专利号:US-11897914-B2 优先权日:2021-11-29 标题 :Synthesis of 2′ protected nucleosides 发明人:POON WING C; ZOU RUIMING; LAU ALDRICH N K; YU DAVID; Du Gengyu; YAO YUN-CHIAO; ZHAO GANG 权利人:HONGENE BIOTECH CORP 摘要:Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.
专利号:US-2025091989-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)), 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-12006337-B2 优先权日:2018-05-30 标题:Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof 发明人:HOLTZMAN MICHAEL J; ROMERO ARTHUR G; GEROVAC BENJAMIN J; HAN ZHENFU; KEELER SHAMUS P; WU KANGYUN; ZHANG YONG 权利人:WASHINGTON UNIVERSITY ST LOUIS 摘要:Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutically for a variety of diseases, including cancer and respiratory diseases. Methods of synthesis of the compounds are also disclosed.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:US-5414097-A 优先权日:1991-12-13 标 题:Purification of esters of tetrahydro-pyran-4-carboxylic acid 发明人:FISCHER ROLF; GOETZ NORBERT; KUEKENHOEHNER THOMAS; RUST HARALD; SCHNURR WERNER 权利人:BASF AG 摘要:A process for purifying esters of tetrahydropyran-4-carboxylic acid of the formula I ##STR1## where R 1 to R 3 are each C 1 -C 4 -alkyl, and R 2 and R 3 are each additionally hydrogen, from mixtures produced in the reaction of butyrolactones of the formula II ##STR2## where R 2 and R 3 have the abovementioned meanings, and R 4 is hydrogen, alkyl of 1-6 carbons or acyl of the formula --CO--R 2 , with alcohols of the formula R 1 OH in the presence of oxide catalysts, by distillation, which entails n a) removing overhead, in a first column with 5-25 theoretical plates with a distillate pressure of 700-1100 mbar and a distillate temperature of 50°-80° C., an alcohol and up to 10% of the water, n b) transferring the bottom product from the first column into a second column with 18-40 theoretical plates, into which a water entrainer is metered between plates 15 and 30, and is circulated, and which operates with a distillate pressure of 35-350 mbar and a distillate temperature of 18°-70° C., with the esters of tetrahydropyran-4-carboxylic acid being removed between plates 8 and 18 at 90°-150° C., and, where appropriate, n c) feeding the bottom product from the second column into a third column with 5-25 theoretical plates, and returning the overhead products at a distillate pressure of 1-100 mbar and a distillate temperature of 90°-140° C. to the synthesis of the esters of tetrahydropyran-4-carboxylic acid.
专利号:US-2016319312-A1 优先权日:2013-07-29 标 题 :Synthesis method for l-cyclic alkyl amino acid and pharmaceutical composition having thereof 发明人:HONG HAO; ZHENG CHANGSHENG; GUO LINA 权利人:ASYMCHEM LABORATORIES (TIANJIN) CO LTD; ASYMCHEM LIFE SCIENCE (TIANJIN) CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LABORATORIES (FUXIN) CO LTD; JILIN ASYMCHEM LABORATORIES CO LTD 摘要:A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD + , and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is n n n n n n n n n n where n 1 ≧1, m 1 ≧0 and the M 1 is H or a monovalent cation; the Structural Formula (II) is n n n n n n n n n n where n 2 ≧0, m 2 ≧0, the M 2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.