Aica riboside analogs

Details Aica riboside analogs Aica riboside analogs

C - Chemistry, Metallurgy

07

H

C07H 19/052 (2006.01) A61K 31/415 (2006.01) A61K 31/675 (2006.01) A61K 31/70 (2006.01) C07D 233/88 (2006.01) C07D 233/90 (2006.01) C07F 9/6506 (2006.01)

Patent

CA 2067151

Analogs of 5-amino-1-beta-D-ribofuranosylimidazole-4-carboxamide (AICA riboside) are provided which are useful in increasing extracellular levels of adenosine. The analogs have the formula of: (see formula I) or a pharmaceutically acceptable salt thereof wherein X is -O- or -CH2-; R1 is hydrogen, amino, hydrocarbylamino, acylamino or dihydrocarbylaminoalkyleneimino; R2 is hydrogen, cyano, hydrocarbylimidate, carboxamidoxime, hydrocarbyloxyamidine, carboxamide, or carboxylic acid or an amide; a carboxyester having the formula -C(=O)OR', wherein R' is (C1-C6) alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C14)aryl, (C1-C4)alkyl- (C6-C10)aryl, or (C6-C14)cycloalkyl, the (C6-C19)cycloalkyl being optionally substituted by one or more (C6-C14)aryl groups; a thioester having the formula -C(=O)SR', wherein R' is as defined above; or a salt thereof, or R2 is a group of the formula: (see formula II) wherein alk is alkylene of 2 to 8 carbon atoms; R3 is hydrogen, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C6-C14) aryl, (C1-C4) alkyl- (C6-C10) aryl, or (C6-C14) cycloalkyl, the (C6-C14)cycloalkyl being optionally substituted by one or more (C6-C14)aryl groups, amino, hydrocarbylamino, halogen, hydroxy, hydrocarbyloxy, sulfhydryl, or hydrocarbylthio; R4 and R5 are independently hydrogen, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C6-C14) aryl, (C1-C4) alkyl- (C6-C10)aryl, or (C6-C14) cycloalkyl, the (C6-C14) cycloalkyl being optionally substituted by one or more (C6-C14)aryl groups, acyl having the formula -C(=O)R' wherein R' is as defined above, or hydrocarbyloxycarbonyl; R6 is hydrogen, (C1-C6)alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, (C6-C14) aryl, (C1-C4) alkyl-(C6-C10) aryl, or (C6-C14) cycloalkyl, the (C6-C14) cycloalkyl being optionally substituted by one or more (C6-C14)aryl groups, halogen, hydroxy, hydrocarbyloxy, sulfhydryl, hydrocarbylthio, sulfamyloxy, amino, hydrocarbylamino, azido, acyloxy or hydrocarbyloxycarboxy or a phosphate ester group or a salt thereof; provided that when R1 is amino, R2 is unsubstituted carboxamide, R3 is hydrogen; R4 and R5 are hydrogen, acyl having the formula -C(=O)R' wherein R' is as defined above, or hydrocarbyloxycarbonyl; then R6 is not hydroxy, acyloxy or hydrocarbyloxycarboxy.

Affiliated with

Also associated with

Rating

Aica riboside analogs does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Aica riboside analogs, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Aica riboside analogs will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1474476