885618-54-2

Usage

Uses

Used in Pharmaceutical Industry:
4-(2-Chloro-6-((4-Methylpiperazin-1-yl)Methyl)thieno[3,2-d]pyriMidin-4-yl)Morpholine is used as a potential pharmaceutical agent for its unique structural features that may allow it to interact with biological systems in novel ways. The presence of the morpholine ring and the 4-methylpiperazin-1-ylmethyl group could provide opportunities for the compound to target specific receptors or enzymes, potentially leading to the development of new therapeutics.
Used in Research Applications:
In the research field, 4-(2-Chloro-6-((4-Methylpiperazin-1-yl)Methyl)thieno[3,2-d]pyriMidin-4-yl)Morpholine can be utilized as a research tool to study the interactions of complex molecules with biological systems. Its unique structure may offer insights into the design of new drugs or the understanding of molecular recognition processes, contributing to the advancement of medicinal chemistry and drug discovery.

Upstream product

• 109-01-3 1-methyl-piperazine 
• 885618-31-5 2-chloro-4-morpholinothieno[3,2-d]pyrimidine-6-carbaldehyde 

Relevant academic research and scientific papers

Pharmaceutical compounds

Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1- ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110α. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer.

PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS

Thienopyrimidines of formula (Ia) or (Ib): wherein R1, R2, R3, are as defined in the claims.

PHARMACEUTICAL COMPOUNDS

Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; n is 1 or 2; R1 is a group of formula (II); wherein m is 0 or 1; R30 is H or C1-C6 alkyl; R4 and R5 form, together with the N atom to which they are attached, a 5- or 6-membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R4 and R5 is alkyl and the other is a 5- or 6-membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6-membered saturated N-containing heterocyclic group as defined above; R2 is selected from formula (a); wherein R6 and R7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and formula (b); wherein Y is a C2-C4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted; and R3 is an indazole group which is unsubstituted or substituted; and the pharmaceutically acceptable salt thereof have activity as inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.