Abstract: Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is the treatment of prostatic hypertrophy with an estradiol derivative of the formula (II): ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3; and X is hydroxy or halogen.

Abstract: Disclosed is an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3, which is useful a growth inhibiting agent.

Abstract: A phenylalanine-glycine derivative of the general formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described.The novel conjugate of the phenylalanine-glycine derivative and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered singly or as a mixture with phenylalanine.

Abstract: Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

Abstract: A pharmaceutical composition comprising a compound of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a saturated or unsaturated aliphatic acyl having 2 to 25 carbon atoms or benzoyl group and R.sup.3 is a hydrogen atom or alkyl group, and a pharmaceutically acceptable carrier is disclosed. Further, a novel compound of the general formula (I) wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, pivaloyl, capryloyl, lauroyl, palmitoyl, stearoyl, linoleoyl, docosahexaenoyl, or benzoyl group, and R.sup.3 is a hydrogen atom or methyl group, is also disclosed.

Abstract: Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

Abstract: A phenylalanine-glycine compound of formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described. The novel conjugate of the phenylalanine-glycine compound and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered alone or as a mixture with phenylalanine.

Abstract: Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

Abstract: This invention provides a method of inhibiting aromatase and treating of estrogen-dependent diseases in a patient by administering azole derivatives as nonsteroidal inhibitors. The azole derivative has the formula ##STR1## where R.sub.1 a is hydrogen or a (C.sub.1 -C.sub.5) alkyl; R.sub.2 is a hydrogen or a (C.sub.1 -C.sub.5) alkyl; R.sub.3 is any of a halogen, a (C.sub.1 -C.sub.5)alkyl, a haloalkyl, a phenyl, a cyano, or nitro; n is 0 to 5; and Y is a nitrogen atom or CH.

Abstract: The present invention discloses a novel, labelled vitamin D.sub.3 derivative in which hydrogen atoms on the skeleton portion, i.e. 6- and 19-positions, are substituted with a deuterium atom or a tritium atom, as well as a novel production process of the labelled vitamin D.sub.3 derivative carried out by way of sulfur dioxide addition reaction of a vitamin D.sub.3 derivative. The labelled portion of the novel vitamin D.sub.3 is resistant against in vivo metabolism and make a long period tracing of its pharmacodynamics in a living body possible.

Abstract: Disclosed herein are polysaccharides extracted from marine algae and an antiviral drug containing as active ingredient polysaccharides extracted from seaweeds.

Abstract: Disclosed herein are lectins extracted form a plant of the class Dicotyledoneae and an antiretoviral drug comprising as an active ingredient an effective amount of the lectins.

Abstract: Disclosed herein are an anti-tumor substance obtained by bonding an anti-tumor agent to human immunoglobulin, and a process for producing the same.

Abstract: Disclosed herein are the derivatives of substituted cephalosporanic acid represented by the formula (I): ##STR1## wherein R.sup.1 represents a 4-pyridylthiomethyl group, an alpha-aminobenzyl group, a cyanomethyl group or a 1-tetrazolylmethyl group; R.sup.2 represents a hydrogen atom, an acetoxy group or a (5-methyl-1,3,4-thiadiazol-2-yl)thio group; R.sup.3 represents a hydrogen atom, a hydroxyl group, a carbamoyl group, an alkyl group having 1 to 4 carbon atoms or --(CONH).sub.m (CH.sub.2).sub.n --COOH wherein m is 0 or 1, n is 0, 1 or 2 and the carboxyl group may have been converted to a salt or an ester thereof; p is 0, 1 or 2 and X represents carbon atom or nitrogen atom, and antibiotics comprising the derivatives of substituted cephalosporanic acid represented by the formula (I).

Abstract: Disclosed herein are an anti-tumor substance obtained by bonding an anti-tumor agent to human immunoglobulin, and a process for producing the same.

Abstract: Disclosed herein are a derivative of a substituted cephalosporanic acid, represented by the formula (I): ##STR1## wherein p is 0, 1 or 2 and R.sup.1 represents a hydrogen atom, a hydroxyl group, a carbamoyl group, an alkyl group having 1 to 4 carbon atoms or --(CONH).sub.m (CH.sub.2).sub.n --COOH wherein m is 0 or 1; n is 0, 1 or 2 and the carboxyl group may have been converted to the salt or the ester thereof, and an antibiotic comprising a derivative of substituted cephalosporanic acid represented by the formula (I).

Abstract: The present invention relates to a platinum compound having the formula ##STR1## wherein R represents hydrogen atom, an alkali metal atom or a lower alkyl group. The platinum compound is effective as an antitumor and antimicrobial drug.

Abstract: Disclosed is a novel pharmaceutical composition having antitumor (anti-cancer) activity without causing pyrexia and anaphylaxis, formed by an amide bonding between an antibody obtained by the purification of the antibody to tumor (cancer) antigen via affinity-chromatography and an antitumor substance (anti-cancer drug).

Abstract: The present invention relates to a platinum compound having the formula ##STR1## wherein R represents hydrogen atom, an alkali metal atom or a lower alkyl group. The platinum compound is effective as an antitumor and antimicrobial drug.

Abstract: Disclosed is a novel pharmaceutical composition having antitumor activity without causing pyrexia and anaphylaxis formed by an amido bonding between an antibody obtained by the purification of the antibody to tumor antigen via affinity-chromatography and an antitumor substance.