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Last Updated: March 28, 2024

Claims for Patent: 8,591,943


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Summary for Patent: 8,591,943
Title:Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors
Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
Inventor(s): Deng; Yongqi (Newton, MA), Sun; Binyuan (Chestnut Hill, MA), Zeng; Hongbo (Westford, MA), Richards; Matthew (Somerville, MA), Shipps, Jr.; Gerald W. (Stoneham, MA), Cheng; Cliff C. (Cambridge, MA), Zhao; Yinyan (Rockville, MD), McRiner; Andrew (Melrose, MA), Meng; Zhaoyang (Lansdale, PA), Nan; Yang (Lansdale, PA), Patel; Mehul F. (Willow Grove, PA), Wrona; Iwona E. (Sharon, MA), Reddy; Panduranga Adulla (Walpole, MA), Eklov; Brian M. (Kalamazoo, MI), Tang; Shuyi (Belmont, MA), Liu; Duan (Arlington, MA), Mandal; Amit K. (Shrewsbury, MA), Zhao; Lianyun (Blue Bell, PA), Siddiqui; M. Arshad (Newton, MA)
Assignee: Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:13/263,193
Patent Claims:1. A method of treating a disease by inhibiting a mTOR, comprising administering to a patient in need of such treatment an amount of a first compound represented by the structural Formula I: ##STR01967## or a pharmaceutically acceptable salt, or ester thereof, wherein: R is independently selected from the group consisting of halo, hydroxyl, amino, --CN, H, --(C.sub.1-C.sub.6)alkyl, alkoxy, --C(.dbd.O)alkyl, heteroaryl and aryl, wherein each of said heteroaryl and aryl can be unsubstituted or substituted with one or more alkyl or halo; R.sup.1 is independently selected from the group consisting of heterocycloalkyl, spiroheterocycloalkyl, heterocyclenyl, --NR.sup.3R.sup.4, cycloalkyl, heteroaryl, aryl, alkynyl, heterocyclenylalkyl, cycloalkylalkyl, heteroarylalkyl, heteroarylalkynyl, --N-heteroaryl, and arylalkyl, wherein each of said heterocycloalkyl, spiroheterocycloalkyl, heterocyclenyl, cycloalkyl, heteroaryl, aryl, alkynyl, heterocyclenylalkyl, cycloalkylalkyl, heteroarylalkyl, heteroarylalkynyl, --N-heteroaryl and arylalkyl can be unsubstituted or substituted with one or moieties independently selected from the group X; X is alkoxyl, alkyl, --C(O)alkyl, --C(O)-hydroxyalkyl, --C(O).sub.2alkyl, --C(O).sub.2H, hydroxyalkyl, --S(O).sub.2alkyl, hydroxyl, heterocycloalkyl, --NH-heterocycloalkyl, -trihaloalkyl, -dihaloalkyl, -monohaloalkyl, --N--S(O).sub.2-alkyl, --C(O)-heteroaryl, -alkyl-C(O).sub.2H, -alkyl(CO)N(CH.sub.3)--O--CH.sub.3, -alkyl(CO)-heteroaryl, --C(O).sub.2-alkyl, -alkyl-C(O)--NH.sub.2, --NH.sub.2, heteroaryl, -alkyl-CN, --C(O).sub.2-arylalkyl, halo, carboxyesteralkyl, --C(O)--NH.sub.2, -alkyl-C(O).sub.2alkyl, heteroarylalkyl, --C(O)-heteroaryl, --C(O)-alkyl-O-alkyl, -alkyl(CO)NS(O).sub.2-cycloalkyl, -alkyl(CO)N--S(O).sub.2--CF.sub.3, --N-alkyl, --SO.sub.2-cycloalkyl, -alkyl(CO)NS(O).sub.2-alkyl, -alkyl-C(O)--N(alkyl).sub.2, -alkyl-NS(O).sub.2-alkyl, alkyl(CO)NS(O).sub.2-cycloalkyl, --CO--CO.sub.2H, --C(O).sub.2-alkyl-aryl, --SO.sub.2--CF.sub.3 or --C(O)H, wherein each of said heterocycloalkyl, heteroaryl or --C(O)-heteroaryl can be unsubstituted or substituted with one or more alkyl; R.sup.2 is pyridyl optionally substituted with one or more moieties independently selected from the group consisting of alkyl, alkoxyl, --CN, aryloxyl, aryl, halo, hydroxyl, --C(CH.sub.3).sub.2CN, trifluoromethyl, difluoromethyl, monofluoromethyl, heterocycloalkyl, and arylalkyl; R.sup.3 is cycloalkyl or heteroaryl, wherein each of said cycloalkyl or heteroaryl can be unsubstituted or substituted with one or more moieties independently selected from the group consisting of X; and R.sup.4 is H; and optionally 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.

