IP Library Granted Patent US 10,022,381
Granted Patent B2
US 10,022,381 · App. 14/927,763 · Granted Jul 17, 2018

Triazine compounds as PI3 kinase and mTOR inhibitors

Inventors: Aranapakam Mudumbai Venkatesan (Rego Park, NY); Zecheng Chen (New City, NY); Christoph Martin Dehnhardt (New York, NY); Osvaldo Dos Santos (Astoria, NY); Efren Guillermo Delos Santos (Nanuet, NY); Arie Zask (New York, NY); Jeroen Cunera Verheijen (Highland Mills, NY); Joshua Aaron Kaplan (Nyack, NY); David James Richard (Warwick, NY); Semiramis Ayral-Kaloustian (Tarrytown, NY); Tarek Suhayl Mansour (New City, NY); Ariamala Gopalsamy (Mahwah, NJ); Kevin Joseph Curran (Congers, NY); Mengxiao Shi (Eastchester, NY)
Assignee: Pfizer Inc.
A61K31/5377A61K33/24
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Quick Facts
Patent No.
US 10,022,381
App. No.
14/927,763
Granted
Jul 17, 2018
Kind
B2
Abstract

Compounds of formula I wherein: R 1 is and R 2 , R 4 , and R 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.

Claims (6)

1. A method of treating cancer comprising concurrently administering to a mammal in need thereof a first compound: 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}lphenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea or a pharmaceutically acceptable salt thereof; and a second compound cisplatin, in an amount effective to treat said cancer.

2. The method of claim 1 , wherein said cancer is 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, and brain cancer.

3. The method of claim 2 , wherein said cancer is breast cancer.

4. The method of claim 3 , wherein said breast cancer is triple negative breast cancer.

5. The method of claim 1 , wherein the first compound is a lactic acid salt form (lactate) of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyI)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea.

6. The method of claim 1 , wherein the first compound is a free base form of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 22, 2024
From: VENKATESAN, ARANAPAKAM MUDUMBAI; CHEN, ZECHENG; DEHNHARDT, CHRISTOPH MARTIN; DOS SANTOS, OSVALDO; DELOS SANTOS, EFREN GUILLERMO; ZASK, ARIE; VERHEIJEN, JEROEN CUNERA; KAPLAN, JOSHUA AARON; RICHARD, DAVID JAMES; AYRAL-KALOUSTIAN, SEMIRAMIS; MANSOUR, TAREK SUHAYL; GOPALSAMY, ARIAMALA; CURRAN, KEVIN JOSEPH; SHI, MENGXIAO
To: WYETH
Reel/Frame 068373/0218 →
CHANGE OF NAME Recorded Aug 22, 2024
From: WYETH
To: WYETH LLC
Reel/Frame 068760/0375 →
Continuity (10)
Continuation 14477650 · Sep 4, 2014
Continuation 14259414 · Apr 23, 2014
Continuation 13950584 · Jul 25, 2013
Continuation 13718928 · Dec 18, 2012
Continuation 13490309 · Jun 6, 2012
Continuation 13218571 · Aug 26, 2011
Division 12470521 · May 22, 2009
Provisional Application 61055661 · May 23, 2008
Related Publication 20170119778A1 · May 4, 2017
Related Publication 20170224696A9 · Aug 10, 2017
Cited By (1)
US 12,642,803