608 results about "Pyrimidone" patented technology

This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.

The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed

A pyrimidin-4-one compound can be prepared in a high yield by reacting an aminoarylcarboxylic acid compound with an organic acid compound in the presence of a nitrogen atom-containing compound under relatively simple and moderate reaction conditions.

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R1 represents a C1-C12 alkyl group which may be substituted;R represents, for example, a group represented by the following formula (II):wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group;R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

The invention discloses a method for synthesizing imatinib. The method comprises that: N-(4-methyl-3-3-aminophenyl)-4-(4-methyl-piperazinyl-1-methyl)-benzamide is used as a raw material, and reacts with 4-methyl-(3-pyridyl)-2-pyrimidone under actions of a polypeptide condensation agent and an organic alkali so as to generate the imatinib. The method has the advantages of mild reaction conditions, easy operation, high reaction yield and suitability for industrialized production.

Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

The present invention relates generally to antifugal compositions. In an embodiment, the antifungal compositions are effective for application to nails and surrounding skin, and comprise at least one volatile solvent, at least one film forming substance, and at least one pyrimidone derivative of formula I, such as albaconazole. These compositions are capable of treating an infection caused by fungi, such as onychomychosis.

The invention belongs to the technical field of medicines, and in particular relates to a compound taking thieno-pyrimidone as mother nuclide or a salt thereof, a preparation method and a combination of the compound and application of the compound used as a DPP-IV (dipeptidyl peptidase) inhibitor in preventing or treating diseases benefiting from the DPP-IV inhibition. The compound provided by the invention has the advantages that the preparation process is simple, the raw material is easily available, the compound is suitable for large-scale production, and in-vitro experiment verifies that the compound has good selective inhibition action on the DPP-IV, and hardly has any influence on the activities of DPP-VIII and DPP-IX while effectively inhibiting the activity of the DDP-IV, thereby predicting that the medicine prepared from the compound has very low toxicity and an outstanding advantage.

The present invention provides compositions comprising sucralose and 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one or salts, solvates, and / or esters thereof and methods of making the compositions by spray drying. The present invention also provides ingestible compositions comprising compositions of the present invention and methods of making such foods. The present invention also includes a process of preparing 2-amino-thiophene derivatives, which are key intermediates for preparing 4-amino-5,6-dimethylthieno[2,3-d]pyrimidine-2(1H)-one.

The invention discloses a carbamido pyrimidone modified gelatin injectable self-healing hydrogel and a preparation method thereof. The method comprises the following steps: by taking gelatin as a main chain of a hydrogel polymer, introducing nucleophilic reaction into a side chain and acquiring UPy modified gelatin through quadrupolar hydrogen bond crosslinked carbamido pyrimidone (UPy); and meanwhile, adding ferric ion into the prepared UPy modified gelatin and forming ionic crosslinking, on the basis of a large amount of carboxylic acid groups of the main chain of the gelatin, thereby preparing a multiple hydrogen bond ion interacting double-physical cross-linking hydrogel. The preparation method disclosed by the invention has the advantages of low-cost easily acquired raw materials, simple process, mild preparation condition, low cost and equipment requirements, easiness in scale production and practical application and excellent application prospect. The prepared double-physical cross-linking hydrogel has an excellent self-repairing property and is injectable.

The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

A compound having GSK-3 inhibitory activity. A1 and A3 are a single bond, an aliphatic hydrocarbon group; A2 and A4 are a single bond, CO, COO, CONR, O, OCO, NR, NRCO, NRCOO, etc.; G1 is a single bond, an aliphatic hydrocarbon, aromatic hydrocarbon, heterocyclic; G2 is H, an aliphatic hydrocarbon, an alicyclic hydrocarbon, an aromatic hydrocarbon, heterocyclic; A5 is a single bond, NR; R2 is H, halogen, an aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; A6 is a single bond, NR, CO, NRCO, NRCONR, CONR, COO, O, etc.; R3 is H, halogen, nitro, saturated aliphatic hydrocarbon, alicyclic hydrocarbon, aromatic hydrocarbon, heterocyclic; and R3 may be a trimethylsilyl, formyl, acyl, carboxyl, alkoxylcarbonyl, carbamoyl, alkylcarbamoyl, or cyano group when A6 is CR═CR or C≡C, wherein R is H or an lower aliphatic hydrocarbon group.

The invention discloses pyrimidopyrimidinones useful as Wee-1 kinase inhibitors. The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

The present invention discloses a class of pyrido[1,2-a]pyrimidone analogs as mTOR / PI3K inhibitors, and particularly relates to a compound represented by a formula (I) or a pharmaceutically acceptable salt thereof. The formula (I) is defined in the specification.

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

The present invention relates to novel pyrimidone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrimidone derivatives of the general formula (I) and a method thereof.

Compounds of formula (I), useful for inhibiting PIM-I and / or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.

A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein:R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group;R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted;or R1 and R2 form together a C2-6 alkylene group which may be substituted;or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted;R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; andR4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted.And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and / or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β such as Alzheimer's disease.

The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

The invention relates to the field of biodegradable macromolecule, and aims at providing a preparation method of biodegradable supermolecule polylactic acid microspheres. The method comprises the steps that 2-carbamido-4-[1H]-pyrimidone (UPy) end group modified polylactic acid is dissolved in good solvent, poor solvent is dropwise added under the stirring condition; after stirring continues to be conducted, centrifugal washing is conducted, and solid precipitates are collected; vacuum drying is conducted, and then the biodegradable supermolecule polylactic acid microspheres are obtained. Accordingly, the preparation method is simple and easy to implement, and the feasibility of implementation is high. The morphology of polymer microspheres is regulated through a method of combining liquid-liquid separation and polymer crystallization; meanwhile, the structure and performance are regulated, and the application range is extended. Raw materials of prepared materials all come from biomass renewable resources, can be completely degraded after use, are green and environmentally friendly and have good biocompatibility. Chemical-loading particles are prepared through a chemical and polymer coprecipitation method, use of emulsifier can be effectively avoided, and then the polymer nanoparticles or microspheres have a wider application prospect.