公开(公告)号：AU713235B2

公开(公告)日：1999-11-25

申请号：AU7382896

申请日：1996-09-27

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC

Inventor： FISHER MATTHEW J ,  JAKUBOWSKI JOSEPH A ,  MASTERS JOHN J ,  MULLANEY JEFFREY T ,  PAAL MICHAEL ,  RUHTER GERD ,  RUTERBORIES KENNETH J ,  SCARBOROUGH ROBERT M ,  SCHOTTEN THEO ,  STENZEL WOLFGANG

IPC: A61K31/00 ,  A61K31/42 ,  A61K31/423 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/535 ,  A61K31/537 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/5383 ,  A61P7/00 ,  A61P7/02 ,  C07D221/20 ,  C07D263/52 ,  C07D471/10 ,  C07D498/10 ,  C07D401/06

Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, as shown by formula (I):wherein Q, L, Ai, Bj, R0, R3, R10, m, n, p and q are as defined in the disclosure, which are useful in inhibiting of platelet aggregation.

公开(公告)号：CA2272090A1

公开(公告)日：1998-06-18

申请号：CA2272090

申请日：1997-12-08

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  JAKUBOWSKI JOSEPH A ,  FRANCISKOVICH JEFFRY BERNARD ,  MASTERS JOHN J ,  SMYTH MARK ,  SU TING ,  FISHER MATTHEW J

IPC: A61K31/197 ,  A61K31/27 ,  A61K31/445 ,  A61P9/10 ,  C07C311/06 ,  C07C311/19 ,  C07D211/60 ,  C07D211/62 ,  C07C311/00 ,  A61K31/18 ,  C07D211/04

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

公开(公告)号：CA2233204A1

公开(公告)日：1997-04-03

申请号：CA2233204

申请日：1996-09-27

Applicant: COR THERAPEUTICS INC ,  LILLY CO ELI

Inventor： PAAL MICHAEL ,  RUEHTER GERD ,  SCHOTTEN THEO ,  MULLANEY JEFFREY T ,  RUTHERBORIES KENNETH J ,  MASTERS JOHN J ,  SCARBOROUGH ROBERT M ,  FISHER MATTHEW J ,  JAKUBOWSKI JOSEPH A ,  STENZEL WOLFGANG

IPC: A61K31/00 ,  A61K31/42 ,  A61K31/423 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/535 ,  A61K31/537 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/5383 ,  A61P7/00 ,  A61P7/02 ,  C07D221/20 ,  C07D263/52 ,  C07D471/10 ,  C07D498/10 ,  C07D519/00 ,  C07D401/06 ,  C07D487/10 ,  C07D513/10 ,  C07D491/107 ,  C07D265/12 ,  C07D223/14 ,  A61K31/395 ,  A61K31/675

Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

公开(公告)号：NZ320963A

公开(公告)日：1999-08-30

申请号：NZ32096396

申请日：1996-09-27

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC

Inventor： FISHER MATTHEW J ,  JAKUBOWSKI JOSEPH A ,  MASTERS JOHN J ,  MULLANEY JEFFREY T ,  PAAL MICHAEL ,  RUHTER GERD ,  RUTERBORIES KENNETH J ,  SCARBOROUGH ROBERT M ,  SCHOTTEN THEO ,  STENZEL WOLFGANG

IPC: A61K31/00 ,  A61K31/42 ,  A61K31/423 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/535 ,  A61K31/537 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/5383 ,  A61P7/00 ,  A61P7/02 ,  C07D221/20 ,  C07D263/52 ,  C07D471/10 ,  C07D498/10 ,  C07D401/06 ,  C07D221/00

Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, as shown by formula (I):wherein Q, L, Ai, Bj, R0, R3, R10, m, n, p and q are as defined in the disclosure, which are useful in inhibiting of platelet aggregation.

公开(公告)号：JP2003159088A

公开(公告)日：2003-06-03

申请号：JP2002259364

申请日：2002-09-04

Applicant: UNIV CALIFORNIA ,  COR THERAPEUTICS INC

Inventor： COUGHLIN SHAUN R ,  SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  A61K39/00 ,  A61K39/395 ,  A61K49/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07K7/02 ,  C07K7/06 ,  C07K14/705 ,  C07K16/00 ,  C07K16/28 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/74 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12R1/19 ,  G01N33/53

Abstract: PROBLEM TO BE SOLVED: To provide materials involved in the control of the circulatory system, more specifically, to provide a recombinant material useful for the production of a thrombin receptor, to provide use of the receptor as a diagnostic tool, and to provide a therapeutic agent which either stimulates or blocks thrombin receptor activation and diagnostic compositions relevant to the receptor. SOLUTION: The materials include a mutant thrombin, a DNA molecule, and a recombinant host cell; wherein the mutant thrombin, producible in a recombinant way, is such that the 57- and/or 99- and/or 205-position(s) is (are) different from that(those) in a wild-type thrombin b-chain, the DNA molecule has an expression system capable of producing the thrombin in a host when transformed to the recombinant host and includes a DNA sequence encoding the thrombin linked agonistically to an abnormal regulatory sequence so that the expression system is operable in the host, and the recombinant host cell is subject to transformation by the expression system. COPYRIGHT: (C)2003,JPO

