公开(公告)号：US20060105964A1

公开(公告)日：2006-05-18

申请号：US11255643

申请日：2005-10-21

申请人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton

发明人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton

IPC分类号： A61K31/7052 ,  A61K31/513 ,  A61K31/506 ,  C07D403/14

CPC分类号： C07D401/14 ,  C07D401/06 ,  C07H17/02

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US20070203149A1

公开(公告)日：2007-08-30

申请号：US11677889

申请日：2007-02-22

申请人： Ragulan Ramanathan ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton ,  Diane Grotz ,  Diane Rindgen ,  Amol Tendolkar

发明人： Ragulan Ramanathan ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton ,  Diane Grotz ,  Diane Rindgen ,  Amol Tendolkar

IPC分类号： A61K31/506 ,  A61K31/551 ,  C07D403/14 ,  A61K31/522

CPC分类号： C07D401/14 ,  C07D409/14

摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula I as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的结构式I化合物作为CCR5受体的抑制剂，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物制剂的方法，其包含一种或多种这样的化合物 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法。 本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。 本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣 ，哮喘，过敏或多发性硬化。

公开(公告)号：US20050026939A1

公开(公告)日：2005-02-03

申请号：US10901574

申请日：2004-07-29

申请人： Anima Ghosal ,  Wei Tong ,  Swapan Chowdhury ,  Shmuel Zbaida ,  Mark Wirth ,  Kevin Alton ,  James Patrick ,  Craig Boyle ,  Andrew Stamford

发明人： Anima Ghosal ,  Wei Tong ,  Swapan Chowdhury ,  Shmuel Zbaida ,  Mark Wirth ,  Kevin Alton ,  James Patrick ,  Craig Boyle ,  Andrew Stamford

IPC分类号： C07D473/06 ,  A61K31/522 ,  C07D473/02

CPC分类号： C07D473/06

摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.

摘要翻译： 本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。 进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病， 心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗 综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。