公开(公告)号：EP0011399A1

公开(公告)日：1980-05-28

申请号：EP79302299.7

申请日：1979-10-23

申请人： FISONS plc

发明人： Brown, Roger Charles ,  Brown, Rodney Alan ,  O'Connor, Stephen Eric

IPC分类号： C07D473/08 ,  A61K31/52

CPC分类号： C07D473/08

摘要： The substituted theophyllines of the formula:

(wherein R', R 2 and R 3 , which may be the same or different, each represent alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or phenylalkyl of 7 to 10 carbon atoms, each of which may be unsubstituted or substituted by one or more hydroxy groups, alkoxy or alkylthio groups of 1 to 4 carbon atoms, halogen atoms, cyano groups, nitro groups, carboxy groups, alkoxycarbonyl groups of 2 to 5 carbon atoms, amino groups, alkylamino groups of 1 to 4 carbon atoms or dialkylamino groups of 2 to 8 carbon atoms, or when the group is pehnyl or phenylalkyl, by one or more alkyl groups of 1 to 4 carbon atoms;
or R 2 and R'together represent a hydrocarbon chain of 3 to 6 carbon atoms optionally interrupted by a heteroatom; and n represents an integer from 1 to6) and the acid additional salts thereof, are novel compounds which are useful in the treatment of cardiac disorders. Processes for their preparation and pharmaceutical compositions containing them are also described.

公开(公告)号：EP0217519B1

公开(公告)日：1992-02-05

申请号：EP86306325.1

申请日：1986-08-15

申请人： FISONS plc

发明人： Brown, Roger Charles ,  Robinson, David Hulme ,  Dixon, John

IPC分类号： C07D285/12 ,  C07D417/04 ,  A61K31/41

CPC分类号： C07D253/06 ,  A61K38/00 ,  C07D271/10 ,  C07D285/12 ,  C07D285/135 ,  C07D285/16 ,  C07D417/04 ,  C07K5/0222 ,  C07K5/06086

公开(公告)号：EP0384636A1

公开(公告)日：1990-08-29

申请号：EP90301579.0

申请日：1990-02-14

申请人： FISONS plc

发明人： Baxter, Andrew John Gilby ,  Robinson, David Hulme ,  Brown, Roger Charles

IPC分类号： C07C327/04 ,  A61K31/265 ,  C07C323/60 ,  A61K31/095 ,  C07D207/09 ,  C07D277/04 ,  C07F9/09

CPC分类号： C07F9/5721 ,  C07C323/60 ,  C07C327/32 ,  C07C2601/08 ,  C07D207/10 ,  C07D207/12 ,  C07D277/06 ,  C07F9/3808

摘要： There are described compounds of formula I, processes for their preparation and pharmaceutical formulations containing them,
ZCHR₁COR₂      I
in which R₂ is a group of formula II,
-NR x CHR y COOH      II
in which R x and R y are each alkyl optionally substituted by phenyl; phenylalkyl C7 to 12, phenyl, phenyloxyalkyl, N-alkyl, O-alkyl, or together R x and R y may form a heterocyclic group optionally substituted by alkyl, phenyl; phenylalkyl C7 to 12, phenyl, phenyloxyalkyl, N-alkyl, O-alkyl, or one of R x and R y may be hydrogen,
provided that one of R x and R y , the heterocyclic group formed by R x and R y or the optional substituents is substituted by one or two groups -COOR₉
R₉ is phenyl, -(CH₂) x CONR₁₄R₁₅, -(CH₂) y COOR₁₆ or alkyl optionally substituted by phenyl;
R₁₄, R₁₅, R₁₆, x and y, are as described in the specification,
and pharmaceutically acceptable salts thereof.

摘要翻译： 描述了式I的化合物，其制备方法和含有它们的药物制剂，其中R 2是式II基团的ZCHR1COR2I，其中Rx和Ry各自为烷基任选被苯基取代的-NR x CHR y COOH II; 苯基烷基C7至12，苯基，苯氧基烷基，N-烷基，O-烷基或一起Rx和Ry可以形成任选被烷基，苯基取代的杂环基; 苯基烷基C7至12，苯基，苯氧基烷基，N-烷基，O-烷基或Rx和Ry中的一个可以是氢，条件是Rx和Ry中的一个，由Rx和Ry形成的杂环基或任选的取代基被 一个或两个基团-COOR 9 R 9是苯基， - （CH 2）x CONR 14 R 15， - （CH 2）y COOR 16或任选被苯基取代的烷基; R14，R15，R16，x和y如说明书中所述及其药学上可接受的盐。

公开(公告)号：EP0217519A1

公开(公告)日：1987-04-08

申请号：EP86306325.1

申请日：1986-08-15

申请人： FISONS plc

发明人： Brown, Roger Charles ,  Robinson, David Hulme ,  Dixon, John

IPC分类号： C07D285/12 ,  C07D417/04 ,  A61K31/41

CPC分类号： C07D253/06 ,  A61K38/00 ,  C07D271/10 ,  C07D285/12 ,  C07D285/135 ,  C07D285/16 ,  C07D417/04 ,  C07K5/0222 ,  C07K5/06086

摘要： There are described compounds of formula I,
in which Y is S, 0 or NR 9 ,

n is 0 or 1,
R 9 is hydrogen or alkyl C 1 to 10,
R 3 is hydrogen, alkyl C 1 to 10, cycloalkyl C3 to 10, CF 3 , SR 10 , a 5 or 6 membered heterocyclic group containing one or more S, O or N atoms, NR 4 R 5 , phenyl or phenylalkyl C7 to 12, the phenyl, phenylalkyl and heterocyclic groups optionally being fused to a further phenyl group, the heterocyclic group and any phenyl group optionally being substituted by alkyl C 1 to 6, halogen, alkoxy C 1 to 6, nitro, nitrile, CF 3 , SR 6 , NR 7 R 11 or hydroxy,
R 6 , R 7 and R,,, which may be the same or different, are each hydrogen or alkyl C 1 to 10,
R, and R s , which may be the same or different, are each hydrogen, alkyl C 1 to 10 or phenyl,
R, 10 is alkyl C 1 to 10,
X, is S or 0, and
D is a chain comprising from 2 -16 atoms, which chain carries an O or S containing substituent at a position 2 -6 atoms away from the group C=X,,
and pharmaceutically acceptable salts, esters and amides thereof,
there are also described methods for making the compounds and pharmaceutical formulations, eg for the treatment of hypertension, containing them.