Benzimidazole derivatives as PI3 kinase inhibitors

Patent metadata

Field	Value
Publication number	US-10314845-B2
Application number	US-201815865703-A
Country	US
Kind code	B2
Filing date	Jan 9, 2018
Priority date	Oct 6, 2010
Publication date	Jun 11, 2019
Grant date	Jun 11, 2019

Abstract

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.

First claim

What is claimed is:

1. A method for treating a susceptible PTEN-deficient neoplasm selected from prostate cancer, non-small-cell lung cancer, endometrial cancer, gastric cancer, melanoma, head and neck cancer, breast cancer and a glioma in a human in need thereof comprising the steps of:
(a) analyzing a sample from said neoplasm to determine whether there is a PTEN deficiency in cells of said neoplasm;
(b) selecting a human having said neoplasm with PTEN deficiency; and
(c) administering a therapeutically effective amount the compound of formula

or a pharmaceutically acceptable salt thereof to the human selected in step (b).

Assignees

• Glaxosmithkline Llc

Inventors

• Tedesco Rosanna
• Qu Junya
• Sanchez Robert
• Rivero Ralph A

Classifications

• A61P35/02

  specific for leukemia · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• C07D235/10

  Radicals substituted by halogen atoms or nitro radicals · CPC title