Patent ID: 6342519
Filing Date: 2002-01-29
Classification: A61K,C07D

Abstract:
A novel oxetanone derivative of the formula: wherein:t is an integer from 0 to 1 X-L-Q is an ether or amino linkage wherein: X of the ether or amino is a linking group, L is â€”Oâ€” or â€”NHâ€”, and Q of the ether or amino linkage is a polysaccharide of a sufficient molecular weight or property that such polysaccharide is not absorbed by the digestive system of a mammal such as a dog, cat, non-human primate or a human primate; R is a member selected from the group consisting of: a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by up to eight double or triple bonds; a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by one or more members selected from the group consisting of an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group; a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by up to eight double or triple bonds and is substituted in a position other than alpha to an unsaturated carbon atom by one or more members selected from the group consisting of an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group atoms; phenyl substituted by 0-4 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; benzyl substituted by 0-4 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; biphenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C-1-6-alkyl-SH; phenoxyphenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; phenylthiophenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; and phenyl-C1-6-alkyl-phenyl wherein 0-6 hydrogen atoms on one or more of the phenyl ring and â€”C1-6-alkyl- group is/are replaced independently by a member selected from the group consisting ofâ€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; R1 is a member selected from the group consisting of: Hydrogen, Ar, Ar-C1-5-alkyl and C1-10-alkyl substituted by 0-3 members independently selected from the group consisting of an oxygen atom, a sulfur atom, a sulfinyl group, a sulfonyl group, a-N(â€”R4)â€” group, a â€”C(&boxH;O)â€”N(â€”R4)â€” group, and a â€”N(â€”R4)â€”C(&boxH;O)â€” group, wherein 0-3 carbon atoms of the C1-10-alkyl group can be substituted independently by a member selected from the group consisting of a hydroxy group, thiol group, C1-10-alkoxy group, a C1-10-alkylthio group, a â€”N(â€”R5,â€”R6) group, a â€”C(&boxH;O)â€”N(â€”R7, â€”R8) group, and a â€”N(â€”R9)â€”C(&boxH;O)â€”R10 group; R2 is a member selected from the group consisting of: hydrogen and C1-6-alkyl, or R2 taken with R1 forms a 4-6 membered saturated ring containing 0-4 nitrogen atoms wherein the ring may be substituted by 0-4 R11 groups; R3 is a member selected from the group consisting of: a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by up to eight double or triple bonds; a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by one or more members selected from the group consisting of an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group; a straight or branched chained C1-17-alkyl group which is saturated or optionally substituted by up to eight double or triple bonds and is substituted in a position other than alpha to an unsaturated carbon atom by one or more members selected from the group consisting of an oxygen atom, a sulfur atom, a sulfonyl group or a sulfinyl group atoms; phenyl substituted by 0-4 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; benzyl substituted by 0-4 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; biphenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; phenoxyphenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; phenylthiophenylene substituted by 0-6 members selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; and phenyl-C1-6-alkyl-phenyl wherein 0-6 hydrogen atoms on one or more of the phenyl ring and â€”C1-6-alkyl- group is/are replaced independently by a member selected from the group consisting of â€”C1-6-alkyloxy-C1-6-alkyl, â€”C1-6-alkylthio-C1-6-alkyl, â€”C1-6-alkyl-OH and â€”C1-6-alkyl-SH; R4-R10 are each independently a member selected from the group consisting of: hydrogen and C1-6-alkyl; n is an integer of 0-3; or a pharmaceutically acceptable isomer, and salt thereof.