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US 12,077,612 B2Granted
Peptide compositions
AssigneeRhythm Pharmaceuticals, Inc.
InventorsShubh Sharma, Leonardus H. T. Van Der Ploeg, Bart Henderson
Life of this patent
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Abstract
The present invention relates to polypeptide compounds that are modulators (e.g., agonists and antagonists) of the melanocortin-4 receptor (MC4R) and pharmaceutical compositions comprising same. The compounds described herein are polypeptide of the following structural Formula (I): or a pharmaceutically acceptable salt thereof. Values and preferred values of the variables in structural Formula (I) are described herein.
Claims6
An isolated polypeptide of the following structural Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is —H, or a C1-C6 acyl;
- R2 is —NR3R4, or —OR5 wherein R3, R4, and R5 are each independently is-H or a C1-C6 alkyl;
- A1 Nle;
- A2 and A8 is each independently an amino acid residue selected from Cys, hCys, Glu, or Dpr, wherein A2 and A8 are pairwise selected so as to be able to form a covalent bond between their respective side chains;
- A3 is an amino acid residue selected from Ala, Tle, Val, Leu, Ile, Cha, Pro, Ser, Thr, Lys, Arg, His, Phe, Gln, Sar, Gly, Asn, Aib, or
- A3 is absent, or
- A3 is residue Y, wherein Y is an amino acid selected from amino acids represented by the following structural formulas
- wherein:
- R11 and R12, each independently, is H, —CH3, phenyl, or benzyl;
- R21, R22, R23, and R24, each independently is H, —CH3, —CF3, phenyl, benzyl, F, Cl, Br, I, —OCH3, or —OH;
- R31, R32, R33, R34, R41, R42, and R43, each independently is H, —CH3, —CF3, phenyl, benzyl, F, Cl, Br, I, —OCH3, or —OH;
- A4 is absent or an optionally substituted His;
- A5 is an optionally substituted Phe
- A6 is Arg;
- and
- A7 is Trp,
- wherein any amino acid residue is either in L- or in D-configuration.
16 more elements
Dependencies are inferred from the claim text.