Patent ID: 9216180
Filing Date: 2015-12-22
Classification: A61K,A61P,G01N,G16B,G16C,Y02A

Abstract:
1. A pharmaceutical composition comprising: a compound of the formula (I): a stereoisomer, pharmaceutically acceptable salt, oxide, solvate, or ester thereof, wherein A is selected from the group consisting of: (1) absent; (2) —O—; (3) —CR (4) —S—; (5) —CHR (6) —NR (7) substituted or unsubstituted C (8) substituted or unsubstituted arylene; (9) substituted or unsubstituted heterocyclylene; and (10) substituted or unsubstituted heteroarylene wherein the substituents of A are selected from the group consisting of halogen, OH, CN, NO 2 , C(O), NH 2 , H, C 1-6 alkyl, C 1-6 alkyl substituted with a —COOH, C 2-6 alkenyl, C 2-6 alkynyl, C 4-7 cycloalkylalkyl, and monocyclic aryl; B is selected from the group consisting of: (1) absent; (2) —O—; (3) —CR (4) —NH—C(O)—; (5) —C(S)—NH—; (6) —N═CH—; (7) substituted or unsubstituted C (8) substituted or unsubstituted arylene; (9) substituted or unsubstituted heterocyclylene; and (10) substituted or unsubstituted heteroarylene wherein the substituents of B are selected from the group consisting of halogen, OH, CN, NO 2 , C(O), NH 2 , H, C 1-6 alkyl, C 1-6 alkyl substituted with a —COOH, C 2-6 alkenyl, C 2-6 alkynyl, C 4-7 cycloalkylalkyl, and monocyclic aryl; L 1 to L 4 are independently selected from the group consisting of: (1) absent; (2) —S (3) —S (4) —S (5) —C(S)—NH—; and (6) —NH—; X is C or N; Z is C, O, or S; Y is C or absent; R 1 is absent or, if present, is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, OR 16 , C(O)NR 17 R 18 , NR 19 C(O)R 20 ; R 2 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, OR 16 , NO 2 , C(O)N 17 R 18 , NR 19 C(O)R 20 , heterocyclyl or heteroaryl containing 1-5 heteroatoms selected from the group consisting of nitrogen, sulfur, and oxygen; R 3 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, OR 16 , C(O)NR 17 R 18 , C(O)OR 16 , NR 19 C(O)R 20 ; R 4 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, OR 16 , C(O)OR 16 , C(O)NR 17 R 18 , NR 19 C(O)R 16 , heteroaryl containing 1-5 heteroatoms selected from the group consisting of nitrogen, sulfur, and oxygen; R 5 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, OR 16 , C(O)OR 16 ; R 6 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, OR 16 , NR 17 R 18 , heteroaryl or heterocyclyl containing 1-5 heteroatoms selected from the group consisting of nitrogen, sulfur, and oxygen, N═NR 15 ; R 7 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, OR 16 , NO 2 , NR 19 C(O)R 20 , S(O) 2 NR 17 R 18 ; R 8 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, OR 16 , NR 19 C(O)R 20 ; R 9 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, NO 2 , OR 16 , S(O) 2 NR 21 R 22 ; R 10 is H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, halogen, NR 17 R 18 , OR 16 ; R 1 to R 10 are each optionally substituted 1 to 3 times with substituents selected from the group consisting of halogen, —OH, —OR 21 , —C(O)R 21 , —C(O)OR 21 , C(O)NR 21 R 22 , —NHR 21 , —NR 21 R 22 , —SR 21 , —S(O)R 21 , —S(O) 2 R 21 , NH 2 , CN, NO 2 , C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 4-7 cycloalkylalkyl, mono- or polycyclic aryl, and mono- or polycyclic heteroaryl containing 1 to 5 heteroatoms selected from the group consisting of nitrogen, sulfur, and oxygen and, optionally, oxy substituted; R 11 is H, C 1-6 alkyl, C 2-6 alkenyl, C 3-6 alkynyl, NR 19 C(O)R 20 ; R 12 is H, C 1-6 alkyl, C 2-6 alkenyl, C 3-6 alkynyl, C(O)OR 16 ; R 13 is NHNH; R 14 is C(O)OR 21 ; R 10 and R 12 can combine to form a —NH—C(O)— group; R 13 and R 15 can combine to form a —N—N═N— group; R 15 to R 22 are independently H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 4-7 cycloalkylalky, C 1-6 alkoxy, carboxy, a monocyclic or polycyclic aryl, or a monocyclic or polycyclic heterocyclyl or heteroaryl containing 1-5 heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur, each R 15 to R 22 optionally substituted from 1-3 times with substituents selected from the group consisting of halogen, oxy, OH, CN, NO 2 , —C(O), NH 2 , H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 4-7 cycloalkylalkyl, O-aryl substituted with C 1-6 alkyl, C(O)NHCH 2 -heterocyclyl with 1-5 oxygen, sulfur, or nitrogen heteroatoms, heteroaryl with 1-5 heteroatoms selected from the group consisting of oxygen, sulfur, or nitrogen heteroatoms, —S—C 1-6 alkyl, and a monocyclic aryl; R 21 and R 22 can combine to form a 3-7-membered mono- or polycyclic heterocycle or mono- or polycyclic heteroaryl each containing 1-5 heteroatoms selected from the group consisting of nitrogen, sulfur, and oxygen, where the heterocycle or heteroaryl are optionally substituted from 1 to 3 times with substituents selected from the group consisting of halogen, OH, CN, NO 2 , NH 2 , C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 4-7 cycloalkylalkyl, a monocyclic aryl, and monocyclic heteroaryl; and a pharmaceutically acceptable carrier.