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:WO-2015014261-A1 优先权日:2013-07-30 标 题:Macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof 发明人:SHEN SHUNYI; CHEN DAIJIE; GE HAN; ZHANG ZHIHONG; REN YANSONG; LI ZHONGLEI; FAN QIANYONG; ZHANG YUN; XU YIJUN; LI DAN; LI JIAN 权利人:SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY; CHINA STATE INST PHARM IND 摘要:The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.
专利号:US-7321044-B2 优先权日:2001-10-12 标题 :Synthesis of oxygen-substituted benzocycloheptenes as valuable intermediate products for the production of tissue-selective estrogens 发明人:PLATZEK JOHANNES; BECKMANN WOLFGANG; GEISLER JENS; KIRSTEIN HOLGER; NIEDBALLA ULRICH; OTTOW ECKHARD; RADAU SIGMAR; SCHULZ CLAUDIA; WESSA THOMAS 权利人:SCHERING AG 摘要:The invention relates to intermediate products and a new process for the production of benzocycloheptene C. n n n n n n n n n n The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.
专利号:US-6046325-A 优先权日:1998-09-11 标 题:Chemical synthesis of 1,4-oxazin-2-ones 发明人:ASHWOOD MICHAEL STEWART; BISHOP BRIAN CHRISTOPHER; COTTRELL IAN FRANK 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R 1 is a C 1-6 alkyl or arylC 1-4 alkyl group; and R 2 is a hydrogen atom, a halogen atom, or a group selected from C 1-6 alkyl, CF 3 or C 1-6 alkoxy substituted by C 1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.
专利号:US-7358367-B2 优先权日:2002-09-27 标题:Present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-9a-aza9a-homoerythromycin a 9a, 11-cyclic carbamates 发明人:FAJDETIC ANDREA; KOBREHEL GABRIJELA; LAZAREVSKI GORJANA; MUTAK STJEPAN 权利人:GLAXOSMITHKLINE ZAGREB 摘要:The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R 1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C 1 -C 6 alkyl group, C 2 -C 6 alkenyl group or X individually stands for C 1 -C 6 alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH 2 ) n —Ar or X individually stands for (CH 2 ) n -heterocycloalkyl, wherein (CH 2 ) n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C 1 -C 3 dialkyl, CN, SO 2 NH 2 , C 1 -C 3 alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C 1 -C 3 dialkyl, CN, SO 2 NH 2 , C 1 C 3 alkil, —C(O)—, COOH or R 1 together with R 2 stands for ketone, R 2 individually stands for hydrogen or together with R 1 stands for ketone or together with R 3 stands for ether, R 3 individually stands for hydroxyl, a group of the formula —OX or together with R 2 stands for ether, R 4 individually stands for hydrogen, C 1 -C 4 alkyl group or C 2 -C 4 alkenyl group, and R 5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections
专利号:US-4334079-A 优先权日:1980-11-03 标 题:Synthesis of substituted benzyl esters 发明人:GREENE JAMES M; BUNNELL CHARLES A 权利人:LILLY CO ELI 摘要:A process for preparing certain substituted benzyl esters of phenylacetic acids by esterification in a solvent in which the salt of the acid is insoluble, and in the presence of a phase transfer catalyst.
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合成参考文献
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