Proline derivatives and compositions for their use as inhibitors of HIV protease
AssigneeMiles Inc.
InventorsRudolf H. Hanko, Thomas Gould, Paul P. Tamburini
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Abstract
The present disclosure describes novel peptidomimetic compounds which contain a novel class of isosteres and which inhibit the proteolytic activity of HIV protease and further describes therapeutic compositions comprising said compounds, a method of treatment for patients having the AIDS virus involving administering a therapeutically effective amount of the novel compounds of the present invention, and a method of preparation for said isosteres.
Claims12
A compound selected from the group consisting of:
- (2S, 3S) N-methyl 2-(3-carbobenzyloxyamino-5-methyl-hexanoyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR25## (2R, 3R) N-methyl 2-(3-carbobenzyloxyamino-5-methyl-hexanoyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR26## (2S, 3S) N-[2-(3-carbobenzyoxyamino-5-methyl hexan-1olyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR27## (2R, 3R) N-[2-(3-carbobenzoxyamino-5-methyl hexan-1-olyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR28## (2S, 3S) N-[methyl 2-(3-(N-carbobenzyloxy-.beta.-cyano-alanyl) amino-5-methyl-hexanoyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR29## (2S, 3S) N-[methyl 2-3-(N-carbobenzyloxy-asparaginyl) amino-5-methyl-hexanoyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR30## (2S, 3S) N-[2-(3-N-carbobenzyloxy-asparginyl)amino-5-methyl hexan-1-olyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR31## (2S, 3S) N-]methyl 2-(3-N-guinaldyl-asparginyl)amino-5-methyl-hexanoyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR32## (2S, 3S) N-[2-(3-(N-guinaldyl-asparginyl)amino-5-methyl hexan-1-olyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR33## (2R, 3R) N-[2-(3-(N-guinaldyl-asparginyl)amino-5-methyl hexan-1-olyl)]-prolyl-isoleucine N-benzyl amide of the formula ##STR34##
The compound (2S, 3S) N-[methyl 2-(3-carbobenzyloxyamino-5-methyl-hexanoyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR35##
The compound (2R, 3R) N-[methyl 2-(3-carbobenzyloxyamino-5-methyl-hexanoyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR36##
The compound (2S, 3S) N-[2-(3-carbobenzyoxyamino-5-methyl hexan-1-olyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR37##
The compound (2R, 3R) N-[2-(3-carbobenzoxyamino-5-methyl hexan-1-olyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR38##
The compound (2S, 3S) N-[methyl 2-(3-(N-carbobenzyloxy-.beta.-cyano-alanyl) amino-5-methyl-hexanoyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR39##
The compound (2S, 3S) N-[methyl 2-3-(N-carbobenzyloxy-asparaginyl) amino-5-methyl-hexanoyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR40##
The compound (2S, 3S) N-[2-(3-(N-carbobenzyloxy-asparaginyl)amino-5-methyl hexan-1-olyl)]-Prolyl-leucine N-Benzyl amide of the formula:
- ##STR41##
The compound (2S, 3S) N-[methyl 2-(3-(N-quinaldyl-asparaginyl)amino-5-methyl-hexanoyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR42##
The compound (2S, 3S) N-[2-(3-(N-quinaldyl-asparaginyl) amino-5-methyl hexan-1-olyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR43##
The compound (2R, 3R) N-[2-(3-(N-quinaldyl-asparaginyl) amino-5-methyl hexan-1-olyl)]-Prolyl-Isoleucine N-Benzyl amide of the formula:
- ##STR44##
Dependencies are inferred from the claim text.