33 results about "Thiazide derivatives" patented technology

The preset invention relates to use of antipsychotic phenothiazine derivative for eliminating cancer stem cells (CSCs) and / or preventing a cancer. The invention also provides a pharmaceutical composition for treating a cancer, and / or preventing or delaying cancer recurrence comprising trifluoperazine and an anti-cancer drug, such as gefitinib or cisplatin.

The present invention provides a phenothiazine-derivative color-measuring method that can detect a phenothiazine-derivative color even at a wavelength longer than the wavelength that exhibits maximum absorption. A phenothiazine-derivative color is detected, by adding a 5-hydroxy-1-(4-sulfophenyl)-4-(4-sulfophenylazo)pyrazole-3-carboxylic acid salt, 6-hydroxy-5-(4-sulfophenylazo)-2-naphthalenesulfonic acid salt, 3-hydroxy-4-(4-sulfonaphthylazo)-2,7-naphthalenedisulfonic acid salt, 7-hydroxy-8-(4-sulfonaphthylazo)-1,3-naphthalenedisulfonic acid salt, 3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodospiro[isobenzofuran-1(3H),9′-(9H)xanthene]-3-one salt, 3′,6′-dihydroxy-2′,4′,5′,7′-tetrabromo-4,5,6,7,-tetrachlorospiro[isobenzofuran-1(3H),9′-[9H]xanthene]-3-one salt, 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodospiro[isobenzofuran-1(3H),9′-[9H]xanthene]-3-one salt or flavonoid-based color to the reaction system containing a phenothiazine-derivative color, and then measuring the light absorbance at a wavelength of 610 to 730 nm.

The invention provides a screening method and screening kit for a cell protecting agent. Specifically, the invention provides a method for screening a cell protecting agent showing an Hsp90-binding activity and a heat shock protein expression-inducing activity but having no Hsp90 client protein degradation-promoting activity. The method comprises the following steps (1) to (3): (1) measuring the binding property of a test compound to Hsp90; (2) measuring the activity of a test compound to induce the expression of a heat shock protein, or measuring the activity of a test compound to disrupt an Hsp90 / HSF-1 complex, by using a cell capable of expressing the heat shock protein; and (3) measuring the activity of a test compound to induce the degradation of an Hsp90 client protein by using a cell capable of expressing the Hsp90 client protein. The invention further provides specifically a kit for screening a cell protecting agent, comprising (1) Hsp90; (2) a reagent for measuring the heat shock protein expression-inducing activity; (3) an imidazothiazine derivative; and (4) a reagent for quantifying an Hsp90 client protein.

Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine derivative of the formula:wherein R14 is a C1-C24 straight chain or branched alkyl group; or a C6-C24 aryl or arylalkyl group; R15 is a C1-C6 alkyl or a C6-C30 aryl or alkylaryl group; and X is chlorine, bromine or iodine. The dithiazine may be isolated from a whole spent fluid (WSF) formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing dithiazine or dithiazine derivative and a corrosion inhibiting formulation may be used to inhibit corrosion in the well.

The invention provides a phenothiazine derivative. The phenothiazine derivative has a structure shown as a formula (I) or a formula (II), wherein in the formula (I), R[1] is selected from one or moreof H, CH3, C2H5, the formula shown in the description and the formula shown in the description; n is an integer and is 1 or 2; in the formula (II), R[1] is selected from one or more of the formula shown in the description and the formula shown in the description. The phenothiazine derivative with the specific structure, provided by the invention, has relatively good water solubility, high sensitivity, good selectivity, good light stability and high bioavailability, and has very good affinity with Abeta1-42 aggregates. Therefore, the phenothiazine derivative provided by the invention not only can be used as a fluorescent molecular probe applied to imaging of Abeta protein plaques, but also can be used for early diagnosis of Alzheimer's disease.

A compound represented by general formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt has an Abeta production inhibitory activity or BACE 1 inhibitory activity, and is thus useful as an agent for treating neurodegenerative diseases caused by Abeta as typified by Alzheimer's disease. In the formula, ring A represents a C6-14 aryl group or the like; L represents -NRLCO- (wherein RL represents a hydrogen atom or the like) or the like; ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a C1-3 alkylene group or the like; Z represents an oxygen atom or the like; R<1> and R<2> each independently represents a hydrogen atom or the like; and R<3>, R<4>, R<5> and R<6> each independently represents a hydrogen atom, a halogen atom or the like.

