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Last Updated: October 21, 2019

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Claims for Patent: 8,586,576

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Summary for Patent: 8,586,576
Title:Substituted pyrazolo[1,5-a]pyrimidines 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: Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:11/710,644
Patent Claims:1. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a patient in need thereof comprising administering a therapeutically effective amount of at least one compound, or a pharmaceutically acceptable salt thereof, to said patient, wherein said compound is selected from the group consisting of the compounds of the formulas: ##STR05219## ##STR05220## ##STR05221## ##STR05222## ##STR05223## ##STR05224## ##STR05225## ##STR05226## ##STR05227## ##STR05228## ##STR05229## ##STR05230## ##STR05231## ##STR05232## ##STR05233##

2. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a mammal in need thereof, comprising administering to said mammal an amount of a first compound, or a pharmaceutically acceptable salt thereof; and an amount of at least one second compound, said second compound being an anti-cancer agent; wherein the amounts of the first compound and said second compound result in a therapeutic effect, wherein said first compound is selected from the group consisting of the compounds of the formulas: ##STR05234## ##STR05235## ##STR05236## ##STR05237## ##STR05238## ##STR05239## ##STR05240## ##STR05241## ##STR05242## ##STR05243## ##STR05244## ##STR05245## ##STR05246## ##STR05247## ##STR05248##

3. The method of claim 2, further comprising radiation therapy.

4. The method of claim 2, wherein said anti-cancer agent is selected from the group consisting of a cytostatic agent, cisplatin, doxorubicin, taxotere, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilones, tamoxifen, 5-fluorouracil, methoxtrexate, temozolomide, cyclophosphamide, 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta- [1,2-b]pyridin-11-yl-]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide, tipifarnib, L778,123 (a farnesyl protein transferase inhibitor), BMS 214662 (a farnesyl protein transferase inhibitor), gefitinib, erlotinib, antibodies to EGFR, imatinib, interferon alfa-2b, aramycin, 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, Pentostatine, Vinblastine, Vincristine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, 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, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine, Hexamethylmelamine, bevacuzimab, tositumomab, bortezomib, ibritumomab tiuxetan, arsenic trioxide, Vinorelbine, Porfimer, Liposomal, Thiotepa, Altretamine, Melphalan, Trastuzumab, Lerozole, Fulvestrant, Exemestane, Fulvestrant, lfosfomide, Rituximab, cetuximab, and alemtuzumab.

5. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a mammal in need thereof, comprising administering to said mammal an amount of a first compound, or a pharmaceutically acceptable salt thereof; and an amount of temozolomide: wherein the amounts of the first compound and said temozolomide result in a therapeutic effect, wherein said first compound is selected from the group consisting of the compounds of the formulas: ##STR05249## ##STR05250## ##STR05251## ##STR05252## ##STR05253## ##STR05254## ##STR05255## ##STR05256## ##STR05257## ##STR05258## ##STR05259## ##STR05260## ##STR05261## ##STR05262## ##STR05263## ##STR05264## ##STR05265##

6. The method of claim 5, further comprising radiation therapy.

7. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a mammal in need thereof, comprising administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, wherein said compound is selected from the group consisting of the compounds of the formulas: ##STR05266## ##STR05267## ##STR05268## ##STR05269## ##STR05270## ##STR05271## ##STR05272## ##STR05273## ##STR05274## ##STR05275## ##STR05276## ##STR05277## ##STR05278## ##STR05279## ##STR05280## ##STR05281## ##STR05282##

8. The method of claim 7, further comprising administering radiation therapy.

9. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a mammal in need thereof, comprising administering to said mammal a pharmaceutical composition comprising (i) a therapeutically effective amount of a first compound, or a pharmaceutically acceptable salt thereof, and (ii) an anti-cancer agent, wherein the amounts of said first compound and anti-cancer agent result in therapeutic effect, further wherein said first compound is selected from the group consisting of the compounds of the formulas: ##STR05283## ##STR05284## ##STR05285## ##STR05286## ##STR05287## ##STR05288## ##STR05289## ##STR05290## ##STR05291## ##STR05292## ##STR05293## ##STR05294## ##STR05295## ##STR05296## ##STR05297## ##STR05298## ##STR05299##

