Invention Grant
- Patent Title: Pyrazole derivatives as protein kinase modulators
- Patent Title (中): 吡唑衍生物作为蛋白激酶调节剂
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Application No.: US14180440Application Date: 2014-02-14
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Publication No.: US09283226B2Publication Date: 2016-03-15
- Inventor: Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
- Applicant: Astex Therapeutics Ltd , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
- Applicant Address: GB Cambridge GB London GB London
- Assignee: ASTEX THERAPEUTICS LIMITED,THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL,CANCER RESEARCH TECHNOLOGY LIMITED
- Current Assignee: ASTEX THERAPEUTICS LIMITED,THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL,CANCER RESEARCH TECHNOLOGY LIMITED
- Current Assignee Address: GB Cambridge GB London GB London
- Agency: Heslin Rothenberg Farley & Mesiti P.C.
- Priority: GB0329617.5 20031223
- Main IPC: A61K31/415
- IPC: A61K31/415 ; C07D231/12 ; A61K31/5377 ; C07D401/04 ; C07D401/10 ; C07D401/12 ; C07D401/14 ; C07D403/10 ; C07D403/12 ; C07D405/04 ; C07D413/10 ; A61K31/4155 ; A61K31/4178 ; A61K31/454 ; A61K31/496 ; A61K31/497 ; A61K45/06

Abstract:
The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
Public/Granted literature
- US20140271662A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS Public/Granted day:2014-09-18
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