885698-74-8

Upstream product

• 927-68-4 bromoethyl acetate 
• 78818-15-2 4-benzyloxycarbonylpiperazin-2-one 

Downstream Products

• 955979-13-2 4-(2-hydroxy-ethyl)-3-oxo-piperazine-1-carboxylic acid benzyl ester 
• 1590403-75-0 C₂₄H₂₁F₄N₃O₄ 
• 1590411-01-0 C₃₂H₂₇F₄N₃O₆ 

Relevant academic research and scientific papers

THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS

Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

ANTI-FIBROTIC PYRIDINONES

This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.

ANTI-FIBROTIC PYRIDINONES

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

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.