4927 results about "Thiazole" patented technology

Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and / or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

The invention discloses certain N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity:wherein R1, R2, R3, R4, and R5 in the formula (1) each has the same meaning as defined in the specification.

The present invention discloses two crystal models and the preparation method of the anti-hyperuricemia drug 2-(3-ayano-4-isobuoxy phenyl)-4-methyl-5- thiazole acid. The preparation method of the crystal models commonly uses the low-toxicity ethanol, ethyl acetate or acetone as the solvent; the safety is relatively high. In addition, the hygroscopicity of the two crystal models is low in the high-humidity environment and the two crystal models are suitable for the steady pharmaceutical preparation.

The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

The disclosure provides compounds, compositions, and methods for modulating PPARδ receptor. In one embodiment, the compounds of the disclosure comprise a tri-substituted thiazole group. The substituent at the 2-position of the thiazole group provides steric bulk to the compounds. The compounds, compositions, and methods may be useful, for example, in the treatment of cancer.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.

The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero ring-substituted oxime derivative. A tetrazoyloxime derivative represented by the general formula (1): <CHEM> X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a cyano group, a methanesulfonyl group, a nitro group, a trifluoromethyl group, or an aryl group; A represents a 1-alkyltetrazoyl-5-yl group or a 5-alkyltetrazoyl-1-yl group; and Het represents a pyridyl group having a substituent or a thiazoyl group having a substituent, and a plant disease controlling agent containing the same as an active ingredient are disclosed.

PCT No. PCT / US96 / 11613 Sec. 371 Date Sep. 14, 1998 Sec. 102(e) Date Sep. 14, 1998 PCT Filed Jul. 12, 1996 PCT Pub. No. WO97 / 03945 PCT Pub. Date Feb. 6, 1997Compounds of formula (I) wherein: R1 is -(CR4R5)nC(O)O(CR4R5)mR6, -(CR4R5)nC(O)NR4(CR4R5)mR6, (CR4R5)nO(CR4R5)mR6, or -(CR4R5)rR6: W is alkynyl or 2 carbon atoms; R3 is H or R7; Z is C(O)R13, (CH2)0-1C(O)OR13, (CH2)0-1C(O)NR10R13, (CH2)0-1C(R8R8)OR8, -NHC(O)R7, (CH2)0-1NR10R13, NH[C(O)C(O)OR8], CH2NH[C(O)CNR10R13], CH2S(O)qR7, CH[S(O)qR7]2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R7 is -(CR4R5)qR11 or C1-6 alkyl wherein the R11 or C1-6 alkyl group is unsubstituted or substituted one or more times by methyl or ethyl unsubstituted or substituted by 1-3 fluorines, -NR8R10, -CO2R8, -O(CH2qR8, -NR8C(O)R8 or R12; or the pharmaceutically acceptable salts thereof.

The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

A thienotriazolodiazepine compound of the following formula (I)a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound.Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.

The invention relates to processes for preparing compounds having the formula,and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

A coating composition used for coating of a steel material and / or aluminum material comprises a corrosion inhibitor, a base resin and a curing agent. The corrosion inhibitor may be selected from cerium compounds, lanthanum compounds, molybdate salt compounds, gluconic acid derivative salts, porous base materials, triazole compounds, thiazole compounds, tetracyclines, and metal phosphate salt compounds of ascorbic acid. The base resin may include a xylene-formaldehyde-resin-modified amino-containing epoxy resins obtained by reacting an epoxy resin having an epoxy equivalent of from 180 to 2500 with a xylene formaldehyde resin and an amino-containing compound. The curing agent may be a blocked polyisocyanate compound obtained by blocking an isocyanate group of a polyisocyanate compound with a blocking agent.

The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

Thiazolidinedione (TZD) and its pharmacologically active derivatives can be used, in combination with agonists of glucagon-like peptide-1 (GLP-1), to treat non-insulin dependent diabetes mellitus, optionally with other therapies, by improving glycemic control while minimizing side effects, such as heart hypertrophy and elevated fed-state plasma glucose, which are associate with both TZD and GLP-1 monotherapies. Thus, the co-administration of TZD and GLP-1 helps regulate glucose homeostasis in Type II diabetic patients.

