Invention Grant
- Patent Title: 2-(hetero)aryl-benzimidazole and imidazopyridine derivatives as inhibitors of asparagime emethyl transferase
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Application No.: US14769402Application Date: 2014-02-20
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Publication No.: US09856252B2Publication Date: 2018-01-02
- Inventor: Paul Anthony Stupple , Scott Raymond Walker , Jo-Anne Pinson , Helen Rachel Lagiakos , Gillian Elizabeth Lunniss , Ian Peter Holmes , Alexandra Elizabeth Stupple , Ylva Elisabet Bergman , Richard Charles Foitzik , Wilhelmus Johannes Antonius Kersten , Michelle Ang Camerino
- Applicant: Cancer Therapeutics CRC Pty Ltd
- Applicant Address: AU Bundoora, Victoria
- Assignee: Cancer Therapeutics CRC Pty Ltd
- Current Assignee: Cancer Therapeutics CRC Pty Ltd
- Current Assignee Address: AU Bundoora, Victoria
- Agency: Stites & Harbison PLLC
- Agent Richard S. Myers, Jr.
- Priority: GB1302927.7 20130220
- International Application: PCT/GB2014/050491 WO 20140220
- International Announcement: WO2014/128465 WO 20140828
- Main IPC: C07D413/00
- IPC: C07D413/00 ; C07D401/00 ; C07D513/02 ; C07D471/04 ; C07D235/18 ; C07D519/00

Abstract:
Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from: a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are β to one another; L1 is selected from: (i) A1—O—CH2—A2; (ii) A1—CH2—O—A2; (iii) A1—C(═O)—NH—A2; (iv) A1—CH(OH)—A2; (v) A1—CH2—NH—C(═O)—A2; (vi) A1—S—CH2—A2; (vii) A1—CH2—S—A2; (viii) A1—CH2—A2; and (ix) A1—CH(CH3)—O—A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.
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