Abstract: A regime or regimen for loosening/slackening and/or relaxing cutaneous and/or subcutaneous human skin tissue, advantageously for cosmetically/therapeutically treating skin wrinkles and fine lines, comprises administering to a candidate subject in need of such treatment, a thus-effective amount of at least one inhibitor of at least one calcium channel.

Abstract: A diseased state based on acute or chronic obstruction of vessels and/or bronchi, acute or chronic inflammation and/or edema formation is advantageously treated by the combined administration of a PDE inhibitor with either an adenylate cyclase agonist or a guanylate cyclase agonist to a subject in need of such therapy. Administration can be either concurrent or in either order.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: 1

Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases.

Abstract: Compositions for controlling harmful fungi, containing in a solid or liquid carrier a) at least one p-hydroxyaniline derivative of the formula I b) at least one amide compound of the formula II A—CO—NR8—R9  (II) where the substituents have the meanings indicated in the description; and methods of controlling harmful fungi using compositions of this type are described.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: This invention provides a method of treating an animal with pyrophosphate gout or osteoarthritis comprising administering an effective amount of a calcium antagonist, thereby reducing calcium pyrophosphate crystal deposition in the animal.

Abstract: The present invention relates to new imidic acid derivatives of the formula (I) to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: Disclosed herein are compounds of the formula I wherein A and C are independently H, alkyl of 1-6 carbon atoms, hydroxy, or alkoxy of 1-6 carbon atoms; B is hydroxy or alkoxy of 1-6 carbon atoms; and Y is cyano,  —C(NR1 R2)═C(CN)2; wherein X═O or S, and R1 and R2 are independently  H, benzyl, —CH(CH3)C6H6,  —(CH2)nC6H6, phenyl; —CO2R;  n=2-4; R is lower alkyl of 1-6 carbon atoms which are useful for treating inflammation and immunological diseases.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Y is O, S or NR6; A is independently hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R6 is independently hydrogen or (C1-C4)alkyl; R2 is independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl; R3 is independently hydrogen or (C1-C4)alkyl; R4 and R5 is independently hydrogen, (C1-C4)alkyl, aryl, aralkyl, aryl(C2-C8)alkenyl, aryl(C2-C8)alkynyl, heterocyclic, or heterocyclic(C1-C4)alkyl wherein if one of R4 and R5 is hydrogen or (C1-C4)alkyl than the other of R4 and R5 is other than hydrogen or (C1-C4)alkyl, and its enantiomers and stereoisomers and agronomically acceptable salts.

Abstract: The present invention provides compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of diseases whose treatment benefits from the inhibition of phosphodiesterase (PDE-IV) or Tumor Necrosis Factor (TNF) including asthma, allergic diseases, rheumatoid arthritis, osteoarthritis, septic shock. The compounds provided by this invention have formula (I) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein.

Abstract: The present invention is directed to fungicidal compositions for agricultural and horticultural use, characterized in that the composition comprises a benzamidoxime composed represented by a general formula [I]: ##STR1## wherein R.sup.1 represents alkyl, alkenyl, etc., R.sup.2 represents phenyl, heterocycle, etc., X.sup.1 represents haloalkyl, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 each independently represent hydrogen, halogeno, alkyl, etc., r.sub.1 and r.sub.2 each independently represent hydrogen, halogeno, alkyl, etc., and a so-called acrylate fungicide as the active ingredients. The fungicidal compositions according to the present invention are combination compositions of fungicidal components, which can improve fungicidal activity obtainable with each component in the combination with a less dose in total of each components.

Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or dissorders whose course involves increased connective tissue or cartilage degradation.

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 provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, and to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors.

Abstract: A sulfur-containing amino acid compound having a high inhibitory activity on LTA.sub.4 hydrolase which is represented by the following formula: ##STR1## wherein R.sup.1 represents H, alkyl, optionally substituted phenyl alkyl, alkanoyl or optionally substituted benzoyl; R.sup.2 represents ester, amide or carboxyl; R.sup.3 represents hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylthio, halogen atom, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R.sup.4 represents alkyl; A.sup.1 represents alkylene; and A.sup.2 represents alkylene.

Abstract: This invention relates to componds of formula I ##STR1## which are useful as PDE IV inhibitors and for treating diseases related thereto.

Abstract: Disclosed are nitrosated and nitrosylated .alpha.-adrenergic receptor antagonists, compositions of an .alpha.-adrenergic receptor antagonist (.alpha.-antagonist), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.cndot.); and uses for each of them in treating human impotence or erectile dysfunction.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.

Abstract: Pharmaceutical compositions containing non-racemic mixtures of verapamil are described, as well as a process of making pharmaceutical compositions containing unequal amounts of R- and S-verapamil.A process for customizing a pharmaceutical composition containing R-verapamil and S-verapamil to optimize a selected pharmaceutical activity comprises selecting a pharmaceutical activity possessed by R-verapamil or S-verapamil, alone or in combination, and then determining a target plasma level for R-verapamil and S-verapamil to achieve that activity is also described. A dosage form for administering the drug is selected. Based on dosage form, one determines the relative amounts of R- and S-verapamil to incorporate into the dosage form to achieve the targeted plasma levels. The dosage form can then be formulated.

Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in the specification, and pharmaceutically tolerated salts thereof.

Abstract: A method for preventing settlement of aquatic fouling organisms on surface of an aquatic structure without environmental hazard is provided. The method is based upon absolutely novel concept to prevent the settlement by means of thick slime layer, i.e. bio-jelly, deposited on said surface. The present invention also provides a bio-jelly producing agent and a bio-jelly producing paint both useful for the present method. Further, the present invention provides a novel low toxic antifouling agent.

