HYDROXYLATED AND METHOXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS

• US 20160235754A1
• Filed: 04/28/2016
• Published: 08/18/2016
• Est. Priority Date: 07/06/2006
• Status: Abandoned Application

• Current Assignee: Array Biopharma Incorporated (Pfizer Inc.), Genentech, Inc. (Roche Holding AG)
• Original Assignee: Array Biopharma Incorporated (Pfizer Inc.), Genentech, Inc. (Roche Holding AG)
• 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
• Application Number:
  US15/140,874
• Publication Number:
  US 20160235754A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/517 ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 25/28 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 Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07D 239/70 condensed with carbocyclic rings or ring systems
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 403/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 405/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 407/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/14 containing three or more hetero rings
• CPC Class Codes: C07D 413/12 linked by a chain containing hetero atoms as chain links

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.

Claims

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.

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.

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.