Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: An emulsifiable pesticidal suspension concentrate composition is provided comprising (a) a pesticidally effective amount of a liquid pesticide of low solubility in water, for example a chloroacetamide herbicide such as acetochlor, (b) a pesticidally effective amount of a solid particulate pesticide, more particularly a salt-forming pesticide, for example a glyphosate herbicide, in solid particulate form, dispersed in the liquid pesticide, (c) a stabilizing amount of a suspension aid, (d) an emulsifying agent in an amount sufficient to emulsify the concentrate composition in a suitable volume of water to form a dilute sprayable composition, and (e) zero to an assay adjusting amount of an inert liquid in which the liquid pesticide is soluble or miscible. The concentrate composition is substantially non-aqueous. The liquid and solid pesticides are selected to be chemically compatible with each other.

Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

Abstract: The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A—B is selected from NHCO, OCH2, SCH2, NHCH2, trans-vinylene, and ethynylene; R1 is linked to ring C at a carbon ortho to the position of A—B attachment and is defined herein; n is 1 or 2; R2 and R3 are alkyl, haloalkyl or together from cycloalkyl or halocycloalkyl as defined herein; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Salts and esters of compounds of formula (I) are also described.

Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.

Abstract: Mammalian hair growth is reduced by applying to the skin a composition that increases cellular ceramide levels.

Abstract: The present invention relates to a nonsteroidal agonist compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine; R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ; R.sub.5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R.sub.4 ; R.sub.6 is a hydrogen, an alkyl, or a haloalkyl; A.sub.1 and A.sub.2 is the same or different, each is direct link or an alkylene; X.sub.1 is an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R.sub.

Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.

Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: Anandamide analogues useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.

Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: A composition which is suitable for controlling fungal pests, comprising conventional additives and an effective amount of a p-hydroxyaniline derivative of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted bicycloalkyl, unsubstituted or substituted bicycloalkenyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy,and a liquid or solid carrier, its use, the use of the compounds I for controlling fungal pests, and the use of the compounds I for the preparation of the compositions.

Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, antiinflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C.sub.3 of the aromatic ring and at C.sub.10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.

Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity, the compounds having the formula A described herein.

Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.

Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.

Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.

Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.

Abstract: Fluorinated alkene compounds useful for controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the formula BrCF.sub.2 CFClCH.sub.2 CO--R where R is R.sub.1 or R.sub.2. R.sub.1 is --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic or aromatic group; an aliphatic amine group; an aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken with the N of R.sub.1 are an amino acid or a cyclic group or R.sub.1 is --OR.sub.5, where R.sub.5 is an aliphatic or aromatic group; an aliphatic amine group; or an aliphatic carboxylic acid group. R.sub.2 is --SR.sub.5 or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic, aromatic or heterocyclic group; an aliphatic amine group; an aliphatic carboxylic acid group; R.sub.5 and R.sub.6 when taken with the N of R.sub.2 are an amino acid or a cyclic group; R.sub.5 and R.sub.6 when taken with the N of R.sub.

Abstract: The present invention is directed to anticoccidial methods, animal feed premixes, and animal feeds, employing a specified o-phenylenediamine or benzimidazole. The present invention is also directed to anticoccidial methods, animal feed premixes, and animal feeds employing two active agents. In such combined therapy, a first substance is a polyether antibiotic, and the second substance is a designated o-phenylenediamine, benzimidazole, or benzimidazoline.

Abstract: A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: ##STR1## where R1=OR.sub.1 ', SR.sub.1 ', or N(R.sub.1 'R.sub.1 ").sub.2, where R.sub.1 ' and R.sub.1 " are H or lower alkyl groups, and R.sub.2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

Abstract: Anandamides useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.

