04-06-2015 дата публикации
Номер: US20150151003A1
Принадлежит:
Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided. 157-. (canceled)62. The compound of any one of or , wherein Abu is an antigen binding unit with binding specificity to human EGFR.63. The compound of any one of or , wherein Abu is an antigen binding unit with binding specificity to human CD20.64. The compound of any one of or , wherein Abu is an antigen binding unit with binding specificity to human Her2.65. The compound of any one of or , wherein Abu is an antibody comprising SEQ ID NOs: 1 and 2 , or SEQ ID NOs: 3 and 4 , or SEQ ID NOs: 5 and 6 , or SEQ ID NOs: 7 and 8 , or SEQ ID NOs: 9 and 10 , or SEQ ID NOs: 11 and 12 , or SEQ ID NOs: 13 and 14.66. The compound of any one of or , wherein Abu is selected from C225 , EGF-ABX , EGF-ABX , NIMO , Matu , rituxamab , Cetuximab , trastuzumab and Pertuzumab.72. The method of claim 71 , wherein the antigen binding unit is an antibody comprising SEQ ID NOs: 1 and 2 claim 71 , or SEQ ID NOs: 3 and 4 claim 71 , or SEQ ID NOs: 5 and 6 claim 71 , or SEQ ID NOs: 7 and 8 claim 71 , or SEQ ID NOs: 9 and 10 claim 71 , or SEQ ID NOs: 11 and 12 claim 71 , or SEQ ID NOs: 13 and 14. This application is a continuation of U.S. patent application Ser. No. 13/838,868, filed on Mar. 15, 2013, which claims priority under 35 U.S.C. §119 from CN 201210564166.7, filed on Dec. 21, 2012, and CN 201310081710.7, filed on Mar. 14, 2013, each of which are incorporated herein by reference in their entirety for all purposes.The present invention provides maytansinoid derivatives, including maytansinoid derivatives for linking to antigen binding unit and maytansinoid drug linked ...
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