Abstract: This invention recites substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The substituents A, B, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.

Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.

Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.

Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.

Abstract: Autoinducer molecules, e.g., N-(3-oxododecanoyl)homoserine lactone, for Pseudomonas aeruginosa are described. The molecules regulate gene expression in the bacterium. Therapeutic compositions and therapeutic methods involving analogs and/or inhibitors of the autoinducer molecules also are described. The molecules are useful for treating or preventing infection by Pseudomonas aeruginosa.

Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.

Abstract: A method for coloring Keratin-containing fibers which comprises applying a composition containing a compound of formula A—CH?B—CH?A???(I).

Abstract: The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.

Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.

Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.

Abstract: An electron accepting monomer having the formula: 1

Abstract: The present invention relates to azadioxacycloalkenes of the formula I in which the substituents R1 to R5 and X, the index n and the bridge member W have the following meanings: R1 is C1-C4-alkyl, halogen, C1-C4-haloalkyl, C3-C6-cycloalkyl; R2 is C1-C4-alkyl, C1-C4-haloalkyl, C3-C4-alkenyl, C3-C4-haloalkenyl, C3-C4-alkynyl or C3-C4-haloalkynyl; R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl or unsubstituted or substituted phenyl; R4 is ═CRaRb, —CRd═CRaRb or ═N—ORc, where Ra, Rb, Rc and Rd are each as defined in claim 1; R5 is nitro, cyano, halogen, C1-C6-alkyl or, in the case that n is 2, additionally a bridge which is attached to two adjacent ring atoms; n is 0, 1, 2, 3 or 4, where the substituents R1 may be different if n is greater than 1; X is C1-C4-alkoxy-N═, C1-C4-alkoxy-CH═ or R6—CH═, where R6 is as defined in claim 1 W is unsubstituted or substituted C1-C3-alkylene.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; and R3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.

Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.

Abstract: Compounds of formula I wherein W is optionally substituted alkylene; Y is N or CRa; Ra is hydrogen, halogen or alkyl; R1n represents hydrogen or 1 to 4 substituents; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is optionally substituted alkyl, cycloalkyl, aryl or hetaryl; A is N—OR4, CH—OR4, CH—SR4 or CHR5; R4 is alkyl or haloalkyl; R5 is halogen, alkyl or haloalkyl; methods and intermediates for their preparation. The compounds and compositions comprising them are useful for combating animal pests and harmful fungi.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.

Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.

Abstract: The invention relates to novel heterocyclic imino derivatives, several processes for their preparation and their use for controlling pests.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

Abstract: New azadioxacycloalkenes of the formula (I): ##STR1## wherein Z, G, Ar, E and A are as defined herein, fungicidal compositions containing them, processes for preparing them, and methods of using them to combat fungi.

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

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: The present invention relates to new 2-Phenyl-1-?4-(amino-1-yl-alk-1-ynyl)benzyl!-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below.

Abstract: An N-substituted phenylcarbamic acid derivative represented by the general formula (I): ##STR1## ?wherein R.sup.1 is H, a (C.sub.1-6)alkyl group, a halo(C.sub.1-6)alkyl group, a (C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, a (C.sub.2-6)alkenyl group, a (C.sub.2-6)alkynyl group or a halo(C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, R.sup.2 is H, a (C.sub.1-6)alkyl group, a halo(C.sub.1-6)alkyl group, a (C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, a (C.sub.2-6)alkenyl group, a (C.sub.2-6)alkynyl group, a halo(C.sub.1-6)alkoxy(C.sub.1-6)alkyl group or a cyano(C.sub.1-6)alkyl group, R.sup.3 is a (C.sub.1-6)alkyl group or a halo(C.sub.1-6)alkyl group, each of R.sup.4 and R.sup.5 is a specific group, and Y is O or S! which is very effective in controlling powdery mildew, scab, late blight and gray mold; a process for producing said derivative; an agricultural and horticultural fungicide containing said derivative as an active ingredient; an intermediate of said derivative; and a process for producing the intermediate.

Abstract: The application relates to new azadioxacycloalkenes of the formula (I) ##STR1## in which Z, G, Ar, E and A have the meaning given in the description, to a process for their preparation, and to their use as fungicides.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 is halogen, C.sub.1 -C.sub.3 alkyl, halo-C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo-C.sub.1 -C.sub.3 alkoxy or cyano and/or two substituents R.sub.1 which are bonded to adjacent C atoms of the phenyl ring together are --O--CH.sub.2 --O--; R.sub.2 is hydrogen, halogen or methyl;R.sub.3 is fluorine, chlorine, bromine or C.sub.1 -C.sub.3 alkyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl; either R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, ##STR2## --COCO--R.sub.8, --CO--R.sub.9 or S(O).sub.m --N(R.sub.10)--COO--R.sub.11 andR.sub.6 is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.6 alkenyl, halo-C.sub.3 -C.sub.4 alkenyl, C.sub.3 C.sub.5 alkynyl, halo-C.sub.3 -C.sub.5 alkynyl, C.sub.1 -C.sub.3 alkoxy-C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl; or R.sub.5 and R.sub.6 together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sub.7 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl; R.

Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: The compound N-(.beta.-ketocaproyl)L-homoserine lactone is shown to be an autoinducer that enhances gene expression in a wide variety of microorganisms. Use can be made of this property for diagnostic purposes, e.g., when gene expression causes bioluminescence or antibiotic production, or to promote bacterial growth. The invention claims use for these purposes of the compound and analogs of formula (I) where n is 2 or 3, each of X and Y is O, S or NH, and R is optionally-substituted C1-C12 alkyl or acyl. Some of these are also claimed as new compounds.

Abstract: The invention discloses side-chain homologous vitamin D derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, B, and D have the meanings defined in the specification and either (1) A is a direct bond between carbon atoms 20 and 22 and X is an oxy alkylene radical, --(CH.sub.2).sub.n O-- where n is 1 to 3; (2) A is a methylene bridge, --CH.sub.2 --, between carbon atoms 20 and 22 and X is either an alkylene radical, --(CH.sub.2).sub.n -- or an oxy alkylene radical, --(CH.sub.2).sub.n O--, where n is 1 to 3; or (3) if A is a direct bond and B and D together form a second bond, then X(R.sup.5) (R.sup.6) is ##STR2## The compounds possess proliferation-inhibiting and cell-differentiating activity.

Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Abstract: This invention relates to L-arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: The invention provides compounds of formula ##STR1## wherein X, R and R.sup.1 are defined in the specification. These compounds are useful as antibiotic agents.

Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 is halogen, C.sub.1 -C.sub.3 alkyl, halo-C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halo-C.sub.1 -C.sub.3 alkoxy or cyano and/or two substituents R.sub.1 which are bonded to adjacent C atoms of the phenyl ring together are --O--CH.sub.2 --O--; R.sub.2 is hydrogen, halogen or methyl;R.sub.3 is fluorine, chlorine, bromine or C.sub.1 -C.sub.3 alkyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl;either R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, ##STR2## --COCO--R.sub.8,--CO--R.sub.9 or S(O).sub.m --N(R.sub.10)--COO--R.sub.11 andR.sub.6 is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.6 alkenyl, halo-C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.5 alkynyl, halo-C.sub.3 -C.sub.5 alkynyl, C.sub.1 -C.sub.3 alkoxy-C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl; or R.sub.5 and R.sub.6 together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sub.7 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl; R.

Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.

Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.