423183-88-4

Upstream product

• 56-05-3 2-Amino-4,6-dichloropyrimidine 
• 1765-93-1 4-fluoroboronic acid 
• 98305-74-9 2-amino-6-(4'-fluorophenyl)-pyrimidin-4-ol 
• 1999-00-4 ethyl 3-(4'-fluorophenyl)-3-oxopropionate 

Relevant academic research and scientific papers

Synthesis and Investigation of Phthalazinones as Antitubercular Agents

A series of 2- and 7-substituted phthalazinones was synthesised and their potential as anti-tubercular drugs assessed via Mycobacterium tuberculosis (mc26230) growth inhibition assays. All phthalazinones tested showed growth inhibitory activity (MIC 100 μm), and those compounds containing lipophilic and electron-withdrawing groups generally exhibited better anti-tubercular activity. Several lead compounds were identified, including 7-((2-amino-6-(4-fluorophenyl)pyrimidin-4-yl)amino)-2-heptylphthalazin-1(2H)-one (MIC=1.6 μm), 4-tertbutylphthalazin-2(1H)-one (MIC=3 μm), and 7-nitro-phthalazin-1(2H)-one (MIC=3 μm). Mode of action studies indicated that selected pyrimidinyl-phthalazinones may interfere with NADH oxidation, however, the mode of action of the lead compound is independent of this enzyme. MIC=minimum inhibitory concentration.

TRIAZOLE COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONISTS

Described herein are triazole compounds of Formula (I): and pharmaceutically acceptable salts thereof. Methods of making and using compounds of Formula (I) are also described. Compounds of Formula (I) and pharmaceutically acceptable salts thereof can be useful as adenosine receptor antagonists, for example in the treatment of diseases or conditions mediated by the adenosine receptor, such as cancer, movement disorders, or attention disorders.

Aminopyrimidine compound and preparation method and application thereof

The invention relates to an aminopyrimidine compound and a preparation method and application thereof, in particular to an aminopyrimidine compound shown as a formula (I) or pharmaceutically acceptable salts thereof, a stereoisomer, a tautomer, a polymorph, a solvate, an N-oxide, an isotope labeled compound, a metabolite or a prodrug, a pharmaceutical composition containing the compound, a preparation method of the compound and application of the compound to prevention or treatment of adenosine A2a receptor related diseases.

TRIAZOLO-PYRIMIDINE COMPOUNDS AND USES THEREOF

The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.

ADENOSINE RECEPTOR BINDING COMPOUNDS

The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.

Triazolopyrimidine derivative, preparation method thereof, and application thereof in medicines

The invention relates to a triazolopyrimidine derivative, a preparation method thereof, and an application thereof in medicines. In particular, the invention relates to the triazolopyrimidine derivative represented as the general formula (I), a preparation method thereof, a medicine composition containing the derivative, and an application of the derivative as a treatment agent, especially an application as an A2a receptor antagonist, and an application in preparation of a medicine for relieving symptoms and diseases by inhibiting the A2a receptor; wherein the substituent groups in the generalformula (I) are defined as the specification.

HETEROARYL[4,3-C]PYRIMIDINE-5-AMINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF

A heteroaryl[4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and medical uses thereof. Specifically, a heteroarylo[4,3-c]pyrimidin-5-amine derivative represented by a general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and uses thereof as therapeutic agents, in particular, a use as a A2a receptor antagonist and A use in preparation of a medicament for treatment of conditions or symptoms that are ameliorated by inhibiting the A2a receptor; various substituent groups in the general formula (I) have the identical meanings as those in the specification.

NOVEL PYRIMIDINE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM

The present invention provides new heterocyclic compounds, particularly substituted pyrimidines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.

PYRIMIDINE DERIVATIVES FOR TREATMENT OF HYPERPROLIFERATIVE DISORDERS

Pyrimidine derivatives of formula (I) in which J and Y represent aromatic or heteroaromatic rings; R2, G, G', and G" represent substituent groups and R2a represents H or halogen; L represents a linking group; and M represents CH or N. Pharmaceutical compositions containing these compounds, and methods of using these compounds in treatment of hyperproliferative diseases such as cancer are also disclosed and claimed.

HETEROARYLOXY-SUBSTITUTED PHENYLAMINOPYRIMIDINES AS RHO-KINASE INHIBITORS

The invention relates to heteroaryloxy-substituted phenylaminopyrimidines, to methods for the production thereof, and to the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular diseases. The inventive compounds inhibit Rho-kinase.