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Last Updated: March 28, 2024

Claims for Patent: 7,196,092


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Summary for Patent: 7,196,092
Title:N-heteroaryl 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)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:11/244,776
Patent Claims:1. A compound of the formula: ##STR00519## wherein R.sup.18 is an alkyl or heterocyclyl with said heterocyclyl being linked to the isothiazole ring shown in the formula above via a carbon atom on said heterocyclyl, or a pharmaceutically acceptable salt, solvate, ester or prodrug of said compound.

2. The compound of claim 1, wherein R.sup.18 is methyl.

3. The compound of claim 1, wherein said heterocyclyl is selected from the group consisting of: ##STR00520##

4. The compound of claim 3, wherein said heterocyclyl is: ##STR00521##

5. A compound of formula: ##STR00522## or a pharmaceutically acceptable salt, solvate, ester or prodrug of said compound.

6. A method of inhibiting cyclin dependent kinases2 (CDK2) in a patient, comprising administering a therapeutically effective amount of the compound of claim 1, or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, to said patient.

7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1, or a pharmaceutically acceptable salt, ester or prodrug thereof, in combination with at least one pharmaceutically acceptable carrier.

8. The pharmaceutical composition of claim 7, additionally comprising one or more anti-cancer agents selected from the group consisting of cytostatic agent, taxotere, taxol, etoposide, irinotecan, camptostar, topotecan, paclitaxel, docetaxel, epothilones, tamoxifen, 5-fluorouracil, methoxtrexate, temozolomide, cyclophosphamide, SCH 66336, R115777, L778,123, BMS 214662, 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, 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.RTM. (cetuximab), Liposomal, Thiotepa, Altretamine, Melphalan, Trastuzumab, Lerozole, Fulvestrant, Exemestane, Fulvestrant, Ifosfomide, Rituximab, C225, and Campath.

9. A method of inhibiting cyclin dependent kinases2 (CDK2) in a patient, comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 7 to said patient.

Details for Patent 7,196,092

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Recordati Rare Diseases, Inc. ELSPAR asparaginase For Injection 101063 01/10/1978 ⤷  Try a Trial 2022-09-04
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 06/04/1986 ⤷  Try a Trial 2022-09-04
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 ⤷  Try a Trial 2022-09-04
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b Injection 103132 ⤷  Try a Trial 2022-09-04
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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