Renin inhibiting N-(2-amino-2-oxoethyl)butanediamide derivatives
US5541163A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 17, 1993 |
| Grant date | Jul 30, 1996 |
| Priority date | — |
| Expiry date | Sep 17, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D295/215
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Disclosed herein are compounds of the formula: EQU A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--B wherein A is R.sup.3 R.sup.4 NC(O)CH.sub.2 wherein, for example, R.sup.3 is hydrogen or alkyl and R.sup.4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.