公开(公告)号：US10562918B2

公开(公告)日：2020-02-18

申请号：US15882924

申请日：2018-01-29

Applicant: ACEA BIOSCIENCES INC.

Inventor： Xiao Xu ,  Xiaobo Wang ,  Long Mao ,  Li Zhao ,  Biao Xi

IPC: C07D519/00 ,  C07D403/12 ,  C07D417/12 ,  C07D473/18 ,  C07D487/04 ,  C07D401/12 ,  C07D239/52 ,  C07D239/49 ,  C07D239/48 ,  C07D239/47

Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.

公开(公告)号：US10168318B2

公开(公告)日：2019-01-01

申请号：US15613052

申请日：2017-06-02

Applicant: ACEA Biosciences, Inc.

Inventor： Yama A. Abassi ,  Naichen Yu ,  Josephine Atienza ,  Xiao Xu ,  Xiaobo Wang

IPC: G01N33/50 ,  C12Q1/00 ,  G01N27/02 ,  G01N33/543

Abstract: A method of identifying a potential therapeutic compound that affects a Receptor Tyrosine Kinase (RTK) pathway in cancer cells, which includes: providing a device capable of measuring cell-substrate impedance; culturing cancer cells in serum-free media in at least two wells of the device; adding to a first well a proposed therapeutic compound that affects a RTK pathway and a RTK stimulating factor for the RTK pathway to form a test well, and adding to another well the RTK stimulating factor to form a control well; continuously monitoring cell-substrate impedance of the at least two wells and optionally determining cell indices from the monitored cell-substrate impedance; and determining a difference in impedance or optionally cell index between the test well and control well; and if significantly different, concluding the proposed therapeutic compound is therapeutically active in the RTK pathway within the cancer cells.

公开(公告)号：US10067121B2

公开(公告)日：2018-09-04

申请号：US14541024

申请日：2014-11-13

Applicant: ACEA Biosciences, Inc.

Inventor： Yama A. Abassi ,  Naichen Yu ,  Josephine Atienza ,  Xiao Xu ,  Xiaobo Wang

IPC: G01N33/50 ,  C12Q1/00 ,  G01N27/02 ,  G01N33/543

CPC classification number: G01N33/5041 ,  C12Q1/002 ,  G01N27/021 ,  G01N33/5014 ,  G01N33/5438 ,  G01N2333/4716 ,  G01N2333/705 ,  G01N2333/91205 ,  G01N2500/04 ,  G01N2500/10

Abstract: Use of cell-substrate impedance based methods for screening for agonists of G-Protein Coupled Receptors (GPCRs) or inhibitors of a Receptor Tyrosine Kinases (RTKs), identifying compounds that affect GPCR or RTK pathways, validating molecular targets involved in a GPCR or RTK signaling pathways, monitoring dose-dependent functional activation of GPCR or RTK; determining desensitization of a GPCR and identifying a compound capable of affecting RTK activity in cancer cell proliferation.

公开(公告)号：US09623027B2

公开(公告)日：2017-04-18

申请号：US14712794

申请日：2015-05-14

Applicant: ACEA BIOSCIENCES INC.

Inventor： Xiao Xu ,  Xiaobo Wang ,  Long Mao ,  Li Zhao ,  Biao Xi

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  A61K45/06

Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.

公开(公告)号：US09586965B2

公开(公告)日：2017-03-07

申请号：US14420341

申请日：2013-07-11

Applicant: ACEA BIOSCIENCES INC.

Inventor： Xiao Xu ,  Xiaobo Wang ,  Long Mao ,  Li Zhao ,  Biao Xi

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61P35/00 ,  A61P29/00 ,  A61P17/06

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways.

Abstract translation: 本发明涉及某些吡咯并嘧啶衍生物，含有它们的药物组合物及其使用方法，包括治疗增殖紊乱和与激酶失调相关的其它疾病的方法（例如但不限于EGFR（包括HER ），Alk，PDGFR，BLK，BMX / ETK，BTK，FLT3（D835Y），ITK，JAK1，JAK2，JAK3，TEC和TXK）和/或各自的途径。

公开(公告)号：US20150210702A1

公开(公告)日：2015-07-30

申请号：US14420341

申请日：2013-07-11

Applicant: ACEA BIOSCIENCES INC.

Inventor： Xiao Xu ,  Xiaobo Wang ,  Long Mao ,  Li Zhao ,  Biao Xi

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways.

