New Pyrimidine Chemical Compounds for Treating Tumors

This patent describes specific new chemical compounds, called N-phenyl-2-pyrimidine-amine derivatives, designed with precise molecular structures for potential use in treating cancer.

What it covers

This patent claims a specific group of N-phenyl-2-pyrimidine-amine chemical compounds, identified by a general chemical structure called Formula I. The claims precisely define various parts of this molecule, known as 'R' groups (R1 through R10), along with X, Y, and n. For example, R1 can be 4-pyrazinyl or 1-methyl-1H-pyrrolyl, and R2 and R3 are hydrogen or lower alkyl. Crucially, one or two of the R4-R8 positions must include a nitro group, a fluoro-substituted lower alkoxy group, or a specific radical of Formula II, which itself has detailed definitions for R9, X, Y, n, and R10. The patent abstract states these compounds can be used in the therapy of tumoral diseases. An example compound would have R1 as 4-pyrazinyl, R2 and R3 as hydrogen, and one of R4-R8 as a radical of Formula II where R10 is an aliphatic radical with at least 5 carbon atoms.

What it doesn't cover

• —Does not cover pyrimidine derivatives that do not match the exact N-phenyl-2-pyrimidine-amine core structure of Formula I.
• —Does not cover compounds where the R1 substituent is not one of the specifically listed groups, such as 4-pyrazinyl or 1-methyl-1H-pyrrolyl.
• —Does not cover compounds where the R10 radical in Formula II has fewer than 5 carbon atoms if it is an aliphatic radical.
• —Does not cover compounds where the R4-R8 substituents do not include at least one of the specified nitro, fluoro-substituted lower alkoxy, or Formula II radicals.
• —Does not cover compounds where the R10 radical is an aromatic-aliphatic radical but the phenyl portion is substituted differently than described in claim 3.

The clever bit

The novelty lies in the specific combination of chemical groups attached to the N-phenyl-2-pyrimidine-amine core, particularly the detailed definitions for R1 and the specific requirements for at least one of the R4-R8 positions, which together yield compounds with therapeutic potential for tumors.

Why it matters

This patent is foundational in pharmaceutical chemistry, defining a class of compounds with potential anti-tumor activity. It represents early work by Ciba Geigy, a company that later became part of Novartis, a major player in oncology. Such patents are critical for establishing intellectual property around new drug candidates, guiding further research and development in cancer treatment.

Real-world examples

• 1.Imatinib (Gleevec) - a pyrimidine derivative developed by Novartis for treating certain cancers.
• 2.Other tyrosine kinase inhibitors used in oncology.
• 3.Early-stage drug candidates targeting specific tumor pathways.