2. The method according to claim 1, wherein the one or more anti-cancer agents are selected from the group consisting of Adriamycin, Altretamine, Amidox, Aminoglutethimide, Amsacrine, Anastrazole, Antibodies to EGFR, 3-AP, Aphidicolon, Ara-C, Arsenic trioxide, L-Asparaginase, Bevacizumab, Bleomycin, BMS 214662, Bortezomib, Busulfan, Campath, Camptostar, Capecitabine, Carboplatin, Carmustine, Centrosome associated protein E ("CENP-E") inhibitors, Cetuximab, Cladribine, Chlorambucil, Chlormethine, Chlorotrianisene, Cisplatin, Clofarabine, cyclophosphamide, Cytarabine, a Cytostatic agent, Cytoxan, Dacarbazine, Dactinomycin, Daunorubicin, Dasatinib, Deforolimus, Deoxycoformycin, Didox, Diethylstilbestrol, Docetaxel, Doxorubicin, Dromostanolone, Droloxafine, Epirubicin, Epothilone, ERK inhibitors, Erlotinib, Etoposide, 17.alpha.-Ethinylestradiol, Estramustine, Exemestane, Floxuridine, Fludarabine, Fludarabine phosphate, 5-Fluorouracil, Fluoxymesterone, Flutamide, Fulvestrant, Gefitinib, Gemcitabine, Gemtuzumab ozogamcicin, Goserelin, GSK-923295, Hexamethylmelamine, Hydroxyprogesterone, Hydroxyurea, Ibritumomab Tiuxetan, Idarubicin, Ifosfamide, Imatinib mesylate, Intron, Irinotecan, ispinesib, KSP inhibitors, L778,123, Lapatinib, Leucovirin, Leuprolide, Lerozole, Letrazole, Levamisole, Liposomal Doxorubicin, Liposomal, Lomustine, Lonafarnib, Medroxyprogesteroneacetate, Megestrolacetate, Melphalan, 6-Mercaptopurine, Methoxtrexate, Methylprednisolone, Methyltestosterone, Mithramycin, Mitomycin-C, Mitotane, Mitoxantrone, Navelbene, Nilotinib, Oxaliplatin, Paclitaxel, Panitubimab, Pentostatin, Pipobroman, Porfimer, Prednisolone, Prednisone propionate, Procarbazine, Reloxafine, Rituximab, Satriplatin, SB-743921, Sml1, Sorafinib, Streptozocin, Sunitinib, Tamoxifen, Taxotere, Taxol, Temozolomide, Teniposide, Testolactone, Testosterone, Tezacitabine, 6-Thioguanine, Thiotepa, Tipifarnib, Topotecan, Toremifene, Tositumomab, Trastuzumab, Triamcinolone, Triapine, Triethylenemelamine, Triethylenethiophosphoramine, Trimidox, Uracil mustard, Vinblastine, Vincristine, Vindesine, and Vinorelbine.

Details for Patent 8,591,943

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 2039-02-26
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 06/04/1986 ⤷  Try a Trial 2039-02-26
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 ⤷  Try a Trial 2039-02-26
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b Injection 103132 ⤷  Try a Trial 2039-02-26
Genentech, Inc. RITUXAN rituximab Injection 103705 11/26/1997 ⤷  Try a Trial 2039-02-26
Idec Pharmaceuticals Corp. RITUXAN rituximab Injection 103737 02/19/2002 ⤷  Try a Trial 2039-02-26
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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