专利号:US-10654862-B2 优先权日:2015-03-18 标题 :Methods for the chemical synthesis of pyrrole-linked bivalent compounds, and compositions thereof 发明人:CRAN JOHN 权利人:AVEKSHAN LLC 摘要:The present invention in various aspects relates to the synthesis of pyrrole-linked bivalent compounds, including but not limited to norBNI, as well as pharmaceutical compositions comprising the same.
专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-2005272934-A1 优先权日:2004-06-01 标题 :Process for the synthesis of thalidomide 发明人:ALPEGIANI MARCO; MAZZONI ANDREA; VERGANI DOMENICO; CABRI WALTER 权利人:ANTIBIOTICOS SPA 摘要:The invention relates to a process for the preparation of thalidomide (I) n n ncomprising the reaction between glutamine (II) n nand a phthaloylating agent, preferably phthalic anhydride, to give N-phthaloyl-glutamine, which is directly transformed in thalidomide.
专利号:US-9303014-B2 优先权日:2013-05-01 标题:Synthesis of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione 发明人:RUCHELMAN ALEXANDER L; COHEN BENJAMIN M; CHOUDHURY ANUSUYA; KREILEIN MATTHEW M; LEONG WILLIAM W; MAN HON-WAH 权利人:CELGENE CORP 摘要:Provided herein are processes for the preparation of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt thereof.
专利号:UA-45408-C2 优先权日:1997-02-01 标 题 :Substituted piperidine-2,6, -DIONY (Option) METHOD OF PRODUCING (option), pharmaceutical compositions MODELING METHOD immune response of mammals, a method for inhibiting antigen-triggered synthesis of interleukin-2 in mammals
专利号:US-9522899-B2 优先权日:2009-06-01 标 题:Methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2, 6-dioxopiperidine, and intermediates thereof 发明人:YAN RONG; YANG HAO; XU YONGXIANG 权利人:NANJING CAVENDISH BIO-ENGINEERING TECH CO LTD; YAN RONG; NANJIAN CAVENDISH BIO-ENGINEERING TECH CO LTD 摘要:The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.
摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 391. 参考文献:10.1007/bf02979158 摘要:Lee J, Son K, Kim M, Jung G, Choi J, Lee ES, Park M. The effect of N-substituted alkyl groups on anticonvulsant activities of N-Cbz-alpha-amino-N-alkylglutarimides. Arch Pharm Res. 1999 Oct;22(5):491–5. doi: 10.1007/bf02979158.