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11. 发明申请

WO1998016523A3 SELECTIVE FACTOR XA INHIBITORS 审中-公开
公开(公告)号：WO1998016523A3
公开(公告)日：1998-04-23
申请号：PCT/US1997018291
申请日：1997-10-10
申请人： COR THERAPEUTICS, INC.
发明人： COR THERAPEUTICS, INC. , ZHU, Bing-Yan , SCARBOROUGH, Robert, M.
IPC分类号： C07K05/06

12. 发明申请

WO1996040744A1 KETOHETEROCYCLIC INHIBITORS OF FACTOR Xa 审中-公开
标题翻译：因子XA的酮类化合物抑制剂
公开(公告)号：WO1996040744A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009290
申请日：1996-06-05
申请人： COR THERAPEUTICS, INC. , MARLOWE, Charles, K. , SCARBOROUGH, Robert, M. , LAIBELMAN, Alan, M. , SINHA, Uma , ZHU, Bing-Yan
发明人： COR THERAPEUTICS, INC.
IPC分类号： C07K05/06
CPC分类号： C07K5/06 , A61K38/00 , C07K5/06078 , C07K5/06095 , C07K5/06139
摘要： 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.
摘要翻译：公开了与哺乳动物因子Xa有关的新型化合物，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。

13. 发明申请

WO1996014843A2 PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：用作蛋白激酶抑制剂的药用吡唑组合物
公开(公告)号：WO1996014843A2
公开(公告)日：1996-05-23
申请号：PCT/US1995014723
申请日：1995-11-09
申请人： COR THERAPEUTICS, INC.
发明人： COR THERAPEUTICS, INC. , GIESE, Neill, A. , LOKKER, Nathalie , LAIBELMAN, Alan, M. , SCARBOROUGH, Robert, M.
IPC分类号： A61K31/415
CPC分类号： A61K31/455 , A61K31/415 , A61K31/4155 , A61K31/4439
摘要： 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.
摘要翻译：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。

14. 发明申请

WO1996013274A1 PROCESS FOR PRODUCTION OF INHIBITED FORMS OF ACTIVATED BLOOD FACTORS 审中-公开
标题翻译：生产激活血液因子抑制形式的方法
公开(公告)号：WO1996013274A1
公开(公告)日：1996-05-09
申请号：PCT/US1995013940
申请日：1995-10-27
申请人： COR THERAPEUTICS, INC.
发明人： COR THERAPEUTICS, INC. , KING, Robert, S.
IPC分类号： A61K38/36
CPC分类号： C12N9/6432 , C07K14/75 , C12Y304/21006 , Y10S530/829
摘要： A process, as shown in the figure, for producing a highly purified preparation of an inhibited form of an activated blood factor entails providing a partially purified preparation containing the blood factor of interest, treating the partially purified preparation to convert the blood factor to an inhibited activated form in a single step, and then purifiying the resulting inhibited activated blood factor.
摘要翻译：如图所示，用于生产抑制形式的活化血液因子的高度纯化的制剂的方法需要提供含有目标血液因子的部分纯化的制剂，处理部分纯化的制剂以将血液因子转化为抑制活化形式，然后净化所得的抑制的活化血液因子。

15. 发明申请

WO1996013259A3 METHOD AND COMPOSITIONS FOR INHIBITING PROTEIN KINASES 审中-公开
公开(公告)号：WO1996013259A3
公开(公告)日：1996-05-09
申请号：PCT/US1995013882
申请日：1995-10-26
申请人： COR THERAPEUTICS, INC.
发明人： COR THERAPEUTICS, INC. , GIESE, Neill, A. , LOKKER, Nathalie
IPC分类号： A61K31/365

16. 发明申请

WO1995004136A1 RECEPTOR FUNCTION ASSAYS 审中-公开
标题翻译：受体功能测定
公开(公告)号：WO1995004136A1
公开(公告)日：1995-02-09
申请号：PCT/US1994008571
申请日：1994-07-29
申请人： COR THERAPEUTICS, INC. , GIESE, Neill, A.
发明人： COR THERAPEUTICS, INC.
IPC分类号： C12N09/12
CPC分类号： G01N33/5008 , G01N2333/9121
摘要： Methods are provided for assaying the function (e.g., activation) of signal-transducing receptors on cells. The methods are useful for identifying compounds that are agonists or antagonists of receptor function. The assays utilize a two-antibody sandwich assay employing an immobilized first antibody that specifically binds and captures the receptor of interest along with any tightly associated proteins or polypeptides and a second antibody directed against (i) an epitope of the receptor that is characteristic of the activated but not the unactivated state, (ii) an epitope of a protein or molecule characteristically bound to activated receptor but not to unactivated receptor, or (iii) an epitope of the receptor that is characteristic of the unactivated but not the activated state. In one embodiment, the level of binding of the second antibody is determined and correlated with the presence of activated receptor, and thus with activation in response to the treatment received by the cells. The methods provided by the invention will find particular use for detecting activation of tyrosine kinase growth factor receptors.
摘要翻译：提供了用于测定细胞上信号转导受体的功能（例如激活）的方法。该方法可用于鉴定作为受体功能的激动剂或拮抗剂的化合物。该测定法利用采用固定化的第一抗体的双抗体夹心测定法，其特异性结合并捕获感兴趣的受体以及任何紧密相关的蛋白质或多肽，以及针对（i）受体表位的第二抗体，其特征在于活化但不是未活化状态，（ii）特征性结合活化受体但不结合未活化受体的蛋白质或分子的表位，或（iii）受体的表位，其是未活化但不是活化状态的特征。在一个实施方案中，确定第二抗体的结合水平并与活化受体的存在相关，并因此响应于由细胞接受的治疗而激活。本发明提供的方法将特别用于检测酪氨酸激酶生长因子受体的活化。

