Abstract: Disclosed are novel sulfenate esters and thiosulfinate esters that induce the expression of metabolic enzymes, particularly Phase II enzymes such as glutathione-s-transferase, DT-diaphorase and Ferritin H when administered to a subject. Also disclosed, such compounds are effective to displace a zinc ion from retroviral zinc finger nucleocapsid proteins effective to inhibit HIV replication. The present invention is further directed to novel methods of making these compounds, and any compounds produced by the process of making these novel compounds.

Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and a process for their preparation are described. The compounds are suitable, for example, as anorectics.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to form fungicidal compositions.

Abstract: A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are useful in controlling such protozoan parasites as Giardia lamblia, Leishmania major, Entamoeba histolytica, Cryptosporidium parvum, Toxoplasma gondii and microsporidia.

Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

Abstract: Ophthalmic compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by topically administering to the mammalian eye the ophthalmic composition of the invention which contains as the active ingredient one or more gamma aminobutyric acid agonist compounds.

Abstract: A compound of the general formula I ##STR1## where the indices and the substituents have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, N(OCH.sub.3)CO.sub.2 CH.sub.3 and C(CONHCH.sub.3).dbd.NOCH.sub.3 ;R.sup.2 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl and C.sub.1 -C.sub.4 -alkoxy;m is 0 or 1;R.sup.3 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl and C.sub.1 -C.sub.4 -alkoxy;n is 0, 1, 2 or 3, it being possible for the substituents R.sup.3 to be different from each other when n is 2 or 3;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl and phenyl;X and Y are C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or a C.sub.1 -C.sub.

Abstract: This invention relates to a novel 2-hydroxypropionic acid derivative and its manufacturing method. Based on its mechanism to inhibit the CPT I, 2-hydroxypropionic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and fewer side effects.

Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: The invention relates to novel oximether and acrylic acid derivatives of the formula (I) ##STR1## in which Z, G, Ar, E, R.sup.1 and R.sup.2 have the meanings as given in the specification, to processes for their preparation and to their use as fungicides.

Abstract: The present invention relates generally to methods and compositions for treating amyloidogenic diseases such as Alzheimer's disease and the development of type II diabetes, in which deposition of amyloid in organs such as the brain and pancreas interfere with neurological function and insulin release, respectively. The methods and compositions are directed toward increasing the activity of scavenger cells within the body at recognizing and removing amyloid deposits from affected tissues and organs. Scavenger cells may be targeted to amyloid deposits by means of spontaneously-occurring chemical modifications called advanced glycosylation endproducts (AGEs). Compositions are described which increase scavenger cell activity towards AGE-modified amyloid.

Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.

Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 .ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

Abstract: The present invention relates to novel 10-deacetyl-14.beta.-hydroxybaccatine III derivatives. The novel derivatives, having cytotoxic and antitumour activity, are prepared from this synton after functionalization of the hydroxyls at 1-, 14- as thiocarbonate, iminocarbonate and sulfite and possible oxidation of the hydroxyl at C.sub.10. These derivatives are subjected to a subsequent esterification at position 13- with a variously substituted isoserine chain. The products of the invention can be administered by the injective or oral route, when suitably formulated.

Abstract: Aliphatic nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group and their congeners having efficacy as neuroprotective agents are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono-, di- or tetra-nitrate ester.

Abstract: Conformationally constrained diacylglycerol analogues, pharmaceutical compositions comprising such analogues, and methods of using such analogues as agonists and antagonists of protein kinase C.

Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: Aliphatic Nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group having efficacy as vasodilators are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono, di or tetra nitrate ester.

Abstract: There is disclosed a method for increasing retinal and optic nerve head blood velocity by topical application of carbonic anhydrase inhibitors to the eye.

Abstract: The present invention provides a composition and method of administering same for inhibiting the growth of microorganisms. The composition of the present invention includes sufficient amounts of a peracetic acid or peracetic acid/peracid blend and a non-oxidizing biocide. The method of the present invention includes the step of adding sufficient amounts of the peracetic acid or peracetic acid/peracid blend and the non-oxidizing biocide to industrial process waters.

Abstract: Provided is a method of treating multiple sclerosis employing certain aryl-substituted rhodanines.

Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations exhibiting insulin resistent non-impaired glucose tolerance (IRNIGT) in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed.

