abstract |
MC-3 / MC-4 receptor ligands are revealed, which compound including all enantiomeric and diastereomeric forms and pharmaceutically acceptable salts thereof, said compound has the formula (1) wherein A is a conformationally restricted ring system that is select from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprise from 5 to 8 atoms; W is a pending unit having the formula (2), wherein R is selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; the aforementioned rings comprise from 3 to 12 atoms; J is selected from the group consisting of:) - [c (R '') d] k-; wherein each R '' independently is hydrogen, linear or branched C1-12 alkyl, -SUB, two R units '' can be taken together with an oxygen atom to form a carbonyl unit, two R units '' of any unit J or a unit R '' and a unit R 'of a unit T can be taken together to form a fused carbocyclic or heterocyclic ring, bicyclic ring, or spiroanulated ring comprising from 3 to 7 atoms; index d has the value of 1 or 2; the index k has the value of 1 or 2; ii) -N-; iii) -NR'-, wherein R 'is hydrogen, linear or branched C1-6 alkyl, or a SUB unit; iv) -O-; v) -S-; vi) -P (O) - or -P (O) 2-; vii) and mixtures thereof; L is a linking unit; B comprises a unit that is selected from the group consisting of: a) hydrogen; b) substituted or unsubstituted aromatic carbocyclic rings; c) substituted or unsubstituted aromatic heterocyclic rings; and d) mixtures thereof; And it is a pending unit that comprises at least one heteroatom; Z is a pending unit, which comprises an aromatic carbocyclic ring. A pharmaceutical composition comprising A) an effective amount of said compound; B) the balance of carriers, excipients, and auxiliary ingredients. Use of a compound to manufacture a pharmaceutical composition according to a method of treating a disorder comprising administering an effective amount of said compound to an animal subject that needs to be treated that is selected from the group consisting of insulin resistance, intolerance to glucose, type 2 diabetes mellitus, coronary artery disease, high blood pressure, hypertension, dyslipidemia, cancer, menstrual irregularities, hirsutism, infertility, and others as described in memory, in a subject or animal that requires treatment. |