Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

Abstract: The invention relates to the active lactam compounds with inhibitory effect (anti-proliferative effect) on cancer cells, which are isolated from adlay (Coix lachryma-jobi L. var. ma-yuen Stapf) bran. In the present invention, structures and activities in vitro of the active lactam compounds are further characterized. The active compounds exhibited a strong anti-proliferative effect on cancer cells, such as human lung cancer cell and human colorectal carcinoma cell.

Abstract: The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.

Abstract: This invention concerns the remote detection of threat clouds and evaluation of their components. Also included is the remote detection and evaluation of contamination on surfaces or in air streams. To enable this detection, fluorophores that are attached to POSS are used with two-photon LIF imaging that provides enhanced background-free imaging even in the presence of scattering particles such as dust, sand and water droplets.

Abstract: Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumours, bacterial, fungal or viral infections, or autoimmune diseases.

Abstract: Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.

Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.

Abstract: The present invention relates to novel phenyl-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y, Z and R3 are as defined above, to processes and intermediates for their preparation and to their use as pesticides, microbicides and herbicides.

Abstract: Spirolactam targeting compounds, related compounds, uses of such compounds, and methods of making such compounds are disclosed.

Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.

Abstract: Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R5O, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R11; R3 represents OR6, NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physiolo

Abstract: Disclosed herein are novel spiro beta-lactone/gamma lactams for use in treating bacterial infections and cancer. The compounds are characterized by a terminal electron-withdrawing group such as a nitro group. Screening data shows antimicrobial activity against various bacterial cell lines, particularly gram-positive bacteria, and anti-cancer activity.

Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.

Abstract: A compound represented by the following formula (I) or a salt thereof and a medicament such as an angiogenesis inhibitor and an antitumor agent which comprises said compound or a physiologically acceptable salt thereof as an active ingredient.

Abstract: The present invention provides methods of making substituted phenylketoenols of the general formula I, wherein V, W, X, Y, Z and Het are as defined herein. The compounds have pesticidal and herbicidal activity.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and W are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: A compound represented by the following formula (I) or a salt thereof and a medicament such as an angiogenesis inhibitor and an antitumor agent which comprises said compound or a physiologically acceptable salt thereof as an active ingredient.

Abstract: The invention concerns substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives depicted by the formula: X is alkyl, halogen or alkoxy; Y is hydrogen, alkyl, halogen, alkoxy or alkyl halide; Z is alkyl, halogen or alkoxy; n is 0, 1, 2 or 3; G is hydrogen (a) or one of the groups (b), (c), (d), (e), (f) or (g) as defined in the specification. The invention also concerns methods of preparing the substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivative compounds, intermediate compounds thereof and use of substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivative compounds as pest-control agents.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: The invention provides spiro[pyrrolidine-2,3′-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, &agr;-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles). The new libraries can be assayed using any of many known screening procedures for activity, e.g., biological activity. For example, the libraries can be screened for activity as drugs (e.g., anticancer drugs, antibiotics, antiviral drugs, antiinflammatory drugs, analgesics, immunomodulators, neuroleptics, sedatives, stimulants, or diagnostic aids), bioseparation agents, or pesticides (e.g., herbicides, insecticides, or rodenticides).

Abstract: The present invention relates to new compounds of the formula (I) in which X, Y and Z have the meanings given in the description and Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups  and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and n are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor.

Abstract: The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, .alpha.-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles).

Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in whichHet represents one of the groups ##STR1## wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.

Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.

Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.

Abstract: The invention concerns substituted spiroheterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives of formula (I) in which A and B together with the carbon atom to which they are bound, are an unsubstituted or substituted 5- or 6-membered ring including at least one hetero atom; X is alkyl, halogen or alkoxy; Y is hydrogen, alkyl, halogen, alkoxy or alkyl halide; Z is alkyl, halogen or alkoxy; n is 0, 1, 2 or 3; G is hydrogen (a) or one of the groups (b), (c), (d), (e), (f) or (g), E is a metal-ion equivalent or an ammonium ion; L and M are each oxygen or sulphur and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the description. The invention also concerns methods of preparing such compounds as well as intermediates of formula (XVII) and (II) in which A, B, X, Y, Z and n are as defined in claim 1 and R.sup.8 is alkyl. Compounds of formula (I) are suitable for use as pest-control agents.

Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, W, X, Y and Z have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of monoamine re-uptake and are useful for treating diseases in mammals wherein insufficient synaptic levels of monoamine are implicated. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.

Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

Abstract: The present invention relates to new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded form an unsubstituted or substituted 5- to 7-membered ring which is interrupted by at least one hetero atom,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or one of the groups ##STR2## E represents a metal Ion equivalent or an ammonium ion, L represents oxygen or sulphur,M represents oxygen or sulphur andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description, to processes for their preparation, and to their use as pesticides.

Abstract: The present invention relates to spiro?3H-indole-3(2H),3'-pyrrolidine! derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and to the pharmaceutical and cosmetic compositions comprising them.

Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.

Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.

Abstract: Compounds for formula I ##STR1## in which X represents O, NR.sup.a, S, SO or SO.sub.2 and R is as defined in the specification; and non-toxic metabolically labile esters or amides thereof; and pharmaceutically acceptable salts thereof are useful as modulators of metabotropic glutamate receptor function.

Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

Abstract: The present invention relates to an oxindole compound having the formula 5-cyclohexyl-1,3-dihydro-1-[2-[4-(phenylmethyl)-1-piperazinyl]ethyl]-2H-in dol-2-one for the prevention or treatment of cognitive dysfunctions.

Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## represents a metal ion equivalent or an ammonium ion, L and M represents oxygen and/or sulphur,R.sup.1 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl, which can be interrupted by hetero atoms, optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl or substituted hetaryloxyalkyl,R.sup.2 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or in each case optionally substituted phenyl or benzyl,R.sup.3, R.sup.

Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications.

Abstract: Benzylideneindene compounds, which are useful not only as the photoconductive material for electrophotography, but also as a charge transporting material employed in a function-separating type photoconductor in which an organic or inorganic pigment is used as a charge generating material, and an electrophotographic photoconductor containing at least one of the above benzylideneindene compounds in a photoconductive layer thereof, are disclosed.

Abstract: Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.

Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.