On April 9, 2004, D’Orchymont, Hugues; Van Hijfte, Luc; Zimmermann, Andre published a patent.Reference of 4-Bromo-5-nitroisoquinoline The title of the patent was Preparation of indazolecarboxamides as CDK1, CDK2, and CDK4 inhibitors for treating CDK-related diseases, in particular cancer. And the patent contained the following:
Title compounds I [R1 = H, halo, NH2, NHR2, NHCOR2, NO2, CN, CH2NH2, CH2NHR2, (un)substituted Ph, heteroaryl; Ar = (un)substituted Ph, heteroaryl; R2 = Ph, heteroaryl, (un)substituted alkyl (substituent = Ph or heteroaryl); n = 0, 1, 2, or 3; PG = protecting group selected from trimethylsilylethoxymethyl, mesitylenesulfonyl; their free bases, addition salts with acids, solvates and hydrates; with the exclusion of certain compounds] were prepared as cyclin-dependent kinase (CDK)-1, CDK2, and CDK4 inhibitors for treating cdk-related diseases, in particular cancer. For instance, reacting indazole-3-carboxylic acid with N-phenyl-1,4-phenylenediamine in the presence of DCC gave 58% II. I displayed IC50 values < 20 μM for the inhibition of CDK2, CDK1, and CDK4 in a test for measuring the enzymic activity of CDK2/Cyclin A, CDK1/Cyclin B, and CDK4/Cyclin D1, resp. I are useful for treating cancers, autoimmune diseases, inflammations, cardiovascular diseases, viral and fungal infections, hematol. diseases, and degenerative diseases of muscular system. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Reference of 4-Bromo-5-nitroisoquinoline
The Article related to indazolecarboxamide preparation cdk1 cdk2 cdk4 inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 4-Bromo-5-nitroisoquinoline
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem