Patent classifications
C07D279/08
VINYL FLUORIDE CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.7, and each of R.sup.a, R.sup.b, R.sup.1, R.sup.2, R.sup.3, R.sup.8 R.sup.9 and R.sup.10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.
##STR00001##
VINYL FLUORIDE CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.7, and each of R.sup.a, R.sup.b, R.sup.1, R.sup.2, R.sup.3, R.sup.8 R.sup.9 and R.sup.10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.
##STR00001##
POLYMER COMPRISING A PLURALITY OF PHENOTHIAZINE GROUPS AND METHODS OF MAKING THE SAME
A non-leaching mediator may include a polymer having a polymeric backbone, and a plurality of phenothiazine groups bonded to the polymeric backbone. The plurality of phenothiazine groups may include at least one of a phenothiazine group having the general formula (IV):
##STR00001##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded, and a phenothiazine group having the general formula (V):
##STR00002##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded.
POLYMER COMPRISING A PLURALITY OF PHENOTHIAZINE GROUPS AND METHODS OF MAKING THE SAME
A non-leaching mediator may include a polymer having a polymeric backbone, and a plurality of phenothiazine groups bonded to the polymeric backbone. The plurality of phenothiazine groups may include at least one of a phenothiazine group having the general formula (IV):
##STR00001##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded, and a phenothiazine group having the general formula (V):
##STR00002##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded.
Polymer comprising a plurality of phenothiazine groups and methods of making the same
A non-leaching mediator may include a polymer having a polymeric backbone, and a plurality of phenothiazine groups bonded to the polymeric backbone. The plurality of phenothiazine groups may include at least one of a phenothiazine group having the general formula (IV): ##STR00001##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded, and a phenothiazine group having the general formula (V): ##STR00002##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded.
Polymer comprising a plurality of phenothiazine groups and methods of making the same
A non-leaching mediator may include a polymer having a polymeric backbone, and a plurality of phenothiazine groups bonded to the polymeric backbone. The plurality of phenothiazine groups may include at least one of a phenothiazine group having the general formula (IV): ##STR00001##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded, and a phenothiazine group having the general formula (V): ##STR00002##
and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded.
Selective BACE1 inhibitors
The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof. ##STR00001##
Selective BACE1 inhibitors
The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof. ##STR00001##
IGF-1R SIGNALING PATHWAY INHIBITORS USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease.
IGF-1R SIGNALING PATHWAY INHIBITORS USEFUL IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
The present invention provides compounds acting as Insulin/IGF signaling modulators useful in the treatment of neurodegenerative diseases and disorders. The invention provides pharmaceutical compositions including such compounds, and methods of using these compounds and compositions for the treatment of neurodegenerative diseases, in particular neurodegenerative diseases caused by proteotoxicity such as Alzheimer's disease.