Patent number: 7067525
Abstract: Compounds having the formula (I), G is a novel side chain selected from C2-6alkenyl, A3-aryl, —OR18, heteroaryl, A1-cyano, A2—OR17, A1—C(?O)R18, A1—CO2R18, A1—C(?O)NR18R19, A1—OC(?O)R18, A1—NR18C(?O)R19, A1—OC(?O)NR18R19, A1—NR18CO2R19, A1—NR18SO2R17, A1—SO2R17, A1—NR20C(?O)NR18R19, and A1—SR18; or when y is 0 or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from —NR21R22, —OR23, —NR21C(?O)R24, —NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.
Type:
Grant
Filed:
October 29, 2003
Date of Patent:
June 27, 2006
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Guixue Yu, John Macor, Timothy Herpin, R. Michael Lawrence, George C. Morton, Rejean Ruel, Graham S. Poindexter, Edward H. Ruediger, Carl Thibault
Publication number: 20050080090
Abstract: Compounds of the formula (1) where R1 is of formula (II), (III), or (IV), or (V); R2 is —R4, —O—R4, —O—S(O)2—R4, —NR4R5, R4—(CH2)b—NH(C?X)—(CH2)C—, R4—(CH2)b—O(C—O)NH—(CH2)c—(C?O)NH—, R4—(C?O)NH—(C?O)NH—, —CH2)b—NH(C?X)—(CH2)c—R4, R4—(CH2)b—O(C?O)CH2)c—, —(CH2)b—O(C?O)—(CH2)c—R4, —NH(C?X)NH—R4, R4—O(C?O)O—, —O(C?O)NH—R4, R4—O(C?O)NH—, —(CH2)b—(C?O—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C?O)—NR4, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formula —R4, —R4R5, —O—R4, or —S(O)d—R4; R3 is hydrogen, C1 to C6 alkyl, C1 to C6 alkylaryl, or aryl; R4 and R5 are each independently (XV), (XVI), (XVII), (XVII) hydrogen, —CF3, C1 to C6 alkyl, C1 to C6 alkylaryl, with the proviso that when R2 is —R4 or —OR4, R4 is not hydrogen or C1 to C6 alkyl these compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used
Type:
Application
Filed:
August 21, 2003
Publication date:
April 14, 2005
Inventors:
Bertrand Chenard, John Macor, Barbara Segelstein