7-heterocyclyl quinoline and thieno[2,3-b]yridine derivatives useful as antagonists of gonadotropin releasing hormone

A compound of the formula (I)

• wherein
• L1 is selected from the group consisting of CH2, CH(CH3) and C(CH3)2;
• R1 and R2 are independently selected from the group consisting of alkyl, cycloalkyl, aryl, aralkyl, heteroaryl and heterocycloalkyl;
• wherein the aryl, heteroaryl or heterocycloalkyl group is optionally substituted with one or more substituents independently selected from halogen, alkyl, alkoxy, nitro, NH2, NH(alkyl), N(alkyl)2, —C(O)-alkyl, —C(O)-aryl or —C(O)-cycloalkyl;
• X is selected from the group consisting of O, S and NRA;
• where RA is selected from hydrogen, alkyl, aryl or aralkyl;
• R4 is selected from the group consisting of —C(O)—RB, —C(O)O—RB, —C(O)NH2, —C(O)—NHRB, —C(O)—N(RB)2, and —C(O)NHNH2;
• wherein RB is selected from the group consisting of alkyl, aryl, aralkyl and cycloalkyl;
• alternatively X is N and is taken together with R4 to form a ring structure selected from the group consisting of pyrazolyl, dihydropyrazolyl, isoxazolinyl and dihydropyrimidinyl;
• wherein the ring structure is optionally substituted with one or more RC;
• wherein each RC is independently selected from the group consisting of oxo, alkyl, alkoxy, amino, alkylamino, dialkylamino, aryl, —O-aryl, aralkyl and —O-aralkyl;
• L2 is selected from the group consisting of alkyl;
• R3 is selected from the group consisting of alkyl, cycloalkyl, aryl, aralkyl, heteroaryl and heterocycloalkyl;
• wherein the cycloalkyl, aryl, aralkyl, heteroaryl or heterocycloalkyl group is optionally substituted with one or more substituents independently selected from halogen, alkyl, alkoxy, nitro, NH2, NH(alkyl), N(alkyl)2, cyano or sulfonamido;
• R5 is selected from the group consisting of halogen, cycloalkyl, aryl, aralkyl, heteroaryl or heterocycloalkyl;
• wherein the cycloalkyl, aryl, aralkyl, heteroaryl or heterocycloalkyl group is optionally substituted with one or more substituents selected from halogen, alkyl, alkoxy, nitro, NH2, NH(alkyl), N(alkyl)2, cyano or sulfonamido;
• provided that when X is O, then R5 is selected from the group consisting of heteroaryl or heterocycloalkyl;
• wherein the heteroaryl or heterocycloalkyl group is optionally substituted with one or more substituents selected from halogen, alkyl, alkoxy, nitro, NH2, NH(alkyl), N(alkyl)2, cyano or sulfonamido;
• and pharmaceutically acceptable salts, esters and pro-drugs thereof.