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:
Jan. 08, 2019

Filed:

Nov. 24, 2014
Applicants:

Qi-ying HU, Needham, MA (US);

Hidetomo Imase, Somerville, MA (US);

Inventors:

Qi-Ying Hu, Needham, MA (US);

Hidetomo Imase, Somerville, MA (US);

Assignee:

Novartis AG, Basel, CH;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 38/00 (2006.01); A61K 47/48 (2006.01); C07K 1/113 (2006.01); C07K 7/64 (2006.01); A61K 47/54 (2017.01); A61K 47/62 (2017.01); A61K 47/64 (2017.01); A61K 47/68 (2017.01);
U.S. Cl.
CPC ...
A61K 47/48038 (2013.01); A61K 47/542 (2017.08); A61K 47/62 (2017.08); A61K 47/646 (2017.08); A61K 47/68 (2017.08); A61K 47/6803 (2017.08); A61K 47/6849 (2017.08); C07K 1/1133 (2013.01); C07K 7/64 (2013.01); C07K 2317/40 (2013.01);
Abstract

The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.


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