公开(公告)号：US08809538B2

公开(公告)日：2014-08-19

申请号：US13143998

申请日：2010-01-07

申请人： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

发明人： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

IPC分类号： C07D403/00 ,  C07D403/14 ,  A61K31/454 ,  A61K31/4545

CPC分类号： C07D413/14 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04

摘要： A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.

摘要翻译： 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。

公开(公告)号：US08962596B2

公开(公告)日：2015-02-24

申请号：US13640099

申请日：2011-04-11

申请人： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

发明人： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D498/04

摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

摘要翻译： 式I化合物及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是一种或多种JAK激酶的抑制剂， 可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。

公开(公告)号：US20110275608A1

公开(公告)日：2011-11-10

申请号：US13143998

申请日：2010-01-07

申请人： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

发明人： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

IPC分类号： A61K31/454 ,  C07D417/14 ,  C07D413/14 ,  C07D409/06 ,  C07D417/06 ,  C07D401/06 ,  A61K31/4535 ,  C07D409/14 ,  A61K31/4725 ,  C07D471/04 ,  A61K31/437 ,  C07D498/04 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/10 ,  C07D413/06

CPC分类号： C07D413/14 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04

摘要： A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.

摘要翻译： 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。

公开(公告)号：US20130131039A1

公开(公告)日：2013-05-23

申请号：US13640099

申请日：2011-04-11

申请人： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

发明人： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

IPC分类号： C07D487/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D498/04

摘要： Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

摘要翻译： 式I化合物（此处应该插入式）及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是抑制剂 的一种或多种JAK激酶，并且可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞的排斥，以及血液系统疾病和恶性肿瘤及其并发症。