公开(公告)号：NO304267B1

公开(公告)日：1998-11-23

申请号：NO914962

申请日：1991-12-16

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  WOLF DAVID LAWRENCE ,  CHARO ISRAEL F

IPC: A61K35/58 ,  A61K38/02 ,  A61K38/12 ,  A61K38/17 ,  A61K38/36 ,  A61K38/57 ,  A61K38/00 ,  A61P7/02 ,  C07K1/14 ,  C07K1/20 ,  C07K7/00 ,  C07K7/06 ,  C07K7/64 ,  C07K14/00 ,  C07K14/435 ,  C07K14/46 ,  C07K14/745 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78 ,  C12N1/21 ,  C12N15/09 ,  C12N15/12 ,  C12P21/00 ,  C12P21/02 ,  C12Q1/56 ,  C12R1/19 ,  G01N33/86 ,  C07K14/81 ,  G01N33/566

Abstract: An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formula R 2 N(CH2)4CHNHCO- wherein each R is independently H, alkyl(1-6C) or at most one R is R -C=NR wherein R is H, alkyl(1-6C), phenyl or benzyl, or is NR 2 in which each R is independently H or alkyl(1-6C) and R is H, alkyl(1-6C), phenyl or benzyl, or R -C=NR is a radical selected from the group consisting of: where m is an integer of 2-3, and each R is independently H or alkyl(1-6C); and wherein one or two (CH2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

公开(公告)号：MX9709908A

公开(公告)日：1998-07-31

申请号：MX9709908

申请日：1997-12-08

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M ,  ZHU BING-YAN

IPC: C07D277/24 ,  A61K31/42 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K38/00 ,  A61P7/02 ,  A61P9/00 ,  C07C311/64 ,  C07D263/14 ,  C07D263/56 ,  C07D277/68 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078 ,  C07K5/08 ,  C07K05/06 ,  A61K38/05

Abstract: Se describen compiestos novedosos, sus sales y composiciones relacionadas con los mismos que tienen actividad contra el factor Xade mamífero; los compuestos son utiles in vitro o in vivo para prevenir o tratar trastornos de coagulacion.

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：ZA964754B

公开(公告)日：1997-03-11

申请号：ZA964754

申请日：1996-06-06

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  MARLOWE CHARLES K ,  ZHU BING-YAN

IPC: C07D277/24 ,  A61K31/42 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K38/00 ,  A61P7/02 ,  A61P9/00 ,  C07C311/64 ,  C07D263/14 ,  C07D263/56 ,  C07D277/68 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/078 ,  C07K5/08 ,  C07K ,  A61K

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

公开(公告)号：ZA964753B

公开(公告)日：1997-02-27

申请号：ZA964753

申请日：1996-06-06

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  LAIBELMAN ALAN M ,  SCARBOROUGH ROBERT M ,  SINHA UMA ,  ZHU BING-YAN

IPC: A61P7/02 ,  C07C279/24 ,  C07C281/06 ,  C07C309/30 ,  A61K38/00 ,  C07C335/38 ,  C07K5/06 ,  C07K5/068 ,  C07K5/072 ,  C07K5/08 ,  A61K ,  C07D ,  C07C

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.

公开(公告)号：ZA9604753B

公开(公告)日：1997-02-27

申请号：ZA9604753

申请日：1996-06-06

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M ,  LAIBELMAN ALAN M ,  SINHA UMA ,  ZHU BING-YAN

IPC: A61K38/00 ,  A61P7/02 ,  C07C279/24 ,  C07C281/06 ,  C07C309/30 ,  C07C335/38 ,  C07K5/06 ,  C07K5/068 ,  C07K5/072 ,  C07K5/08 ,  A61K ,  C07C ,  C07D

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

公开(公告)号：CA2203517A1

公开(公告)日：1996-05-23

申请号：CA2203517

申请日：1995-11-09

Applicant: COR THERAPEUTICS INC

Inventor： LOKKER NATHALIE ,  LAIBELMAN ALAN M ,  GIESE NEILL A ,  SCARBOROUGH ROBERT M

IPC: C07D231/38 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/455 ,  A61P43/00 ,  C07D231/40 ,  C07D401/06 ,  C07D405/04 ,  C07D409/06

Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5 or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl.

公开(公告)号：NO914962A

公开(公告)日：1992-01-31

申请号：NO914962

申请日：1991-12-16

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  WOLF DAVID LAWRENCE ,  CHARO ISRAEL F

IPC: A61K38/00 ,  A61K35/58 ,  A61K38/02 ,  A61K38/12 ,  A61K38/17 ,  A61K38/36 ,  A61K38/57 ,  A61P7/02 ,  C07K1/14 ,  C07K1/20 ,  C07K7/00 ,  C07K7/06 ,  C07K7/64 ,  C07K14/00 ,  C07K14/435 ,  C07K14/46 ,  C07K14/745 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78 ,  C12N1/21 ,  C12N15/09 ,  C12N15/12 ,  C12P21/00 ,  C12P21/02 ,  C12Q1/56 ,  C12R1/19 ,  G01N33/86 ,  A61K37/64 ,  G01N33/566

CPC classification number: C07K14/75 ,  A61K38/12 ,  A61K38/1703 ,  A61K38/57 ,  C07K14/46 ,  C07K14/755 ,  C07K14/78

公开(公告)号：FI915919A0

公开(公告)日：1991-12-16

申请号：FI915919

申请日：1991-12-16

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  WOLF DAVID LAWRENCE ,  CHARO ISRAEL F

IPC: A61K38/00 ,  A61K35/58 ,  A61K38/02 ,  A61K38/12 ,  A61K38/17 ,  A61K38/36 ,  A61K38/57 ,  A61P7/02 ,  C07K1/14 ,  C07K1/20 ,  C07K7/00 ,  C07K7/06 ,  C07K7/64 ,  C07K14/00 ,  C07K14/435 ,  C07K14/46 ,  C07K14/745 ,  C07K14/75 ,  C07K14/755 ,  C07K14/78 ,  C12N1/21 ,  C12N15/09 ,  C12N15/12 ,  C12P21/00 ,  C12P21/02 ,  C12Q1/56 ,  C12R1/19 ,  G01N33/86 ,  A61K

Abstract: An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formula R 2 N(CH2)4CHNHCO- wherein each R is independently H, alkyl(1-6C) or at most one R is R -C=NR wherein R is H, alkyl(1-6C), phenyl or benzyl, or is NR 2 in which each R is independently H or alkyl(1-6C) and R is H, alkyl(1-6C), phenyl or benzyl, or R -C=NR is a radical selected from the group consisting of: where m is an integer of 2-3, and each R is independently H or alkyl(1-6C); and wherein one or two (CH2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.

公开(公告)号：AU747531B2

公开(公告)日：2002-05-16

申请号：AU6962398

申请日：1998-04-13

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M ,  ZHU BING-YAN

IPC: A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61P7/02 ,  A61P43/00 ,  C07D211/26 ,  C07D241/08 ,  C07D243/08 ,  C07D295/15 ,  C07D295/205 ,  C07D401/06 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/062 ,  C07K5/083 ,  C07D295/20

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.