945397-13-7

Upstream product

• 110-91-8 morpholine 
• 7087-27-6 1-fluoro-3-(methylsulfonyl)-5-nitrobenzene 
• 3819-88-3 1-fluoro-3-iodo-5-nitrobenzene 

Downstream Products

• 945397-18-2 3-(methylsulfonyl)-5-morpholinoaniline 

Relevant academic research and scientific papers

Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors

Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The JAK family consists of four highly homologous members: JAK1-3 and TYK2. The development of small-m

COMPOUND, COMPOUND FOR USE IN THE TREATMENT OF A PATHOLOGICAL CONDITION, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR PREPARING SAID COMPOUND

The invention concerns a compound, wherein the compound is a substance according to the following formula (I) wherein the ring A is a pyrrolidine, piperidine, morpholine, or imidazole residue or a substituted pyrrolidine, piperidine, morpholine, or imidaz

Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors

The receptor tyrosine kinase EPHA2 has gained attention as a therapeutic drug target for cancer and infectious diseases. However, EPHA2 research and EPHA2-based therapies have been hampered by the lack of selective small-molecule inhibitors. Herein we rep

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors

Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A bis-anilino pyrimidine PAK1 inhibitor was identified and optimized through structure-based drug design to improve PAK1 potency and achieve high kinase selectivity, giving in vitro probe compound AZ13705339 (18). Reduction of lipophilicity to lower clearance afforded AZ13711265 (14) as an in vivo probe compound with oral exposure in mouse. Such probes will allow further investigation of PAK1 biology.

INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS

Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same.

PYRIMIDINE DERIVATIVES

The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, ring A, n, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.

NOVEL PYRIMIDINE DERIVATIVES 698

The invention concerns compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.

Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines

Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent series of 3,5-disubstituted anilin