On July 21, 2011, Kallander, Lara S.; Lawhorn, Brian Griffin; Philip, Joanne; Zhao, Yongdong published a patent.Formula: C6H8N2O2S The title of the patent was 3-[(6-Aminopyrimidin-4-yl)amino]benzenesulfonamide compounds useful as TNNI3K inhibitors, their preparation, and methods of use in the treatment of congestive heart failure. And the patent contained the following:
Title compounds I are disclosed [wherein R1 = C1-4 alkyl; R2 = H, halo; R3 = H, halo, (un)substituted alkyl or alkoxy, aryl, OH, cycloalkyl, alkylthio, amino, (di)(alkyl)amino; R4 = H, halo, (un)substituted alkyl or alkoxy, OH, (halo)alkylthio, alkylsulfonyl, (un)substituted amino; R5 = H; or R4 and R5 form a 5 or 6 membered ring, optionally substituted or containing one or two addnl. N/O/S atoms; R6 = alky(en/yn)yl, cycloalkyl, (un)substituted (hetero)aryl; and salts]. I are inhibitors of cardiac troponin I-interacting kinase (TNNI3K), also known as CARK (for cardiac ankyrin repeat kinase), a protein kinase that exhibits highly selective expression for cardiac tissues and which has been shown to interact with components of the sarcomere, including troponin I. Approx. 380 compounds I are claimed as the free base, and were prepared as salts and/or free bases. Numerous intermediates were also prepared For instance, the intermediate 3-[(6-chloro-4-pyrimidinyl)amino]-N-methylbenznesulfonamide and 3-biphenylamine were microwaved together in isopropanol in the presence of concentrated HCl at 150° for 20 min to give invention compound II, isolated as the trifluoroacetate. In bioassays using human TNNI3K, I exhibited pXC50 ≥ approx. 6.0. For instance, two compounds I inhibited hTNNI3K with a mean pXC50 of approx. 7.0. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Formula: C6H8N2O2S
The Article related to pyrimidinylamino benzenesulfonamide preparation tnni3k inhibitor treatment congestive heart failure, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C6H8N2O2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica