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US 2003/0119858 A1Published application
Conformationally constrained compounds as pharmaceutical agents
OwnerJustin Stephen Bryans, David Christopher Horwell +1inventors
InventorsJustin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
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Abstract
Novel substituted amino acids of formula 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Claims19
A compound of formula
- 17
- or a pharmaceutically acceptable salt thereof or a prodrug thereof wherein
- R1 to R10 are each independently selected from hydrogen or a straight or branched alkyl of from 1 to 6 carbons, benzyl, or phenyl;
- m is an integer of from 0 to 3;
- n is an integer of from 1 to 2;
- o is an integer of from 0 to 3;
- p is an integer of from 1 to 2;
- q is an integer of from 0 to 2;
- r is an integer of from 1 to 2;
- s is an integer of from 1 to 3;
- t is an integer of from 0 to 2;
- and
- u is an integer of from 0 to 1.
10 more elements
A compound selected from:
- 2-Benzyl-2-aza-spiro[4.5]decane-4,4-dicarboxylic acid dimethyl ester hydrochloride;
- 2-Aza-spiro[4.5]decane-4,4-dicarboxylic acid dimethyl ester hydrochloride;
- 1-Benzyloxymethyl-2-aza-spiro[3.5]nonane-2-carboxylic acid tert-butyl ester;
- 1-Hydroxymethyl-2-aza-spiro[3.5]nonane-2-carboxylic acid tert-butyl ester;
- 2-Aza-spiro[3.5]nonane-1,2-dicarboxylic acid 2-tert-butyl ester;
- [3 aS-(3α7aα)]-7a-tert-Butoxycarbonylmethyl-1-oxo-octahydro-isoindole-2-carboxylic acid tert-butyl ester;
- and
- [3aS-(α7aα)]-3a-tert-Butoxycarbonylmethyl-octahydro-isoindole-2-carboxylic acid tert-butyl ester.
5 more elements
Dependencies are inferred from the claim text.