Palatin Technologies Incorporated

Kevin D Burris

Shubh D Sharma

Yi-Qun Shi

Papireddy Purma

Annette M Shadiack

Ramesh Rajpurohit

Zhijun Wu

Yadi Reddy Bonuga

Yiqun Shi

A melanocortin-4 receptor agonist cyclic peptide of the formula where R, R, R, R, R, R, R, R, R, x, y and z are as defined in the specification, and a method of treating sexual dysfunction, including male erectile dysfunction and female sexual dysfunction, and other melanocortin 4 receptor responsive conditions and disorders.

N-alkylated cyclic peptide melanocortin agonists

Melanocortin receptor-specific compounds with diamine groups of the general formula and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L, L, L, R, R, R, Rand X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

Melanocortin receptor-specific piperazine compounds with diamine groups

A melanocortin receptor-specific compound of the general formula of structure I: where X, R, R, R, R, R, R, Rand Rare as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.

Melanocortin receptor-specific compounds

There is provided compounds having the formula of structure I: wherein the groups &#x2014;C(R)(CH)CH(R)(CH)-Q and &#x2014;C(R)(CH)CH(R)(CH)-J are the same, and R, R, R, R, R, R, J, Q, W, X, L, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.

Diamine-containing, tetra-substituted piperazine compounds having identical 1- and 4-substituents

A method of modulating energy homeostasis in a mammal without eliciting a sexual response by administration of a therapeutically effective amount of a pharmaceutical composition including a melanocortin receptor compound of the formula: where Ris a bond or a linker unit including from one to six backbone atoms and an unsubstituted naphthalene group, and L, R, Rand Rare as defined in the specification.

Naphthalene-containing melanocortin receptor-specific small molecule

Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where X, W, J, Q, L, L, L, R, R, R, and Rare as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

Melanocortin receptor-specific piperazine and keto-piperazine compounds

Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q is a substituted or unsubstituted aromatic carbocyclic ring group, L, R, R, R, R, r, x and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

Substituted melanocortin receptor-specific single acyl piperazine compounds

A highly selective melanocortin-4 receptor antagonist cyclic hexapeptide of the formula where R, R, R, R, R, R, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

Cyclic peptides for treatment of cachexia

A highly selective melanocortin-4 receptor antagonist cyclic peptide of the formula where R, R, R, R, R, R, R, R, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders.

Growing community of inventors

Washington Crossing, PA, United States of America

Kevin D Burris