577 results about "Pyrimidone" patented technology

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.

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.

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.

This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.

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 invention provides 5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one compounds that are selective inhibitors of KDR and FGFR kinases, and are useful in the treatment of cancers. The compounds have the generic structure I

where Ar, Ar′, and R¹ are as set forth in the present specification. The invention also provides pharmaceutical compositions containing these compounds and methods for their use.

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.

The present invention relates to novel pyrimidones 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 novel pyrimidones of the general formula (I).

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.

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.

The present invention encompasses compounds of formula (I)

wherein the groups R¹ to R⁴, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

A pyrimidone derivative represented by formula (I) or a salt thereof:

• • Wherein:
  • R1 represents a hydrogen atom or a C_1-6 alkyl group which may be substituted by a C_6,10 aryl group;
  • R2 represents a C_1-10 alkyl group which may be substituted, a C_2-6 alkenyl group which may be substituted, a C_3-6 alkynyl group which may be substituted, a C_3-6 cycloalkyl group which may be substituted, or a C_6-10 ARYL group which may be substituted;
  • or R1 and R2 form together a C_2-6 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 C_1-4 alkyl group, C_1-4 alkoxy group or halogen atom; and
  • R4 represents a C_1-10 alkyl group optionally substituted by a hydroxyl group, amino, C_1-6 monoalkylamino group, C_2-12 dialkylamino group or C_6,10 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.

The invention discloses a telechelic quadruple-hydrogen bond unit compound and asynthesis method thereof, and relates to a compound and a synthesis method thereof. The telechelic quadruple-hydrogen bond unit compound is pentaerythritol-(polycaprolactone-carbamido pyrimidone)4. The synthesis method comprises the following steps: firstly synthesizing a intermediate coupling agent pentaerythritol-polycaprolactone, and then synthesizing quadruple-hydrogen bond unit carbamido pyrimidone, and finally synthesizing pentaerythritol-(polycaprolactone-carbamido pyrimidone)4. The polyester with low toxicity, biocompatibility and biodegradability is selected so that the pollution to the environment is small; the green chemistry requirement is satisfied; the total yield is improved, and the resource is saved; as compoared with a linear supermolecular structure, a network state supermolecular structure with higher mechanical property and mechanical strength is formed.

The invention is directed to Compounds of Formula I:

optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.

A preparation method of spandex fiber with the high resilience mainly comprises the following steps: (1) carrying out mixed reaction on raw materials including polytetramethylene ether glycol (PTMEG) and 4,4-methylene diphenyl diisocyanate (MDI) in a solvent for preparing isocyanate end-capped prepolymer; (2) preparing a special chain extender mixture solution, wherein the quantity of a UPy(2-carbamido-4[1H]-pyrimidone) type diamine compound in a chain extender accounts for 5-15 mol% of the total quantity; (3) stepwise adding the chain extender mixed solution into a prepolymer solution while stirring, and reacting to form a polyurethane urea solution; (4) spinning the polyurethane urea solution to prepare the spandex fiber with the high resilience. The preparation method of the spandex fiber with the high resilience, provided by the invention, meets the requirements on the high resilience of spandex in a plurality of application fields.

The invention relates to a high molecular thermoplastic elastomer technology, and aims to provide a polylactic acid/hydrogenated polybutadiene thermoplastic supramolecular elastomer and a preparation method thereof. The polylactic acid/hydrogenated polybutadiene thermoplastic supramolecular elastomer contains a PLA-PEB-PLA triblock copolymer containing a PLA block and a PEB block as a basic unit; and the terminal group of the basic unit is a 2-carbamido-4[1H]-pyrimidone group capable of forming quadruple hydrogen bonds. According to the high molecular thermoplastic elastomer technology, by adjusting the proportions of PLA and PEB, the intensity and the modulus of the elastomer are easy to adjust; because a UPy group is used as the structural unit, the elastomer is high in binding force and has reversibility; the prepared elastomer has better mechanical property; simultaneously, the elastomer also has the functions of memorizing shapes, self-repairing and the like; PLA is used as the hard section of the supramolecular elastomer; PLA can be prepared on the basis of renewable biomass resources and degraded after being used; and the polylactic acid/hydrogenated polybutadiene thermoplastic supramolecular elastomer is low in pollution to the environment, environmentally friendly and resource-saving.

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:

wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.