公开(公告)号：WO0192249A3

公开(公告)日：2002-04-11

申请号：PCT/US0118016

申请日：2001-06-01

Applicant: COR THERAPEUTICS INC ,  KANTER JAMES ,  MARLOWE CHARLES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  BUTKE GREG ,  JACOBSEN BARRY ,  WALKER DERRICK

Inventor： KANTER JAMES ,  MARLOWE CHARLES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  BUTKE GREG ,  JACOBSEN BARRY ,  WALKER DERRICK

IPC: C07D311/20 ,  C07D311/22 ,  C07D311/58 ,  A61K31/35

CPC classification number: C07D311/58 ,  C07D311/20 ,  C07D311/22

Abstract: Disclosed are processes for producing a (2S) or (2R) 4-oxo-chroman-2-yl acyl compounds and chroman-2-yl acyl compounds, esters or amides thereof as well as derivatives thereof. Such processes may involve chiral synthesis or achiral synthesis, preferably coupled with a resolution procedure. Such compounds, particularly (2S) or (2R) acetic acid esters, are useful intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are processes for making derivatives of such substantially pure, or enhanced compositions of single (2R) or (2S) enantiomer intermediates or processes for producing final products or salts from such desired enantiomers.

Abstract translation: 公开了制备（2S）或（2R）-4-氧代 - 苯并二氢吡喃-2-基酰基化合物和色满-2-基酰基化合物，其酯或酰胺及其衍生物的方法。 这样的方法可以涉及手性合成或非手性合成，优选与解析程序偶联。 这些化合物，特别是（2S）或（2R）乙酸酯是生产血小板聚集抑制剂和/或本身是有效的血小板聚集抑制剂的有用中间体。 进一步公开的是制备单一（2R）或（2S）对映异构体中间体的这种基本上纯的或增强的组合物的衍生物的方法或从所需的对映异构体制备最终产物或盐的方法。

公开(公告)号：WO0216599A2

公开(公告)日：2002-02-28

申请号：PCT/US0126510

申请日：2001-08-27

Applicant: CURAGEN CORP ,  COR THERAPEUTICS INC ,  BURGESS CATHERINE E ,  CONLEY PAMELA B ,  GROSSE WILLIAM M ,  HART MATTHEW ,  KEKUDA RAMESH ,  SHIMKETS RICHARD A ,  SPYTEK KIMBERLY A ,  SZEKERES EDWARD S JR ,  TOMLINSON JAMES E ,  TOPPER JAMES N ,  YANG RUEY BIN

Inventor： BURGESS CATHERINE E ,  CONLEY PAMELA B ,  GROSSE WILLIAM M ,  HART MATTHEW ,  KEKUDA RAMESH ,  SHIMKETS RICHARD A ,  SPYTEK KIMBERLY A ,  SZEKERES EDWARD S JR ,  TOMLINSON JAMES E ,  TOPPER JAMES N ,  YANG RUEY-BIN

IPC: A61K38/00 ,  C07K14/47 ,  C12N15/00

CPC classification number: C07K14/47 ,  A61K38/00

Abstract: Disclosed herein are nucleic acid sequences that encode novel polypeptides. Also disclosed are polypeptides encoded by these nucleic acid sequences, and antibodies, which immunospecifically-bind to the polypeptide, as well as derivatives, variants, mutants, or fragments of the aforementioned polypeptide, polynucleotide, or antibody. The invention further discloses tehrapeutic, diagnostic and research methods for diagnosis, treatment, and prevention of disorders involving any one of these novel human nucleic acids and proteins.

