Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4]...

Details Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4]... Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4]...

2007-04-10

2007-04-10

Coleman, Brenda (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S561000

Reexamination Certificate

active

10399596

ABSTRACT:
The present invention concerns compounds for use as a medicine having the formula (I), the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1represents hydrogen, C1-6alkyl, C1-4alkylthio, C1-4alkyloxy, or halo; R2represents hydrogen or C1-6alkyl; R3represents phenyl substituted with halo, cyano, C1-4alkyloxy, C1-4alkylthio, C1-6alkyl, haloC1-6alkyl; 2-thienyl; or 3-thienyl, R4represents hydrogen; or R2and R4form an extra bond, which are active against dermatophytes, and their preparation; it further relates to compositions comprising them, as well as their use as a medicine.

REFERENCES:
F. Corelli et al., “Sistemi eterociclici”, Farmaco Ed. Sci., vol. 39, No. 8, pp. 707-717 (1984).
S. Raines et al., “Mannich Reactions. Synthesis of 4,5-Dihydropyrrolo[1,2-α] quinoxalines, 2,3,4,5-Tetrahydro-1H-pyrrolo[1,2-α][1,4] diazepines and 5,6-Dihydro-4H-pyrrolo[1,2-α] [1,4] benzodiazepines”, J. Heterocycl. Chem., vol. 13, pp. 711-716 (1976).
G.W.H. Cheeseman et al., “Further Cyclisation Reactions of 1-Arylpyrroles”, J. Chem. Soc., pp. 2732-2734 (1971).
S. Vomero et al., “Ricerche su composti eterociclici azotati”, Farmaco Ed. Sci., vol. 35, No. 2, pp. 110-119 (1980).
PCT International Search Report, dated Feb. 20, 2002, for PCT Int'l Pat. No. WO02/34752.
Corelli, F. et al., “Heterocyclic Systems”,Sistemi Eterociclici, Institute of Pharmaceutical Chemistry and Toxicology, 1984, 707-717, Full English Language Translation from Italian.
Vomero, S. et al., “Research in Relation to Nitrogenated Heterocyclic Systems”,Institute of Pharmaceutical Chemistry and Toxicology, 1980, 110-119, Full English Language Translation from Italian.

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