164658-40-6

Upstream product

• 108-42-9 3-chloro-aniline 
• 164658-38-2 1-(2-chloropyridin-4-yl)-3-(dimethylamino)prop-2-en-1-one 
• 6145-41-1 3-chlorophenylguanidine 
• 164658-41-7 N-(3-chloro-phenyl)-4-(N-oxido-pyridin-4-yl)-2-pyrimidineamine 
• 38647-81-3 (3-Chlorophenyl)guanidine nitrate 

Downstream Products

• 164658-61-1 [4-(2-amino-pyridin-4-yl)-pyrimidin-2-yl]-(3-chloro-phenyl)-amine 
• 442162-43-8 1-{4-[2-(3-Chloro-phenylamino)-pyrimidin-4-yl]-pyridin-2-yl}-pyrrolidin-2-one 
• 442161-45-7 3-{4-[2-(3-chloro-phenylamino)-pyrimidin-4-yl]-pyridin-2-yl}-4-methyl-oxazolidin-2-one 
• 164658-13-3 N-(3-chloro-phenyl)-4-[2-(3-hydroxy-propyl-amino)-pyridin-4-yl]-2-pyrimidineamine 
• 1082008-29-4 4-{2-[(3-chlorophenyl)amino]pyrimidin-4-yl}-N-[3-(2-oxoazepan-1-yl)propyl]pyridine-2-carboxamide 

Relevant academic research and scientific papers

Identification of pyrimidine derivatives as hSMG-1 inhibitors

hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound.

Pharmacologically active pyridine derivatives and processes for the preparation thereof

N-phenyl-2-pyrimidineamine derivatives of formula I STR1 wherein the substituents are as defined in claim 1 and the derivatives of formula I can be used, for example, in the treatment of tumour diseases.

Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof

Described are N-phenyl-2-pyrimidineamine derivatives of formula I STR1 wherein R1 is a substituted cyclic radical, the cyclic radical being bonded at a ring carbon atom in each case and being selected from phenyl, pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, --C(=O)--OR3, --C(=O)--R4, --SO2 --N(R5)--R6, --N(R7)--R8, --OR9 and fluorine-substituted lower alkyl, wherein R3, R4, R5, R6, R7, R8 and R9 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino; and R2 is selected from halogen, cyano, carbamoyl, --C(=O)--OR10, --C(=O)--R11, --SO2 --N(R12)--R13, --N(R14)--R15, --OR16 and fluorine-substituted lower alkyl, wherein R10, R11, R12, R13, R14, R15 and R16 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino. Those compounds can be used, for example, in the treatment of tumour diseases.