公开(公告)号：EP3793993A1

公开(公告)日：2021-03-24

申请号：EP19804043.8

申请日：2019-05-13

申请人： ARIAD Pharmaceuticals, Inc.

发明人： DURAK, Landon, J. ,  LANGSTON, Marianne ,  SHARMA, Pradeep, Kumar ,  NGUYEN, Thai, Hiep ,  LI, Shuanglian ,  ZHANG, Xiaoguang

IPC分类号： C07D403/04 ,  A61P35/00

公开(公告)号：EP3778584A1

公开(公告)日：2021-02-17

申请号：EP20178478.2

申请日：2015-05-13

申请人： ARIAD Pharmaceuticals, Inc.

发明人： HUANG, Wei-sheng ,  GONG, Yongjin ,  LI, Feng ,  BENCIVENGA, Nicholas, E. ,  DALGARNO, David, C. ,  KOHLMANN, Anna ,  SHAKESPEARE, William, C. ,  THOMAS, Ranny, M. ,  ZHU, Xiaotian ,  WEST, Angela, V. ,  YOUNGSAYE, Willmen ,  ZHANG, Yun ,  ZHOU, Tianjun

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04

摘要： Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFRand mutant HER2 activity, are described herein.

公开(公告)号：EP3760618A1

公开(公告)日：2021-01-06

申请号：EP20177579.8

申请日：2015-10-21

申请人： ARIAD Pharmaceuticals, Inc.

发明人： ROZAMUS, Leonard, W. ,  SHARMA, Pradeep

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P35/00

摘要： Novel crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

公开(公告)号：EP3548479A1

公开(公告)日：2019-10-09

申请号：EP17811814.7

申请日：2017-11-29

申请人： ARIAD Pharmaceuticals, Inc.

发明人： HUANG, Wei-Sheng ,  ZHANG, Yun ,  YOUNGSAYE, Willmen ,  ZHU, Xiaotian ,  GENO, Erin

IPC分类号： C07D403/12 ,  C07D471/04 ,  C07D239/48 ,  A61P35/00 ,  A61K31/505 ,  A61K31/506

公开(公告)号：EP3210609A1

公开(公告)日：2017-08-30

申请号：EP17162419.0

申请日：2009-05-21

申请人： ARIAD PHARMACEUTICALS, INC.

发明人： WANG, Yihan ,  HUANG, Wei-Sheng ,  LIU, Shuangying ,  SHAKESPEARE, William, C. ,  THOMAS, R., Mathew ,  QI, Jiwei ,  LI, Feng ,  ZHU, Xiaotian ,  KOHLMANN, Anna ,  DALGARNO, David, C. ,  ROMERO, Jan, Antoinette, C. ,  ZOU, Dong

IPC分类号： A61K31/505 ,  A61K31/513

CPC分类号： C07F9/6533 ,  C07D239/48 ,  C07F9/587 ,  C07F9/650941 ,  C07F9/65122 ,  C07F9/65127 ,  C07F9/65216 ,  C07F9/65217 ,  C07F9/65218 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561 ,  C07F9/65616 ,  C07F9/65685 ,  C07F9/657172 ,  C07F9/65846

摘要： The invention features compounds of the general formula (VIa) in which the variable groups are as defined herein, and to their preparation and use.

公开(公告)号：EP3157916A1

公开(公告)日：2017-04-26

申请号：EP15810340.8

申请日：2015-05-13

申请人： ARIAD Pharmaceuticals, Inc.

发明人： HUANG, Wei-sheng ,  GONG, Yongjin ,  LI, Feng ,  BENCIVENGA, Nicholas, E. ,  DALGARNO, David, C. ,  KOHLMANN, Anna ,  SHAKESPEARE, William, C. ,  THOMAS, Ranny, M. ,  ZHU, Xiaotian ,  WEST, Angela, V. ,  YOUNGSAYE, Willmen ,  ZHANG, Yun ,  ZHOU, Tianjun

IPC分类号： C07D403/14 ,  C07D473/16

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07F9/65583

摘要： Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.

