Melanocortin receptor-specific peptides
Inventors
Shi, Yi-Qun • Sharma, Shubh D • Dodd, John H • Yang, Wei • Chen, Xin
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10632171-B2
Publication Date
2020-04-28
Expiration Date
Abstract
Melanocortin receptor-specific cyclic peptides of the formula where R1, R3, R4, R9 and R10 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.
Core Innovation
The invention relates to a cyclic peptide of a structural formula, including all enantiomers, stereoisomers or diastereoisomers thereof, or a pharmaceutically acceptable salt of any of the foregoing. The cyclic peptide is characterized by extensive substituent variables and structural constraints, including R1, R3, R4, R9, R10, R11, R12, R13, R15a, R15b, and R17, together with ring/substitution relationships and exclusions within the general formula.
The structural definition specifies that R1 is H or a C1 to C7 acyl group comprising a linear or branched alkyl or a cycloalkyl or both a linear alkyl and a cycloalkyl. R3 is H, CH3, or CH2, and when R3 is CH2 it forms with R4 a ring of a general structure, with R4 being H or a (CH2)z group or a (CH2)w-R12-(CH2)w-R13 arrangement with optional substitution. The definition also includes conditional ring-forming relationships and explicit exclusions based on particular combinations of R1, R9, R3, and R10.
The disclosed subject matter includes melanocortin receptor-specific cyclic peptides and pharmaceutically acceptable salts thereof, and also describes cyclic heptapeptide formula (II) with a lactam-containing cyclic bridge. The description includes examples of cyclic peptide variants distinguished by amino-acid substitutions within the cyclized peptide segment and modifications at the N- and C-terminus, including Ac-Arg-cyclo(...) and carboxyl-terminated forms.
Claims Coverage
The provided claim coverage centers on one independent structural claim directed to a cyclic peptide with a complex structural formula and another independent treatment claim for melanocortin receptor-mediated disease; the structural claim includes broad stereochemical coverage and pharmaceutically acceptable salts, together with detailed substituent constraints and exclusions. In total, two inventive features are reflected at the independent-claim level.
Cyclic peptide defined by a complex structural formula with stereochemical coverage
A cyclic peptide of a structural formula, including all enantiomers, stereoisomers or diastereoisomers thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein R1, R3, R4, R9, R10, R11, R12, R13, R15a, R15b, and R17 are defined by specified structural options, ring-closure relationships, optional substitutions, and exclusions for certain combinations.
Treatment of a melanocortin receptor-mediated disease by administering a pharmaceutical composition
A method for treating a melanocortin receptor-mediated disease, indication, condition, or syndrome in a mammal by administering the pharmaceutical composition of claim 9.
The independent claim coverage is centered on a cyclic peptide structural formula with extensive substituent and ring-formation constraints, including explicit exclusions, together with a method of treatment for melanocortin receptor-mediated disease using a pharmaceutical composition.
Stated Advantages
The peptides are positioned to prevent, ameliorate, or treat melanocortin receptor-mediated diseases and related indications.
The background describes an unmet need for melanocortin receptor-specific peptide therapeutics and limited clinical advancement.
Documented Applications
Preventing, ameliorating, or treating melanocortin receptor-mediated diseases, indications, conditions, and syndromes in a mammal by administering the pharmaceutical composition.
Targeting MC4-R ligand activity, including sexual dysfunction/erectile function and obesity/energy homeostasis and feeding modulation.
In vivo functional outcomes are referenced, including rat penile erections.
Interested in licensing this patent?