17. 发明申请

WO1992014750A1 RECOMBINANT THROMBIN RECEPTOR AND RELATED PHARMACEUTICALS 审中-公开
标题翻译：重组血红蛋白受体和相关药物
公开(公告)号：WO1992014750A1
公开(公告)日：1992-09-03
申请号：PCT/US1992001312
申请日：1992-02-19
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , COR THERAPEUTICS, INC.
发明人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , COR THERAPEUTICS, INC. , COUGHLIN, Shaun, R. , SCARBOROUGH, Robert, M.
IPC分类号： C07K07/00
CPC分类号： C12N9/6429 , A61K38/00 , A61K39/00 , C07K14/705 , C07K16/28 , C12Y304/21005 , Y10S530/837
摘要： The DNA encoding the cell surface receptor for thrombin has been cloned and sequenced. The availability of this DNA permits the recombinant production of thrombin receptor which can be produced at cell surfaces and is useful in assay systems both for the detection of thrombin and for the evaluation of candidate thrombin agonists and antagonists. Further, the elucidation of the structure of the thrombin receptor permits the design of agonist and antagonist compounds which are useful diagnostically and therapeutically. The availability of the thrombin receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof which are also useful diagnostically or therapeutically.
摘要翻译：编码凝血酶细胞表面受体的DNA已被克隆并测序。该DNA的可用性允许重组产生可在细胞表面产生的凝血酶受体，并且可用于检测凝血酶和用于评价候选凝血酶激动剂和拮抗剂的测定系统。此外，阐明凝血酶受体的结构允许设计在诊断和治疗上有用的激动剂和拮抗剂化合物。凝血酶受体的可用性还允许产生与受体本身或其特异性区域特异性免疫反应的抗体，其在诊断或治疗上也是有用的。

18. 发明申请

WO0194335A8 METHODS FOR PRODUCING CHIRAL CHROMONES, CHROMANES, AMINO SUBSTITUTED CHROMANES AND INTERMEDIATES THEREFOR 审中-公开
标题翻译：方法生产CHIRAL CHROMONES，CHROMANES，AMINO取代的CHROMANES及其中间体
公开(公告)号：WO0194335A8
公开(公告)日：2003-11-06
申请号：PCT/US0117980
申请日：2001-06-01
申请人： LILLY CO ELI , COR THERAPEUTICS INC , BRIGGS BARBARA , HANSEN MARVIN , KANTER JAMES , MULLINS JOHN J G , RUHTER GERD , UDODONG UKO , VERRAL DANIEL II , ZMIJEWSKI MILTON JR
发明人： BRIGGS BARBARA , HANSEN MARVIN , KANTER JAMES , MULLINS JOHN J G , RUHTER GERD , UDODONG UKO , VERRAL DANIEL II , ZMIJEWSKI MILTON JR
IPC分类号： A61K31/353 , A61P7/02 , C07D311/22 , C07D311/24 , C07D311/58 , C07D311/74 , C07D311/70
CPC分类号： C07D311/74 , A61K31/353 , C07D311/22 , C07D311/24 , C07D311/58
摘要： Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.
摘要翻译：公开了生产富集至少一种（2R或2S）对映异构体，优选苯并二氢吡喃-2-基羧酸化合物和色满-2-基羧酸酯的色淀组合物的方法步骤和新方法，其是制备血小板聚集抑制剂的中间体， /或本身是有效的血小板聚集抑制剂。进一步公开的是用于拆分手性中间体或最终产物以提供所需对映异构体的酶法。

19. 发明申请

WO0194330A8 METHODS FOR PRODUCING AMINO SUBSTITUTED CHROMANES 审中-公开
标题翻译：生产氨基取代的颜料的方法
公开(公告)号：WO0194330A8
公开(公告)日：2003-11-06
申请号：PCT/US0117688
申请日：2001-06-01
申请人： COR THERAPEUTICS INC , KANTER JAMES , MULLINS JOHN J G , SCARBOROUGH ROBERT , WALKER DERRICK , HENSE THOMAS
发明人： KANTER JAMES , MULLINS JOHN J G , SCARBOROUGH ROBERT , WALKER DERRICK , HENSE THOMAS
IPC分类号： A61P7/00 , C07D311/20 , C07D311/22 , C07D311/58 , C07D311/70 , A61K31/35
CPC分类号： C07D311/22 , C07D311/20 , C07D311/58
摘要： Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.
摘要翻译：本发明公开了生产色氨酸化合物，优选苯并二氢吡喃-2-基乙酸化合物和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。

20. 发明申请

WO0112600A9 INHIBITORS OF FACTOR Xa 审中-公开
标题翻译：因子的抑制剂Xa
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
申请人： 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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

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