公开(公告)号：US06319695B1

公开(公告)日：2001-11-20

申请号：US07961076

申请日：1992-10-14

申请人： Chi-Huey Wong ,  Yoshitaka Ichikawa ,  Gwo-Jenn Shen ,  Kun-Chin Liu

发明人： Chi-Huey Wong ,  Yoshitaka Ichikawa ,  Gwo-Jenn Shen ,  Kun-Chin Liu

IPC分类号： C12P1918

CPC分类号： C07H5/02 ,  C07H3/06 ,  C07H11/04 ,  C07H13/04 ,  C07H13/08 ,  C07H15/18 ,  C07H19/20 ,  C12P19/18 ,  C12P19/26

摘要： This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.

摘要翻译： 本发明考虑了碳水化合物，特别是岩藻糖基化碳水化合物的酶促生产的改进方法。 还考虑了使用化学和酶学方法改进的1或2-磷酸糖基酯的合成。 然后将磷酸化糖苷用于产生糖核苷酸，其又被用作供体糖用于受体碳水化合物的糖基化。 本文特别优选使用所公开的岩藻糖基化方法。

公开(公告)号：US5393879A

公开(公告)日：1995-02-28

申请号：US931014

申请日：1992-08-17

申请人： Chi-Huey Wong ,  Kun-Chin Liu

发明人： Chi-Huey Wong ,  Kun-Chin Liu

IPC分类号： C07H7/06 ,  C07H7/00

CPC分类号： C07H7/06

摘要： Nucleoside and nucleotide analogs corresponding to structural Formula I, below, are disclosed, in that structural formula, B is a ##STR1## purine base attached at the 9-position or pyrimidine base, attached at the 1-position R is hydrogen or PO.sub.3 .sup.= M.sup.+2, where M.sup.+2 is a mono- or divalent cation, and R.sup.1 is hydrogen or hydroxyl.

摘要翻译： 公开了对应于下面结构式I的核苷和核苷酸类似物，其结构式为B是连接在9-位或嘧啶碱基上的第一个嘌呤碱基，其连接在1-位R是氢或PO 3 = M + 2，其中M + 2是单价或二价阳离子，R1是氢或羟基。

公开(公告)号：US5276120A

公开(公告)日：1994-01-04

申请号：US835237

申请日：1992-02-13

申请人： Chi-Huey Wong ,  Tetsuya Kajimoto ,  Kun-Chin Liu ,  Lihren Chen

发明人： Chi-Huey Wong ,  Tetsuya Kajimoto ,  Kun-Chin Liu ,  Lihren Chen

IPC分类号： C07C247/04 ,  C07C311/18 ,  C07D211/46 ,  C07D211/56 ,  C07D211/94 ,  C07F7/08 ,  C07F9/09 ,  C12N9/12 ,  C12P19/04 ,  C12P19/18 ,  C12P19/26 ,  C07D211/40 ,  C07D207/12

CPC分类号： C07C247/04 ,  C07C311/18 ,  C07D211/46 ,  C07D211/56 ,  C07D211/94 ,  C07F7/0812 ,  C07F9/091 ,  C12N9/1241 ,  C12P19/04 ,  C12P19/18 ,  C12P19/26

摘要： A process for the preparation of a 1,5-dideoxyazafuranose or 1,6-dideoxy-azapyranose is disclosed. In such a process, an azido-substituted .alpha.-ketose phosphate having a five- or a six-carbon chain is hydrogenated in the presence of a palladium catalyst. The carbon atom bearing the azido substituent and the carbon atom of the keto group of the .alpha.-ketose phosphate starting material are separated by two or three carbon atoms.

摘要翻译： 公开了一种制备1,5-二脱氧氮杂蒽酮糖或1,6-二去氧 - 氮杂焦糖的方法。 在这种方法中，在钯催化剂存在下氢化具有五或六碳链的叠氮基取代的（α） - 酮磷酸酯。 带有叠氮基取代基的碳原子和（α） - 酮磷酸酯原料的酮基的碳原子被两个或三个碳原子分开。

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：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：US07335500B2

公开(公告)日：2008-02-26

申请号：US09992680

申请日：2001-11-19

申请人： Chi-Huey Wong ,  Yoshitaka Ichikawa ,  Gwo-Jenn Shen ,  Kun-Chin Liu

发明人： Chi-Huey Wong ,  Yoshitaka Ichikawa ,  Gwo-Jenn Shen ,  Kun-Chin Liu

IPC分类号： C12P19/22

CPC分类号： C07H5/02 ,  C07H3/06 ,  C07H11/04 ,  C07H13/04 ,  C07H13/08 ,  C07H15/18 ,  C07H19/20 ,  C12P19/18 ,  C12P19/26

摘要： This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.

摘要翻译： 本发明考虑了碳水化合物，特别是岩藻糖基化碳水化合物的酶促生产的改进方法。 还考虑了使用化学和酶学方法改进的1或2-磷酸糖基酯的合成。 然后将磷酸化糖苷用于产生糖核苷酸，其又被用作供体糖用于受体碳水化合物的糖基化。 本文特别优选使用所公开的岩藻糖基化方法。

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。