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1. 发明授权

US08796258B2 Cyclic azabenzimidazole derivatives useful as anti-diabetic agents 有权
标题翻译：用作抗糖尿病药的环状氮杂苯并咪唑衍生物
公开(公告)号：US08796258B2
公开(公告)日：2014-08-05
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/00 , C07D513/02
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

2. 发明申请

US20130123237A1 NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 有权
标题翻译：用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物
公开(公告)号：US20130123237A1
公开(公告)日：2013-05-16
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/4985 , A61K31/351 , A61K31/397 , A61K31/4412 , C07D471/04 , A61K31/496
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

3. 发明授权

US08071768B2 Alkylquinoline and alkylquinazoline kinase modulators 有权
标题翻译：烷基喹啉和烷基喹唑啉激酶调节剂
公开(公告)号：US08071768B2
公开(公告)日：2011-12-06
申请号：US11422349
申请日：2006-06-06
申请人： Nand Baindur , Michael David Gaul , Kevin Douglas Kreutter , Christian Andrew Baumann , Alexander J. Kim , Guozhang Xu , Robert W. Tuman , Dana L. Johnson
发明人： Nand Baindur , Michael David Gaul , Kevin Douglas Kreutter , Christian Andrew Baumann , Alexander J. Kim , Guozhang Xu , Robert W. Tuman , Dana L. Johnson
IPC分类号： C07D401/00 , C07D413/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G，Q和X如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是FLT3抑制剂， /或c-kit和/或TrkB，使用这些化合物降低或抑制细胞或受试者中FLT3和/或c-kit和/或TrkB的激酶活性，以及使用这些化合物预防或治疗在受试者中是与FLT3和/或c-kit和/或TrkB相关的细胞增殖性病症和/或病症。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

4. 发明授权

US07067512B2 Substituted 1,4-benzodiazepines and uses thereof 失效
标题翻译：取代的1,4-苯并二氮杂及其用途
公开(公告)号：US07067512B2
公开(公告)日：2006-06-27
申请号：US10292876
申请日：2002-11-13
申请人： Tianbao Lu , Louis V Lafrance, III , Daniel J Parks , Karen L Milkiewicz , Raul R Calvo , Maxwell D Cummings , Alexander J Kim , Bruce L Grasberger , Theodore E Carver, Jr.
发明人： Tianbao Lu , Louis V Lafrance, III , Daniel J Parks , Karen L Milkiewicz , Raul R Calvo , Maxwell D Cummings , Alexander J Kim , Bruce L Grasberger , Theodore E Carver, Jr.
IPC分类号： C07D243/12 , C07D243/18 , C07D243/24 , A61K31/55
CPC分类号： C07D401/04 , C07D243/14 , C07D403/10 , C07D405/04 , C07D409/04
摘要： The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M are defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0–8, m is 0–8, i is 1–8 and j is 0–8.
摘要翻译：本发明涉及新的1,4-苯二氮卓类药物，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d和M在本文中定义; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 9是环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基（烷基），芳烷基或杂芳基烷基，其各自任选被取代; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

5. 发明授权

US10442819B2 Tricyclic compounds as inhibitors of mutant IDH enzymes 有权
公开(公告)号：US10442819B2
公开(公告)日：2019-10-15
申请号：US15532549
申请日：2015-12-01
申请人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号： A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

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