C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/03 (2006.01) A61K 38/06 (2006.01) C07K 5/02 (2006.01) C07K 7/02 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2077948
4-18787/A Abstract Further novel 5-amino-4-hydroxyhexanoic acid derivatives as therapeutic agents Described are compounds of the formula Image (1), wherein R1 is hydrogen, lower alkoxycarbonyl, heterocyclycarbonyl, benzyloxycarbonyl that is unsubstituted or substituted by up to three radicals which may be the same or different and are selected from fluorine, halo-lower alkyl, lower akanoyl, sulfo, lower alkylsulfonyl and cyano; heterocycloxycarbonyl wherein heterocyclyl is bonded by way of a carbon atom; one of the mentioned carbonyl radicals wherein the bonding carbonyl group has been replaced by a thiocarbonyl group; heterocyclylsulfonyl, lower alkyl- sulfonyl or N-(heterocyclyl-lower alkyl)-N-lower alkylaminocarbonyl, B1 is a bond or a bivalent radical of an .alpha.-amino acid, which radical is bonded N-terminally to R1 and C-terminally to the amino group at the R2-CH2-carrying carbon atom, each of R2 and R3, independently of the other, is phenyl or cyclohexyl, those radicals being unsubstituted or substituted by from one to three radicals which may be the same or different and are selected from hydroxy, loweralkoxy, halogen, halo-lower alkyl, sulfo, lower alkyl- sulfonyl, cyano and nitro, A1 is a bond between -C=O and A2 or is a bivalent radical of an .alpha.-amino acid, which radical is bonded N-terminally to the group -C=O and C-terminally to A2, A2 is a bivalent radical of an .alpha.-amino acid, which radical is bonded N-terminally to A1 and C-terminally to the group NR4R5, or A1 and A2 together form a bivalent radical of a dipeptide, of which the central amide bond is reduced and which is bonded N-terminally to the group -C=O and C-terminally to the group NR4R5, and R4 and R5, together with the bonding nitrogen atom, are unsubstituted or substituted thiomorpholino or morpholino, and the salts of those compounds if salt-forming groups are present, or hydroxy-protected derivatives thereof. Those HIV protease-inhibitors are used in the treatment of AIDS.
Bold Guido
Faessler Alexander
Lang Marc
Schneider Peter
Van Hoogevest Peter
Fetherstonhaugh & Co.
Novartis Ag
LandOfFree
Further novel 5-amino-4-hydroxyhexanoic acid derivatives as... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Further novel 5-amino-4-hydroxyhexanoic acid derivatives as..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Further novel 5-amino-4-hydroxyhexanoic acid derivatives as... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1571028