64 results about "URAT1 Inhibitors" patented technology

The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.[in the formula,R1 is -Q1-A1 and the like; is a double bond or a single bond; when is a double bond, W1 is a nitrogen atom or a group represented by the general formula: ═C(Ra)—, and W2 is a nitrogen atom or a group represented by the general formula: ═C(Rb)—; when is a single bond, W1 is a group represented by the general formula: —C(Raa)(Rab)— or a group represented by the general formula: —(C═O)—, and W2 is a group represented by the general formula: —C(Rba)(Rbb)—, a group represented by the general formula: —(C═O)— or a group represented by the general formula: —N(Rbc)—; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi′)n; and Z is a hydroxyl group or COOR2 and the like.

The invention belongs to the field of medicinal chemistry and particularly relates to hURAT1 (human urate anion transporter 1) inhibitors and an application thereof. Specifically, the hURAT1 inhibitors are compounds with structure shown as formula (I) or (II) in the description or pharmaceutically acceptable salts of the compounds. Experiments prove that the compounds have good inhibition effect on uric acid transport of the hURAT1 in an HEK293 transfection cell, which shows that the compounds have good application prospect in treatment of hyperuricemia or gout.

The invention relates to the medicine field of hyperuricemia and gout. Specifically, the present invention relates to a class of uric acid transporter 1 (URAT1) inhibitors containing a tetrazolium structure, their preparation methods, pharmaceutical compositions containing them, and their application in the preparation and treatment of hyperuricemia and gout . Wherein, each substituent is as shown in the description.

The invention discloses a polymorph I of an S-configuration axially chiral enantiomer of 2-(5-bromo-4-(4-cyclopropylnaphthalene-1-yl)-4H-1,2,4-triazole-3-yl-thio)acetic acid, and CuKalpha radiation based X-ray powder diffraction spectrum represented with the angle 2theta at least have diffraction peaks at 7.02 degrees plus or minus 0.2 degrees, 11.14 degrees plus or minus 0.2 degrees, 14.10 degrees plus or minus 0.2 degrees, 14.60 degrees plus or minus 0.2 degrees, 15.44 degrees plus or minus 0.2 degrees, 16.98 degrees plus or minus 0.2 degrees, 20.98 degrees plus or minus 0.2 degrees, 21.86 degrees plus or minus 0.2 degrees and 28.02 degrees plus or minus 0.2 degrees. Compared with an amorphous form, the polymorph I is good in stability, almost has no hygroscopicity, is high in crystal form purity, and facilitates drug preparation, storage and transportation.

Cycloalkyl acid derivatives, a preparation method thereof, and a pharmaceutical application thereof are described. In particular, a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level are described, wherein definitions of substituent groups in general formula (I) are the same as the definitions in the specification.

The invention relates to the field of medicine for treating hyperuricemia and gout. Concretely, the invention relates to an urate transporter 1(URAT1) inhibitor containing a triazole propionate structure, a preparation method thereof, and an application of a pharmaceutical composition containing the urate transporter 1 inhibitor in preparation of medicines for treating hyperuricemia and gout. Each substituent is shown in a specification.

The present invention relates to a compound having an URAT1 inhibitory activity, and to an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound.More specifically, the present invention relates to a compound represented by the formula (I):whereinR1 is -Q1-A1 or the like; R2 is a hydrogen atom, a halogen atom, a lower alkyl group or the like; W1, W2, W3 and W4 are each independently a nitrogen atom or a methine group optionally having substituents, or the like; X and Y are each a single bond, an oxygen atom or the like; Z is a hydroxyl group or COOR3 or the like.

The invention relates to the field of drugs related to hyperuricemia and gout, in particular to a compound as shown in a formula I and a preparation method thereof, and application of the compound serving as a novel URAT1 inhibitor, particularly application of the compound serving as a therapeutic agent for diseases related to abnormal level of uric acid, wherein the definitions of M, R1, R2, R3,R4, R5, R6, R7 and n formula I are as described in the description.

The invention provides carboxylic acid URAT1 inhibitors containing a naphthylmethyltriazole structure and represented by a general formula (I) which is described in the specification, a preparation method for the inhibitors, pharmaceutical compositions containing the inhibitors, and application of the inhibitors to preparation of drugs used for treating hyperuricemia and gout. The inhibitors as shown in the formula (I) have strong URAT1 inhibitory effect, normally have much stronger inhibitory effect compared with conventional URAT1 inhibitors with the structural characteristic that triazole and a naphthalene ring are directly linked by a covalent bond, and can be used as active ingredients for preparation of therapeutics used for treating gout and hyperuricemia. The inhibitors as shown inthe formula (I) are effective in wide dosage range; for example, the dosage of the inhibitors is about 1-1000 mg for each person each day.

