Appeal No. 95-1618
Application 08/033,456
The Claimed Subject Matter
The claims on appeal are directed to 4-, 5-, 6-, and 7-azaoxindole derivatives which according
to appellants are useful, inter alia, in the prevention or treatment of chronic inflammatory diseases,
allergy, psoriasis, various bone diseases, and immune dysfunctions such as systemic lupus
erythematosis. Claim 1 is representative of the claimed subject matter and is reproduced below.
1. A compound of the formula
wherein one of A, B, D and E is N and the others are CH; X and Y are independently selected from
3 3 3 3 3 3
hydrogen, OR , hydroxy, (C -C ) alkyl, CF , COR , halogen, C00R , CONR R , CN, NO , SR ,1 6 3 3 2
3 3 3 3 11 4 2 5
SOR , S0 R and SO NR R ; R is (C -C ) alkyl or CONHR ; R is (C -C ) alkyl, (CH ) R wherein2 3 2 1 6 1 8 2 n
n is 0 or 1, or NHR R is (C -C ) alkyl, phenyl, benzyl, allyl or hydrogen, wherein said phenyl and the8 3
1 6
phenyl moiety of said benzyl may optionally be substituted with one or more substituents
independently selected from fluoro, chloro, bromo, iodo, hydroxy, (C -C )alkyl, (C -C )alkoxy and1 3 1 3
4 3 3
CF R is hydrogen, (C -C )alkyl, (C -C ) cycloalkyl, COR wherein R is as defined above, phenyl,3 4 1 6 3 8
substituted phenyl, heteroaryl or substituted heteroaryl, wherein the heteroaryl moiety of each of said
heteroaryl and substituted heteroaryl groups is selected from thiophene and furan, and wherein each
of said substituted phenyl and substituted heteroaryl groups is substituted with one or two
substituents independently selected from fluoro, chloro, bromo, iodo, hydroxy, (C -C ) alkyl, (C -C )1 3 1 3
alkoxy and CF R is (C -C ) cycloalkyl, hydrogen, phenyl, substituted phenyl, heteroaryl and5
3 3 8
substituted heteroaryl, wherein the heteroaryl moiety of each of said heteroaryl and substituted
heteroaryl groups is selected from thiophene and furan, and each of said substituted phenyl and
substituted heteroaryl groups is substituted with one or two substituents independently selected from
6
fluoro, chloro, bromo, iodo, hydroxy, (C -C ) alkyl, (C -C ) alkoxy and trifluoromethyl; R is phenyl,1 3 1 3
thiophene or furan, wherein said phenyl, thiophene and furan may be optionally substituted with one
-2-
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