Abstract: Compounds of the formula 1

Abstract: The invention relates to triazole compounds of formula (I), in which R1, R2, A and B have the meanings given in the description. The compounds provided for in the invention have a high affinity for the dopamine-D3-receptor and can therefore be used for the treatment of diseases which respond to the influence of dopamine-D3-ligands.

Abstract: A chromene compound which develops yellow to red color, a high color density and a little initial color and which, when used in combination with an existing photochromic compound that exhibits blue color so as to develop a neutral tint, maintains uniformity in the color tone at the time of developing color or fading color, or exhibits a very large color fading rate.

Abstract: This invention relates to substituted benzo[1,2-b:5,4-b′]dipyran-4-amines which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and a topic disorders (for example, a topic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzo[1,2-b:5,4-b′]dipyran-4-amines which are CCR5 receptor antagonists. Furthermore, since CD8+T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therpeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

Abstract: Secretion of small molecules from systemic blood circulation into urine is one of the physiologically essential functions of the kidney. Human organic anion transporter (hOAT1) is a key component in the renal tubular secretion of negatively charged molecules including a variety of important therapeutics. In some cases, compounds interacting with hOAT1 may induce pharmacokinetic drug-drug interactions or cause nephrotoxicity. We developed a fluorescence-based, 96-well format assay using CHO cells stably expressing hOAT1, which allows for the evaluation of interactions between small molecules and hOAT1. The assay is based on the inhibition of the transport of 6-carboxyfluorescein, a high-affinity hOAT1 substrate (Km=3.9 &mgr;M), which was identified among several other fluorescent organic anions.

Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.

Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: 2-Alkoxydecahydro-2,3a,4,4,7-pentamethyl-3,7a-methano-7aH-indeno[5,6-b]furans are valuable novel woody fragrances for the preparation of perfume oils.

Abstract: A method of preparing tetrahydrocannabinol using extraction of plant material with a non-polar solvent followed by vacuum distillation and collection of a constant boiling fraction. Additional distillation steps and chromatographic steps, including HPLC reversed phase HPLC and flash chromatography, may be performed.

Abstract: The present invention relates to non-psychoactive derivatives of tetrahydro-cannabinol, which exhibit anti-inflammatory, analgesic and leukocyte antiadhesion activities. The invention includes novel derivatives of (3R,4R)-&Dgr;8-tetrahydrocannabinol-11-oic acids [hereinafter referred to as (3R,4R)-&Dgr;8-THC-11-oic acid], as well as pharmaceutical compositions containing the (3R,4R)-&Dgr;8-THC-11-oic acid derivatives. The invention further covers methods of administering the novel derivatives and pharmaceutical compositions as therapeutic agents in the treatment of pain and tissue inflammation. Non-psychoactive derivatives of &Dgr;8-THC-11-oic acid are described which have analgesic and anti-inflammatory properties.

Abstract: The invention relates to the use of substituted aminomethyl-chromans for the treatment of neuronal degeneration and for the promotion of neuronal regeneration in cerebral injuries and chronic disorders of the nervous system.

Abstract: A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.

Abstract: Highly specific biocatalytic reactions have been used to create a population of derivatives from a single starting compound. Examples demonstrate synthesis of derivatives of taxol, taxol-2'-adipate, taxol-2'-vinyl adipate, 2,3-(methylenedioxy) benzaldehyde, (.+-.)-(2-endo, 3-exo)-bicyclo (2.2.2)octo-5-ene-2,3-dimethanol, adenosine and erythromycin.

Abstract: A set of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structures ##STR1## wherein R.sub.1 -R.sub.6 are hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrite, lower alkoxy, linking group, or, when taken together, R.sub.1 and R.sub.6 is benzo, or, when taken together, R.sub.4 and R.sub.5 is benzo; R.sub.7 -R.sub.10, R.sub.12 -R.sub.16 and R.sub.18 may be hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrite, lower alkoxy, linking group; R.sub.11 and R.sub.17 may be hydrogen, lower alkyl, lower alkene, lower alkyne, phenyl, aryl, linking group; Y.sub.1 -Y.sub.4 are hydrogen, lower alkyl, or cycloalkyl, or, when taken together, Y.sub.1 and R.sub.2, Y.sub.2 and R.sub.1 Y.sub.3 and R.sub.3, and/or Y.sub.4 and R.sub.4 is propano, ethano, or substituted forms thereof, and X.sub.1 -X.sub.

Abstract: A broad class of photosensitive compounds having enhanced in vivo target tissue selectivity and versatility in photodynamic therapy. Many furocoumarin compounds, such as psoralens, exhibit cytostatic activity when photoactivated but exhibit little in vivo specificity for selectively accumulating in any particular target tissue such as atheromatous plaques. Reactive Oxygen Producing Photosensitizers ("ROPPs") are photoactivatable compounds having an affinity for hyperproliferating cells (such as atheromatous plaque cells), which when photoactivated, produce cytotoxic reaction products. The photoactivity of a ROPP, such as a porphyrin, may be reduced by metalating the porphyrin while the selective affinity of the metalized ROPP for hyperproliferating tissue remains substantially unchanged.

