Abstract: This invention relates to intermediates, and processes thereto, for the preparation of tetrahydropyrido[2,3-d]pyrimidines which are useful for the treatment of susceptable neoplasms. The intermediates have the following formula II; ##STR1## wherein the R, R.sup.1 and A groups are as defined in the specification.

Abstract: Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising carrying out a stereoselective addition reaction of an o-(aminoalkylamino) thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the objective compound (VI).

Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.

Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.4 alkyl, hydrogen and, alternatively, R.sub.1 and R.sub.2, together with the attached cationic nitrogen atom can form a 5 to 6-membered heterocyclic ring selected from the group of ##STR2## and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.

Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 together with the attached cationic nitrogen atom forms a 5 to 6-membered heterocyclic ring containing a hetero oxygen atom in addition to the heteronitrogen atom and is selected from the group of ##STR2## and X is an anion. These benzamide heterocyclic derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.

Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a piperidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: A renin inhibiting compound of the formula: ##STR1## wherein X is O, NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-methoxymethoxy)piperidin-1- yl)carbonyl-2-phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopr opylhexanamide.

Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.

Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or control of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.

Abstract: The invention relates to a process for making compounds of formula: ##STR1##

Abstract: A solvent soluble heterocyclic o-hydroxy thione carrying a lipophilic group and the process for the selective extraction of gallium, and certain other related metals, especially from solutions containing excess aluminium.

Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.

Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomeric form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.

Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: This invention relates to a process for resolving racemic or optically enriched 2-benzyl-4-piperidone-succinic acid, comprising reacting such compound with (+)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylamine, (-)-cis-N-benzyl-2-(hydroxymethyl)-cyclohexylamine or (+)-dehydroabietylamine.

Abstract: Novel N-cyclohexylbenzamide derivatives of formula: ##STR1## where R.sub.1 represents an alkoxy radical capable of cyclizing with the aromatic ring;R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, a halogen or an alkoxy, amino, alkylamino or alkyl-carbonylamino group, andZ represents a differently substituted piperidinyl group; and their addition salts with pharmaceutically acceptable acids.The compounds of formula I are powerful gastrointestinal motility stimulants.

Abstract: Substituted anilides of the formula I ##STR1## (where R.sup.1 is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, cyano, nitro, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl;X is methylene, ethylene, vinylene;R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl or together are tetra- or pentamethylene;R.sup.4 is C.sub.1 -C.sub.4 -alkyl, methoxy;n is 2, 3 or 4),and the physiologically tolerated acid addition salts thereof, the pharmaceutical use thereof, drugs produced therefrom and the use thereof for treating cardiac arrhythmias and/or for lowering the heart rate, are described.

Abstract: Disclosed is a piperidine derivatives of a formula: ##STR1## wherein R.sup.0 indicates a hydrogen atom or a group R--CO).sub.n where R is an alkyl, alkylene or arylene group capable of having 1 to 4 carboxylic group;R.sup.1 indicates a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an acyl group having 2 to 7 carbon atoms, or an arylalkyl group having 7 to 10 carbon atoms;R.sup.2 and R.sup.2' respectively indicate a hydrogen atom, or an alkyl group having 1 to 4 carbon atoms;R.sup.3 and R.sup.4 in combination indicate a group .dbd.CH--R.sup.5, or R.sup.3 indicates a hydrogen atom and R.sup.4 indicates either --CH.sub.2 --R.sup.5 wherein R.sup.5 is a substituted or non-substituted phenyl group or a substituted or non-substituted cyclohexyl group the substituent being an alkyl having 1 to 4 carbon atoms, or a 2-furyl group or a tetrahydrofuryl group; andn indicates an integer of 1 to 4.The piperidine derivatives are improved photostabilizer to various organic materials including poly-.alpha.

Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl;Y is ##STR2## --CH.sub.2 --, --O--, --S--, or --SO.sub.2 --; X is --CH.dbd. or --N.dbd.;R.sup.2 is hydrogen when n is 0, otherwise it is hydrogen or --OH;n is one of the integers 0, 1, 2, 3, 4, 5 or 6;A is ##STR3## where R.sup.3 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl; or ##STR4## where R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms; with the provisos that:a) X is --CH.dbd. when Y is ##STR5## --O-- or --S-- and when Y is ##STR6## and R.sup.2 is --OH; b) X is --N.dbd. when A is ##STR7## and c) A is ##STR8## when Y is --S-- or --SO.sub.2 -- and X is --CH.dbd., and their pharmaceutically acceptable salts are Class III antiarrhythmic agents.

Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.

Abstract: Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH=CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.

Abstract: A renin inhibiting compound of the formula: ##STR1## wherein X is O NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-(methoxymethoxy)piperidin-1 -yl)carbonyl-2- phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopropylhexanamid e.

Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.

Abstract: Compounds having the formula ##STR1## in which: R.sub.1 is hydrogen or fluoro;R.sub.2 is halo, trihalomethyl, pentahaloethyl, mono- or difluoromethyl, di-, tri- or tetrafluoroethyl, C.sub.1 -C.sub.2 fluoroalkylthio, C.sub.1 -C.sub.2 fluoroalkoxy, methylthio, methylsulfonyl, halomethylsulfonyl, C.sub.1 -C.sub.2 alkyl or methoxy;R.sub.3 is hydrogen or halo;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.4 alkenyl; C.sub.2 -C.sub.4 alkynyl; C.sub.1 -C.sub.4 haloalkyl; C.sub.2 -C.sub.4 haloalkenyl; C.sub.1 -C.sub.4 alkoxy; C.sub.2 -C.sub.4 alkoxyalkyl, 3-trifluoromethylphenyl, or --(CH.sub.2).sub.n Y;R.sub.5 and R.sub.6 are hydrogen, or R.sub.5 and R.sub.6 together form a bond;R.sub.7 is C.sub.1 -C.sub.4 alkyl;R.sub.8 and R.sub.9 are hydrogen, or R.sub.8 and R.sub.9 together form a bond;Y is cyano; 4-chlorophenyl; C.sub.3 -C.sub.6 cycloalkyl, furyl or tetrahydrofuryl optionally substituted by halo or C.sub.1 -C.sub.4 alkyl; or COR.sub.10 in which R.sub.10 is hydroxy, C.sub.1 -C.sub.5 alkoxy, C.sub.

Abstract: Compounds of formula ##STR1## wherein the substituents are defined hereinbelow, useful in the treatment of bronchospasm are described.

Abstract: N-Phenyl-N-(4-piperdinyl)amide derivatives are disclosed having the general formula (I): ##STR1## wherein X, Ar, R and R.sup.1 are defined, including isomeric forms thereof and acid addition salts thereof. The compounds exhibit analgesic activity. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).

Abstract: 1-Carbonyl derivatives of 4-pentafluorophenoxypiperidines and methods for treating convulsions, depression, and hypertension utilizing compounds or compositions thereof are disclosed.

Abstract: A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.

Abstract: Carbonyl derivatives of 4-pentafluorophenoxypiperidines and methods for treating convulsions, depression, and hypertension utilizing compounds or compositions thereof are disclosed.

Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## where R.sup.3,R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl or gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.

Abstract: Substituted 1-oxy-4-acyloxypiperidines or 1-oxy-4-acylaminopiperidines of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, alkyl or substituted alkyl, R.sub.5 is hydrogen, alkyl, cycloalkyl, allyl or benzyl, X is --O-- or --NE--, E is hydrogen, alkyl or cycloalkyl, A is an n-valent aliphatic or aromatic hydrocarbon radical, and n is 1 to 4 are effective in providing melt flow stabilization to polymeric materials during processing.

Abstract: This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.

Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, is exhibited by a compound of the formula ##STR1## m is 0 to 3; R is selected from:(1) alkyl;(2) substituted alkyl;(3) alkoxy;(4) alkenyl;(5) cycloalkyl;(6) phenyl; and(7) substituted aryl; andR.sup.1 and R.sup.2 are as defined in the specification.

