Abstract: Disclosed herein are compounds of formula Ar—N(SO2F)2, wherein Ar is selected from an optionally substituted aryl, an optionally substituted five-membered heteroaryl, or an optionally substituted six-membered heteroaryl. Also disclosed are methods of synthesizing the above compounds by reacting a compound of formula Ar—NH—R9 with MN(SO2F)2.
Type:
Grant
Filed:
August 14, 2018
Date of Patent:
November 17, 2020
Assignees:
BioDuro, LLC, Pfizer Inc.
Inventors:
Hua Zhou, Paramita Mukherjee, Rongqiang Liu, Christopher W. Am Ende, Tianjing Deng
Abstract: Disclosed herein are processes for formulating a protein or a peptide for oral delivery, the process comprising the steps of: obtaining a powder containing the protein or peptide; obtaining an amount of an enteric polymer, wherein the enteric polymer is neutralized so that it is soluble in water; optionally obtaining at least one excipient; mixing the protein or peptide, the neutralized enteric polymer, and optionally the at least one excipient to obtain a First Dispersion; granulating the First Dispersion on a fluidized bed to obtain a Second Dispersion; whereby the protein or peptide in the Second Dispersion undergoes less than 50% proteolysis under gastric conditions.
Abstract: Disclosed herein are compounds of formula Ar—N(SO2F)2, wherein Ar is selected from an optionally substituted aryl, an optionally substituted five-membered heteroaryl, or an optionally substituted six-membered heteroaryl. Also disclosed are methods of synthesizing the above compounds by reacting a compound of formula Ar—NH—R9 with MN(SO2F)2.
Type:
Application
Filed:
August 14, 2018
Publication date:
February 14, 2019
Applicants:
BIODURO, LLC, PFIZER INC.
Inventors:
Hua ZHOU, Paramita MUKHERJEE, Rongqiang LIU, Christopher W. AM ENDE, Tianjing DENG
Abstract: Disclosed herein are processes for formulating a protein or a peptide for oral delivery, the process comprising the steps of: obtaining a powder containing the protein or peptide; obtaining an amount of an enteric polymer, wherein the enteric polymer is neutralized so that it is soluble in water; optionally obtaining at least one excipient; mixing the protein or peptide, the neutralized enteric polymer, and optionally the at least one excipient to obtain a First Dispersion; granulating the First Dispersion on a fluidized bed to obtain a Second Dispersion; whereby the protein or peptide in the Second Dispersion undergoes less than 50% proteolysis under gastric conditions.