Abstract: Substantially pure neocarzinostatin anticancer agents have the formula (A):(SMA)-(NCS)-(SMA) (A)wherein (NCS) is a divalent neocarzinostatin residue and (SMA) comprises the monovalent residue of a styrene-maleic acid copolymer having a weight-average molecular weight of from 800 to 2,500, said (NCS) residue being bonded to said (SMA) residues via amide linkages formed between primary amino groups of the neocarzinostatin molecule and carbonyl groups of the styrene-maleic acid copolymer.

Abstract: A novel process is provided for the preparation of optical isomers of certain sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking agents which can be used for various treatments such as for the treatment of congestive heart failure.

Abstract: This disclosure describes compositions of matter useful as growth inhibitors of transplanted tumors in mammals: and this invention discloses a method of inducing the regression and/or palliation of various types of tumors in mammals (mammary cancer, liver cancer, skin cancer, etc.), said method comprising giving to said mammals an effective amount of a compound of the following formula: ##STR1## [wherein A represents an imidazolyl group or a pyridyl group, l represents 0 or 1, m and n each, which may be the same of different, represents an integer of 1 to 6, and, R represents a hydrogen atom or a lower alkyl group], or a salt thereof; the invention also discloses a method of inhibition (or prevention) of metastasis of the various cancers.The above formula compounds have low toxicity, and it is expected to apply various types of administration thereof such as oral administration and parenteral administration.

Abstract: A spherical pellet like composition of nicardipine composed of small granular nuclei such as sugar particles coated with amorphous nicardipine or a salt thereof, a pH-dependent additive and a surface active agent. The spherical pellet like composition of nicardipine may have a further coating of a medicament permeating material as an outermost coating. The spherical pellet like composition may be mixed with the spherical pellet like composition coated with the medicament permeating material.

Abstract: A novel crystal form of N.sup..alpha. -[[(S)-4-oxo-2-azetidinyl]-carbonyl]-L-histidyl-L-prolinamide is provided and a process for preparing such crystals. The crystals provided by the present invention are the dihydrate form of the compound which exhibits a specific X-ray powder diffraction pattern, infared absorption spectrum and thermogravimetry-differential scanning calorimetry. The compound in its novel crystal form is useful in the treatment of consciousness disturbances and memory disorders.

Abstract: Novel neocarzinostatin anticancer agents have the formula:(SMA)--(NCS)wherein (NCS) is a neocarzinostatin residue, n is an integer ranging from 1 to 35, and (SMA) comprises the residue of a half-esterified styrene-maleic acid copolymer having an average molecular weight of from 1,000 to 10,000, said half-esterified styrene-maleic acid copolymer comprising (i) styrene residues, (ii) maleic acid residues covalently bonded to (NCS), (iii) free maleic acid residues, and (iv) half-esterified maleic acid residues, and further wherein the total amount of said residues (ii) and (iii) ranges from an average of 0.1 per molecule to 60 mole % of said (SMA).

Abstract: A novel process is provided for the preparation of optical isomers of certain sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking agents which can be used for various treatments such as for the treatment of congestive heart failure.

Abstract: A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.

Abstract: Long acting formulations of amosulalol hydrochloride are provided, wherein the frequency of administering the hypotensive agent is minimized and wherein such formulations are prepared by compounding amosulalol hydrochloride with an enterosoluble material and optionally the inclusion of an organic acid.

Abstract: Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.

Abstract: Sulfates of glutathione monoalkyl esters (alkyl.gamma.-L-glutamyl-L-cysteinylglycinates) are new and can be prepared by reaction of glutathione with an alcohol in the presence of sulfuric acid. This process forms virtually no diesters, which are toxic compounds and must be completely removed when the sulfates are used as medicine. In addition, since pure glutathione monoester sulfates can be isolated from reaction mixture, high-purity free glutathione monoesters, which have importance as therapeutical and preventive medicines, can be obtained by treatment with a neutralizer or by mere desalting.

Abstract: A granular composition of difficultly digestible polysaccharides (dietary fiber) is composed of a combination of one or more difficultly digestible polysaccharides selected from polysaccharides derived from roots of the plant such as glucomannan, polysaccharides derived from fruits of plants such as pectin, polysaccharides derived from seaweeds such as galactomannan, carragheenin, alginic acid, etc., various kinds of celluloses, and various kinds of brans and one or more difficultly digestible polysaccharides selected from alginates, alginic acid esters, agar, carboxymethyl cellulose salts, and pulullan.The granular composition of this invention is useful as a dietary food or dietary food additive.

Abstract: Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.

Abstract: Novel coumarin compounds of the formula ##STR1## wherein R.sup.1 represents an imidazolyl group or a pyridyloxy group which may be substituted by lower alkyl group(s); R.sub.2 represents a hydrogen atom or a lower alkyl group; and m represents an integer of 1 to 6; and the salts thereof, which inhibit platelets aggregation.

Abstract: Novel cephalosporin compounds of the formula ##STR1## wherein the wavy line means syn-form and anti-form bonds, R.sup.1 represents a cyanomethyl group, a thiocarbamoylmethyl group or an aminothiazolylmethyl group, and A represents a unsubstituted or substituted pyridinio group; and salts thereof. These compounds have excellent antibacterial activities.

Abstract: A patch having good transdermal property which utilizes a suppository base e.g. triglyceride of a vegetable saturated fatty acid having 12 to 18 carbon atoms together with a penetration enhancer.

Abstract: Sustained release pharmaceutical compositions of a solid medical material which contains an amorphous solid medical material, polyethylene oxide, and at least one basic substance selected from the group consisting of hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methyl cellulose, polyvinyl pyrrolidone, carboxyvinyl polymer, hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, methyl meta-acrylate meta-acrylic acid copolymer, polyvinylacetal diethylaminoacetate, dimethylaminoethyl meta-acrylate meta-acrylic acid copolymer, 2-methyl-5-vinylpyridinemethyl acrylate meta-acrylic acid copolymer, citric acid, urea, succinic acid and amino acid, and may further contain one basic substance selected from the group consisting of a surface active agent, polyethylene glycol, propylene glycol, glycerin, a glycerin fatty acid ester and a vegetable oil (first embodiment); and in the case where the solid medical material in nicardipine, the composition may consist only of the amorphous nicardipine o

Abstract: The 7-methoxy-3-heterocyclic thiomethyl cephalosporin derivative possessing excellent antimicrobial activity represented by the general formula ##STR1## wherein R.sup.1 represents ##STR2## group or HOOC-- group, R.sup.2 represents a nitrogen-containing heterocyclic group, and M represents a hydrogen atom or a cation residue forming a salt.

Abstract: A formulation is provided for the transdermal administration of nicardipine hydrochloride. The formulation is comprised of nicardipine hydrochloride dissolved or suspended in a mixed liquid composed of an urea and at least one compound selected from the group consisting of propylene glycol, a monohydric alcohol having 2 to 4 carbon atoms, lactic acid, thioglycol, a middle chain fatty acid glyceride and a sorbitan middle chain fatty acid ester compounded with a transdermal formulation base.

Abstract: The invention relates to novel 7.alpha.-methoxycephalosporin derivatives having at the 7.beta.-position an amido group acylated by a 1,3-dithietane carboxylic acid residue and to 7.beta.-isothiazolylthioacetamido-7.alpha.-methoxycephalosporins having antibacterial activity by themselves and, as the case may be, capable of being converted into the aforesaid 7.alpha.-methoxycephalosporin derivatives. The compounds of this invention exhibit excellent antibacterial activity and are particularly effective against gram negative bacteria.