Invention Grant
- Patent Title: 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2 pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof
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Application No.: US15587270Application Date: 2017-05-04
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Publication No.: US10259806B2Publication Date: 2019-04-16
- Inventor: Ian Collins , Thomas Peter Matthews , Tatiana Faria Da Fonseca Mchardy , James Osborne , Michael Lainchbury , Michael Ian Walton , Michelle Dawn Garrett
- Applicant: Cancer Research Technology Limited
- Applicant Address: GB London
- Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
- Current Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
- Current Assignee Address: GB London
- Agency: Fenwick & West LLP
- Main IPC: C07D413/14
- IPC: C07D413/14 ; C07D413/02 ; C07D401/12 ; A61K9/00 ; A61K31/4745 ; A61K31/5377 ; A61K31/7068 ; A61K45/06
![5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2 pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof](/abs-image/US/2019/04/16/US10259806B2/abs.jpg.150x150.jpg)
Abstract:
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as “TFM compounds”) which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or a thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; (e) ionizing radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme.
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