| 摘要 |
This invention relates to bicyclic amide compounds, pharmaceutical compositions and methods for use in the prevention and treatment of a variety of conditions and/or disease states including cerebral insufficiency, through the enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors as defined herein. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in other disorders wherein a deficiency in neurotrophic factors is implicated, as well as other disorders as described herein. |
| 主权项 |
1. A compound according to formula A: wherein: W is oxygen; X, Y and Z are independently selected from the group consisting of —N, or —CR, wherein: R is H, —Br, —Cl, —F, —CN, —NO2, —OR1, —SR1, —NR12, —C1-C6 branched or un-branched alkyl, which may be un-substituted or substituted, wherein: R1is H, —C1-C6 branched or un-branched alkyl which, may be un-substituted or substituted, n is 0, 1, 2, 3, 4, 5 m is 0, 1, 2, 3, 4, 5 p is 0, 1, 2, 3, 4, 5 R2 and R3 are each independently selected from H, a halogen, —CN, —NO2, —OR1, —SR1, —NR12, CF3, OH, C═O, a —C1-C6 branched or un-branched alkyl, which may be un-substituted or substituted, a —C2-C6 branched or un-branched alkenyl, which may be un-substituted or substituted, a —C2-C6 branched or un-branched alkynyl, which may be un-substituted or substituted, a —C3-C7 cycloalkyl which may be un-substituted or substituted, an aryl which may be un-substituted or substituted , a heterocycle which may be un-substituted or substituted, a carboxyalkyl which may be un-substituted or substituted, a carboxyaryl which may be unsubstituted or substituted, a carboxyheteroaryl which may be un-substituted or substituted, a sulfonylalkyl which may be un-substituted or substituted, a sulfonylaryl which may be unsubstituted or substituted or a sulfonylheteroaryl which may be un-substituted or substituted, E and F are each independently selected from CH2m, CR2R3, A, CH2A, CR2═CR3 or are absent, with the proviso that E and F are not both absent; G is CR2R3, A, CH2A, CR2═CR3, CH2C═O, CH2CR2R3, or absent, A is O, S, SO, SO2, C═O or CR2R3; or a pharmaceutically acceptable salt, solvate, or polymorph thereof. |
