Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-06-07
2005-06-07
Desai, Rita (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S304400, C548S215000, C548S217000
Reexamination Certificate
active
06903128
ABSTRACT:
There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0):and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein:A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)r-A2, A1-(CH2)r-A2-, where A1and A2are each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9;B is a member independently selected from the group consisting of the following:E is a single bond; —O—; —NR10—; —CH═CH—; —CC—; S(═O)q; —CR11R12NR10—; or —CR11R12—;X is —O—; —C(═O)—; —S(═O)q—; or —NR10—; X1, X2and X3are each independently selected from the group consisting of CH, CR9or N; Y is a single bond; —C(═O)—; —C(═S)—; or —S(═O)2—; R7is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(═O)R5; (CH2)kNR6C(═O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with 0 to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R9; or R7may be taken together with R8to form a cycloalkyl or heterocyclyl ring; or R7may be taken together with R11to form a cycloalkyl or heterocyclyl ring; and R8is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy.
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Chupak Louis S.
Duplantier Allen J.
Lau Wan F.
Milici Anthony J.
Benson Gregg C.
Desai Rita
Pfizer Inc
Richardson Peter C.
Ronau Robert T.
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