Inhibitors of NAALADase enzyme activity
First Claim
Patent Images
1. A compound having the following formula:
- ##STR13## where R is hydrogen, C1 -C9 straight or branched chain alkyl or alkenyl group, C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, or Ar1, wherein said alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl groups are optionally substituted with C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, C1 -C4 alkyl, C1 -C4 alkenyl, hydroxy, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched chain alkyl or alkenyl, C1 -C4 alkoxy, C1 -C4 alkenyloxy, phenoxy, benzyloxy, amino, or Ar1, and where Ar1 is selected from the group consisting of 1-naphthyl, 2-naphthyl, and phenyl, having one to three substituents which are independently selected from the group consisting of hydrogen, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched alkyl or alkenyl, C1 -C4 alkoxy or C1 -C4 alkenyloxy, phenoxy, benzyloxy, and amino;
or pharmaceutically acceptable salts or hydrates thereof.
4 Assignments
0 Petitions
Accused Products
Abstract
The present invention includes compounds, compositions, and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include phosphonate derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia and for treatment of prostate disease and prostate cancer by inhibition of NAALADase enzyme.
-
Citations
24 Claims
-
1. A compound having the following formula:
- ##STR13## where R is hydrogen, C1 -C9 straight or branched chain alkyl or alkenyl group, C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, or Ar1, wherein said alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl groups are optionally substituted with C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, C1 -C4 alkyl, C1 -C4 alkenyl, hydroxy, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched chain alkyl or alkenyl, C1 -C4 alkoxy, C1 -C4 alkenyloxy, phenoxy, benzyloxy, amino, or Ar1, and where Ar1 is selected from the group consisting of 1-naphthyl, 2-naphthyl, and phenyl, having one to three substituents which are independently selected from the group consisting of hydrogen, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched alkyl or alkenyl, C1 -C4 alkoxy or C1 -C4 alkenyloxy, phenoxy, benzyloxy, and amino;
or pharmaceutically acceptable salts or hydrates thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
- ##STR13## where R is hydrogen, C1 -C9 straight or branched chain alkyl or alkenyl group, C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, or Ar1, wherein said alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl groups are optionally substituted with C3 -C8 cycloalkyl, C3 or C5 cycloalkyl, C5 -C7 cycloalkenyl, C1 -C4 alkyl, C1 -C4 alkenyl, hydroxy, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched chain alkyl or alkenyl, C1 -C4 alkoxy, C1 -C4 alkenyloxy, phenoxy, benzyloxy, amino, or Ar1, and where Ar1 is selected from the group consisting of 1-naphthyl, 2-naphthyl, and phenyl, having one to three substituents which are independently selected from the group consisting of hydrogen, halo, hydroxyl, nitro, trifluoromethyl, C1 -C6 straight or branched alkyl or alkenyl, C1 -C4 alkoxy or C1 -C4 alkenyloxy, phenoxy, benzyloxy, and amino;
-
12. A compound selected from the group consisting of:
-
2- Methylhydroxyphosphinyl!oxy!pentanedioic Acid; 2- Ethylhydroxyphosphinyl!oxy!pentanedioic Acid; 2- Propylhydroxyphosphinyl!oxy!pentanedioic Acid; 2- Butylhydroxyphosphinyl!oxy!pentanedioic Acid; 2- Phenylhydroxyphosphinyl!oxy!pentanedioic Acid; 2- (Phenylmethyl)hydroxyphosphinyl!oxy!pentanedioic Acid; 2- ((2-Phenylethyl)methyl)hydroxyphosphinyl!oxy!pentanedioic Acid. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
-
Specification
-
- Resources
Litigation Campaign Assessment
Thank you for your request. You will receive a custom alert email when the Litigation Campaign Assessment is available.
×
-
Current AssigneeEisai Incorporated (Eisai Medical Research Incorporated)
-
Original AssigneeGuilford Pharmaceuticals Inc. (Eisai Medical Research Incorporated)
-
InventorsSlusher, Barbara S., Tays, Kevin L., Jackson, Paul F., Maclin, Keith M.
-
Primary Examiner(s)Rotman, Alan L.
-
Application NumberUS08/775,586Time in Patent Office595 DaysField of Search562/8, 562/24, 514/75US Class Current514/75CPC Class CodesA61K 31/194 having two or more carboxyl...A61K 31/661 Phosphorus acids or esters ...A61K 38/05 DipeptidesA61K 38/06 TripeptidesC07F 9/301 Acyclic saturated acids whi...C07F 9/4075 Esters with hydroxyalkyl co...C07F 9/4465 of aliphatic aminesC07F 9/58 Pyridine ringsC07F 9/65515 the oxygen atom being part ...C07F 9/6552 the oxygen atom being part ...
