47 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.

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.

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.