Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: A method for treating a disease associated with the estrogen receptor-&bgr;, comprising the step of administering a therapeutically-effective amount of a compound that satisfies the equation: (Ki&agr;A/Ki&bgr;A)/(Ki&agr;E/Ki&bgr;E)>1, optionally having the general structure (I).

Abstract: This invention provides methods of using Protein-tyrosine phosphatase (PTPase) inhibitors for lowering the cardiovascular risk profile in mammals experiencing or subject to type II diabetes or Syndrome X, including lowering levels of blood lipoproteins, free fatty acids and triglycerides, as well as treating, preventing or inhibiting atherosclerosis and other cardiovascular and cerebebrovascular disorders.

Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: This invention provides methods of using a pharmacological combination of a biguanide agents, such as metformin, and one or more PTPase inhibiting agents and, optionally, one or more sulfonlylurea agents, including glyburide, glyburide, glipizide, glimepiride, chlorpropamide, tolbutamide, or tolazamide, for treatment in a mammal of Syndrome X, type II diabetes or metabolic disorders mediated by insulin resistance or hyperglycemia. Further included in this invention is a method of modulating blood glucose levels in a mammal utilizing the combination of one or more PTPase inhibiting agents and one or more sulfonlylurea agents.

Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These compounds are disclosed as being useful as anti coagulants.

Abstract: The use of compounds of the milbemycin class as inhibitors of efflux pumps in microbes or other cells is described, along with pharmaceutical compositions incorporating a milbemycin. Also described is a method of screening for compounds which inhibit a CDR1, CDR2, BEN, or FLU1 efflux pump or a pump with components having a high level of protein level sequence similarity with the components of those efflux pumps.

Abstract: The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.

Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1˜C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1˜C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.

Abstract: Compounds related to lactacystin and lactacystin lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carbo

Abstract: Novel 3-phenyl-pyrones of the formula in which A, D, X and Y are each as defined in the description, a process for preparing these substances and their use as pesticides, fungicides and herbicides.

Abstract: The invention concerns the use of a compound of the formula (I) in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.

Abstract: The present invention relates to novel substituted &bgr;,&ggr;-fused 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, craniocerebral trauma, states of pain or CNS-mediated spasms.

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: The invention relates to cyclopentabenzofuran derivatives, processes for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-&kgr;B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.

Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.

Abstract: Compounds of formula (I) wherein W is —OH or —NHOH; X is an optionally substituted heterocycle, NR1SO2R2, heterocyclylalkythio, CONR2R3 or NR1COR2; Y, Z, R1-R3 and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.

Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention relates to an Extract of Echinops spinosus L (Asteraceae) and organic solvent soluble fractions of the extract that may be used in the treatment of cancer.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.

Abstract: A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.

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: 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: 2-Phenylpyran-4-one derivatives of formula (I): 1

Abstract: The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: —O— or —S—, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.

Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

Abstract: The present invention concerns novel 7-deoxy taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: The invention relates to a method of simultaneous high-throughput preformulation quantification of potential drug candidates, where an aliquot of a mixture of solutions containing different compounds is injected into a high pressure liquid chromatograph. The concentration of each compound can be determined by high pressure liquid chromatographic analysis, and correlated to a physico-chemical property of the compound.

Abstract: Combinations of diterpenoid triepoxides and anti-proliferative agents are used in a combination therapy to treat hyperproliferative disorders. Anti-proliferative agents of interest include agents active in killing tumor cells, as well as immunosuppressants, and a variety of other agents that reduce cellular proliferation in targeted tissues. Synergistic combinations provide for comparable or improved therapeutic effects, while lowering adverse side effects.

Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The invention concerns novel phenylcyclidine derivatives with selective affinity for low affinity receptors, methods for preparing them, pharmaceutical compositions containing them and their use as protective agents for central or peripheral nervous system cells against acute or chronic degeneration, or as an anticonvulsant.

Abstract: The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix.

Abstract: The present invention provides a protective agent for nervous system structural cells comprising a prostaglandin I derivative, preferably a prostaglandin I2 derivative, particularly beraplost, as an active component. This medicine exhibits excellent effects as a protective agent for nervous system structural cells, and is effective as an excellent agent for preventing or curing cerebrovascular disorder, cerebral nerve cell disorder, ischemic cerebral disorder, dementia, and peripheral nerve disorder due to diabetic or the like.

Abstract: The diarylbenzopyran derivatives represented by formula I, and the pharmaceutically acceptable salts thereof, are disclosed. The composition comprising the compound of formula I, or a pharmaceutically acceptable salt thereof, shows an excellent selective inhibition of cyclooxygenase-2.

Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.

Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to 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 relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Methods are provided for the treatment and prophylaxis of viral infection and disease associated with such infection.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: A composition for intranasal administration comprising a full or partial D1-agonist of the dopamine receptor.

Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.

Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.