Abstract: Insect repellent compositions are provided comprising mixtures of:(a) from about 5 to about 95%, by weight, of an N-alkyl neoalkanamide having the formula: ##STR1## wherein R.sub.1 R.sub.2, and R.sub.3 are alkyl groups and the sum of the carbon atoms therein is from 6 to 12, and wherein R.sub.4 is either a hydrogen atom or an alkyl group having one to two carbon atoms, and wherein R.sub.5 is methyl, ethyl, or propyl; and(b) from about 5 to about 95%, by weight, of N,N-diethyl-meta-toluamide (DEET).Preferred repellent composition comprise mixtures of N-methyl neodecanamide (MNDA) and DEET which provide synergistic repellency effects against a variety of insects including cockroaches, silverfish, mosquitoes, flies and ants. The repellent compositions may be applied directly to surfaces to be treated or they may be incorporated in detergent compositions such as laundry detergents, floor and wall cleaners, rug cleaners and shampoos, hair shampoos and liquid and bar soaps.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: There are provided with a novel N-substituted-3-halopropiolamide compound, a method of producing the compound, and a composition for controlling noxious organisms containing the compound. The present compound exhibits superior antimicrobial and antifungal effects. Pest control agents containing the compound can advantageously be used for wide applications.

Abstract: The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of azabiaglo and related compounds.

Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## in which R represents halogen or halogenoalkyl,R.sup.1 represents halogen, alkyl or halogenoalkyl,n represents the numbers 0, 1, 2 or 3,X.sup.1, X.sup.2, X.sup.3 and X.sup.4 independently of one another represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio or halogenoalkylthio, andZ represents hydrogen,which have the utility as pesticides and fungicides.

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: N-monosubstituted neoalkanamides of 11 to 14 carbon atoms wherein the substituent on the amide nitrogen is cyclic (aromatic or cycloaliphatic, such as aryl or cycloalkyl) and of at least five carbon atoms, have been discovered to be insect repellent, providing that any aromatic substituent is unsubstituted at the ortho position and that when the neoalkanoyl moiety is pivaloyl the total number of carbon atoms in the N-cyclic neoalkanamide is at least 12. Such neoalkanamides are useful as repellents against cockroaches, including American, German and Oriental cockroaches, and are also effective against mosquitoes (both Anopheles and Aedes), black flies and carpenter ants, and to some extent against deer ticks. They may be applied to areas, locations and items which are desirably to be kept free of such insects, with applications being direct or of solutions or emulsions thereof, preferably by spraying, or in detergent compositions or other products to be applied to such areas, etc.

Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.

Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

Abstract: A method of controlling fungus is provided which comprises contacting said fungus with a fungicidally effective amount of a compound having the following structure: ##STR1## wherein R is a halogen atom, andR.sup.1 is selected from the group consisting of substituted or unsubstituted, straight or branched alkyl having from about 1 to 6 carbon atoms,alkoxy having from about 1 to 6 carbon atoms,halo, provided that when any R.sup.1 is chloro, n is 2 and at least one R.sup.1 is meta-chloro,substituted or unsubstituted sulfamoyl, andsubstituted or unsubstituted carbamoyl,where n is 1 or 2.

Abstract: Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-based moiety (or a guanidine moiety) coupled to a straight chain polyamine.These polyamines as well as a method for regulating NMDA through a spermidine-like effect on NMDA receptors by exposing a cell membrane to selected polyamines are also provided.

Abstract: Compounds of general formula: ##STR1## in which A and R are defined in the description. Medicaments containing the same and useful for the treatment of melatoninergic disorders.

Abstract: A new animal model for Inflammatory Bowel Disease, including idiopathic ulcerative colitis and Chron's disease, as well as methods for problems such as an animal, is provided. Chronic ulcerative condition is induced by topical administration of a sulfhydryl blocker, such as N-ethylmaleimide or iodoacetamide, to the colon. The new animal model is useful for studying the pathogenesis of chronic ulcerative disease, and prevention and treatment thereof, and for evaluating drugs suspected of being useful in the treatment of same.

Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.

Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.

Abstract: A method and composition for controlling molluscs employs fluorinated carboxanilides.

Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.