507 results about "Isoxazole" patented technology

The present invention is concerned with isoxazole-pyridine derivatives of formula Iwherein X, R1 to R6 are as described herein. The compounds are active on the GABA A α5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.

Methods for increasing the level of neurotrophic factors and neurotrophic factor receptors in the brain of a mammal afflicted with a pathology which produces neurodegeneration without significant loss of memory or learning comprising administering to a mammal an effective amount of an allosteric upmodulator of alpha -amino-3-hydroxy-5-methyl-isoxazole-4-proprionic acid (AMPA) receptors.

Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.

This invention relates generally to the detection of genetic differences among soybeans. More particularly, the invention relates to soybean quantitative trait loci (QTL) for tolerance or sensitivity to HPPD-inhibitor herbicides, such as mesotrione and isoxazole herbicides, to soybean plants possessing these QTLs, which map to a novel chromosomal region, and to genetic markers that are indicative of phenotypes associated with tolerance, improved tolerance, susceptibility, or increased susceptibility. Methods and compositions for use of these markers in genotyping of soybean and selection are also disclosed, as are methods and compositions for use of these markers in selection and use of herbicides for weed control. Also disclosed are isolated polynucleotides and polypeptides relating to such tolerance or sensitivity and methods of introgressing such tolerance into a plant by breeding or transgenically or by a combination thereof. Plant cells, plants, and seeds produced are also provided.

Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I or II:wherein the variables are as defined herein.

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

A compound represented by the formula (I) wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group; W is a bond or a divalent aliphatic hydrocarbon group; Y is a group of the formula: —OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.

The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and / or prophylactic treatment of cognitive disorders like Alzheimer's disease.

A nonaqueous electrolyte battery having improved storage stability is disclosed. The battery includes a positive electrode; s negative electrode in which the active material is lithium or a compound capable of absorbing and desorbing lithium; and a nonaqueous electrolyte containing an organic solvent, at least 10 wt % of which is dioxolane, a solute and a storage stabilizing additive which is an oxygen acid ester, isoxazole, oxazole or oxazoline or a derivative thereof. The additive reduces the self-discharge rate of the battery during storage.

A compound of formula (I): (wherein R1-R10 are each independently hydrogen, halogen, optionally substituted lower alkyl or the like, X1 is —O—, —S—, —NR11— (wherein R11 is hydrogen, lower alkyl or the like), —CR12R13CO—, —(CR12R13)mO—, —O(CR12R13)m- (wherein R12 and R13 are each independently hydrogen or lower alkyl and m is a integer between 1 and 3) or the like, X2 is a bond, —O—, —S—, —NR14— (wherein R14 is hydrogen, lower alkyl or the like, R14 and R6 can be taken together with the neighboring atom to form a ring) or —CR15R16— (wherein R15 and R16 are each independently hydrogen or lower alkyl, R15 and R6 or R10 can be taken together with the neighboring carbon atom to form a ring, R16 and R9 can be joined together to form a bond), X3 is COOR17, C(═NR17)NR18OR19 or the like), a pharmaceutically acceptable salt or a solvate thereof.

The present invention provides compounds of Formula I:and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR and methods for their preparation and use.

The invention aims to provide a method for synthesis and preparation of [2-methyl-3- (4,5-dihydro-3-isoxazole)-4-(methyl sulfonyl) phenyl]-(5-hydroxy-1-methyl-1H-parazole-4-based) ketone (topramezone). According to the method, raw materials are simple and easy to obtain, post-processing is simple, the total recovery is high, the defects existing in the prior art and the defects concerning cost are overcome, and an important reference can be provided for industrial production.

An agri-horticultural fungicide containing a substituted isoxazole alkylamine derivative represented by the formula (I) as an active ingredient exhibits no crossreaction with known drug resistant fungi and exerts a sufficient activity for preventing plant disease damages: wherein R1 and R2 each represent a hydrogen atom, a (substituted) alkyl, or the like; X is a single bond, alkylene, or the like; Y1 represents a (substituted) lower alkyl, (substituted) cycloalkyl, (substituted) phenyl, (substituted) heteroaryl, or the like; Y2 represents a (substituted) cycloalkyl, (substituted) phenyl, (substituted) heteroaryl, or the like; and Z represents a (substituted) alkylene, —O-((substituted)alkylene)-, —NR-((substituted)alkylene)- or the like.

Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

The invention provides a compound of formula I:wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

A cyclic tertiary amine compound which is capable of inhibiting the production of inflammatory cytoines. The compound having a structure represented by the following formula (I): wherein A represents an optionally substituted trivalent group which is benzene, pyrimidine, pyrrole, pyridine, pyridazine, furan, thiopene, pyrazole, imidazole, isoxazole or isothiazole; R1 represents an aryl or a heteroaryl group, which is unsubstituted or substituted; R2 represents a heteroaryl group which is unsubtituted or substituted; and R3 represents a cyclic tertiary amino group, or a pharmacologically acceptable salt of the compound.

