专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US06291684B1 Process for the preparation of aziridinyl epothilones from oxiranyl epothilones 有权
公开(公告)号：US06291684B1
公开(公告)日：2001-09-18
申请号：US09528230
申请日：2000-03-17
申请人： Robert M. Borzilleri , Soong-Hoon Kim , Alicia Regueiro-Ren , Gregory D. Vite
发明人： Robert M. Borzilleri , Soong-Hoon Kim , Alicia Regueiro-Ren , Gregory D. Vite
IPC分类号： C07D20326
CPC分类号： C07D491/04
摘要： The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.

12. 再颁专利

USRE41895E1 Epothilone derivatives 有权
公开(公告)号：USRE41895E1
公开(公告)日：2010-10-26
申请号：US12539496
申请日：2009-08-11
申请人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri , James A. Johnson
发明人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri , James A. Johnson
IPC分类号： C07D493/04 , C07D491/04 , C07D413/04 , A61K31/4184 , A61K31/423 , A61P35/00
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

13. 发明授权

US07253283B2 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的三环调节剂及其用途
公开(公告)号：US07253283B2
公开(公告)日：2007-08-07
申请号：US11035176
申请日：2005-01-13
申请人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： C07D417/02 , C07D413/02 , A61K31/473
CPC分类号： C07D417/12 , A23K20/168 , A23K50/40 , C07D233/88 , C07D277/46 , C07D405/12 , C07D453/06
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或其药学上可接受的盐，其中B，J，K，Z，R，R a，R b，R b， >，R“，R”，“O”，m和n如本文所定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

14. 发明授权

US06602883B1 Inhibitors of farnesyl protein transferase 失效
公开(公告)号：US06602883B1
公开(公告)日：2003-08-05
申请号：US09566396
申请日：2000-05-05
申请人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
发明人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D403/06 , C07D403/12 , C07D409/14
摘要： Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

15. 发明授权

US06387926B1 Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US06387926B1
公开(公告)日：2002-05-14
申请号：US09087179
申请日：1998-05-29
申请人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
发明人： Rajeev S. Bhide , Charles Z. Ding , John T. Hunt , Soong-Hoon Kim , Katerina Leftheris
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D403/06 , C07D403/12 , C07D409/14
摘要： Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.
摘要翻译：公开了抑制法尼基蛋白转移酶（FTase）和致癌蛋白Ras的法呢基化的喹啉和苯并氮杂衍生物。因此，这些化合物可用作抗癌剂。所述化合物还可用于治疗除癌症以外的疾病。

16. 发明授权

US6011029A Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US6011029A
公开(公告)日：2000-01-04
申请号：US802329
申请日：1997-02-20
申请人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
发明人： Charles Z. Ding , Soong-Hoon Kim , John T. Hunt , Toomas Mitt , Rajeev Bhide , Katerina Leftheris
IPC分类号： C07D401/14 , A61K31/00 , A61K31/35 , A61K31/4178 , A61K31/495 , A61K31/498 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/675 , A61P35/00 , A61P43/00 , C07D20060101 , C07D243/14 , C07D245/06 , C07D401/04 , C07D401/10 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/044 , C07D491/048 , C07D495/04 , C07D497/04 , C07D513/04 , C07F9/645 , C07D243/24
CPC分类号： C07D243/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
摘要： The present invention comprises benzodiazepine compounds having farnesyl transferase inhibitory activity.
摘要翻译：本发明包括具有法呢基转移酶抑制活性的苯并二氮杂类化合物。

17. 发明授权

US07544808B2 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-κB活性的三环调节剂及其用途
公开(公告)号：US07544808B2
公开(公告)日：2009-06-09
申请号：US11773506
申请日：2007-07-05
申请人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David S. Weinstein , John L. Gilmore , James Sheppeck , Bingwei Vera Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： C07D277/20 , A61K31/425
CPC分类号： C07D417/12 , A23K20/168 , A23K50/40 , C07D233/88 , C07D277/46 , C07D405/12 , C07D453/06
摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
摘要翻译：提供了新的非甾体化合物，其可用于治疗与糖皮质激素受体，AP-1和/或NF-κB活性的调节相关的疾病，包括肥胖，糖尿病，炎症和免疫疾病，并且具有式（I ）或其立体异构体或前药或其药学上可接受的盐，其中B，J，K，Z，R，Ra，Rb，Rc，Rd，Rq，Rw，m和n在本文中定义。还提供了治疗肥胖症，糖尿病和包含所述化合物的炎性或免疫相关疾病的药物组合物和方法。

18. 发明申请

US20070255055A1 EPOTHILONE DERIVATIVES 有权
公开(公告)号：US20070255055A1
公开(公告)日：2007-11-01
申请号：US11763636
申请日：2007-06-15
申请人： Gregory Vite , Soong-Hoon Kim , Robert Borzilleri , James Johnson
发明人： Gregory Vite , Soong-Hoon Kim , Robert Borzilleri , James Johnson
IPC分类号： C07D225/02
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of the formula Q is selected from the group consisting of G is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo, W is O or NR15; X is O or H,H; Y is selected from the group consisting of O; H,OR16; OR17,OR17; NOR18; H,NOR19; H,NR20R21; H,H; or CHR22; OR17OR17 can be a cyclic ketal; Z1 and Z2 are selected from the group consisting of CH2, O, NR23, S, or SO2, wherein only one of Z and Z2 is a heteroatom; B1 and B2 are selected from the group consisting of OR24, or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H they can form a six-membered ring ketal or acetal; D is selected from the group consisting of NR28R29, NR30COR31 or saturated heterocycle; R1, R2, R3, R4, R5, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26, and R27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R1 and R2 are alkyl can be joined to form a cycloalkyl; R3 and R4 are alkyl can be joined to form a cycloalkyl; R9, R10, R16, R17, R24, R25, and R31 are selected from the group H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33, and R30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; R15, R23 and R29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C═O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein W and X are both O; and R1, R2, R7, are H; and R3, R4, R6, are methyl; and R8, is H or methyl; and Z1, and Z2, are CH2; and G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and Q is as defined above are excluded.

19. 发明授权

US07125899B2 Epothilone derivatives 有权
标题翻译：埃博霉素衍生物
公开(公告)号：US07125899B2
公开(公告)日：2006-10-24
申请号：US10405886
申请日：2003-04-03
申请人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri , James A. Johnson
发明人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri , James A. Johnson
IPC分类号： C07D493/04 , C07D417/06 , C07D227/20 , A61K31/425 , A61P35/00
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to epothilone derivatives, having the following formula: in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are defined herein, methods for preparation of the derivatives and intermediates thereof.
摘要翻译：本发明涉及具有下式的埃坡霉素衍生物：其中变量G，W，Q，X，Y，B 1，B 2，Z，SUB > 1，Z 2和R 1-R 7是本文定义的衍生物及其中间体的制备方法。

20. 再颁专利

USRE39356E1 Process for the preparation of epothilone analogs 有权
公开(公告)号：USRE39356E1
公开(公告)日：2006-10-17
申请号：US11056606
申请日：2005-02-11
申请人： Wen Sen Li , John E. Thornton , Zhenrong Guo , Shankar Swaminathan , Robert M. Borzilleri , Soong-Hoon Kim , Denis Favreau
发明人： Wen Sen Li , John E. Thornton , Zhenrong Guo , Shankar Swaminathan , Robert M. Borzilleri , Soong-Hoon Kim , Denis Favreau
IPC分类号： C07D491/00 , C07D417/00
摘要： The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式