Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.Pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pair using such compounds.

Abstract: Compounds of formula I ##STR1## in which A is S(O).sub.p or O;p is 0, 1 or 2;g is 0, 1, 2, 3, or 4;n is 2 or 3; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are optional substituents have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, cerebral ischemia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, non-insulin dependent diabetes mellitus, hyperglycemia, and stress.

Abstract: Compounds of the general formula ##STR1## have a pronounced tendency to form liquid crystalline S (smectic) phases. Thus, optically inactive compounds of the formula I also have a tilted smectic phase, in particular an S.sub.C phase, in addition to a nematic phase. In contrast, many optically active compounds of the formula I additionally have, inter alia, a tilted smectic chiral phase, in particular a chiral S.sub.C phase, in addition to a cholesteric phase. The stated compounds are therefore particularly suitable as components and as dopants, respectively, for the preparation of a very wide range of liquid crystalline mixtures. The class of compounds comprising compounds of the general formula I offers a broad range of novel components and mixtures for optimization and modification of liquid crystalline mixtures.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: Compounds based on heterobicyclic derivatives, of general formula (I): ##STR1## possessing fungicidal activity.

Abstract: The present invention relates to oxa(di)azabicyclic and thia(di)azabicyclic compounds, a method for their preparation and their use as herbicides.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention discloses novel compounds useful as alkaline phosphatase inhibitors and therapeutic agents. Preferably, the novel compounds are useful as selective inhibitors of human alkaline phosphatases as opposed to Escherichia coli alkaline phosphatases. The novel compounds can also be used as cancer therapeutic agents, anti-depressive agents, anti-anergic agents, and antihelminthic agents. The novel compounds have the following general formula: ##STR1## wherein R' is an aryl, aryl ether, aryl thioether, aromatic heterocyclic, aromatic heterocyclic thioether, or aromatic heterocyclic ether group. More preferably, R' is a phenyl or a pyridine. Most preferably, R' is of the following formula: ##STR2## 2-thiopyridine, or ##STR3## 2-oxypyridine. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', and R.sub.5 ' can be the same or different, and at least one of which is selected from the group consisting of: H, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, phenyl, C.

Abstract: The invention relates to substituted benzimidazolyl derivatives of the general formula ##STR1## wherein A and R.sub.a to R.sub.c are defined as in claim 1, the mixtures of position isomers thereof and the salts thereof which have valuable properties.These compounds have valuable pharmacological properties, particularly angiotensin-antagonistic effects and preferably angiotensin-II-antagonistic effects.

Abstract: The present invention is concerned with the use of certain 3-aminopyrazolo-heterocyclic compounds for the colorimetric determination of hydrogen peroxide, hydrogen peroxide-forming systems, peroxidase, peroxidate-active substances and electron-rich aromatic compounds. The present invention is also concerned with corresponding processes of determination and with agents appropriate therefor. Furthermore, the present invention is concerned with new 3-aminopyrazolo-heterocyclic compounds.

Abstract: Compounds based on heterobicyclic derivatives displaying fungicidal activity, having the general formula (I): ##STR1##

Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomemlar nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.

Abstract: The present invention is concerned with the use of certain 3-aminopyrazolo-heterocyclic compounds for the colorimetric determination of hydrogen peroxide, hydrogen peroxide-forming systems, peroxidase, peroxidate-active substances and electron-rich aromatic compounds. The present invention is also concerned with corresponding processes of determination and with agents appropriate therefor. Furthermore, the present invention is concerned with new 3-aminopyrazolo-heterocyclic compounds.

Abstract: The invention relates to a novel process for the preparation of imidazothiazolone derivatives of formula I, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in the claims, which are suitable for the preparation of D-(+)-biotin.

Abstract: The present invention relates to novel 6-aryl-5,6-dihydroimidazo[2,1-b]thiazole derivatives having immunostimulating properties, which are useful for treating humans and warm-blooded animals suffering from disorders and/or diseases wherein the immune system is impaired or suppressed. Processes of preparing said novel compounds and compositions containing the same as active ingredient.

Abstract: Novel compounds are provided which exhibit high levels of anti-parasitic activity, specifically against parasites of the genus Trypanosoma. The compounds are comprised of aryl-substituted quaternary heteroaromatic salts which include a positively charged imidazolium or other heterocyclic ring, a linking group, a phenyl ring, and a polar functional group. The polar functional group is preferably a quanylhydrazone or a heterocyclic hydrazone. A method is also provided for treating the diseases associated with Trypanosoma parasites which comprises administering to infected animals or humans an effective amount of a compound of the present invention.

Abstract: A method of inhibiting the 5-lipoxygenase pathway in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a diaryl- substituted imidazole fused to a thiazole pyrrolidine, thiazide or piperidine ring to such animal.

Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.

