2-benzoylaminobenzamide derivatives as Bcl-3 inhibitors

• US 10,450,285 B2
• Filed: 07/31/2014
• Issued: 10/22/2019
• Est. Priority Date: 07/31/2013
• Status: Active Grant

• Current Assignee: Cardiff University
• Original Assignee: Cardiff University
• Inventors: Westwell, Andrew David, Brancale, Andrea, Clarkson, Richard William Ernest, Soukupova, Jitka
• Primary Examiner(s): Heyer, Dennis
• Application Number:
  US14/908,035
• Publication Number:
  US 20160185740A1
• Time in Patent Office: 1,909 Days
• Field of Search: None
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/4402 only substituted in position 2, e.g. pheniramine, bisacodyl
• CPC Class Codes: A61K 31/4453 only substituted in position 1, e.g. propipocaine, diperodon
• CPC Class Codes: A61K 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61K 31/5375 1,4-Oxazines, e.g. morpholine
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: A61P 35/04 specific for metastasis
• CPC Class Codes: C07C 237/42 having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
• CPC Class Codes: C07D 213/40 Acylated substituent nitrogen atom
• CPC Class Codes: C07D 295/13 to an acyclic saturated chain

Abstract

The invention relates to a compound of general formula (I):

wherein R¹, R², R³, R⁴, Q, m and n are as defined herein. The compounds are inhibitors of Bcl3 and are useful for the treatment of cancer, particularly metastatic cancer.

Claims

1. A compound selected from:

2-[(2-methoxybenzoyl)amino]-N-(2-morpholin-4-ylethyl)benzamide;

2-[(3-methoxybenzoyl)amino]-N-(2-morpholin-4-ylethyl)benzamide;

2-[(4-nitrobenzoyl)amino]-N-(2-morpholin-4-ylethyl)benzamide;

2-[(2-methylbenzoyl)amino]-N-(2-morpholin-4-ylethyl)benzamide;

3,5-difluoro-N-(2-[(2-morpholin-4-ylethyl)carbamoyl]phenyl)benzamide;

2,6-difluoro-N-(2-[(2-morpholin-4-ylethyl)carbamoyl]phenyl)benzamide;

2,4-difluoro-N-(2-[(2-morpholin-4-ylethyl)carbamoyl]phenyl)benzamide;

2-[(4-fluorobenzoyl)amino]-N-(pyrrolidin-3-ylmethyl)benzamide;

2-[(4-fluorobenzoyl)amino]-N-(piperidin-3-ylmethyl)benzamide;

2-[(4-fluorobenzoyl)amino]-N-(piperazin-3-ylmethyl)benzamide;

N-(2-aminoethyl)-2-(2-fluorobenzamido)benzamide;

2-[(2-fluorobenzoyl)amino]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide; and

2-[(2-fluorobenzoyl)amino]-3-methoxy-N-(2-morpholin-4-ylethyl)benzamide;

or a pharmaceutically or veterinarily acceptable salt thereof.