Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2C19-related (CYP2C19) metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by the subject upon intravenous or oral administration of a 13C-labeled CYP2C19 substrate compound. The present invention is useful as anon-invasive, in vivo assay for evaluating CYP2C19 enzyme activity in a subject using the metabolite 13CO2 in expired breath, to phenotype individual subjects and to determine the selection, optimal dosage and timing of drug administration.

Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2D6 isoenzyme (CYP2D6)-related metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by a the subject upon intravenous or oral administration of a 13C-labeled CYP2D6 substrate compound. The present invention is useful as an in vivo phenotype assay for evaluating CYP2D6-related activity using the metabolite 13CO2 in expired breath and to determine the optimal dosage and timing of administration of CYP2D6 substrate compound.

Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2C19-related (CYP2Cl9) metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by the subject upon intravenous or oral administration of a 13C-labeled CYP2C19 substrate compound. The present invention is useful as a non-invasive, in vivo assay for evaluating CYP2C19 enzyme activity in a subject using the metabolite 13CO2 in expired breath, to phenotype individual subjects and to determine the selection, optimal dosage and timing of drug administration.

Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2C19-related (CYP2Cl9) metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by the subject upon intravenous or oral administration of a 13C-labeled CYP2C19 substrate compound. The present invention is useful as a non-invasive, in vivo assay for evaluating CYP2C19 enzyme activity in a subject using the metabolite 13CO2 in expired breath, to phenotype individual subjects and to determine the selection, optimal dosage and timing of drug administration.

Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2D6 isoenzyme (CYP2D6)-related metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by a the subject upon intravenous or oral administration of a 13C-labeled CYP2D6 substrate compound. The present invention is useful as an in vivo phenotype assay for evaluating CYP2D6-related activity using the metabolite 13CO2 in expired breath and to determine the optimal dosage and timing of administration of CYP2D6 substrate compound.

Abstract: The present invention relates, generally to a method of determining and assessing L-3,4-dihydroxyphenylalanine (a.k.a., Levodopa; L-dopa; or LD) metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by the subject upon intravenous or oral administration of a 13C-labeled substrate, such as levodopa. The present invention is useful as an in vivo phenotype assay for individualizing LD/Carbidopa(CD) therapy in Parkinsons disease patients by optimizing the dose and timing of the dose of dopamine decarboxylase (DDC) inhibitor like CD for systemic suppression of dopamine metabolism by evaluating DDC enzyme activity using the metabolite 13CO2 in expired breath.

Abstract: The present invention provides triazoloquinazoline and pyrazolotriazolopyrimidine derivatives represented by the following general formula (1): 1

Abstract: Disclosed is triazolopurine derivatives represented by the general formula (I): wherein R1 and R2 are as defined in the description. This compounds exhibit affinity for adenosine A3 receptor and are therefore useful as the ingredient of pharmaceutical compositions.

Abstract: Disclosed is a triazolopurine derivative represented by the general formula: wherein R1 and R2 represent the same groups as those described in the specification; and A represents a group: wherein R3 represents the same groups as those described in the specification. This compound is incorporated in a pharmaceutical composition because of its affinity to an adenosine A3 receptor, and is used as an adenosine A3 receptor antagonist or a remedy for asthma.

Abstract: The present invention provides a novel process for preparing a series of quinazolin-4-one derivatives in high yields with reduced amounts of byproducts, the process comprising reacting, in the presence of a base, a trialkylsilyl halide with a compound represented by the formula ##STR1## wherein; R.sup.5 is a phenyl group which may have 1 to 3 substituents each selected from a lower alkyl group, a lower alkoxy group or a halogen atom, a lower alkyl group, a phenyl-lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, a lower alkenyl group, a lower alkoxy-lower alkyl group or a lower alkynyl group; R.sup.6 is a lower alkyl group, a halogen-substituted lower alkyl group, a lower alkoxycarbonyl group or a phenyl group which may have, as a substituent, a lower alkyl group or a group of the formula ##STR2## wherein A is an oxygen atom or a single bond, Z is a lower alkylene group, R.sup.7 is a lower alkyl group and R.sup.

Abstract: The present invention provides a phosphonic diester derivative of the following general formula (1): ##STR1## wherein A represents an oxygen atom or a sulfur atom; R.sup.1, R.sup.2, R.sup.9 and R.sup.10 are the same or different and they each represent a hydrogen atom, a lower alkoxy group, a nitro group, a lower alkyl group, a halogen-substituted lower alkyl group or a halogen atom; R.sup.3 represents a phenyl group, --B--R.sup.6 (wherein B represents an oxygen atom or a sulfur atom and R.sup.6 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl group, a phenyl(lower)alkyl group optionally having a halogen atom as a substituent on the phenyl ring, a phenoxy(lower)alkyl group, a lower alkoxycarbonyl(lower)alkyl group, a carboxy(lower)alkyl group or a lower alkenyl group) or --NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.

Abstract: The present invention provides a phosphonic diester derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and they each represent a hydrogen atom, a lower alkyl group, a halogen atom, a cyano group, a hydroxyl group, or a lower alkoxy group optionally having a halogen atom, a phenyl group or a hydroxypiperidino group as a substituent; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group optionally having a halogen atom or a cyano group as a substituent; and R.sup.5 and R.sup.6 are the same or different and they each represent a hydrogen atom or a lower alkyl group.The derivative of the present invention has excellent hypolipidemic, vasodepressor and hypoglycemic activities and is useful as therapeutic and preventive agents for hyperlipidemic diseases, hypertension and diabetes.

Abstract: The invention provides a phosphonic diester derivative of the general formula ##STR1## The phosphonic diester derivative of the invention has hypoglycemic and hypolipidemic activities, for instance, and is of value as an antidiabetic or anti-hyperlipidemic agent.