C07D231/16

Propionic acid derivatives and methods of use thereof

Provided herein are compounds and pharmaceutical compositions of formula I ##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.

Propionic acid derivatives and methods of use thereof

Provided herein are compounds and pharmaceutical compositions of formula I ##STR00001##
where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.

DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT.sub.2A serotonin receptor.

##STR00001##

Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.

The present invention also relates to the method of prophylaxis or treatment of 5-HT.sub.2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT.sub.2A serotonin receptor.

##STR00001##

Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.

The present invention also relates to the method of prophylaxis or treatment of 5-HT.sub.2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

COMPOSITION OF A 5-HT2A SEROTONIN RECEPTOR MODULATOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to certain compositions of a 5-HT.sub.2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

Aryl sulfonohydrazides

Compound of formula I: ##STR00001##
wherein: A is selected from: (i) ##STR00002##
where R.sup.F1 is H or F; (ii) ##STR00003## (iii) a N-containing C.sub.6 heteroaryl group; and B is ##STR00004##
where X.sup.1 is either CR.sup.F2 or N, where R.sup.F2 is H or F; X.sup.2 is either CR.sup.3 or N, where R.sup.3 is selected from H, Me, Cl, F OMe; X.sup.3 is either CH or N; X.sup.4 is either CR.sup.F3 or N, where R.sup.F3 is H or F; where only one or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be N; and R.sup.4 is selected from I, optionally substituted phenyl, optionally substituted C.sub.5-6 heteroaryl; optionally substituted C.sub.1-6 alkyl and optionally substituted C.sub.1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.

Aryl sulfonohydrazides

Compound of formula I: ##STR00001##
wherein: A is selected from: (i) ##STR00002##
where R.sup.F1 is H or F; (ii) ##STR00003## (iii) a N-containing C.sub.6 heteroaryl group; and B is ##STR00004##
where X.sup.1 is either CR.sup.F2 or N, where R.sup.F2 is H or F; X.sup.2 is either CR.sup.3 or N, where R.sup.3 is selected from H, Me, Cl, F OMe; X.sup.3 is either CH or N; X.sup.4 is either CR.sup.F3 or N, where R.sup.F3 is H or F; where only one or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be N; and R.sup.4 is selected from I, optionally substituted phenyl, optionally substituted C.sub.5-6 heteroaryl; optionally substituted C.sub.1-6 alkyl and optionally substituted C.sub.1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.

PYRAZOLE DERIVATIVE

A pyrazole derivative having the following formula stru-1:

##STR00001##

The pyrazole derivative is used for prevention and control of pests.

PYRAZOLE DERIVATIVE

A pyrazole derivative having the following formula stru-1:

##STR00001##

The pyrazole derivative is used for prevention and control of pests.

Processes for the preparation of pyrazole derivatives useful as modulators of the 5-HT2A serotonin receptor

The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT.sub.2A serotonin receptor activity. ##STR00001## The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.