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2. 发明申请

US20080287419A1 APOPTOSIS PROMOTERS 有权
标题翻译： APOPTOSIS促销者
公开(公告)号：US20080287419A1
公开(公告)日：2008-11-20
申请号：US12120914
申请日：2008-05-15
申请人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
发明人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
IPC分类号： A61K31/553 , C07D413/02 , A61K31/5377 , C07D223/02 , A61K31/496 , A61P35/00 , C07D295/00 , A61K31/55 , C07D267/02
CPC分类号： C07D295/155 , C07D487/08 , C07D491/08
摘要： Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
摘要翻译：公开了抑制抗凋亡家族蛋白成员的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达一种或多种抗凋亡家族蛋白质成员。

3. 发明授权

US5631401A Inhibitors of protein farnesyltransferase and squalene synthase 失效
标题翻译：蛋白质法呢基转移酶和角鲨烯合酶抑制剂
公开(公告)号：US5631401A
公开(公告)日：1997-05-20
申请号：US378334
申请日：1995-01-24
申请人： Herman H. Stein , William R. Baker , Anthony K. L. Fung , Saul H. Rosenberg , Todd W. Rockway , Stephen A. Fakhoury , David S. Garvey , B. Gregory Donner , William J. McClellan , Stephen J. O'Connor , Rajnandan Prasad , Wang Shen , Gerard M. Sullivan
发明人： Herman H. Stein , William R. Baker , Anthony K. L. Fung , Saul H. Rosenberg , Todd W. Rockway , Stephen A. Fakhoury , David S. Garvey , B. Gregory Donner , William J. McClellan , Stephen J. O'Connor , Rajnandan Prasad , Wang Shen , Gerard M. Sullivan
IPC分类号： C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C323/40 , C07D211/16 , C07D211/70 , C07D217/06 , C07D277/34 , C07D295/135 , C07D307/52 , C07D307/58 , C07D307/91 , C07D317/64 , C07D333/20 , C07D333/32 , C07C229/46 , A61K31/19 , A61K31/195
CPC分类号： C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C323/40 , C07D211/16 , C07D211/70 , C07D217/06 , C07D277/34 , C07D295/135 , C07D307/52 , C07D307/58 , C07D307/91 , C07D317/64 , C07D333/20 , C07D333/32 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
摘要翻译：本发明提供式IMA的化合物或其药学上可接受的盐，其可用于抑制蛋白法呢基转移酶和癌基因蛋白Ras的法呢基化或抑制从头角鲨烯生产导致胆固醇生物合成的抑制，除了可用于这些方法的中间体之外，本发明化合物的制备，药物组合物以及使用这些化合物的方法。

6. 发明申请

US20100298323A1 APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES 有权
标题翻译：用于治疗癌症和免疫和自发性疾病的病毒诱导剂
公开(公告)号：US20100298323A1
公开(公告)日：2010-11-25
申请号：US12793413
申请日：2010-06-03
申请人： Milan Bruncko , Yujia Dai , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Robert A. Mantei , William J. McClellan , Chang H. Park , Cheol-Min Park , Andrew M. Petros , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Todd M. Hansen
发明人： Milan Bruncko , Yujia Dai , Hong Ding , George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Aaron R. Kunzer , Robert A. Mantei , William J. McClellan , Chang H. Park , Cheol-Min Park , Andrew M. Petros , Xiaohong Song , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Todd M. Hansen
IPC分类号： A61K31/496 , C07D405/12 , C07D405/14 , C07D413/14 , C07D413/12 , C07D295/155 , C07D403/14 , C07D401/12 , C07D417/14 , A61K31/5377 , A61K31/495 , A61P35/00 , A61P35/02
CPC分类号： C07D213/76 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D211/06 , C07D211/58 , C07D213/74 , C07D213/84 , C07D231/56 , C07D235/06 , C07D277/24 , C07D295/14 , C07D295/30 , C07D309/04 , C07D309/32 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
摘要翻译：公开了抑制抗凋亡Bcl-2蛋白活性的化合物，含有化合物的组合物和治疗疾病的方法，其中表达抗凋亡Bcl-2蛋白。

7. 发明申请

US20100249133A1 APOPTOSIS PROMOTERS 有权
标题翻译： APOPTOSIS促销者
公开(公告)号：US20100249133A1
公开(公告)日：2010-09-30
申请号：US12772951
申请日：2010-05-03
申请人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
发明人： Milan Bruncko , Hong Ding , Steven W. Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol Min Park , Xiahong Song , Xilu Wang
IPC分类号： A61K31/496 , A61K31/4965 , A61K31/5377
CPC分类号： C07D295/155 , C07D487/08 , C07D491/08
摘要： Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
摘要翻译：公开了抑制抗凋亡家族蛋白成员的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达一种或多种抗凋亡家族蛋白质成员。