Abstract: Disclosed herein is a method of using compounds of the formula:A-N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)-Bwherein A is R.sup.3 R.sup.4 NC(O)CH.sub.2 when, for example, R.sup.3 is hydrogen or alkyl and R.sup.4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolyl-methyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, ?1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl!amino for the treatment of congestive heart failure.

Abstract: The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 andJ represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.

Abstract: The invention relates to the use of 2-(N-(2-aminoethyl)amino)acetic acid derivatives of the formula I ##STR1## in which R denotes, for example, phenyl or thienyl, and their pharmacologically acceptable acid addition salts as pharmacological active compounds.

Abstract: 3-Isothiazolone compositions which are stable, free from turbidity, and do not corrode metal storage containers are disclosed. These compositions further have no possibility of coagulating latex or generating nitrosamine.

Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is R.sup.3 R.sup.4 NC(O)CH.sub.2 wherein, for example, R.sup.3 is hydrogen or alkyl and R.sup.4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Abstract: A composition for restoring and maintaining gastrointestinal health comprises 40-60% by weight of an immunoglobulin composition comprising concentrated immunologically active immunoglobulins and 40-60% by weight of soluble dietary fiber selected from inulin, fructo-oligosaccharides, pectin, guar gum, and mixtures thereof. The immunoglobulin and fiber-containing composition can optionally contain one or more of a beneficial human intestinal microorganism, components of a non-immune natural defense system, an iron-sequestering molecule, and gluconic acid. Preferred beneficial human intestinal microorganisms include lactobacilli and bifidobacteria. The immunologically active immunoglobulins are preferably purified from bovine milk, milk products, or whey. Methods of use are also described.

Abstract: The invention relates to the use of 2-(N-(2-aminoethyl)amino)acetic acid derivatives of the formula I ##STR1## in which R denotes, for example, phenyl or thienyl, and their pharmacologically acceptable acid addition salts as pharmacological active compounds.

Abstract: A compound of the general formula I: ##STR1## is disclosed as a potent anticonvulsant drug. Pharmaceutical compositions and methods of treatment are also disclosed.

Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.

Abstract: Compounds of formula ##STR1## Ar is optionally substituted phenyl, furyl, pyridyl, or thienyl; Y is selected from hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl; L is selected from ##STR2## and R.sup.1 and R.sup.2 are alkyl or together define a group of formula ##STR3## are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Abstract: The present invention is related to the protection of moist stratified squamous epithelia against damage from exposure to noxious luminal agents. Protection of moist stratified squamous epithelia against these noxious luminal agents is afforded by chemical compounds having one of the following reactive groups in their molecule: X--SO.sub.3.sup.-, where X represents oxygen or carbon, and XO.sub.4.sup.= or X.sub.2 O.sub.7.sup.=, where X represents an element from group VIb or sulfur of group VIa of the periodic table. Compounds that provide protection against injury to moist stratified squamous epithelia that illustrate the protective characteristic of these reactive species are the sulfonates, the sulfate esters and the tetrahedral-shaped divalent oxy-anions of the transition metals in group VIb or of sulfur.

Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each independently represents a halogen atom or an alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, alkenoxy, cyano or nitro group; R.sub.3 and R.sub.4 each independently represents a hydrogen atom or an alkyl group; R.sub.5 represents a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonylalkyl group; X and Y each independently represents an oxygen or sulphur atom or a group N--R, in which R is a hydrogen atom or an alkyl group; n is 0-3; r is 0 or 1; m is 0-4; and A or B represents a group of the general formula: ##STR2## wherein R.sub.6 represents a hydrogen or halogen atom, or an alkyl group; and R.sub.7 represents a halogen atom or an alkyl group; the other of A and B being a hydrogen atom or as for R.sub.1 or R.sub.2, have useful pesticidal activity.

Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.

Abstract: The invention relates to salts formed between basic H.sub.2 -receptor antagonists and a complex of bismuth with a carboxylic acid, and solvates of such salts, excluding salts in which the basic H.sub.2 -receptor antagonist is ranitidine. Examples of suitable carboxylic acids are citric acid and tartaric acid. Examples of basic H.sub.2 -receptor antagonists are cimetidine, sufotidine famotidine and nizatidine.The salts are useful in the treatment of gastrointestinal disorders, particularly gastroduodenal conditions. The salts show the antisecretory activity associated with the basic H.sub.2 -receptor antagonist together with antibacterial activity against Campylobacter pylori, and they also possess cytoprotective properties.

Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.

Abstract: Compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n and p are as herein defined; exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Compounds of this class are also useful for the treatment of glaucoma, peptic ulcers, hypertension, congestive heart failure and other types of edema. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.

Abstract: Disclosed are the use of hexamethylenetetramine as a stabilizer for 3-isothiazolones under basic conditions, i.e. above pH 7.0, and compositions comprising HMT and 3-isothiazolones.

Abstract: The present invention relates to propanamines of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted in an identical or different manner with halogen atoms, or lower alkyl, lower haloalkyl or lower alkoxy radicals;R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkyalkyl radical,R5 is a 5-to 7-membered cycloalkyl radical or a phenyl radical, andW represents a heterocycle .dbd.C[Q--(CH.sub.2).sub.n --Q] in which Q is an oxygen or sulfur atom and n is 2 or 3,and their acid addition salts with pharmaceutically acceptable acids. The invention also relates to antidiarrheal pharmaceutical compositions comprising the claimed propanamines.

Abstract: Disclosed is a 1,3,2-dioxathiolan-S-oxide derivative as represented by the general formula (I): ##STR1## (where R.sub.1 and R.sub.2 are identical to or different from each other and each is a hydrogen atom or a lower alkyl group;X is a halogen atom, a cyano group, a lower alkyl group, a haloalkyl group or a phenyl group;m is 0 or an integer from 1 to 5; and when small m is greater than 1 each x can be the same or different andn is 1 or 2).A 1,3,2-dioxathiolan-2-oxide derivative of the compound as represented by the general formula (I-I) is prepared by reacting a hydroxymethylcyclopentanol derivative with thionyl chloride; and a 1,3,2-dioxathiolan-2,2-dioxide derivative (I-II) thereof is prepared by oxidizing the compound (I-I). The compounds (I) can be employed as fungicides and intermediate compounds for the preparation of azolylmethylcyclopentanol derivatives.

Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.

Abstract: A 1,3,2-dioxathiolane oxide derivative is represented by the following formula: ##STR1## wherein X represents --S(O)-- or --S(O).sub.2 --;R.sup.1 represents a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group;R.sup.2 represents a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, andR.sup.3 and R.sup.4 may be the same or different and independently represent a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together form an alkylene group.

Abstract: The present invention is related to the protection of moist stratified squamous epithelia against damage from exposure to noxious luminal agents. Protection of moist stratified squamous epithelia against these noxious luminal agents is afforded by chemical compounds having one of the following reactive groups in their molecule: X--SO.sub.3.sup.-, where X represents oxygen or carbon, and XO.sub.4.sup.= or X.sub.2 O.sub.7.sup.=, where X represents an element from group VIb or sulfur of group VIa of the periodic table. Compounds that provide protection against injury to moist stratified squamous epithelia that illustrate the protective characteristic of these reactive species are the sulfonates, the sulfate esters and the tetrahedral-shaped divalent oxy-anions of the transition metals in group VIb or of sulfur.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefor.

Abstract: Provided is a method for treating Type I diabetes in mammals utilizing certain aryl-substituted rhodanine derivatives.

Abstract: An antimicrobial composition comprises a clathrate compound containing a water-soluble microbicide, and a dispersion medium.For example, the composition may comprise of a clathrate compound containing a water-soluble microbicide and having a particle size of 200 mesh at maximum, said clathrate compound being formed of 5-chloro-2-methyl-4-isothiazoline-3-one and at least one polymolecular host compound selected from the group consisting of 1, 1-di (2,4-dimethylphenyl)-2-propyne-1-ol; 1,1,6,6-tetra(2,4-dimethylphenyl)-2,4-hexadiyne-1,6-diol; 1,1-bis(4-hydroxyphenyl)cyclohexane; N,N,N',N'-tetra(cyclohexyl)-[1,1'biphenyl]-2,2'-dicarboxyamide; 2,2'-methylenebis(4-chlorophenol), deoxycholic acid; and 2,5-di-tert-butylhydroquinone and a dispersion medium.