1,2,4-triazole derivatives as tankyrase inhibitors

    公开(公告)号:US11926614B2

    公开(公告)日:2024-03-12

    申请号:US17253668

    申请日:2019-06-19

    摘要: The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or a C3-6 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.

    Modulator for a digital amplifier

    公开(公告)号:US10476517B2

    公开(公告)日:2019-11-12

    申请号:US16092883

    申请日:2017-04-12

    发明人: Florian Hühn

    摘要: The present disclosure relates to a modulator for a digital amplifier and a device comprising such a modulator and a digital amplifier.The modulator includes a pulse shaper and a control unit for controlling the pulse shaper to convert an input signal into a bit stream configured for a digital amplifier which encodes an amplitude value per clock of a carrier signal. The pulse shaper can represent a respective amplitude value of the input signal with different bit patterns. The control unit includes an assignment of the control commands to associated amplitude values resulting from amplification of the associated bit patterns with the digital amplifier is stored or at least is provided in that the control unit selects a control command per clock by means of the assignment and the amplitude value of the input signal and drives the pulse shaper accordingly.

    Optical system and method for spectroscopy

    公开(公告)号:US10416081B2

    公开(公告)日:2019-09-17

    申请号:US15725448

    申请日:2017-10-05

    摘要: Optical systems and methods for spectroscopy are described. The optical system may be particularly suitable for Raman spectroscopy and includes a multispectral excitation source, designed to emit monochromatic excitation radiation successively at at least two different excitation wavelengths along a common beam axis; an elongated flow volume with a longitudinal axis, designed to direct a particle flow along the longitudinal axis; an excitation beam path, designed to irradiate the monochromatic excitation radiation into the flow volume at a first position and the second position that are located in the flow volume and the first position is spaced apart from the second position; and a detection device, designed to wavelength-selectively filter and detect a portion of a radiation scattered from the first position at a first filter wavelength and to wavelength-selectively filter and detect a portion of a radiation scattered from the second position at a second filter wavelength.