Abstract: The present invention provides an antifeedant and a contact insecticide using the components contained in Cyperaceae species. In particular, the present invention provides an insect antifeedant and a contact insecticide comprising as an active ingredient at least one compound selected from the group consisting of scabequinone, remirol, cyperaquinone and the derivatives thereof.

Abstract: A class of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structure ##STR1## wherein R.sub.1 -R.sub.6 are hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group, or combinations thereof, or, when taken together, R.sub.1 and R.sub.6 is benzo, or, when taken together, R.sub.4 and R.sub.5 is benzo; Y.sub.1 -Y.sub.4 are hydrogen or lower alkyl, or, when taken together, Y.sub.1 and R.sub.2, Y.sub.2 and R.sub.1 Y.sub.3 and R.sub.3, or Y.sub.4 and R.sub.4 is propano, ethano, or substituted forms thereof; and X.sub.1 -X.sub.3 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylate, sulfonic acid, --CH.sub.2 OH, and linking group. In another aspect, the invention includes reagents labeled with the 4,7-chlororhodamine dye compounds, including deoxynucleotides, dideoxynucleotides, and polynucleotides.

Abstract: High-purity isochroman compounds can be obtained in high yields according to a simple and economical process for preparing isochroman compounds, comprising the step of adding an aquesous solution of formaldehyde having a concentration of 40 to 70 wt. % to a complex of an arylalkanol represented by the following general formula (II) with a Friedel-Crafts catalyst to cyclize the arylalkanol: ##STR1## wherein R.sub.1 and R.sub.2 each stands for a hydrogen atom, a lower alkyl group or a lower alkoxyl group, or alternatively R.sub.1 and R.sub.2 are respectively bonded to adjacent carbon atoms with mutual bonding of R.sub.1 and R.sub.2 together with the carbon atoms respectively bonded to R.sub.1 and R.sub.2 to form a benzene ring, a naphthalene ring, or a C.sub.5 or C.sub.6 cycloalkane or cycloalkene which may have 1 to 6 lower alkyl groups; and R.sub.3 stands for a hydrogen atom or a lower alkyl group.

Abstract: A class of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structure ##STR1## wherein R.sub.1 -R.sub.6 are hydrogen, fluorine, chlorine, lower alkyl lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, lining group, or combinations thereof or, when taken together, R.sub.1 and R.sub.6 is benzo, or, when taken together, R.sub.4 and R.sub.5 is benzo; Y.sub.1 -Y.sub.4 are hydrogen or lower alkyl or, when taken together, Y.sub.1 and R.sub.2 is propano and Y.sub.2 and R.sub.1 is propano, or, when taken together, Y.sub.3 and R.sub.3 is propano and Y.sub.4 and R.sub.4 is propano; and X.sub.1 -X.sub.3 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl carboxylate, sulfonic acid, --CH.sub.2 OH, and linking group. In another aspect, the invention includes reagents labeled with the 4,7-dichlororhodamine dye compounds, including deoxynucleotides, dideoxynucleotides, and polynucleotides.

Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.

Abstract: A broad class of photosensitive compounds having enhanced in vivo target tissue selectivity and versatility in photodynamic therapy. Many furocoumarin compounds, such as psoralens, exhibit cytostatic activity when photoactivated but exhibit little in vivo specificity for selectively accumulating in any particular target tissue such as atheromatous plaques. Reactive Oxygen Producing Photosensitizers ("ROPPs") are photoactivatable compounds having an affinity for hyperproliferating cells (such as atheromatous plaque cells), which when photoactivated, produce cytotoxic reaction products. The photoactivity of a ROPP, such as a porphyrin, may be reduced by metalating the porphyrin while the selective affinity of the metalized ROPP for hyperproliferating tissue remains substantially unchanged.

Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.

Abstract: The invention is concerned with the 7R/7S-diastereoisomer mixture of the formula ##STR1## in pure form, essentially free of the corresponding (4R)-isomers. The invention also concerns the 2R/2S-diastereoisomer mixture of the formula ##STR2## in pure form which is useful as an intermediate for producing I. In addition, the invention concerns a process for obtaining I by subjecting II to isochromane ring closure. Odorant compositions containing I and the use of I as an odorant are also described.

Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis. In the formula,X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms Or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.

Abstract: Described are methyl, substituted propyl-substituted pentamethyl indane derivatives defined according to the structure: ##STR1## wherein R.sub.1 represents chloro, hydroxyl or OR.sub.6 ; and R.sub.5 represents methyl or hydrogen with the proviso that when R.sub.1 is chloro, R.sub.5 is hydrogen, and wherein the structure represents a mixture wherein in the mixture in one of the compounds R.sub.4 and R.sub.4 ' are both methyl and R.sub.7 is methyl (about 90% by weight); and in the other compounds one of R.sub.4 or R.sub.4 ' is methyl and the other is ethyl (about 10% by weight of the compounds) and R.sub.7 is hydrogen; and uses thereof in augmenting, enhancing or imparting aromas in or to perfume compositions.Also described are processes for preparing such methyl, substituted propyl-substituted pentamethyl indane derivatives using as a starting material the mixture of compounds defined according to the structure: ##STR2## also know as GALAXOLIDE.RTM. (trademark of International Flavors & Fragrances Inc.).

