公开(公告)号：EP2168581A2

公开(公告)日：2010-03-31

申请号：EP09150479.5

申请日：2000-11-09

申请人： OSI Pharmaceuticals, Inc.

发明人： Connell, Richard, D. ,  Moyer, James, D. ,  Morin, Michael, J. ,  Kajiji, Shama, M. ,  Foster, Barbara, A. ,  Ferrante, Karen, J. ,  Norris, Timothy ,  Raggon, Jeffrey, W. ,  Silberman, Sandra, L.

IPC分类号： A61K31/505 ,  C07D239/94

CPC分类号： A61K45/06 ,  A61K31/517 ,  C07D239/94 ,  A61K2300/00

摘要： The present invention relates to crystalline forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride, their production in essentially pure form, and their use. The invention also relates to the pharmaceutical compositions containing the crystalline forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine as hydrochloride and to methods of treating hyperproliferative disorders, such as cancer, by administering the compound.

摘要翻译： 本发明涉及N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺盐酸盐，它们在本质上纯的形式生产，并且它们的使用的结晶形式。 因此，本发明涉及含有N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺盐酸盐的结晶形式，药物组合物和治疗过度增殖性疾病，：如癌症的方法，通过 给予化合物。

公开(公告)号：EP2152671A1

公开(公告)日：2010-02-17

申请号：EP08750765.3

申请日：2008-05-22

申请人： Prosidion Limited

发明人： BLOXHAM, Jason ,  BRADLEY, Stuart, Edward ,  DUPREE, Tom, Banksia ,  FRY, Peter, Timothy ,  HANRAHAN, Patrick, Eric ,  KRULLE, Thomas, Martin ,  PROCTER, Martin, James ,  SAMBROOK-SMITH, Colin, Peter ,  SCHOFIELD, Karen, Lesley ,  SMYTH, Donald ,  STEWART, Alan, John, William

IPC分类号： C07D213/62 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/44 ,  A61P3/04

CPC分类号： C07D213/62 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu- opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity.

公开(公告)号：EP1658289B1

公开(公告)日：2009-03-18

申请号：EP04781205.2

申请日：2004-08-16

申请人： OSI Pharmaceuticals, Inc.

发明人： CASTELHANO, Arlindo, L. ,  CREW, Andrew, Phillip ,  DONG, Han-Qing ,  LAUFER, Radoslaw ,  LI, An-Hu ,  QIU, Li ,  SAMBROOK SMITH, Colin, Peter ,  ZHANG, Tao

IPC分类号： C07D471/04 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D471/04

摘要： Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.

公开(公告)号：EP1819332B1

公开(公告)日：2009-03-11

申请号：EP05821654.0

申请日：2005-12-02

申请人： Prosidion Limited

发明人： KRULLE, Thomas Martin ,  ROWLEY, Robert John ,  THOMAS, Gerard Hugh

IPC分类号： A61K31/437 ,  A61K31/4375 ,  A61P3/10 ,  C07K5/078 ,  C07K5/097 ,  A61K38/05 ,  A61K38/06

CPC分类号： C07D471/04 ,  A61K38/00 ,  C07K5/06139

摘要： Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.

公开(公告)号：EP1283735B1

公开(公告)日：2008-12-31

申请号：EP01927848.0

申请日：2001-04-02

申请人： Prosidion Limited

发明人： DEMUTH, Hans-Ulrich ,  GLUND, Konrad

IPC分类号： A61P3/10 ,  A61K31/00 ,  A61K31/40 ,  A61K31/426

CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/40 ,  A61K31/426 ,  Y10S514/866

摘要： The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic β-cells and to cause differentiation of pancreatic epithelial cells into insulin producing β-cells. Oral administration of a DP IV inhibitor causes the active form of GLP-1 to be preserved longer under physiological conditions. The extended presence of GLP-1, in particular in the pancreatic tissue facilitates differentiation and regeneration of the β-cells already present that are in need of repair. These repaired insulin producing cells can contribute to the correction and maintenance of normal physiological glycemic levels.

