公开(公告)号：EP2104535B9

公开(公告)日：2011-06-15

申请号：EP07854747.8

申请日：2007-11-21

申请人： IRM LLC

发明人： TULLY, David C. ,  CHATTERJEE, Arnab K. ,  VIDAL, Agnes ,  BURSULAYA, Badry ,  SPRAGGON, Glen

IPC分类号： A61P11/00 ,  A61K31/425 ,  A61P11/06 ,  A61K31/444 ,  A61P11/08 ,  C07K5/06 ,  A61K31/401 ,  A61P29/00

CPC分类号： C07K5/06191 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/06086

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

公开(公告)号：EP2104535B1

公开(公告)日：2010-12-29

申请号：EP07854747.8

申请日：2007-11-21

申请人： IRM LLC

发明人： TULLY, David C. ,  CHATTERJEE, Arnab K. ,  VIDAL, Agnes ,  BURSULAYA, Badry ,  SPRAGGON, Glen

IPC分类号： A61P11/00 ,  A61K31/425 ,  A61P11/06 ,  A61K31/444 ,  A61P11/08 ,  C07K5/06 ,  A61K31/401 ,  A61P29/00

CPC分类号： C07K5/06191 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/06086

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

公开(公告)号：EP2190826A2

公开(公告)日：2010-06-02

申请号：EP08798753.3

申请日：2008-08-27

申请人： IRM LLC

发明人： MARSILJE, Thomas H. ,  LU, Wenshuo ,  CHEN, Bei ,  HE, Xiaohui ,  BURSULAYA, Badry ,  LEE, Christian Cho-Hua ,  GRAY, Nathanael S.

IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00 ,  A61P31/00

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF- 1 R) or anaplastic lymphoma kinase (ALK).

公开(公告)号：EP2019837A1

公开(公告)日：2009-02-04

申请号：EP07762204.1

申请日：2007-05-15

申请人： IRM LLC

发明人： TULLY, David, C. ,  CHATTERJEE, Arnab, K. ,  PETRASSI, Hank, Michael, James ,  BURSULAYA, Badry ,  SPRAGGON, Glen

IPC分类号： C07K5/06 ,  C07K5/08 ,  A61K38/55 ,  A61P11/00 ,  A61P11/06 ,  A61P11/10

CPC分类号： C07K5/0806 ,  A61K38/00 ,  C07K5/06165

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

摘要翻译： 本发明提供了可用于调节通道活化蛋白酶的化合物和药物组合物，以及使用这些化合物治疗，改善或预防与通道活化蛋白酶相关的病症的方法，所述病症包括但不限于前列腺素，PRSS22，TMPRSS11（ 例如TMPRSS11B，TMPRSS11E），TMPRSS2，TMPRSS3，TMPRSS4（MTSP-2），matriptase（MTSP-1），CAP2，CAP3，胰蛋白酶，组织蛋白酶A或嗜中性粒细胞弹性蛋白酶。

公开(公告)号：EP2773635A1

公开(公告)日：2014-09-10

申请号：EP13729219.9

申请日：2013-06-05

申请人： IRM LLC

发明人： LELAIS, Gerald ,  EPPLE, Robert ,  MARSILJE, III, Thomas H. ,  MICHELLYS, Pierre-Yves ,  MCNEILL, Matthew H. ,  LONG, Yun ,  LU, Wenshuo ,  CHEN, Bei ,  BURSULAYA, Badry ,  JIANG, Songchun

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D471/04 ,  C07D513/04 ,  A61K31/4439

CPC分类号： C07D401/14 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.

摘要翻译： 本发明提供了可用于调节EGFR活性的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与异常或失调的EGFR活性相关的病症的方法。

公开(公告)号：EP2167498A1

公开(公告)日：2010-03-31

申请号：EP08770796.4

申请日：2008-06-12

申请人： IRM LLC

发明人： BURSULAYA, Badry ,  CHENG, Dai ,  JIANG, Jiqing ,  KARANEWSKY, Donald, S. ,  LIU, Yi ,  PAN, Shifeng ,  WAN, Yongqin ,  WANG, Xia ,  XIE, Yun, Feng ,  YANG, Yang

IPC分类号： C07D413/14 ,  C07D413/02 ,  A61K31/536 ,  A61P37/02

CPC分类号： C07D413/14 ,  C07D413/02

摘要： The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1, 4, 5- trisphosphate 3 -kinase B (ITPKb).

