Abstract: There is disclosed a method for evaluation of the safety of a chemical compound, which includes the steps of: (a) reacting a chemical compound with recombinant yeast cells expressing, or in other words producing, human cytochrome P450 molecular species P450 1A2, P450 2C9, P450 2E1 and P450 3A4 together with a yeast NADPH-P450 reductase, which may be in the form of a fused enzyme with each of said human cytochrome P450 molecular species, or with the cell free extracts of the yeast cells; and (b) analyzing the resulting metabolite to determine the safety of the compound. According to this method, it can be determined whether a test compound will be converted into a carcinogenic or mutagenic form through the metabolism in the human liver, and whether the test compound or its metabolite has mutagenicity.

Abstract: Triphenylmethane derivatives represented by the general formula: 1

Abstract: An oligonucleotide which can hybridize with a human-derived cytochrome P450IIC18 gene, one of the enzymes participating in the metabolic decomposition of medicines, has a GC content of 40-70%, and comprises 8 to 500 nucleotide units. The use of the oligonucleotide in the recognition or amplification of a DNA having the base sequence of this gene enables the presence or absence of mutation to be readily diagnosed and analyzed before the administration of a medicine. Thus it becomes possible to determine a safe dose of a medicine which has been difficult to use because of the occurrence of individual difference in drug-metabolizing ability and to use also a medicine which takes an active form by the action of this enzyme according to individuals.

Abstract: The present invention relates to a novel radioactive benzodiazepine derivative represented by the formula: ##STR1## wherein R is hydrogen or a lower alkyl; X* is radioactive iodine or bromine; Y is hydrogen or a halogen; and Z is a halogen or nitro group; and the salt thereof.The compound of the present invention enables to non-invasively detect the presence of benzodiazepine receptors in human or animal brains, other organs or tissues. Additionally, it enables to dynamically trace the change in receptor concentration either. It is very useful as a radioactive diagnostic agent for nuclear medicine in vitro or in vivo or as a radiopharmaceutical.

Abstract: A radioactive propyl 2-iodospiroperidol of the formula: ##STR1## wherein I* is a radioactive iodine atom. The radioactive compound has a high affinity for dopamine receptors and is very useful as a radioactive diagnostic agent and as a radiopharmaceutical.

Abstract: The present invention relates to a novel radioactive benzodiazepine derivative represented by the formula: ##STR1## wherein R is hydrogen or a lower alkyl; X* is radioactive iodine or bromine; Y is hydrogen or a halogen; and Z is a halogen or nitro group; and the salt thereof.The compound of the present invention enables to non-invasively detect the presence of benzodiazepine receptors in human or animal brains, other organs or tissues. Additionally, it enables to dynamically trace the change in receptor concentration either. It is very useful as a radioactive diagnostic agent for nuclear medicine in vitro or in vivo or as a radio-pharmaceutical.

Abstract: A radioactive 2-iodospiroperidol represented by the formula: ##STR1## wherein X represents a radioactive iodine atom. This compound has a strong affinity for dopamine receptor and is very useful as a nuclear medical diagnostic agent of dopamine receptor and as a radioactive medicine.

Abstract: 17.alpha.-[(E)-2-Iodovinyl]-estra-1,3,5(10)-triene-3,17.beta.-diol wherein the iodine atom is radioactive can be produced from (E)-[3-acyloxy-17.beta.-hydroxyestra-1,3,5(10)-triene-17.alpha.-yl]vinyl dihydroxyborane in an excellent yield by iodinating the same and hydrolyzing the resulting 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol.

Abstract: A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.

Abstract: Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.

Abstract: Penicillins of the formula: ##STR1## wherein R is an unsubstituted phenyl group or a substituted phenyl group having one or more hydroxyl groups or a cyclohexadienyl group and A represents a monocyclic or polycyclic nitrogen-containing heterocyclic aromatic ring, which are useful as antimicrobial agents having a broad antimicrobial spectrum against gram-positive and gram-negative bacteria including Pseudomonas and can be produced advantageously from the phenacyl ester of 6-aminopenicillanic acid through a series of steps.

Abstract: Novel penicillins of the formula: ##STR1## wherein the ring A is a benzene ring or a 5 or 6-membered heteroaromatic ring containing one or two nitrogen atoms as the hetero atom, on which one or more of lower alkyl, lower alkoxy, lower alkylthio, lower haloalkyl, lower alkylenedioxy halogen, hydroxyl, nitro, free or protected amino, lower alkylamino, di(lower)alkylamino and lower alkanoylamino may be present, Z is a nitrogen atom or a methylene group, X is an oxygen atom or a sulfur atom, Y is a hydrogen atom, a lower alkoxycarbonyl group or a lower alkanoyl group, R.sub.1 is a free or protected hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen atom or a halogen atom, and their non-toxic pharmaceutically acceptable salts, and their preparation.

Abstract: Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.

Abstract: Novel penicillins of the formula: ##SPC1##Wherein the ring A is a benzene ring or a 5 or 6-membered heteroaromatic ring containing one or two nitrogen atoms as the hetero atom, on which one or more of lower alkyl, lower alkoxy, lower alkylthio, lower haloalkyl, lower alkylenedioxy, halogen, hydroxyl, nitro, free or protected amino, lower alkylamino, di(lower)alkylamino and lower alkanoylamino may be present, Z is a nitrogen atom or a methylene group, X is an oxygen atom or a sulfur atom, Y is a hydrogen atom, a lower alkoxycarbonyl group or a lower alkanoyl group, R.sub.1 is a free or protected hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen atom or a halogen atom, and their non-toxic pharmaceutically acceptable salts, and their preparation.

Abstract: Penicillins of the formula: ##SPC1##Wherein R is an unsubstituted phenyl group or a substituted phenyl group having one or more hydroxyl groups or a cyclohexadienyl group and A represents a monocyclic or polycyclic nitrogen-containing heterocyclic aromatic ring, which are useful as antimicrobial agents having a broad antimicrobial spectrum against gram-positive and gram-negative bacteria including Pseudomonas and can be produced advantageously from the phenacyl ester of 6-aminopenicillanic acid through a series of steps.