Claims for Patent: 7,196,078

Summary for Patent: 7,196,078

Title:	Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
Abstract:	In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Inventor(s):	Guzi; Timothy J. (Chatham, NJ), Paruch; Kamil (Garwood, NJ), Dwyer; Michael P. (Scotch Plains, NJ), Labroli; Marc (Mount Laurel, NJ), Keertikar; Kartik M. (East Windsor, NJ)
Assignee:	Schering Corpoartion (Kenilworth, NJ)
Application Number:	11/245,401
Patent Claims:	1. A compound selected from the group consisting of the compounds of the formula: ##STR05216## ##STR05217## ##STR05218## ##STR05219## ##STR05220## ##STR05221## ##STR05222## ##STR05223## ##STR05224## ##STR05225## ##STR05226## ##STR05227## ##STR05228## or a pharmaceutically acceptable salt, ester or prodrug thereof. 2. A method of inhibiting a cyclin dependent kinase in a patient, comprising administering a therapeutically effective amount of at least one compound of claim 1, or a pharmaceutically acceptable salt, ester or prodrug thereof, to said patient, wherein said cyclin dependent kinase is CDK1 or CDK2. 3. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound of claim 1, or a pharmaceutically acceptable salt, ester or prodrug thereof, in combination with at least one pharmaceutically acceptable carrier. 4. The pharmaceutical composition of claim 3, additionally comprising one or more anti-cancer agents selected from the group consisting of a cytostatic agent, taxotere, taxol, etoposide, irinotecan, camptostar, topotecan, paclitaxel, docetaxel, epothilones, tamoxifen, 5-fluorouracil, methoxtrexate, temozolomide, cyclophosphamide, SCH 66336, R115777, L778,123, BMS214662, Iressa.RTM., (gefitinib) Tarceva.RTM. (erlotinib hydrochloride), antibodies to EGFR, Gleevec.RTM. (imatinib), intron, ara-C, adriamycin, cytoxan, gemcitabine, Uracil mustard, Chlormethine, Ifosfamide, Melphalan, Chlorambucil, Pipobroman, Triethylenemelamine, Triethylenethiophosphoramine, Busulfan, Carmustine, Lomustine, Streptozocin, Dacarbazine, Floxuridine, Cytarabine, 6-Mercaptopurine, 6-Thioguanine, Fludarabine phosphate, oxaliplatin, leucovirin, ELOXATIN.TM., Pentostatine, Vinblastine, Vincristine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mithramycin, Deoxycoformycin, Mitomycin-C, L-Asparaginase, Teniposide 17.alpha.-Ethinylestradiol, Diethylstilbestrol, Testosterone, Prednisone, Fluoxymesterone, Dromostanolone propionate, Testolactone, Megestrolacetate, Methylprednisolone, Methyltestosterone, Prednisolone, Triamcinolone, Chlorotrianisene, Hydroxyprogesterone, Aminoglutethimide, Estramustine, Medroxyprogesteroneacetate, Leuprolide, Flutamide, Toremifene, goserelin, Cisplatin, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine, Hexamethylmelamine, Avastin, herceptin, Bexxar, Velcade, Zevalin, Trisenox, Xeloda, Vinorelbine, Porfimer, Erbitux, Liposomal, Thiotepa, Altretamine, Melphalan, Trastuzumab, Lerozole, Fulvestrant, Exemestane, Fulvestrant, Ifosfomide, Rituximab, C225.RTM., and Campath. 5. A method of inhibiting a cyclin dependent kinase in a patient, comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 3 to said patient, wherein said cyclin dependent kinase is CDK1 or CDK2. 6. A pharmaceutical composition comprising (i) a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt, ester or prodrug thereof, and (ii) temozolomide. 7. A method of inhibiting a cyclin dependent kinase, comprising administering the pharmaceutical composition of claim 6 wherein said cyclin dependent kinase is CDK1 or CDK2. 8. A compound of the formula: ##STR05229## or a pharmaceutically acceptable salt, ester or prodrug thereof. 9. A compound of the formula: ##STR05230## or a pharmaceutically acceptable salt, ester or prodrug thereof. 10. A compound of the formula: ##STR05231## or a pharmaceutically acceptable salt, ester or prodrug thereof. 11. A compound of the formula: ##STR05232## or a pharmaceutically acceptable salt, ester or prodrug thereof. 12. A compound of the formula: ##STR05233## or a pharmaceutically acceptable salt, ester or prodrug thereof. 13. A compound of the formula: ##STR05234## or a pharmaceutically acceptable salt, ester or prodrug thereof. 14. A compound of the formula: ##STR05235## or a pharmaceutically acceptable salt, ester or prodrug thereof. 15. A compound of the formula: ##STR05236## or a pharmaceutically acceptable salt, ester or prodrug thereof. 16. A compound of the formula: ##STR05237## or a pharmaceutically acceptable salt, ester or prodrug thereof. 17. A compound of the formula: ##STR05238## or a pharmaceutically acceptable salt, ester or prodrug thereof. 18. A compound of the formula: ##STR05239## or a pharmaceutically acceptable salt, ester or prodrug thereof. 19. A compound of the formula: ##STR05240## or a pharmaceutically acceptable salt, ester or prodrug thereof. 20. A compound of the formula: ##STR05241## or a pharmaceutically acceptable salt, ester or prodrug thereof. 21. A compound of the formula: ##STR05242## or a pharmaceutically acceptable salt, ester or prodrug thereof. 22. A compound of the formula: ##STR05243## or a pharmaceutically acceptable salt, ester or prodrug thereof. 23. A compound of the formula: ##STR05244## or a pharmaceutically acceptable salt, ester or prodrug thereof. 24. A compound of the formula: ##STR05245## or a pharmaceutically acceptable salt, ester or prodrug thereof. 25. A compound of the formula: ##STR05246## or a pharmaceutically acceptable salt, ester or prodrug thereof. 26. A compound of the formula: ##STR05247## or a pharmaceutically acceptable salt, ester or prodrug thereof. 27. A compound of the formula: ##STR05248## or a pharmaceutically acceptable salt, ester or prodrug thereof. 28. A composition comprising (i) a compound of any of claims 8 27 and (ii) temozolomide. 29. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any of claims 8 27, or a pharmaceutically acceptable salt, ester or prodrug thereof, in combination with at least one pharmaceutically acceptable carrier.

Details for Patent 7,196,078

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	01/10/1978		2022-09-04
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132	06/04/1986		2022-09-04
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132			2022-09-04
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	Injection	103132			2022-09-04
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2022-09-04