Cambridge Neuroscience, Inc.

Cornell Research Foundation Inc.

Lee David Margolin

Stanley M Goldin

Lain-Yen Hu

N Laxma Reddy

Andrew Gannett Knapp

Subbarao Katragadda

James B Fischer

Kazumi Kobayashi

Graham J Durant

Sharad S Magar

Kevin D McCormick

Deborah Daly

James Fisher

Laxma Reddy

Andy Knapp

Modulators of neurotransmitter release including substituted guanidines, N'-aminoguanidines, and N,N'N',N''-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Substituted aminoguanidines and methods of use thereof

The present invention provides N,N'-diaryl substituted guanidines having therapeutic utility. The compounds of the present invention are represented by the formula: ##STR1## wherein R and R.sup.1 represent hydrogen or other group and Ar and Ar.sup.1 represent selected aryl groups, and at least one being acenaphthyl.

Therapeutic guanidines

Hydrazinedicarboximidamide compounds and pharmaceutical composition

Substituted guanidines and derivatives thereof as modulators of

Substituted hydrazinedicarboximidamides and methods of use thereof

Aminoguanidines and methods of use of same

Acenaphthyl substituted guanidines and methods of use thereof

Acenaphthyl-substituted guanidines and methods of use thereof

Substituted hydrazinecarboximidamides and methods of use thereof

Substituted adamantyl guanidines and methods of use there of

Modulators of neurotransmitter release including substituted guanidines, and N'-aminoguanidines, and N,N'N', N''-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

A compound consisting of a base, a ribose and a fucose, in which the base is a purine or a pyrimidine, the ribose has R.sub.1 and R.sub.2 attached respectively to any two of 2'-O, 3'-O and 5'-O, and the fucose has R.sub.3, R.sub.4 and R.sub.5 attached respectively to any three of 1'-O, 2'-O, 3'-O and 4'-O, wherein each R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H, acetate, sulfate, phosphate, or a metallic salt of acetate, sulfate or phosphate; and the base is linked to the ribose via a bond between 9-N of the base and 1'-O of the ribose when the base is a purine or via a bond between 1-N of the base and 1'-C of the ribose when the base is a pyrimidine and the ribose is linked to the fucose via a bond between any one of 2'-O, 3'-O and 5'-O of the ribose and 1'-C of the fucose.

Fucosylated guanosine disulfates as excitatory amino acid antagonists

Growing community of inventors

Belmont, MA, United States of America

Lee David Margolin