123 results about "Benzothiazine" patented technology

Q is —N=or CR2 X is S, O or NOR3 Y is —O—, —S—, —SO— or —SO2—R and R1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl groupR2 is H or a substituentR3 is H, or —C(O)R4 R4 is a substituted or unsubstituted aliphatic or aromatic groupn is an integer from 0 to 1Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine / threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.

The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and / or 6′ halo and / or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.

The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and / or 6′ halo and / or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.

KATP channel openers (KCOs) are useful for the prophylactic and / or therapeutic treatment of CNS chronic inflammation associated with a disease or state in a mammal, including a human. The administration of KCOs, including the groups of benzopirans, cyanoguanidines, thioformamides, benzothiadiazines, pyridyl nitrates, pyrimidine sulfates, cyclobutenediones, DHP-related compounds, tertiary carbinols, 6-sulfonil-chromenes, 1,2,3-triazoles, pyridothiadiazines, benzothiazines, halogenquinazolins and phenylbenzimidazoles, and in particular, the compound diazoxide, result in a reduction of reactive microglial response in various CNS pathologies such as axonal injury, brain tumors, traumatic damage, neurodegeneration, spinal cord injury, infectious and autoimmune diseases. KCOs, isotopically modified, are also useful for the preparation of diagnostic agents for detection and follow-up of CNS chronic inflammation.

The invention belongs to the medicine field, and particularly relates to benzothiazinethione derivatives and preparation methods and uses thereof. In the aspect of the present invention, novel benzothiazinethione derivatives of formula I are provided, the benzothiazinethione derivatives of the invention are new compounds obtained based on extensive screening. Experimental results show that the benzothiazinethione derivatives of formula I have obvious inhibitory effects on mycobacterium tuberculosis, with effects equivalent to or even better than that of isoniazide (MIC 90 =0.8µM). The benzothiazinethione derivatives of formula I have anti-mycobacterium tuberculosis activities, and provide new choices for the development and application of antitubercular agents.

The invention relates to benzothiazine-4-ketone compounds (shown in the formula I and formula I' in the description) containing basic nitrogen heterocyclic fragments, preparing methods and medical application of the benzothiazine-4-ketone compounds and antituberculosis drug compositions with the benzothiazine-4-ketone compounds as effective constituents, in particular to a 6-trifluoromethyl-8-nitryl-4H-benzo[e][1,3] thiazine-4-ketone compound. A 2-substituent group is 1-nitrogen heterocyclic alkyl or dinitrogen heterocyclic alkyl. R represents H, an alkyl group of 1-4 C atoms, heterocyclic alkyl of 4-7 C atoms, a phenyl group and a substituted phenyl; R1 represents H, an alkyl group of 1-3 C atoms and heterocyclic alkyl of 3-6 C atoms; R2 represents H, an alkyl group of 1-4 C atoms, heterocyclic alkyl of 4-7 C atoms, a phenyl group and substituted phenyl; n1 represents 0-1; n2 represents 1-3; n3 represents 1 and 3.

The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11[beta]-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen.

The present invention provides a compound of formula (I), wherein Q is -N= or CR2; X is S, O or NOR3; Y is -O-, S-, -SO- or -SO2-; R and R1 are independently is H, substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl-yl; group; R2 is H or a substituent; R3 is H, or -C(O)R4; R4 is substituted or unsubstituted Substituted aliphatic or aromatic groups; n is an integer 0-1. Compounds of formula (I) and their physiologically acceptable salts are inhibitors of serine / threonine and tyrosine kinase activity. Several tyrosine kinases whose activity can be inhibited by these compounds are involved in the angiogenic process. Thus, these chemical compounds are able to ameliorate disease states in which angiogenesis or endothelial cell proliferation is a factor. These compounds are useful in the treatment of cancer and hyperproliferative diseases.

The invention discloses a method for preparing 2-amino benzothiazine. The method comprises the steps of preparing the 2-amino benzothiazine by addition reaction of catalytic o-amino ethyl cinnamate and isothiocyanate under the catalysis of trifluoromethanesulfonic acid rare-earth compound Ln(OTf)3 serving as a catalyst, wherein Ln represents a triad rate-earth metal ion and is one of lanthanum, neodymium, samarium or ytterbium, OTf represents trifluoromethanesulfonic acid radical and the chemical structural formula of o-amino ethyl cinnamate is shown in the specification; and the general formula of the chemical structure of isothiocyanate is RNCS. In the method, the catalyst is good in chemical selectivity, high in reactivity, mild in reaction condition, and short in reaction time; the reaction has high atom economy and does need a solvent; and the yield of a target product can be up to 99%.

The invention discloses a benzothiazinone compound and a preparation method and application of the benzothiazinone compound as an antituberculosis drug, and particularly relates to a novel compound with a benzothiazinone skeleton. The compound has an inhibition effect on tubercle bacillus, especially tubercle bacillus with clinical drug resistance. Results show that the compound shows an obvious antibacterial effect, the antibacterial effect far exceeds that of a positive control isoniazide, and particularly, compared with a positive control pBTZ169, the compound has an obvious and good cLogPvalue.

