C07K14/665

Bioconjugates of neuropeptides derivatives

A bioconjugate comprising at least one neuropeptide covalently bond to at least one hydrocarbon compound of squalene structure.

Bioconjugates of neuropeptides derivatives

A bioconjugate comprising at least one neuropeptide covalently bond to at least one hydrocarbon compound of squalene structure.

MU OPIOID RECEPTOR AGONIST ANALOGS OF THE ENDOMORPHINS

The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2, and in some embodiments, a 2′,6′-dimethyltyrosine (Dmt) residue in place of the N-terminal tyrosine residue a position 1. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

MU OPIOID RECEPTOR AGONIST ANALOGS OF THE ENDOMORPHINS

The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2, and in some embodiments, a 2′,6′-dimethyltyrosine (Dmt) residue in place of the N-terminal tyrosine residue a position 1. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

MU OPIOID RECEPTOR AGONIST ANALOGS OF THE ENDOMORPHINS

The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic analogs of endomorphin. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

MU OPIOID RECEPTOR AGONIST ANALOGS OF THE ENDOMORPHINS

The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic analogs of endomorphin. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

DELTA RECEPTOR AGONIST PEPTIDES AND USE THEREOF
20170291922 · 2017-10-12 ·

Peptides effective as delta opioid receptor agonists and compositions comprising same are provided. Further provided are methods for targeting medical conditions amenable to treatment with an opioid receptor agonist, including but not limited to, conditions involving pain as well as reducing cocaine craving.

Melanocortin Receptor Ligands
20170240595 · 2017-08-24 · ·

The present invention is directed to compounds according to formula,


(R.sup.2R.sup.3)-A.sup.1-c(A.sup.2-A.sup.3-A.sup.4-A.sup.5-A.sup.6-A.sup.7-A.sup.8-A.sup.9)-A.sup.10-R.sup.1,

and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

OPIOID PEPTIDE

The present invention relates to an opioid peptide represented by general formula TyrGlyGly-X1-X2-X3-X4, wherein: X1 is represented by Thr or Glu; X1 is represented by Gly or Thr or Ala; X3 is represented by Ala or Val or Gly or Glu; and X4 is represented by His or Gln or Thr or SEQ ID NO:1, or HisTyr or GlnTyr or ThrTyr.

The invention also relates to pharmaceutical and food compositions comprising the peptide and to the use of the same for analgesic purposes, and/or for providing a feeling of satiety to a subject.

MELANOCORTIN RECEPTOR LIGANDS
20220127305 · 2022-04-28 ·

The present invention is directed to compounds according to formula,


(R.sup.2R.sup.3)-A.sup.1-c(A.sup.2-A.sup.3-A.sup.4-A.sup.5-A.sup.6-A.sup.7-A.sup.8-A.sup.9)-A.sup.10-R.sup.1,

and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.