公开(公告)号：WO9640743A3

公开(公告)日：1997-01-23

申请号：PCT/US9609285

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： 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 ,  A61K38/55

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，其盐和与其相关的组合物。 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：WO9614843A3

公开(公告)日：1996-05-23

申请号：PCT/US9514723

申请日：1995-11-09

Applicant: COR THERAPEUTICS INC

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

CPC classification number: A61K31/455 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4439

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. 00000

Abstract translation: 公开了选择性抑制激酶的方法，其包括将含有激酶的组合物与式（I）化合物接触，其中：R 1是低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6- 多芳基，多芳基羰基，多杂芳基或多杂芳基羰基; R 2是低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6-元杂环芳族，低级烃基，5-或6-元杂环芳族羰基，多芳族或多杂芳族; R3是H或低级烷基; R5是H，低级烷基，低级烃基，芳基低级烷基，杂芳基低级烷基，5-或6-元杂环芳族，卤素或氰基; R6为H或低级烃基。 00000

公开(公告)号：CA2224076A1

公开(公告)日：1996-12-19

申请号：CA2224076

申请日：1996-06-05

Applicant: COR THERAPEUTICS INC

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

IPC: A61K38/00 ,  A61P7/02 ,  C07C279/24 ,  C07C281/06 ,  C07C309/30 ,  C07C335/38 ,  C07K5/06 ,  C07K5/068 ,  C07K5/072 ,  C07K5/08 ,  C07K5/09 ,  C07K5/023 ,  C07K5/027 ,  A61K38/06 ,  C07K5/097 ,  G01N1/28

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：AU6590296A

公开(公告)日：1996-12-30

申请号：AU6590296

申请日：1996-06-05

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M JR ,  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 ,  A61K38/55

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：CA2224180A1

公开(公告)日：1996-12-19

申请号：CA2224180

申请日：1996-06-05

Applicant: COR THERAPEUTICS INC

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

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 ,  C07K5/09 ,  C07K5/027 ,  A61K38/06 ,  C07K5/097 ,  G01N1/28

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：NZ312840A

公开(公告)日：1999-11-29

申请号：NZ31284096

申请日：1996-06-05

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M ,  LAIBELMAN ALAN M ,  SINHA UMA ,  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

Abstract: The present invention relates to ketoheterocyclic containing compounds of the formula 1 which are inhibitors of the isolated factor Xa which treats a condition in a mammal characterised by undesired thrombosis. Also claimed is a pharmaceutical composition caused by thrombosis, and a method for inhibiting the coagulation of biological samples.

公开(公告)号：NZ313367A

公开(公告)日：1999-10-28

申请号：NZ31336796

申请日：1996-06-05

Applicant: COR THERAPEUTICS INC

Inventor： MARLOWE CHARLES K ,  SCARBOROUGH ROBERT M ,  LAIBELMAN ALAN 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 ,  C07K5/10 ,  A61K38/55

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：AU4156196A

公开(公告)日：1996-06-06

申请号：AU4156196

申请日：1995-11-09

Applicant: COR THERAPEUTICS INC

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

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 the formula: 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：CA2318199A1

公开(公告)日：1999-07-22

申请号：CA2318199

申请日：1999-01-08

Applicant: COR THERAPEUTICS INC

Inventor： LAIBELMAN ALAN M ,  JANTZEN HANS-MICHAEL ,  CONLEY PAMELA B ,  FRETTO LARRY J ,  SCARBOROUGH ROBERT M

IPC: A61K31/549 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00 ,  A61K31/54 ,  C07D277/00 ,  C07D285/00

Abstract: The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.

公开(公告)号：AU700964B2

公开(公告)日：1999-01-14

申请号：AU4156196

申请日：1995-11-09

Applicant: COR THERAPEUTICS INC

Inventor： GIESE NEILL A ,  LOKKER NATHALIE ,  LAIBELMAN ALAN M ,  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 the formula: 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.