Abstract: The present invention relates to novel phenylimidazolone compounds of the formula ##STR1## wherein A is a bond or C.dbd.T;R is --H, Alk, halo-Alk, cyano-Alk, or phenyl;R.sup.1 is --H, Alk, halogen, halo-Alk, --CN; or when A is a bond, R and R.sup.1 may together form a saturated, partially saturated, or unsaturated three to seven member carbon ring, and the ring may be substituted at any position independently with one or more Alk, --O--Alk, --CN, halogen, --OH, or .dbd.O groups;T is O or S;U is --H;V is --OH, or U and V may together form a bond;W is halogen or --CN, and when W is halogen, R.sup.1 is --CN;X is --H or halogen;Y is --H, halogen, --CN, Alk, --CF.sub.3, or --OCF.sub.3 ;Z is --H, halogen, --OH, Alk, aryloxy, C.sub.1-6 acyl, --NH.sub.2, --NO.sub.2, --NR.sup.2 SO.sub.2 R.sup.2, --N(SO.sub.2 R.sup.2).sub.2, --NR.sup.2 COR.sup.

Abstract: A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represents an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed.

Abstract: The present invention relates to derivatives of 3,4-dehydropiperidin-5-one having herbicidal activity. The derivatives have the formula ##STR1## as defined in the claims. The present invention further relates to a herbicidal composition and a method for controlling weeds which grow among agricultural crops.

Abstract: Novel N-(3-hydroxy-4-piperidinyl)benzamides and derivatives thereof, said compounds being useful as stimulators of the motility of the gastro-intestinal system.

Abstract: N-Phenyl-N-(4-piperdinyl)amide derivatives are disclosed having the general formula (I): ##STR1## wherein X, Ar, R and R.sup.1 are defined, including isomeric forms thereof and acid addition salts thereof. The compounds exhibit analgesic activity. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).

Abstract: The invention relates to novel, therapeutically active 4,4-disubstituted piperidine derivatives of the formula (I), ##STR1## wherein R.sup.1 means hydrogen or --CONHR group, whereinR stands for hydrogen, C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the latter two being optionally substituted on their aromatic moiety by one or more, same or different halogen(s) or one of more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.2 stands for an ethynyl or acetyl group;R.sup.3 and R.sup.4, which are the same or different, represent hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl group or hydroxyl group optionally esterified by a C.sub.1-4 alkanoic acid; andn is 1 or 2,as well as their pharmaceutically acceptable acid addition and quaternary ammonium salts.

Abstract: Disperse dyes, which produce dyeings of excellent thermomigration fastness, consisting of a chromophore and a lactam or oxime radical which detaches on heating to leave an isocyanate or isothiocyanate group, which reacts with a suitable group in the environment. The disclosed dyes are described by the formula ##STR1## where F is the radical of a dye which is free of water-solubilizing groups,B is a bridge member or a direct bond,Z is O or S andV is the radical of a group H--V, where H--V is an oxime of the formula ##STR2## or a lactam of the formula ##STR3## in which R.sup.1 and R.sup.2 are each independently of the other substituted or unsubstituted alkyl or aryl, orR.sup.1 and R.sup.2 together with the carbon atom linking them form a cycloaliphatic ring,R is hydrogen or alkyl andn is an integer from 4 to 11.

Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.

Abstract: Urea derivatives of the following formula: ##STR1## wherein R.sub.2 indicates a piperidino or pyrrolidino group which may be substituted with a hydroxy group or a lower alkyl group having 1 to 13 carbon atoms; A indicates an ethylene group, propylene group, butylene group or butenylene group; R.sub.2 indicates a straight or branched alkyl group having 1 to 20 carbon atoms, a benzyl group, or a phenyl group which may have 1 to 3 substituents such as a lower alkyl group having 1 to 6 carbon atoms, a lower alkoxy group having 1 to 3 carbon atoms, a halogen atom, a trifluoromethyl group, an amino group, a nitro group or a methylenedioxy group; and X indicates an oxygen or sulfur atom, as well as the hydrates and pharmaceutically acceptable salts thereof are useful antiulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.