Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 represent a hydrogen atom or an optionally substituted alkyl group, or R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or alkyl-substituted nitrogen atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.

Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.

Abstract: 3,6-Dimethyl-2(3H)-benzofuranone is a new, valuable flavor material. A process for its industrial-scale preparation was developed.

Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.

Abstract: The present invention relates to novel substituted bicyclic lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, cranial cerebral trauma, states of pain or CNS-mediated spasms.

Abstract: There is provided an agent for reducing body fat, comprising as an active ingredient a dioxabicyclo[3.3.0]octane derivative represented by formula (I): wherein R1 to R6 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, provided that R1 and R2 and/or R4 and R5 combine together to form a methylene or ethylene group; and n, m, and l are each 0 or 1.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: This invention provides a series of substituted propanamines useful as tachykinin receptor antagonists. This invention also provides methods employing these substituted propanamines as well as pharmaceutical formulations comprising these compounds.

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

Abstract: This invention describes the use of the compounds of general formula I in which A, B, A, Ar, R1, R2 and R3 have the meaning that is indicated in more detail in the description, for the production of pharmaceutical agents with anti-inflammatory action. The compounds of general formula I show a clear dissociation between anti-inflammatory and metabolic action.

Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.

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: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

Abstract: A method for potentiating an organic nitrate having vasodilating activity by administering to a subject an effective amount of the organic nitrate with a potentiating amount of a thromboxane receptor antagonist and a reducing agent. Formulations and synergistic compositions are also described.

Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.

Abstract: Methods for treating diseases associated with toxicity of Apolipoprotein E (“apoE”). Specifically, the present invention relates to new methods for treating a mammal having a condition associated with toxicity of apolipoprotein E cleavage fragments containing residues 130-169, comprising administering to said mammal a pharmacologically effective amount of compound or a pharmaceutically acceptable sale, derivative or fragment thereof to interfere with the receptor-binding site associated with residues 130-169 of the apolipoprotein E molecule in said mammal.

Abstract: The invention relates to a method for treating pruritus by administering a therapeutically effective amount of a PAF antagonist to a mammal afflicted with pruritus. The PAF antagonists may, for example, be selected from synthetic PAF analogues, natural products isolated from plants having PAF antagonist activity, and triazolobenzodiazepines. The PAF antagonists are preferably applied topically to the afflicted site but systemic such as oral, parenteral, nasal and intrarectal administration, is also possible.

Abstract: Cyclic amino acid derivatives of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

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: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.

Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

Abstract: The present invention relates to the use of cembranoids to inhibit nicotinic acetylcholine receptors.

Abstract: Compounds of the formula wherein R,R′, A,B,T and x have the meaning given in the specification possess uPA (urokinase-type plasminogen activator) antagonist activity and can be employed as antitumor and/or antimetastatic agents.

Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is —H or —OR7a in which R7a is —H or a hydroxy protecting group; R2a is —H, halo, or —OR8a in which R8a is —H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is —O— or —S—; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.

Abstract: A method of treatment, in an organism, of a vascular condition, comprising administration of at least one agent at a level which enhances NO and which does not appreciably alter normal systemic vascular tone in said organism. At least one agent is an NO donor selected from the group consisting of glyceryl trinitrate, isosorbide 5-mononitrate, isosorbide dinitrate, pentaerythritol tetranitrate, erythrityl tetranitrate, sodium nitroprusside, 3-morpholinosydnonimine molsidomine, S-nitroso-N-acetylpenicillamine, S-nitrosoglutathione, and N-hydroxy-L-arginine.

Abstract: Disclosed are compounds which inhibit .beta.-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 .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.

Abstract: Compound of formula (I): ##STR1## wherein: B represents optionally substituted (C.sub.1 -C.sub.6)-alkylene,W represents oxygen or sulphur,R represents hydrogen, hydroxy, R', or OR', R' being as defined in the description,G.sub.1 and G.sub.11 are as defined in the description,G.sub.2 represents a group selected from: ##STR2## wherein R.sub.20, R.sub.21, and R.sub.2 are as defined in the description, and medicinal products containing the same which are useful as melatoninergic ligands.

Abstract: The present invention provides new benzofuranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases.The present invention is a new benzofuranone derivative represented by a particular general formula (I). ##STR1## In the production, a particular benzofuranone compound and a particular benzaldehyde are reacted.

Abstract: This invention relates to novel compositions containing temporary visual indicators and methods for using these compositions. Specifically, this invention relates to a sunscreen composition containing an indicator that is visible when the substance is applied to the skin, but becomes invisible shortly after application. The continued presence of the indicator allows the indicator to be reactivated temporarily to the visible form so that a user can verify the presence of the sunscreen. The visible indicator ensures that the sunscreen is applied evenly and completely to the area to be protected, but becomes invisible so as not to interfere with the action of the sunscreen or discolor the skin.

Abstract: A method of decreasing atherosclerosis and its complications, such as myocardial infarction, stroke and peripheral vascular disease, wherein the method involves administering to a human or an animal an amount of goserelin acetate sufficient to decrease atherosclerosis and its complications.

Abstract: This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Abstract: A method of anesthetizing a tooth requiring tooth preparation, caries removal or manual manipulation thereof is disclosed. The method includes the steps of applying a composition having a high concentration of potassium to the tooth requiring tooth preparation, caries removal or manual manipulation, the composition being adapted to anesthetize the tooth so that the tooth may be drilled or manually manipulated, whereby the potassium enters the dentinal tubules and odontoblastic fibrils and penetrates the pulpal tissues of the tooth for anesthetizing the tooth. The improvement consists essentially of applying a solution of EDTA, EGTA, and citric acid to the tooth before the application of the potassium composition, the solution of EDTA, EGTA, and citric acid effectively removing a smear layer from the tooth so as to facilitate the penetration of the potassium solution through the dentinal tubules and odontoblastic fibrils.

Abstract: Compounds of formula I are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors (namely of type IV). They and pharmaceutical compositions in which they are active ingredients are useful as bronchial therapeutics, for elimination of erectile dysfunction and for treatment of disorders, particularly those of inflammatory nature. The compounds are distinguished by low toxicity, good enteral absorption (high bioavailability), a great therapeutic breadth and the absence of significant side effects.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: This invention relates to a composition for controlling house dust mites. The composition comprises neem seed kernel extract containing azadirachtin, an alcoholic extract of plant resins, plant polyphenols or phenolic compound, fungistat used in food industry and a dispersion medium. The invention further includes a process of preparing the same by dispersing the above ingredients in a dispersion medium.

Abstract: Substantially pure preparations of phosphosesquiterpenes are described. The compounds inhibit farnesyl-protein transferase activity and are useful for the treatment of cancer. Methods for inhibiting farnesyl-protein transferase activity are also described.

Abstract: Compounds of the formula ##STR1## which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.

Abstract: Methods and pharmaceutical compositions for inactivating an envelope virus using an oil-in-water emulsion including an oil, a surfactant, and an organic phosphate-based solvent are disclosed. These methods can be used to inactivate a wide variety of envelope viruses, such as HIV.

Abstract: The present invention provides an antifeedant and a contact insecticide using the components contained in Cyperaceae species. In particular, the present invention provides an insect antifeedant and a contact insecticide comprising as an active ingredient at least one compound selected from the group consisting of scabequinone, remirol, cyperaquinone and the derivatives thereof.

Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.

Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring that is furan;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--;X is O or S;n is 2;m is 0 or 1;p is 0, 1, or 2;R, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are herein defined;or an agronomic salt thereof.

Abstract: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.

Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.

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.