Hydroxylated and methoxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors

Patent metadata

Field	Value
Publication number	US-2016235754-A1
Application number	US-201615140874-A
Country	US
Kind code	A1
Filing date	Apr 28, 2016
Priority date	Jul 6, 2006
Publication date	Aug 18, 2016
Grant date	—

Abstract

The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula

Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

First claim

What is claimed is:

1 . A pharmaceutical composition comprising (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

2 . A method of treating prostate cancer in a mammal, said method comprising administering to said mammal a therapeutically effective amount of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one, or a pharmaceutically acceptable salt thereof.

3 . A method of treating breast cancer in a mammal, said method comprising administering to said mammal a therapeutically effective amount of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one, or a pharmaceutically acceptable salt thereof.

4 . A method of treating prostate cancer in a mammal, said method comprising administering to said mammal a therapeutically effective amount of a pharmaceutical composition as described in claim 1 .

5 . A method of treating breast cancer in a mammal, said method comprising administering to said mammal a therapeutically effective amount of a pharmaceutical composition as described in claim 1 .

Assignees

• Array Biopharma Inc
• Genentech Inc

Inventors

• Mitchell Ian S
• Blake James F
• Xu Rui
• Kallan Nicholas C
• Xiao Dengming
• Spencer Keith Lee
• Bencsik Josef R
• Wallace Eli M
• Schlachter Stephen T
• Leivers Anna L
• Liang Jun
• Safina Brian
• Zhang Birong
• Chabot Christine
• Do Steven

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P29/00

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

• C07D409/14

  containing three or more hetero rings · CPC title