N-[(S)-2-(N'-Acetyl-hydrazino)-1-benzyl-2-oxo-ethyl]-2-amino-acetamide 、 BOC-D-蛋氨酸砜 以the desired compound (0.67 g) is obtained in a similar manner to (III)of Example 45的产率得到BOC-(D)-Met(O2)-Gly-Phe-NHNH-COCH3
[EN] C-28 AMINES OF C-3 MODIFIED BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS<br/>[FR] AMINES EN C28 DE DÉRIVÉS D'ACIDE BÉTULINIQUE MODIFIÉ EN C-3 EN TANT QU'INHIBITEURS DE MATURATION DU VIH
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012106188A1
公开(公告)日:2012-08-09
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof: a compound of formula (I), a compound of formula (II), and a compound of formula (III).
C-28 AMINES OF C-3 MODIFIED BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS
申请人:Regueiro-Ren Alicia
公开号:US20130029954A1
公开(公告)日:2013-01-31
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof:
a compound of formula I
a compound of formula II
and a compound of formula III
Novel tetrapeptidehydrazide derivatives, inclusive of a pharmacologically acceptable acid addition salt thereof, which has the general formula (I): ##STR1## [wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or the side chain of a D-.alpha.-amino acid; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, or a saturated or unsaturated and straight or branched lower aliphatic acyl group which may optionally be substituted by hydroxy, amino, lower alkoxy, halogen, oxo, lower alkylthio or lower alkylthiooxide], are useful as analgesics.