US2022024939A1PendingUtilityA1

Substituted 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidin-3-ones

69
Assignee: RECURIUM IP HOLDINGS LLCPriority: Mar 9, 2018Filed: Oct 8, 2021Published: Jan 27, 2022
Est. expiryMar 9, 2038(~11.7 yrs left)· nominal 20-yr term from priority
C07D 221/18C07D 221/04A61P 35/00A61K 31/519C07D 491/048C07D 471/04C07D 519/00C07D 487/04
69
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A compound of Formula (I), or a pharmaceutically acceptable salt thereof, having the structure: 
       
         
           
           
               
               
           
         
       
       wherein:
 R 1  is selected from the group consisting of hydrogen, halogen and a substituted or unsubstituted C 1 -C 6  alkyl; 
 Ring A is selected from the group consisting of a substituted or unsubstituted phenyl and a substituted or unsubstituted 5-6 membered monocyclic heteroaryl; 
 Ring B is selected from the group consisting of a substituted or unsubstituted monocyclic 5-7 membered carbocyclyl and a substituted or unsubstituted 5-7 membered monocyclic heterocyclyl; 
 
       
         
           
           
               
               
           
         
         R 2  is selected from the group consisting of 
         m is 0, 1, 2 or 3; 
         R 3  is selected from the group consisting of halogen and a substituted or unsubstituted C 1 -C 6  alkyl; 
         X is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, a substituted or unsubstituted 4-6 membered monocyclic heterocyclyl, a substituted or unsubstituted amine(C 1 -C 6  alkyl), a substituted or unsubstituted —NH—(CH 2 ) 1-6 -amine, a mono-substituted amine, a di-substituted amine, an amino, a substituted or unsubstituted C 1 -C 6  alkyl, a substituted or unsubstituted C 1 -C 6  alkoxy, a substituted or unsubstituted C 3 -C 6  cycloalkoxy, a substituted or unsubstituted (C 1 -C 6  alkyl)acyl, a substituted or unsubstituted C-amido, a substituted or unsubstituted N-amido, a substituted or unsubstituted C-carboxy, a substituted or unsubstituted O-carboxy, a substituted or unsubstituted O-carbamyl and a substituted or unsubstituted N-carbamyl; 
         Y is CH or N; 
         Y 1  is CR 4A  or N; 
         Y 2  is CR 4B  or N; 
         Ring C is selected from the group consisting of a substituted or unsubstituted C 6 -C 10  aryl, a substituted or unsubstituted monocyclic 5-10 membered heteroaryl, a substituted or unsubstituted monocyclic 5-7 membered carbocyclyl, a substituted or unsubstituted 5-7 membered monocyclic heterocyclyl and a substituted or unsubstituted 7-10 membered bicyclic heterocyclyl; 
         R 4A  and R 4B  are independently selected from the group consisting of hydrogen, halogen and an unsubstituted C 1-4  alkyl; and 
         R 5  is a substituted or unsubstituted 5-7 membered monocyclic heterocyclyl. 
       
     
     
         2 . A pharmaceutical composition comprising an effective amount of the compound of  claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, excipient or combination thereof. 
     
     
         3 . A method for ameliorating or treating a cancer comprising administering an effective amount of  claim 1 , or a pharmaceutically acceptable salt thereof, to a subject having the cancer, wherein the cancer is selected from a brain cancer, a cervicocerebral cancer, an esophageal cancer, a thyroid cancer, a small cell cancer, a non-small cell cancer, a breast cancer, a lung cancer, a stomach cancer, a gallbladder/bile duct cancer, a liver cancer, a pancreatic cancer, a colon cancer, a rectal cancer, an ovarian cancer, a choriocarcinoma, an uterus body cancer, an uterocervical cancer, a renal pelvis/ureter cancer, a bladder cancer, a prostate cancer, a penis cancer, a testicular cancer, a fetal cancer, Wilms' cancer, a skin cancer, malignant melanoma, a neuroblastoma, an osteosarcoma, an Ewing's tumor, a soft part sarcoma, an acute leukemia, a chronic lymphatic leukemia, a chronic myelocytic leukemia, polycythemia vera, a malignant lymphoma, multiple myeloma, a Hodgkin's lymphoma, and a non-Hodgkin's lymphoma. 
     
     
         4 . A method for inhibiting replication of a malignant growth or a tumor comprising contacting the malignant growth or the tumor with an effective amount of  claim 1 , or a pharmaceutically acceptable salt thereof, wherein the malignant growth or tumor is due to a cancer selected from a brain cancer, a cervicocerebral cancer, an esophageal cancer, a thyroid cancer, a small cell cancer, a non-small cell cancer, a breast cancer, a lung cancer, a stomach cancer, a gallbladder/bile duct cancer, a liver cancer, a pancreatic cancer, a colon cancer, a rectal cancer, an ovarian cancer, a choriocarcinoma, an uterus body cancer, an uterocervical cancer, a renal pelvis/ureter cancer, a bladder cancer, a prostate cancer, a penis cancer, a testicular cancer, a fetal cancer, Wilms' cancer, a skin cancer, malignant melanoma, a neuroblastoma, an osteosarcoma, an Ewing's tumor, a soft part sarcoma, an acute leukemia, a chronic lymphatic leukemia, a chronic myelocytic leukemia, polycythemia vera, a malignant lymphoma, multiple myeloma, a Hodgkin's lymphoma, and a non-Hodgkin's lymphoma. 
     
     
         5 . A method for ameliorating or treating a malignant growth or a tumor comprising contacting the malignant growth or the tumor with an effective amount of  claim 1 , or a pharmaceutically acceptable salt thereof, wherein the malignant growth or tumor is due to a cancer selected from a brain cancer, a cervicocerebral cancer, an esophageal cancer, a thyroid cancer, a small cell cancer, a non-small cell cancer, a breast cancer, a lung cancer, a stomach cancer, a gallbladder/bile duct cancer, a liver cancer, a pancreatic cancer, a colon cancer, a rectal cancer, an ovarian cancer, a choriocarcinoma, an uterus body cancer, an uterocervical cancer, a renal pelvis/ureter cancer, a bladder cancer, a prostate cancer, a penis cancer, a testicular cancer, a fetal cancer, Wilms' cancer, a skin cancer, malignant melanoma, a neuroblastoma, an osteosarcoma, an Ewing's tumor, a soft part sarcoma, an acute leukemia, a chronic lymphatic leukemia, a chronic myelocytic leukemia, polycythemia vera, a malignant lymphoma, multiple myeloma, a Hodgkin's lymphoma, and a non-Hodgkin's lymphoma.

Cited by (0)

No later patents cite this yet.

References (0)

No backward citations on record.