Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-04-15
2000-08-29
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 80, 546 81, 546 82, 546 83, A61K 31395, A61K 31435, C07D491147
Patent
active
061109282
DESCRIPTION:
BRIEF SUMMARY
CROSS-REFERENCES
This application is a 371 of PCT/EP96/04346 filed Oct. 7, 1996.
The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives for the control of endoparasites, to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8 (7H)-dione derivatives and processes for their preparation.
Some 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives are already known. However, nothing is known of their use against endoparasites (cf. for example: T. Hisano et al. Chem. Pharm. Bull. 35 (3), (1987) pages 1049-1057; Heterocycles 29 (6), (1989) pages 1029-1032; Chem. Pharm. Bull. 38 (3), (1990) pages 605-611; Chem. Pharm. Bull. 39 (1), (1991) pages 10-17).
The present invention relates to: 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo-[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof, ##STR2## in which R.sup.1 represents hydrogen, straight-chain or branched alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl, heteroarylalkyl, which are optionally substituted, alkoxycarbonyl, which are optionally substituted, represent a 5- or 6-membered ring, which can optionally be interrupted by oxygen, sulfur, sulfoxyl or sulfonyl and is optionally substituted, alkoxycarbonyl, which are optionally substituted, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, amino, alkylamino, dialkylamino, cycloalkylamino, which are optionally substituted, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, which are optionally substituted, formyl, alkoxydicarbonyl or optionally represents a radical from the group consisting of G.sup.1, G.sup.2, G.sup.3 and G.sup.4 ##STR3## in which R.sup.6 represents hydrogen, straight-chain or branched alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, which are optionally substituted, represent a 5- or 6-membered ring, which can optionally be interrupted by oxygen, sulfur, sulfoxyl or sulfonyl and is optionally substituted, stand, straight-chain or branched alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aryl-alkyl, heteroaryl, heteroarylalkyl, which are optionally substituted, or optionally substituted, ##STR4## can denote carboxyl, thiocarboxyl, --C.dbd.CH--NO.sub.2, --C.dbd.CH--CN, --C.dbd.N--R.sup.9, sulfoxyl, sulfonyl, --P(O)--OR.sup.10 or P(S)--OR.sup.10, halogenoalkylcarbonyl, alkylsulfonyl, nitro or cyano, and cycloalkyl, aryl, arylalkyl, hetaryl or hetarylalkyl, which are optionally substituted, or optionally represents a radical from the group consisting of G.sup.5 and G.sup.6 ##STR5## in which ##STR6## can denote carboxyl, thiocarboxyl or sulfonyl, Y represents oxygen, sulfur or --NR.sup.12, amino group linked via a nitrogen atom, straight-chain or branched alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, which are optionally substituted, or 5-, 6- or 7-membered ring system or for a 7 to 10-membered bicyclic ring system, which can optionally also be interrupted by oxygen, sulfur, sulfoxyl, sulfonyl, carbonyl, --N--O, --N.dbd., --NR.sup.14 -- or by quaternized nitrogen and is optionally substituted, alkinyl, cycloalkyl, cycloalkylalkyl, alkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cyano, aryl, arylalkyl, heteroaryl, heteroarylalkyl stand which are optionally substituted, isomers or isomer mixtures of different composition, depending on the nature of the substituents. The invention relates both to the pure isomers and to the isomer mixtures. one or two double bonds between the carbon atom which carries the substituent R.sup.2 and the adjacent carbon atom, and/or between the carbon atom and the adjacent nitrogen atom which carry the substituents R.sup.1 and R.sup.5. carries the substituent R.sup.1 and the adjacent nitrogen atom with a substituent R.sup.5, the compounds of the formula (I) are in the form of their salts. 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivativ
REFERENCES:
Takuzo Hisano et al, Reaction of Aromatic N-Oxide. . . ; Fac. of Pharmaceutical Sc. pp. 1049-1057, Sep. 9, 1986.
Harder Achim
Jeschke Peter
Mencke Norbert
Akorli Godfried R.
Bayer Aktiengesellschaft
Desai Rita
Gil Joseph C.
Rotman Alan L.
LandOfFree
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