The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

The invention provides an enzyme-linked immunosorbent kit for inspecting sulfa drugs, comprising an ELISA plate which is coated with coating antigen, an enzyme label, sulfa drug specific antibody working liquid (being contained when the antigen is coated on the ELISA plate and the enzyme label is enzyme labeling antibody or antibody is coated on the ELISA plate and the enzyme label is enzyme labeling antigen), sulfamethoxy-isoxazole standard product solution, substrate color development solution, stop solution, concentrated washing liquid and concentrated complex solution. The invention further discloses a method which applies the enzyme-linked immunosorbent kit for inspecting the sulfa drugs, and the method comprises the steps of firstly carrying out the pre-treatment on a sample, then using the kit for inspecting and finally analyzing the inspection result. The provided enzyme-linked immunosorbent kit can be used for inspecting the residual amount of the sulfa drugs in animal tissues(chicken, pork, fish and shrimp), honey, eggs, milk, feeds and other samples, the operation is simple, the cost is low, the sensitivity is high and the enzyme-linked immunosorbent kit can be monitore d on-site and is applicable in screening mass samples.

Problem: To provide an optical recording medium having a recording layer improved in light stability that is capable of writing and reading of high-density optical information by a short-wavelength laser beam.Means for Solving the Problems: There is provided an optical recording medium with a recoding layer comprising an organic dye compound, wherein the recording layer contains a metal complex compound composed of a pyridone azo compound represented by the following the general formulas [I] to [III] and a divalent ion of metal coordinated to it such as nickel, cobalt, iron, zinc, copper, manganese and the like, wherein the pyridone azo compound contains a 6-hydroxy-2-pyridone structure as a coupling component and isoxazole, 1,2,4-triazole or pyrazole structure as a diazo component.(In the general formulas [I] to [III], R1 to R10 each is independently a hydrogen atom or monovalent functional group.)

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

The present invention relates to famesoid X receptors (FXR, NR1 H4) FXR is a member of the nuclear receptor class of ligand-activated transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease and metabolic syndrome.

Azole compounds represented by formula I:wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.

The invention provides parecoxib sodium which is prepared by controlling an intermediate impurity and in particular provides a preparation method of a parecoxib sodium compound as well as the intermediate impurity and an application of the parecoxib sodium compound. According to the preparation method provided by the invention, 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol is used as an isomer impurity for preparing 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an intermediate of the parecoxib sodium, the quality of the 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol is controlled in the preparation of the parecoxib sodium, specifically, the impurity content is required not to be higher than 0.5 percent, and an important significance is provided for the product quality of the parecoxib sodium; by obtaining the 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an isomer impurity of the important 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol and further studying 3-methyl-4,5-diphenyl-4,5-dihydro-isoxazole-5-alcohol in the aspects of preparation process, detection process and purification process, important quality monitoring significance is provided for the process with the 5-methyl-3,4-diphenyl-4,5-dihydro-isoxazole-5-alcohol as an industrial production raw material.

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR3 and (Ar1)2CR4 is optionally substituted benzhydryl.

Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation.

This invention provides an electrode electrolyte for a solid polymer-type fuel cell, in which a cost problem and a problem related to recovery of catalyst metals are solved, having excellent proton conductivity, dimensional stability and heat resistance.An electrode electrolyte for a solid polymer electrolyte-type fuel cell contains a polymer, which has a polyphenylene structure as a main chain and both a sulfonic acid group and a nitrogen-containing heterocyclic group as a side chain. A side chain having the nitrogen-containing heterocyclic group has a structure represented by the following general formula (D).(In formula, Z represents at least one kind of structures selected from a group consisting of a direct bond, —O— and —S—, Y represents at least one kind of structures selected from a group consisting of —CO—, —SO2—, —SO—, —CONH—, —COO—, —(CF2)1— (1 is an integer of 1 to 10) and —C(CF3)2— and R20 represents a nitrogen-containing heterocyclic group. q represents an integer of 1 to 5 and p represents an integer of 0 to 4.)The above nitrogen-containing heterocyclic group is at least one kind of group derived from a compound selected from the group consisting of nitrogen-containing heterocyclic compounds including pyrrole, thiazole, isothiazole, oxazole, isoxazole, pyridine, imidazole, imidazoline, pyrazole, 1,3,5-triazine, pyrimidine, pyridazine, pyrazine, indole, quinoline, isoquinoline, purine, benzimidazole, benzoxazole, benzothiazole, tetrazole, tetrazine, triazole, carbazole, acridine, quinoxaline and quinazoline and derivatives thereof.