Abstract translation: 本发明涉及某些吡咯并嘧啶衍生物，含有它们的药物组合物及其使用方法，包括治疗增殖紊乱和与激酶失调相关的其它疾病的方法（例如但不限于EGFR（包括HER ），Alk，PDGFR，BLK，BMX / ETK，BTK，FLT3（D835Y），ITK，JAK1，JAK2，JAK3，TEC和TXK）和/或各自的途径。

公开(公告)号：US20210364494A1

公开(公告)日：2021-11-25

申请号：US16635911

申请日：2018-08-01

Applicant: ACEA BIOSCIENCES, INC.

Inventor： Nan Li ,  Yama Abassi ,  Xiao Xu ,  Xiaobo Wang

IPC: G01N33/483 ,  G01N1/14 ,  G01N27/02

Abstract: A method of assessing cytolysis of cancer cells, the method including: providing a cell substrate impedance monitoring cartridge having a plurality of chambers, each chamber having an electrode array configured for measuring cell-substrate impedance, wherein different chambers are preloaded with different target cells embodied as cancer cells of different lineage, origin or stage; adding effector cells to the plurality chambers for interaction with the target cells, wherein the effector cells are immune cells; monitoring cell-substrate impedance of the plurality of chambers before and after adding the effector cells and optionally deriving an impedance-based parameter from the impedances; and determining effectiveness of effector cell killing of the different target cells by comparing the impedances or impedance-based parameters over time.

公开(公告)号：US20200278339A1

公开(公告)日：2020-09-03

申请号：US16752298

申请日：2020-01-24

Applicant: ACEA Biosciences, Inc.

Inventor： Xiaobo Wang ,  Wei Ouyang ,  Nan Li ,  Biao Xi ,  Yama A. Abassi ,  Xiao Xu

IPC: G01N33/487

Abstract: Extracellular recording devices with reference electrodes positioned in a cell free zone and methods of conducting extracellular recording. Parallel cell-substrate impedance monitoring and extracellular recording of excitable cells such as excitable cells, cardiomyocytes, and cardiomyocyte precursor cells using devices that switch between extracellular recording and impedance monitoring modes.

公开(公告)号：US10018581B2

公开(公告)日：2018-07-10

申请号：US13802174

申请日：2013-03-13

Applicant: ACEA BIOSCIENCES, INC

Inventor： Xiaobo Wang ,  Xiao Xu

IPC: B01L3/00 ,  G01N27/02 ,  C12M1/32 ,  C12M1/34 ,  G01N27/327

CPC classification number: G01N27/02 ,  C12M23/12 ,  C12M41/36 ,  G01N27/3276 ,  Y10T29/49117

Abstract: A method for assaying target molecules in a sample liquid, the method comprising: providing an impedance monitoring device operably connected to an impedance analyzer; adding a sample liquid suspected of having target molecules to the well thereby permitting binding of target molecules to the capture molecules; monitoring impedance of the well; and determining the presence, amount or concentration of target molecules in the liquid sample from the monitored impedance. The device includes a nonconducting substrate having a well, at least two electrodes fabricated on a bottom of the well and on a same plane, wherein the surfaces of the at least two electrodes are modified with capture molecules configured to bind target molecules in a liquid sample, and at least two connection pads electrically connected to the at least two electrodes.

公开(公告)号：US20170370907A1

公开(公告)日：2017-12-28

申请号：US15613052

申请日：2017-06-02

Applicant: ACEA Biosciences, Inc.

Inventor： Yama A. Abassi ,  Naichen Yu ,  Josephine Atienza ,  Xiao Xu ,  Xiaobo Wang

IPC: G01N33/50 ,  G01N33/543 ,  C12Q1/00 ,  G01N27/02

CPC classification number: G01N33/5041 ,  C12Q1/002 ,  G01N27/021 ,  G01N33/5014 ,  G01N33/5438 ,  G01N2333/4716 ,  G01N2333/705 ,  G01N2333/91205 ,  G01N2500/04 ,  G01N2500/10

Abstract: A method of identifying a potential therapeutic compound that affects a Receptor Tyrosine Kinase (RTK) pathway in cancer cells, which includes: providing a device capable of measuring cell-substrate impedance; culturing cancer cells in serum-free media in at least two wells of the device; adding to a first well a proposed therapeutic compound that affects a RTK pathway and a RTK stimulating factor for the RTK pathway to form a test well, and adding to another well the RTK stimulating factor to form a control well; continuously monitoring cell-substrate impedance of the at least two wells and optionally determining cell indices from the monitored cell-substrate impedance; and determining a difference in impedance or optionally cell index between the test well and control well; and if significantly different, concluding the proposed therapeutic compound is therapeutically active in the RTK pathway within the cancer cells.