75634-03-6

Upstream product

• 1193-21-1 4,6-dichloropyrimidine 
• 5720-06-9 2-Methoxyphenylboronic acid 

Downstream Products

• 1073484-78-2 C-(3-[6-(2-methoxy-phenyl)-pyrimidin-4-ylamino]-phenyl)-N-methyl-methanesulfonamide 
• 1073484-37-3 C-(3-[6-(2-methoxy-phenyl)-pyrimidin-4-ylamino]-phenyl)-N-propyl-methanesulfonamide 
• 848639-98-5 4-[6-(2-methoxy-phenyl)-pyrimidin-4-yl-amine]-benzoic acid 
• 1606169-13-4 ethyl (4-{[6-(2-methoxyphenyl)pyrimidin-4-yl]amino}phenyl)phenylphosphinate 
• 1606169-12-3 ethyl (4-{[6-(2-methoxyphenyl)pyrimidin-4-yl]amino}phenyl)propylphosphinate 
• 1606169-20-3 diethyl (3-{[6-(2-methoxyphenyl)pyrimidin-4-yl]amino}phenyl)phosphonate 

Relevant academic research and scientific papers

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.

Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity

The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50??6?μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity.

NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS

Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.

Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor

Background and Purpose The cyclin-dependent kinase CDK9 is an important therapeutic target but currently available inhibitors exhibit low specificity and/or narrow therapeutic windows. Here we have used a new highly specific CDK9 inhibitor, LDC000067 to interrogate gene control mechanisms mediated by CDK9. Experimental Approach The selectivity of LDC000067 was established in functional kinase assays. Functions of CDK9 in gene expression were assessed with in vitro transcription experiments, single gene analyses and genome-wide expression profiling. Cultures of mouse embryonic stem cells, HeLa cells, several cancer cell lines, along with cells from patients with acute myelogenous leukaemia were also used to investigate cellular responses to LDC000067. Key Results The selectivity of LDC000067 for CDK9 over other CDKs exceeded that of the known inhibitors flavopiridol and DRB. LDC000067 inhibited in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrated a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis. Analysis of de novo RNA synthesis suggested a wide ranging positive role of CDK9. At the molecular and cellular level, LDC000067 reproduced effects characteristic of CDK9 inhibition such as enhanced pausing of RNA polymerase II on genes and, most importantly, induction of apoptosis in cancer cells. Conclusions and Implications Our study provides a framework for the mechanistic understanding of cellular responses to CDK9 inhibition. LDC000067 represents a promising lead for the development of clinically useful, highly specific CDK9 inhibitors.

INHIBITORS OF PROTEIN KINASES

The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I).

INHIBITORS OF PROTEIN KINASES

Compounds of general Formula I, wherein R1, R2, R3, x, A and Ra are as defined herein are inhibitors of cyclin-dependent kinases and are useful for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

Inhibitors of protein kinases

The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceutical compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

INHIBITORS OF PROTEIN KINASES

The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I).

4, 6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES

The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.

ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES

The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.