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US 8,076,331 B2Granted
Substituted pyridazine derivatives
AssigneeCephalon, Inc.
InventorsRobert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
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Abstract
The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
Claims30
A compound of Formula I:
- wherein:
- R1 is H, —OR7, —SR7, —SOR7, —SO2R7, —NR9R10, halogen, C1-4 alkyl, C4-10 cycloalkyl, C1-4 haloalkyl, C6-12 aryl, 5-10 membered heteroaryl, or 3-10 membered heterocycloalkyl, wherein each of said C1-4 alkyl, C4-10 cycloalkyl, C1-4 haloalkyl, C6-12 aryl, 5-10 membered heteroaryl, and 3-10 membered heterocycloalkyl is optionally substituted by 1, 2, or 3 R11;
- R2 and R3 are independently H or C1-4 alkyl;
- or R2 and R3 are taken together to form a C4-10 cycloalkyl or phenyl, wherein each of said C4-10 cycloalkyl and phenyl is optionally substituted by 1, 2, or 3 halogen or C1-4 alkyl;
- each R4 is independently H or C1-4 alkyl or OH;
- each R5 is independently C1-4 alkyl, or hydroxyalkyl;
- each R6 is independently halogen, C1-4 haloalkyl, —OH, C1-4 alkyl, —O—C1-4 alkyl, —NR9R10, or CN;
- R7 is C1-4 alkyl, C4-10 cycloalkyl, 5-10 membered heteroaryl, C6-12 aryl,
- C6-12 arylC1-6alkyl, 5-10 membered heteroarylalkyl, or a 3-10 membered heterocycloalkyl;
- R9 and R10 are independently H, C1-4 alkyl, or arylalkyl;
- each R11 is halogen, —OH, —OC1-4 alkyl, C1-4 alkyl, C1-4 haloalkyl, or —CN;
- X is O or S;
- m is 2, 3, 4, 5, or 6;
- n is 0, 1, or 2;
- y is 0, 1, 2, 3, or 4;
- z is 0, 1, 2, 3, or 4;
- or a stereoisomer or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.