8. 发明授权

US4618683A Tetrahydro-6,7-dimethoxy-1H-benz[e]isoinodolines useful in the treatment of hypertension and as sedatives 失效
标题翻译：可用于治疗高血压和镇静剂的四氢-6,7-二甲氧基-1H-苯并[e]异壬醇
公开(公告)号：US4618683A
公开(公告)日：1986-10-21
申请号：US673458
申请日：1984-11-20
申请人： John F. DeBernardis , Daniel J. Kerkman , William J. McClellan
发明人： John F. DeBernardis , Daniel J. Kerkman , William J. McClellan
IPC分类号： C07D209/56 , C07D209/62 , C07D209/66 , C07D405/06 , C07D405/12 , C07D491/056 , C07D491/02 , A61K31/40
CPC分类号： C07D405/06 , C07C255/00 , C07D209/62 , C07D209/66
摘要： Disclosed herein are tetrahydro-benzo[e]isoindolines represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are independently selected from hydrogen, loweralkyl of 1 to 4 carbon atoms, hydroxy, loweralkoxy of 1 to 3 carbon atoms, allyloxy, benzyloxy, benzoyloxy, thiomethyl, halo, ##STR2## wherein t is 0 or 1, n is 0 to 5 and R.sub.11 and R.sub.14 are independently selected from hydrogen, halo, hydroxy, loweralkyl of 1 to 4 carbon atoms, loweralkoxy of 1 to 3 carbon atoms or amino; orR and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen and the proviso that two of R, R.sub.1, or R.sub.2 must be other than methoxy in the 7 and 8 positions when the remaining one of R, R.sub.1 or R.sub.2 is hydrogen; andR.sub.3 is hydrogen, loweralkyl of 1 to 4 carbon atoms, halo-substituted loweralkyl of 1 to 4 carbon atoms, amino-substituted loweralkyl of 1 to 4 carbon atoms, amino-substituted arylalkyl, allyl, thioloweralkyl, loweralkanol, or ##STR3## wherein R.sub.12 and R.sub.13 are independently selected from hydrogen, hydroxy, amino, loweralkoxy of 1 to 3 carbon atoms and s is 1 to 3; or ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.8 and R.sub.9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.8 and R.sub.9 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.10 is hydrogen, methoxy, amino, or halo; and the pharmaceutically acceptable salts thereof.
摘要翻译：本文公开的是由下式表示的四氢 - 苯并[e]异吲哚啉其中R 1，R 2和R 2独立地选自氢，1至4个碳原子的低级烷基，羟基，1至3个碳原子的低级烷氧基，烯丙氧基，苄氧基，苯甲酰氧基，硫代甲基，卤素，其中t为0或1，n为0至5，R 11和R 14独立地选自氢，卤素，羟基，1至4个碳原子的低级烷基，1至3碳的低级烷氧基原子或氨基; 或R和R 1，或R 1和R 2可以一起形成亚甲二氧基或亚乙二氧基桥; 条件是R，R 1或R 2中的至少一个必须不是氢，并且条件是R，R 1或R 2中的两个在7和8位中必须不同于甲氧基，当R，R 1或 R2是氢; R 3为氢，1至4个碳原子的低级烷基，1至4个碳原子的卤素取代的低级烷基，1至4个碳原子的氨基取代的低级烷基，氨基取代的芳基烷基，烯丙基，硫代低级烷基，低级链烷醇，其中R 12和R 13独立地选自氢，羟基，氨基，1至3个碳原子的低级烷氧基，s为1至3; 或其中m为0,1或2，p为0或1，R 7为氢或1至4个碳原子的低级烷基，R 8和R 9独立地选自氢，羟基，甲氧基，1至4碳的低级烷基原子或卤素，或R8和R9可以一起形成亚甲二氧基或亚乙二氧基桥; 或式“IMAGE”的1,4-苯并二恶烷，其中q为1,2或3，R 10为氢，甲氧基，氨基或卤素; 及其药学上可接受的盐。

9. 发明授权

US08084607B2 Apoptosis promoters 有权
公开(公告)号：US08084607B2
公开(公告)日：2011-12-27
申请号：US12390945
申请日：2009-02-23
申请人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol-min Park , Andrew M. Petros , Xiaohong Song , Noah P. Tu , Xilu Wang , Michael D. Wendt
发明人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron R. Kunzer , Christopher L. Lynch , William J. McClellan , Cheol-min Park , Andrew M. Petros , Xiaohong Song , Noah P. Tu , Xilu Wang , Michael D. Wendt
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07D277/74 , C04B35/632 , C07C323/25 , C07C2601/16 , C07D205/04 , C07D207/16 , C07D211/46 , C07D211/60 , C07D211/74 , C07D213/70 , C07D213/75 , C07D233/06 , C07D233/84 , C07D239/06 , C07D263/58 , C07D277/36 , C07D295/13 , C07D295/192 , C07D307/64 , C07D335/02 , C07D401/12 , C07D403/04 , C07D409/12 , C07D487/04 , C07D487/08
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

10. 发明授权

US07754886B2 N-acylsulfonamide apoptosis promoters 失效
标题翻译： N-酰基磺酰胺凋亡启动子
公开(公告)号：US07754886B2
公开(公告)日：2010-07-13
申请号：US12364987
申请日：2009-02-03
申请人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人： David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号： C07C211/00 , A61K31/445
CPC分类号： C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要： N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译：具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂，可用于促进凋亡。还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。

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