The invention relates to a method for ammonolyzing and synthesizing meloxicam under the catalysis of Lewis acid. Under the catalysis of silicate Lewis acid, the meloxicam is synthesized from 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid ethyl ester 1,1-dioxide and 2-amino-5methylthiazol. Compared with the direct ammonolysis method, the method has the advantages that: (1) the reaction time is about 4 to 6 hours which is shortened by four times and ammonolysis is complete; and (2) the ammonolysis yield is high which is more than or equal to 85 percent; decomposers and carbides are avoided; the product is easy to purify; the method for synthesizing the meloxicam is suitable for mass production; the product purity reaches 99 percent through HPLC detection; the product is light yellow green; and the product quality meets Chinese pharmacopoeia 2005.

The invention relates to a novel green synthetic method. According to the method, N1,N3-disubstituted imidazole type ionic liquid is taken as a solvent, NH-sulfoximine is taken as a raw material, a diazo compound, alkyne and sulfur ylide are taken as coupling reagents, and a 1,2-benzothiazine derivative is mildly and efficiently synthesized through a transition metal catalyzed C-H activation / cyclization reaction. Compared with other technologies, the condition is milder, the operation is simple, the method is safe, and the environmental friendliness is achieved; the catalytic activity is high,the reaction yield is high, and the application range of substrates is wide; the solvent and catalysts can be recycled, so that the reaction cost is reduced.

The invention belongs to the technical field of organic chemistry, in particular to a benzothiazole compounds and a preparation method for the compounds. The structures of the compounds are attributed and determined by the methods like <1>H NMR, <13>CNMR, IR, MS, elementary analysis, and a single-crystal X-ray diffraction, etc. The invention uses a silver triflate as a catalyst to prepare 4-methylene-1H-benzo[d] [1, 3] thiazine-2(4H)-imine framework compounds by mixing an ortho-alkynyl aniline and an isothiocyanate in a tetrahydrofuran to react at a room temperature. The method of the invention has the advantages of mild reaction condition, simple operation, lower cost, fewer side effects and high purity of the product; thereby having a great application prospect.

The invention relates to a benzothiazine-4-one compound containing 2,7-diazaspiro[3.5]nonane fragments and a preparation method thereof and in particular relates to 6-trifluoromethyl-8-nitro-4H-benzo[e][1,3]thiazine-4-one compounds. The 2-position substituent group is 2,7-diazaspiro[3.5]nonane-7-yl, wherein Ar represents phenyl, pyridyl, naphthyl, quinolyl, pyrazinyl, pyrimidyl, pyrazolyl, imidazolyl, furyl or thienyl, and optionally, the hydrogen atom at any position of the groups can be substituted by the group R; the group R is selected from alkyl having 1-4 carbon atoms, alkoxy having 1-3carbon atoms, halogen, -CF3, -OCF3, -NO2 or -CN.

The present invention provides improved methods for synthesizing novel benzothiazepine compounds. In particular, the invention relates to a new method that generally is used to make the substituted 2,3,4,5-tetrahydro-1,4-benzothiazepine compounds of a general formulawhich then may be used to make many other benzothiazepine compounds.

The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. More particularly, the present invention relates to novel alkyl carboxylic acids of the general, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. The present invention also relates to processes for the preparation of the compounds of formula (I), novel intermediates, processes for their preparation, their use in the preparation of the above said compounds and their use as antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds.

The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria.The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.The solution of the present invention is a compound of the formula Iwherein R1 and R2 are, independently each from other, NO2, CN, CONR7R8, COOR9, CHO, halogen, NR7R8, SO2NR7R8, SR9, OCF3, mono-, di or trifluoromethyl;R3 and R4 are, independently each from other, H, a saturated or unsaturated, linear or branched aliphatic radical having 1-7 chain members, cycloalkyl having 3-6 carbon atoms, benzyl, SR9, OR9;R5 and R6 are, independently each from other, a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-8 chain members, cycloalkyl having 3-6 carbon atoms, phenyl, or R5 and R6 together represent a bivalent radical —(CR92)m—, or R5 and R6 together represent bivalent radicals:wherein m is 1-4, or represent bivalent radicals a saturated or unsaturated mono or polyheterocycles with heteroatoms N, S, O and substituted by (R10)x, wherein x is 1-4;R7, R8 and R9 are, independently each from other H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, mono-, di or trifluoromethyl, halogen, phenyl, or R3 and R4 together represent a bivalent radical —(CH2)n— wherein n is 2-7;R10 is H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, NO2, NR7R8, CN, CONR7R8, COOR9, CHO, halogen, SO2NR7R8, SR9, OR9, OCF3, mono-, di or trifluoromethyl, benzyl or phenyl.