摘要:
Cyclic constructs which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and a cyclic linkage including one or two amide bonds, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要:
Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, and y are as defined in the specification, together with methods for synthesizing ring-constrained amino acid surrogates of formula I and peptidomimetics incorporating the same, and methods of use of peptidomimetics in the treatment of various diseases, syndromes and conditions.
摘要:
Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R′, Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti-hypertensive, cardiovascular, renal or endocrine effects are desired.
摘要:
Ring-constrained amino acid surrogates of formula I: where R1, R2, R3, R4, R5, R6a, R6b, R7, and y are as defined in the specification, methods for synthesizing ring-constrained amino acid surrogates of formula I, methods of use of ring-constrained amino acid surrogates of formula I, including use in linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I and linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I.
摘要:
Linear and cyclic peptides are provided specific to one or melanocortin receptors, and which exhibit agonist, antagonist, or mixed agonist-antagonist activity. In one embodiment, a linear peptide of the following general formula is provided:
摘要:
Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z 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.
摘要:
A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.
摘要:
Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, x and y 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, including obesity, diabetes, modulation of feeding behavior and related metabolic syndrome.
摘要:
A melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, compositions and formulations including the peptide of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including sexual dysfunction such as male erectile dysfunction and female sexual dysfunction.
摘要:
Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z 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.