US 12,234,457 B2
P-ethoxy nucleic acids for BCL2 inhibition
Ana Tari Ashizawa, Bellaire, TX (US); and Peter Nielsen, Bellaire, TX (US)
Assigned to BIO-PATH HOLDINGS, INC., Bellaire, TX (US)
Appl. No. 16/606,443
Filed by Bio-Path Holdings, Inc., Bellaire, TX (US)
PCT Filed Apr. 19, 2018, PCT No. PCT/US2018/028267
§ 371(c)(1), (2) Date Oct. 18, 2019,
PCT Pub. No. WO2018/195253, PCT Pub. Date Oct. 25, 2018.
Claims priority of provisional application 62/487,302, filed on Apr. 19, 2017.
Prior Publication US 2021/0123058 A1, Apr. 29, 2021
Int. Cl. C12N 15/113 (2010.01); A61K 9/127 (2006.01); A61K 31/7125 (2006.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01)
CPC C12N 15/1135 (2013.01) [A61K 9/127 (2013.01); A61K 31/7125 (2013.01); A61P 35/00 (2018.01); A61P 35/02 (2018.01); C12N 2310/11 (2013.01); C12N 2310/31 (2013.01); C12N 2310/345 (2013.01)] 26 Claims
 
1. A composition comprising a population of oligonucleotides, wherein the oligonucleotides hybridize to a BCL2 polynucleotide gene product, wherein oligonucleotides of the population are composed of nucleoside molecules linked together through phosphate backbone linkages, wherein 50% to 80% of the phosphate backbone linkages in each oligonucleotide are P-ethoxy backbone linkages, and wherein 25% to 50% of the phosphate backbone linkages in each oligonucleotide are phosphodiester backbone linkages, wherein oligonucleotides of the population comprise:
(a) the sequence according to SEQ ID NO: 1, and wherein the phosphate backbone linkages at least between nucleotides 5 and 6, between nucleotides 7 and 8, between nucleotides 9 and 10, between nucleotides 11 and 12, and between nucleotides 14 and 15 of the oligonucleotides of the population are phosphodiester backbone linkages; or
(b) the sequence according to SEQ ID NO: 2, and wherein the phosphate backbone linkages at least between nucleotides 5 and 6, between nucleotides 7 and 8, and between nucleotides 9 and 10 of the oligonucleotides of the population are phosphodiester backbone linkages.