Abstract: The present invention discloses a ?-(3,5-dimethoxybenzylidene)-??-hydrocarbyl methylene cyclic ketone with the following formula: wherein R is aryl or alkyl, its preparation method is: the cyclic ketone blended with morpholine are subjected to azeotropic dehydration to give enamine, the enamine is condensed with 3,5-dimethoxybenzaldehyde and then condensed with alkyl or aryl formaldehyde under acidic or basic conditions to give the product, the present invention further discloses an antitumor agent comprising ?-(3,5-dimethoxybenzylidene)-??-hydrocarbyl methylene cyclic ketone or medically acceptable salts and pharmaceutically acceptable carriers thereof.

Abstract: The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.

Abstract: The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formula 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formula C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.

Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand Timoptic™ and Compound A.

Abstract: The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.

Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.

Abstract: The present invention relates to the use of certain spiro, ketone and carboxylic acid compounds for the inhibition of the peptidyl-prolyl cis/trans isomerase activity of cyclophilins and the use of these compounds for the production of a cosmetic or pharmaceutical composition for the promotion of hair growth or for the treatment or prevention of inflammatory autoimmune diseases, of diseases caused by fungi, of bacterial infections, of viral infections, of diseases caused by parasites, protozoa or worms, of cancer, of diseases of cells, of fibrosing diseases, and of non-neoplastic changes and diseases which are attributable to prions and changes in the structure and function of cellular proteins and cells.

Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.

Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.

Abstract: Substituted phenanthrene-9,10-diones in accord with structural diagram I, 1

Abstract: The present invention relates to the compounds of formula: in which R1, R2, R3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.

Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries, which composition comprises 40 to 98% by weight of the UV absorber or the UV absorber mixture, 0.01 to 30% by weight of one or more signal substance(s) and 0.1 to 20% by weight of one or more pesticidally active compound(s) of the formulae (I) to (V) as specified, and a method of controlling harmful insects and representatives of the order Acarina using this composition.

Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.

Abstract: New compounds of formula I are described: 1

Abstract: This invention is novel indanone compositions useful for inhibiting cell proliferation disorders in mammals.

Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.

Abstract: This invention is a method for inhibiting cell proliferation using indanones.

Abstract: The invention relates to the use of substituted cyclopentane-diones and cyclopentane-triones for the preparation of medicaments which as chloride channel blockers are suitable for controlling airway diseases, secretory diarrhea and inflammatory diseases.

Abstract: The invention provides a composition for the treatment for the hair, scalp and skin to improve condition and to assist in hair regrowth which comprises a pharmaceutically acceptable oxalate of a group Ia or Ia or ammonium oxalate metal disposed in a pharmaceutically acceptable carrier of diluent therefor. Preferably, the group IIa metal is calcium and the pharmaceutically acceptable carrier or diluent is an ointment.

Abstract: This invention provides methods of treating a physiological disorder associated with an excess of tachykinins in a mammal which comprises administering to a mammal in need of said treatment a compound selected from a series of substituted dihydronaphthalenes and naphthalenes.

Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.

Abstract: Substituted imidazoles such as 2-butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-5-(hydroxy methyl)imidazole and 2-butyl-4-chloro-1-[(2'-carboxybiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imi dazole and pharmaceutically acceptable salts thereof are useful for treating central nervous system disorders, such as cognitive and learning disorders, mediated by angiotensin II.

Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.

Abstract: A method of controlling a pest which comprises bringing into contact with the pest a pest-controlling amount of an agent selected from the group consisting of(1) a non-formamidine -p-octopamine agonist having substantial activity toward an octopamine receptor present in the pest;(2) a compound directly and substantially stimulating the enzyme, adenylate cyclase; and(3) a cyclic adenosine monophosphate (cAMP) analogue.

Abstract: The invention is dealing with arylindane-1,3-diones of the formula: ##STR1## which can be used in the treatment of inflammatories, psoriasis and asthma.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.