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21. 发明授权

US08629136B2 Bisfluoroalkyl-1,4-benzodiazepinone compounds 有权
标题翻译：双氟烷基-1,4-苯并二氮杂酮化合物
公开(公告)号：US08629136B2
公开(公告)日：2014-01-14
申请号：US13426730
申请日：2012-03-22
申请人： Ashvinikumar V. Gavai , Claude A. Quesnelle , Soong-Hoon Kim , Francis Y. Lee
发明人： Ashvinikumar V. Gavai , Claude A. Quesnelle , Soong-Hoon Kim , Francis Y. Lee
IPC分类号： C07D243/24 , A61K31/5513 , A61P35/00
CPC分类号： C07D243/24 , A61K31/138 , A61K31/337 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译：公开了式（I）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地是F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。

22. 发明授权

US08536327B2 Epothilone derivatives 有权
标题翻译：埃博霉素衍生物
公开(公告)号：US08536327B2
公开(公告)日：2013-09-17
申请号：US11763636
申请日：2007-06-15
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： C07D313/00
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of the formula where the variables are as defined in the disclosure.
摘要翻译：本发明涉及下式的化合物，其中变量如本公开所定义。

23. 发明申请

US20120283241A1 IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：咪达唑啶酮可用作激酶抑制剂
公开(公告)号：US20120283241A1
公开(公告)日：2012-11-08
申请号：US13552795
申请日：2012-07-19
申请人： Brian E. Fink , Libing Chen , Ashvinikumar V. Gavai , Liqi He , Soong-Hoon Kim , Andrew James Nation , Yufen Zhao , Litai H. Zhang
发明人： Brian E. Fink , Libing Chen , Ashvinikumar V. Gavai , Liqi He , Soong-Hoon Kim , Andrew James Nation , Yufen Zhao , Litai H. Zhang
IPC分类号： A61K31/5025 , A61P35/00 , A61P17/06 , A61K31/538 , A61P35/02 , A61K31/5377 , C07D498/04 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04 , C07D498/04
摘要： The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式（I）咪唑并哒嗪抑制蛋白激酶活性，从而使其成为抗癌剂。

24. 再颁专利

USRE42930E1 Aziridinyl-epothilone compounds 有权
标题翻译：氮丙啶基 - 埃坡霉素化合物
公开(公告)号：USRE42930E1
公开(公告)日：2011-11-15
申请号：US13089067
申请日：2011-04-18
申请人： Gregory D. Vite , Soong-Hoon Kim
发明人： Gregory D. Vite , Soong-Hoon Kim
IPC分类号： C07D277/22 , C07D203/26
CPC分类号： C07D491/04 , A61K47/551 , A61K47/65
摘要： The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —O2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.
摘要翻译：本发明涉及如本文进一步描述的氮杂环丙烷基埃坡霉素化合物和/或其药学上可接受的盐和/或溶剂合物，其具有下式：其中K是-O - ， - S-或-NR 7 - ; A是 - （CR 8 R 9） - （CH 2）m-Z-，其中Z是 - （CHR 10） - ， - C（= O） - ， - C（= O）-C（= O） - ， - OC ） - ， - N（R 11）C（= O） - ， - O 2 - 或-N（R 11）SO 2 - ; B1是羟基或氰基，R1是氢或B1和R1一起形成双键; R2，R3和R5独立地是氢，烷基，取代的烷基，芳基或取代的芳基; 或者R 2和R 3可以与它们所连接的碳一起形成任选取代的环烷基; R4是氢，烷基，烯基，取代的烷基，取代的烯基，芳基或取代的芳基; R6是氢，烷基或取代的烷基; R7，R8，R9，R10，R11和R12独立地是氢，烷基，取代的烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环烷基，取代的杂环烷基，杂芳基或取代的杂芳基; 并且R 13是芳基，取代的芳基，杂芳基或取代的杂芳基。

25. 再颁专利

USRE41911E1 Epothilone derivatives 有权
公开(公告)号：USRE41911E1
公开(公告)日：2010-11-02
申请号：US12539492
申请日：2009-08-11
申请人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri
发明人： Gregory D. Vite , Soong-Hoon Kim , Robert M. Borzilleri
IPC分类号： C07D498/08 , 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 as defined herein, methods for the preparation of the derivatives and intermediates thereof.

