1026029-33-3

Upstream product

• 3934-20-1 2,6-Dichloropyrimidine 
• 99768-12-4 4-methoxycarbonylphenylboronic acid 

Downstream Products

• 1026029-57-1 C₁₇H₁₄N₄O₂ 
• 1026029-53-7 C₁₇H₁₅N₅O₂ 
• 1026029-73-1 C₁₈H₁₄ClN₃O₂ 
• 1236002-82-6 methyl 4-(2-(4-methylpyridin-2-ylamino)pyrimidin-4-yl)benzoate 
• 1236002-85-9 methyl 4-(2-(5-ethyl-1,3,4-thiadiazol-2-ylamino)pyrimidine-4-yl)benzoate 
• 1236002-94-0 methyl 4-(2-(1-benzyl-1H-benzo[d]imidazol-2-ylamino)pyrimidin-4-yl)benzoate 
• 1619927-67-1 N-(cyano(d₂-methyl))-4-(2-(4-(2',2',6',6'-d₄-morpholino)phenylamino)pyrimidin-4-yl)benzamide 
• 1619927-66-0 N-(cyanomethyl)-4-(2-(4-(2', 2', 6', 6'-d₄-morpholino) phenylamino) pyrimidin-4-yl) benzamide 
• 1619927-65-9 N-(cyano(d₂-methyl))-4-(2-(4-(3',3',5',5'-d₄-morpholino)phenylamino)pyrimidin-4-yl)benzamide 
• 1619927-64-8 N-(cyanomethyl)-4-(2-(4-(3',3',5',5'-d₄-morpholino)phenylamino)pyrimidin-4-yl)benzamide 
• 945749-71-3 4-(2-(4-(morpholinophenyl)amino)pyrimidin-4-yl)benzoic acid 
• 1619927-63-7 N-(cyano(d₂-methyl))-4-(2-(4-(morpholinophenyl)amino)pyrimidin-4-yl)benzamide 
• 1056634-68-4 Momelotinib 
• 1619927-69-3 N-(cyano(d₂-methyl))-4-(2-(4-(d₈-morpholino)phenylamino)pyrimidin-4-yl)benzamide 

Relevant academic research and scientific papers

Preparation method of JAK inhibitor momelotinib

The invention relates to a preparation method of a JAK inhibitor momelotinib. The preparation method provided by the invention has the advantages of simple preparation route, mild preparation conditions, cheap and easily available raw materials and relatively low synthesis cost.

Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections

Clinically, leukemia patients often suffer from the limited efficacy of chemotherapy and high risks of infection by invasive fungal pathogens. Herein, a novel therapeutic strategy was developed in which a small molecule can simultaneously treat leukemia and invasive fungal infections (IFIs). Novel Janus kinase 2 (JAK2) and histone deacetylase (HDAC) dual inhibitors were identified to possess potent anti-proliferative activity toward hematological cell lines and excellent synergistic effects with fluconazole to treat resistant Candida albicans infections. In particular, compound 20a, a highly active and selective JAK2/HDAC6 dual inhibitor, showed excellent in vivo antitumor efficacy in several acute myeloid leukemia (AML) models and synergized with fluconazole for the treatment of resistant C. albicans infections. This study highlights the therapeutic potential of JAK2/HDAC dual inhibitors in treating AML and IFIs and provides an efficient strategy for multitargeting drug discovery.

DEUTERATED PHENYL AMINO PYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention relates to a deuterated phenyl amino pyrimidine compound and pharmaceutical composition containing the same. Specifically provided are a deuterated phenyl amino pyrimidine compound as represented by formula (I), and pharmaceutical composition containing the compound, or polymorph, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound of the present invention can treat and/or prevent JAK kinase-related diseases, such as bone marrow proliferative disease, cancer, immunologic diseases and the like.

PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines

4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many drug-like molecules and biologically active compounds. A method for the quick assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald-Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. This method's convenience and practicality is demonstrated through the preparation of several novel non-nucleoside reverse transcriptase inhibitor (NNRTI) analogues.

Pyrimidine-based inhibitors of CaMKIIδ

Non-ATP competitive pyrimidine-based inhibitors of CaMKIIδ were identified. Computational studies were enlisted to predict the probable mode of binding. The results of the computational studies led to the design of ATP competitive inhibitors with optimized hinge interactions. Inhibitors of this class possessed improved enzyme and cellular activity compared to early leads.