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US 5,705,504 AGranted
Piperidine derivatives with PAF antagonist activity
AssigneeJ. Uriach & Cia. S.A.
InventorsElena Carceller, Pere J. Jimenez, Nuria Recasens, Jordi Salas, Carmen Almansa, Javier Bartroli
Life of this patent
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Abstract
Compounds of general formula I and their salts and solvates are PAF antagonists and as such are useful in the treatment of various diseases or disorders mediated by PAF. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
Claims21
A compound of formula I:
- ##STR12## wherein:
- m represents 0, 1 or 2;
- a, b and c represent CR, wherein each R independently represents hydrogen or C.sub.1-4 alkyl;
- R.sup.1 represents C.sub.1-4 alkyl or C.sub.3-7 cycloalkyl;
- A represents --CO--, --SO.sub.2 --, --NHCO-- or --OCO--;
- B represents a group of formula (i), and when A represents --CO-- or --SO.sub.2 --, then B can also represent a group of formula (ii) or (iii) ##STR13## n represents 0, 1, 2 or 3;
- one of R.sup.2 or R.sup.3 represents C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl or aryl, and the other represents hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.3-7 cycloalkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, aryl or aryl-C.sub.1-4 alkyl;
- Z represents hydrogen, C.sub.1-4 alkyl, --CH.sub.2 --OR.sup.4, --COOR.sup.4 or --CONR.sup.4 R.sup.5, and when A represents --CO-- or --SO.sub.2 --, then Z can also be hydroxy, --NR.sup.4 R.sup.5, --NR.sup.6 C(.dbd.O)OR.sup.4, --NR.sup.6 C(.dbd.O)R.sup.4, --NR.sup.6 C(.dbd.O)NR.sup.4 R.sup.5, --N(OH)C(.dbd.O)NR.sup.4 R.sup.5 or --NR.sup.6 SO.sub.2 R.sup.4 ;
- or Z and R.sup.3 together form a C.sub.2-5 polymethylene chain in which case R.sup.2 represents C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl or aryl;
- R.sup.4 represents hydrogen, C.sub.1-4 alkyl, aryl or aryl-C.sub.1-4 alkyl;
- R.sup.5 and R.sup.6 independently represent hydrogen or C.sub.1-4 alkyl;
- R.sup.7 represents C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, aryl, aryl-C.sub.1-4 alkyl or bisaryl-C.sub.1-4 alkyl;
- Y represents hydrogen, C.sub.1-4 alkyl, aryl, aryl-C.sub.1-4 alkyl, --C(.dbd.O)OR.sup.4, --C(.dbd.O)R.sup.4, --C(.dbd.O)NR.sup.4 R.sup.5, or --SO.sub.2 R.sup.4 ;
- aryl, whenever appearing in the above definitions, represents phenyl or phenyl substituted with 1, 2, 3 or 4 groups independently selected from halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, cyano, nitro, amino, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkylcarbonyloxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylthio, C.sub.1-4 alkylcarbonylamino or C.sub.1-4 alkoxycarbonylamino;
- and the salts and solyates thereof.
12 more elements
Dependencies are inferred from the claim text.