公开(公告)号：WO0216362A3

公开(公告)日：2002-06-13

申请号：PCT/US0141751

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

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: 本发明涉及对激酶的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，其抑制这些激酶的活性。 本发明还涉及抑制激酶并通过抑制激酶的磷酸化来治疗哺乳动物的疾病状态的方法。 本发明的一个特定方面提供了抑制PDGF受体的磷酸化以阻碍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，血管性 重建，癌症和肾小球硬化。

公开(公告)号：WO0119798A2

公开(公告)日：2001-03-22

申请号：PCT/US0025195

申请日：2000-09-15

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  JIA ZHAOZHONG JON ,  HUANG WENRONG ,  SONG YONGHONG ,  KANTER JAMES ,  SCARBOROUGH ROBERT M

IPC: C07D231/14 ,  A61K31/33 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61P7/02 ,  A61P7/04 ,  A61P43/00 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D277/20 ,  C07D277/56 ,  C07D333/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07D231/00

CPC classification number: C07D213/75 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/56 ,  C07D333/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of formula A Q D E G J X in which D is a direct link, a substituted or unsubsituted phenyl or naphtyl gourp or a heterocyclic ring system; G is substituted or unsubstituted phenyl or a heterocyclic ring system; X is a substituted or unsubstituted phenyl or naphtyl group or a heterocyclic ring system; and the other variables are as defined in the claims, 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: 其中D是直接键，取代或未取代的苯基或萘基金属或杂环系的式A Q D E G J X的化合物; G是取代或未取代的苯基或杂环系; X是取代或未取代的苯基或萘基或杂环系; 并且其它变量如权利要求中所定义，其公开的与其相关的盐和组合物具有抗哺乳动物因子Xa的活性。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：WO0071515A3

公开(公告)日：2001-01-25

申请号：PCT/US0014193

申请日：2000-05-24

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61K31/401 ,  A61K31/402 ,  A61K31/451 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  C07C311/46 ,  C07D207/16 ,  C07D211/60 ,  C07D241/04 ,  C07D243/08 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  A61K31/40 ,  A61P7/00 ,  C07C311/39

CPC classification number: C07D401/04 ,  C07C311/46 ,  C07D207/16 ,  C07D211/60 ,  C07D241/04 ,  C07D243/08 ,  C07D403/04 ,  C07D413/04

Abstract: Compounds, e.g. described in Table (1), 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: 化合物，例如 在表（1）中描述了它们与其相关的盐和组合物具有抗哺乳动物因子Xa的活性。 该化合物可用于体内或体内用于预防或治疗凝血障碍。

公开(公告)号：EP0804452A4

公开(公告)日：1998-08-12

申请号：EP94925135

申请日：1994-07-26

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M ,  SUNDELIN JOHAN

IPC: C12N15/09 ,  A61K38/00 ,  A61K48/00 ,  C07H21/04 ,  C07K7/06 ,  C07K7/08 ,  C07K14/705 ,  C07K14/72 ,  C07K16/28 ,  C12N5/10 ,  C12P21/02 ,  C12R1/91 ,  C07H21/00 ,  C07K2/00 ,  C07K7/00

CPC classification number: C07K7/06 ,  A61K38/00 ,  A61K48/00 ,  C07K7/08 ,  C07K14/723

Abstract: The DNA encoding the C140 cell surface receptor has been cloned and sequenced. The availability of this DNA permits the recombinant production of the C140 receptor which can be produced at cell or oocyte surfaces and is useful in assay systems both for the detection of substances which affect its activity, including agonists and antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in these assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof.

公开(公告)号：EP0557442A4

公开(公告)日：1994-10-05

申请号：EP92901061

申请日：1991-11-14

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 ,  C12N15/12

CPC classification number: C07K14/75 ,  A61K38/00 ,  C07K14/46 ,  C07K16/18 ,  Y10S530/856

公开(公告)号：BR0107282A

公开(公告)日：2004-07-06

申请号：BR0107282

申请日：2001-10-01

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SU TING ,  LI WENHAO ,  GOLDMAN ERICK A ,  ZHANG PENGLIE ,  JIA ZHAOZHONG JON ,  SCARBOROUGH ROBERT M

IPC: C07D241/06 ,  A61K31/438 ,  A61K31/495 ,  A61K31/496 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D241/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D491/10 ,  C07D491/113 ,  C07D401/12

公开(公告)号：AU746596B2

公开(公告)日：2002-05-02

申请号：AU5507900

申请日：2000-08-31

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

IPC: C07D413/12 ,  C07D417/12

公开(公告)号：AU746471B2

公开(公告)日：2002-05-02

申请号：AU8826998

申请日：1998-08-11

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  A61K38/04 ,  A61P7/02 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078

公开(公告)号：AU743735B2

公开(公告)日：2002-02-07

申请号：AU4898897

申请日：1997-10-10

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  C07K5/06 ,  A61K38/05

公开(公告)号：NZ502877A

公开(公告)日：2001-11-30

申请号：NZ50287798

申请日：1998-08-11

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M

IPC: A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  A61P9/10 ,  C07K5/062 ,  C07K5/078 ,  C07K5/06 ,  A61K38/05

Abstract: Compounds of formula (I) wherein: R1 and R2 are independently selected from H, C1-6alkyl, C3-8cycloalkyl, C1-3alkylaryl, C1-3alkyl-C3-8cycloalkyl and aryl; R3 is H, C1-6alkyl, or R2 and R3 are taken together to form a carbocyclic ring; q is an integer from 0-2, r and t are an integer from 0-4, s is an integer from 0-1; A is selected from R8, -NR8R9, or a formula from group (a); D is selected from a direct link, C3-8cycloalkyl, C1-6alkenyl, C1-6alkenylaryl, aryl and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from N, 0 and S; E is selected from a direct link, -CO-, -SO2-, -O-CO-, -NR14-SO2- and -NR14-CO-, where R14 is selected from H, -OH, C1-6alkyl, aryl and C1-4alkylaryl; G is selected from a direct link, C3-8cycloalkyl, aryl, and a five to ten membered heterocyclic ring system containing 1-4 heteroatoms selected from N, 0 and S; J is selected from the group consisting of R15, -NR15R16, or a formula from group (b); K', K", K"' and K"" are independently selected from -CH-, -CR4-, -CR5- and -N-; with the proviso that no more than one of K', K", K"' and K"" are -CR4- and no more than one of K', K", K"' and K"" are -CR5-; Q is selected from the group consisting of H, or a formula of group (c); where R21 and R22 are independently selected from H, C1-3alkyl and aryl; and T is selected from the group H, -COOR23, -CONR23R24, -CF3, -CF2CF3 and a group having the formula from group (d); where R23 and R24 are independently selected from H, C1-6alkyl, aryl and C1-4alkylaryl; U' and U" are independently selected from -O-, -S-, -N- and -NH-; with the proviso that at least one of U' or U" is -N- or -NH-; R25 is selected from H, C1-6alkyl, C2-6alkenyl, C0-6alkylaryl, C2-6alkenylaryl, C0-6alkylheterocyclo, C2-6alkenylheterocyclo, -CF3 and -CF2CF3; V is selected from -S-, -SO-, -SO2-, -O- and -NR26-, where R26 is selected from H, C1-6alkyl and benzyl; and W is selected from the formula (e). The compounds may be used in pharmaceutical compositions for preventing or treating a condition characterised by undesired thrombosis, angina, myocardial infarction, transient ischemic attack, thrombotic stroke, disseminated intravascular coagulation.