123 results about "Pyrimidinedione" patented technology

The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.

The present invention provides novel cycloalkyl-substituted pyrimidine dione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

The invention relates to a synthetic method for 5-chloro-6-(2-iminopyrrolidinyl-1-yl)methyl-2,4-(1H,3H)pyrimidinedione hydrochloride. The synthetic method comprises the following steps: with S-methylisothiourea sulfate as a starting raw material, subjecting S-methylisothiourea sulfate and ethyl chloroacetoacetate to a cyclization reaction under an alkaline condition so as to obtain 6-(chloromethyl)-2-(methylthio)pyrimidine-4(3H)-one; carrying out a chlorination reaction on a pyrimidine ring so as to obtain 5-chloro-6-(chloromethyl)-2-(methylthio)pyrimidine-4(3H)-one; then carrying out a hydrolysis reaction under an acidic condition so as to obtain 5-chloro-6-(chloromethyl)pyrimidine-2,4-(1H,3H)-dione; and reacting 5-chloro-6-(chloromethyl)pyrimidine-2,4-(1H,3H)-dione with 2-iminopyrrolidinyl hydrochloride so as to obtain 5-chloro-6-(2-iminopyrrolidinyl-1-yl)methyl-2,4-(1H,3H)pyrimidinedione hydrochloride, i.e., a finished product of hydrochloride. The synthetic method has the advantages of simple operation, a stable intermediate, easy availability, high yield and easy realization of industrial production.

The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. Specifically, bicyclic heteroaryl derivatives containing a imidazole, thiazole or oxazole fused to a pyridinone, pyrimidinone or pyrimidindione are provided. These compounds have therapeutic utility toward treating an ACC enzyme mediated disorder such as obesity in a subject, upon administration in an effective amount to said subject.

The invention belongs to the technical field of medicines, and in particular relates to a new intermediate shown as a formula I and used for preparing pyrimidinedione DPP-IV (dipeptidyl peptidase IV) inhibitors, such as 2-({6-[(3R)-3-aminopiperidine-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl}methyl) cyanophenyl or salts thereof or analogs thereof, and a preparation method of the new intermediate. The formula I is described in the specification.

The invention provides a preparation method of 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-2,4(1H,3H)-pyrimidine dione or salts thereof, which comprises the following steps: by using 6-methylpyrimidyl-2,4(1H,3H)-dione as an initial raw material, carrying out 6- site methyl oxidation and 5- site hydrogen chlorination, reducing the 6- site formyl group, carrying out condensation with 2-aminopyrrolidine or corresponding salts to obtain the target product. The method is simple to operate and stable in technique, is suitable for industrial production, and has the advantages of high yield, high purity and low cost.

2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R<1 >is a C6-10 aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-4 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl, C1-6 alkoxymethyl, C1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, N-(C1-3 alkyl)aminomethyl, N,N-di(C1-3 alkyl)aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl)amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R<2 >is hydrogen, halogen, nitro, cyano, C1-3 alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl)amino, C1-3 alkylcarbamol, di(C1-3 alkyl)carbamoyl, C1-3 alkyl, C3-6 cycloalkyl or benzyl; R<3 >and R<4 >are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino acetamido, trifluoroacetamido, azido, C1-3 alkyl, C-1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C-1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.

The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

The present invention relates to inhibitors of MALT1 proteolytic and / or autoproteolytic activity. More specifically, it relates to compounds such as, but not limited to peptide derivates such as Z-LSSR-CHO (see SEQ ID NO:1), Z-LSSR-CMK (see SEQ ID NO:1), Z-GASR-CHO (see SEQ ID NO:2), and Z-GASR-CMK (see SEQ ID NO:2), and small compounds such as 5-{[5-(3-chloro-4-methylphenyl)-2-furyl]methylene}-2-thioxodihydro-4,6(1H,5H)-pyrimidinedione and variants thereof, and the use of those compounds for the preparation of a medicament. The invention relates further to a method to screen for inhibitors of the MALT1 proteolytic and / or autoproteolytic activity.

The invention relates to a synthetic method of three elagolix impurities which is important to the synthesis of high-quality elagolix. The invention mainly focuses on the study on a preparation methodof (R)-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-3-[2-(2-oxopyrrolidine-1-yl)-2-phenylethyl]pyrimidin-2,4(1H,3H)-dione (II), diethyl (R)-4,4'-[[2-[5-(2-fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl]azadiyl]-dibutyrate (III), and 2,2'-difluoro-3,3'-dimethyoxy-1,1'-biphenyl (IV). A synthesis route is shown in the description.

The invention discloses a kind of pyrimidine diketone compounds containing a benzoxazine ring and application thereof. The pyrimidine diketone compounds containing the benzoxazine ring are compounds with the structure shown as a general formula (1) in the specification, and in the formula (1), R1 is selected from hydrogen or an alkyl with the carbon atom number of 1-6, R2 is an ester with the carbon atom number of 2-10, and X is selected from halogen. The pyrimidine diketone compounds containing the benzoxazine ring possess high weeding activity.

