ROS1 inhibitor and its use
    154.
    发明授权

    公开(公告)号:US09962378B2

    公开(公告)日:2018-05-08

    申请号:US14927825

    申请日:2015-10-30

    CPC classification number: A61K31/4743

    Abstract: The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.

    PacketUsher: accelerating computer-intensive packet processing

    公开(公告)号:US09961002B2

    公开(公告)日:2018-05-01

    申请号:US14972062

    申请日:2015-12-16

    CPC classification number: H04L47/125 H04L45/24 H04L47/2483 H04L69/22

    Abstract: Compute-intensive packet processing (CIPP) in a computer system comprising a programmable computing platform is accelerated by using a packet I/O engine, implemented on the platform, to perform packet I/O functions, where the packet I/O engine is configured to achieve direct access to a network interface card (NIC) from a user application. For a Linux-based computer system, standard I/O mechanisms of Linux are bypassed and only the packet I/O engine is used in performing the I/O functions. Furthermore, the computer system is configured to: process a batch of packets, instead of packet by packet, in every function call; and when moving a packet between a buffer of an individual user application and a queue of the packet I/O engine, copy a packet descriptor of the packet instead the entire packet. In addition, workflows across different working threads are balanced and parallelism is exploited to fully utilize resources of the platform.

    Hydroxynaphthoquinone compounds for treatment of non-small cell lung cancer

    公开(公告)号:US09913811B2

    公开(公告)日:2018-03-13

    申请号:US15186795

    申请日:2016-06-20

    CPC classification number: A61K31/122

    Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.

    COBALT-POLYPYRIDYL COMPLEX FOR TREATMENT OF CANCER, A PHARMACEUTICAL COMPOSITION AND A KIT COMPRISING IT

    公开(公告)号:US20180050044A1

    公开(公告)日:2018-02-22

    申请号:US15242883

    申请日:2016-08-22

    CPC classification number: A61K31/555 A61K31/28 A61K45/06 A61K2300/00

    Abstract: A method for treating a subject suffering from a cancer, in particular a multidrug-resistant cancer includes administrating a cobalt-polypyridyl complex to the subject. A method for suppressing the growth of cancer cells, in particular inducing autophagy of the cancer cells, inducing cell cycle arrest of the cancer cells and/or inhibiting cell invasion of the cancer cells and for specifically targeting cancer cells with multidrug-resistance includes contacting said cancer cells with the cobalt-polypyridyl complex. A pharmaceutical composition and a kit are provided and include the cobalt-polypyridyl complex. Unexpectedly, the cobalt-polypyridyl complex is especially suitable to treat cancer, in particular multidrug-resistant cancer with an exceptionally increased cytotoxic activity towards multidrug-resistant cancer cells.

    HYDROXYNAPHTHOQUINONE COMPOUNDS FOR TREATMENT OF NON-SMALL CELL LUNG CANCER

    公开(公告)号:US20170360721A1

    公开(公告)日:2017-12-21

    申请号:US15186795

    申请日:2016-06-20

    CPC classification number: A61K31/122

    Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.

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