公开(公告)号：US06323187B1

公开(公告)日：2001-11-27

申请号：US09316571

申请日：1999-05-21

申请人： Benjamin R. Yerxa ,  William Pendergast ,  Janet L. Rideout ,  Maryse Picher ,  Richard C. Boucher, Jr. ,  M. Jackson Stutts

发明人： Benjamin R. Yerxa ,  William Pendergast ,  Janet L. Rideout ,  Maryse Picher ,  Richard C. Boucher, Jr. ,  M. Jackson Stutts

IPC分类号： A01N4304

CPC分类号： A61K31/7048 ,  A61K31/70 ,  C07H19/207 ,  C07H21/00

摘要： The present invention relates to P1-(cytidine 5′-)-P-(uridine 5′-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.

摘要翻译： 本发明涉及P2Y2和/或P2Y4嘌呤能受体的高度稳定和选择性激动剂的P1-（胞苷5' - ） - （ - 尿苷5' - ）四磷酸及其盐，酯和酰胺及其制剂 。 本发明的化合物可用于治疗慢性阻塞性肺疾病如慢性支气管炎，原发性纤毛运动障碍，囊性纤维化，以及预防由于不动的肺炎，以及诱导痰及其咳痰。 此外，由于它们具有清除保留的粘液分泌物和刺激睫状肌搏动频率的一般能力，本发明的化合物也可用于治疗鼻窦炎和中耳炎。