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Last Updated: March 29, 2024

Claims for Patent: 9,345,786


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Summary for Patent: 9,345,786
Title:Maytansinoid derivatives
Abstract: 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.
Inventor(s): Li; Shengfeng (Belmont, CA), Deng; Xiaobin (Guangzhou, CN), Tan; Songnuan (Guangzhou, CN), Tang; Weijia (Guangzhou, CN), Qin; Chao (Guangzhou, CN)
Assignee: Bio-Thera Solutions, Ltd., Co. (Science City, CN)
Application Number:13/837,783
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,345,786
Patent Claims:1. A compound of Formula Ia: ##STR00067## or a pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or halo; Y is selected from the group consisting of hydrogen, C.sub.1-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl, and --C(.dbd.O)R.sup.5; R.sup.1 is selected from the group consisting of hydrogen, --OH, --OC(.dbd.O)R.sup.5 and --OR.sup.5; R.sup.2 is hydrogen or C.sub.1-C.sub.6 alkyl; R.sup.3 is methyl, --CH.sub.2OH, or --CH.sub.2C(.dbd.O)R.sup.6; R.sup.4 is --OH or --SH; R.sup.5 is C.sub.1-C.sub.6 alkyl or benzyl; R.sup.6 is C.sub.1-C.sub.6 alkyl, phenyl or benzyl; R.sup.7 is hydrogen, C.sub.1-C.sub.6 alkyl or an amino acid side chain; R.sup.8 is hydrogen or C.sub.1-6 alkyl; p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; Z is independently hydrogen or C.sub.1-C.sub.4 alkyl or two Z with the carbon atom to which they are attached to form a C(.dbd.O); L is selected from the group consisting of C.sub.1-C.sub.20 alkylene, substituted C.sub.1-C.sub.20 alkylene, and substituted C.sub.1-C.sub.20 alkylene wherein one or more of the --CH.sub.2-- groups are independently replaced with --O--, --NR.sup.8--, --C(O)--, --C(.dbd.O)NR.sup.8--, or --NR.sup.8C(.dbd.O)--; wherein said substituted C.sub.1-C.sub.20 alkylene is C.sub.1-C.sub.20 alkylene substituted with 1 to 4 R.sup.23, wherein each R.sup.23 is independently unsubstituted C.sub.1-6 alkyl; and Abu is an antigen binding unit and wherein the wavy line () represents linkage of the Abu through a thioether bond.

2. The compound of claim 1, which is: ##STR00068## or a salt thereof.

3. The compound of claim 1, which is of Formula IIIa: ##STR00069## or a pharmaceutically acceptable salt or solvate thereof, wherein X is H or Cl; Y is H or methyl; R.sup.7 is hydrogen, C.sub.1-C.sub.6 alkyl or an amino acid side chain; R.sup.8 is hydrogen or C.sub.1-C.sub.6 alkyl; p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; and Abu is an antigen binding unit.

4. The compound of claim 1, which is of Formula IVa: ##STR00070## or a pharmaceutically acceptable salt or solvate thereof, wherein X is H or Cl; Y is H or methyl; R.sup.7 is hydrogen, C.sub.1-C.sub.6 alkyl or an amino acid side chain; R.sup.8 is hydrogen or C.sub.1-C.sub.6 alkyl; p is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; m is selected from an integer of 1 to 20; and Abu is an antigen binding unit.

5. The compound of claim 1, which is of Formula Va: ##STR00071## or a pharmaceutically acceptable salt or solvate thereof.

6. The compound of claim 1, selected from the group consisting of ##STR00072## ##STR00073## or a pharmaceutically acceptable salt thereof; wherein m is selected from an integer of 1 to 20.

7. The compound of claim 1, wherein Abu is an antigen binding unit with binding specificity to human EGFR.

8. The compound of claim 1, wherein Abu is an antigen binding unit with binding specificity to human CD20.

9. The compound of claim 7, wherein Abu is an antibody, antibody fragment, or cell specific ligands.

10. The compound of claim 1, wherein Abu is an antibody comprising SEQ ID 1 and 2, or SEQ ID 3 and 4, or SEQ ID 5 and 6, or SEQ ID 7 and 8, or SEQ ID 9 and 10, or SEQ ID 13 and 14.

11. The compound of claim 1, wherein Abu is an antibody comprising Bat0202 (SEQ ID NO: 1) and/or Bat0204 (SEQ ID NO: 2).

12. The compound of claim 1, wherein Abu is Bat0206.

13. The compound of claim 1, wherein Abu is selected from C225, EGF-ABX, EGF-ABX, NIMO, Matu, rituxamab, Cetuximab, and Pertuzumab.

14. A pharmaceutical composition comprising a compound of claim 1.

15. A method of treating a proliferative, inflammatory or immunological disease or condition in a patient in need thereof comprising administering to the patient an effective amount of a compound of claim 1.

Details for Patent 9,345,786

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Eli Lilly And Company ERBITUX cetuximab Injection 125084 02/12/2004 ⤷  Try a Trial 2039-02-26
Eli Lilly And Company ERBITUX cetuximab Injection 125084 03/28/2007 ⤷  Try a Trial 2039-02-26
Genentech, Inc. PERJETA pertuzumab Injection 125409 06/08/2012 ⤷  Try a Trial 2039-02-26
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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