Claims
- 1. A compound of the formula ##STR11## wherein X and Y independently represent carboxy or carboxy esterified in form of a pharmaceutically acceptable ester; R and R.sub.o independently represent aryl-lower alkyl in which aryl represents biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acylamino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; or a pharmaceutically acceptable salt of any said compound with a salt-forming group.
- 2. A compound according to claim 1 of the formula ##STR12## wherein A, X, Y, R and R.sub.o have meaning as defined in said claim; or a pharmaceutically acceptable salt of any said compound with a salt-forming group.
- 3. A compound according to claim 1 of the formula ##STR13## wherein R.sub.1 and R.sub.2 independently represent aryl-lower alkyl in which aryl represents biphenyl or naphthyl each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acylamino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, hydroxy, lower alkoxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; a mono- or bis-carboxylic acid derivative selected from a (C.sub.1 -C.sub.20)alkyl ester; an (amino, acylamino, mono- or di-lower alkylamino, carboxy or lower carboalkoxy)-substituted lower alkyl ester; an aryl-(lower) alkyl ester in which aryl represents optionally substituted phenyl or pyridyl; a lower alkanoyloxy-(lower alkyl ester; a 3-phthalidyl or (lower alkyl, lower alkoxy or halo)-substituted 3-phthalidyl ester; a (hydroxy, lower alkanoyloxy or lower alkoxy)-substituted lower alkoxymethyl ester; a bicycloalkyloxycarbonyl-lower alkyl ester having up to 10 carbon atoms in the bicycloalkyl group; a 1-(lower alkoxycarbonyloxy)-lower alkyl ester; a 3-cholestanyl or 3-cholestenyl ester; a monosaccharidyl or protected monosaccharidyl ester; and a polyhydroxy-lower alkyl or protected polyhydroxy-lower alkyl ester; or a pharmaceutically acceptable salt of any said compound with a salt forming group.
- 4. A compound according to claim 3 of formula II wherein R.sub.1 and R.sub.2 represent 2-(2-naphthyl)-ethyl and A represents --CH.sub.2 --CH.sub.2 --; or a pharmaceutically acceptable salt thereof.
- 5. A compound according to claim 3 of formula II wherein R.sub.1 and R.sub.2 represent 4-biphenylmethyl and A represents --CH.sub.2 CH.sub.2 CH.sub.2 --; or a pharmaceutically acceptable salt thereof.
- 6. An enkephalinase inhibiting pharmaceutical composition for administration to mammals comprising an effective amount of a compound of claim 1 in combination with one or more pharmaceutical carriers.
- 7. A method of inhibiting enkephalinase activity in mammals which comprises administering to a mammal in need thereof an effective amount of a compound of claim 1 or of a pharmaceutical composition comprising said compound in combination with one or more pharmaceutical carriers.
- 8. A method of treating conditions responsive to inhibition of enkephalinase in mammals which comprises administering to a mammal in need thereof an effective amount of a compound of claim 1 or of a pharmaceutical composition comprising said compound in combination with one or more pharmaceutical carriers.
- 9. A method according to claim 8 of treating pain, psychotic disorders or hypertension.
CROSS-REFERENCE TO RELATED APPLICATION
This is a divisional of application Ser. No. 098,755 filed on Sept. 17, 1987, now U.S. Pat. No. 4,939,261, which is a continuation of application Ser. No. 772,067, filed Sept. 9, 1985, now abandoned, which is a continuation-in-part of application Ser. No. 618,617 filed June 8, 1984, now abandoned.
US Referenced Citations (6)
Divisions (1)
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Number |
Date |
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Parent |
98755 |
Sep 1987 |
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Continuations (1)
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Number |
Date |
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Parent |
772067 |
Sep 1985 |
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Continuation in Parts (1)
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Number |
Date |
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Parent |
618617 |
Jun 1984 |
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