Oxypiperidine derivatives and methods of use thereof
AssigneeSchering Corporation
InventorsJianhua Chao, Robert G. Aslanian
Life of this patent
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Abstract
The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.
Claims33
A compound having the structure:
- or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, wherein:
- Y is a bond, -alkylene-, —C(O)—, —OC(O)— or —NHC(O)—;
- R1 is aryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl or heteroaryl, wherein an aryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl or heteroaryl group can be optionally substituted with up to 3 substituents, which can be the same or different, and are selected from alkyl, —O-alkyl, halo, haloalkyl, —O-haloalkyl, —CN, —C(O)OR3, —N(R4)2, —C(O)N(R4)2, —C(O)R5, —NHC(O)R5, —NHS(O)2R3 or —S(O)2N(R4)2, and wherein R1 is cycloalkyl, the cycloalkyl group can be optionally fused to an aryl or heteroaryl ring;
- R2 is aryl, heterocycloalkyl, heterocycloalkenyl or heteroaryl, wherein an aryl, heterocycloalkyl, heterocycloalkenyl or heteroaryl group can be optionally substituted with up to 3 substituents, which can be the same or different, and are selected from alkyl, cycloalkyl, heterocycloalkyl, heteroaryl, —O-alkyl, —O-aryl, halo, haloalkyl, —O-haloalkyl, —CN, —OC(O)R5, —C(O)OR3, —N(R4)2, —C(O)N(R4)2, —C(O)R5, —NHC(O)R5, —NHS(O)2R3 or —S(O)2N(R4)2;
- each occurrence of R3 is independently H, alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl;
- each occurrence of R4 is independently H, alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl;
- each occurrence of R5 is independently H, alkyl, aryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, —O-alkyl, —NH-alkyl, —O-aryl or —NH-aryl;
- p is an integer ranging from 0 to 2;
- q is an integer ranging from 0 to 2;
- r is an integer ranging from 0 to 2;
- and
- s is an integer ranging from 0 to 2.
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A compound having the structure:
- or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof.
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Dependencies are inferred from the claim text.