Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases
US-9624268-B2 · Apr 18, 2017 · US
US10787490B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10787490-B2 |
| Application number | US-201615745371-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 15, 2016 |
| Priority date | Jul 15, 2015 |
| Publication date | Sep 29, 2020 |
| Grant date | Sep 29, 2020 |
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Peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases, are described.
Opening claim text (preview).
What is claimed is: 1. A peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt thereof, wherein the peptide inhibitor is: (SEQ ID NO: 1115) [Palm]-[isoGlu]-[PEG4]-[Pen]-NTWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1116) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2-Nal]- [Aib]-[Lys(PEG4-isoGlu-Palm)]-NN-NH 2 ; (SEQ ID NO: 1117) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(Ac)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1118) [Octanyl]-[IsoGlu]-[PEG4]-[Pen]-NTWQ-[Pen]-[Phe[4- (2-aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1119) [Octanyl]-[PEG4]-[Pen]-NTWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1120) [Palm]-[PEG4]-[Pen]-NTWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1121) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-(2- Nal]-[Aib]-[Lys(PEG4-Octanyl)]-NN-NH 2 ; (SEQ ID NO: 1122) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-(2- Nal]-[Aib]-[Lys(PEG4-Palm)]-NN-NH 2 ; (SEQ ID NO: 1123) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)-(PEG4-Palm)]-(2-Nal]-[Aib]- [Lys(Ac)]NN-NH 2 ; (SEQ ID NO: 1124) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)-(PEG4- Lauryl)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1125) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(PEG4-Palm)-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1126) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(PEG4-Lauryl)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1127) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)-(PEG4- IsoGlu-Palm)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1128) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)-(PEG4- IsoGLu-Lauryl)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1129) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(PEG4-IsoGlu-Palm)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1130) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-a-Me- K(PEG4-IsoGlu-Lauryl)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1131) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(IVA)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1132) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(Biotin)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1133) Ac-[Pen]-QTWQ-[Pen]-Phe(4-CONH 2 )-[2-Nal]-[a- MeLys(Octanyl)]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1134) Ac-[Pen]-[Lys(IVA)]-TWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1135) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2- Nal]-[Aib]-[Lys(Ac)]-[Lys(IVA)]-N-NH 2 ; (SEQ ID NO: 1136) Ac-[Pen]-[Lys(Biotin)]-TWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1137) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2- Nal]-[Aib]-[Lys(Ac)]-[Lys(Biotin)]-N-NH 2 ; (SEQ ID NO: 1138) Ac-[Pen]-[Lys(Octanyl)]-TWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1139) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2- Nal]-[Aib]-[Lys(Ac)]-[Lys(octanyl)]-N-NH 2 ; (SEQ ID NO: 1140) Ac-[Pen]-[Lys(Palm)]-TWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]--[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1141) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2- Nal]-[Aib]-[Lys(Ac)]-Lys(Palm)]-N-NH 2 ; (SEQ ID NO: 1142) Ac-[Pen]-[Lys(PEG8)]-TWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]--[Aib]-[Lys(Ac)]-NN-NH 2 ; (SEQ ID NO: 1143) Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]-[2- Nal]-[Aib]-[Lys(Ac)]-[Lys(PEG8)]-N-NH 2 ; (SEQ ID NO: 1144) Ac-[Pen]-K(Peg11-Palm)TWQ-[Pen]-[Phe[4-(2- ami
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title
Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title
Inhibitors; Suppressors · CPC title
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