Palatin Technologies Incorporated

Papireddy Purma

Shubh D Sharma

Kevin D Burris

Yi-Qun Shi

Zhijun Wu

Yadi Reddy Bonuga

Annette M Shadiack

Ramesh Rajpurohit

Yiqun Shi

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.

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Plainsboro, NJ, United States of America

Papireddy Purma