Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-&agr;v&bgr;3 are inhibited by an inhibitor compound of formula (I): wherein G1 and G2 are each independently NH—C(O)—O—R1, —NH—C(O)—O—(CH2)v—(C6H4)—X3, —NH—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—O—(CH2)v—(C6H4)—X3,or NH—C(O)—CH2—(C6H4)—X3; Y1 and Y2 are each independently OH, C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl, benzyl, or NH2; R1 is C1-C4 alkyl; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is halo, nitro, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is —C≡C—, —C6H4—, cis-CH═CH—, trans CH═CH—, cis-CH2—CH═CH—CH2—, trans —CH2—CH═CH—CH2—, 1, 4-naphthyl, cis-1,3-cyclohexyl, trans-1,

Abstract: Dithiocarbamate, particularly tetraethylthiuram disulfide, and thiocarbamate anions strongly inhibit the growth of cancer cells of a variety of cell types. Such inhibitory effect is enhanced by heavy metal ions such as copper ions, cytokines and ceruloplasmin. A method is presented for using tetraethylthiuram disulfide to reduce tumor growth, and to potentiate the effect of other anticancer agents.

Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention provides conjugates of fatty amines and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparations of the fatty amine-pharmaceutical agent conjugates are provided.

Abstract: Disclosed are methods of treating acute and chronic inflammation in the lung caused by inhalation of smoke, endometriosis, Behcet's disease, uveitis, ankylosing spondylitis, pancreatitis, cancer, Lyme disease, sepsis, chronic obstructive pulmonary disease, traumatic arthritis, congestive heart failure and restenosis following percutaneous transluminal coronary angioplasty, known to be cytokine mediated, using aromatic heterocyclic compounds described in WO 00/55139.

Abstract: An inoculant tolerant, aqueous fungicidal composition, is provided which is substantially free of organic solvents, comprising a fungicidally effective amount of at least one fungicidally active compound; a stabilizing effective and nitrogen-fixing bacteria tolerant amount of a preservative; and at least one anionic surfactant. The composition is tolerant to nitrogen-fixing bacteria such as Rhizobium spp. when applied concurrently or sequentially to plant propagation materials such as seeds; the inventive compositions are storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and have good fungicidal efficacy.

Abstract: The invention relates to agents which combat the hepatitus A virus, containing only minimal amounts of chlorine-containing and/or chlorine cleaving active ingredients, or none of said substances. The inventions also relates to the use of these agents and to a method for their production.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: An insect pest eradication system comprised of a non-lethal knockout agent and an insecticide. The present invention also relates to a method of eradicating insects, particularly those found in earthen colonies, by treating the insects with a non-lethal knockout agent, such as trans-dichloroethylene, in combination with a suitable insecticide for the targeted insects.

Abstract: The present invention provides a fungicidal composition characterized by containing as active ingredients

Abstract: The present invention is in particular related to the use of rivastigmine in the manufacture of a medicament for the treatment of ocular disorders.

Abstract: The present invention relates to free-radically polymerizable, siloxane-containing urethane (meth)acrylates which comprise, in incorporated form, a) at least one compound which contains at least one active hydrogen atom and at least one free-radically polymerizable &agr;,&bgr;-ethylenically unsaturated double bond per molecule, b) at least one diisocyanate, c) at least one compound which contains two active hydrogen atoms per molecules, d) at least one compound which contains at least one active hydrogen atom and at least one siloxane group per molecule, to water-soluble or water-dispersible polymers which comprise these urethane (meth)acrylates in copolymerized form, to the use of these polymers, and to cosmetic compositions which comprise these polymers.

Abstract: The present invention relates to discodermolidate acid salts of formula I 1

Abstract: An aqueous dispersion comprising a halopropargyl compound (HPC) and a partially hydrolysed polyvinyl alcohol (PHPVA). The aqueous dispersions are useful for inhibiting the growth of micro-organisms on or in a medium, especially an industrial medium such as paint films, metal working fluids, wood, latices and plastic materials.

