公开(公告)号：EP1959961A2

公开(公告)日：2008-08-27

申请号：EP06850222.8

申请日：2006-12-01

申请人： Rigel Pharmaceuticals, Inc.

发明人： PARMAR, Manjeet M.

IPC分类号： A61K31/538

CPC分类号： A61K31/538 ,  A61K9/127 ,  A61K31/70

摘要： The present invention provides formulations containing at least one unsaturated amphiphilic lipid and an amphipathic or hydrophobic drug and methods of making these formulations. In particular, the present invention provides formulations of at least one unsaturated phospholipid and an amphipathic or hydrophobic pyrimidine drug, methods of making these formulations and the use of such formulations in a variety of contexts, including, for example, the treatment of proliferative disorders, such as tumors and cancers.

公开(公告)号：EP1699446B1

公开(公告)日：2008-05-28

申请号：EP04814853.0

申请日：2004-12-18

申请人： Rigel Pharmaceuticals, Inc.

发明人： HOLSZTYNSKA, Elzbieta, J. ,  LO, Ray ,  SUN, Thomas, W. ,  WANG, Steven, X.

IPC分类号： A61K31/16

CPC分类号： C07D413/04 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2077 ,  A61K31/42 ,  A61K31/4439 ,  C07D261/08

摘要： Provided are compositions and methods for protecting a compound comprising a haloalkylamide moiety from metabolic transformation by hydrolases. In one aspect, the disclosure is directed to increasing the bioavailability and tissue delivery of a anti-HCV compound comprising a haloalkylamide moiety by protecting the compound from inactivation by carboxylesterases. Specific approaches for limiting metabolic transformation include use of carboxylesterase inhibitors to inhibit metabolism of the compound, or use of orally administered compositions designed to deliver the compound to the small intestine or large intestine. Further provided are methods of treating or preventing HCV infection in a subject.

公开(公告)号：EP1922310A2

公开(公告)日：2008-05-21

申请号：EP06814315.5

申请日：2006-09-07

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  SYLVAIN, Catherine ,  HOLLAND, Sacha ,  ZHANG, Jing ,  PARTRIDGE, John J. ,  CLOUGH, Jeffrey ,  ARGADE, Ankush

IPC分类号： C07D249/14 ,  A61K31/4196 ,  A61P35/00

CPC分类号： C07D403/12 ,  C07D249/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Triazole derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using tfrs* derivatives in treating diseases or conditions associated with AxI catalytic activity are also disclosed.

公开(公告)号：EP1716416A4

公开(公告)日：2008-02-13

申请号：EP05723184

申请日：2005-02-16

申请人： RIGEL PHARMACEUTICALS INC

发明人： LORENS JAMES ,  HOLLAND SACHA J ,  XU WEIDUAN

IPC分类号： G01N33/53 ,  A61K31/7105 ,  A61K39/395 ,  G01N33/50 ,  G01N33/574

CPC分类号： G01N33/5029 ,  G01N33/5011 ,  G01N33/5064

公开(公告)号：EP1689850A4

公开(公告)日：2008-02-13

申请号：EP04810665

申请日：2004-11-10

申请人： RIGEL PHARMACEUTICALS INC

发明人： PAYAN DONALD G ,  JENKINS YONCHU

IPC分类号： C12Q1/70 ,  A61K38/17 ,  A61K39/21 ,  C07K1/00 ,  C12N20060101 ,  G01N33/569

CPC分类号： G01N33/56988 ,  G01N2333/163 ,  G01N2333/9015

公开(公告)号：EP1856135A1

公开(公告)日：2007-11-21

申请号：EP06718943.1

申请日：2006-01-19

申请人： Rigel Pharmaceuticals, Inc.

发明人： SINGH, Rajinder ,  BHAMIDIPATI, Somasekhar ,  MASUDA, Esteban

IPC分类号： C07F9/6561 ,  C07D498/04 ,  A61K31/675 ,  A61K31/5383 ,  A61P37/00

CPC分类号： C07D498/04 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65742

摘要： The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

公开(公告)号：EP1268847B1

公开(公告)日：2007-11-07

申请号：EP01924655.2

申请日：2001-04-03

申请人： Rigel Pharmaceuticals, Inc.

发明人： ISSAKANI, Sarkiz, D. ,  HUANG, Jianing ,  SHEUNG, Julie ,  PRAY, Todd, R.

IPC分类号： C12Q1/25 ,  G01N33/573 ,  G01N33/543 ,  G01N33/58

CPC分类号： G01N33/582 ,  C12Q1/25 ,  C12Q1/37 ,  G01N33/573 ,  G01N2333/9015 ,  G01N2500/00 ,  Y10S436/805

摘要： The invention relates to assays for measuring ubiquitin ligase activity and for identifying modulators of ubiquitin ligase enzymes.

公开(公告)号：EP0693126B9

公开(公告)日：2007-09-12

申请号：EP94912387.1

申请日：1994-04-01

申请人： Rigel Pharmaceuticals, Inc.

发明人： MILES, Vincent J. ,  MATHEWS, Michael B. ,  KATZE, Michael G. ,  WITHERELL, Gary ,  WATSON, Julia C.

IPC分类号： C12N15/64 ,  C12N15/62 ,  C12N15/81 ,  C12N15/85 ,  C12N15/11 ,  C12N9/12 ,  C12N1/19 ,  C12Q1/48 ,  C12Q1/68 ,  A61K48/00

CPC分类号： C12N15/1131 ,  A61K48/00 ,  C07K14/4703 ,  C07K2319/00 ,  C12N9/12 ,  C12N15/67 ,  C12N15/81 ,  C12Q1/6897 ,  C12Q1/70

公开(公告)号：EP1824489A2

公开(公告)日：2007-08-29

申请号：EP05844183.3

申请日：2005-11-15

申请人： Rigel Pharmaceuticals, Inc.

发明人： ARGADE, Ankush ,  SINGH, Rajinder ,  LI, Hui

IPC分类号： A61K31/506 ,  A61K31/4353

CPC分类号： C07D239/48 ,  A61K31/495 ,  C07D413/12

摘要： The present invention provides stereoisomers and stereoisomeric mixtures of 3­-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.

公开(公告)号：EP1497461A4

公开(公告)日：2007-06-06

申请号：EP03719802

申请日：2003-04-15

申请人： RIGEL PHARMACEUTICALS INC

发明人： HITOSHI YASUMICHI ,  JENKINS YONCHU

IPC分类号： C12Q1/68 ,  G01N33/50 ,  G01N33/574 ,  G01N33/68 ,  A61K39/395

CPC分类号： G01N33/5091 ,  C12Q1/6886 ,  C12Q2600/158 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/574 ,  G01N33/6872 ,  G01N2333/4703 ,  G01N2500/00