Benzofurazan compounds which enhance AMPA receptor activity
AssigneeCortex Pharmaceuticals, Inc.
InventorsGary A. Rogers, Christopher M. Marrs
Life of this patent
Estimating the term…
Abstract
Compounds of general structural formula (1) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior. 1
Claims30
A compound having the structure:
- 5
- in which:
- R1 is oxygen or sulfur;
- R2 and R3 are independently selected from the group consisting of —N═, —CR═, and —CX═;
- M is ═N— or ═CR4—, wherein R4 and R8 are independently R or together form a single linking moiety linking M to the ring vertex 2′, the linking moiety being selected from the group consisting of a single bond, —CRR′—, —CR═CR′—, —C(O)—, —O—, —S(O)y—, —NR—, and —N═;
- and
- R5 and R7 are independently selected from the group consisting of —(CRR′)n—, —C(O)—, —CR═CR′—, —CR═CX—, —CRX—, —CXX′—, —S—, and —O—, and
- R6 is selected from the group consisting of —(CRR′)m—, —C(O)—, —CR═CR′—, —CRX—, —CXX′—, —S—, and —O—;
- wherein
- X and X′ are independently selected from —Br, —Cl, —F, —CN, —NO2, —OR, —SR, —NRR′, —C(O)R, —CO2R, or —CONRR′, wherein two groups R or R′ on an individual group X, or on two adjacent groups X, may together form a ring;
- and
- R and R′ are independently selected from (i) hydrogen, (ii) C1-C6 branched or unbranched alkyl, which may be unsubstituted or substituted with one or more functionalities selected from halogen, nitro, alkoxy, hydroxy, alkylthio, amino, keto, aldehyde, carboxylic acid, carboxylic ester, or carboxylic amide, and wherein two such alkyl groups on a single carbon or on adjacent carbons may together form a ring, and (iii) aryl, which may be unsubstituted or substituted with one or more functionalities selected from halogen, nitro, alkoxy, hydroxy, aryloxy, alkylthio, amino, keto, aldehyde, carboxylic acid, carboxylic ester, or carboxylic amide;
- m and p are, independently, 0 or 1;
- and
- n and y are, independently, 0, 1 or 2.
Dependencies are inferred from the claim text.