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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 10682371 B1

PDFFull Text
Date of Patent:
Jun. 16, 2020

Filed:

Aug. 21, 2015

Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof

Applicant:

Yafei Shanghai Biolog Medicine Science & Technology Co. Ltd., Pudong, Shanghai, CN;

Inventors:

Chen Liu, Shanghai, CN;

Yuan Liu, Shanghai, CN;

Assignee:

YAFEI SHANGHAI BIOLOG MEDICINE SCIENCE & TECHNOLOGY CO. LTD., Shanghai, CN;

Attorney:

Knobbe, Martens, Olson & Bear LLP

Primary Examiner:

James H Alstrum-Acevedo

Assistant Examiner:

Kaipeen E Yang

Int. Cl.
CPC ...
A61K 31/7072 (2006.01); A61K 47/65 (2017.01); A61K 47/54 (2017.01); A61K 31/7076 (2006.01); A61K 31/4745 (2006.01); A61K 31/7068 (2006.01); A61K 31/337 (2006.01); A61P 35/00 (2006.01); A61K 31/136 (2006.01); A61K 31/198 (2006.01); A61K 31/427 (2006.01); A61K 31/475 (2006.01); A61K 31/505 (2006.01); A61K 31/519 (2006.01); A61K 31/704 (2006.01); A61K 31/7048 (2006.01);
U.S. Cl.
CPC ...
A61K 31/7076 (2013.01); A61K 31/136 (2013.01); A61K 31/198 (2013.01); A61K 31/337 (2013.01); A61K 31/427 (2013.01); A61K 31/475 (2013.01); A61K 31/4745 (2013.01); A61K 31/505 (2013.01); A61K 31/519 (2013.01); A61K 31/704 (2013.01); A61K 31/7048 (2013.01); A61K 31/7068 (2013.01); A61K 31/7072 (2013.01); A61K 47/54 (2017.08); A61K 47/65 (2017.08); A61P 35/00 (2018.01);
Abstract

Provided is an anticancer compound including a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, Ris a normal functional group or a protection group; Ris Ala, Thr, Val or Ile; Ris Ala, Val or Asn; Ris a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is RH. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.

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