公开(公告)号：US5290776A

公开(公告)日：1994-03-01

申请号：US886798

申请日：1992-05-21

申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  C07D487/04 ,  C07D405/14 ,  A51K31/53

CPC分类号： C07D487/04

摘要： A compound of the formula I ##STR1## wherein: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 is phenyl, a C-linked aromatic 5- or 6-membered heterocyclic ring containing one of oxygen and sulphur and/or one or two nitrogen, or (1-8C)alkyl, alkenyl or alkynyl unsubstituted or substituted by a phenyl or a C-linked aromatic 5- or 6-membered heterocylic ring containing one of oxygen and sulphur and/or one or two nitrogen, any phenyl being unsubstituted or substituted by one, two or three of (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, hydroxy, benzyloxy and (1-5C)alkanoyloxy;A is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof, processes for the manufacture of the compounds, and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

摘要翻译： 式I化合物（*化学结构*）Ⅰ其中：R1为氢，（1-6C）烷基或（1-4C）烷酰基; R2是苯基，含有氧和硫之一和/或一个或两个氮的C-连接的芳香族5-或6-元杂环，或未被取代或被苯基取代或（1-8C）烷基， 含有一个氧和硫和/或一个或两个氮的C连接的芳族5-或6-元杂环，任何未被取代或被一个，两个或三个（1-4C）烷基取代的苯基（1-4C ）烷氧基，卤素，三氟甲基，羟基，苄氧基和（1-5C）烷酰氧基; A是N或CT，其中T是氢或（1-4C）烷基; 或其药学上可接受的盐，用于制备化合物的方法和含有它们的药物组合物。 这些化合物可用作腺苷拮抗剂。

公开(公告)号：US5270311A

公开(公告)日：1993-12-14

申请号：US708265

申请日：1991-05-28

申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

IPC分类号： A61K31/53 ,  A61P9/08 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P43/00 ,  C07D487/04 ,  C07D403/14

CPC分类号： C07D487/04

摘要： The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno;R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is hydrogen, (3-12C)cycloalkyl, (3-6C)alkenyl, phenyl(3-6C)alkenyl, tetrafluorophenyl, pentafluorophenyl, 5- or 6-membered heteroaryl, optionally substituted (1-6C)alkyl or optionally substituted phenyl;X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a 4 to 6-membered saturated heterocyclic ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists. The invention further provides novel intermediates useful in the manufacture of the compounds of formula I. ##STR1##

公开(公告)号：US5246932A

公开(公告)日：1993-09-21

申请号：US887211

申请日：1992-05-21

申请人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

发明人： Peter W. R. Caulkett ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

IPC分类号： A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D519/00

摘要： A compound of the formula I ##STR1## wherein: A.sup.1 and A.sup.2 are each independently N or CT in which T is hydrogen or (1-4C)alkyl;R.sup.1 and R.sup.2 are each independently hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;X.sup.1 and X.sup.2 are each independently O, S or NH; andL is a (3-7C)cycloalkylene group or a (1-8C)alkylene chain optionally interrupted or extended by a group selected from phenylene, phenyleneoxy or oxyphenyleneoxy, the phenylene portion of said group being unsubstituted or substituted by one of halogen, hydroxy and (1-4C)alkoxy, provided that all heteroatoms in the group X.sup.1 --L--X.sup.2 are separated from one another by at least two carbon atoms; or a pharmaceutically acceptable salt thereof, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

公开(公告)号：US5356894A

公开(公告)日：1994-10-18

申请号：US94572

申请日：1993-07-21

申请人： Peter W. Rodney ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

发明人： Peter W. Rodney ,  Geraint Jones ,  Michael G. Collis ,  Simon M. Poucher

IPC分类号： C07D487/04 ,  A61K31/535 ,  C07D413/06

CPC分类号： C07D487/04

摘要： R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;R.sup.2 (when not as hereinbelow defined together with X) is (1-6C)alkyl substituted by a group of formula R.sup.10 Xb(CO).sub.m in which m is 0 or 1, provided that when m is 0, X and Xb are separated by at least two carbon atoms, Xb is an imino group of formula --NRb in which Rb together with R.sup.10 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring;and X is oxy, thio, sulphinyl, sulphonyl or an imino group of formula --NRa-- in which Ra is hydrogen, (1-6C)alkyl or together with R2 and the adjacent nitrogen atom forms a morpholino, thiomorpholino, piperidino or azetidino ring; andA is N or CT in which T is hydrogen or (1-4C)alkyl;or a pharmaceutically acceptable salt thereof; processes for the manufacture of the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

摘要翻译： 本发明涉及新颖的药学上有用的式I化合物，其中Q是任选带有1或2个独立地选自（1-4C）烷基和卤代的取代基的5元杂芳基; R1是氢，（1-6C）烷基或（1-4C）烷酰基; R2（当不与X一起定义时不同时）是由式R 10 X b（CO）m取代的（1-6C）烷基，其中m为0或1，条件是当m为0时，X和Xb被 至少两个碳原子，Xb是式-NRb的亚氨基，其中Rb与R10和相邻的氮原子一起形成吗啉代，硫代吗啉代，哌啶子基或氮杂环丁烷环; 并且X是式-NR a的氧基，硫基，亚磺酰基，磺酰基或亚氨基，其中R a是氢，（1-6C）烷基或与R 2一起并且相邻的氮原子形成吗啉代，硫代吗啉代，哌啶子基或氮杂环丁烷环 ; A为N或CT，其中T为氢或（1-4C）烷基; 或其药学上可接受的盐; 用于制备含有它们的化合物和药物组合物的方法。 这些化合物可用作腺苷拮抗剂。