26. 发明申请

US20100113458A1 IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS 有权
标题翻译：咪达唑啶酮可用作激酶抑制剂
公开(公告)号：US20100113458A1
公开(公告)日：2010-05-06
申请号：US12575589
申请日：2009-10-08
申请人： Brian E. Fink , Libing Chen , Ashvinikumar V. Gavai , Liqi He , Soong-Hoon Kim , Andrew James Nation , Yufen Zhao , Litai H. Zhang
发明人： Brian E. Fink , Libing Chen , Ashvinikumar V. Gavai , Liqi He , Soong-Hoon Kim , Andrew James Nation , Yufen Zhao , Litai H. Zhang
IPC分类号： A61K31/5025 , C07D487/00
CPC分类号： C07D487/04 , C07D498/04
摘要： The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式（I）咪唑并哒嗪抑制蛋白激酶活性，从而使其成为抗癌剂。

27. 发明申请

US20070149534A1 PYRROLOTRIAZINE KINASE INHIBITORS 有权
标题翻译：吡咯啉激酶抑制剂
公开(公告)号：US20070149534A1
公开(公告)日：2007-06-28
申请号：US11560378
申请日：2006-11-16
申请人： Ping Chen , Yufen Zhao , Brian Fink , Soong-Hoon Kim
发明人： Ping Chen , Yufen Zhao , Brian Fink , Soong-Hoon Kim
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as antiproliferative agents.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐。式I化合物抑制Trk受体如TrkA，TrkB，TrkC或Flt-3的酪氨酸激酶活性，从而使其成为抗增殖剂。

28. 发明申请

US20060287371A1 Epothilone derivatives 有权
标题翻译：埃博霉素衍生物
公开(公告)号：US20060287371A1
公开(公告)日：2006-12-21
申请号：US11512623
申请日：2006-08-30
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： A61K31/427 , C07D417/02
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of the 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.
摘要翻译：本发明涉及下式的化合物，其中变量G，W，Q，X，Y，B 1，B 2，Z 1， Z 2，Z 2和R 1 -R 7如本文所定义，其衍生物的制备方法和中间体。

29. 发明申请

US20050187242A1 Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof 有权
标题翻译：糖皮质激素受体，AP-1和/或NF-kB活性的三环调节剂及其用途
公开(公告)号：US20050187242A1
公开(公告)日：2005-08-25
申请号：US11035176
申请日：2005-01-13
申请人： David Weinstein , John Gilmore , James Sheppeck , Bingwei Yang , Soong-Hoon Kim , Wayne Vaccaro
发明人： David Weinstein , John Gilmore , James Sheppeck , Bingwei Yang , Soong-Hoon Kim , Wayne Vaccaro
IPC分类号： A23K1/165 , A23K1/18 , A61K31/473 , C07D233/88 , C07D277/46 , C07D413/02 , C07D417/02 , C07D417/12 , C07D453/06
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。

30. 发明授权

US06800653B2 Epothilone derivatives 有权
标题翻译：埃博霉素衍生物
公开(公告)号：US06800653B2
公开(公告)日：2004-10-05
申请号：US10144879
申请日：2002-05-14
申请人： Alicia Regueiro-Ren , Robert M. Borzilleri , Gregory D. Vite , Soong-Hoon Kim
发明人： Alicia Regueiro-Ren , Robert M. Borzilleri , Gregory D. Vite , Soong-Hoon Kim
IPC分类号： A61K31425
CPC分类号： C07D417/06 , A61K31/427 , A61K31/5377 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
摘要翻译：本发明涉及12,13位修饰的埃坡霉素衍生物，衍生物的制备方法及其中间体。

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