Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.

Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.

Abstract: Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.

Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof

Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: An insecticidal and miticidal composition comprising as active ingredients 4-bromo-2-(4-chloro-phenyl)-1-(ethoxymethyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile and a pyrethroid insecticidal ingredient(s). This insecticidal and miticidal composition is effective against pests and mites which are resistant against the insecticidal and miticidal agents on the market.

Abstract: The present invention relates to compounds of general formula (I), 1

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) useful for oral testosterone replacement therapy. Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds bind reversibly to the androgen receptor.

Abstract: Agents which inhibit PDH kinase such as dichloroacetic acid, its salts and derivatives are described as being useful in the treatment of ischaemia in limbs. In particular, dichloroacetic acid and its salts are useful in treating intermittent claudification.

Abstract: The present invention relates to the use of individual fumaric acid derivatives or mixtures thereof for preparing a pharmaceutical composition for treating mitochondrial diseases, especially for treating Parkinson's syndrome, Alzheimer's disease, Chorea Huntington disease, retinopathia pigmentosa and mitochondrial encephalomyopathy. Preferably, the fumaric acid derivative(s) is/are those selected from the group consisting of fumaric acid dialkyl esters or fumaric acid monoalkyl esters in the form of the free acid or a salt thereof.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: The presently disclosed invention relates to compounds of general formula I: 1

Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating disease

Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.

Abstract: A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site.

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.

Abstract: The following products:

Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula 1

Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives.

Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of cystic fibrosis.

Abstract: Fungicidal compounds of formula (I): wherein W is CH3O.

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

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

Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Abstract: A fungicidal mixture comprises a) a phenyl benzyl ether derivative of the formula I.a, I.b or I.c,  and/or a carbamate of the formula Id where X is CH or N, n is 0, 1 or 2 and R is halogen, Cl-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a salt or adduct thereof, and b) a N-acetonylbenzamide of the formula II  where: R1 and R3 independently of one another are each halogen or C1-C4-alkyl; R2 is cyano, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl or C1-C4-alkoxy; R4 is hydrogen or C1-C4-alkyl; R5 is C2-C4-alkyl; R6 is thiocyano, isothiocyano or halogen, or a salt or adduct thereof, in a synergistically effective amount.

Abstract: The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I 1

Abstract: Disclosed and claimed is a method for treating tumors using sulfonylamino-substituted N-aryl- or heteroarylcarboxamide derivatives.

Abstract: The compound of formula 1 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: The present invention discloses novel naphthylsalicylanilides of the general formula wherein W is a substituted or unsubstituted naphthyl ring. The substitution on W includes replacing one or more —H with —OH, alkyl, O-alkyl, branched alkyl, or cycloalkyl, containing 1-6 carbon atoms or combinations thereof. Y is a substituted or unsubstituted phenyl ring or substituted or unsubstituted naphthyl ring. The substitution for Y includes replacement of one or more —H atoms with CN, CF3, NO2, methoxy, benzoyl, phenoxy, phenoxymethyl or combinations thereof. These compounds are useful as antibacterial against gram negative and gram positive bacteria and as antiinflammatory agents.

Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.

Abstract: The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A—B is selected from NHCO, OCH2, SCH2, NHCH2, trans-vinylene, and ethynylene; R1 is linked to ring C at a carbon ortho to the position of A—B attachment and is defined herein; n is 1 or 2; R2 and R3 are alkyl, haloalkyl or together from cycloalkyl or halocycloalkyl as defined herein; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Salts and esters of compounds of formula (I) are also described.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved

Abstract: The invention concerns aryloxypropanolamnine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive. These derivatives comply with the general formula (I) in which R2 represents one of the following groups: —CH2—, —CH2—CH2, —CH(CH3)—CH2—C(CH3)—CH—, —C(CH3)2—CH2— or a bond; Q represents: (i) a phenyl radical 3,4-substituted alkylene dioxy determining with the phenyl radical, a non-substituted benaodioxane unit, a non-substituted benzodioxol unit, or a 2-substituted benzodioxol unit, (ii) a phenyl radical 3 and/or 4-substituted, by a O—(CH2)x—COOR5 group, (iii) a condensed polycyclic hydrocarbon comprising at least two condensed cycles, (iv) a cyclic hydrocarbon system, optionally cross-linked, and constituting a cycloalkane comprising 1, 2 or 3 cycles.

Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.

Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.

Abstract: This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, atherosclerosis, psoriasis, autoimmune disease such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.

Abstract: A fungicidal mixture comprises a.1) a carbamate of the formula I.a, in which X is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a.2) the oxime ether carboxamide of the formula I.b  and b.1) 4-[2-methyl-3-(4-tert-butylphenyl)propyl]-2,6-dimethylmorpholine  or b.2) 4-(C10-C13-alkyl)-2,6-dimethylmorpholine  or b.3) (RS)-1-[3-(4-tert-butylphenyl)-2-methylpropyl]piperidine  and c) a further active ingredient from the class of the strobilurin fungicides (III), in a synergistically effective amount.

Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.

Abstract: A fungicidal mixture comprises a) a phenyl benzyl ether derivative of the formula I.a, I.b or I.c,  and/or a carbamate of the formula Id where X is CH or N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different if n is 2, or a salt or adduct thereof, and (b) a N-acetonylbenzamide of the formula II  where: R1 and R3 independently of one another are each halogen or C1-C4-alkyl; R2 is cyano, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl or C1-C4-alkoxy; R4 is hydrogen or C1-C4-alkyl; R5 is C2-C4-alkyl; R6 is thiocyano, isothiocyano or halogen, or a salt or adduct thereof, in a synergistically effective amount.

Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The invention employs GLP-1(7-37), GLP-1(7-36)amide, and certain related compounds in combination with an oral hypoglycaemic agent for treating diabetes mellitus.

Abstract: Phenylacetic acid derivatives of the formula I