Invention for 4,6 pyrimidinyl derivatives and their uses

Invented by Nathanael S. Gray, Tinghu Zhang, Dana Farber Cancer Institute Inc

The market for 4,6 pyrimidinyl derivatives and their uses has been steadily growing in recent years. These derivatives, which are chemical compounds derived from the pyrimidine molecule, have found a wide range of applications in various industries, including pharmaceuticals, agriculture, and materials science. One of the primary uses of 4,6 pyrimidinyl derivatives is in the field of pharmaceuticals. These compounds have shown promising potential as therapeutic agents for the treatment of various diseases and conditions. For example, some derivatives have exhibited anti-cancer properties, making them potential candidates for developing novel cancer treatments. Others have shown efficacy in treating neurological disorders, such as Alzheimer’s disease and Parkinson’s disease. The versatility of these derivatives in targeting different biological pathways makes them attractive for drug discovery and development. In the agricultural sector, 4,6 pyrimidinyl derivatives have gained attention for their potential use as crop protection agents. These compounds have shown insecticidal and fungicidal properties, making them valuable tools for farmers in protecting their crops from pests and diseases. Additionally, some derivatives have demonstrated herbicidal activity, which can be utilized to control weed growth in agricultural fields. The demand for effective and sustainable agricultural solutions has contributed to the growing market for these derivatives in the agrochemical industry. Furthermore, 4,6 pyrimidinyl derivatives have found applications in materials science. These compounds possess unique properties that make them suitable for various material applications. For instance, some derivatives have been used as dyes and pigments, providing vibrant colors and high stability to different materials, including textiles, plastics, and coatings. Additionally, their ability to form complex structures has made them useful in the development of advanced materials, such as organic semiconductors and liquid crystals, which have applications in electronics and display technologies. The market for 4,6 pyrimidinyl derivatives is expected to continue its growth trajectory in the coming years. The increasing demand for innovative pharmaceuticals, sustainable agricultural solutions, and advanced materials is driving the research and development efforts in this field. Moreover, advancements in synthetic chemistry and molecular modeling techniques are facilitating the discovery and design of new derivatives with enhanced properties and targeted functionalities. However, it is important to note that the development and commercialization of 4,6 pyrimidinyl derivatives face certain challenges. The complex synthesis routes and the need for rigorous safety and efficacy testing pose obstacles to their large-scale production and regulatory approval. Additionally, the competitive landscape in the pharmaceutical and agrochemical industries requires continuous innovation and differentiation to succeed in the market. In conclusion, the market for 4,6 pyrimidinyl derivatives and their uses is expanding across various industries. These compounds offer a wide range of applications in pharmaceuticals, agriculture, and materials science, making them valuable tools for addressing societal challenges. As research and development efforts continue, the market is expected to witness further growth, driven by the demand for novel therapeutics, sustainable agricultural solutions, and advanced materials.

The Dana Farber Cancer Institute Inc invention works as follows

The present invention provides novel compounds (Formula (I), as well as pharmaceutically acceptable salts (solvates, hydrates), polymorphs (co-crystals), tautomers (stereoisomers), isotopically labelled derivatives (prodrugs), and compositions of these compounds. The invention also includes kits and methods that use the compounds or compositions to treat or prevent proliferative disease (e.g. cancers such as lung cancer, breast carcinoma, leukemia lymphoma melanoma multiple myeloma brain cancer neuroblastoma), benign tumors, angiogenesis and autoinflammatory and inflammatory diseases in a patient. The treatment of a proliferative disorder in a subject using a composition or compound of the invention can inhibit the aberrant activities of a kinase, such as. a protein kinase (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase(PIP4K) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g., PI5P4K?, PI5P4K?, or PI5P4K?)) In the subject.

Background for 4,6 pyrimidinyl derivatives and their uses


Other Definitions


Pharmaceutical compositions, kits, and administration

Methods and Uses for Treatment


Synthesis of the Compounds”.

Example 1. The synthesis of (E)-N-(3-((6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide

5-bromo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (Compound 1)

1-(phenylsulfonyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrrolo[2,3-b]pyridine (Compound 2)

5-(6-chloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (Compound 3)

N1-(6-(1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)benzene-1,3-diamine (Compound 4)

4-nitro-N-(3-((6-(1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)amino)phenyl)benzamide (Compound 5)

4-amino-N-(3-((6-(1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)amino)phenyl)benzamide (Compound 6)

(E)-4-(4-(dimethylamino)but-2-enamido)-N-(3-((6-(1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)amino)phenyl)benzamide (Compound 7)

(E)-N-(3-((6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide (Compound 8)

Example 2. “Example 2.





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