Claims
- 1. An alkyl carboxy amino acid ester compound having the following formula:
- 2. The compound of claim 1 wherein
R1 is CH3; wherein R2 is H; wherein R3 and R4 are independently
1) H 2) C1-C6-alkyl, 3) C3-C4-alkenyl, 4) C3-C5-cycloalkyl, 5) C1-C6-alkyl-CO—, 6) C1-C6-alkyl-OCO—, 7) C1-C6-alkyl-NHCO—, 8) HCO—, or R3 and R4 taken together can be —CH2(CH2)nCH2— in which n is an integer selected from the group consisting of 0, 1, 2 and 3; and wherein R5 and R6 are independently
1) C1-C6-alkyl, 2) C3-C4-alkenyl, or 3) C3-C5-cycloalkyl; and pharmaceutically acceptable salts of these compounds.
- 3. The compound of claim 2 wherein
R3 and R4 taken together can be —CH2(CH2)nCH2— in which n is an integer selected from the group consisting of 0, 1, 2 and 3; and pharmaceutically acceptable salts of these compounds.
- 4. The compound of claim 1 selected from the group consisting of:
(2S,4R)-4-methyl glutamic acid dimethyl ester; (2S,4R)-4-methyl glutamic acid diethyl ester; (2S,4R)-4-methyl glutamic acid di-tert-butyl ester; (2R,4S)-4-methyl glutamic acid dimethyl ester; (2R,4S)-4-methyl glutamic acid diethyl ester; and (2R,4S)-4-methyl glutamic acid di-tert-butyl ester.
- 5. A pharmaceutical composition comprising
a compound for selectively modulating ion flow through the kainate receptor in combination with a pharmaceutically acceptable carrier for administration to a patient in need thereof, wherein the compound is an alkyl carboxy amino acid compounds having the formula: 4wherein
R1, R2, R5 and R6 are independently 1) C1l-C6-alkyl, 2) C3-C4-alkenyl, 3) C3-C5-cycloalkyl; R3 and R4 are independently
1) H 2) C1-C6-alkyl, 3) C3-C4-alkenyl, 4) C3-C5-cycloalkyl, 5) C1-C6-alkyl-CO— 6) C1-C6-alkyl-OCO— 7) C1-C6-alkyl-NHCO— 8) HCO—, or 9) C3-C6-alkynyl; R3 and R4 taken together can be —CH2(CH2)nCH2—; n is 0-3; and pharmaceutically acceptable salts of these compounds.
- 6. The composition of claim 5 wherein
R1 is CH3; wherein R2 is H; wherein R3 and R4 are independently
1) H 2) C1-C6-alkyl, 3) C3-C4-alkenyl, 4) C3-C5-cycloalkyl, 5) C1-C6-alkyl-CO—, 6) C1-C6-alkyl-OCO—, 7) C1-C6-alkyl-NHCO—, 8) HCO—, or R3 and R4 taken together can be —CH2(CH2)nCH2— in which n is an integer selected from the group consisting of 0, 1, 2 and 3; and wherein R5 and R6 are independently
1) C1-C6-alkyl, 2) C3-C4-alkenyl, or 3) C3-C5-cycloalkyl; and pharmaceutically acceptable salts of these compounds.
- 7. The composition of claim 6 wherein
R3 and R4 taken together can be —CH2(CH2)nCH2—in which n is an integer selected from the group consisting of 0, 1, 2 and 3; and pharmaceutically acceptable salts of these compounds.
- 8. The composition of claim 5 selected from the group consisting of:
(2S,4R)-4-methyl glutamic acid dimethyl ester; (2S,4R)-4-methyl glutamic acid diethyl ester; (2S,4R)-4-methyl glutamic acid di-tert-butyl ester; (2R,4S)-4-methyl glutamic acid dimethyl ester; (2R,4S)-4-methyl glutamic acid diethyl ester; and (2R,4S)-4-methyl glutamic acid di-tert-butyl ester. and pharmaceutically acceptable salts of these compounds.
- 9. A method for treating a patient having a disorder associated with excessive or insufficient activation of the kainate subtype of the ionotropic EAA receptors comprising administering to the patient an effective amount of the pharmaceutical composition of claim 5 to alleviate the symptoms of the disorder.
- 10. The method of claim 9 wherein the disorder is selected from the group consisting of neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders.
- 11. The method of claim 9 wherein the disorder is pain comprising administering to the patient an effective amount of the pharmaceutical composition to alleviate the pain.
- 12. The method of claim 9 wherein the disorder is selected from the group of cognitive disorders associated with deactivation, suboptimal activation, and over-activation of the kainate receptor.
- 13. The method of claim 9 wherein the disorder is a decrease or loss of memory, learning, or associated mental processes comprising administering to the patient an effective amount of the pharmaceutical composition to enhance or increase cognition.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] Priority is claimed to U.S. Provisional application Ser. No. 60/244,411, filed Oct. 30, 2000, the teachings of which are incorporated herein.
Provisional Applications (1)
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Number |
Date |
Country |
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60244411 |
Oct 2000 |
US |