C-ring modified tricyclic benzonaphthiridinone protein kinase inhibitors and use thereof

Patent metadata

Field	Value
Publication number	US-9938268-B2
Application number	US-200913140090-A
Country	US
Kind code	B2
Filing date	Dec 2, 2009
Priority date	Dec 17, 2008
Publication date	Apr 10, 2018
Grant date	Apr 10, 2018

Abstract

Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.

First claim

What is claimed is:

1. A compound selected from the group consisting of:
4-Fluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-2-trifluoromethyl-1-benzamide;
2,3-Difluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
3, 4-Difluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
3, 5-Difluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
4-Fluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
2-Fluoro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-3-trifluoromethyl-benzamide;
3, 5-Dichloro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
2,6-Dichloro-N-[4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide;
3-Fluoro-N-[3-fluoro-4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-2-benzamide;
4-Fluoro-N-[2-fluoro-4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-2-trifluoromethyl-benzamide;
3, 4-Difluoro-N-[3-fluoro-4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide; and
2, 3-Difluoro-N-[3-fluoro-4-(6-oxo-5,6,7,8,9,10-hexahydrobenzo[c][1,8]naphthyridin-1-ylamino)-phenyl]-1-benzamide.

2. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, or any mixture thereof, and a pharmaceutically acceptable carrier, excipient, adjuvant and/or diluent.

Assignees

• Xiao Yufang
• Huck Bayard R
• Sutton Amanda E
• Richardson Thomas E
• Karra Srinivasa R
• Merck Patent Gmbh

Inventors

• Xiao Yufang
• Huck Bayard R
• Sutton Amanda E
• Richardson Thomas E
• Karra Srinivasa R

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/02

  Immunomodulators · CPC title