Palatin Technologies Incorporated

Zhijun Wu

Shubh D Sharma

Yi-Qun Shi

Ramesh Rajpurohit

Kevin D Burris

Papireddy Purma

Annette M Shadiack

Yadi Reddy Bonuga

Yiqun Shi

Bolun Hu

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

The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residue, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-, 6- and 8-membered and 5-5- and 6-5-bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.

Peptidomimetics of biologically active metallopeptides

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

Melanocortin receptor-specific compounds of the general formulas and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, L is a linker, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q includes a substituted or unsubstituted aromatic carbocyclic ring, R, R, y and z are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration, and optionally with one or two additional ring substituents as defined, which compounds bind to one or more melanocortin receptors and are optionally an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.

Substituted melanocortin receptor-specific piperazine compounds

A substituted piperazine compound having the structure I: or the structure IX: or an enantomeric, stereoisomeric or diastereomeric form of the foregoing, and pharmaceutically acceptable salts thereof, where J, L, Q, W, A, R, R, z and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration, which compounds bind to one or more melanocortin receptors and may be employed in pharmaceutical preparations for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.

Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R, R, and Rare as described in the specification, preferably where Ris a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where Roptionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

Pyrrolidine melanocortin-specific compounds

Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where X is CHor C&#x2550;O, R, R, and Rare as described in the specification, preferably where Ris a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where Roptionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

Piperazine melanocortin-specific compounds

Melanocortin receptor-specific bicyclic compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R, R, RX and z are as described in the specification, which are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

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Plainsboro, NJ, United States of America

Zhijun Wu