Abstract:
The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; R1 is fluorine or bromine; R2 is ethynyl, C1-C3alkoxy, C1-C3haloalkoxy, or C1-C3alkoxy-C1-C3alkoxy-; and Q is a pyran-3,5-dione-4-yl, a thiopyran-3,5-dione-4-yl, a piperidine-3,5-dione-4-yl, a cyclopentane-1,3-dione-2-yl, a cyclohexane-1,3, 5-trione-2-yl, a cyclohexane-1,3-dione-2-yl, or a cycloheptane-1,3-dione-2-yl, or a derivative thereof (e.g. a fused such as fused bicyclic derivative, and/or a spirocyclic derivative), or an enol ketone tautomer derivative thereof, wherein Q is further defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. Preferably, X is methyl; and/or R1 is fluorine; and/or R2 is —O—R2A, wherein R2A is methyl, ethyl, trifluoromethyl, difluoromethyl, trifluoroethyl, or —CH2CH2OCH3. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the weeds and/or to the plants and/or to the locus thereof.
Abstract:
An object of the present invention is to provide a therapeutic preparation and method for diseases associated with cartilage loss, cartilage degeneration and/or cartilage thinning. The present invention provides a therapeutic preparation comprising a pterosin derivative or a pharmaceutically acceptable salt thereof for diseases associated with cartilage loss, cartilage degeneration and/or cartilage thinning; and a therapeutic method for the diseases.
Abstract:
Bioavailability of Coenzyme-Q 10 (“Co-Q10”), an oil-soluble substance, can be enhanced in a subject by modifying, e.g. nanonizing or charging, the form of Co-Q10. Co-Q10 bioavailability also can be enhanced by administering Co-Q10 to the subject as an oil (lipid)-based and water (hydro)-based mixed composition, along with other optional components, such as oils, resins and other carriers. Accordingly, the invention provides various Co-Q10 compositions, e.g. compositions comprised of (i) Co-Q10 dissolved in one or more Co-Q10-soluble oils and (ii) Co-Q10 in admixture with at least one water-dispersible agent. A Co-Q10 complex of the invention, therefore, yields an increased cell absorption rate, as well as an enhanced percentage of Co-Q10 peak absorption, compared to previously known compounds. Methods for making and using the aforementioned compositions also are provided.
Abstract:
The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
Abstract:
This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.
Abstract:
The present invention discloses a separating and purifying (4R, 6R)-4-hydroxy-2,2,6-trimethyl cyclohexanone comprising the steps of:reacting a diastereomer mixture of (4R, 6R)-4-hydroxy-2,2,6-trimethyl cyclohexanone represented by the formula (I) ##STR1## and (4S, 6R)-4-hydroxy-2,2,6-trimethyl cyclohexanone represented by the formula (II) ##STR2## with a reagent which reacts with the hydroxyl groups at least equimolar to the compound represented by the formula (II) to thereby convert the compound represented by the formula (II) into (4S, 6R)-4-hydroxy-2,2,6-trimethyl cyclohexanone derivative represented by the formula (III) ##STR3## (where R represents a group modifying the hydroxyl group) by modification with priority of the hydroxyl group in the formula (II), andseparating the compound of the formula (I) from the compound of the formula (III) through the difference in solubility to water or an organic solvent. According to the invention, (4R, 6R)-4-hydroxy-2,2,6-trimethyl cyclohexanone is easily separated with a high yield.
Abstract:
Method of preparing 4-disubstituted phenyl-1-tetralones of formula ##STR1## in which X represents halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and Y, situated in position 2' or 3', represents halogen or C.sub.1 -C.sub.4 alkyl, this method being characterized in that it comprises the reaction, in the presence of an acid agent, of .alpha.-naphthol of formula (II) with a phenyl compound of formula (III): ##STR2## where X represents halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and Y is situated in the ortho or meta position with respect to X and represents halogen or C.sub.1 -C.sub.4 alkyl.
Abstract:
A therapeutic and prophylactic agent for peptic ulcers comprising as an effective ingredient a cyclohexane derivative represented by general formula (I): ##STR1## wherein A represents a group shown by formula, >CH.sub.2, ##STR2## wherein X represents ethynylene, vinylene or ethylene, Y represents oxo or a hydroxy group; R.sup.1, R.sup.3, R.sup.4 and R.sup.5 each represents a hydrogen atom or alkyl; R.sup.2 represents a hydrogen atom, alkyl or a group shown by --OR.sup.8 ;R.sup.6 represents a hydrogen atom, oxo or a group shown by --OR.sup.8 ; and R.sup.7 represents a hydrogen atom or a group shown by --OR.sup.8, wherein R.sup.8 represents a hydrogen atom or an organic residue.
Abstract:
Novel antiandrogenic compositions comprising an anti-androgenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.-position and a non-toxic, pharmaceutical carrier or excipient and a method of treating hyperandrogenic conditions in warm-blooded animals.