Abstract: The present invention provides compounds having useful antibacterial activity and pharmaceutical compositions comprising one or more of these compounds. The invention further relates to a method of treating a bacterial infection in a patient, comprising administering to the patient an effective mount of one or more of the antibacterial compounds of the invention.

Abstract: Novel compounds of general formula I: 1

Abstract: Pyrazole carboxamide derivatives of the formula: 1

Abstract: The present invention provides pyrazole and pyrazolone derivatives. Preferred compounds of the invention are useful as RNA polymerase inhibitors. Further preferred compounds of the invention are useful as antimicrobial agents.

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: Compounds of formula I useful for inhibiting the pain enhancing effects of E-type prostaglandins are disclosed wherein A is a ring system in which the —CH(R3)N(R2)B—R1 and —OR4 groups are positioned in a 1,2 relationship to one another on ring carbon atoms. B is a ring system having R1 in a 1,3 or 1,4 relationship with the —CH(R1)N(R2)— linking group. A, B, R1, R2, R3 and R4 are as defined in the specification and may be substituted. Also disclosed are pharmaceutically-acceptable salts, in vivo-hydrolysable esters and amides of compounds of formula I, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and the use of such compounds as therapeutic agents.

Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y 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-5 and/or CCR-3.

Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) 1

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders.

Abstract: An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic actio

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.

Abstract: Benzylidenepyrazolones of the formula I, Useful as herbicides.

Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: in which U is —(CH2)n—; Q is hydroxy; R is in which V, W, Y, and Z are each hydrogen; X is a five- or six-membered heterocycle; optionally substituted with halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkoxyalkyl, haloalkoxyalkyl, or aminocarbonyl; and the heterocycle is optionally connected to the phenyl ring through a —O—, —S—, —(CH2)p, —C(O)—, or —O—(CR3R4)q linkage; R1 and R2 are independently selected from phenyl or pyridyl substituted with haloalkyl or haloalkoxy; R3 and R4 are independently selected from hydrogen and methyl; n and p are independently 1, 2, or 3; and q is 1 or 2; with the proviso that at least one of R1 and R2 is substituted in the para position; no more than two of R3 and R4 are methyl; each aliphatic moiety contains not more t

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: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts thereof, are disclosed as effective insecticides: wherein U is —(CH2)n—; Q is hydroxy; and R is: and wherein V, W, Y, and Z are each hydrogen; X is a five- or six-membered heterocycle; optionally substituted with bromine, chlorine, fluorine, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkoxyalkyl, haloalkoxyalkyl, or aminocarbonyl; and the heterocycle is optionally connected to the phenyl ring through a —O—, —S—, —(CH2)p, —C(O)—, or —O—(CR3R4)q linkage; R1 and R2 are independently selected from phenyl or pyridyl substituted with pentahalothio, haloalkylthio, haloalkylsulfinyl, or haloalkylsulfonyl; phenyl substituted with —OC(M)2O—, where M is bromine, chorine or fluorine, to provide a dihalobenzodioxolyl fused ring; or pyridyl substituted with —OC(M)2O— to provide a dihalodioxol

Abstract: The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein Ar.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl and lower haloalkyl groups; Ar.sup.2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 are linked to each other to form an alkylene group containing 2 to 4 carbon atoms which may have a lower alkyl group; and R.sup.

Abstract: An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W.sup.1 and W.sup.2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.

Abstract: Novel pyrazole derivatives are provided which are cannabinoid receptor modulators.

Abstract: The present invention relates to certain 3-benzylaminopiperidines which are tachykinin receptor antagonists and are useful in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1, R.sup.2, Ar.sup.1 and HetAr.sup.2 are as described in the specification.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Abstract: The present invention relates to novel 1-sulfonyl-3-phenylpyrazoles of the formula I ##STR1## and agriculturally useful salts of I.

Abstract: The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein A represents a nitrogen atom or a group represented by C--R.sup.5 ; Ar.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl and lower haloalkyl groups; Ar.sup.2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; R.sup.1 represents a hydrogen atom, a lower alkyl group or a bond formed by linking to R.sup.5 ; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 are linked to each other to form an alkylene group containing 2 to 4 carbon atoms which may have a lower alkyl group; and R.sup.

Abstract: Compounds of structure (I) ##STR1## the corresponding N-oxides and agriculturally acceptable salts are disclosed as effective insecticides. In said formula, U is --(CH.sub.2)n--; Q is hydroxy, R is formula (II) ##STR2## in which V, W, Y and Z are hydrogen; X is a five- or six-membered heterocycle optionally substituted; and the heterocycle is optionally connected to the phenyl ring through a --O--, --S-- --CH.sub.2)p--, or --O(CR.sup.3 R.sup.4)q linkage; R.sup.1 and R.sup.2 are independently selected from phenyl or pyridyl substituted with haloalkyl or haloalkoxy; R.sup.3, R.sup.4, n, p, and 1 are as defined in the specification.

Abstract: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 is selected from hydrido, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkynyl, C.sub.1 -C.sub.20 -haloalkyl, aryl-C.sub.1 -C.sub.20 -alkyl, heterocyclic-C.sub.1 -C.sub.20 -alkyl, heteroaryl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -hydroxyalkyl, C.sub.1 -C.sub.10 -alkoxyalkyl, C.sub.1 -C.sub.20 -cyanoalkyl, C.sub.1 -C.sub.20 -aminoalkyl, C.sub.1 -C.sub.20 -alkylamino-C.sub.1 -C.sub.20 -alkyl, carboxy-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkoxycarbonyl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxyaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxy-N-C.sub.1 -C.sub.20 -alkyl-aminocarbonyl-C.sub.1 -C.sub.20 -alkyl, arylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl and aminocarbonyl-C.sub.1 -C.sub.20 -alkyl;wherein R.sup.

