Cysteine protease inhibitors
First Claim
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1. A cysteine protease inhibitor of formula (I):
- ##STR12## wherein Z is a peptide or peptide mimetic cysteine protease binding moiety having between 2 and 5 amino acid residues or amino acid mimetics for between 1 and 5 amino acid residues, wherein the sum of the amino acid residues and the amino acid residues for which there is one or more amino acid mimetics is between 2 and 5 and the cysteine protease binding moiety is capable of binding to a cysteine protease;
R1 is alkyl or alkenyl, optionally substituted with 1-3 halo or hydroxy, alkylamino, dialkylamino, alkyldialkylamino, or cycloalkyl, alkylcycloalkyl, alkenylcycloalkyl, (C5 -C12) aryl;
(C5 -C12)arylalkyl or(C5 -C12)arylalkenyl, wherein the aryl groups of the arylalky or arylalkenyl comprises 0-4 heteroatoms selected from N, O and S, and are optionally substituted with halo, cyano, nitro, haloalkyl, amino, aminoalkyl, dialkylamino, alkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, carboxyl, carboalkoxy, alkylcarboxamide, (C5 -C6)aryl, --O--(C5 -C6)aryl, arylcarboxamide, alkylthio or haloalkylthio; and
one of Y and X is O and the other is N, said N being optionally substituted with alkyl or alkenyl optionally substituted with 1-3 halo atoms;
(C5 -C6) aryl, arylalkyl or arylalkenyl optionally comprising 1-3 heteroatoms selected from N, O and S, and optionally substituted with halo, cyano, nitro, haloalkyl, amino, aminoalkyl, dialkylamino, alkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, carboxyl, carboalkoxy, alkylcarboxamide, arylcarboxamide, alkylthio or haloalkylthio;
wherein at least one of Y or X is N;
ora pharmaceutically acceptable salt thereof.
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Abstract
The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R1 is optionally substituted alkyl or aryl.
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Citations
146 Claims
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1. A cysteine protease inhibitor of formula (I):
- ##STR12## wherein Z is a peptide or peptide mimetic cysteine protease binding moiety having between 2 and 5 amino acid residues or amino acid mimetics for between 1 and 5 amino acid residues, wherein the sum of the amino acid residues and the amino acid residues for which there is one or more amino acid mimetics is between 2 and 5 and the cysteine protease binding moiety is capable of binding to a cysteine protease;
R1 is alkyl or alkenyl, optionally substituted with 1-3 halo or hydroxy, alkylamino, dialkylamino, alkyldialkylamino, or cycloalkyl, alkylcycloalkyl, alkenylcycloalkyl, (C5 -C12) aryl;
(C5 -C12)arylalkyl or(C5 -C12)arylalkenyl, wherein the aryl groups of the arylalky or arylalkenyl comprises 0-4 heteroatoms selected from N, O and S, and are optionally substituted with halo, cyano, nitro, haloalkyl, amino, aminoalkyl, dialkylamino, alkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, carboxyl, carboalkoxy, alkylcarboxamide, (C5 -C6)aryl, --O--(C5 -C6)aryl, arylcarboxamide, alkylthio or haloalkylthio; andone of Y and X is O and the other is N, said N being optionally substituted with alkyl or alkenyl optionally substituted with 1-3 halo atoms;
(C5 -C6) aryl, arylalkyl or arylalkenyl optionally comprising 1-3 heteroatoms selected from N, O and S, and optionally substituted with halo, cyano, nitro, haloalkyl, amino, aminoalkyl, dialkylamino, alkyl, alkenyl, alkynyl, alkoxy, haloalkoxy, carboxyl, carboalkoxy, alkylcarboxamide, arylcarboxamide, alkylthio or haloalkylthio;wherein at least one of Y or X is N;
ora pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146)
- ##STR12## wherein Z is a peptide or peptide mimetic cysteine protease binding moiety having between 2 and 5 amino acid residues or amino acid mimetics for between 1 and 5 amino acid residues, wherein the sum of the amino acid residues and the amino acid residues for which there is one or more amino acid mimetics is between 2 and 5 and the cysteine protease binding moiety is capable of binding to a cysteine protease;
Specification