Dipeptide compounds containing histidine or N-methyl histidine processes for their preparation and compositions containing them
US5057496A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 6, 1988 |
| Grant date | Oct 15, 1991 |
| Priority date | — |
| Expiry date | Dec 6, 2008 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/0207
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group; PA1 X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ; PA1 X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--; PA1 R.sup.2 represents a C.sub.4-6 cycloalkyl group; PA1 R.sup.3 represents a group CHR.sup.6 R.sup.7 (where R.sup.6 is a hydrogen atom or a hydroxyl group and R.sup.7 is a pyridinyl ring); PA1 X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups; PA1 R.sup.4, and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring; PA1 and salts and solvates thereof. The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency. Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.