Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: The synthesis of asymmetric tetrasubstituted cyclooctatetraenes (“COTs”) and the use of said compounds in organic light emitting diodes is reported, wherein said COTs represent a class of wide gap electron transporters that are readily deposited in vacuum.

Abstract: The invention concerns the compounds of formula I wherein R1 and R2 independently are hydrogen, acyl, alkoxycarbonyl or alkyl; either the sulfamoyloxy side chain is bound to the 6 position; R3 is alkyl; alkenyl; alkinyl; a cycloalkyl moiety optionally substituted by alkyl, alkoxy or halogen; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; or is 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; and R4 is hydrogen; alkyl; hydroxy; or alkoxy; or the sulfamoyloxy side chain is bound to the 7 position; R3 has the significance indicated above for R4; and R4 has the significance indicated above for R3; X is O or S; and the symbol - - - is a single or a double bond; in free form or salt form. They can be prepared by sulfamoylation of corresponding hydroxylated compounds, by reduction and/or by N-substitution. They are indicated for use as pharmaceuticals, particularly in the prophylactic or curative treatment of illnesses responsive to steroid sulfatase inhibition.

Abstract: Compounds of the formula where R1 and R2, independently are alkyl groups having 2 to 8 carbons; R3 is hydrogen or lower alkyl; X is S, O or N—R4 where R4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH2)n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR5, CONR6R7, —CH2OH, CH2OR8, CH2OCOR8, CHO, CH(OR9)2, CHOR10O, —COR11, CR11(OR9)2, or CR11OR10O, where R5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R5 is phenyl or lower alkylphenyl, R6 and R7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R9 is lower alkyl, R10 is divalent alkyl radical of 2-5 carbons and R11 is alkyl, cycloalkyl or alkenyl containing 1

Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: A triketone derivative represented by the following formula or a salt thereof: wherein, Y1, Y2, Y3, n, p, R1, R2, R3, R4 and X are as defined in claims, prevents growth of a wide variety of cropland weeds in small application rates without causing injury to crops.

Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.

Abstract: The invention relates to compounds of formula (I): wherein: R1, R2 and R3 are as defined in the description, X is as defined in the description, Y represents an oxygen atom, a sulphur atom, a C(H)q group, SO or SO2, n is equal to from 0 to 5, A represents a NR5R6 group, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Abstract: The present invention provides novel compounds of formula I 1

Abstract: The present invention provides novel compounds of formula I 1

Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed.

Abstract: An intermediate represented by the following formula (XVIII), wherein A is a sulfur atom or the group —CH═CH—; L is an alkylene group which may be substituted, an alkenylene group which may be substituted, or an alkynylene group which may be substituted; W represents a leaving group selected from the group consisting of a halogen atom, an alkyl sulfonyloxy group, and an aryl sulfonyloxy group, and Z represents the group; (wherein R1 is an alkyl group which may be substituted, an aromatic carbocyclic group which may be substituted, or an aralkyl group which may be substituted, X1, X2, and X3 individually represent an oxygen atom or a sulfur atom, and G represents an ethylene group or a trimethylene group, of which one or more hydrogen atoms of the ethylene group or trimethylene group may be replaced by a halogen atom, alkyl group, aromatic carbocyclic group, aralkyl group, or alkylidene group).

Abstract: The present invention relates to new compounds of formula (I) wherein R1 to R3, U, V, W, Z and m have the significances given in the description, their use as antidotes, in herbicidal compositions for the control of weeds and plants in useful plant cultivation.

Abstract: The present invention provides compounds of formula I and processes for the preparation and purification thereof. Compounds of formula I are useful as intermediates in the manufacture of 6-(arylcarbonyl)-4-oximino-dihydrobenzothiopyran herbicidal agents.

Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof: 1

Abstract: The present invention provides compounds of formula I and processes for the preparation and purification thereof.

Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: Compounds of the formula 1

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

Abstract: This invention involves compounds having the following structure: 1

Abstract: The present invention provides a compound of the formula (I): wherein R1, R2, R3 and R4 are each independently hydrogen, optionally substituted alkyl, hydroxy, optionally substituted alkoxy or the like, R5 is optionally substituted alkyl, optionally substituted aryl, optionally substituted heterocyclic or the like, R6 is hydrogen, optionally substituted alkyl or the like, R7 is hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heterocyclic or the like, A is S or O and a broken line represents presence or absence of a bond, pharmaceutically acceptable salt or hydrate thereof and a pharmaceutical composition or a pharmaceutical composition for use as an endothelin receptor antagonist, a peripheral circulation insufficiency-improving agent or a macrophage foam cell formation inhibitor comprising the compound.

Abstract: The present invention relates to novel naphthopyrans having a cyclic group annelated in position 6,7. These naphthopyrans have formula (I) given below: These compounds (I) have advantageous photochromic properties. The invention also covers a method of preparing these naphthopyrans, as well as their applications as photochromes and compositions and (co)polymers matrices comprising them.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.

Abstract: There is provided a process for the dehalogenation of a compound of formula II via the use of a transition metal catalyst and ammonium formate at atmospheric pressure.

