US 12,281,180 B2
Peptoid-peptide macrocycles, pharmaceutical compositions and methods of using the same
Kent Kirshenbaum, New York, NY (US); Susan Logan, New York, NY (US); Timothy Craven, Seattle, WA (US); Amanda Kasper, New York, NY (US); Richard A. Bonneau, New York, NY (US); and Jeffrey A Schneider, New York, NY (US)
Assigned to New York University, New York, NY (US)
Appl. No. 17/259,914
Filed by New York University, New York, NY (US)
PCT Filed Jul. 12, 2019, PCT No. PCT/US2019/041674
§ 371(c)(1), (2) Date Jan. 12, 2021,
PCT Pub. No. WO2020/014652, PCT Pub. Date Jan. 16, 2020.
Claims priority of provisional application 62/796,460, filed on Jan. 24, 2019.
Claims priority of provisional application 62/697,893, filed on Jul. 13, 2018.
Prior Publication US 2021/0269482 A1, Sep. 2, 2021
Int. Cl. C07K 7/56 (2006.01); A61P 35/00 (2006.01); C07K 5/083 (2006.01); A61K 38/00 (2006.01)
CPC C07K 7/56 (2013.01) [A61P 35/00 (2018.01); C07K 5/0806 (2013.01); A61K 38/00 (2013.01)] 9 Claims
 
1. A peptoid-peptide macrocycle having the following structure:

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wherein R2 is an amino acid sidechain of glycine, D-alanine, D-valine, D-leucine, D-isoleucine, D-tyrosine, D-proline, D-serine, D-glutamic acid, D-tryptophan, D-phenylalanine, D-methionine, D-arginine, D-histidine, D-glutamine, D-lysine, D-aspartic acid, D-threonine, D-cysteine, D-asparagine, L-alanine, L-valine, L-leucine, L-isoleucine, L-tyrosine, L-proline, L-serine, L-glutamic acid, L-tryptophan, L-phenylalanine, L-methionine, L-arginine, L-histidine, L-glutamine, L-lysine, L-aspartic acid, L-threonine, L-cysteine, or L-asparagine; each R1 is independently chosen from methoxy-ethyl

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4-methoxy-phenyl-ethyl

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3,5-dimethoxy-phenyl

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(S)-4-methoxy-phenyl-ethyl

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(S)-4-fluoro-phenyl-ethyl

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2-phenoxy-ethyl

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isopropoxy-propyl

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methoxy-propyl

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and 3,4-dimethoxyphenyl

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and the subscript n is an integer from 0 to 15.