公开(公告)号：EP1309569A2

公开(公告)日：2003-05-14

申请号：EP01973654.5

申请日：2001-08-17

Applicant: Millennium Pharmaceuticals, Inc. ,  KYOWA HAKKO KOGYO CO., LTD. ,  Pandey, Anjali ,  Scarborough, Robert M. ,  Matsuno, Kenji ,  Ichimura, Michio ,  Nomoto, Yugi ,  Fujiwara, Shigeki ,  Ide, Shinichi ,  Tsukuda, Eiji ,  Irie, Junko ,  Oda, Shoji

Inventor： PANDEY, Anjali ,  SCARBOROUGH, Robert, M. ,  MATSUNO, Kenji ,  ICHIMURA, Michio ,  NOMOTO, Yuji ,  FUJIWARA, Shigeki ,  IDE, Shinichi ,  TSUKUDA, Eiji ,  IRIE, Junko ,  ODA, Shoji

IPC: C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D403/12

Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

公开(公告)号：WO2008086188A2

公开(公告)日：2008-07-17

申请号：PCT/US2008/050244

申请日：2008-01-04

Applicant: MILLENNIUM PHARMACEUTICALS, INC. ,  ZHU, Bing-yan ,  BAUER, Shawn M. ,  JIA, Zhaozhong J. ,  SONG, Yonghong ,  PROBST, Gary D. ,  ZHANG, Yanchen ,  SCARBOROUGH, Carroll, Executrix For Scarborough, Robert M. (deceased)

Inventor： ZHU, Bing-yan ,  BAUER, Shawn M. ,  JIA, Zhaozhong J. ,  SONG, Yonghong ,  PROBST, Gary D. ,  ZHANG, Yanchen ,  SCARBOROUGH, Carroll, Executrix For Scarborough, Robert M. (deceased)

IPC: C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/421 ,  A61P9/00

CPC classification number: C07D409/14 ,  C07D333/38 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

Abstract translation: 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，酯或前药，其是因子Xa的抑制剂。 本发明还涉及用于制备这种化合物的中间体，含有这些化合物的药物组合物，预防或治疗多种不想要的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

公开(公告)号：WO2006055951A3

公开(公告)日：2006-05-26

申请号：PCT/US2005/042293

申请日：2005-11-21

Applicant: PORTOLA PHARMACEUTICALS, INC. ,  SONG, Yonghong ,  ZHU, Bing-Yan ,  WANG, Shumei ,  BAUER, Shawn ,  SCARBOROUGH, Robert, M.

Inventor： SONG, Yonghong ,  ZHU, Bing-Yan ,  WANG, Shumei ,  BAUER, Shawn ,  SCARBOROUGH, Robert, M.

IPC: C07D207/00 ,  A61K31/47

Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

公开(公告)号：WO2004060362B1

公开(公告)日：2004-10-07

申请号：PCT/US0341620

申请日：2003-12-29

Applicant: MILLENNIUM PHARM INC ,  SCARBOROUGH ROBERT M ,  PANDEY ANJALI ,  MEHROTRA MUKUND

Inventor： SCARBOROUGH ROBERT M ,  PANDEY ANJALI ,  MEHROTRA MUKUND

IPC: A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/506 ,  A61P7/02 ,  A61P9/10 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D401/04 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/506 ,  C07D413/04 ,  C07D417/04

Abstract: This invention provides compounds that are inhibitors of the TGF-beta signaling pathway. The compounds are represented by formula (I), where A' is N or CH; Ring B is preferably a triazolyl, imidazolyl, or thiazolyl ring; -X-D- is a linker group; and G is an optionally substituted aryl or heteroaryl ring. The compounds are useful for treating cardiovascular disease.

Abstract translation: 本发明提供了作为TGF-β信号传导途径抑制剂的化合物。 该化合物由式（I）表示，其中A'是N或CH; 环B优选为三唑基，咪唑基或噻唑基环; -X-D-是连接基团; G是任选取代的芳基或杂芳基环。 这些化合物可用于治疗心血管疾病。

公开(公告)号：WO0194331A8

公开(公告)日：2003-11-06

申请号：PCT/US0118014

申请日：2001-06-01

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC ,  ANTOINE LUC ,  BOQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  VAN HOECK JEAN-PIERRE

Inventor： ANTOINE LUC ,  BOQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  VAN HOECK JEAN-PIERRE

IPC: C07D311/58 ,  C07D311/70 ,  A61K31/353 ,  A61P7/02

CPC classification number: C07D311/58

Abstract: Disclosed are processes for producing benzopyran compounds, reduced 2-(chroman-2-yl) acetic acid compounds and 2-(6-aminochroman-2-yl)acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

