Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

Abstract: This invention pertains to a process for the preparation of 2,5-dihydrofurans by the isomerization of &ggr;,&dgr;-epoxyalkenes in the presence of a catalyst system comprising an organotin compound and an alkali metal iodide.

Abstract: Disclosed herein are compounds selective for a 5-HT1D receptor, the compounds having the general formula (I): Also disclosed is the use of these compounds as pharmaceuticals to treat indications where stimulation of a 5-HT1D receptor is indicated such as migrane.

Abstract: Cosmetic/pharmaceutical/dermatological compositions suited for promoting desquamation of the skin of a mammalian organism in need of such treatment and/or to stimulate epidermal renewal and thus to combat intrinsic and/or extrinsic aging thereof, via topically applying same to the skin of such organism, comprise a cutaneous aging-combating effective amount of at least one polyholoside, preferably a heterogeneous polyholoside, in a topically applicable, cosmetically/pharmaceutically/dermatologically acceptable vehicle, carrier or diluent therefor.

Abstract: A method for treating diseases which involve interaction of neurokinin B with NK3 receptors in humans. The method comprises administering a therapeutically effective amount of a NK3 antagonist compound having the formula: in which: R1 and R11 together represent a —(CH2)3-group.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is

Abstract: The present invention is related to methods for treating pathological conditions resulting from an estrogen deficiency, such as cardiovascular disease and osteoporosis, and is further related to methods for treating estrogen-dependent cancer, such as breast and uterine cancer, employing compounds of formula I

Abstract: Nitric oxide scavengers, such as dithiocarbamate-containing compounds, are used to reduce side effects caused by therapeutic administration of nitric oxide sources by administering the nitric oxide scavenger(s) to the subject after the therapeutic effect of the nitric oxide source has been achieved. For example, the nitric oxide source can be coadministered with the nitric oxide scavenger, with the latter formulated in a time release vehicle selected to delay release of the scavenger for a period of time sufficient to ensure that the therapeutic goal of the nitric oxide source has been achieved before release of the scavenger. Formulations and kits, including a bubble pack with pairwise arrangement of unit doses of a desired nitric oxide source and nitric oxide scavenger, are also provided.

Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: 7-Aza-bicyclo[2.2.1]-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.

Abstract: Newly-created fluorenone drugs can be used to prevent, treat, or otherwise reduce damage to a brain or spinal cord following a medical crisis. These new drugs are markedly improved analogs of previously-known fluorenone compounds that were never commercialized or developed into medically useful treatments. The new analogs have the following structure: where X is a lower alkyl, substituted alkyl, or cycloalkyl group, R is selected from certain types of ether, ester, or amide groups, and Y1 and Y2 are halogen, hydrogen, or methyl. These new compounds can penetrate a blood-brain barrier and potently inhibit the unwanted release of excitotoxic neurotransmitters by astrocyte cells following an injury or insult to the brain or spinal cord. As an illustration, some of these new analogs were more than 30 times more potent than the previously known best compound in reducing aspartate release by stressed astrocytes.

Abstract: The invention provides novel mepiquat plant growth regulator compositions which have improved hygroscopicity and corrosion characteristics. The novel mepiquat plant growth regulator compositions of the invention can be readily prepared from technical mepiquat chlorid inter alia by electrochemical ion exchange processes or by quaternization of N-methylpiperidine with dimethylcarbonate as starting material.

Abstract: Compounds of formula (I) wherein R is hydroxy, hydrogen, alkenyl, alkynyl or aryl, and R1 is aryl or heteroaryl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: Nitroxyl compounds represented by general formula (I) which are usable in acquiring information about active oxygen or in vivo free radicals as biological images such as magnetic resonance images or magnetoencephalograms, wherein A represents hydrogen or —L—(CH2)n—OCOR (wherein L represents —COO— or -alkylene-COO—; and R represents C1-4 alkyl); R1, R2, R3, and R4 represent each C1-4 alkyl; and n is a number of from 1 to 4. Drugs and reagents containing the above compounds are usable in preventing, treating or diagnosing ischemic diseases, digestive diseases, cancer, cranial nervous diseases accompanied by nerve degeneration, inflammation, cataracts, or drug-induced organopathy.

Abstract: The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I): which are usefull as Farnesyl-Protein Transferase inhibitors.

Abstract: A non-crystalline silica solid is obtainable by a process comprising the step of contacting in a liquid medium at least one silica precursor with at least one template comprising a polyethyleneimine or a mixture of two or more thereof.

Abstract: The present invention relates to a method for producing 1,1,1,3,3-pentafluoropropane. This method includes the steps of (a) adding hydrogen fluoride to 1-chloro-3,3,3-trifluoropropene in the presence of an addition catalyst to obtain 1,1,1,3-tetrafluoro-3-chloropropane; and (b) disproportionating the 1,1,1,3-tetrafluoro-3-chloropropane into the 1,1,1,3,3-pentafluoropropane and 1,1,1-trifluoro-3,3-dichloropropane, in the presence of a disproportionation catalyst. This method is a useful method for producing 1,1,1,3,3-pentafluoropropane in an industrial scale, because its steps (a) and (b) are respectively superior in selectivity and yield. According to the invention, 1-chloro-3,3,3-trifluoropropene may be produced by a method including a step of reacting 1,1,1,3,3-pentachloropropane with hydrogen fluoride in a gas phase in the presence of a fluorination catalyst. This method is useful, because yield of 1-chloro-3,3,3-trifluoropropene is high.