Patent classifications
C07C311/37
SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF SSAO AND USES THEREOF
The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:
##STR00001##
The invention also relates to methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF SSAO AND USES THEREOF
The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:
##STR00001##
The invention also relates to methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
Compounds for use in the treatment of mycobacterial infections
The present invention concerns compounds of general formula (I): ##STR00001##
in which Y and Z are chosen from CH and N; T is chosen from CO or SO.sub.2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway.
Compounds for use in the treatment of mycobacterial infections
The present invention concerns compounds of general formula (I): ##STR00001##
in which Y and Z are chosen from CH and N; T is chosen from CO or SO.sub.2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway.
Fluorescent pI Markers for Isoelectric Focusing Separations and Fluorescent Labeling
UV-Absorbing and fluorescent pI markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.
Fluorescent pI Markers for Isoelectric Focusing Separations and Fluorescent Labeling
UV-Absorbing and fluorescent pI markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.
Sodium Channel Modulators
The present disclosure relates generally to compounds having activity as voltage-gated sodium channel blockers and their use in the field of therapeutic treatment, including the therapy or management of conditions associated with excessive, unwanted, inadequate or otherwise undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In some embodiments, the disclosure relates to aryloxy-substituted amines for use as sodium channel blockers or modulators. Methods for their manufacture and compositions containing the compounds are also disclosed.
COMPOUNDS
The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing compounds capable of absorbing electromagnetic radiation energy and having improved properties.
Enzyme inhibitors
The present subject matter relates generally to compounds having the formula (I): ##STR00001##
wherein each of X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and n are as defined herein. Compounds of formula (I) may act as inhibitors of the thioredoxin reductase enzyme system. The subject matter also relates to use, formulation and preparation of the compounds. The compounds may be useful in the treatment of inflammatory and oxidative diseases and conditions. The compounds may also provide useful anti-proliferative and anti-apoptotic effects.
Enzyme inhibitors
The present subject matter relates generally to compounds having the formula (I): ##STR00001##
wherein each of X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and n are as defined herein. Compounds of formula (I) may act as inhibitors of the thioredoxin reductase enzyme system. The subject matter also relates to use, formulation and preparation of the compounds. The compounds may be useful in the treatment of inflammatory and oxidative diseases and conditions. The compounds may also provide useful anti-proliferative and anti-apoptotic effects.