Potent and selective, sulfamide-based human β3-adrenergic receptor agonists
摘要:
A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(1)- or beta(2)-AR. (C) 2004 Elsevier Ltd. All rights reserved.
Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
Method of treating a patient having precancerous lesions with phenyl purinone derivatives
申请人:Cell Pathways, Inc.
公开号:US06200980B1
公开(公告)日:2001-03-13
Derivatives of Phenyl Purinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.