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:
Feb. 27, 2018

Filed:

Aug. 21, 2014
Applicant:

Martin-luther-universitaet Halle-wittenberg, Halle (Saale), DE;

Inventor:

Andreas Hilgeroth, Halle, DE;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 471/04 (2006.01); A61K 31/4375 (2006.01); A61K 31/437 (2006.01);
U.S. Cl.
CPC ...
A61K 31/437 (2013.01); A61K 31/4375 (2013.01); C07D 471/04 (2013.01);
Abstract

Novel enzyme inhibitors for treatment of breast cancer combine the inhibition of enzymes that combat aggressive breast cell growth both synergistically and additively. Pyrido-annulated indoles developed act in a selectively inhibiting manner on the enzymes HER2 and/or Brk in the nanomolar to picomolar concentration range in screening more than 200 kinases of the human kinome. The enzyme inhibitors inhibit the growth of breast cancer cells in the nanomolar concentration range without exhibiting critical toxic effects. The derivatization at the 6-position of the 4-chloro-α-carboline is achieved without by-products and, similarly to the derivatization at the 4-position with the aniline derivatives, takes place at high purity with quantitative yields.


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