Publication details

Pyrazolopyrimidines as Cyclin Dependent Kinase Inhibitors

Authors

GUZI Timothy PARUCH Kamil DWYER Michael DOLL Ronald GIRIJAVALLABHAN Viyyoor KNUTSON Chad MCKITTRICK Brian DILLARD Lawrence TRAN Vinh HE Zhen JAMES Ray PARK Haengsoon

Year of publication 2004
Type Patent
MU Faculty or unit

Faculty of Science

Publisher World Intellectual Property Organization
State United States
Patent's number WO 2004/022062 A1
Description The title pyrazolo[1,5-a]pyrimidines [I; Q = SO2NR6R7, CONR6R7, CO2R7; R2 = (un)substituted alkyl, alkynyl, alkynylalkyl, cycloalkyl, CF3, CO2R6, aryl, arylalkyl, heteroarylalkyl, heterocyclyl, etc., wherein aryl is optionally substituted; R3 = H, halogen, NR5R6, CONR5R6, CO2R4, each (un)substituted alkyl, alkynyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl, etc.; R4 = H, halo, alkyl; R5 = H, alkyl; R6 = H, each (un)substituted alkyl, aryl, arylalkyl, cycloalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl; R7 = each (un)substituted alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R5 and R6 in the moiety -NR5R6, may be joined together to form an (un)substituted cycloalkyl or heterocyclyl] or pharmaceutically acceptable salts or solvates thereof are prepd. In its many embodiments, the present invention also provides methods of prepg. such compds., pharmaceutical compns. contg. one or more such compds. I, methods of prepg. pharmaceutical formulations comprising one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with cyclin dependent kinase using such compds. I or pharmaceutical compns. The disease assocd. with cyclin dependent kinase is selected from the group consisting of; (1) cancer of the bladder, breast, colon, kidney, liver, lung, small cell lung cancer, esophagus, gall bladder, ovary, pancreas, stomach, cervix, thyroid, prostate, and skin, including squamous cell carcinoma; (2) leukemia, acute lymphocytic leukemia, acute lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, hairy cell lymphoma and Burkitt's lymphoma; (3) acute and chronic myelogenous leukemia, myelodysplastic syndrome and promyelocytic leukemia; (4) fibrosarcoma and rhabdomyosarcoma; (5) astrocytoma, neuroblastoma, glioma and schwannomas; and (6) melanoma, seminoma, teratocarcinoma, osteosarcoma, xeroderma pigmentosum, keratoacanthoma, thyroid follicular cancer and Kaposi's sarcoma.

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