Peptides capable of inhibiting the activity of hiv protease,...

Details Peptides capable of inhibiting the activity of hiv protease,... Peptides capable of inhibiting the activity of hiv protease,...

C - Chemistry, Metallurgy

07

K

C07K 5/02 (2006.01) A61K 31/395 (2006.01) A61K 38/04 (2006.01) C07D 205/04 (2006.01) C07D 207/16 (2006.01) C07D 207/22 (2006.01) C07D 207/24 (2006.01) C07D 207/28 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 487/08 (2006.01) C07D 491/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2103536

ABSTRACT OF THE DISCLOSURE Compounds of formula (I): Image (I) [wherein: R1 is hydrogen, alkyl, aralkyl, -CORa, -CORb, -CSRa, -CSRb, -SO2Rb, -CONHRb, -CSNHRb, -CONRbRb or -CSNRbRb; R2 is hydrogen or alkyl; R3 is hydrogen, alkylidene, substituted alkyl, or Rb; R4 is optionally substituted alkyl, cycloalkyl, or aryl; R5 is RbO-, RbRbN-, RbHN-, aralkyloxycarbonyloxy or aralkyl- oxycarbonylamino, or R5 is -(CH2)p-D-(CH2)r- [where D is a single bond, carbonyl, oxygen, sulfur, -NH-, -(CH2=CH2)- or -NHCO-; and p and r are each 0 or an integer from 1 to 5]; A is -(CH2)m-B-(CH2)n- [where B is a single bond, carbonyl, oxygen, sulfur, -NH-, -(CH2=CH2)- or -NHCO-; and m and n are each 0 or an integer from 1 to 5]; Ra is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; Rb is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl or arylalkenyl]; and pharmaceutically acceptable salts and esters thereof and pro-drugs therefor, have the ability to inhibit the activity of HIV protease and may thus be used for the treatment and prophylaxis of AIDS.

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