Tight-binding inhibitors of leukotriene A.sub.4 hydrolase
US5455271A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 17, 1993 |
| Grant date | Oct 3, 1995 |
| Priority date | — |
| Expiry date | Jun 17, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C327/42
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Inhibitors of leukotriene A.sub.4 hydrolase are disclosed, corresponding to Formula I, below: ##STR1## wherein the depicted --NH.sub.2 group is in the (S) configuration; --W is --CH.sub.2 SH, --CH.sub.2 NH.sub.2 or C(.dbd.Z)--Y, wherein .dbd.Z is .dbd.O, or --H and --OH; and --Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C.sub.1 -C.sub.6 alkylenecarboxyl, (f) C.sub.1 -C.sub.6 alkyl, (g) C.sub.2 -C.sub.6 alkenyl, (h) C.sub.1 -C.sub.6 alkylenephenyl and (i) --C(.dbd.O)--X--R.sup.1 wherein X is O or NH and, R.sup.1 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylenecarboxyl, and benzyl; R.sup.2 is hydrogen, benzyloxy or 2-naphthylmethyloxy, and a pharmaceutically acceptable acid addition salt thereof. Inhibitors wherein --W is --CH.sub.2 SH, --CH.sub.2 NH.sub.2 or C(.dbd.Z)--Y wherein .dbd.Z is .dbd.O and --Y is --C(.dbd.O)--X--R.sup.1 are particularly preferred, as are those compounds wherein .dbd.Z is .dbd. O and --Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C.sub.1 -C.sub.6 alkylenecarboxyl, (f) C.sub…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.