| 主权项 |
1. A cosmetic method of modifying the contour of a subject's externally exposed body part containing fat, the method comprising administering to said body part an amount of a compound of Formula I, I-1, I-2, or I-3 effective to modify the contour of said body part, wherein Formula I is represented by: or a pharmaceutically acceptable salt thereof; wherein:
R1 is —(C1-C6)alkylene-X1, —(C3-C6)cycloalkyl-X1, —CO2R6, —C(O)R6, —OH, or —N(R6)C(O)—(C1-C6)alkyl;X1 is —CO2R6, —C(O)R6, —C(O)N(R7)R6, —N(R7)C(O)R6, or —OR6;R2 and R3 each represent independently hydrogen or —(C1-C6)alkyl;R4 is hydrogen, —(C1-C6)alkyl, —(C3-C7)cycloalkyl, —(C1-C6)alkoxy, or —(C3-C7)cycloalkoxy;R5 is phenyl, 5-6 membered heteroaryl, —(C3-C7)cycloalkyl, —(C1-C6)alkoxy, or aralkyl, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —(C1-C6)alkyl, —(C3-C5)cycloalkyl, hydroxyl, and —(C1-C6)alkoxy; or R5 is hydrogen or —(C1-C6)alkyl; andR6 and R7 each represent independently hydrogen or —(C1-C6)alkyl;Formula I-1 is represented by: or a pharmaceutically acceptable salt thereof, wherein:R1 and R6 each represent independently for each occurrence hydrogen, halogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;R2 is —N(R7)R8, —OR7, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;R3 is hydrogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;R4 is aralkyl or heteroaralkyl, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —(C1-C6)alkyl, —(C3-C6)cycloalkyl, hydroxyl, —(C1-C6)alkoxy, —N(R7)R8, —C(O)N(R7)R8, and —N(R7)C(O)R8;R5 is hydrogen, —(C1-C6)alkyl, —(C3-C6)cycloalkyl, —CO2R7, —C(O)N(R7)R8, or —N(R7)C(O)R8;R7 and R8 each represent independently for each occurrence hydrogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl; or when R7 and R8 are attached to the same nitrogen atom, then R7 and R8 may be taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocycle; andn is 1, 2, or 3;Formula I-2 is represented by: or a pharmaceutically acceptable salt thereof, wherein:R1 and R3 each represent independently for each occurrence hydrogen, halogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl;R2 is —(C1-C6)alkyl, —(C3-C6)cycloalkyl, phenyl, 5-6 membered heteroaryl, aralkyl, or —(C1-C6)alkoxy, wherein said cycloalkyl, phenyl, 5-6 membered heteroaryl, and aralkyl are optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —(C1-C6)alkyl, —(C3-C6)cycloalkyl, hydroxyl, and —(C1-C6)alkoxy;R4 is —(C1-C6)alkylene-X1 or —(C3-C6)cycloalkyl-X1;X1 is —C(O)N(R5)R6, —N(R5)C(O)R6, —CO2R6, —C(O)R6, —OR6, or —N(R5)R6;R5 and R6 each represent independently hydrogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl; or when R5 and R6 are attached to the same nitrogen atom, then R5 and R6 may be taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocycle; andn is 1, 2, or 3; andFormula I-3 is represented by: or a pharmaceutically acceptable salt thereof, wherein:R1 is phenyl, 5-6 membered heteroaryl, aralkyl, —(C1-C6)alkyl, —(C3-C6)cycloalkyl —(C1-C6)alkylene-OH, or —(C1-C6)alkylene-O—(C1-C6)alkyl, wherein said phenyl, 5-6 membered heteroaryl, aralkyl, and cycloalkyl are optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —(C1-C6)alkyl, —(C3-C6)cycloalkyl, hydroxyl, —(C1-C6)alkoxy, and —N(R5)R6;R2 and R3 each represent independently for each occurrence hydrogen, —(C1-C6)alkyl, or halogen;R4 is —C(O)N(R5)R6, —N(R5)C(O)R6, —CO2R6, —C(O)R6, —(C1-C6)alkylene-N(R5)R6, —(C1-C6)alkylene-OR6, or —(C1-C6)alkoxy;R5 and R6 each represent independently for each occurrence hydrogen, —(C1-C6)alkyl, or —(C3-C6)cycloalkyl; or when R5 and R6 are attached to the same nitrogen atom, then R5 and R6 may be taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocycle; andn and m each represent independently 1 or 2. |