Abstract: A compound of the formula I ##STR1## wherein A and C are independently H, alkyl of 1-6 carbon atoms, hydroxy, or alkoxy of 1-6 carbon atoms;B is hydroxy or alkoxy of 1-6 carbon atoms; andY is cyano, ##STR2##--C(NR.sub.1 R.sub.2).dbd.C(CN).sub.2 ;wherein X=O or S, and R.sub.1 and R.sub.2 are independently H, benzyl, --CH(CH.sub.3), C.sub.6 H.sub.5--(CH.sub.2).sub.n C.sub.6 H.sub.6, phenyl; --CO.sub.2 R;n=2-4; R is lower alkyl of 1-6 carbon atomsis used for treating inflammation and immunological diseases.

Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity, the compounds having the formula A described herein.

Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.

Abstract: Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof. ##STR1## R.sup.1 to R.sup.5 : a hydrogen atom, --OR.sup.9 (R.sup.9 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.), etc.,R.sup.6 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.,R.sup.7 : a hydrogen atom, a cyano group, a C.sub.1 -C.sub.5 alkyl group, --SO.sub.q R.sup.15 (q: 0, 1, 2, R.sup.15 : a thienyl group, a phenyl group, etc.) etc.,R.sup.8 : a cyano group, --CR.sup.22 R.sup.23 X (R.sup.22, R.sup.23 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc., X: --NR.sup.24 R.sup.25 (R.sup.24, R.sup.25 : a C.sub.1 -C.sub.5 alkyl group, etc., an alkylene group by combining, etc.)), etc.The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.

Abstract: N-Phenyl-2-cyano-3-hydroxycrotonamide derivatives and their use as pharmaceuticals having an immunomodulatory property.The use of N-phenyl-2-cyano-3-hydroxycrotonamide derivatives of the formula I ##STR1## in which R.sup.1 is a hydrogen atom or (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is CN, CX.sub.3, WCX.sub.3, W(CH.sub.2).sub.n CX.sub.3, NO.sub.2, (CH.sub.2).sub.n CX.sub.3, or halogen, in which X is halogen, W is an oxygen or sulfur atom and n is an integer from 1 to 3, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, CN or --CO--R.sup.4, in which R.sup.4 is (C.sub.1 -C.sub.4)-alkyl or (C.sub.3 -C.sub.6)-cycloalkyl, and/or their physiologically tolerable salts, for the treatment of rheumatic diseases, autoimmune diseases, and of rejection reactions of the organ recipient to the transplanted organ, is described.

Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.

Abstract: A stilbene derivative of the following general formula (I) or a pharmaceutically acceptable acid addition salt thereof have low toxicity, but are water soluble and effective as carcinostatics: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent an alkyl group having 1 to 3 carbon atoms; X represents a hydrogen atom or a nitrile group; Y represents an alkyloxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 6 carbon atoms or a halogen atom.

Abstract: A class of .omega.-amino-.alpha.-phenylalkanonitrile derivatives is described having use in treatment of cardiovascular dysfunctions such as hypertension. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is methoxy, R.sub.3 is hydrido, R.sub.4 is isopropyl, R.sub.5 is methyl and R.sub.6 is selected from linear alkyl, phenylpropyl, phenylbutyl and phenylpentyl.

Abstract: Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production: these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.

Abstract: The present invention provides compounds of the formula ##STR1## wherein Y is a naphthyl, tetrahydronaphthyl, pyridyl, quinolyl, isoquinolyl or indolyl ring system, R is a moiety which is an acrylic acid, a CN-substituted acrylic acid, acrylamide, acrylonitrile or thioacrylamide, or a group of formulae (e) to (j): ##STR2## wherein R.sub.3 is OH or NH.sub.2, R.sub.1 is H, alkyl or alkanoyl, R.sub.2 is H, halogen, CN or alkyl; and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts thereof are useful as tyrosine kinase inhibitors.

Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.

Abstract: Novel cyclohexane-ylidene derivatives of formula (I) are described. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.

Abstract: The invention relates to an insecticidal composition which comprises at least one pyrethroid, at least one UV absorbing agent and at least one antioxidant from the group consisting of tocopherol derivatives and citric acid esters. This insecticidal composition can in particular be used as an emulsion or on a powdery carrier for the control of flying and crawling insects such as flies and cockroaches.

Abstract: The invention is directed to improved methods for modulating the human sexual response by administering a vasodilator to the circulation by a route of administration that avoids the "first-pass" effect.

Abstract: Mammalian hair growth is reduced by applying to the skin a composition including an inhibitor of protein kinase C.

Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.

Abstract: A stilbene derivative of the following general formula (I) or a pharmaceutically acceptable acid addition salt thereof have low toxicity, but are water soluble and effective as carcinostatics: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent an alkyl group having 1 to 3 carbon atoms; X represents a hydrogen atom or a nitrile group; Y represents an alkyloxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 6 carbon atoms or a halogen atom.

Abstract: A stable active substance emulsion of the oil-in-water type with a phospholipid as emulsifier is described, where the active substance dissolved in the lipid phase has one or more basic groups, is hydrophobic and oil-soluble, and has a pKa of at least 7.5, the aqueous phase is set at an acid pH, and the disperse phase gives a positive zeta potential of at least +15, but preferably +30, mV after dilution of the emulsion ready for administration to a fat content of 0.08% by weight.

Abstract: This invention relates to the novel compounds and pharmaceutical compositions of Formulas (I) and (II).This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I) or (II).

Abstract: The invention relates to diketontrile derivatives which have been discovered useful against arthropods, plant nematodes, helminth protozoan pests or as intermediates for such useful compounds which have a general formula: ##STR1##