Abstract: Pyrazole derivatives of the general formula (I) or salts thereof, ##STR1## wherein each symbols are as defined in the specification, herbicides containing the above compounds as active ingredients, and aromatic carboxylic acid derivatives or salts thereof suitable as intermediates for the production of the above pyrazole derivatives.The above pyrazole derivatives or salts thereof, provided by the present invention, cause no phytotoxicity on upland field crops such as corn, etc., and can selectively control a broad range of upland weeds such as grass weeds and broad-leaved weeds at a low dosage in pre-emergence treatment and in post-emergence treatment.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention provides CLA esters and uses thereof. More particularly, the present invention provides a composition for topical use comprising CLA esters and a topical carrier. In addition, the present invention specifically provides tocopheryl CLA esters, ascorbyl CLA esters and retinyl CLA esters.

Abstract: A compound having structure (1) wherein (a) X is selected from the group consisting of O, S, SO, or SO.sub.2 ; (b) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 4 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms; (c) Z is branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; (d) W is O or S; and (e) R is straight, branched or cyclic alkyl or aryl, saturated or mono- or di-unsaturated with double or triple bonds, R having from 1 to about 15 atoms other than hydrogen; pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.

Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.

Abstract: Benzoyl derivatives of the formula I ##STR1## where the substituents L, M, X, Y and n have the meaning given in claim 1 andQ for [sic] a cyclohexane-1,3-dione ring, which is linked in the 2-position, of the formula II, ##STR2## where R.sup.15, R.sup.16, R.sup.18 and R.sup.20 are hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.19 is hydrogen, C.sub.1 -C.sub.4 -alkyl or a group --COOR.sup.14,R.sup.17 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -cycloalkyl, it being possible for these groups, if desired, to carry one to three of the following substituents: halogen, C.sub.1 -C.sub.4 -alkylthio or C.sub.1 -C.sub.4 -alkoxy,orR.sup.17 is tetrahydropyran-3-yl, tetrahydropyran-4-yl or tetrahydrothiopyran-3-ylorR.sup.17 and R.sup.20 together form a bond or a three to six-membered carbocyclic ring,where in the case where Y=C.dbd.O, X is not equal to NR.sup.23,and agriculturally utilizable salts, a process for their preparation and their use as herbicides are described.

Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB.sub.4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfuslon injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.

Abstract: The present invention provides novel heteroaryl compounds having the general formula (I): ##STR1## their pharmaceutical compositions to be used as human and veterinary medicine, particularly in the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic conditions, and their use in cosmetic compositions.

Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.

Abstract: This invention relates to substituted heterocyclic benzocycloalkenes of general formula I or pharmaceutically acceptable salts thereof, to a method of producing them and to their use as analgesics.

Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.

Abstract: The present invention provides compounds of formula I and processes for the preparation and purification thereof. ##STR1## Compounds of formula I are useful as intermediates in the manufacture of 6-(arylcarbonyl)-4-oximino-dihydrobenzothiopyran herbicidal agents.

Abstract: Dienoic retinoids having activity for retinoid X receptors or are panagonists on retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.

Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: A triketone compound of the following formula: ##STR1## wherein Y.sup.1 is C.sub.1 to C.sub.4 alkyl, a halogen or a C.sub.1 to C.sub.4 haloalkyl; each of Y.sup.2 and Y.sup.3 is independently C.sub.1 to C.sub.4 alkyl; Y.sup.4 is hydrogen, C.sub.1 to C.sub.4 alkyl or a halogen; n is 0, 1 or 2; p is 0 or 1; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1 to C.sub.4 alkyl or phenyl; or when p is 1, either R.sup.1 or R.sup.2 and either R.sup.3 or R.sup.4 optionally bond to each other to form an intramolecular double bond; and X is a group of the formula ##STR2## in which each of R.sup.5 and R.sup.6 is independently a hydrogen atom, a C.sub.1 to C.sub.4 alkyl group or a phenyl group. The triketone compound is useful as a herbicide to control a broad range of upland weeks at a low dosage without causing phytotoxicity on corn.

Abstract: The present invention relates to cyclohexanedione derivatives or salts thereof and herbicides containing the cyclohexanedione derivatives and/or salts thereof as active ingredients, the cyclohexanedione derivatives having the general formula (I). ##STR1## The cyclohexanedione derivatives or the salts thereof can selectively control a broad range of upland soil weeds at a low dosage without causing phytotoxicity on crops cultivated in upland fields such as corn, in both upland pre-emergence and post-emergence treatments.

Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.

Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.Pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pair using such compounds.

Abstract: A triketone compound of the following formula: ##STR1## wherein Y.sup.1 is C.sub.1 to C.sub.4 alkyl, a halogen or a C.sub.1 to C.sub.4 haloalkyl; each of Y.sup.2 and Y.sup.3 is independently C.sub.1 to C.sub.4 alkyl; Y.sup.4 is hydrogen, C.sub.1 to C.sub.4 alkyl or a halogen; n is 0, 1 or 2; p is 0 or 1; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1 to C.sub.4 alkyl or phenyl; or when p is 1, either R.sup.1 or R.sup.2 and either R.sup.3 or R.sup.4 optionally bond to each other to form an intramolecular double bond; and X is oxygen or sulfur. The triketone compound is useful as a herbicide to control a broad range of upland weeds at a low dosage without causing phytotoxicity on corn.