公开(公告)号：WO0100656A3

公开(公告)日：2001-05-25

申请号：PCT/US0017718

申请日：2000-06-28

Applicant: ORTHO MCNEIL PHARM INC ,  COR THERAPEUTICS INC

Inventor： ZHANG HAN-CHENG ,  MARYANOFF BRUCE E ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  C07K5/065 ,  A61K38/05

CPC classification number: C07K5/06078 ,  A61K31/416 ,  A61K38/00

Abstract: The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

Abstract translation: 本发明涉及新颖的吲唑拟肽化合物，其可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性病症，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂 ，和神经变性疾病。 还公开了包含本发明的取代的吲唑肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

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。

公开(公告)号：WO0047554A3

公开(公告)日：2001-08-09

申请号：PCT/US0003405

申请日：2000-02-11

Applicant: COR THERAPEUTICS INC

Inventor： SONG YONGHONG ,  ZHU BING-YAN ,  SCARBOROUGH ROBERT M ,  CLIZBE LANE ,  JIA ZHAOZHONG JON ,  SU TING ,  TENG WILLY

IPC: C07D295/14 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/216 ,  A61K31/341 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/505 ,  A61K31/517 ,  A61P7/00 ,  A61P7/02 ,  A61P7/04 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P31/04 ,  A61P43/00 ,  C07C257/18 ,  C07C311/29 ,  C07C311/46 ,  C07C311/51 ,  C07D213/56 ,  C07D213/58 ,  C07D213/70 ,  C07D213/74 ,  C07D213/75 ,  C07D217/22 ,  C07D231/12 ,  C07D233/61 ,  C07D239/42 ,  C07D239/94 ,  C07D257/04 ,  C07D295/16 ,  C07D307/54 ,  C07D401/12 ,  C07D521/00 ,  A61K31/16 ,  A61K31/33 ,  C07D231/56

CPC classification number: C07D231/12 ,  C07C311/46 ,  C07C311/51 ,  C07C2601/10 ,  C07D217/22 ,  C07D233/56 ,  C07D239/94 ,  C07D249/08 ,  C07D307/54 ,  C07D401/12

Abstract: Novel compounds of formula in which A is a substituted or unsubstituted phenyl, naphthyl or monocyclic heterocyclic ring, D is a substituted or unsubstituted phenyl or aromatic six-membered heterocyclic ring, K is a substituted or unsubstituted phenyl, naphthyl or bicyclic heterocyclic ring, and the other variables are as defined in the claims, their salts and other derivatives and compositions related thereto having activity against mammalian Factor Xa are disclosed. The coumpounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract translation: 其中A是取代或未取代的苯基，萘基或单环杂环的新型式的化合物，D是取代或未取代的苯基或芳族六元杂环，K是取代或未取代的苯基，萘基或双环杂环，以及 其他变量如权利要求中所定义，公开了其与其相关的盐和其它衍生物和组合物具有抗哺乳动物因子Xa的活性。 固体在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：WO0236587A3

公开(公告)日：2002-08-22

申请号：PCT/US0145400

申请日：2001-11-01

Applicant: COR THERAPEUTICS INC ,  KANTER JAMES ,  PANDEY ANJALI ,  ROBINSON JAMES ,  SCARBOROUGH ROBERT M

Inventor： KANTER JAMES ,  PANDEY ANJALI ,  ROBINSON JAMES ,  SCARBOROUGH ROBERT M

IPC: C07D239/86 ,  A61K31/517 ,  A61K31/5377 ,  A61P9/10 ,  A61P13/12 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07D239/94

CPC classification number: C07D239/94

Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and slats or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

Abstract translation: 本发明提供含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 本发明还提供了可用于该方法的中间体化合物，以及由该方法生产的最终产物及其板条或前药。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。

公开(公告)号：WO0216361A2

公开(公告)日：2002-02-28

申请号：PCT/US0141750

申请日：2001-08-17

Applicant: COR THERAPEUTICS INC ,  KYOWA HAKKO KOGYO KK ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT M ,  MATSUNO KENJI ,  ICHIMURA MICHIO ,  NOMOTO YUGI ,  FUJIWARA SHIGEKI ,  IDE SHINICHI ,  TSUKIDA EIJI ,  IRIE JUNKO ,  ODA SHOJI

Inventor： PANDEY ANJALI ,  SCARBOROUGH ROBERT M ,  MATSUNO KENJI ,  ICHIMURA MICHIO ,  NOMOTO YUGI ,  FUJIWARA SHIGEKI ,  IDE SHINICHI ,  TSUKIDA EIJI ,  IRIE JUNKO ,  ODA SHOJI

IPC: A61P35/00 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D487/00

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

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 inhibitng 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和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。