公开(公告)号：EP1996193A2

公开(公告)日：2008-12-03

申请号：EP07753017.8

申请日：2007-03-13

申请人： OSI Pharmaceuticals, Inc.

发明人： BUCK, Elizabeth, A. ,  GRIFFIN, Graeme ,  BARR, Sharon, M.

IPC分类号： A61K31/436 ,  A61K31/498 ,  A61K45/06 ,  A61P35/00

CPC分类号： A61K45/06 ,  A61K31/436 ,  A61K31/498 ,  A61K2300/00

摘要： The present invention provides a method for manufacturing a medicament intended for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in combination with an EGFR kinase inhibitor, characterized in that an mTOR inhibitor is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for manufacturing a medicament intended for treating tumors or tumor metastases in a patient in combination of an EGFR kinase inhibitor, characterized in that an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).

公开(公告)号：EP1963320A1

公开(公告)日：2008-09-03

申请号：EP06839003.8

申请日：2006-12-05

申请人： OSI Pharmaceuticals, Inc.

发明人： DONG, Han-qing ,  FOREMAN, Kenneth ,  LI, An-Hu ,  MULVIHILL, Mark, Joseph ,  PANICKER, Bijoy ,  STEINIG, Arno, G. ,  STOLZ, Kathryn, M. ,  WENG, Qinghua ,  JIN, Meizhong ,  VOLK, Brian ,  WANG, Jing ,  WANG, Ti ,  BEARD, James, D.

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D471/04

摘要： Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least one of the Ab1, Aurora-A, BIk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-IR, Ron, Met, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.

摘要翻译： 由式（I）表示的化合物或其立体异构体或药学上可接受的盐是Ab1，Aurora-A，BIk，c-Raf，cSRC，Src，PRK2，FGFR3，Flt3，Lck，Mek1，PDK中至少一种的抑制剂 -1，GSK3β，EGFR，p70S6K，BMX，SGK，CaMKII，Tie-2，IGF-1R，Ron，Met和KDR激酶用于治疗和/或预防各种疾病和病症，例如 癌症。

公开(公告)号：EP1959925A2

公开(公告)日：2008-08-27

申请号：EP06851156.7

申请日：2006-12-01

申请人： (OSI) Eyetech, Inc.

发明人： CAMPBELL, Kathleen, M. ,  CALIAS, Perry ,  COOK, Gary, P. ,  GANLEY, Mary, A.

IPC分类号： A61K9/00 ,  A61K9/50 ,  A61K31/00

CPC分类号： A61K38/1866 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/1647 ,  A61K31/00

摘要： Formulations for controlled, sustained release of biologically active agents for the treatment of ocular disorders have been developed. These formulations are based on solid microparticles formed of the combination of biodegradable, synthetic polymers such as poly(lactic acid) (PLA), poly(glycolic acid) (PGA), and copolymers thereof. The microparticles are characterized by low burst levels and efficient drug loading and sustained release.

公开(公告)号：EP1075539B1

公开(公告)日：2008-08-06

申请号：EP99923518.7

申请日：1999-04-28

申请人： SMITHKLINE BEECHAM PLC

发明人： CLARKE, Stephen, Edward

IPC分类号： C12Q1/26 ,  C07D311/16

CPC分类号： C07D311/16 ,  C12Q1/26

摘要： Coumarin derivatives as substrates for cytochrome P450 enzyme.

摘要翻译： 香豆素衍生物作为细胞色素P450酶的底物。

公开(公告)号：EP1883638A1

公开(公告)日：2008-02-06

申请号：EP06740222.2

申请日：2006-03-30

申请人： OSI Pharmaceuticals, Inc.

发明人： CREW, Andrew, Philip ,  DONG, Han-Qing ,  PANICKER, Bijoy

IPC分类号： C07D487/04 ,  A61K31/4188 ,  A61P35/00

CPC分类号： C07D487/04

摘要： Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.