45 results about "Imidazothiazole" patented technology

The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.

The present invention provides compounds, compositions and methods for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of cell proliferative disorders such as cancer.

The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.

This invention concerns the use of a compound of formula (I)a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, whereinZ is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-;Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl;L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl or C1-6alkyl-O—;Het1 represents morpholinyl; pyrazolyl or imidazolyl;Het4 represents morpholinyl, pyrazolyl or imidazolyl;Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.

This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

The present invention relates to compounds of formula I which are capable of inhibiting p38 in vivo or in vitro.

Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I,a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.

The invention relates to the technical field of medicines, and relates to benzimidazothiazole carboxamide compound and application thereof. The benzimidazothiazole carboxamide compound comprises derivatives and pharmaceutically acceptable salts of the benzimidazothiazole carboxamide compound, and the general structure of benzimidazothiazole carboxamide compound is as shown in the description, wherein R1 and R2 are as described in the claims and the description. The benzimidazothiazole carboxamide compound and pharmaceutically acceptable acid addition salts of the benzimidazothiazole carboxamide compound can be combined with existing drugs or used alone as an epidermal growth factor tyrosine kinase inhibitor for treating associated diseases caused by transduction disorder of epidermal growth factor receptor signals such as small cell lung cancer, squamous cell carcinoma, adenocarcinoma, large cell carcinoma, colorectal cancer, mammary cancer, ovarian cancer and renal cell carcinoma.

This invention concerns the use of a compound of formula (I)a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, whereinZ is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-;Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl;L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl or C1-6alkyl-O—;Het1 represents morpholinyl; pyrazolyl or imidazolyl;Het4 represents morpholinyl, pyrazolyl or imidazolyl;Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the α7 nicotinic receptor is beneficial.

The invention discloses a preparation method of 5,6-dihydro-6-(2-naphthyl)imidazo[2,1-b]thiazole oxalate, comprising step 1: adding 2-vinyl to the solvent Naphthalene is the raw material, hydrogen peroxide and brominated compounds, and a catalyst is added to react in the reaction temperature range of -20°C to 200°C to obtain brominated intermediates. The amount of hydrogen peroxide is 0.5-5 equivalents, and the amount of brominated compounds is 1 ‑10 equivalents; step 2: add 2‑aminothiazole and solvent to the brominated intermediate obtained in step 1, without catalyst, react in the reaction temperature range of ‑20°C-200°C to obtain the thiazole intermediate, the The amount of 2-aminothiazole is 0.8-2 equivalents; Step 3: Add one or both of dihydrate oxalic acid and anhydrous oxalic acid and a solvent to the thiazole intermediate obtained in step 2, at -20°C-300°C Reaction in the reaction temperature range obtains 5,6-dihydro-6-(2-naphthyl) imidazo[2,1-b]thiazole oxalate. The reaction route is short and the pollution is small.

The present invention provides a compounds 7a-f to 18a-f and 19a-f to 30a-f of general formula A, useful as potential anticancer agents against human cancer cell lines. The present invention further provides a process for the preparation of imidazothiazole-chalcone hybrids 7a-f to 18a-f and 19a-f to 30a-f of general formula Awherein

The invention discloses a benzimidazolo[2,1-b]thiazole compound and an application thereof, belonging to the technical field of medicine. The benzimidazolo[2,1-b]thiazole analogs synthesized in the present invention have an inhibitory activity of more than 90% on FLT3, wherein the compounds (compounds 2, 4, 6, 8 and 10) have an inhibitory activity on FLT3-ITD kinase IC 50 lower values, especially for compound 2, whose IC 50 value is only 5.60nM, therefore, the compound of the present invention can be used as the inhibitor of FLT3, or be used for preparing medicine, and said medicine can affect the enzymatic activity of one or more tyrosine kinases and interfere with the enzyme activity produced by said Kinase-transduced signals to regulate or inhibit diseases associated with abnormal cell proliferation hold great promise.

The invention discloses a preparation method of 5-(2-oxytetrahydrothiophene imidazole-4(2H)-alkenyl pentanoic acid compounds. The preparation method comprises the following steps: performing reactionon (3S,7aR)-6-substituted benzyl-7-alkoxy-3-substituted phenyl tetrahydroimidazole[1,5-c]thiazole-5(3H)-ketone and 1-cyclohexene oxytrimethylsilane to generate (3S,7aR)-6-substituted benzyl-7-(2-oxycyclohexyl)-3-substituted tetrahydroimidazole[1,5-c]thiazole-5(3H)-ketone, and sequentially performing ring-opening reaction, reduction ring-opening reaction, cyclization and elimination reaction to obtain the 5-(2-oxytetrahydrothiophene imidazole-4(2H)-alkenyl pentanoic acid compounds. The preparation method has the advantages of little side reaction, high yield, environmental friendliness, mild and easily controlled reaction condition and simplicity in aftertreatment, and is suitable for industrialized production.

The invention discloses an application of N-(5-bromo-2-methoxyphenyl)benzoimidazothiazole carboxamide in preparation of drugs for inhibiting and killing streptococcus mutans type strains or in preparation of drugs for inhibiting formation of a streptococcus mutans type strain biofilm. Experiments prove that the compound shows good bacteriostatic and bactericidal activities against the streptococcus mutans type strains in a floating state, and the inhibition rate of the compound to the streptococcus mutans biofilm reaches 99% or more when the final concentration of the compound in a culture medium reaches 4 mg / L. The compound can be used as a novel lead compound for preventing dental caries, and has broad application prospects in preparation of oral streptococcus mutans biofilm inhibitors.

The present invention provides a new process for the preparation of a substituted imidazothiazolone compound. The process of the present invention uses a fluoride-free Lewis acid which is cheap and friendly to environment, and provides high selectivity and yield.

The invention belongs to the technical field of intelligent manufacturing, and specifically relates to a preparation method of a composite conductive polymer flexible sensing array. The method proposed by the present invention is to combine tetrahydro-(4R)-carboxy-(2S)-phenylthiazole, (7aR)-3-phenyl-1H, 3H-imidazo[1,5- c ]thiazole-(6,7aH)-5,7-diketone, polyvinylpyrrolidone, polyvinylidene fluoride, polylactic acid, polypyrrole, and polythiophene are added in tetrahydrofuran, and heated in an autoclave to obtain sensing ink; On the surface of the nylon fabric, the pattern of the sensing ink array is screen-printed and dried in a hot embossing machine to obtain a composite conductive polymer flexible sensing array. The composite conductive polymer flexible sensing array is used as a liner, sandwiched between the inner and outer rings of the aviation joint bearing, and the sensing sensitivities of the flexible sensing array to stress and strain, temperature and humidity are respectively 7.9~9.3 on the aviation bearing testing machine. ,-2.16×10 ‑3 ~‑1.92×10 ‑3 K ‑1 And 937%~998%.