Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-05-09
2006-05-09
Kifle, Bruck (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C540S461000
Reexamination Certificate
active
07041696
ABSTRACT:
The present invention relates to interleukin-1β converting enzyme inhibitors having the formula:R is a carbocyclic or heterocyclic ring;R1is a cysteine trap;R2a, R2a′, R2b, and R2b′are each independently hydrogen, C1–C4alkyl, C1–C4alkoxy, and mixtures thereof; or R2a′and R2b′can taken together to form a double bond;L and L1are linking groups having the formula:T is selected from the group consisting of:i) —NR6—;ii) —O—;iii) —NR6S(O)2—;iv) —S(O)2NR6—; andv) mixtures thereof;R6is hydrogen, substituted or unsubstituted C1–C20linear, branched, or cyclic alkyl, C6–C20aryl, C7–C20alkylenearyl, and mixtures thereof; the indices w, w1, and w2are each independently 0 or 1;i) hydrogen;ii) C1–C4linear, branched, and cyclic alkyl;iii) R3aand R3bor R4a, and R4bcan be taken together to form a carbonyl unit;iv) two R3aor two R3bunits from adjacent carbon atoms or two R4aor two R4bunits from adjacent carbon atoms can be taken together to form a double bond; andv) mixtures thereof;the index m is from 0 to 5; the index n is from 0 to 5.
REFERENCES:
Thorsett, E.D., “Conformationally Restricted Inhibitors of Angiotensin Converting Enzyme”,Actualites de Chimie Therapeutique, 1986, vol. 13, pp. 257-268.
Beal, L.M. et al., “A Sequential Electrochemical Oxidation—Olefin Metathesis Strategy for the Construction of bicyclic Lactam Based Peptidomimetics”,Tetrahedron Letters, 1998, vol. 39, pp. 4639-4642.
Grossmith, C.E. et al., “Synthesis of Novel Unsaturated Bicyclic Lactams by Ring-Closing Metathesis”,Synlett, 1990, No. 10, pp. 1660-1662.
Chen Jian
De Biswanath
Demuth, Jr. Thomas Prosser
Laufersweiler Michael Christopher
O'Neil Steven Victor
Echler Sr. Richard S.
Kifle Bruck
The Procter & Gamble & Company
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