Patent classifications
A61K31/438
HETEROAROMATIC DERIVATIVES HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
A composition comprising the compounds of Formula (I):
##STR00001## or pharmaceutically acceptable salts thereof, wherein: R.sup.1 is substituted or unsubstituted aromatic heterocyclyl or the like; R.sup.2 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; n is 1 or 2; R.sup.4 is substituted or unsubstituted non-aromatic nitrogen-containing heterocyclyl or the like; L is —NR.sup.8— or the like; R.sup.8 is a hydrogen atom or the like; R.sup.8 is each independently a hydrogen atom or the like; R.sup.8 is each independently a hydrogen atom or the like; p is 1 or 2; and R.sup.7 is a group represented by Formula:
##STR00002## wherein R.sup.9 is substituted or unsubstituted alkyloxy or the like; R.sup.10 is a hydrogen atom or the like; R.sup.11 is halogen or the like; and m is 0 or 1.
HETEROAROMATIC DERIVATIVES HAVING SEROTONIN RECEPTOR BINDING ACTIVITY
Provided are compounds having a serotonin 5-HT2A receptor inverse agonism, pharmaceutically acceptable salts thereof, and a composition comprising them,
A composition comprising the compounds of Formula (I):
##STR00001## or pharmaceutically acceptable salts thereof, wherein: R.sup.1 is substituted or unsubstituted aromatic heterocyclyl or the like; R.sup.2 is each independently a hydrogen atom or the like; R.sup.3 is each independently a hydrogen atom or the like; n is 1 or 2; R.sup.4 is substituted or unsubstituted non-aromatic nitrogen-containing heterocyclyl or the like; L is —NR.sup.8— or the like; R.sup.8 is a hydrogen atom or the like; R.sup.8 is each independently a hydrogen atom or the like; R.sup.8 is each independently a hydrogen atom or the like; p is 1 or 2; and R.sup.7 is a group represented by Formula:
##STR00002## wherein R.sup.9 is substituted or unsubstituted alkyloxy or the like; R.sup.10 is a hydrogen atom or the like; R.sup.11 is halogen or the like; and m is 0 or 1.
Cyclopropylamine compound as LSD1 inhibitor and use thereof
Provided is a cyclopropylamine compound as lysine-specific demethylase 1 (LSD1) inhibitor, and a use thereof in preparation of drug for treating diseases associated with LSD1. The cyclopropylamine compound is a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof. ##STR00001##
Cyclopropylamine compound as LSD1 inhibitor and use thereof
Provided is a cyclopropylamine compound as lysine-specific demethylase 1 (LSD1) inhibitor, and a use thereof in preparation of drug for treating diseases associated with LSD1. The cyclopropylamine compound is a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof. ##STR00001##
Melanocortin 4 receptor antagonists and uses thereof
Described herein are compounds of Formula I: ##STR00001##
and their pharmaceutically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
Compositions containing a pharmacophore with selectivity to diseased tissue and methods of making same
Compositions and methods useful for delivery of targeted therapies for pulmonary arterial hypertension, sepsis, cancer and cachexia. The compositions and methods are based on peptide pharmacophores that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. Peptide pharmacophores may selectively target tumor vasculature, regenerating tissue, wounded tissue, inflamed tissue, fibrotic tissue, remodeled tissue, tissue characterized by elevated heparanase levels, and have the ability to internalize into such diseased cells.
Compositions containing a pharmacophore with selectivity to diseased tissue and methods of making same
Compositions and methods useful for delivery of targeted therapies for pulmonary arterial hypertension, sepsis, cancer and cachexia. The compositions and methods are based on peptide pharmacophores that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. Peptide pharmacophores may selectively target tumor vasculature, regenerating tissue, wounded tissue, inflamed tissue, fibrotic tissue, remodeled tissue, tissue characterized by elevated heparanase levels, and have the ability to internalize into such diseased cells.
RIFABUTIN TREATMENT METHODS, USES, AND COMPOSITIONS
The invention provides systems and methods for increased clinical efficacy of rifabutin against A. baumannii. The invention takes advantage of the discovery of a ferric-coprogen (FhuE) receptor that is responsible for the uptake of rifabutin into A. baumannii cells. Methods preferably include obtaining a sample from a patient suspected of having an infection; performing a test on the sample to identify an infection of A. baumannii in the patient; and providing a formulation of rifabutin for treating the patient that, when administered to the patient, maximizes a resultant AUC and/or C.sub.max. The method may include administering the formulation of rifabutin to the patient. Preferably the formulation is delivered to the patient, e.g., by intravenous injection and results in a C.sub.max is that greater than about 2 mg/L and optionally less than about 50 mg/L.
RIFABUTIN TREATMENT METHODS, USES, AND COMPOSITIONS
The invention provides systems and methods for increased clinical efficacy of rifabutin against A. baumannii. The invention takes advantage of the discovery of a ferric-coprogen (FhuE) receptor that is responsible for the uptake of rifabutin into A. baumannii cells. Methods preferably include obtaining a sample from a patient suspected of having an infection; performing a test on the sample to identify an infection of A. baumannii in the patient; and providing a formulation of rifabutin for treating the patient that, when administered to the patient, maximizes a resultant AUC and/or C.sub.max. The method may include administering the formulation of rifabutin to the patient. Preferably the formulation is delivered to the patient, e.g., by intravenous injection and results in a C.sub.max is that greater than about 2 mg/L and optionally less than about 50 mg/L.
RIFABUTIN TREATMENT METHODS, USES, AND COMPOSITIONS
The invention provides systems and methods for increased clinical efficacy of rifabutin against A. baumannii. The invention takes advantage of the discovery of a ferric-coprogen (FhuE) receptor that is responsible for the uptake of rifabutin into A. baumannii cells. Methods preferably include obtaining a sample from a patient suspected of having an infection; performing a test on the sample to identify an infection of A. baumannii in the patient; and providing a formulation of rifabutin for treating the patient that, when administered to the patient, maximizes a resultant AUC and/or C.sub.max. The method may include administering the formulation of rifabutin to the patient. Preferably the formulation is delivered to the patient, e.g., by intravenous injection and results in a C.sub.max is that greater than about 2 mg/L and optionally less than about 50 mg/L.