PCT No. PCT / KR97 / 00084 Sec. 371 Date Nov. 10, 1998 Sec. 102(e) Date Nov. 10, 1998 PCT Filed May 15, 1997 PCT Pub. No. WO97 / 43266 PCT Pub. Date Nov. 20, 19976-aryloxy and 6-arylcarbonyl 2,4-pyrimidinedione derivatives of the formula(I) having high antiviral activity against HIV-1 and low toxicity are useful for treating AIDS: wherein: R1 is hydrogen or a C1-10 alkyl group optionally having a substituent selected from the group consisting of aryl, hydroxy, C1-10 alkoxy and C2-5 alkylcarbonyloxy groups; R2 is hydrogen or a C1-10 alkyl group optionally having an aryl substituent; R3 and R4 are each hydrogen or a C1-3 alkyl group; and A is oxygen or a carbonyl group.

The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The present invention relates to a compound of formula (I)or its stereoisomers, tautomers, solvates, hydrates, prodrugs, pharmaceutically acceptable salts or mixtures thereof, or pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. The present invention also provides a method for the prophylaxis or treatment of a medical condition associated with protein kinase, by administering a pharmaceutically effective amount of the compound of formula (I) or salts thereof.

The invention provides a preparation method of a tipiracil intermediate which is 6-(chloromethyl)-2, 4-(1H, 3H)-pyrimidinedione. 6-methyl-2, 4-(1H, 3H)-pyrimidinedione as an initial raw material undergoes an iodine replacement reaction at the 5th site of a compound and then the product undergoes reduction and chlorination reactions at the 6th site to produce a desired product. The preparation method has the advantages of stable processes, high yield and low cost and is suitable for industrial production.

The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

The invention relates to a novel crystal of pyrimidinedione compound hydrochloride and a preparation method thereof. The invention discloses the novel crystal of 5-chloro-6-[(2-imino-1-pyrrolidyl)methyl]-2,4(1H, 3H)-pyrimidinedione hydrochloride shown in the formula I and the preparation method thereof. The novel crystal can produce X-ray diffraction peaks at diffraction angles 2 theta of 11.73 degrees, 13.03 degrees, 17.33 degrees, 17.97 degrees, 23.45 degrees, 27.23 degrees, 29.40 degrees and 32.85 degrees, has good stability and reappearance and is suitable for medicine development and application.

The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention discloses a new crystal form of Tipracil hydrochloride and a preparation method thereof. Particularly, the invention relates to a crystal form of Tipracil hydrochloride shown in the formula (1), namely 5-chloro-6-[(2-imino-pyrrolidine) methyl]-2,4(1H,3H)-pyrimidinedione hydrochloride, and a preparation method of the new crystal form of Tipracil hydrochloride. The crystal form is stable and easily prepared and meets the application requirement of medicine preparations. The formula (1) is shown in the specification.

The present invention relates to uracil-based compounds, to a method for producing the compounds, and to herbicides comprising the compounds as active ingredients. R1, R2, R3, R4, R5, X, Y, Z, and W are as defined in the detailed description of the invention. [Keywords] uracil, herbicides, pyrimidinedione.

The invention discloses a quinazoline ketone derivative and a preparation method and application thereof.The compound is of the structure as shown in the general formula (I).The invention further relates to a drug composition containing the compound in the formula (I).Activity screening experiments show that the compound has good anti-acne-virus and anti-adenovirus activity, and therefore application of the compound to preparing anti-acne-virus and anti-adenovirus drugs is also provided.Please see the formula (I) in the description.

The invention relates to a pyrimidinedione derivative capable of inhibiting a monocarboxylate transporter, the pyrimidinedione derivative is a formula (I) compound and / or a pharmaceutically acceptablesalt thereof, and / or a stereoisomer thereof, and / or a solvate thereof, the compound has the effect of inhibiting the activity of the monocarboxylate transporter, and also comprises a pharmaceutical composition containing the formula (I) compound and the use of the pharmaceutical composition in treatment.

Disclosed are fungicidal mixtures, compositions and methods for controlling plant diseases relating to combinations comprising (a) at least one compound selected from phenylamidines of Formula I, N-oxides, and agriculturally suitable salts thereof (I) wherein A is C3alkylene, optionally substituted with one or two methyl; W is CR<5>R<6>R<7>or SiR<8>R<9>R<10>; and R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<9> and R<10>are as defined in the disclosure; and (b) at least one compound selected from alkylenebis(dithiocarbamate) fungicides, compounds acting at the bc1complex of the fungal mitochondrial respiratory electron transfer site, cymoxanil, compounds acting at the demethylase enzyme of the sterol biosynthesis pathway, morpholine and piperidine compounds that act on the sterol biosynthesis pathway, phenylamide fungicides, pyrimidinone fungicides, chlorothalonil, carboxamides acting at complex II of the fungal mitochondrial respiratory electron transfer site, quinoxyfen, metrafenone, cyflufenamid, cyprodinil, copper compounds, phthalimide fungicides, fosetyl-aluminum, benzimidazole fungicides, cyazofamid, fluazinam, iprovalicarb, propamocarb, validamycin, dichlorophenyl dicarboximide fungicides, zoxamide and dimethomorph, and their agriculturally suitable salts.

The present invention provides an FTD and TPI-containing orally administrable pharmaceutical composition which can be orally administered and is stable even under high-humidity conditions.An orally administrable pharmaceutical composition which comprises α,α,α-trifluorothymidine and 5-chloro-6-(2-iminopyrrolidine-1-yl)methyl-2,4(1H,3H)-pyrimidine dione hydrochloride as active ingredients and additives having a critical relative humidity of 85% or more at 25° C. as an excipient.