Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.

Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.

Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including anti-ulcerogenic and gastrointestinal cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.

Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.

Abstract: Quinoline compounds having the formula: ##STR1## wherein R is a phenyl group or an aromatic heterocyclic group, Z is an aliphatic heterocyclic group or an amine, and R.sub.1 is hydrogen or a carboxy-protecting group. The compounds here disclosed have antibacterial properties.

Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.

Abstract: The present invention is directed to pyridazino[4,3-c]isoquinolines of Formula I ##STR1## wherein R represents methyl, phenyl or substituted phenyl groups, R.sub.1 represents inter alia amino or substituted amino, alkoxy or cycloalkoxy groups, having pharmacological activity, to process for preparing them and to the pharmaceutical compositions containing them. The compounds of the invention possess anti-anxiety activity.

Abstract: This invention is directed to compounds of the formula ##STR1## wherein X is a thiazine or thiazepine of the formula ##STR2## These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.

Abstract: Novel substituted thiacycloalkeno [3,2-b] pyridines are described. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstrictor activity.

Abstract: N-fluoro-N-perfluoromethyl sulfonamide compounds are provided as fluorinating agents for the fluorination of organic compounds by either the direct electrophilic fluorination of organic compounds or by the fluorination of organic compound carbanions.

Abstract: This invention relates to novel isoxazolo-pyrido-phenoxazine and isothiazolo-pyridophenoxazine derivatives having antibacterial properties and compositions containing methods of treating mammalian patients with these new derivatives.

Abstract: This invention relates to novel isoxazolo-pyrido-benzoxazine and isothiazolo-pyrido-benzoxazine derivatives having antibacterial properties.

Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.

Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.

Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.

Abstract: This invention relates to a process for the production of benzothiazolyl sulphenamides corresponding to the following general formula: ##STR1## in which a corresponding 2-mercaptobenzothiazole or a dibenzothiazolyl-2,2'-disulphide is reacted with a primary or secondary amine at temperatures of from 0 to 100.degree. C. in the presence of ammonia, oxygen, a copper-containing catalyst and a reaction medium containing an excess of the primary or secondary amine or of a mixture of that amine with water and/or a water-miscible organic solvent.Benzothiazolyl sulphenamides are valuable vulcanization accelerators.

Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.

Abstract: Disclosed is a process for producing a heterocyclic compound having as the side chain group a nitromethylene group of the formula: ##STR1## wherein Y, R and n are as defined in the specification, which comprises reacting a 2,2-dihalonitroethylene compound with a 1-aminoalkanethiol compound or a 1-N-substituted derivative thereof.

Abstract: A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.

Abstract: Novel 3-amino-tetrahydro-1,3-thiazine-2,4-diones as well as skin treating compositions on the basis of a physiologically compatible carrier and customary additions containing these novel 3-amino-tetrahydro-1,3-thiazin-2,4-dione derivatives as active ingredients for thickening the epidermis. The skin treating compositions are applied 1-2 times daily on the skin for about 3 to 4 weeks. Due to the thickening of the epidermis they cause a strengthening of the skin protection, in particular against sun rays, cold and the contact with harmful environmental substances of all kinds. Moreover, the skin treating compositions are suitable for prophylactically fighting the so-called ageing of skin.

Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.

Abstract: A new class of anti-spasmodic compounds having three branch chains is provided. These compounds have the general formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are saturated straight chain or branched alkyl groups contained from 1 to 8 carbon atoms, and are separated or linked to one another to form an aliphatic ring system. k is an integer from 0 to 5, and the total number of carbon atoms in R.sub.1 plus R.sub.2 plus R.sub.3 plus k are equal to or less than 12. Furthermore, l is an integer from 1 to 3, m is an integer from 1 to 3, n is an integer from 1 to 3, and X may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the m chain and the n chain is a methyl group.

Abstract: New 3-carbamoyl- and 3-thiocarbamoyl-tetrahydro-1,3-thiazine-2-thiones are disclosed as skin treatment compositions based upon physiologically-compatible carriers and a content of these compounds as active substance for increasing the skin protection, in particular against sun radiation and contact with environmental substances of all types. The skin treatment compositions are also suitable for prophylactic control of so-called aging skin. The compositions are applied to the skin one or two times daily for about 3-4 weeks.

Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: Disclosed is a process for producing a heterocyclic compound having a nitromethylene group as the side chain, of the formula ##STR1## wherein Y represents a hydrogen atom, a halogen atom or a lower alkyl group, R represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aralkyl group, an alkenyl group, an alkynyl group or an acyl group, and n represents an integer of 2, 3 or 4,which comprises reacting a 2,2,2-trihalo-1-nitroethane compound with a 1-aminoalkanethiol compound or a 1-N-substituted derivative thereof.

Abstract: Compounds are described of the formulae (1a) and 1b) ##STR1## in which: R.sup.1 is -H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl,W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH--,Y is a saturated heterocyclic amino group having 5-8 ring members,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) cinnamyl, and Z is --CH.sub.2 OH, --CHO or --CONHR.sup.4 where R.sup.4 is --H or methyl,and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction, and may be formulated for use as antithrombotic and antiasthmatic agents.

Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.