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Last Updated: March 29, 2024

Claims for Patent: 8,445,486


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Summary for Patent: 8,445,486
Title:Triazine compounds as PI3 kinase and mTOR inhibitors
Abstract: Compounds of formula I ##STR00001## wherein: R.sup.1 is ##STR00002## and R.sup.2, R.sup.4, and R.sup.6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
Inventor(s): Venkatesan; Aranapakam Mudumbai (Rego Park, NY), Chen; Zecheng (New City, NY), Dehnhardt; Christoph Martin (New York, NY), Dos Santos; Osvaldo (Astoria, NY), Delos Santos; Efren Guillermo (Nanuet, NY), Zask; Arie (New York, NY), Verheijen; Jeroen Cunera (Highland Mills, NY), Kaplan; Joshua Aaron (Nyack, NY), Richard; David James (Warwick, NY), Ayral-Kaloustian; Semiramis (Tarrytown, NY), Mansour; Tarek Suhayl (New City, NY), Gopalsamy; Ariamala (Mahwah, NJ), Curran; Kevin Joseph (Congers, NY), Shi; Mengxiao (Eastchester, NY)
Assignee: Wyeth LLC (Madison, NJ)
Application Number:13/490,309
Patent Claims:1. The compound 1-{4-[4-morpholin-4-yl-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazi- n-2-yl]phenyl}-3-pyridin-4-ylurea, or a pharmaceutically acceptable salt thereof.

2. A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

3. The composition of claim 2, wherein the pharmaceutically acceptable carrier is suitable for oral administration and the composition comprises an oral dosage form.

4. The composition of claim 2, wherein the pharmaceutically acceptable carrier is suitable for intravenous administration and the composition comprises an intrasvenous dosage form.

5. The composition comprising a compound of claim 1; a second compound selected from the group consisting of a topoisomerase I inhibitor, a MEK 1/2 inhibitor, a HSP90 inhibitor, procarbazine, dacarbazine, gemcitabine, capecitabine, methotrexate, taxol, taxotere, mercaptopurine, thioguanine, hydroxyurea, cytarabine, cyclophosphamide, ifosfamide, nitrosoureas, cisplatin, carboplatin, mitomycin, dacarbazine, procarbizine, etoposide, teniposide, campathecins, bleomycin, doxorubicin, idarubicin, daunorubicin, dactinomycin, plicamycin, mitoxantrone, L-asparaginase, doxorubicin, epirubicin, 5-fluorouracil, docetaxel, paclitaxel, leucovorin, levamisole, irinotecan, estramustine, etoposide, nitrogen mustards, BCNU, carmustine, lomustine, vinblastine, vincristine, vinorelbine, oxaliplatin, imatinib mesylate, bevacizumab, hexamethylmelamine, topotecan, tyrosine kinase inhibitors, tyrphostins, herbimycin A, genistein, erbstatin, hydroxyzine, glatiramer acetate, interferon beta-1a, interferon beta-1b, natalizumab and lavendustin A; and a pharmaceutically acceptable carrier.

6. A method of treating a cancer selected from the group consisting of leukemia, skin cancer, bladder cancer, breast cancer, uterus cancer, ovary cancer, prostate cancer, lung cancer, colon cancer, pancreas cancer, renal cancer, gastric cancer, soft tissue sarcoma, bone sarcoma, and brain cancer, said method comprising administering to a mammal in need thereof the compound 1-{4-[4-morpholin-4-yl-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazi- n-2-yl]phenyl}-3-pyridin-4-ylurea, or a pharmaceutically acceptable salt thereof, in an amount effective to treat the cancer.

7. The method of claim 6, wherein said cancer is renal cell carcinoma.

8. The method of claim 6, wherein said cancer is acute lymphoblastic leukemia.

9. The method of claim 6, wherein said cancer is acute malignant melanoma.

10. A method of claim 6 wherein said cancer is soft-tissue or bone sarcoma.

Details for Patent 8,445,486

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 2028-05-23
Bayer Healthcare Pharmaceuticals Inc. BETASERON interferon beta-1b For Injection 103471 07/23/1993 ⤷  Try a Trial 2028-05-23
Biogen Inc. AVONEX interferon beta-1a For Injection 103628 05/17/1996 ⤷  Try a Trial 2028-05-23
Biogen Inc. AVONEX interferon beta-1a Injection 103628 05/28/2003 ⤷  Try a Trial 2028-05-23
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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