The invention belongs to the technical field of pesticide formulation and in particular relates to a composite bactericidal composite and applications thereof in aspect of preventing and curing the fungicidal and bacteria diseases of grains, fruits and vegetables. The composite bactericidal composite comprises effective ingredient A and B, wherein the effective ingredient A is prochloraz or othermetal salt composite, and the effective ingredient B comprises at least one of penconazole, imazalil sulfate, ethirimol, bupirimate, SYP-Z048, thifluzamide, mandipropamid, ethaboxam, polyoxin, polyoxin B, benziothiazolinone, famoxadone, dithianon and zinc thiazole. The composite has high efficiency, low toxicity, low residue, good environment compatibility and low cost.

A polishing slurry including an oxidant, a metal oxide dissolver, a metal inhibitor and water and having a pH from 2 to 5. The metal oxide dissolver contains one or more types selected from one or more acids (A-group) selected from acids of which the dissociation constant (pKa) of a first dissociable acid group is less than 3.7 and from which five acids of lactic acid, phthalic acid, fumaric acid, maleic acid and aminoacetic acid are excluded, ammonium salts of the A-group and esters of the A-group, and one or more types selected from one or more acids (B-group) selected from acids of which the dissociation constant (pKa) of a first dissociable acid group is 3.7 or more and the five acids, ammonium salts of the B-group and esters of the B-group. The metal inhibitor contains one or more types selected from the group consisting of aromatic compounds having a triazole skeleton and one or more types selected from the group consisting of aliphatic compounds having a triazole skeleton and compounds having any one of pyrimidine skeleton, imidazole skeleton, guanidine skeleton, thiazole skeleton and pyrazole skeleton. The polishing slurry having a high metal-polishing rate, reducing etching rate and polishing friction, results in the production, with high productivity, of semiconductor devices reduced in dishing and erosion in metal wiring.

This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and / or prevented include rheumatoid arthritis.

A material for making elastomeric nitrile rubber articles is disclosed. In particular, the process and material formulation can produce nitrile rubber based articles, which exhibit force-strain characteristics that are comparable to those of natural rubber latex articles, while maintaining the tensile strength properties of nitrile rubber. The process includes an accelerator composition at the pre-cure stage having a dithiocarbamate, a thiazole, and a guanidine compound. The invention also includes an elastomeric nitrile rubber product made by the process, such as examination, surgical, or work gloves, which can have an exterior coating over naked rubber selected from either a silicone emulsion or oil, glycerin solution, a combined mixture of silicone and glycerin / glycerol, a fluorocarbon release agent, or a natural or synthetic hydrocarbon-based oil in amounts that do not degrade said substrate rubber material.

The present invention relates to an organic electroluminescent device comprising a substrate, a cathode, at least two organic material layers comprising a light-emitting layer, and an anode in the sequentially laminated form, in which the organic material layers comprise an organic material layer comprising a compound having a functional group selected from the group consisting of an imidazole group, an oxazole group and a thiazole group between the cathode and the light-emitting layer. The organic electroluminescent device according to the present invention comprises an organic material layer comprising a compound having a functional group selected from the group consisting of an imidazole group, an oxazole group and a thiazole group between a cathode and a light-emitting layer, thus having an improved electron injection characteristic to provide an organic electroluminescent device of an inverted structure operating at a low voltage.

Abstract of Disclosure The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain;B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g / mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

The present invention discloses a medicine with actions of resisting plant virus and resisting tumor-N-substituted benzothiazolyl-1-substituted phenyl-0.0-dialkyl-alpha- aminophosphonates derivative, its preparation method and biological activity. Said invention also provides its structure formula, and also provides its extensive application for inhibiting tobacco mosaic virus (TMV) activity and inhibiting activity of human body prostatic cancer cell PC3 and others.

The invention provides a fungicide composition containing an active component A and an active component B, and application thereof in preventing and controlling various agricultural fungal diseases. The active component A in the composition is one of two methoxyl acrylic ester compounds; and as shown above, the active component B of the compound A1 and the compound A2 is one of the following fungicide varieties: thiocarbamate compounds or salt thereof, aliphatic compounds or salt thereof, carbamate compounds or salt thereof, oxazole compounds or salt thereof, thiazole compounds or salt thereof, amide compounds or salt thereof, organophosphorus compounds or salt thereof, imidazole compounds or salt thereof, antibiotic compounds or salt thereof, pyridine compounds or salt thereof and triazole compounds or salt thereof.