Abstract: Medical devices, compositions and methods for treating or preventing atherosclerotic plaque rupture are disclosed. Specifically, medical devices that deliver to a treatment site metalloproteinase inhibitors (MMPI) are disclosed. The medical devices include catheters, guide wires, vascular stents, micro-particles, electronic leads, probes, sensors, drug depots, transdermal patches, and vascular patches. Representative MMPIs included zinc chelators, urea derivatives, caprolactone-based inhibitors, phoshoinamides, piperazines, sulfonamides, tertiary amines, carbamate derivatives, mercaptoalcohols, mecaptoketones, antimicrobial tertracyclines, non-antimicrobial tetracyclines, and derivatives and combinations thereof. In one embodiment a self-expanding vascular stent is coated with at least one MMPI and deployed at a site within an artery where vulnerable plaque has been identified.

Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: New active compound combinations of valinamide derivatives of the formula (I) in which R1 and R2 has the meaning given in the description, with known fungicidal active substances, and their use for combating phytopathogenic fungi are described.

Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I: where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: The present invention provides a method of treating a disease or a disorder responsive to inhibition of nuclear factor-&kgr;B transcription factors comprising administering to a patient in need thereof a sulfonylaminocarbonyl derivative, or a pharmaceutically acceptable salt thereof. The methods of the present invention are useful for treating, for example, rheumatoid arthritis, osteoarthritis, an autoimmune disease, psoriasis, asthma, a cardiovascular disease, an acute coronary syndrome, congestive heart failure, Alzheimer's disease, multiple sclerosis, cancer, type 2 diabetes, metabolic syndrome X, or inflammatory bowel disease.

Abstract: Compositions and methods for chemotherapy are disclosed. The compositions and methods disclose herein are effective inhibitors of chemotherapy-induced nephrotoxicity, yet unexpectedly do not inhibit the antineoplastic activity of the chemotherapeutic compound. The chemotherapeutic compositions and methods of the invention comprise an inhibitor of catalytic iron. In a preferred embodiment, the inhibitor is a cytochrome P450 inhibitor and the chemotherapeutic compound is cisplatin.

Abstract: The present invention provides methods comprising one or more zinc ionophores for treating or reversing the effects of stress, including surgical stress in patients in need thereof.

Abstract: Compounds of formula (I) wherein R1 is C1-C4-alkyl or cyclopropyl; R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl; or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl, CN, or aryl, heteroaryl, heterocyclyl, aryloxy, heteroaryloxy or heterocyclyloxy, whereby the above-mentioned groups may be substituted by identical of different substituents, R5 signifies hydrogen or methyl; R6 and R7 are C1-C4-alkyl; have microbicidal, insecticidal and acaricidal activity and may be used for the control of pests and plant-pathogenic fungi in agriculture, horticulture and in the field of hygiene.

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 present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: This invention is directed to stabilized antimicrobial compositions comprising an iodopropynyl compound, and a benzylidene camphor.

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

Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1

Abstract: The invention relates to novel active substance combinations of valinamide derivatives of formula (I), wherein R1 and R2 have the meaning cited in the description, and fenamidone. The invention also relates to the use of novel active substance combinations to combat phytopathogenic fungi.

Abstract: A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1 represents a C3-C8 cycloalkyl group, an optionally substituted C6-C14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C6-C14 aryloxy group, or an optionally substituted C7-C15 arylmethyl group; R2 and R3 independently represent hydrogen atom or a C1-C5 alkyl group, or R2 and R3 may combine to represent a C2-C7 alkylene group; or X represents R7—A— wherein R7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or —N—R8 where R8 represents hydrogen atom or a C1-C5 alkyl group, Y represents an oxygen atom or a sulfur atom, R4 and R

Abstract: Methods and compositions for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The compositions contain a mast cell stabilizing disulfide derivative as an active ingredient.

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III  in which R13 is C3-C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1-C4-alkyl or C1-C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.

Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.

Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: A composition includes synergistic amounts of: (a) a compound formula (I) wherein X represents ═CH— or ═N—; E represents an electron-withdrawing radical; R represents optionally substituted hetarylalkyl; A represents hydrogen, alkyl, or a bifunctional group which is linked to the radical Z; Z represents alkyl, —NH-alkyl, —N(alkyl)2 or a bifunctional group which is linked to the radical A, and (b) a fungicidal active compound, excluding cyclopropylcarboxamide derivatives and azolylmethylcycloalkanes. The combination of imidacloprid and a fungicidal active compound selected from the group consisting of tebuconazole and compounds of the formula is excluded.

Abstract: A wood treatment material having a synergistic combination of fungicides including boron-containing compounds, organo-iodine compounds and amine-oxides is provided. This combination is shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with this combination. Also provided is wood treated by this combination, and a method of treatment for composite wood.

Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.

Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a &bgr;-blocker are provided, wherein the &bgr;-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca2+ activated potassium channel (IKCa), and the use of such compounds for the treatment or alleviation of diseases or conditions relating to immune dysfunction.

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: 1) Fungicidal compositions comprising a compound (I) which is (4S)-4-methyl-2-methylthio-4-phenyl-1-phenylamino-2-imidazolin-5-one and a compound (II) chosen from the group comprising: (IIA) propamocarb; (IIB) the S-methyl ester of 1,2,3-benzo-thiadiazole-7-carbothioic acid, of formula: (IIC) cyprodinil; (IID) 2-hydroxybenzoic acid or salicylic acid, its esters and its salts, in particular the alkali-metal salts and the alkaline-earth metal salts; the compound (IIF) or 8-t-butyl-2-(N-ethyl -N-n-propylamino)methyl-1,4-dioxaspiro [4.5]decane, also known as spiroxamine; the compound (IIG) or isopropyl ester of [2-methyl-1-(1-p-tolylethylcarbomyl)propyl] acid, also known as fencaramide; the compound (IIH) or 4-chloro-2-cyano-1-dimethylsulphamoyl-5-(4-methylphenyl)imidazole; the compound (I)/compound (II) ratio being between 0.01 and 50, preferably between 0.01 and 10.

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides a composition comprising an amine oxide and an iodine containing biocide. Another embodiment of the present invention is a method for preserving and/or waterproofing a wood substrate by contacting the composition with the wood substrate.

Abstract: A preparation is disclosed for producing enhanced blood flow in tissue thus causing beneficial effects such as promoting hair growth on scalp tissuelacking sufficient hair, restoring normal sexual function in males with erectile dysfunction. Specifically, this is a preparation which provides local delivery of the amino acid L-arginine, an important biological precursor to the main substance which is responsible for relaxation of blood vessels permitting enhancement of blood flow. In the preferred embodiments, the L-arginine is provided so that it can be topically applied to the scalp or penis. The preparation also contains an agent which aids in the transfer of L-arginine into the tissue. In the preferred embodiments this agent overcomes the resistance to transfer caused by the high charge density of L-arginine. In the preferred embodiments this means is high ionic strength created by addition of choline chloride, magnesium chloride and sodium chloride.

Abstract: A fungicidal mixture comprises a.1)a phenyl benzyl ether derivative of the formula I.a, I.b or I.c, or a.2) a carbamate of the formula I.d, where X is CH and N, n is 0, 1 or 2 and R is halogen, C1-C4-alkyl and 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 fungicidally active compound from the class of the benzimidazoles or benzimidazole-releasing precursors (II), in a synergistically effective amount.

Abstract: This invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr [4-bromo-2-(chlorophenyl)-1-(ethoxymethyl)-5-(trifluoromethyl)pyrrole-3-carbonitrile] in combination with asynergistic amount of at least one of a carbamate-type insecticidal compound.

Abstract: Synergistic fungicidal composition comprising propamocarb and a derivative of phosphorous acid; and process for the curative or preventative control of phytopathogenic fungi by use of such a composition.