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US 5,508,273 AGranted
Substituted phosphonic acids and derivatives useful in treating bone wasting diseases
AssigneeOrtho Pharmaceutical Corporation
InventorsScott Beers, Elizabeth A. Malloy, Charles Schwender
Life of this patent
Estimating the term…
Abstract
Compounds represented by the formula I: ##STR1## are disclosed as agents for use in treating bone wasting diseases.
Claims19
A compound represented by the general formula I:
- ##STR7## wherein R.sup.1 and R.sup.2 are the same or different and are selected from any of H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkyl NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are the same or different and selected from either C.sub.1 -C.sub.4 alkyl or H, or aralkyl wherein the alkyl portion has 1 carbon atom and the aryl portion is optionally independently substituted with any of halo, nitro, C.sub.1 -C.sub.2 alkyl or methylsulfonyl;
- wherein AR is selected from any of aryl or substituted aryl wherein the substituents are independently selected from any of C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, cyano, halo, hydroxy, nitro, phenoxy, phenyl, or trifluoromethyl;
- wherein R.sup.5 is independently selected from any of carboxyl, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalkyl, or aralkyl, wherein aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl, nitro, phenoxy, phenyl or trifluoromethyl;
- wherein R.sup.6 is selected from any of hydrogen, carboxy, carboalkoxy, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalky (C.sub.3 -C.sub.7), or aralkyl, where aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl, nitro, phenoxy, phenyl, or trifluoromethyl;
- or the optical isomers, enantiomers, diastereomers, or pharmaceutically acceptable salts thereof:
- with the proviso the following compounds are excluded from the definition of formula I;
- a) R.sup.1 R.sup.2 are alkyl, AR is phenyl or phenyl substituted by halo, alkoxy, alkyl, trifluoromethyl, R.sup.5 is carboxyl, phenyl, 1-naphthyl, substituted phenyl, 1-(4-NO.sub.2)-naphthyl, cyclopentyl or cyclohexyl, (CH2).sub.n Aryl where aryl is phenyl and n=1 or 2, and R.sup.6 =hydrogen and
- b) R.sup.1 R.sup.2 is hydrogen, AR is phenyl, R.sup.5 is carboxyl, phenyl or (CH2)nAryl where Aryl is phenyl and n=1 or 2, and R.sup.6 is hydrogen.
5 more elements
A pharmaceutical composition comprising the compound represented by the general formula I:
- ##STR8## wherein R.sup.1 and R.sup.2 are the same or different and are selected from any of H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkyl NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are the same or different and selected from either C.sub.1 -C.sub.4 alkyl or H, or aralkyl wherein the alkyl portion has 1 carbon atom and the aryl portion is optionally independently substituted with any of halo, nitro, C.sub.1 -C.sub.2 alkyl or methylsulfonyl;
- wherein AR is selected from any of aryl or substituted aryl wherein the substituents are independently selected from any of C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, cyano, halo, hydroxy, nitro, phenoxy, phenyl, or trifluoromethyl;
- wherein R.sup.5 is independently selected from any of carboxyl, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalkyl, or aralkyl, wherein aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl nitro, phenoxy, phenyl or trifluoromethyl;
- wherein R.sup.6 is selected from any of hydrogen, carboxy, carboalkoxy, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalky (C.sub.3 -C.sub.7), or aralkyl, where aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl, nitro, phenoxy, phenyl, or trifluoromethyl;
- or the optical isomers, enantiomers, diastereomers, or pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable carrier, said compound being present in a therapeutically effective amount for treating a bone wasting disease.
2 more elements
A method of treating a bone wasting disease comprising administering the compound represented by the general formula I:
- ##STR9## wherein R.sup.1 and R.sup.2 are the same or different and are selected from any of H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkyl NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are the same or different and selected from either C.sub.1 -C.sub.4 alkyl or H, or aralkyl wherein the alkyl portion has 1 carbon atom and the aryl portion is optionally independently substituted with any of halo, nitro, C.sub.1 -C.sub.2 alkyl or methylsulfonyl;
- wherein AR is selected from any of aryl or substituted aryl wherein the substituents are independently selected from any of C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, cyano, halo, hydroxy, nitro, phenoxy, phenyl, or trifluoromethyl;
- wherein R.sup.5 is independently selected from any of carboxyl, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalkyl, or aralkyl, wherein aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl, nitro, phenoxy, phenyl or trifluoromethyl;
- wherein R.sup.6 is selected from any of hydrogen, carboxy, carboalkoxy, C.sub.3 -C.sub.7 cycloalkyl, aryl, COaryl, COalkyl, COcycloalky (C.sub.3 -C.sub.7), or aralkyl, where aryl is phenyl, naphthyl or substituted aryl wherein the substituents are independently selected from any of amino, acylamino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.8 alkyl, carboxy, C.sub.1 -C.sub.4 carboalkoxy, cyano, halo, hydroxy, methylsulfonamido, methylsulfonyl, phenylsulfonamido, phenylsulfonyl, nitro, phenoxy, phenyl, or trifluoromethyl;
- or the optical isomers, enantiomers, diastereomers, or pharmaceutically acceptable salts thereof, to an animal afflicted with said disease in an amount effective for treating the bone wasting disease.
2 more elements
Dependencies are inferred from the claim text.