Patent ID: 7691896

Claim:
Nucleophilic substituted analogs of Salinosporamide A, having the Formula Ia: wherein: R 1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, n-butyl, iso-butyl, and tert-butyl, each optionally substituted by halogen R 2 is selected from the group consisting of substituted or unsubstituted C 1 -C 8 alkyl, substituted or unsubstituted C 2 -C 8 alkenyl, substituted or unsubstituted C 2 -C 8 alkynyl, substituted or unsubstituted, saturated or unsaturated, C 3 -C 8 cycloalkyl, benzyl and substituted benzyl; wherein the substituent groups are independently selected from the group consisting of C 1 -C 4 alkoxy, amido, halogen and aryl; and Nu is a Nucleophile selected from the group consisting of: carb-sulfides having the formula RS— wherein R can be substituted or unsubstituted C 1 -C 8 alkyl, substituted or unsubstituted C 2 -C 8 alkenyl, substituted or unsubstituted C 2 -C 8 alkynyl, substituted or unsubstituted, saturated or unsaturated, C 3 -C 8 cycloalkyl, benzyl and substituted benzyl; wherein the substituent groups are independently selected from the group consisting of C 1 -C 4 alkoxy, amido, halogen and aryl; cyanide having the formula CN—; azide having the formula N 3 —; carboxylates having the formula RCO 2 —, wherein R can be substituted or unsubstituted C 1 -C 8 alkyl, substituted or unsubstituted C 2 -C 8 alkenyl, substituted or unsubstituted C 2 -C 8 alkynyl, substituted or unsubstituted, saturated or unsaturated, C 3 -C 8 cycloalkyl, benzyl and substituted benzyl; wherein the substituent groups are independently selected from the group consisting of C 1 -C 4 alkoxy, amido, halogen and aryl; substituted C 1 -C 8 alkyl; substituted or unsubstituted C 2 -C 8 alkenyl; substituted or unsubstituted C 2 -C 8 alkynyl; substituted or unsubstituted, saturated or unsaturated, C 3 -C 8 cycloalkyl; benzyl and substituted benzyl; wherein the substituent groups for each are independently selected from the group consisting of C 1 -C 4 alkoxy, amido, halogen and aryl; and NH 3 , hydrazine, water, polyamines, polyols, amino alcohols, amino thiols, dithiols, thioacetamides, acetamidine, carbon monoxide, carbonate having the formula CO 3 , acetate having the formula CH 3 CO; and dithiocarbamates.