Abstract: D-(+)-biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in Patent claim 1, in a simple, stereospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

Abstract: Optically active hydantoins of the formula I ##STR1## wherein X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in Patent claim 1, are useful intermediate products for the preparation of D-(+)-biotin.

Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.

Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.

Abstract: A method for preparation of polycyclic 1,3-thiazolidines is described. The method comprises reacting a fluoride ion source, in a solvent, with an onium salt synthesized by the reaction of a nitrogenous heteroaromatic compound with a halomethyl trimethylsilylmethyl sulfide, the halomethyl trimethylsilylmethyl sulfide being selected from the group consisting of chloromethyl trimethylsilylmethyl sulfide, bromomethyl trimethylsilylmethyl sulfide, or iodomethyl trimethylsilylmethyl sulfide.

Abstract: 5,6-dihydroimidazo[2,1-b]thiazole-2-carboxamide derivatives represented by the following general formula [I] ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are either the same or different and mean individually a hydrogen atom or lower alkyl group, Y denotes a specific phenyl-containing substituted amino group, and their salts. These compounds have excellent immuno-modulating activities.

Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.

Abstract: The invention provides certain herbicidal thiazolotriazole sulphonamides, processes for their preparation, and compositions containing them, the compounds being of the formula: ##STR1## where: R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, hydroxy, halo, cyano, substituted or unsubstituted alkyl, alkoxy, alkenyloxy, alkynyloxy, aryl, aralkyl, heteroaryl or carbamoyl, or a group --COR.sup.a or --CO.sub.2 R.sup.a or where R.sup.a is hydrogen or alkyl; or R.sup.1 and R.sup.2 together represent an alkylene chain of 3 or 4 carbon atoms;R.sup.3 represents a substituted or unsubstituted aryl, heterocyclyl or benzheterocyclyl group; andR.sup.4 represents hydrogen, an alkali-metal atom, an ammonium group, a substituted or unsubstituted alkyl, alkenyl, alkynyl, acyl, alkoxycarbonyl or aralkyl group, a heterocyclic group, or a group of the formula: ##STR2## where R.sup.1 and R.sup.2 are as defined hereinbefore.

Abstract: Nitrofuran derivatives of formula (I) ##STR1## in which n is 0 or 1 and R is a selected heterocyclic radical have useful antibacterial, antiparasitic and antifungal activity.

Abstract: This invention relates to novel compounds having antidotal activity so as to be useful in the protection of cultivations of agrarian interest from the toxic action of non-selective weed-killers. The novel compounds of this invention have the formula: ##STR1## wherein R=alkyl, phenyl; R.sup.1 =OR.sup.4 =alkyl, cycloalkyl, cyclohexylmethyl, allyl, propargyl, phenyl or benzyl, optionally substituted; R.sup.2 =H or R.sup.1 and R.sup.2 together form a bond between carbonyl and the nitrogen atom which they are linked to; X=O, S; R.sup.3 is the same are R.sup.4, but is different from 3,5-dichlorophenyl.

Abstract: A novel process is described for preparation of biotin comprising preparation of substituted 3H, 5H-imidazo[1,5c]tetrahydro thiazoles by contacting the boron trifluoride adduct of an appropriate thiazoline with the metallic derivative of an ester enolate, reducing the ester, hydrolyzing the thiazolidine moiety and hydrolyzing or oxidizing the resultant compound. Intermediates obtained in the preparation of biotin by the above process and alternate procedures for preparing said intermediates are also presented. A novel process for preparation of d-biotin is also given.

Abstract: 5,6-dihydroimidazo[2,1-b]thiazole-2-carboxamide derivatives represented by the following general formula [I] ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are either the same or different and mean individually a hydrogen atom or lower alkyl group, Y denotes a specific phenyl-containing substituted amino group, and their salts. These compounds have excellent immuno-modulating activities.

Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.

Abstract: D-(+)-Biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in patent claim 1, in a simple, stereospecific manner.Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

Abstract: Cardiotonic fused aromatic bicyclic ring substituted thiazole compounds and their salts, methods for increasing cardiac contractility in humans and other mammals by the use of said compounds, pharmaceutical compositions including said compounds and methods for compound preparation.

Abstract: A process for the preparation of a thieno-imidazole derivative, particularly descarboxybiotin, a useful intermediate for the preparation of d-biotin, which comprises reacting a thio-substituted intermediate, for example descarboxythiobiotin, with an epoxy compound in an alkanol solvent; and a process for the preparation of said intermediate by reacting a substituted imidazothiazole alcohol with anhydrous hydrogen fluoride.

Abstract: Novel 3,5-di-tert-butyl-4-hydroxyphenyl-substituted heterocyclic compounds shown by the formula ##STR1## wherein .circle.Het -- represents a specific heterocyclic group and the salts thereof.The compounds have an anti-inflammatory, an anti-pyretic, an analgesic, an anti-arthritic, and an immunoregulatory activity. Hence, they are particularly useful as an antirheumatics.

