Processes for preparing tubulysin derivatives and conjugates thereof

US9505747B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9505747-B2
Application numberUS-201314388311-A
CountryUS
Kind codeB2
Filing dateMar 29, 2013
Priority dateMar 29, 2012
Publication dateNov 29, 2016
Grant dateNov 29, 2016

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

Official abstract text for this publication.

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.

First claim

Opening claim text (preview).

What is claimed is: 1. A process for preparing a compound of the formula or a salt or solvate thereof; wherein Ar 1 is optionally substituted aryl or optionally substituted heteroaryl; Ar 2 is optionally substituted aryl or optionally substituted heteroaryl; L is selected from the group consisting of…

Assignees

Inventors

Classifications

  • Chemistry & Metallurgy · mapped topic

  • Chemistry & Metallurgy · mapped topic

  • Chemistry & Metallurgy · mapped topic

  • C07D417/14Primary

    Chemistry & Metallurgy · mapped topic

  • Chemistry & Metallurgy · mapped topic

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What does patent US9505747B2 cover?
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 includ…
Who is the assignee on this patent?
Endocyte Inc
What technology area does this patent fall under?
Primary CPC classification C07D417/14. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Nov 29 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).