Abstract: Described are methyl, substituted propyl-substituted pentamethyl indane derivatives defined according to the structure: ##STR1## wherein R.sub.1 represents hydroxyl or methyl; and R.sub.2 represents hydrogen, chloro or OR.sub.6 ; and R.sub.3 represents hydrogen or methyl with the provisos:(i) when R.sub.1 is hydroxyl, R.sub.2 is hydrogen and R.sub.3 is methyl; and(ii) when R.sub.1 is methyl, one of R.sub.2 is chloro or OR.sub.6 and R.sub.3 is hydrogenaugmenting, enhancing or imparting aromas in or to perfume compositions, colognes and perfumed articles including but not limited to solid or liquid anionic, cationic, nonionic or zwitterionic detergents, perfumed polymers, fabric softener compositions, fabric softener articles, cosmetic powders and hair preparations.Also described are processes for preparing such methyl, substituted propyl-substituted pentamethyl indane derivatives using as a starting material the mixture of compounds defined according to the structure: ##STR2## also know as GALAXOLIDE.RTM.

Abstract: A cyclopropachromen derivative represented by formula (I): ##STR1## The compounds are capable of promoting the extension of nerve dendrites and are useful as improving and treating agents for cerebral organic disorders and psychic function disorders.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: Iso- and heterocyclic phenylsulphonamides can be prepared by reaction of corresponding iso- and heterocyclic amines with phenylsulphonic acid derivatives. The iso- and heterocyclic phenylsulphonamides have thrombocyte aggregation-inhibiting and thromboxane A.sub.2 antagonist action and can be used in medicaments.

Abstract: Process for the preparation of polycyclic ethers of formula ##STR1## wherein X represents --(CH.sub.2).sub.n --, index n stands for integer 0 or 1, symbol R.sup.4 designates a hydrogen atom or a methyl radical, symbols R.sup.1 and R.sup.2, identical or different, represent each a hydrogen atom or a lower alkyl radical from C.sub.1 to C.sub.3 and R designates either a C.sub.1 to C.sub.6 linear or branched alkyl radical, or a substituted or unsubstituted alkylene radical having 2 or 3 carbon atoms in the main chain, said alkylene radical forming a ring such as indicated by the dotted line, which process comprises the cyclization by means of an acidic agent of an unsaturated compound:a) of formula ##STR2## having a double bond in one of the positions indicated by the dotted lines, and wherein index m defines an integer number equal to 1 or 2, symbol R.sup.

Abstract: Flavone-3-carboxylic acid compounds corresponding to the Formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, lower alkyl, halogen, hydroxy, or etherified or esterified hydroxy, and Z-R.sup.6 stands for a basically substituted alkoxy or amino group, as well as processes and intermediate products for their production. The compounds exhibit inflammation-inhibiting pharmacological activity.

Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.

Abstract: A process for purifying lysocellin which comprises mixing lysocellin solids with sufficient halogen acid to convert fatty acid ester salt impurities into water-soluble metal halogen salts and water-insoluble free fatty acids and to convert lysocellin salts into water-soluble metal halogen salts and water-insoluble lysocellin acid, separating the halogen salts from the lysocellin acid and fatty acid solids, mixing the lysocellin acid and fatty acid solids with sufficient caustic reagent to convert free fatty acids into water-soluble alkali metal salts and to convert lysocellin acid into a water-insoluble alkali metal lysocellin salts, and separating the water-soluble fatty acid alkali metal salts from the alkali metal lysocellin solids.

Abstract: This invention relates to novel compounds of formula [I], a process for their production, and their use as a herbicide. ##STR1## wherein A represents the bond ##STR2## in which X is a hydrogen atom, a chlorine atom, a nitro group or a trifluoromethyl group;B represents a hydrogen atom, a methyl group or a methoxy group; andAr represents one member selected from the group consisting of ##STR3## in which R.sup.1 to R.sup.38, are as defined hereinafter.

Abstract: The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.

Abstract: Mixtures of racemic (+)pyrano[3,4-b]indole-1-acetic acids are resolved with (-)-borneol to obtain the substantially pure (+) and (-)-enantiomers. The resolution involves the formation of a mixture of the diastereoisomeric pyrano[3,4-b]indole-1-acetic acid, (-)-borneol esters, separation of the diastereoisomeric esters, and hydrolysis of the latter esters.

Abstract: A process for the preparation of an isochromane of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and denote hydrogen, lower alkyl or lower alkoxy, or together form a cyclopentane or cyclohexane ring which is optionally substituted by lower alkyl andR.sup.3 denotes hydrogen or lower alkyl,comprising reacting an alcohol of the formula ##STR2## with formaldehyde and a carboxylic acid anhydride of the formula ##STR3## or with a methylene diester of the formula ##STR4## in which R.sup.4 represents a lower alkyl radical, in the presence of an acid catalyst. The products are known, having a musk-like odor.

Abstract: Novel compounds of the following general formula: ##STR1##