摘要翻译： 本文描述了调节激酶活性的化合物和药物组合物，包括突变型EGFR和突变型HER2激酶活性，以及​​化合物，药物组合物和治疗与激酶活性相关的疾病和病症的方法，包括突变型EGFR和突变型HER2活性。

公开(公告)号：EP2704572B1

公开(公告)日：2015-12-30

申请号：EP12779411.3

申请日：2012-05-04

申请人： ARIAD PHARMACEUTICALS, INC.

发明人： DALGARNO, David, C. ,  HUANG, Wei-sheng ,  SHAKESPEARE, William, C. ,  WANG, Yihan ,  ZHU, Xiaotian

IPC分类号： A01N43/54 ,  A01N43/66 ,  A61K31/505 ,  A61K31/53 ,  C07D401/00

CPC分类号： C07D239/48 ,  A61K31/4025 ,  A61K31/444 ,  A61K31/4523 ,  A61K31/505 ,  A61K31/506 ,  A61K31/538 ,  A61K31/553 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.

公开(公告)号：EP2001517A2

公开(公告)日：2008-12-17

申请号：EP07754113.4

申请日：2007-03-29

申请人： Cell Genesys Inc. ,  ARIAD PHARMACEUTICALS, INC.

发明人： HARDING, Thomas, C. ,  FANG, Jianmin ,  RIVERA, Victor, M. ,  MINH, Nguyen ,  CLACKSON, Timothy, P. ,  JOOSS, Karin

IPC分类号： A61K48/00 ,  C07H21/02 ,  C07H21/04

CPC分类号： C12N15/86 ,  A61K48/0066 ,  C07K14/005 ,  C07K16/2863 ,  C07K2319/50 ,  C12N2750/14143 ,  C12N2770/32122 ,  C12N2830/002

摘要： Single AAV vector constructs for regulated expression of an immunoglobulin molecule or fragment thereof and methods of making and using the same are described. The AAV vectors comprise a regulated promoter operably linked to the coding sequence for a first and second immunoglobulin coding sequence, a sequence encoding a self-processing cleavage site between the coding sequence for the first and second immunoglobulin coding sequence and a additional proteolytic cleavage site, which provides a means to remove the self processing peptide sequenc from an expressed immunoglobulin molecule or fragment thereof. The vector constructs find utility in enhanced production of biologically active immunoglobulins or fragments thereof in vitro and in vivo.

公开(公告)号：EP1408978A2

公开(公告)日：2004-04-21

申请号：EP02742236.9

申请日：2002-06-21

申请人： ARIAD PHARMACEUTICALS, INC.

发明人： METCALF, Chester, A., III ,  SHAKESPEARE, William, C. ,  SAWYER, Tomi, K. ,  WANG, Yihan ,  BOHACEK, Regine

IPC分类号： A61K31/505 ,  C07D409/14

CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07F9/65122 ,  C07F9/65127 ,  C07F9/65583

摘要： This invention relates to compounds of the general formula (I), in which R?A, RB, RC, RD¿, and z are as defined herein, and to their preparation and use.

公开(公告)号：EP0898709A2

公开(公告)日：1999-03-03

申请号：EP97922393.0

申请日：1997-04-18

申请人： ARIAD PHARMACEUTICALS, INC.

发明人： LYNCH, Berkley, A. ,  MACNEIL, Ian, A. ,  ZOLLER, Mark, J.

IPC分类号： G01N21 ,  G01N33

CPC分类号： G01N33/542

摘要： An in vitro assay method permits the identification of a test substance which inhibits the mutual association of a pair of proteins. The method includes the steps of providing a pair of proteins capable of mutual association, one of said proteins bearing a covalently linked fluorophore; preparing a mixture containing the two proteins and at least one test substance; irradiating the mixture with polarized light of a suitable wavelength permitting excitation of the fluorophore as indicated by emission of polarized light; measuring the degree of polarization of the emission, and determining the effect of the presence or concentration of the test substance in decreasing the observed emission polarization of a mixture of the two proteins alone. Inhibitory activity of in the test substance correlates with decreased depolarization values.