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:
Nov. 29, 2016

Filed:

Mar. 29, 2013
Applicant:

Endocyte, Inc., West Lafayette, IN (US);

Inventors:

Iontcho Radoslavov Vlahov, West Lafayette, IN (US);

Hari Krishna R. Santhapuram, West Lafayette, IN (US);

Paul Joseph Kleindl, Lebanon, IN (US);

Christopher Paul Leamon, West Lafayette, IN (US);

Fei You, West Lafayette, IN (US);

Assignee:

Endocyte, Inc., West Lafayette, IN (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 277/56 (2006.01); A61K 38/00 (2006.01); C07D 417/14 (2006.01); C07K 5/02 (2006.01); C07K 7/02 (2006.01); C07D 213/71 (2006.01); C07C 241/02 (2006.01); C07D 213/76 (2006.01); C07D 417/12 (2006.01); C07F 7/18 (2006.01);
U.S. Cl.
CPC ...
C07D 417/14 (2013.01); C07C 241/02 (2013.01); C07D 213/71 (2013.01); C07D 213/76 (2013.01); C07D 277/56 (2013.01); C07D 417/12 (2013.01); C07F 7/188 (2013.01); C07F 7/1892 (2013.01); C07K 5/02 (2013.01); C07K 7/02 (2013.01);
Abstract

The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.


Find Patent Forward Citations

Loading…