Abstract translation: 公开了制备苯并吡喃化合物，还原的2-（色满-2-基）乙酸化合物和2-（6-氨基苯并二氢吡喃-2-基）乙酸酯的方法，其为制备血小板聚集抑制剂的中间体和/或本身是有效的 血小板聚集抑制剂。

公开(公告)号：WO2002072578A3

公开(公告)日：2002-09-19

申请号：PCT/US2002/007187

申请日：2002-03-08

Applicant: MILLENNIUM PHARMACEUTICALS ,  SCARBOROUGH, Robert, M. ,  PANDEY, Anjali

Inventor： SCARBOROUGH, Robert, M. ,  PANDEY, Anjali

IPC: D01F6/52

Abstract: The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. More particularly, the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

公开(公告)号：WO0192249A3

公开(公告)日：2002-04-11

申请号：PCT/US0118016

申请日：2001-06-01

Applicant: COR THERAPEUTICS INC ,  KANTER JAMES ,  MARLOWE CHARLES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  BUTKE GREG ,  JACOBSEN BARRY ,  WALKER DERRICK

Inventor： KANTER JAMES ,  MARLOWE CHARLES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  BUTKE GREG ,  JACOBSEN BARRY ,  WALKER DERRICK

IPC: C07D311/20 ,  C07D311/22 ,  C07D311/58 ,  A61K31/35

CPC classification number: C07D311/58 ,  C07D311/20 ,  C07D311/22

Abstract: Disclosed are processes for producing a (2S) or (2R) 4-oxo-chroman-2-yl acyl compounds and chroman-2-yl acyl compounds, esters or amides thereof as well as derivatives thereof. Such processes may involve chiral synthesis or achiral synthesis, preferably coupled with a resolution procedure. Such compounds, particularly (2S) or (2R) acetic acid esters, are useful intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are processes for making derivatives of such substantially pure, or enhanced compositions of single (2R) or (2S) enantiomer intermediates or processes for producing final products or salts from such desired enantiomers.

Abstract translation: 公开了制备（2S）或（2R）-4-氧代 - 苯并二氢吡喃-2-基酰基化合物和色满-2-基酰基化合物，其酯或酰胺及其衍生物的方法。 这样的方法可以涉及手性合成或非手性合成，优选与解析程序偶联。 这些化合物，特别是（2S）或（2R）乙酸酯是生产血小板聚集抑制剂和/或本身是有效的血小板聚集抑制剂的有用中间体。 进一步公开的是制备单一（2R）或（2S）对映异构体中间体的这种基本上纯的或增强的组合物的衍生物的方法或从所需的对映异构体制备最终产物或盐的方法。

公开(公告)号：WO1996040743A2

公开(公告)日：1996-12-19

申请号：PCT/US1996009285

申请日：1996-06-05

Applicant: COR THERAPEUTICS, INC. ,  MARLOWE, Charles, K. ,  SCARBOROUGH, Robert, M. ,  LAIBELMAN, Alan, M. ,  SINHA, Uma ,  ZHU, Bing-Yan

Inventor： COR THERAPEUTICS, INC.

IPC: C07K05/06

CPC classification number: C07K5/06095 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06086 ,  C07K5/06191

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract translation: 公开了与哺乳动物因子Xa具有活性的新型化合物，其盐和与其有关的组合物。 该化合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：GB201416934D0

公开(公告)日：2014-11-12

申请号：GB201416934

申请日：2014-09-25

Applicant: SCARBOROUGH ROBERT

公开(公告)号：GB2471206A

公开(公告)日：2010-12-22

申请号：GB201011699

申请日：2009-06-04

Applicant: SCARBOROUGH ROBERT JAMES

Inventor： SCARBOROUGH ROBERT JAMES

IPC: A63H18/02 ,  A63H21/00 ,  A63H33/00 ,  A63H33/32 ,  B62B15/00

Abstract: An integral releasable fastening means on a flexible sheet or sheets 1 comprises an integral hook like member 10 and corresponding integral slits 11 formed on the side edges of the sheet/s. The hook like members 10 are adapted to engage with a corresponding slit 11 to secure the sheet/s in a desired configuration. The fastenings allow different parts of the same sheet to be fastened together creating chosen curved configurations 4, or allow a plurality of sheets to be fastened together. The sheet/s may be arranged into chosen arrangements for multiple uses dependant on the sheet/s size and configuration formed. The sheet/s may be of a composition allowing repeat application and removal of graphics.