专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2005100968-A1 优先权日:2000-02-23 标题 :Self-encoded combinatorial synthesis of compound multiplets 发明人:GALLOP MARK A; DOWER WILLIAM J; BARRETT RON W 权利人:XENOPORT INC 摘要:The present invention provides a variety of methods for synthesizing, encoding and decoding compounds in a combinatorial library. One step or cycle in the synthetic methods of the invention is a self-encoding step in which different pairs of components, each pair with a known and different molecular weight difference, are reacted with supports, whereby two compounds differing in molecular weight are formed on each support. The molecular weight difference between the two compounds on the support encodes for a particular component pair. Libraries of compounds formed according to the methods of the invention are also provided.
专利号:US-10807953-B2 优先权日:2015-03-02 标题:Processes and intermediates for the preparation of Pimavanserin 发明人:BILJAN TOMISLAV; DOGAN JASNA; METSGER LEONID; PIPERCIC SARA MORASI; RATKAJ MARINA; SKUGOR MAJA MATANOVIC; WANG YI 权利人:PLIVA HRVATSKA D O O 摘要:The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
专利号:US-7741492-B2 优先权日:2005-02-28 标题:Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate 发明人:HUGUET CLOTET JOAN; DALMASES BARJOAN PERE 权利人:INKE SA 摘要:It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).
专利号:US-2023046065-A1 优先权日:2019-11-25 标题 :MERGING C(sp3)-H ACTIVATION WITH DNA-ENCODING 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Palladium-catalyzed C(sp3)—H arylation of aliphatic carboxylic acids, amides and ketones with BNA-encoded aryl iodides in water is disclosed, Furthermore, sequential C—H arylation chemistry enabled the on-DNA synthesis of structurally-diverse scaffolds containing enriched C(sp3) character, chiral centers, cyclopropane, cyclobutane, and heterocycles. That new chemistry permits preparation of a DNA—encoded library (BEL) technology that can dramatically expedite hit identification in drug discovery owing to its ability to perform protein affinity selection with millions or billions of molecules in a single experiment. The sequential functionalization of multiple C—H bonds provides an unique avenue for creating diversity and complexity from simple starting materials. The use of water as solvent, the presence of DMA, and the extremely low concentration of DMA-encoded coupling partners (0.001 M) have previously hampered the development DMA-encoded C(sp3)—H activation reactions, but many of those hurdles have now been overcome.
专利号:EP-1259823-A2 优先权日:2000-02-23 标题 :Self-encoded combinatorial synthesis of compound multiplets
参考文献:10.1007/s10847-025-01278-0 摘要:Liu J, Ye X, Chen L, Jia A, Zhang Q. The biological activity of tetrakis(benzoxazine) calix[4]resorcinarenes and as a host for small molecules. J Incl Phenom Macrocycl Chem. 2025 Feb 01;105(5-6):349–62. doi: 10.1007/s10847-025-01278-0.