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US 4,757,050 AGranted
Ureido renin inhibitors
AssigneeE. R. Squibb & Sons, Inc.
InventorsSesha I. Natarajan, Denis E. Ryono, Edward W. Petrillo, Jr.
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## are disclosed. These compounds intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as antihypertensive agents.
Claims20
A compound of the formula ##STR128## including a pharmaceutically acceptable salt thereof wherein:
- X is ##STR129## R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.9 are independently selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, --(CH.sub.2).sub.n -aryl, --(CH.sub.2).sub.n -heterocyclo, --(CH.sub.2).sub.n --OH, --(CH.sub.2).sub.n --NH.sub.2, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S-lower alkyl, --(CH.sub.2).sub.n --O-lower alkyl, --(CH.sub.2).sub.n --O--(CH.sub.2).sub.g --OH, --(CH.sub.2).sub.n --O--(CH.sub.2).sub.g --NH.sub.2, --(CH.sub.2).sub.n --S--(CH.sub.2).sub.g --OH, ##STR130## R.sub.2 is hydrogen, lower alkyl, --(CH.sub.2).sub.m -aryl, --(CH.sub.2).sub.m -cycloalkyl, or --(CH.sub.2).sub.n -heterocyclo;
- R.sub.6 and R'.sub.6 are independently selected from the group consisting of lower alkyl, cycloalkyl, aryl and heterocyclo;
- p is zero or one;
- m and m' are independently selected from the group consisting of zero and an integer from 1 to 5;
- n is an integer from 1 to 5;
- g is an integer from 2 to 5;
- R.sub.7 is ##STR131## R.sub.8 is 2,4-dinitrophenyl, ##STR132## q is zero or one;
- R.sub.10 is hydroxy, --O-lower alkyl, --O--(CH.sub.2).sub.m -cycloalkyl, --O--(CH.sub.2).sub.m -aryl, --O--(CH.sub.2).sub.n -heterocyclo, --NH.sub.2, or --O-salt forming ion;
- the term lower alkyl refers to straight or branched chain radicals having up to seven carbon atoms;
- the term cycloalkyl refers to saturated rings of 4 to 7 carbon atoms;
- the term halo refers to Cl, Br, and F;
- the term halo substituted lower alkyl refers to such lower alkyl groups in which one or more hydrogens have been replaced by chloro, bromo or fluoro groups;
- the term aryl refers to phenyl, 1-naphthyl, 2-naphthyl, mono substituted phenyl, 1-naphthyl, or 2-naphthyl wherein said substituent is lower alkyl of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, halogen, hydroxy, amino, --NH-alkyl wherein alkyl is of 1 to 4 carbons, or --N(alkyl).sub.2 wherein alkyl is of 1 to 4 carbons, di or tri substituted phenyl, 1-naphthyl or 2-naphthyl wherein said substituents are methyl, methoxy, methylthio, halogen or hydroxy;
- and
- the term heterocyclo refers to fully saturated or unsaturated rings of 5 or 6 atoms containing one or two O or S atoms and/or one to four N atoms provided that the total number of hetero atoms in the ring is 4 or less and bicyclic rings wherein the five or six membered ring containing O, S and N atoms as defined above is fused to a benzene ring.
12 more elements
Dependencies are inferred from the claim text.