Claims
- 1. A xanthine derivative of formula I ##STR55## wherein R.sup.1 is C.sub.1-6 -alkyl, C.sub.3-4 -alkenyl or C.sub.3-4 -alkynyl;
- R.sup.2 is C.sub.1-6 -alkyl, C.sub.3-4 -alkenyl or C.sub.3-4 -alkynyl;
- R.sup.3 represents a group of formula ##STR56## wherein R.sup.a may represent H, or C.sub.1 -C.sub.4 alkyl, and
- R.sup.b may represent H, or C.sub.1 -C.sub.4 alkyl, or
- R.sup.3 represents a group of formula ##STR57## wherein A=O, S; n,m=0,1,2,3 or 4 and n+m=2,3 or 4 and one of the two rings may be mono- or polysubstituted by OR.sup.4, C.sub.1-6 -alkyl, C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl, C.sub.1-4 -alkylidene, phenyl, substituted phenyl, optionally substituted aralkyl, NR.sup.5 R.sup.6, COOR.sup.4, CONR.sup.5 R.sup.6, OR.sup.4, SR.sup.4, OR.sup.7, --(CH.sub.2).sub.1-4 --NR.sup.5 R.sup.6,--(CH.sub.2).sub.1-4 CONR.sup.5 R.sup.6, C.sub.1-4 -alkyl-S--R.sup.4, C.sub.1-4 -alkyl-OR.sup.4, .dbd.O, C.sub.1-4 -alkyl-OR.sup.7, C.sub.1-4 -alkyl-COOR.sup.4, NHR.sup.7, optionally substituted C.sub.3-6 -cycloalkyl, or
- R.sup.3 represents a group of formula ##STR58## wherein A=CH.sub.2 ; n,m=0,1,2,3 or 4 and n+m=2,3 or 4 and one of the two rings is mono- or polysubstituted by OR.sup.4, C.sub.1-6 -alkyl, C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl, C.sub.1-4 -alkylidene, phenyl, substituted phenyl, optionally substituted aralkyl, NR.sup.5 R.sup.6, COOR.sup.4, CONR.sup.5 R.sup.6, OR.sup.4, SR.sup.4, OR.sup.7, --(CH.sub.2).sub.1-4 --NR.sup.5 R.sup.6, --(CH.sub.2).sub.1-4 CONR.sup.5 R.sup.6, C.sub.1-4 -alkyl-S--R.sup.4, C.sub.1-4 -alkyl-OR.sup.4, .dbd.O, C.sub.1-4 -alkyl-OR.sup.7, C.sub.1-4 -alkyl-COOR.sup.4, NHR.sup.7, optionally substituted C.sub.3-6 -cycloalkyl, or
- R.sup.3 represents a group of formula ##STR59## with A=O or --CH.sub.2 --CH.sub.2 --, whilst the ring system is optionally substituted by one or more C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, NR.sup.5 R.sup.6, COOR.sup.4, CONR.sup.5 R.sup.6, OR.sup.4, OR.sup.7, SR.sup.4, .dbd.O, CH.sub.2 OR.sup.4, CH.sub.2 OR.sup.7, CH.sub.2 COOR.sup.4, CH.sub.2 CONR.sup.5 R.sup.6 ;
- R.sup.4 represents hydrogen, C.sub.1-8 -alkyl, optionally substituted C.sub.3-6 -cloalkyl, optionally substituted C.sub.1-4 -alkylphenyl, C.sub.3-6 -alkenyl, optionally substituted aralkyl;
- R.sup.5 represents hydrogen, a C.sub.1-6 -alkyl group, optionally substituted C.sub.3-6 -cycloalkyl, optionally substituted aralkyl;
- R.sup.6 represents hydrogen, a C.sub.1-6 -alkyl group, optionally substituted aralkyl, a group of general formula --(CH.sub.2).sub.n --NR.sup.5 R.sup.6 (where R.sup.5 may be the same or different), --(CH.sub.2).sub.n --CN, --(CH.sub.2).sub.n --OR.sup.4, --(CH.sub.2).sub.n --OR.sup.7, --(CH.sub.2).sub.n --NHR.sup.7 wherein
- n=2,3,4,5,6,7or 8,
- or R.sup.5 and R.sup.6 together form an optionally substituted five, six- or seven-membered ring which may contain a further heteroatom from the group comprising oxygen, sulphur or nitrogen, whilst the nitrogen atom may be substituted by the group R.sup.4 ;
- R.sup.7 represents an amino acid group, linked via the carbonyl function, of a naturally occuring amino acid, CO--C.sub.1-13 -alkyl, optionally substituted CO--C.sub.1-13 -alkylphenyl;
- in the form of a racemate, an optically active compound, a pure diastereomer or mixture of diastereomers or a pharmacologically acceptable acid addition salt thereof.