Abstract: Compounds of formula (I), wherein R.sub.1 is fluorine, hydroxy, (C.sub.1-5) alkoxy, (C.sub.1-5) alkylthio, hydroxy(C.sub.1-5)alkoxy, a -NR.sub.10 R.sub.11, group, cyano, (C.sub.1-5) alkyl-sulphonyl or (C.sub.1-5) alkylsulphinyl; R.sub.2 and R.sub.3 are each (C,.sub.4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C.sub.1-3) alkyl or (C.sub.1-3) alkoxy; each of R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is independently hydrogen, halogen or trifluoromethyl, and when R.sub.1 is fluorine, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and/or R.sub.9 may also be fluoromethyl; with the proviso that at least one of substituents R.sub.4 or R.sub.7. is other than hydrogen; each of R.sub.10 and R.sub.11 is independently hydrogen or (C.sub.1-5) alkyl, or R.sub.10 and R.sub.

Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.

Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.

Abstract: Novel pyrazole derivatives are provided which are cannabinoid receptor agonists.

Abstract: A class of heteroaromatic compounds incorporating a substituted five-membered heteroaromatic nucleus which contains at least two nitrogen atoms are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia and depression.

Abstract: Compounds of Formula I ##STR1## wherein, R.sub.1 through R.sub.7 are described herein. These compounds inhibit the production of arachidonic acid products associated with 5-lipoxygenase and cyclooxygenase and are useful in the treatment of inflammatory disorders.

Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.

Abstract: 1-Alkyl-4-benzoyl-5-hydroxy-1H-pyrazole compounds in which the benzoyl moiety is substituted in the 2-position with groups such as halo or alkyl, in the 4-position with an alkylsulfonyl group, and in the 3-position with an acyclic or cyclic derivatized amino group, such as 1-ethyl-4-(2-chloro-4-methylsulfonyl-3-(morpholin-4-yl)benzoyl-5-hydroxy-1 H-pyrazole, were prepared and found to be useful for the control of a variety of broadleaf and grassy weeds. The compounds can be applied either preemergently or postemergently and can be used to control undesirable vegetation in corn, rice, and wheat crops.

Abstract: The present invention provides a plant disease control agent containing as active ingredient one or more compounds of the formula ?1!A--COOR.sup.1 ?1!whereinR.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, andA represents a group of the formula (A-1) or (A-2) ##STR1## R.sup.2 represents a C.sub.1 -C.sub.4 alkyl group, R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group,R.sup.4 represents a halogen atom or a C.sub.1 -C.sub.4 alkyl group, andR.sup.5 represents a C.sub.1 -C.sub.4 alkyl group.Further, the compound of A-1 in the formula ?1! in which R.sup.3 is a halogen atom is also included in the present invention.

Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF.sub.1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein Ar, R.sub.1, R.sub.2, A, and Z are various organic and inorganic substituents.

Abstract: Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including --COOR.sup.9 and --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also provided.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention relates to the compounds of general formula ##STR1## used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.

Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.

Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.

Abstract: Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1## wherein: Ar1 and Ar2 can be independantly aromatic, heteroaromatic, or condensed heteroaromatic unsubstituted or substituted with amino, alkoxy, sulfonamido, alkyl, heteroalkyl, halo;m is 0 or 1;n is 0, 1, or 2;het is an aromatic or nonaromatic heterocyclic ring, substituted with alkyl, halo, or alkoxy substituents; andX is a branched or straight chain aliphatic or halogen substituent.

Abstract: The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.

Abstract: A piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof:R.sup.1 --X--A--R.sup.2 (I)wherein R.sup.1 is selected from the group consisting of substituted or unsubstituted pyrazine, naphthalenedicarboxylic acid imide, bicyclo oct-5-ene-2,3-dicarboxylic acid imide and pyromellitimide;X is --(CH.sub.2).sub.n --, --O(CH.sub.2).sub.n --, --S(CH.sub.2).sub.n --, --NH(CH.sub.2).sub.n --, --SO.sub.1 NH(CH.sub.2).sub.n --, ##STR1## --CH.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## wherein n is an integer of 1 through 7 and R.sup.3 is hydrogen, lower alkyl or a benzyl, ##STR3## --O--CH.sub.2 CH.sub.2 CH.dbd. or ##STR4## R.sup.2 is hydrogen, lower alkyl, benzyl, benzyl substituted with hydroxy, methoxy or chlorine, benzoyl, benzyl with a fluorine substituent, pyridyl, 2-hydroxyethyl, pyridylmethyl or ##STR5## wherein Z represents a halogen atom.

Abstract: Compounds of formula (I) ##STR1## wherein one of X and Y represents nitrogen, and the other of X and Y represents oxygen, sulphur or N--R.sup.2 ; Q represents a substituted five- or six- membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the sole heteroatom and is linked to the five-membered heteroatomic ring containing the moieties X and Y via a carbon atom; as well as substituted 1,3-dioxopropane precursors thereto, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia.

Abstract: 1-(Substituted phenyl)-3-(thioimidate)pyrazoles having systemic activity, arthropodicidal (especially insecticidal) and nematocidal compositions comprising same and methods for controlling arthropods (especially insects) and nematodes.

Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.