| 主权项 |
1. An azapeptide analogue of GHRP-6 that binds to CD36 and exhibits reduced binding to the growth hormone secretagogue receptor-1a relative to GHRP-6, wherein said azapeptide, analogue is of Formula I.3:
A-Xaa1-Xaa2-Xaa3-N(RA)—N(RB)—C(O)-Xaa′3-Xaa′4-B I.3 wherein Xaa1 is His, D-His, Ala, D-Ala, Phe or D-Phe; Xaa2 is Trp or D-Trp; Xaa3 is Ala or D-Ala; Xaa′3 is Phe, D-Phe, Ala or D-Ala; Xaa′4 is Lys, D-Lys, Ala or D-Ala; and not more than one of Xaa1, Xaa′3 and Xaa′4 is Ala or D-Ala; A is 1) H, 2) C1-C6 alkyl, 3) C2-C6 alkenyl, 4) C2-C4 alkynyl, 5) C3-C7 cycloalkyl, 6) haloalkyl, 7) heteroalkyl, 8) aryl, 9) heteroaryl, 10) heteroalkyl, 11) heterocyclyl, 12) heterobicyclyl, 13) C(O)R3, 14) SO2R3, 15) C(O)OR3, or 16) C(O)NR4R5, wherein the alkyl, the alkenyl, the alkynyl and the cycloalkyl are optionally substituted with one or more R1 substituents; and wherein the aryl, the heteroaryl, the heterocyclyl and the heterobicyclyl are optionally substituted with one or more R2 substituents; B is 1) OH, 2) OR3, or 3) NR4R5; RA and RB are independently chosen from 1) H, 2) C1-C6 alkyl, 3) C2-C6 alkenyl, 4) C2-C6 alkynyl, 5) C3-C7 cycloakyl, 6) C5-C7 cycloalkenyl, 7) haloalkyl, 8) heteroalkyl, 9) aryl, 10) heteroaryl, 11) heterobicyclyl, or 12) heterocyclyl, wherein the alkyl, alkenyl, alkynyl and the cycloalkyl and cycloalkenyl are optionally substituted with one or more R1 substituents; and wherein the aryl, the heteroaryl, the heterocyclyl and the heterobicyclyl are optionally substituted with one or more R2 substituents, or alternatively; RA and RB together with the nitrogen to which each is bonded form a heterocyclic or a heterobicyclic ring; R1 is 1) halogen; 2) NO2, 3) CN, 4) haloalkyl, 5) C3-C7 cycloalkyl, 6) aryl, 7) heteroaryl, 8) heterocyclyl, 9) heterobicyclyl, 10) OR6, 11) S(O)2R3, 12) R4R5, 13) NR4S(O)2R3, 14) COR6, 15) C(O)OR6, 16) CONR4R5, 17) S(O)2NR4R5, 18) OC(O)R6, 19) SC(O)R3, 20) NR6C(O)NR4R5, 21) heteroalkyl, 22) NR6C(NR6)NR4R5, or 23) C(NR6)NR4R5; wherein the aryl, heteroaryl, heterocyclyl, and heterobicyclyl are optionally substituted with one or more R2 substituents; R2 is 1) halogen, 2) NO2, 3) CN, 4) C1-C6 alkyl, 5) C2-C6 alkenyl, 6) C2-C4 alkynyl, 7) C3-C7 cycloalkyl, 8) haloalkyl, 9) ORE, 10) NR4R5, 11) SR6, 12) CORE, 13) C(O)OR6, 14) S(O)2R3, 15) CONR4R5, 16) S(O)2NR4R5, 17) aryl, 18) heteroaryl, 19) heterocyclyl, 20) heterobicyclyl, 21) heteroalkyl, 22) NR6C(NR6)NR4R5, or 23) C(NR6)NR4R5, wherein the aryl, the heteroaryl, the heterocyclyl, and the heterobicyclyl are optionally substituted with one or more R7 substituents; R3 is 1) C1-C6 alkyl, 2) C2-C6 alkenyl, 3) C2-C4 alkynyl, 4) C3-C7 cycloalkyl, 5) haloalkyl, 6) aryl, 7) heteroaryl, 8) heterocyclyl, or 9) heterobicyclyl, wherein the alkyl, the alkenyl, the all and the cycloalkyl are optionally substituted with one or more R1 substituents; and wherein the aryl, the heteroaryl, the heterocyclyl and the heterobicyclyl are optionally substituted with one or more R2 substituents; R4 and R5 are independently chosen from 1) H, 2) C1-C6 alkyl, 3) C2-C6 alkenyl, 4) C2-C6 alkynyl, 5) aryl, 6) heteroaryl, or 7) heterocyclyl, or R4 and R5 together with the nitrogen to which they are bonded form a heterocyclic ring; R6 is 1) H, 2) C1-C6 alkyl; 3) C2-C6 alkenyl, 4) C2-C6 alkynyl, 5) aryl, 6) heteroaryl, or 7) heterocyclyl; R7 is 1) halogen, 2) NO2, 3) CN, 4) C1-C6 alkyl, 5) C2-C6 alkenyl, 6) C2-C4 alkynyl, 7) C3-C7 cycloalkyl, 8) haloalkyl, 9) OR6, 10) NR4R5, 11) SR6, 12) COR6, 13) C(O)OR6, 14) S(O)2R3, 15) CONR4R5, 16) S(O)2NR4R5, 17) heteroalkyl, 18) NR6C(NR5)NR4R5, or 19) C(NR6)NR4R5; or a salt thereof; wherein the following compound is excluded: His-D-Trp-Ala-AzaTyr-DPhe-Lys-NH2. |
