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公开(公告)号:US20190382381A1
公开(公告)日:2019-12-19
申请号:US16547734
申请日:2019-08-22
Inventor: Linda N. CASILLAS , John David HARLING , Afjal Hussain MIAH , Mark David RACKHAM , Ian Edward David SMITH
IPC: C07D403/14 , A61P29/00 , C07D487/04 , C07D417/14 , C07D401/14
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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公开(公告)号:US20190338042A1
公开(公告)日:2019-11-07
申请号:US16455957
申请日:2019-06-28
Inventor: Christopher John FRANCIS , Hua-Xin GAO , Yufeng LI , Niranjan YANAMANDRA
IPC: C07K16/28 , A61K39/395 , A61K31/7008 , A61K31/7028 , C07K16/30 , A61K45/06
Abstract: Disclosed herein are combinations of an OX40 modulator and a TLR4 modulator, pharmaceutical compositions thereof, uses thereof, and methods of treatment comprising administering said combination, including uses in cancer.
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公开(公告)号:US10457674B2
公开(公告)日:2019-10-29
申请号:US16073355
申请日:2017-02-10
Inventor: Niall Andrew Anderson , Nicholas Paul Barton , Sebastien Andre Campos , Edward Paul Cannons , Anthony William James Cooper , Kenneth David Down , Kevin James Doyle , Julie Nicole Hamblin , Graham George Adam Inglis , Armelle Le Gall , Vipulkumar Kantibhai Patel , Simon Peace , Andrew Sharpe , Gemma Victoria White
IPC: C07D413/14 , C07D213/76 , A61P25/28 , A61P11/06 , A61P37/08 , A61P25/24 , A61P15/08
Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
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公开(公告)号:US20190322734A1
公开(公告)日:2019-10-24
申请号:US15772664
申请日:2016-10-31
Inventor: Paul-Peter TAK
IPC: C07K16/24 , A61K39/395 , A61K31/519
Abstract: An antibody antagonist of GM-CSF for use in the treatment of a patient suffering from rheumatoid arthritis (RA), wherein said antibody is administered to said patient according to the following treatment regimen: i. a first period wherein the antibody is administered once a week; and ii. a second period wherein the antibody is administered every other week and then ceased once said patient has sustained remission for a continuous period of at least two months.
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公开(公告)号:US20190262356A1
公开(公告)日:2019-08-29
申请号:US16408718
申请日:2019-05-10
Inventor: Jae U. JEONG , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, JR. , Daohua Zhang
IPC: A61K31/553 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/55 , C07D267/14 , C07D498/04 , C07D281/10 , C07D223/08 , C07D403/12 , C07D487/04
Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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公开(公告)号:US20190256608A1
公开(公告)日:2019-08-22
申请号:US15780331
申请日:2016-12-01
Inventor: Patrick A. MAYES , Laura M. SEESTALLER-WEHR , Lyuben TSVETKOV , Niranjan YANAMANDRA , Jingsong YANG
Abstract: Disclosed herein are combinations of an antigen binding protein that binds BCMA with a antigen binding protein that bind to an immunomodulatory agents, such as PD-1 or OX40, pharmaceutical compositions thereof, uses thereof, and methods of treatment comprising administering said combinations, including uses in cancer.
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公开(公告)号:US20190247382A1
公开(公告)日:2019-08-15
申请号:US16376858
申请日:2019-04-05
Inventor: Michael P. Demartino , Huiping Amy Guan
IPC: A61K31/4439 , A61K31/4412 , C07D213/69
Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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公开(公告)号:US20190231887A1
公开(公告)日:2019-08-01
申请号:US16255947
申请日:2019-01-24
Inventor: Alan Hornsby DAVIDSON , Alan Hastings DRUMMOND , Lindsey Ann NEEDHAM
IPC: A61K47/54 , C07D277/46 , C07D471/04 , C07C237/22 , C07D215/233 , C07D213/73
CPC classification number: A61K47/542 , A61K47/54 , C07C237/22 , C07C2601/08 , C07D213/73 , C07D215/233 , C07D277/46 , C07D471/04
Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.
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公开(公告)号:US10364254B2
公开(公告)日:2019-07-30
申请号:US15752639
申请日:2016-08-15
Inventor: Haifeng Cui , Alan Hennessy , Qi Jin , Timothy James Miles , Stephen Frederick Moss , Neil David Pearson
IPC: A61P31/04 , C07D498/04 , C07D513/04 , C07D519/00
Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
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公开(公告)号:US10351627B2
公开(公告)日:2019-07-16
申请号:US15246662
申请日:2016-08-25
Inventor: Yao-Bin Liu , Patrick Mayes , Radha Shah Parmar
IPC: C07K16/28 , A61K39/395 , A61K45/06 , C07K16/30 , A61K39/00
Abstract: The present invention relates to an ICOS binding protein or antigen binding portion thereof that is an agonist to human ICOS and does not induce complement, ADCC, or CDC when placed in contact with a T cell in vivo and methods of treating cancer, infectious disease and/or sepsis with said ICOS binding protein or antigen binding portion thereof. Further the ICOS binding proteins or antigen binding portions thereof of the present invention are capable of activating a T cell when placed in contact with said T cell; stimulating T cell proliferation when placed in contact with said T cell and/or inducing cytokine production when placed in contact with said T cell. The present invention relates to ICOS binding proteins or antigen binding portions thereof comprising one or more of: SEQ ID NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:4; SEQ ID NO:5; and/or SEQ ID NO:6.
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