10. The method of claim 9, wherein said anti-cancer agent is selected from the group consisting of a cytostatic agent, cisplatin, doxorubicin, taxotere, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilones, tamoxifen, 5-fluorouracil, methoxtrexate, temozolomide, cyclophosphamide, 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta- [1,2-b]pyridin-11-yl-]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide, tipifarnib, L778,123 (a farnesyl protein transferase inhibitor), BMS 214662 (a farnesyl protein transferase inhibitor), gefitinib, erlotinib, antibodies to EGFR, imatinib, interferon alfa-2b, aramycin, 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, Pentostatine, Vinblastine, Vincristine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, Epirubicin, Idarubicin, Mithramycin, Deoxycoformycin, Mitomycin-C, L-Asparaginase, Teniposide 17.alpha.-Ethlnylestradiol, Diethylstilbestrol, Testosterone, Prednisone, Fluoxymesterone, Dromostanolone propionate, Testolactone, Megestrolacetate, Methylprednisolone, Methyltestosterone, Prednisolone, Triamcinolone, Chlorotrianisene, Hydroxyprogesterone, Aminoglutethimide, Estramustine, Medroxyprogesteroneacetate, Leuprolide, Flutamide, Toremifene, goserelin, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine, Hexamethylmelamine, bevacuzimab, tositumomab, bortezomib, ibritumomab tiuxetan, arsenic trioxide, capecitabine, Vinorelbine, Porfimer, Liposomal, Thiotepa, Altretamine, Melphalan, Trastuzumab, Lerozole, Fulvestrant, Exemestane, Fulvestrant, Ifosfomide, Rituximab cetuximab, and alemtuzumab.

11. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia in a patient in need thereof, comprising administering to said patient a pharmaceutical composition comprising a therapeutically effective amount of at least one compound, or a pharmaceutically acceptable salt thereof, to said patient, wherein said compound is selected from the group consisting of the compounds of the formulas: ##STR05300## ##STR05301## ##STR05302## ##STR05303## ##STR05304## ##STR05305## ##STR05306## ##STR05307## ##STR05308## ##STR05309## ##STR05310## ##STR05311## ##STR05312## ##STR05313## ##STR05314## ##STR05315## ##STR05316##

12. The method of claim 11, wherein said pharmaceutical composition further comprises an anti-cancer agent.

13. The method of claim 11, further comprising administration of radiation therapy.

14. The method of claim 12, wherein said anti-cancer agent is selected from the group consisting of a cytostatic agent, cisplatin, doxorubicin, taxotere, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilones, tamoxifen, 5-fluorouracil, methoxtrexate, temozolomide, cyclophosphamide, 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta- [1,2-b]pyridin-11-yl-]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide, tipifarnib, L778,123 (a farnesyl protein transferase inhibitor), BMS 214662 (a farnesyl protein transferase inhibitor), gefitinib, erlotinib, antibodies to EGFR, imatinib, interferon alfa-2b, aramycin, 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, Pentostatine, Vinblastine, Vincristine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, 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, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine, Hexamethylmelamine, bevacuzimab, tositumomab, bortezomib, ibritumomab tiuxetan, arsenic trioxide, capecitabine, Vinorelbine, Porfimer, Liposomal, Thiotepa, Altretamine, Melphalan, Trastuzumab, Lerozole, Fulvestrant, Exemestane, Fulvestrant, Ifosfomide, Rituximab, cetuximab, and alemtuzumab.

15. A method of treating a cancer selected from the group consisting of breast cancer, non-small cell lung cancer (NSCLC), acute myelogenous leukemia (AML), acute lymphoblastic leukemia (ALL), and mantle cell leukemia d3 in a patient in need thereof comprising administering a therapeutically effective amount of at least one compound selected from the group consisting of ##STR05317## or a pharmaceutically acceptable salt thereof.

Details for Patent 8,586,576

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10   Start Trial Merck Sharp & Dohme Corp. (Rahway, NJ) 2022-09-04 RX search
Schering INTRON A interferon alfa-2b VIAL 103132 001 1986-06-04   Start Trial Merck Sharp & Dohme Corp. (Rahway, NJ) 2022-09-04 RX search
Schering INTRON A interferon alfa-2b VIAL 103132 002 1986-06-04   Start Trial Merck Sharp & Dohme Corp. (Rahway, NJ) 2022-09-04 RX search
Schering INTRON A interferon alfa-2b VIAL 103132 003 1986-06-04   Start Trial Merck Sharp & Dohme Corp. (Rahway, NJ) 2022-09-04 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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