Ixazomib, also known as MLN-2238, is a potent proteasome inhibitor (PI) with potential antineoplastic activity. MNL-2238 is also .the biologically active form of MLN9708. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI-Ly10 and PHTX22L models. Although both MLN2238 and bortezomib prolonged overall survival, reduced splenomegaly, and attenuated IgG2a levels in the iMyc(Cα)/Bcl-X(L) GEM model, only MLN2238 alleviated osteolytic bone disease in the DP54-Luc model.
Lee, Kwang Chung; Lin, Chien Hung; Lin, Shu Chuan; Lin, Hua Hsuan. Process for preparing intermediate compound of ixazomib citrate, and ixazomib citrate made thereby. TW I599571. (Assignee Chunghwa Chemical Synthesis & Biotech Co., Ltd., Taiwan)
Bakale, Roger P.; Mallamo, John P.; Roemmele, Renee Caroline. Proteasome inhibitors and processes for their preparation, purification and use. WO 2012177835. (Assignee Cephalon, Inc., USA)
Lei, Meng; Zhu, Yongqiang; Feng, Huayun; Wang, Cheng. A dipeptide boronic acids composed of carboxylic acids and α-amino acids, its ester compounds, preparation method thereof and application in treating solid tumor and blood tumor. CN 105732683. (Assignee Nanjing Forestry University, Peop. Rep. China)
Li, Dequn. Preparation process of boron-containing compound. CN 106518902. (Assignee Chengdu Beisi Kairui Biotechnology Co., Ltd., Peop. Rep. China)
Li, Runtao; Ge, Zemei; Cheng, Qing; Han, Liqiang; Wang, Xin; Cheng, Tieming. Synthesis method of proteasome inhibitor MLN9708. CN 106608883. (Assignee Peking University, Peop. Rep. China)
Zhu, Yongqiang; Lei, Meng; Bai, Enhe; Feng, Huayun. Preparation of deuterated dipeptide boronic acids as proteosome inhibitors. CN 106916177. (Assignee Nanjing Normal University, Peop. Rep. China)
Rajan, Srinivasan Thirumalai; Eswaraiah, Sajja; Reddy, Ghojala Venkat; Reddy, Mallepally Venkat. Process for the preparation of ixazomib citrate. IN 201641044033. (Assignee MSN Laboratories Private Limited, R & D Center, India)
Pandey, Maneesh Kumar; Shukla, Sonu Prasad; Tiwari, Raj Narayan; Sokhi, Sarbjot Singh; Singh, Govind; Lahiri, Saswata; Cabri, Walter. A process for the preparation of ixazomib citrate. WO 2018158697. (Assignee Fresenius Kabi Oncology Limited, India)
Zhu, Yongqiang; Lei, Meng; Bai, Enhe; Feng, Huayun. Preparation of deuterated dipeptide boronic acids as proteosome inhibitors. WO 2018171816. (Assignee Nanjing Lingrui Pharmaceutical Technology Co., Ltd., Peop. Rep. China)
