Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于盐酸体系中,化学反应生成2-氯噻唑 参考文献:Schatzmann,Justus Liebigs Annalen Der Chemie,1891,Vol. 261,P. 19 标题:Schatzmann,Justus Liebigs Annalen Der Chemie,1891,Vol. 261,P. 19
专利信息
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:WO-2023086801-A1 优先权日:2021-11-09 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; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 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:WO-2011095125-A1 优先权日:2010-02-02 标 题:Synthesis methods and purification methods of dasatinib 发明人:YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG 权利人:NAN JING CAVENDISH BIO ENGINEERING TECHNOLOGY CO LTD; YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG 摘要:Synthesis methods of dasatinib are provided, which comprise the following steps: reacting a compound of formula I with a compound of formula II to obtain a compound of formula III, and then connecting the compound of formula III with 2-chloro-6-methylaniline and 1-(2-hydroxyethyl)piperazine in any order to give dasatinib. Furthermore, purification methods of dasatinib are also provided.
专利号:US-9108954-B2 优先权日:2010-02-02 标 题:Synthesis process of dasatinib and intermediate thereof 发明人:YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG 权利人:YAN RONG; YANG HAO; HOU WEN; XU YONGXIANG; NAN JING CAVENDISH BIO ENGINEERING TECHNOLOGY CO LTD 摘要:Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-3839346-A 优先权日:1972-12-18 标 题:N-substituted pyridone and general method for preparing pyridones 发明人:GADEKAR S 权利人:AFFILIATED MED RES 摘要:1. A PROCESS FOR THE SYNTHESIS OF PYRIDONES OF THE FORMULA 1-A,2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE WHEREIN A IS AN AROMATIC RADICAL SELECTED FROM THE GROUP CONSISTING OF PHENYL, TOLYL, CHLOROPHENYL, TRIFLUOROMETHYLPHENYL, NAPHTHYL, PYRIDYL, FURYL, THIENYL, THIAZOLYL, PYRIMIDYL, QUINOLYL, IMIDAZOLYL; UP TO TWO OF THE TERMS R3, R4, R5 AND R6 ARE INDIVIDUALLY EACH HYDROGEN OR ALKYL UP TO 6 CARBON ATOMS, ARYL OR SUBSTITUTED ARYL RADICALS WHICH CONSISTS ESSENTIALLY OF THE STEPS OF REACTING A PYRIDONE OF THE FORMULA 2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE, OR ITS TAUTOMER, 2-(HO-),3-R3,4-R4,5-R5,6-R6-PYRIDINE IN WHICH R3, R4, R5 AND R6 ARE SET FORTH ABOVE, WITH A HALOGENATED COMPOUND OF THE FORMULA AX, WHEREIN X IS EITHER CHLORINE, BROMINE OR IODINE, AT TEMPERATURES RANGING BETWEEN THE MELTING POINT AND BOILING POINT OF SAID HALOGENATED COMPOUND, IN THE PRESENCE OF AN ALKALI METAL CARBONATE AND FINELY DIVIDED METALLIC COPPER.
[参考文献]: Dhiraj Patil, Et Al. Implication Of Novel Thiazolo-Thiophene Derivative (Mcd-Kv-10) For Management Of Asthma. J Enzyme Inhib Med Chem. 2015 Apr;30(2):229-39.
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 448. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 340. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 338. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 341. 摘要:Scholz, U.; Dong, W.; Feng, J.; Shi, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 93.