US2016184311A1PendingUtilityA1

Combination Therapy for the Treatment of Cancer

64
Assignee: CHEN YANPriority: Aug 14, 2013Filed: Aug 7, 2014Published: Jun 30, 2016
Est. expiryAug 14, 2033(~7.1 yrs left)· nominal 20-yr term from priority
Inventors:Yan ChenXizhong HuangSunkyu Kim
A61P 5/32A61P 5/00A61P 43/00A61P 35/02A61P 35/00A61K 31/138A61K 31/5685A61K 31/5377A61K 31/4196A61K 31/436A61K 31/565A61K 31/519A61K 31/551A61K 31/4439A61K 31/5513A61K 45/06A61K 31/56A61K 31/506A61K 31/495A61K 31/427A61K 2300/00
64
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Claims

Abstract

The present disclosure relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof. The present disclosure also relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof, and (3) a third agent which is an agent that regulates the PI3K/Akt/mTOR pathway or a pharmaceutically acceptable salt thereof.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof. 
     
     
         2 . A pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof, and (3) a third agent which is an agent that regulates the PI3K/Akt/mTOR pathway or a pharmaceutically acceptable salt thereof. 
     
     
         3 . The combination of  claim 1 , wherein the agents are administered simultaneously, separately or sequentially. 
     
     
         4 . The combination of  claim 1 , wherein the CDK inhibitor is CDK4/6 inhibitor. 
     
     
         5 . The combination of  claim 4 , wherein the CDK4/6 inhibitor is Compound A1, described by Formula A1 below: 
       
         
           
           
               
               
           
         
       
     
     
         6 . The combination of  claim 4 , wherein the CDK4/6 inhibitor is Compound A2, described by Formula A2 below: 
       
         
           
           
               
               
           
         
       
     
     
         7 . The combination of  claim 4 , wherein the CDK4/6 inhibitor is palbociclib. 
     
     
         8 . The combination of  claim 1  or  2 , wherein the anti-hormonal agent is an aromatase inhibitor. 
     
     
         9 . The combination of  claim 8 , wherein the aromatase inhibitor is non-steroidal. 
     
     
         10 . The combination of  claim 8 , wherein the aromatase inhibitor is steroidal. 
     
     
         11 . The combination is of  claim 8 , wherein the aromatase inhibitor is letrozole. 
     
     
         12 . The combination is of  claim 8 , wherein the aromatase inhibitor is exemestane. 
     
     
         13 . The combination of  claim 1 , wherein the anti-hormonal agent is an estrogen receptor antagonist. 
     
     
         14 . The combination of  claim 13 , wherein the estrogen receptor antagonist is fulvestrant. 
     
     
         15 . The combination of  claim 1 , wherein the anti-hormonal agent is a selective estrogen receptor modulator. 
     
     
         16 . The combination of  claim 15 , wherein the selective estrogen receptor modulator is tamoxifen. 
     
     
         17 . The combination of  claim 2 , wherein the agent that regulates the PI3K/Akt/mTOR pathway is a PI3K inhibitor. 
     
     
         18 . The combination of  claim 17 , wherein the PI3K inhibitor is Compound C1, described by Formula C1 below: 
       
         
           
           
               
               
           
         
       
     
     
         19 . The combination of  claim 17 , wherein the PI3K inhibitor is Compound C2, described by Formula C2 below: 
       
         
           
           
               
               
           
         
       
     
     
         20 . The combination of  claim 2 , wherein the agent that regulates the PI3K/Akt/mTOR pathway is an mTOR inhibitor. 
     
     
         21 . The combination of  claim 20  wherein the mTOR inhibitor is everolimus. 
     
     
         22 . A method of treating cancer comprising administering to a subject the pharmaceutical combination of  claim 1 . 
     
     
         23 . The method of  claim 22 , wherein the cancer is selected from the group consisting of sarcoma, lymphomas, cancer of the lung, bronchus, prostate, breast, pancreas, gastrointestine, colon, rectum, colon, colorectal adenoma, thyroid, liver, intrahepatic bile duct, hepatocellular, adrenal gland, stomach, gastric, glioma, glioblastoma, endometrial, melanoma, kidney, renal pelvis, urinary bladder, uterine corpus, uterine cervix, vagina, ovary, multiple myeloma, esophagus, a leukaemia, acute myelogenous leukemia, chronic myelogenous leukemia, lymphocytic leukemia, myeloid leukemia, brain, a carcinoma of the brain, oral cavity and pharynx, larynx, small intestine, non-Hodgkin lymphoma, melanoma, villous colon adenoma, a neoplasia, a neoplasia of epithelial character, a mammary carcinoma, basal cell carcinoma, squamous cell carcinoma, actinic keratosis, tumor diseases, a tumor of the neck or head, polycythemia vera, essential thrombocythemia, myelofibrosis with myeloid metaplasia, and Waldenstroem disease. 
     
     
         24 . The method of  claim 23 , wherein the cancer is breast cancer. 
     
     
         25 . The method of  claim 22 , wherein the cancer is an estrogen receptor positive cancer. 
     
     
         26 . The method of  claim 23 , wherein the breast cancer is estrogen receptor positive breast cancer. 
     
     
         27 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         and (2) a second agent which is letrozole. 
       
     
     
         28 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is letrozole, and 
         (3) a third agent which is Compound C1, described by Formula C1 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         29 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is letrozole, and 
         (3) a third agent which is Compound C2, described by Formula C2 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         30 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         and (2) a second agent which is fulvestrant. 
       
     
     
         31 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is fulvestrant, and 
         (3) a third agent which is Compound C1, described by Formula C1 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         32 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is fulvestrant, and 
         (3) a third agent which is Compound C2, described by Formula C2 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         33 . A pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is everolimus, and 
         (3) a third agent which is exemestane. 
       
     
     
         34 . A method of treating breast cancer comprising administering to a subject the pharmaceutical combination of  claim 27 . 
     
     
         35 . A method of treating HR+, HER2− breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         and (2) a second agent which is letrozole. 
       
     
     
         36 . A method of treating ER+, HER2− advanced breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         and (2) a second agent which is letrozole. 
       
     
     
         37 . A method of treating ER+ advanced breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is letrozole, and 
         (3) a third agent which is Compound C1, described by Formula C1 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         38 . A method of treating ER+ advanced breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is letrozole, and 
         (3) a third agent which is Compound C2, described by Formula C2 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         39 . A method of treating postmenopausal woman with ER+, HER2− breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         and (2) a second agent which is fulvestrant. 
       
     
     
         40 . A method of treating postmenopausal woman with ER+, HER2− breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is fulvestrant, and 
         (3) a third agent which is Compound C1, described by Formula C1 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         41 . A method of treating postmenopausal woman with ER+, HER2− breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is fulvestrant, and 
         (3) a third agent which is Compound C2, described by Formula C2 below or a pharmaceutically acceptable salt thereof: 
       
       
         
           
           
               
               
           
         
       
     
     
         42 . A method of treating ER+ breast cancer comprising administering to a subject a pharmaceutical combination comprising (1) a first agent which is Compound A1 described by Formula A1 below or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         (2) a second agent which is everolimus, and 
         (3) a third agent which is exemestane.

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