公开(公告)号：JP2002136296A

公开(公告)日：2002-05-14

申请号：JP2001269587

申请日：2001-09-05

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  A61K35/58 ,  A61P7/02 ,  C07K1/00 ,  C07K14/435 ,  C07K14/46 ,  C07K14/75 ,  C07K16/00 ,  C07K16/18 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12P21/02 ,  C12R1/91

Abstract: PROBLEM TO BE SOLVED: To provide another method of antithrombosis treatment by specifically inhibiting the bonding of vWF to a GPIb-IX complex containing platelets. SOLUTION: A DNA molecule composition comprising DNA molecules each containing a sequence encoding a platelet anti-adhesive peptide obtained from snake venoms selected from the following group; Agkistrodon, Bitis, Bothrops, Cerastes, Crotalus, C, Echis carinatus sochurecki, Eristicophis macmahoni, Pseudocerastes persicus, Sistrurus, Trimeresurus, and Vipera.

公开(公告)号：WO0112600A9

公开(公告)日：2002-09-12

申请号：PCT/US0021742

申请日：2000-08-10

Applicant: COR THERAPEUTICS INC ,  ZHU BING-YAN ,  SCARBOROUGH ROBERT M ,  CLIZBE LANE ,  DOUGHAN BRANDON ,  JIA ZHAOZHONG-JON ,  KANE-MAGUIRE KIM ,  MARLOWE CHARLES ,  SONG YONGHONG ,  SU TING ,  TENG WILLY ,  ZHANG PENGLIE

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M ,  CLIZBE LANE ,  DOUGHAN BRANDON ,  JIA ZHAOZHONG-JON ,  KANE-MAGUIRE KIM ,  MARLOWE CHARLES ,  SONG YONGHONG ,  SU TING ,  TENG WILLY ,  ZHANG PENGLIE

IPC: C07D209/08 ,  C07D209/34 ,  C07D209/38 ,  C07D215/08 ,  C07D215/22 ,  C07D215/227 ,  C07D231/56 ,  C07D235/06 ,  C07D235/26 ,  C07D241/38 ,  C07D241/44 ,  C07D243/24 ,  C07D265/36 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D209/04 ,  C07D215/00 ,  C07D235/04 ,  C07D241/36 ,  C07D403/02 ,  C07D498/02

CPC classification number: C07D215/227 ,  C07D209/08 ,  C07D209/34 ,  C07D209/38 ,  C07D215/08 ,  C07D231/56 ,  C07D235/06 ,  C07D235/26 ,  C07D241/38 ,  C07D241/44 ,  C07D243/24 ,  C07D265/36 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) 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，其盐和与其相关的组合物。 式（I）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：WO0216360A3

公开(公告)日：2002-06-13

申请号：PCT/US0141749

申请日：2001-08-17

Applicant: COR THERAPEUTICS INC ,  KYOWA HAKKO KOGYO KK ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT M ,  MATSUNO KENJI ,  ICHIMURA MICHIO ,  NOMOTO YUJI ,  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: A61P35/00 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  A61K31/517 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

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.

Abstract translation: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化症。

公开(公告)号：WO0172708A3

公开(公告)日：2002-05-23

申请号：PCT/US0109374

申请日：2001-03-26

Applicant: COR THERAPEUTICS INC ,  MARLOWE CHARLES K ,  KANE MAGUIRE KIM A ,  ZHU BING YAN ,  SCARBOROUGH ROBERT M

Inventor： MARLOWE CHARLES K ,  KANE-MAGUIRE KIM A ,  ZHU BING-YAN ,  SCARBOROUGH ROBERT M

IPC: A61P7/02 ,  C07D401/12 ,  A61K31/454

CPC classification number: C07D401/12

Abstract: Novel compounds of formula (I), including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

Abstract translation: 描述了新的式（I）化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和具有抗哺乳动物因子Xa活性的前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内用于预防或治疗特征在于不期望的血栓形成的哺乳动物中的病症。

公开(公告)号：WO0226712A2

公开(公告)日：2002-04-04

申请号：PCT/US0142352

申请日：2001-10-01

Applicant: COR THERAPEUTICS INC ,  ZHANG PENGLIE ,  ZUCKETT JINGMEI FAN ,  BAO LIANG ,  SCARBOROUGH ROBERT M ,  ZHU BING YAN

Inventor： ZHANG PENGLIE ,  ZUCKETT JINGMEI FAN ,  BAO LIANG ,  SCARBOROUGH ROBERT M ,  ZHU BING-YAN

IPC: A61P7/00 ,  C07D213/74 ,  C07D213/81 ,  C07D409/12 ,  C07D213/00

CPC classification number: C07D213/74 ,  C07D213/81 ,  C07D409/12

Abstract: Novel quaternary amine-containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

Abstract translation: 描述了具有抗哺乳动物因子Xa的活性的新型含季铵化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物可用于体外或体内用于预防或治疗特征在于不希望的血栓形成的哺乳动物的状况。