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1. A pharmaceutical formulation comprising a compound defined by Formula Iwherein
the dotted lines between A and C2, C1 and C2, C1 and C7, C7 and C5, C5 and C6, and C8 and C9 indicate that a single or double bond may be present, as valence permits; R1 is a carboxylic acid (—COOH), primary amide (e.g., —CONH2), secondary amide (e.g., —CONHR7), tertiary amide (e.g., —CONR7R7), secondary carbamate (e.g., —OCONHR7; —NHCOOR7), tertiary carbamate (e.g., —OCONR7R7; —NR7COOR7), urea (e.g., —NHCONHR7; —NR7CONHR7; —NHCONR7R7, —NR7CONR7R7), carbinol (e.g., —CH2OH; —CHR7OH, —CR7R7OH), ether (e.g., —OR7), ester (e.g., —COOR7), alcohol (—OH), thiol (—SH), primary amine (—NH2), secondary amine (e.g., —NHR7), tertiary amine (e.g., —NR7R7), thioether (e.g., —SR7, sulfinyl group (e.g., —SORA), sulfonyl group (e.g., —SOOR7), sulfino group, halogen, nitrile, or CF3; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; R2 is hydrogen; hydroxy (—OH), thiol (—SH), ether (e.g., —OR7), thioether (e.g., —SR7), primary amine (—NH2), secondary amine (e.g., —NHR7), tertiary amine (e.g., —NR7R7), primary amide (e.g., —CONH2), secondary amide (e.g., —NHCOR7), tertiary amide (e.g., —NR7COR7), secondary carbamate (e.g., —OCONHR7; —NHCOOR7), tertiary carbamate (e.g., —OCONR7R7; —NR7COOR7), urea (e.g., —NHCONHR7; —NR7CONHR7; —NHCONR7R7, —NR7CONR7R7), sulfinyl group (e.g., —SOR7), sulfonyl group (e.g., —SOOR7) sulfino group, halogen, nitrile, or CF3; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; A is nitrogen or oxygen when a double bond is present between A and C2, or oxygen when a single bond is present between A and C2; R3 is hydrogen, a carbonyl group (e.g., —COR7), or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; R4 is absent when A is oxygen and a double bond is present between A and C2, a hydroxy (—OH) group when A is nitrogen and a double bond is present between A and C2, or is hydrogen, a carbonyl group (e.g., —COR7), or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl when A is oxygen and a single bond is present between A and C2; or A is oxygen, a single bond is present between A and C2, and R3 and R4, taken together with A, C2, C3, and O1, form a 5- to 7-membered ring optionally substituted with between one and four substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, and carboxylic acid; R5 is hydrogen; hydroxy (—OH), thiol (—SH), ether (e.g., —OR7), thioether (e.g., —SR7), primary amine (—NH2), secondary amine (e.g., —NHR7), tertiary amine (e.g., —NR7R7), primary amide (e.g., —CONH2), secondary amide (e.g., —NHCOR7), tertiary amide (e.g., —NR7COR7), secondary carbamate (e.g., —OCONHR7; —NHCOOR7), tertiary carbamate (e.g., —OCONR7R7; —NR7COOR7), urea (e.g., —NHCONHR7; —NR7CONHR7; —NHCONR7R7, —NR7CONR7R7), sulfinyl group (e.g., —SOR7), sulfonyl group (e.g., —SOOR7) sulfino group, halogen, nitrile, or CF3; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; R6 is absent when a double bond is present between C8 and C9, is hydrogen; hydroxy (—OH), thiol (—SH), ether (e.g., —OR7), thioether (e.g., —SR7), primary amine (—NH2), secondary amine (e.g., —NHR7), tertiary amine (e.g., —NR7R7), primary amide (e.g., —CONH2), secondary amide (e.g., —NHCOR7), tertiary amide (e.g., —NR7COR7), secondary carbamate (e.g., —OCONHR7; —NHCOOR7), tertiary carbamate (e.g., —OCONR7R7; —NR7COOR7), urea (e.g., —NHCONHR7; —NR7CONHR7; —NHCONR7R7, —NR7CONR7R7), sulfinyl group (e.g., —SOR7), sulfonyl group (e.g., —SOOR7) sulfino group, halogen, nitrile, or CF3; or an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl when a single bond is present between C8 and C9; or a single bond is present between C8 and C9, and R5 and R6, taken together with C8 and C9, form a cyclopropyl or epoxide ring; and R7, when present, is individually for each occurrence an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl group, optionally substituted with between one and five substituents individually selected from alkyl, cyclopropyl, cyclobutyl ether, amine, halogen, hydroxyl, ether, nitrile, CF3, ester, amide, urea, carbamate, thioether, carboxylic acid, and aryl; or a pharmaceutically acceptable salt or prodrug thereof, wherein the compound is present in a therapeutically effective amount to induce weight loss in a pre-obese, obese, or morbidly obese patient; reduce body fat in a pre-obese, obese, or morbidly obese patient; reduce food intake in a pre-obese, obese, or morbidly obese patient; improve glucose homeostasis in a pre-obese, obese, or morbidly obese patient; or combinations thereof. |
