1121633-45-1

Upstream product

• 1215787-31-7 6-bromo-4-chloropyrido[2,3-d]pyrimidine 
• 155690-79-2 6-bromo-3H,4H-pyrido[2,3-d]pyrimidin-4-one 
• 52833-94-0 2-amino-5-bromonicotinicacid 
• 1093963-85-9 2-amino-6-(methylthio)nicotinonitrile 
• 1350452-24-2 2-amino-6-(methylthio)-4-(trimethylsilyl)nicotinonitrile 
• 1508-07-2 1,1-dicyanopropene 
• 1350452-23-1 2-(1-(trimethylsilyl)ethylidene)malononitrile 
• 709652-82-4 2-amino-5-bromonicotinonitrile 
• 122-51-0 orthoformic acid triethyl ester 

Downstream Products

• 1215787-31-7 6-bromo-4-chloropyrido[2,3-d]pyrimidine 
• 155690-79-2 6-bromo-3H,4H-pyrido[2,3-d]pyrimidin-4-one 
• 1594729-05-1 6-(3-chlorophenyl)pyrido[2,3-d]pyrimidin-4-amine 

Relevant academic research and scientific papers

Modular assembly of purine-like bisphosphonates as inhibitors of hiv-1 reverse transcriptase

Bisphosphonates can mimic the pyrophosphate leaving group of the nucleotidyl transfer reaction and effectively inhibit RNA/DNA polymerases. In a search of HIV-1 reverse transcriptase (RT) inhibitors, a new chemotype of nonhydrolyzable purine diphosphate mimic was synthesized. A modular synthetic protocol was developed, utilizing 2-amino-6-(methylthio)-4-(trimethylsilyl)nicotinonitrile as the key synthon in the preparation of highly substituted 2-aminonicotinonitriles. These building blocks were subsequently elaborated to the pyrido[2,3-d]pyrimidine bisphosphonates (PYPY-BPs). Biochemical screening identified analogs of PYPY-BPs that inhibit HIV-1 RT-catalyzed DNA synthesis.

SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE

The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.

2,3-DISUBSTITUTED PYRIDINE COMPOUNDS AS TGF-BETA INHIBITORS AND METHODS OF USE

The invention described herein comprises compounds of formula (IV) and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds (IV) inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin.

Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach

DRAK2 emerged as a promising drug target for the treatment of autoimmune diseases and to prevent graft rejection after organ transplantation. Screening of a compound library in a DRAK2 binding assay led to the identification of an isothiazolo[5,4-b]pyridine derivative as a novel ligand for DRAK2, displaying a Kdvalue of 1.6 μM. Subsequent medicinal chemistry work led to the discovery of a thieno[2,3-b]pyridine derivative with strong DRAK2 binding affinity (Kd= 9 nM). Moreover, this compound also behaves as a functional inhibitor of DRAK2 enzymatic activity, displaying an IC50value of 0.82 μM, although lacking selectivity, when tested against DRAK1. This paper describes for the first time functionally active dual DRAK1 and DRAK2 inhibitors that can be used as starting point for the synthesis of chemical tool compounds to study DRAK1 and DRAK2 biology, or they can be considered as hit compounds for hit-to-lead optimization campaigns in drug discovery programs.