Abstract: Compounds of the formula wherein R is ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are the same or different and are selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, lower alkoxy and naphthyl, provided that when R.sub.1 is lower alkyl, R.sub.2 and R.sub.3 are hydrogen, chlorine, bromine or lower alkoxy, or a pharmaceutically acceptable salt thereof, have anti-carrageenin edema activity, and are useful as anti-inflammatory agents and immuno modulators. They are produced by reacting an amide of the formula ##STR2## wherein R has the same meanings hereinabove, with N,N'-ethylene thiourea.

Abstract: Compounds of the formula ##STR1## wherein R is ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are the same or different and are selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, lower alkoxy and naphthyl, provided that when R.sub.1 is lower alkyl, R.sub.2 and R.sub.3 are hydrogen, chlorine, bromine or lower alkoxy, or a pharmaceutically acceptable salt thereof, have anti-carrageenin edema activity, and are useful as anti-inflammatory agents and immuno modulators. They are produced by reacting an amide of the formula ##STR3## wherein R has the same meanings hereinabove, with N,N'-ethylene thiourea.

Abstract: Novel compounds, viz. 6-phenyl-2,3,5,6-tetrahydroimidazo-[2,1-b]-thiazole derivatives have the following general formula: ##STR1## wherein R is CH.sub.2 COOCH.sub.3, CH.sub.2 COOC.sub.10 H.sub.21, CH.sub.2 CONH.sub.2 X is Br.The compounds possess immunomodulating, antibacterial and antiviral activity.

Abstract: Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, one of Y and Z is a heterocyclic moiety, and the other of Y and Z is hydrogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms are useful as anthelmintics.

Abstract: A novel 2-phenylimidazo[2,1-b]benzothiazole derivative shown by the following formula ##STR1## or a salt thereof which possesses an immunoregulatory action and is useful as an antiallergic agent, an antiasthmatic, and a suppressant of rejection at tissue transplantation and skin graft.

Abstract: A series of bicyclic imidazole and imidazoline derivatives, including their non-toxic acid addition salts, are disclosed. These particular compounds are useful for combatting ectoparasite and helminth infestations in animals, especially sheep and cattle. 2-(2,3-Dimethylphenyl)-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.

Abstract: A novel process is described for preparation of biotin comprising preparation of substituted 3H, 5H-imidazo[1, 5c]tetrahydro thiazoles by contacting the boron trifluoride adduct of an appropriate thiazoline with the metallic derivative of an ester enolate, reducing the ester, hydrolyzing the thiazolidine moiety and hydrolyzing or oxidizing the resultant compound. Intermediates obtained in the preparation of biotin by the above process and alternate procedures for preparing said intermediates are also presented. A novel process for preparation of d-biotin is also given.

Abstract: The invention relates to imidazoazole-alkenoic acid amides of Formula (I) and methods for their production. Also included in the invention are compositions containing said alkenoic acid amides and methods for the use of said alkenoic acid amides and the compositions containing them. In addition, the invention includes the intermediate carbonyl compounds of Formula (II) and the intermediate alkenoic acids of Formula (V) as well as methods for their preparation.

Abstract: Phenethyl derivatives of thiazole of the formula: ##STR1## wherein n is 1 or 2 and R is a naphthyl radical, a phenyl radical or a phenyl radical carrying one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, methylenedioxy and trifluoromethyl radicals and halogen atoms, are useful in therapy in the treatment of depression.

Abstract: Novel derivatives of bicyclic 2-iminothiazolidine oximes and methods of preparing same. This invention is also directed to an insecticidal composition comprising an acceptable carrier and an insecticidally effective amount of a compound of this invention, as well as to a method of controlling insects which comprises subjecting the insects to an insecticidally effective amount of a compound of this invention.

Abstract: Compounds of formula (I) in the 1-form ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is selected from hydrogen, optionally substituted (C.sub.1-7) alkyl, optionally substituted aryl and aromatic heterocyclyl and the dotted line is an optional direct bond, and acid addition salts thereof, are useful in treating worm infections in mammals. Compounds (I) are produced by forming the amide of m-aminotetramisole or by closing the dihydroimidazoline ring.

Abstract: A heterocyclic-substituted oxoalkanoic acid derivative having immunomodulatory activities of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, phenyl which may be substituted by at least one substituent selected from halogen, lower alkyl, lower alkoxy, mono- or di-lower alkyl amino-substituted lower alkoxy, lower alkylthio, lower alkylsulfinyl, amino, nitro and cyano at any position(s) on the nucleus, thienyl or furyl, each of R.sup.2 and R.sup.3 is hydrogen or lower alkyl, A is lower alkylene, X is sulfur or vinylene, Y is nitrogen or methine which may be substituted by lower alkyl, Z is carbonyl or direct bond.