摘要翻译： 本发明提供了一类新的式（I）化合物，包含这些化合物的药物组合物以及使用这些化合物治疗或预防与B细胞活性异常或失调相关的疾病或病症，特别是涉及异常活化 肌醇1,4,5-三磷酸3-激酶B（ITPKb）。

公开(公告)号：EP2057124A2

公开(公告)日：2009-05-13

申请号：EP07799749.2

申请日：2007-07-20

申请人： IRM, LLC

发明人： PAN, Shifeng ,  LIU, Yi ,  XIE, Yun Feng ,  CHENG, Dai ,  WAN, Yongqin ,  HAN, Dong ,  YANG, Yang ,  GAO, Wenqi ,  JIANG, Jiqing ,  BURSULAYA, Badry ,  CHAMBERLAIN, Philip ,  KARANEWSKY, Donald S. ,  WANG, Xia

IPC分类号： C07D231/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D491/048 ,  A61K31/415 ,  A61K31/44 ,  A61P17/00 ,  A61P19/02

CPC分类号： C07D401/12 ,  C07D231/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/08 ,  C07D491/04

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1, 4, 5-trisphosphate 3-kinase B (ITPKb).

公开(公告)号：EP2027143A2

公开(公告)日：2009-02-25

申请号：EP07783835.7

申请日：2007-05-16

申请人： IRM LLC

发明人： TULLY, David C. ,  CHATTERJEE, Arnab K. ,  VIDAL, Agnes ,  PETRASSI, Hank Michael James ,  WANG, Zhiwei ,  BURSULAYA, Badry ,  SPRAGGON, Glen

IPC分类号： C07K5/08 ,  A61K31/423 ,  A61K31/428 ,  A61P11/00

CPC分类号： C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/0827

摘要： The invention provides compounds of formula (1) and pharmaceutically acceptable salts, hydrates, solvates, stereoisomers and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP- 1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.

公开(公告)号：EP2855520A1

公开(公告)日：2015-04-08

申请号：EP13729859.2

申请日：2013-05-31

申请人： IRM LLC

发明人： GEIRSTANGER, Bernhard Hubert ,  GRUNEWALD, Jan ,  BURSULAYA, Badry

IPC分类号： C07K16/00 ,  C07K16/32 ,  C07K7/06 ,  C07K7/08 ,  A61K47/48 ,  C12N9/10

CPC分类号： C07K16/32 ,  A61K47/6815 ,  A61K47/6817 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/00 ,  C07K16/30 ,  C07K2317/24 ,  C07K2317/94 ,  C07K2318/10 ,  C07K2319/90

摘要： The present invention provides methods of site-specific labeling of antibodies, using proteins having 4′-phosphopantetheinyl transferase activity that catalyze post-translational modification of peptide sequences (“peptide tags”) incorporated into one or more specific sites of an antibody of interest. Enzymatic labeling enables quantitative and irreversible covalent modification of a specific serine residue within the peptide tags incorporated into the antibody, and thus creates desirable antibody conjugates.

摘要翻译： 本发明提供的抗体的位点特异性标记的方法，使用具有4'-磷酸转移酶活性的蛋白质也催化掺入感兴趣的抗体的一个或多个特定位点的肽序列（“肽标记”）的翻译后修饰。 酶标记允许掺入抗体的肽标签中的特定丝氨酸残基的定量的和不可逆的共价修饰，并且因此产生所需抗体的缀合物。

公开(公告)号：EP2019837B1

公开(公告)日：2011-03-23

申请号：EP07762204.1

申请日：2007-05-15

申请人： IRM LLC

发明人： TULLY, David, C. ,  CHATTERJEE, Arnab, K. ,  PETRASSI, Hank, Michael, James ,  BURSULAYA, Badry ,  SPRAGGON, Glen

IPC分类号： C07K5/06 ,  C07K5/08 ,  A61K38/05 ,  A61K38/06 ,  A61K38/55 ,  A61P11/00 ,  A61P11/06 ,  A61P11/10

CPC分类号： C07K5/0806 ,  A61K38/00 ,  C07K5/06165

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.