Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
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Abstract
This invention relates to novel N-heterocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.
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Citations
82 Claims
- 1. A compound having the formula (I):
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5. The compounds, (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-hydroxymethylpyrrolidine;
- (2S)-1-(1,2-dioxo-3,3-dimethyl pentyl)-2-pyrrolidinetetrazole;
(2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarbonitrile; and
(2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-aminocarbonyl piperidine; and
compounds 1-25, 27, 28, 31-33, and 35-136 of Tables I, II, and III.
- (2S)-1-(1,2-dioxo-3,3-dimethyl pentyl)-2-pyrrolidinetetrazole;
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6. The compound 1-{2-[3-(4-Fluorophenyl)(1,2,4-oxadiazol-5-yl)]pyrrolidinyl}-3,3-di-methylpentane-1,2-dione.
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7. The compound 3,3-Dimehyl-1-[2-(3-methyl(1,2,4-oxadiazol-5-yl))pyrrolidinyl]pentane-1,2-dione.
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8. A pharmaceutical composition, comprising:
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a) an effective amount of an N-heterocyclic carboxylic acid or carboxylic acid isostere; and
b) a pharmaceutically acceptable carrier. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15)
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16. A method of treating a neurological disorder in an animal, comprising:
administering to the animal an effective amount of an N-heterocyclic carboxylic acid or carboxylic acid isostere to stimulate growth of damaged peripheral nerves or to promote neuronal regeneration. - View Dependent Claims (17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30)
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31. A method of stimulating growth of damaged peripheral nerves, comprising:
administering to damaged peripheral nerves an effective amount of an N-heterocyclic carboxylic acid or carboxylic acid isostere to stimulate or promote growth of the damaged peripheral nerves. - View Dependent Claims (32, 33, 34, 35, 36, 37, 38, 39)
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40. A method for promoting neuronal regeneration and growth in animals, comprising:
administering to an animal an effective amount of a N-heterocyclic carboxylic acid or carboxylic acid isostere to promote neuronal regeneration. - View Dependent Claims (41, 42, 43, 44, 45, 46, 47, 48)
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49. A method for preventing neurodegeneration in an animal, comprising:
administering to an animal an effective amount of a N-heterocyclic carboxylic acid or carboxylic acid isostere to prevent neurodegeneration. - View Dependent Claims (50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61)
- 62. A method for treating alopecia or promoting hair growth in an animal, which comprises administering to said animal an effective amount of an N-heterocyclic carboxylic acid or carboxylic acid isostere.
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69. A pharmaceutical composition comprising:
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(i) an effective amount of a N-heterocyclic carboxylic acid or carboxylic acid isostere for treating alopecia or promoting hair growth in an animal; and
(ii) a pharmaceutically acceptable carrier. - View Dependent Claims (70, 71, 72, 73, 74, 75)
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- 76. A method for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance in an animal, which comprises administering to said animal an effective amount of an N-heterocyclic carboxylic acid or carboxylic acid isostere.
Specification