公开(公告)号：US20100004259A1

公开(公告)日：2010-01-07

申请号：US12373774

申请日：2008-01-24

申请人： Kevin Kun-Chin Liu ,  Yuan Zeng

发明人： Kevin Kun-Chin Liu ,  Yuan Zeng

IPC分类号： A61K31/497 ,  C07D401/04 ,  A61P25/00 ,  A61P25/18

CPC分类号： C07D221/04

摘要： The present invention provides a tartrate salt of Formula (I), Formula I is also known as (7S)-7-[(5-fluoro-2-methyl-benzyl)oxy]-2-[(2R)-2-methylpiperazin-1-yl]-6,7-dihydro-5H-cyclopenta[b]pyridine. The tartrate salt is preferably crystalline. The tartrate salt of Formula I of the invention is useful in the treatment of diseases linked to activation of the 5HT2c receptor in animals including humans, for example, in the treatment of schizophrenia, cognitive deficits including cognitive deficits associated with schizophrenia, anxiety, depression, obsessive-compulsive disorder, epilepsy, obesity, sexual dysfunction, and urinary incontinence, among others.

摘要翻译： 本发明提供式（I）的酒石酸盐，式I也称为（7S）-7 - [（5-氟-2-甲基 - 苄基）氧基] -2 - [（2R）-2-甲基哌嗪 -1-基] -6,7-二氢-5H-环戊二烯并[b]吡啶。 酒石酸盐优选是结晶的。 本发明的式I的酒石酸盐可用于治疗与包括人在内的动物中的5HT2c受体活化相关的疾病，例如精神分裂症的治疗，认知缺陷，包括与精神分裂症相关的认知缺陷，焦虑，抑郁， 强迫症，癫痫，肥胖，性功能障碍和尿失禁等。

公开(公告)号：US20120108588A1

公开(公告)日：2012-05-03

申请号：US13345528

申请日：2012-01-06

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/5377 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/496 ,  A61K31/506 ,  A61P3/10 ,  A61P35/00 ,  A61P9/10 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P25/28 ,  A61P17/00 ,  A61P31/12 ,  A61P1/16 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

公开(公告)号：US08114871B2

公开(公告)日：2012-02-14

申请号：US12532051

申请日：2008-04-10

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/535 ,  A61K31/495 ,  A61K31/497 ,  A61K31/4965 ,  C07D413/14 ,  C07D237/00 ,  C07D239/00 ,  C07D403/14 ,  C07D241/36 ,  C07D401/14

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

公开(公告)号：US09040547B2

公开(公告)日：2015-05-26

申请号：US13617035

申请日：2012-09-14

申请人： Hengmiao Cheng ,  Theodore Otto Johnson, Jr. ,  John Charles Kath ,  Kevin Kun-Chin Liu ,  Elizabeth Ann Lunney ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken ,  Scott Channing Sutton

发明人： Hengmiao Cheng ,  Theodore Otto Johnson, Jr. ,  John Charles Kath ,  Kevin Kun-Chin Liu ,  Elizabeth Ann Lunney ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken ,  Scott Channing Sutton

IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/52 ,  C07D473/16 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D473/18 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，T，V，W，X，Y，Z，环A，R1，R2，R3，R4，R5，R5a，R6，R7 ，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15，R 16，R 17和m如本文所定义。 有新的吡咯并嘧啶和嘌呤衍生物可用于哺乳动物治疗异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。

公开(公告)号：US08999981B2

公开(公告)日：2015-04-07

申请号：US13345528

申请日：2012-01-06

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/5377 ,  A61K31/495 ,  A61K31/499 ,  A61K31/497 ,  C07D413/14 ,  C07D237/02 ,  C07D239/02 ,  C07D241/02 ,  C07D241/36 ,  C07D239/70 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

公开(公告)号：US20130079324A1

公开(公告)日：2013-03-28

申请号：US13617035

申请日：2012-09-14

申请人： Hengmiao Cheng ,  Theodore Otto Johnson, JR. ,  John Charles Kath ,  Kevin Kun-Chin Liu ,  Elizabeth Ann Lunney ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken ,  Scott Channing Sutton

发明人： Hengmiao Cheng ,  Theodore Otto Johnson, JR. ,  John Charles Kath ,  Kevin Kun-Chin Liu ,  Elizabeth Ann Lunney ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Simon Paul Planken ,  Scott Channing Sutton

IPC分类号： A61K31/519 ,  C07D473/18 ,  A61P35/00 ,  A61K31/5377 ,  C07D498/10 ,  A61K31/5386 ,  C07D487/04 ,  A61K31/52

CPC分类号： C07D487/04 ,  C07D473/18 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

公开(公告)号：US20100249128A1

公开(公告)日：2010-09-30

申请号：US12532051

申请日：2008-04-10

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/499 ,  A61K31/496 ,  C07D471/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61P3/10 ,  A61P9/10 ,  A61P9/00 ,  A61P17/00 ,  A61P25/28 ,  A61P35/00 ,  A61P29/00 ,  A61P31/12 ,  A61P1/16 ,  A61P25/00

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。