Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof
US5536737A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 24, 1995 |
| Grant date | Jul 16, 1996 |
| Priority date | — |
| Expiry date | May 24, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D277/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof. The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.