The invention belongs to the field of chemical medicine, particularly relates to a benzothiazine derivative, a preparation method and uses thereof, and provides a benzothiazine derivative, a preparation method and uses thereof, wherein the structure is represented by a formula I. The invention further provides a preparation method and uses of the benzothiazine derivative. The formula I is definedin the specification.

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 preset invention relates to a new method for treating brain tumor with an antipsychotic phenothiazine derivative as a brain tumor cell inhibitor or a brain tumor stem cell inhibitor. In particular, an antipsychotic phenothiazine is accessible to brain via blood-brain barrier, which should be beneficially in treatment of brain tumor.

Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine derivative of the formula:wherein R14 is a C1-C24 straight chain or branched alkyl group; or a C6-C24 aryl or arylalkyl group; R15 is a C1-C6 alkyl or a C6-C30 aryl or alkylaryl group; and X is chlorine, bromine or iodine. The dithiazine may be isolated from a whole spent fluid (WSF) formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing dithiazine or dithiazine derivative and a corrosion inhibiting formulation may be used to inhibit corrosion in the well.

The invention discloses a 5H-[1, 2, 4] triazole [5, 1-b] [1, 3] thiazide derivative with a general formula I, or a pharmaceutically acceptable aquo-complex and salts of the derivative; the derivative comprises a stereisomer or a tautomer, wherein R1 and R2 in the formula I are respectively independent hydrogen, methyl, halogen, hydroxyl, methoxyl, acetyl, propiono, nitro or alkoxy. The 5H-[1, 2, 4] triazole [5, 1-b] [1, 3] thiazide derivative has an obvious inhibiting effect on acetylcholin esterase, and is used for improving the memory of a patient suffering from dementia and Alzheimer's disease. The invention also relates to a preparation method of the compound and an application in preparation of a drug for treating Senile Dementia.

The present invention relates to piperazine phenothiazine derivatives useful as therapeutic agents for treating spasticity, particularly following an ischemia or traumatic injury, or compression syndrome. The invention further relates to a pharmaceutical composition comprising a compound of the invention for treating spasticity.

The preset invention relates to use of antipsychotic phenothiazine derivative for eliminating cancer stem cells (CSCs) and / or preventing a cancer. The invention also provides a pharmaceutical composition for treating a cancer, and / or preventing or delaying cancer recurrence comprising trifluoperazine and an anti-cancer drug, such as gefitinib or cisplatin.

The present invention provides a phenothiazine-derivative color-measuring method that can detect a phenothiazine-derivative color even at a wavelength longer than the wavelength that exhibits maximum absorption. A phenothiazine-derivative color is detected, by adding a 5-hydroxy-1-(4-sulfophenyl)-4-(4-sulfophenylazo)pyrazole-3-carboxylic acid salt, 6-hydroxy-5-(4-sulfophenylazo)-2-naphthalenesulfonic acid salt, 3-hydroxy-4-(4-sulfonaphthylazo)-2,7-naphthalenedisulfonic acid salt, 7-hydroxy-8-(4-sulfonaphthylazo)-1,3-naphthalenedisulfonic acid salt, 3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodospiro[isobenzofuran-1(3H),9′-(9H)xanthene]-3-one salt, 3′,6′-dihydroxy-2′,4′,5′,7′-tetrabromo-4,5,6,7,-tetrachlorospiro[isobenzofuran-1(3H),9′-[9H]xanthene]-3-one salt, 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodospiro[isobenzofuran-1(3H),9′-[9H]xanthene]-3-one salt or flavonoid-based color to the reaction system containing a phenothiazine-derivative color, and then measuring the light absorbance at a wavelength of 610 to 730 nm.

The present invention relates to use of antipsychotic phenothiazine derivative for treatment of cancer. The invention also provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating a cancer, and / or preventing or delaying cancer recurrence based on trifluoperazine. The invention further provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating cancer based on thioridazine and its enantiomers. Additionally, the invention provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating KRAS mutant NSCLC comprising thioridazine.

The present invention relates to use of antipsychotic phenothiazine derivative for treatment of cancer. The invention also provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating a cancer, and / or preventing or delaying cancer recurrence based on trifluoperazine. The invention further provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating cancer based on thioridazine and its enantiomers. Additionally, the invention provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating KRAS mutant NSCLC comprising thioridazine.

Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine derivative of the formula:wherein R14 is a C1-C24 straight chain or branched alkyl group; or a C6-C24 aryl or arylalkyl group; R15 is a C1-C6 alkyl or a C6-C30 aryl or alkylaryl group; and X is chlorine, bromine or iodine. The dithiazine may be isolated from a whole spent fluid (WSF) formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing dithiazine or dithiazine derivative and a corrosion inhibiting formulation may be used to inhibit corrosion in the well.

The invention discloses an iridium complex, a preparation method, and an application thereof. The iridium complex has the structure as the specification, wherein the coordinated group in the section Cis selected from: phenyl, pyridyl, thienyl and pyrimidinyl; the coordinated group in the section N is selected from: pyridyl, pyrimidinyl, pyridazinyl, triazinyl, thiazolyl, imidazolyl, quinolyl, isoquinolyl, quinazolinyl or pteridinyl; the R1 is selected from: alkane derivatives, ether derivatives, halogenated hydrocarbon derivatives, ketone derivatives, benzene derivatives, pyridine derivativesand naphthalene derivatives; R2 is selected from: alcohol derivatives, amine derivatives, benzene derivatives, pyridine derivatives, pyrimidine derivatives, diphenylamine derivatives, carbazole derivatives, carboline derivatives, 9,10-dihydroacridine derivatives, phenoxazine derivatives, phenothiazine derivatives, and azole derivatives. The iridium complex has high carrier transport capability, is easy to synthesize, has stable chemical properties, and is easy to sublimate and purify.

The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters,pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.

A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an Abeta production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Abeta and typified by Alzheimer-type dementia.

The invention provides a phenothiazine derivative. The phenothiazine derivative has a structure shown as a formula (I) or a formula (II), wherein in the formula (I), R[1] is selected from one or moreof H, CH3, C2H5, the formula shown in the description and the formula shown in the description; n is an integer and is 1 or 2; in the formula (II), R[1] is selected from one or more of the formula shown in the description and the formula shown in the description. The phenothiazine derivative with the specific structure, provided by the invention, has relatively good water solubility, high sensitivity, good selectivity, good light stability and high bioavailability, and has very good affinity with Abeta1-42 aggregates. Therefore, the phenothiazine derivative provided by the invention not only can be used as a fluorescent molecular probe applied to imaging of Abeta protein plaques, but also can be used for early diagnosis of Alzheimer's disease.

The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters, pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.

The present invention relates to piperazine phenothiazine derivatives useful as therapeutic agents for treating spasticity, particularly following an ischemia or traumatic injury, or compression syndrome. The invention further relates to a pharmaceutical composition comprising a compound of the invention for treating spasticity.

The present invention relates to use of antipsychotic phenothiazine derivative for treatment of cancer. The invention also provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating a cancer, and / or preventing or delaying cancer recurrence based on trifluoperazine. The invention further provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating cancer based on thioridazine and its enantiomers. Additionally, the invention provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating KRAS mutant NSCLC comprising thioridazine.

Compounds and methods for the preparation of compounds useful as inhibitors of β-site amyloid precursor protein (APP)-lyase are provided.

The present invention addresses the problem of providing an efficient asymmetric synthesis method for an optically active 1,4-benzothiazepine-1-oxide derivative.[Solution] According to the present invention, an optically active 1,4-benzothiazepine-1-oxide derivative is efficiently produced by reacting a 1,4-benzothiazepine derivative or a salt thereof with a reagent containing a titanium compound, a chiral diol compound and water, and an oxidant in a solvent.

The present invention relates to a novel aminoalkylbenzothiazepine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating constipation comprising the same as an active ingredient.

A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C 6-14 aryl group or the like, L is -NR e CO- or the like (wherein R e is a hydrogen atom or the like), Ring B is a C 6-14 aryl group or the like, X is a C 1-3 alkylene group or the like, Y is a single bond or the like, Z is a C 1-3 alkylene group or the like, R 1 and R 2 are each independently a hydrogen atom or the like, and R 3 , R 4 , R 5 and R 6 are independently a hydrogen atom, a halogen atom or the like, has an A² production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A² and typified by Alzheimer-type dementia.