Cysteine protease inhibitors effective for in vivo use
US5374623A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 20, 1992 |
| Grant date | Dec 20, 1994 |
| Priority date | — |
| Expiry date | Aug 20, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C279/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A method of treating medical conditions with proteinase inhibitors of the formula: ##STR1## wherein B is H or an amino acid blocking group for the N-terminal amino acid nitrogen; PA1 R.sub.1 is an optionally protected .alpha.-amino acid side chain such that P.sub.2 is the residue of an .alpha.-amino acid selected from the group consisting of phenylalanine (Phe), leucine (Leu), tyrosine (Tyr) and valine (Val), and substituted analogs thereof, particularly including Tyr(OMe); PA1 R.sub.2 is an optionally protected .alpha.-amino acid side chain such that P.sub.1 is the residue of an .alpha.-amino acid selected from the group consisting of alanine (Ala), arginine (Arg), aspartic acid (Asp), glutamic acid (Glu), histidine (His), homophenylalanine (HPhe), phenylalanine (Phe), ornithine (Orn), serine (Ser) and threonine (Thr), and substituted analogs thereof; PA1 X is a fluorine-free leaving group selected from the group consisting of phenoxy, substituted phenoxy and heterophenoxy; PA1 E and G are one or more atoms more electronegative than carbon; and PA1 D is hydrogen, methyl or a substituted methyl.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.