The invention relates to the field of medicines related to hyperuricemia and gout and in particular relates to urate transporter I (URAT1) inhibitors containing triazole malonic acid structures, a preparation method thereof, a medicine composition containing the URAT1 inhibitors and an application of the URAT1 inhibitors and the medicine composition to preparation of diabetes medicines. In a general formula in the specification, R is selected from H, C1-C8 alkyl and C3-C6 cycloalkyl.

The present invention relates to the pharmaceutical field for the treatment of hyperuricemia and gout. In particular, the present invention relates to a carboxylic acid urate transporter 1 (URAT1) inhibitor of a general formula (I) containing a diarylmethane structure and a preparation method thereof, and a pharmaceutical composition containing the same and a use thereof in the preparation of medicaments for treating hyperuricemia and gout,wherein R1 is selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, F, Cl, Br, I, CN, NO2, SR4 or OR4; R2 is selected from H, F, Cl, Br or I; R3 is selected from H or C1-C4 alkyl; X is selected from S or CH2; wherein R4 is selected from C1-C10 alkyl.

Provided is a method for preparing a URAT1 inhibitor, 2-((5-bromo-4-((4-bromonaphthalen-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio) acetic acid represented by the following formula ZXS-BR, the reaction equation of which being shown as follows. Compared with the prior art, the preparation method provided by the present application is of low cost, ease of handling, ease of quality control, and applicable to industrialization.

The invention relates to the field of medicines related to hyperuricemia and gout and in particular relates to urate transporter I (URAT1) inhibitors containing triazolesulfinylmalonic acid structures, a preparation method thereof, a medicine composition containing the URAT1 inhibitors and an application of the URAT1 inhibitors and the medicine composition to preparation of diabetes medicines. In a general formula in the specification, R is selected from H, C1-C8 alkyl and C3-C6 cycloalkyl.

Disclosed are a crystal form of a URAT1 inhibitor, and a preparation method therefor.

The invention relates to the field of medicines related to hyperuricemia and gout and specifically to 2-nitrophenylsulfonamide derivatives as shown in a general formula (I) which is described in the specification, application of the derivatives as URAT1 inhibitors, particularly as therapeutic agents for diseases associated with abnormal uric acid levels, and a preparation method for the derivatives. Each substituent in the general formula (I) is as defined in the specification.

Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

The invention relates to the field of medicines related to hyperuricemia and gouts and in particular relates to urate transporter 1 (URAT1) inhibitors of succinic acid amide structures containing phenylnaphthalene rings, a preparation method thereof, a medicine composition containing the URAT1 inhibitors and an application of the URAT1 inhibitors and the medicine composition in preparation of diabetes medicines. R<1> and R<2> in a general formula are defined in the specification.

The invention relates to the field of medicines related to hyperuricemia and gout and specifically to the application of 2-(trifluoromethyl)benzenesulfonamide derivatives as URAT1 inhibitors, particularly as therapeutic agents for diseases associated with the abnormal levels of uric acid. The 2-(trifluoromethyl)benzenesulfonamide derivatives of the invention are compounds as shown in a formula (I)which is described in the specification. In the formula (I), R1 and X are as defined in the claims of the specification.

The invention relates to the field of medicines related to hyperuricemia and gout and in particular relates to urate transporter I (URAT1) inhibitors containing triazolesulfonylmalonic acid structures, a preparation method thereof, a medicine composition containing the URAT1 inhibitors and an application of the URAT1 inhibitors and the medicine composition to preparation of diabetes medicines. In a general formula in the specification, R is selected from H, C1-C8 alkyl and C3-C6 cycloalkyl.

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R1a, R2a, R6a, and R7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R3a and R8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R3a and R8a are bonded, R4a and R5a form a benzene ring together with two carbon atoms to which R4a and R5a are bonded or represent any of the groups represented by R1a described above, Wa represents CR10a or N, and where, R10a represents any of the groups represented by R1a, Xa represents an oxygen atom or a sulfur atom, Ya represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Za represents CO2H.)

The invention provides a URAT1 inhibitor, which has a structure as shown in a formula I, or pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof. Compared with a drug Dotinurad on themarket, the series of novel deuterated compounds provided by the invention show a stronger inhibition effect on URAT1 transport protein.

The invention relates to the field of medicine for treating hyperuricemia and gout. Concretely, the invention relates to an urate transporter 1(URAT1) inhibitor containing a triazole propionate structure, a preparation method thereof, and an application of a pharmaceutical composition containing the urate transporter 1 inhibitor in preparation of medicines for treating hyperuricemia and gout. Each substituent is shown in a specification.