933751-05-4

Upstream product

• 74-89-5 methylamine 
• 45438-77-5 5-thiazolylmethyl chloride 
• 38585-74-9 thiazol-5-yl-methanol 
• 167998-61-0 5-(bromomethyl)thiazole 

Downstream Products

• 1169870-36-3 C₃₆H₄₅N₇O₅S₂ 

Relevant academic research and scientific papers

Thiazole alkyl pyridylamine compound and preparation method and application thereof

The present invention discloses a thiazole alkyl pyridylamine compound shown in formula (I) and a preparation method and application thereof, wherein R, R ', Z, R1 and R2 are as defined in the specification. The thiazole alkyl pyridylamine compound shown in formula (I) has bactericidal, acaricidal or herbicidal biologically activity, and has high activity on pathogenic bacteria such as sclerotinia sclerotiorum, botrytis cinerea pers, and the like.

Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)

The HIV protease inhibitor (PI) ritonavir (RTV) has been widely used as a pharmacoenhancer for other PIs, which are substrates of cytochrome P450 3A (CYP3A). However the potent anti-HIV activity of ritonavir may limit its use as a pharmacoenhancer with other classes of anti-HIV agents. Ritonavir is also associated with limitations such as poor physicochemical properties. To address these issues a series of compounds with replacements at the P2 and/or P3 region was designed and evaluated as novel CYP3A inhibitors. Through these efforts, a potent and selective inhibitor of CYP3A, GS-9350 (cobicistat) with improved physiochemical properties was discovered.

Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based cyclin-dependent kinase 4 inhibitors: synthesis, biological evaluation and structure-activity relationships

The design, synthesis, and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitors are described. In continuing our program aim to search for potent CDK4 inhibitors, the introduction of a thiazole group at the hydrazone part has led to marked enhancement of chemical stability. Furthermore, by focusing on the optimization at the C-4′ position of the thiazole ring and the C-6 position of the thieno[2,3-d]pyrimidine moiety, compound 35 has been identified with efficacy in a xenograft model of HCT116 cells. In this paper, the potency, selectivity profile, and structure-activity relationships of our synthetic compounds are discussed.

MODULATORS OF PHARMACOKINETIC PROPERTIES OF THERAPEUTICS

The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.