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.

Date of Patent:
Dec. 20, 2016

Filed:

Sep. 30, 2014
Applicant:

Seattle Genetics, Inc., Bothell, WA (US);

Inventors:

Svetlana O Doronina, Snohomish, WA (US);

Toni Beth Kline, San Francisco, CA (US);

Scott Jeffrey, Snohomish, WA (US);

Peter D Senter, Seattle, WA (US);

Damon Meyer, Bellevue, WA (US);

Assignee:

Seattle Genetics, Inc., Bothell, WA (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 38/04 (2006.01); A61K 47/48 (2006.01); C07K 5/02 (2006.01); C07K 7/02 (2006.01); A61K 39/395 (2006.01); C07K 16/28 (2006.01); A61K 38/00 (2006.01); A61K 39/00 (2006.01);
U.S. Cl.
CPC ...
A61K 47/48415 (2013.01); A61K 39/3955 (2013.01); C07K 5/0205 (2013.01); C07K 7/02 (2013.01); C07K 16/2866 (2013.01); A61K 38/00 (2013.01); A61K 2039/505 (2013.01); C07K 2317/76 (2013.01);
Abstract

Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) having a carboxylic acid equivalent at the C-terminal phenylalanine were prepared and attached to ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand-drug conjugates were active in vitro and in vivo in inhibiting cell proliferation and are represented by the general structure ofL-[(LU)-(D)]wherein L- is Ligand unit; LU is a Linker unit (LU); v is 1; p is an number ranging from about 1 to about 20; and D is a drug moiety having the formula: wherein the moiety —N(R)Zis a phenylalanine bioisostere, wherein Zis —CH(R)Zso that the phenylalanine bioisostere has the structure of Formula A: and wherein the substituents R-R, Xand Zare as defined.


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