公开(公告)号：US20040138242A1

公开(公告)日：2004-07-15

申请号：US10702579

申请日：2003-11-06

申请人： Merck and Co., Inc. ,  Synaptic Pharmaceutical Corporation

发明人： Donghui Cui ,  Margaret R. Davis ,  Michael Dunn ,  Ben E. Evans ,  Hanumath P. Kari ,  Bharat Lagu ,  Dhanapalan Nagarathnam ,  Kamlesh P. Vyas ,  Kanyin Zhang

IPC分类号： A61K031/513 ,  C07D239/02

CPC分类号： C07D239/22 ,  C07D401/12 ,  C07D401/14 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidines which are selective antagonists for human null1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the null1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为人α1a受体的选择性拮抗剂的二氢嘧啶。 本发明还涉及这些化合物用于缓解下尿路组织，治疗良性前列腺增生和用于治疗α1a受体的拮抗作用可能有用的任何疾病的用途。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US20010041707A1

公开(公告)日：2001-11-15

申请号：US09873746

申请日：2001-06-04

申请人： Merck and Co., Inc

发明人： Donghui Cui ,  Margaret R. Davis ,  Michael Dunn ,  Ben E. Evans ,  Hanumath P. Kari ,  Bharat Lagu ,  Dhanapalan Nagarathnam ,  Kamlesh P. Vyas ,  Kanyin Zhang

IPC分类号： A61K031/519 ,  A61K031/513 ,  C07D491/044 ,  C07D239/10

CPC分类号： C07D239/22 ,  C07D401/12 ,  C07D401/14 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidines which are selective antagonists for human null1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the null1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.