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US 2008/0269243 A1Published application
Thiadiazole compounds and methods of use
AssigneeAmgen Inc.
InventorsHolger Monenschein, G. Erich Wohlhieter, Qingping Zeng
Life of this patent
Estimating the term…
Abstract
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Claims11
A compound of Formula I
- wherein:
- Y is —N(R4)R5 or —OR5;
- X is O, S, or N(R6);
- R1 is an aryl or heteroaryl;
- R2 and R3 together with the carbon atom to which they are attached join to form a C3-C10 heterocyclic or carbocyclic ring system;
- R4 is —H, C1-C8 alkyl, —C(O)(CR7R8)t)N(R6)2, —C(O)(CR7R8)t, —C(O)2(CR7R8)t, —(CR7R8)t(aryl), —(CR7R8)t(heteroaryl), —(CR7R8)t(cycloalkyl), or —(CR7R8)t(heterocyclyl);
- R5 and R6 are independently selected from —H and C1-C8 alkyl, or R5 and R6 together with the atoms to which they are linked join to form a 5 to 6-membered heterocyclic ring, or
- R4 and R5 together with the nitrogen atom to which they are linked join to form a 5 to 6-membered heterocylic or heteroaryl ring;
- and
- R7 and R8 are independently selected from —H, C1-C6 alkyl, and aryl;
- wherein n is 1;
- m is an integer from 0 to 2;
- and each t is independently an integer from 0 to 3;
- wherein each of the above alkyl, aryl, heteroaryl, cycloalkyl, heterocyclyl moieties and heterocyclic and carbocyclic rings are optionally and independently substituted by 1-3 substituents selected from
- amino,
- aryl, heteroaryl, cycloalkyl, or heterocyclyl optionally substituted by 1-5 substituents selected from
- C1-C6 alkoxy,
- C1-C6 alkyl optionally substituted by halo,
- aryl,
- halo,
- heteroaryl,
- C1-C6 hydroxyl, and
- —NHS(O)2—C6 alkyl);
- C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 alkoxy, C1-C6 alkylamino,
- C2-C6 alkenyl, or C2-C6 alkynyl, wherein each of which may be interrupted by one or more hetero atoms,
- cyano,
- halo,
- hydroxy,
- nitro, or
- —O-aryl;
- or a pharmaceutically acceptable salt, hydrate, or stereoisomer thereof.
28 more elements
A pharmaceutical composition comprising a pharmaceutically-acceptable carrier and a
Dependencies are inferred from the claim text.