公开(公告)号：US4755594A

公开(公告)日：1988-07-05

申请号：US936766

申请日：1986-12-09

申请人： Alexander J. Bridges ,  Harriet W. Hamilton ,  Walter H. Moos ,  Deedee L. Szotek

发明人： Alexander J. Bridges ,  Harriet W. Hamilton ,  Walter H. Moos ,  Deedee L. Szotek

IPC分类号： C07H19/16 ,  A61K31/70 ,  C07H19/167

CPC分类号： C07H19/16

摘要： The present inventions are novel N.sup.6 -substituted adenosines wherein the N substituent is ##STR1## wherein Ar is an unsubstituted or substituted (1) phenyl, (2) 1- or 2-naphthalenyl, (3) 2- or 3-thienyl, (4) 2- or 3-furanyl, (5) 2-, 4-, or 5-thiazyl, (6) 2-, 3-, or 4-pyridyl, or (7) 2-pyrimidyl wherein the substituents include at least one of lower alkyl, halo, trifluoromethyl, hydroxy, lower alkoxy, lower acyloxyamino, N-lower monoalkyl or N,N-lower dialkylamino, lower thioalkyl, lower alkylsulfonyl, or nitro and R' is hydrogen or alkyl, A is ##STR2## wherein q, q', or q" are one to four, n and m are independently zero to three provided if A is a bond then n and m is at least 2 and if A is other than a bond then n and m is at least one. These novel adenosines have highly desirable central nervous system and cardiovascular activities and therefore the present invention also includes pharmaceutical compositions and methods of use therefor.

摘要翻译： 本发明是新的N6取代的腺苷，其中N取代基是其中Ar是未取代或取代的（1）苯基，（2）1-或2-萘基，（3）2-或3-噻吩基（ 4）2-或3-呋喃基，（5）2-，4-或5-噻唑基，（6）2-，3-或4-吡啶基或（7）2-嘧啶基，其中取代基至少包括 低级烷基，卤素，三氟甲基，羟基，低级烷氧基，低级酰氧基氨基，N-低级单烷基或N，N-低级二烷基氨基，低级硫代烷基，低级烷基磺酰基或硝基，R'是氢或烷基，A是< 其中q，q'或q“为1至4，n和m独立地为0至3，条件是如果A是键，则n和m至少为2，如果A不是键，则n和m是 最后一个。 这些新颖的腺苷具有非常需要的中枢神经系统和心血管活性，因此本发明还包括药物组合物及其用途的方法。