4,5-dihydro-isoxazole derivatives and their pharmaceutical use

Details 4,5-dihydro-isoxazole derivatives and their pharmaceutical use 4,5-dihydro-isoxazole derivatives and their pharmaceutical use

2003-03-31

2008-08-19

Habte, Kahsay T (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S254030, C514S254040, C514S326000, C514S364000, C514S378000, C548S125000, C548S131000, C548S143000, C548S240000, C540S603000, C544S367000, C546S209000

Reexamination Certificate

active

07414048

ABSTRACT:
The present invention is concerned with the compounds of formulawherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide, ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2and R3each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5and R6each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, C(1-6)alkyloxy, cyano, (C═O)R25, (C—O)OR16, (SO2)R16, aminocarbonyloxy, aminoC(1-6)alkyl, NR17R18, N3, Ar or Het; or R5and R6together with the carbon atom to which they are attached, form an Ar or Het; Ar represents an optionally substituted C(6-14)aryl; Het represents an optionally substituted C(1-14)heterocycle; or a N-oxide, pharmaceutically acceptable addition salt, quaternary amine or stereochemically isomeric form thereof; the processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

REFERENCES:
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Abstract of Bondarev et al. Zhurnal Organichesko Khimii (1967), 3(5), 821-6 (Two pages).
Edward F. Kleinman, et al., “Striking Effect of Hydroranic Acid Substitution on the Phosphodiestererase Type 4 (PDE4) and TNF Inhibitory Activity of Two Series of Rolipram Analogues: Implications for a New Active Site Model of PDE4”, Journal of Medicinal Chemistry, Published on Web 1998, vol. 41, No. 3, pp. 266-270, XP002093975.

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