Patent classifications
A61K31/435
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.
COMPOUNDS AND COMBINATIONS THEREOF FOR TREATING NEUROLOGICAL AND PSYCHIATRIC CONDITIONS
Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, an antidepressant, such as bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
AQUEOUS COMPOSITION
A technique is provided for reducing the discoloration of an aqueous composition containing a halogenated isoquinoline derivative during high-temperature preservation. An aqueous composition comprising a compound represented by Formula (1).sub.:
##STR00001## wherein X represents a halogen atom,
or a salt thereof, or a solvate of the compound or the salt thereof, and a β blocker.
AQUEOUS COMPOSITION
A technique is provided for reducing the discoloration of an aqueous composition containing a halogenated isoquinoline derivative during high-temperature preservation. An aqueous composition comprising a compound represented by Formula (1).sub.:
##STR00001## wherein X represents a halogen atom,
or a salt thereof, or a solvate of the compound or the salt thereof, and a β blocker.
Compositions and methods for treating canker sores
Oral compositions and methods of use thereof are provided herein. The oral compositions comprise a first component comprising at least one E.sub.h-raising compound and a pharmaceutically acceptable carrier, and a second component comprising at least one zinc compound, an anti-microbial agent and a pharmaceutically acceptable carrier.
Compositions and methods for treating canker sores
Oral compositions and methods of use thereof are provided herein. The oral compositions comprise a first component comprising at least one E.sub.h-raising compound and a pharmaceutically acceptable carrier, and a second component comprising at least one zinc compound, an anti-microbial agent and a pharmaceutically acceptable carrier.
HEPATITIS C ANTIVIRAL COMPOSITIONS AND METHODS
The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
HEPATITIS C ANTIVIRAL COMPOSITIONS AND METHODS
The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
HEPATITIS C ANTIVIRAL COMPOSITIONS AND METHODS
The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
PYRIDINE DERIVATIVES
The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia.
The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.