公开(公告)号：US20070111998A1

公开(公告)日：2007-05-17

申请号：US11546299

申请日：2006-10-12

申请人： Siripragada Rao ,  Akella Satya Srinivas ,  Shikha Rani ,  Gaddam Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

发明人： Siripragada Rao ,  Akella Satya Srinivas ,  Shikha Rani ,  Gaddam Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/416 ,  A61K31/403 ,  C07D417/02 ,  C07D403/02 ,  C07D413/02

CPC分类号： C07D209/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

摘要： The present invention relates to novel heterocyclic compounds of the general formula (I), as IL-6 inhibitors, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, their metabolites and prodrugs thereof. The present invention more particularly provides novel heterocyclic compounds of the general formula (I). Also included is a method for treatment of cancer, cancer cachexia and inflammatory diseases including immunological diseases, particularly those mediated by cytokines such as IL-6, through pSTAT3 inhibition, in a mammal comprising administering an effective amount of a compound of formula (I) as described above.

摘要翻译： 本发明涉及通式（I）的新型杂环化合物，作为IL-6抑制剂，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其水合物，其溶剂合物，其药学上可接受的盐和组合物 ，它们的代谢物和前药。 本发明更具体地提供了通式（I）的新型杂环化合物。 还包括在哺乳动物中治疗癌症，癌症恶病质和炎性疾病的方法，包括免疫疾病，特别是通过pSTAT3抑制的细胞因子如IL-6介导的疾病，包括给予有效量的式（I）化合物， 如上所述。

公开(公告)号：US20070066569A1

公开(公告)日：2007-03-22

申请号：US11522908

申请日：2006-09-19

申请人： Udayampalayam Senthilkumar ,  Thangavel Arulmoli ,  Venu Lakshmipathi ,  Siripragada Rao

发明人： Udayampalayam Senthilkumar ,  Thangavel Arulmoli ,  Venu Lakshmipathi ,  Siripragada Rao

IPC分类号： A61K31/675 ,  C07F9/22

CPC分类号： C07F9/3873 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/65068

摘要： The present invention is to relate an improved process using anisole as solvent for the preparation of compound of formula (I) and its pharmaceutically acceptable salts thereof. wherein R represents —NR1R2, or a group n=1, 2, 3, 4 and 5, where R1 and R2 may be same or different and independently represents hydrogen, or C1-6 alkyl;

摘要翻译： 本发明涉及使用苯甲醚作为制备式（I）化合物及其药学上可接受的盐的溶剂的改进方法。 其中R表示-NR 1 R 2 2或基团n = 1,2,3,4和5，其中R 1和R 2 可以相同或不同，并且独立地表示氢或C 1-6烷基;

公开(公告)号：US20070060756A1

公开(公告)日：2007-03-15

申请号：US11521541

申请日：2006-09-15

申请人： Veerappan Vijayabaskar ,  Siripragada Rao ,  Prabhakaran Kannan ,  Devasitham Prabhu

发明人： Veerappan Vijayabaskar ,  Siripragada Rao ,  Prabhakaran Kannan ,  Devasitham Prabhu

IPC分类号： C07D401/02

CPC分类号： C07D401/04

摘要： The present invention relates to an improved process for the preparation of compound of formula (I), 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine (Desloratadine) or its pharmaceutically acceptable salts thereof, by reacting a compound of formula (II), 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1 piperidinecarboxylic acid ethyl ester (Loratadine) with sodium hydroxide in a solvent mixture of toluene and polyethylene glycol (PEG 400) at reflux temperature.

摘要翻译： 本发明涉及制备式（I）化合物，8-氯-6,11-二氢-11-（4-亚哌啶基）-5H-苯并[5,6]环庚并[1,2 -b]吡啶（地氯雷他定）或其药学上可接受的盐通过使式（II）化合物，4-（8-氯-5,6-二氢-11H-苯并[5,6]环庚并[1,2 -b]吡啶-11-亚基）-1-哌啶羧酸乙酯（氯雷他定）与氢氧化钠在甲苯和聚乙二醇（PEG400）的溶剂混合物中的混合物。