Abstract: Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.
Abstract: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.
Abstract: 2-(p-prenylphenyl)propionic acid and pharmaceutically acceptable salts thereof are disclosed. They exhibit anti-inflammatory and analgesic activity with low gastrointestinal action.
Abstract: 1-(3-Mercapto-2-methylpropanoyl)prolyl amino acid derivatives of the formula ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or a substituted phenyl-lower alkyl group, R.sub.1 represents a hydrogen atom, R.sub.4 CO--, R.sub.5 S--, or ##STR2## R.sub.2 represents a hydrogen atom or a lower alkyl group, R.sub.3 represents a hydrogen atom, a phenyl group, a lower alkyl group, or a substituted lower alkyl group, or R.sub.2 and R.sub.3 form a heterocyclic ring together with the nitrogen and carbon atoms to which they are respectively bonded; salts of these compounds; compositions comprising these compounds or salts; and processes for preparing these compounds or salts. These compounds and salts have excellent antihypertensive activity.
Abstract: There are disclosed 20-alkoxy-16-alkyl-prostadienoic acid derivatives of the formula: ##STR1## wherein A represents ##STR2## R and R.sup.5, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group, and the pharmaceutically acceptable non-toxic salts thereof. These compounds have excellent pharmacological effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.alpha..
Abstract: A 2-acyl-6-aminomethylphenol derivative having the formula (I): ##STR1## wherein R.sup.1 represents a straight chain or branched chain alkyl group of 1 to 6 carbon atoms unsubstituted or substituted with 1 to 3 halogen atoms; a hydrogen atom or a group having the formula (II):--C.sub.n H.sub.2n --R.sup.7 (II)wherein n represents 0 or an integer of 1 to 6; R.sup.7 represents a cycloalkyl group of 3 to 8 carbon atoms unsubstituted or substituted with at least one lower alkyl group; a phenyl group unsubstituted or substituted with at least one lower alkyl group, a halogen atom, a lower alkoxy group or a lower alkylthio group; a lower alkoxy group; a lower alkylthio group; a lower alkylsulfinyl group; a lower alkylsulfonyl group; an N-lower alkylamino group; an N,N-di-lower alkylamino group; or a pyridyl, furyl or thienyl group; R.sup.
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 novel process for the amidation or esterification which comprises reacting a compound having a carboxy group with a compound having an amino or imino group which can be acylated or with a compound having a hydroxy group in the presence of a sulfonic acid ester of the formula:R.sub.1 --SO.sub.2 --OR.sub.2wherein R.sub.1 is an organic group and R.sub.2 O-- is a residue of a strongly acidic N-hydroxy compound as a condensation agent, and a novel sulfonic acid ester useful as such a condensation agent and a process for the preparation thereof.
Abstract: Novel pyridazine-containing thioamide derivatives of the formula ##STR1## wherein R.sub.1 is ##STR2## wherein A is hydrogen, methyl, phenyl or mercapto, and B is hydrogen or phenyl; R.sub.2 is hydrogen or methyl; R.sub.3 is hydrogen, methyl or phenyl; R.sub.4 is hydrogen or methyl; and n is zero or 1. The derivatives have outstanding gastric antisecretory activity.
Abstract: Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which X is sulfur, oxygen or substituted or unsubstituted imino,M is sulfur or oxygen,R.sup.2 is hydrogen, or a saturated or unsaturated aliphatic hydrocarbon residue,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, halogen, lower alkyl, acyloxymethyl or heterocyclic-thiomethyl which may be substituted with lower alkyl, andR.sup.5 is carboxy or its derivative, and nontoxic, pharmaceutically salt thereof.
Abstract: A method for treating rheumatism and/or arthritis in mammals afflicted therewith by administering an effective amount of N-(2-mercapto-2-methylpropanoyl)-L-cysteine or a pharmacologically acceptable salt thereof.
