Abstract: Methods and compositions for the control of nematodes are disclosed. Specifically, the subject anthelmintic compounds have been found to advantageously control nematodes at concentrations which are non-phytotoxic. The anthelmintic compounds can be used in conjunction with other nematicidal agents such as free fatty acids, fatty acid salts, avermectins, ivermectin, and milbemycin.

Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halog

Abstract: Disclosed is a novel class of thiazole, thiadiazole, and oxadiazole compounds which are substituted at their nuclear carbons by aromatic moieties. These compounds exhibit antifungal activity against a variety of fungi including strains which have proven to be resistant to treatment with known antifungal agents such as Fluconazole.

Abstract: Substituted 3,4-bis-alkylamino -1,2,4-thiadioyoles useful for the control of nematodes are disclosed. Specifically, the subject anthelmintic compounds have been found to advantageously control nematodes at concentrations which are non-phytotoxic. The anthelmintic compounds can be used in conjunction with other nematicidal agents such as free fatty acids, fatty acid salts, avermectins, ivermectin, and milbemycin.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.

Abstract: The present invention is directed to new 1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives of the formula (I), 1

Abstract: The present invention is directed to new 1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives of the formula (I), and pharmaceutically acceptable salts thereof wherein Q, R, X, Y and Z are the same as defined in the claims and the description. 1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives of the present invention have antifungal activity and are useful for the treatment of fungal diseases.

Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. 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: Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.

Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.

Abstract: A compound of the formula where: n, and X are as defined in the specification, and the compound possesses selectivity for inhibition of cyclooxygenase-2.

Abstract: The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof.

Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.

Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: The present invention relates to 2-aryl-&Dgr;2-1,3,4-(oxa and thia)diazoline compounds having the structural formula and compositions and methods comprising those compounds for the control of insect and acarid pests.

Abstract: Composition and methods for treating ocular allergic reactions are disclosed. In particular, the invention is directed to compounds which inhibit human conjunctival mast cell degranulation.

Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.

Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.

Abstract: The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a therapeutically effective amount of a compound having the formula where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—, R6 and R7 are independently hydrogen, C1-C6 alkyl, or acyl; n is 0 to 2; R8 is hydrogen or C1-C6 alkyl; W is S or O; Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10; R9 and R10 are independently hydrogen or C1-C6 alkyl; and R5 is where Y is hydroxy, thiol, amino, or NHCN; X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof.

Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q  II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.

Abstract: The invention relates to novel substituted aminosalicylamides, to a plurality of processes for their preparation and to their use as fungicides, and also to novel intermediates and to a plurality of processes for their preparation.

Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.

Abstract: The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1 ; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.

Abstract: Provided are methods of inhibiting the activity of a serine protease using protease inhibitors that include an alpha-keto heterocycle in their structure. The methods are useful in the treatment of ischemic heart or treatment of symptoms associated with blood coagulation disorders. Also provided are methods for detecting or quantifying the activity of a serine protease in a pure sample.

Abstract: The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).

Abstract: The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such as polioviruses, coxsackieviruses of the A and B groups, or echo virus, cardioviruses such as encephalomyocarditis (EMC), apthoviruses such as foot and mouth disease virus, and flaviviruses such as hepatitis C virus and bovine viral diarrhea virus.Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.

Abstract: The invention relates a concentrated liquid fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent and(a) at least one compound of formula I, ##STR1## (b) one or more additional fungicidal active ingredients, which exist as a suspension of fire particles;(c) a solubilizing agent; and(d) a dispersing agent, which has the capability to adsorb irreversibly on the surfaces of hydrophobic particles suspended in water or polar organic solvents.

Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).

Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: A nutritional composition in a dry powder form for optimizing muscle performance during exercise and for enhancing muscle cell repair and recovery following the cessation of exercise. The dry nutritional composition includes carbohydrates and proteins in a ratio in the range of 2.8 to 4.2 parts of the carbohydrates to 1.0 part of the proteins, wherein the carbohydrates are used for providing energy during exercise and the proteins are used for stimulating the release of insulin to the muscle cells during exercise and for repairing muscle cells after exercise.

Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.

Abstract: Disclosed in this invention is a method of analgesic treatment comprising administering an effective analgesic amount of a substituted 2,4-imidazolidinedione compound.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.

Abstract: A substituted 2,4-imidazolidinedione compound corresponding to the formula I ##STR1## a process for production thereof and the use of these compounds in a pharmaceutical preparation are described. Substituents R1, R2, R3 and R4 have the same meaning as defined in the specification.

Abstract: Carboxylic acid derivatives of the formula I ##STR1## here R.sup.1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

Abstract: There are described compounds of the general formula I ##STR1## where the index and the substituents have the following meanings: R is cyano, halogen, alkyl or alkoxy;n is 0, 1 or 2, it being possible for the substituents R to differ from each other if n is 2;Het is a 5-membered heteroaromatic ring having three nitrogen atoms or two nitrogen atoms and one oxygen or sulfur atom and having attached to it an unsubstituted or substituted 6-membered aromatic or heteroaromatic ring;processes for their preparation, and their use.

Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase. Serine protease inhibitors of the invention are useful in the treatment of, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Abstract: Novel benzotriazoles of the formula ##STR1## in which R, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and Y have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.