- 2. A xanthine derivative of formula I ##STR60## wherein R.sup.1 represents a C.sub.3-4 -alkyl group, a propenyl group or a propargyl group;
- R.sup.2 represents a C.sub.3-4 -alkyl group, a propenyl group or a propargyl group;
- R.sup.3 represents a group of formula ##STR61## wherein R.sup.a may represent H, or C.sub.1 -C.sub.4 alkyl, and
- R.sup.b may represent H, or C.sub.1 -C.sub.4 alkyl, or
- R.sup.3 represents a group of formula ##STR62## optionally substituted by CH.sub.3, OH or OR.sup.7 ; or R.sup.3 represents a oxa- or thiabicyclo[3.3.0]octane, optionally substituted by OR.sup.4, .dbd.O, OR.sup.7 ;
- R.sup.3 represents a bicyclo[3.3.0]octane, substituted by OR.sup.4, .dbd.O, OR.sup.7 ;
- R.sup.4 represents hydrogen, a C.sub.1-3 -alkyl group, benzyl;
- R.sup.5 represents hydrogen, C.sub.1-3 -alkyl group;
- R.sup.6 represents hydrogen, methyl, ethyl, propyl, --(CH.sub.2).sub.n --NH.sub.2, --(CH.sub.2).sub.n --CN, --(CH.sub.2).sub.n --OR.sup.4, --(CH.sub.2).sub.n --OR.sup.7, --(CH.sub.2).sub.n --NR.sup.5 R.sup.5, --(CH.sub.2).sub.n --NHR.sup.7 (wherein n=2 through 8);
- R.sup.7 represents prolinoyl, CO--(CH.sub.2).sub.0-3 --CH.sub.3 or benzoyl,
- in the form of a racemate, an optically active compound, a pure diastereomer or mixture of diastereomers or a pharmacologically acceptable acid addition salt thereof.
- 3. A xanthine derivative of formula ##STR63## wherein R.sup.3 represents a group of formula ##STR64## in the form of a racemate, an optically active compound, a pure diastereomer or mixture of diastereomers or a pharmacologically acceptable acid addition salt thereof.
- 4. A xanthine derivative of formula ##STR65## wherein R.sup.3 represents a bicyclo[3.3.0]octane, substituted by OH, .dbd.O;
- R.sup.3 represent a oxabicyclo[3.3.0]octane,optionally substituted by OH, .dbd.O;
- in the form of a racemate, an optically active compound, a pure diastereomer or mixture of diastereomers or a pharmacologically acceptable acid addition salt thereof.
- 5. A xanthine derivative of formula ##STR66## in the form of a racemate, an optically active compound, a pure diastereomer or mixture of diastereomers or a pharmacologically acceptable acid addition salt thereof.
- 6. A pharmaceutical composition of matter comprising a xanthine derivative as recited in claim 1,2,3,4 and 5.
- 7. A pharmaceutical composition of matter comprising a xanthine derivative as recited in claim 2 and a pharmaceutically acceptable carrier or excipient.
- 8. A pharmaceutical composition of matter comprising a xanthine derivative as recited in claim 8 and a pharmaceutically acceptable carrier or excipient.
- 9. A method of treating disease in a warm-blooded animal receptive to adenosine antagonists which comprises administering to said animal a therapeutically effective mount of a xanthine derivative as recited in claim 1,2,3,4 and 5.
- 10. A method of treating disease in a warm-blooded animal receptive to adenosine antagonists which comprises administering to said animal a therapeutically effective amount of a xanthine derivative as recited in claim 2.
- 11. A method of treating disease in a warm-blooded animal receptive to adenosine antagonists which comprises administering to said animal a therapeutically effective amount of a xanthine derivatives as recited in claim 3.
Priority Claims (1)
Number |
Date |
Country |
Kind |
40 19 892.8 |
Jun 1990 |
DEX |
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Parent Case Info
This application is a continuation of prior U.S. application Ser. No. 08/168,280, filed Dec. 15, 1993, now abandoned, which is a continuation of prior U.S. application Ser. No. 07/834,550, filed as PCT/EP91/01131, Jun. 19, 1991, which is now abandoned.
US Referenced Citations (9)
Continuations (2)
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Number |
Date |
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Parent |
168280 |
Dec 1993 |
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Parent |
834550 |
Mar 1992 |
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