyl ring that is substitued. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译：公开了新的式的化合物。在式1.0中，a表示N或NO，R 1和R 3为卤素，R 2和R 4独立地为H或卤素，条件是至少一个为H，X为C，CH或N，R为环烷基或杂环烷基环，还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。

99. 发明授权

US5925639A Keto amide derivatives useful as farnesyl protein transferase inhibitors 失效
标题翻译：可用作法呢基蛋白转移酶抑制剂的酮酰胺衍生物
公开(公告)号：US5925639A
公开(公告)日：1999-07-20
申请号：US877677
申请日：1997-06-17
申请人： Ronald J. Doll , Tarik Lalwani , Carmen Alvarez
发明人： Ronald J. Doll , Tarik Lalwani , Carmen Alvarez
IPC分类号： A61K31/4427 , A61K31/4545 , A61K31/496 , A61P35/00 , C07D221/16 , C07D401/04 , A61K31/44 , A61K31/495 , C07D401/12
CPC分类号： C07D401/04
摘要： Compounds of the following formula useful for inhibiting Ras function and therefore inhibiting or treating the abnormal growth of cells are disclosed: ##STR1## or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, wherein:R and R.sup.2 are halo;R.sup.1 and R.sup.3 are H and halo, provided that at least one of R.sup.1 and R.sup.3 is H;X is N, CH or C, when the double bond is present at the C-11 position;R.sup.4 is=O, --NHOH, --N.dbd.NHR.sup.6, --N.dbd.NHSO.sub.2 R.sup.6, --N.dbd.NHCOR.sup.6, --N.dbd.NHCONH.sub.2, --N.dbd.NHCOCONH.sub.2, (H, OH), (H, --OR.sup.6), (H, --OCOR.sup.6), (H, OSO.sub.2 R.sup.6) or --E--(CH.sub.2).sub.n1 --G--, wherein n.sub.1 is 1 to 5, and E and G are O, S or N, and are joined to the same carbon to form a cyclic structure;R.sup.5 is H, lower alkyl, or optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or heterocycloalkyl-alkyl;R.sup.6 is lower alkyl or optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or heterocycloalkyl-alkyl;R.sup.7, R.sup.8 and R.sup.9 are independently selected from the group consisting of H, lower alkyl, aryl, and aralkyl; andn is 0-5.
摘要翻译：公开了可用于抑制Ras功能并因此抑制或治疗细胞异常生长的下式的化合物：其N-氧化物或其药学上可接受的盐或溶剂合物，其中：R和R 2为卤素; R1和R3是H和卤素，条件是R1和R3中的至少一个是H; 当C-11位存在双键时，X为N，CH或C; R4是= O，-NHOH，-N = NHR6，-N = NHSO2R6，-N = NHCOR6，-N = NHCONH2，-N = NHCOCONH2，（H，OH），（H，-OR6），（H， OCOR 6），（H，OSO 2 R 6）或-E-（CH 2）n1-G-，其中n1为1至5，并且E和G为O，S或N，并且与相同的碳连接以形成环状结构 ; R5是H，低级烷基或任选取代的芳基，杂芳基，芳烷基，杂芳烷基或杂环烷基 - 烷基; R 6是低级烷基或任选取代的芳基，杂芳基，芳烷基，杂芳烷基或杂环烷基 - 烷基; R 7，R 8和R 9独立地选自H，低级烷基，芳基和芳烷基; n为0-5。

100. 发明授权

US5714609A Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases 失效
标题翻译：可用于抑制G蛋白功能和治疗增殖性疾病的三环酰胺和尿素化合物
公开(公告)号：US5714609A
公开(公告)日：1998-02-03
申请号：US450064
申请日：1995-05-25
申请人： Ronald J. Doll , F. George Njoroge , Stacy W. Remiszewski
发明人： Ronald J. Doll , F. George Njoroge , Stacy W. Remiszewski
IPC分类号： A61K31/4427 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/54 , A61P35/00 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D521/00 , C07D401/08 , C07D403/08
CPC分类号： C07D231/12 , A61K31/444 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , C07D221/16 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
摘要翻译：公开了抑制Ras功能并因此抑制细胞异常生长的方法。该方法包括向生物系统施用式1.0化合物：（IMAGE）（1.0）。特别地，该方法抑制哺乳动物例如人的细胞的异常生长。公开了新的式5.0,5.1和5.2的化合物，其中R是-C（R 20）（R 21）（R 46），和5.3,5.3A和5.3B，其中R是-N（R 25）（R 48）。还公开了制备式5.0,5.1,5.2和5.3的3-取代的化合物的方法。进一步公开的是在制备式5.0,5.1,5.2和5.3的3-取代化合物的方法中的中间体的新化合物。

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