Patent classifications
C07D293/12
Zuclopenthixol hydrochloride derivatives and Ebselen derivatives as ErbB2 inhibitors
The present invention relates to compounds of the following general formula (I) or (II): or a pharmaceutically acceptable salt and/or solvate thereof, for use in the treatment and/or in the prevention of ErbB2 dependent cancers, and pharmaceutical compositions containing such compounds. ##STR00001##
BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF
The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
##STR00001##
BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF
The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
##STR00001##
BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF
The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
##STR00001##
BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF
The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
##STR00001##
Crystalline form of 1,4-bis[1,2-benzisoselenazol-3(2H)-one]-butane, method for preparing same and use thereof
A crystalline form I of 1,4-BIS[1,2-BENZISOSELENAZOL-3(2H)-one]-butane has characteristic peaks at 2? angles of 6.17?0.20?, 12.28?0.20?, 18.44?0.20?, 25.92?0.20? and 30.95?0.20? by X-ray powder diffraction using Cu-K? radiation.
Crystalline form of 1,4-bis[1,2-benzisoselenazol-3(2H)-one]-butane, method for preparing same and use thereof
A crystalline form I of 1,4-BIS[1,2-BENZISOSELENAZOL-3(2H)-one]-butane has characteristic peaks at 2? angles of 6.17?0.20?, 12.28?0.20?, 18.44?0.20?, 25.92?0.20? and 30.95?0.20? by X-ray powder diffraction using Cu-K? radiation.
PHARMACEUTICAL FORMULATIONS
Disclosed herein is glutathione in conjunction with an isoselenazol or isothiazol derivative, e.g., ebselen or ebsulfur derivative, to treat diabetes, lupus, or other chronic inflammatory disease. The glutathione is preferably provided in a rapid release oral formulation that presents the glutathione for absorption in the first part of the ileum. The isoselenazol or isothiazol derivative is preferably provided in a delayed release formulation to avoid overlapping high enteric concentration. These may be provided within the same unit dosage form.
Heterocyclic molecules for biomedical imaging and therapeutic applications
Probes which target diffuse and fibrillar forms of amyloid beta (A) are described. These probes demonstrate high initial brain penetration and facile clearance from non-targeted regions. The agents can be used to image amyloid quantitatively for monitoring efficacy of A-modifying therapeutics and assist in premortem diagnosis of Alzheimer's disease (AD). Disclosed probes can bind A aggregates of preformed A.sub.1-42 fibrils in vitro and can be used to image fibrillar and diffuse plaques ex vivo in brain sections. Disclosed probes can be used to determine A burden in early stages of AD. These probes can be used for multimodality imaging of A. F-AI-187 (1 M) can detect A plaques in brain sections of APP/PS1 mice. F-AI-187 (10 M) can detect A plaques in the frontal lobe in a brain section of a patient with confirmed AD. Some probes can be used for fluorescence imaging of plaque.
Heterocyclic molecules for biomedical imaging and therapeutic applications
Probes which target diffuse and fibrillar forms of amyloid beta (A) are described. These probes demonstrate high initial brain penetration and facile clearance from non-targeted regions. The agents can be used to image amyloid quantitatively for monitoring efficacy of A-modifying therapeutics and assist in premortem diagnosis of Alzheimer's disease (AD). Disclosed probes can bind A aggregates of preformed A.sub.1-42 fibrils in vitro and can be used to image fibrillar and diffuse plaques ex vivo in brain sections. Disclosed probes can be used to determine A burden in early stages of AD. These probes can be used for multimodality imaging of A. F-AI-187 (1 M) can detect A plaques in brain sections of APP/PS1 mice. F-AI-187 (10 M) can detect A plaques in the frontal lobe in a brain section of a patient with confirmed AD. Some probes can be used for fluorescence imaging of plaque.