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US 6,294,575 B1Granted
BTK inhibitors and methods for their identification and use
AssigneeParker Hughes Institute
InventorsFatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
Life of this patent
Estimating the term…
Abstract
The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.
Claims6
A method for treating allergy comprising administering to a patient a therapeutically effective amount of a leflunomide analog of formula I:
- where:
- R1 is (C1-C3)alkyl, (C3-C6)cycloalkyl, phenyl, or NRaRb;
- R2 is hydroxy, (C1-C6)alkoxy (C1-C6)alkanoyloxy amino (C2-C5)alkoxy;
- hydroxy (C2-C5)alkoxy amino (C2-C5)alkanoxy;
- or hydroxy (C2-C5) alkanoxy;
- R3 is cyano or (C1-C3)alkanoyl;
- R4 is hydrogen, (C1-C3)alkyl;
- hydroxy (C2-C5)alkyl;
- or amino (C2-C5)alkyl;
- R5 is aryl, or heteroaryl;
- Ra and Rb are each independently hydrogen, or (C1-C3)alkyl;
- or Ra and Rb together with the nitrogen to which they are attached are pyrrolidino, piperidino, morpholino, or thiomorpholino;
- wherein any aryl, or heteroaryl of R1 and R5 is optionally substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, (C1-C3)alkoxy, (C1-C3)alkyl, (C1-C3)alkanoyl, —S(O)2Rc, or NRaRb wherein Rc is (C1-C3)alkyl, or aryl
- or a pharmaceutically acceptable salt thereof;
- provided that if R5 is phenyl, the phenyl is substituted by —S(O)2Rc, or is substituted by halo and at least one other substituent.
12 more elements
A method for treating anaphylactic shock comprising administering to a patient a therapeutically effective amount of a leflunomide analog of formula I:
- where:
- R1 is (C1-C3)alkyl, (C3-C6)cycloalkyl, phenyl, or NRaRb;
- R2 is hydroxy, (C1-C6)alkoxy (C1-C6)alkanoyloxy amino (C2-C5)alkoxy;
- hydroxy (C2-C5)alkoxy amino (C2-C5)alkanoxy;
- or hydroxy (C2-C5) alkanoxy;
- R3 is cyano or (C1-C3)alkanoyl;
- R4 is hydrogen, (C1-C3)alkyl;
- hydroxy (C2-C5)alkyl;
- or amino (C2-C5)alkyl;
- R5 is aryl, or heteroaryl;
- Ra and Rb are each independently hydrogen, or (C1-C3)alkyl;
- or Ra and Rb together with the nitrogen to which they are attached are pyrrolidino, piperidino, morpholino, or thiomorpholino;
- wherein any aryl, or heteroaryl of R1 and R5 is optionally substituted with one or more substituents independently selected from halo, nitro, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, (C1-C3)alkoxy, (CC3)alkyl, (C1-C3)alkanoyl, —S(O)2Rc, or NRaRb, wherein Rc is (C1-C3)alkyl, or aryl
- or a pharmaceutically acceptable salt thereof;
- provided that if R5 is phenyl, the phenyl is substituted by —S(O)2Rc, or is substituted by halo and at least one other substituent.
12 more elements
Dependencies are inferred from the claim text.