Abstract: Novel method optically active oxazaphosphorin derivatives represented by the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are respectively different from each other and are hydrogen atom(s), lower alkyl group(s), aralkyl group(s), or aryl group(s); and X is a halogen atom. The novel oxazaphosphorin derivative is prepared by reacting an optically active amino alcohol derivative represented by the general formula (II), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a phosphorus compound represented by the general formula (III),POX.sub.3wherein X is the same as defined above.The novel optically active oxazaphosphorin derivatives are useful as intermediates for preparing optically active cyclophosphamide derivatives which are useful therapeutical agents for curing against follicular lymphoadenopathy, lymphosarcomatosis, Hodgkin's disease, lymphosarcoma cell leukaemia, reticulum-cell sarcoma or the like.
Abstract: Novel dibenz[b,f]oxepin and dibenzo[b,f]thiepin derivatives of the formula ##STR1## wherein X is an oxygen or sulfur atom, each of R.sub.1 and R.sub.2 is a hydrogen atom or a methyl group, and R.sub.3 is a hydrogen atom or a 2-(2-hydroxyethoxy)ethyl group; provided that when R.sub.1 is a hydrogen atom, the group ##STR2## is a group other than a 1-carboxyethyl group; and when X is a sulfur atom, both R.sub.1 and R.sub.2 are methyl groups;and pharmaceutically acceptable salts of said compounds in which R.sub.3 is a hydrogen atom. Compositions of said compounds, processes for the preparation of said compounds, and a method of using said compounds are also provided. These novel compounds have excellent anti-inflammatory, analgesic and antipyretic activities.
Abstract: A novel process for preparing cyclo-1,3,2-oxazaphosphoryl derivatives represented by the formula (II), ##STR1## wherein R.sup.2 and R.sup.3 are respectively a lower alkyl group which may have halogen atom(s) or lower alkane-sulfonyloxy group(s) as substituted group(s) and n is an integer of 2 to 6, by acid cleaving the R.sup.1 --N bond of the compound represented by the formula (I), ##STR2## wherein R.sup.1 is an .alpha.-arylalkyl group, by using a strong acid, the compound represented by the formula (II) being effective as an anticancer agent.
Abstract: 2-(4-Ethyl-1-piperazinyl)-4-phenylquinoline and its pharmaceutically acceptable acid addition salts, which are useful as antidepressant agents in the treatment of depression or depressive state in mammals including humans, and processes for the preparation thereof.
Abstract: Substituted phenylacetic acid compounds represented by the following general formula and preparation thereof: ##STR1## wherein R.sup.1 is hydrogen or protected carboxy,R.sup.2 is hydrogen, or protected amino, provided that when R.sup.1 is hydrogen, then R.sup.2 is protected amino, and when R.sup.2 is hydrogen, then R.sup.1 is protected carboxy,R.sup.3 is oxo, hydroxyimino or protected hydroxyimino,R.sup.4 is hydrogen or halogen, andm is an integer of 1 to 3.
Abstract: Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein R.sup.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, aralkyl of 7 to 12 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl optionally substituted by chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms or phenyl, or represents a group --C.sub.p H.sub.2p COOR.sup.5, --C.sub.q H.sub.2q OR.sup.6 or ##STR2## (wherein R.sup.5, R.sup.7 and R.sup.8 represent alkyl of 1 to 4 carbon atoms, R.sup.6 represents hydrogen or alkyl of 1 to 4 carbon atoms, p represents an integer of from 1 to 12, and q represents an integer of from 2 to 12), R.sup.2, R.sup.3 and R.sup.
Abstract: A non-fluidizable composition readily convertible into a fluidizable composition by slight stress or pressure, which can be prepared by cooling an emulsion comprisinng a water-immiscible fatty acid, water and an emulsifier from a temperature sufficient to keep the emulsion at a fluidizable state while stirring, stopping the stirring at a temperature not lower than the temperature 5.degree. C. below the congealing temperature of the emulsion and further continuing the cooling to room temmperature and is useful as a base for shaving creams, hair creams, adhesive pastes, printers' inks, shoe polishes, etc.
Abstract: This invention relates to the compound: N-(mercaptoacyl)-histidine represented by the following formula wherein n is 1 or 2, having activity as an antiarteriosclerosis agent, the intermediate thereof and a process for manufacture thereof.