Abstract translation: 本文公开了编码新型多肽的核酸序列。 还公开了由这些核酸序列编码的多肽，以及免疫特异性结合多肽的抗体以及前述多肽，多核苷酸或抗体的衍生物，变体，突变体或片段。 本发明还公开了用于诊断，治疗和预防与这些新型人核酸和蛋白质中的任何一种相关的病症的治疗，诊断和研究方法。

公开(公告)号：WO0071493A3

公开(公告)日：2002-01-17

申请号：PCT/US0014138

申请日：2000-05-24

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SU TING ,  ZHAOZHANG JON JIA ,  SCARBOROUGH ROBERT M ,  SONG YONGHONG

IPC: A61P7/02 ,  A61K31/167 ,  A61K31/18 ,  A61K31/275 ,  A61K31/277 ,  A61K31/40 ,  A61K31/472 ,  A61K31/4725 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  C07C311/16 ,  C07C311/18 ,  C07C311/40 ,  C07C311/44 ,  C07C311/46 ,  C07D207/16 ,  C07D217/22 ,  C07D401/06

CPC classification number: C07C311/40 ,  C07C311/16 ,  C07C311/18 ,  C07C311/44 ,  C07C311/46

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。

公开(公告)号：WO0142198A3

公开(公告)日：2001-12-13

申请号：PCT/US0042819

申请日：2000-12-13

Applicant: COR THERAPEUTICS INC

Inventor： KANTER JAMES ,  MULLINS JOHN JASON GENTRY ,  SCARBOROUGH ROBERT

IPC: C07C253/30 ,  C07C51/265 ,  C07C201/12 ,  C07C209/36 ,  C07C253/00 ,  C07C255/57 ,  C07C257/18 ,  C07C253/08

CPC classification number: C07C253/00 ,  C07C255/57

Abstract: Novel process steps and novel processes for producing unsubstituted and substituted meta- and para- cyano benzoic acid compounds, as well as salts and derivatives thereof, and intermediates therefor which are useful as intermediates for producing platelet aggregation inhibitors. Further disclosed are processes for producing bicyclic and heterocyclic cyano substituted compounds also having a carboxyl group attached to the same ring structure.

Abstract translation: 用于制备未取代和取代的间位和对 - 氰基苯甲酸化合物的新方法步骤和新方法，以及其盐及其衍生物及其中间体，其可用作制备血小板聚集抑制剂的中间体。 进一步公开的是还具有连接到相同环结构的羧基的双环和杂环氰基取代的化合物的方法。

公开(公告)号：WO0119788A3

公开(公告)日：2001-08-09

申请号：PCT/US0025196

申请日：2000-09-15

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  ZHANG PENGLIE ,  WANG LINGYAN ,  HUANG WENRONG ,  GOLDMAN ERIC ,  LI WENHAO ,  ZUCKETT JINGMEI ,  SONG YONGHONG ,  SCARBOROUGH ROBERT

IPC: A61K31/18 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/5513 ,  A61P7/02 ,  A61P9/10 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  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 ,  C07D521/00 ,  A61K31/33

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 the formula A - Q - D - E - G - J - X in which D is a direct link, a substituted or unsubstituted phenyl or naphthyl group or a heterocyclic ring system; X is a substituted or unsubstituted phenyl or naphthyl group or a heterocyclic 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: 式A-Q-D-E-G-J-X的化合物，其中D是直链，取代或未取代的苯基或萘基或杂环系; X是取代或未取代的苯基或萘基或杂环体系; 并且其它变量如权利要求中所定义，其公开了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：WO0071511A3

公开(公告)日：2001-08-09

申请号：PCT/US0014205

申请日：2000-05-24

Applicant: COR THERAPEUTICS INC

Inventor： SU TING ,  ZHU BING-YAN ,  KANE-MAGUIRE KIM ,  SCARBOROUGH ROBERT M ,  ZHANG PENGLIE

IPC: C07D213/74 ,  A61K31/18 ,  A61K31/198 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4427 ,  A61K31/4453 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07C311/16 ,  C07C311/21 ,  C07C311/46 ,  C07D205/04 ,  C07D207/16 ,  C07D207/20 ,  C07D207/325 ,  C07D213/40 ,  C07D213/64 ,  C07D213/72 ,  C07D213/75 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/68 ,  C07D295/18 ,  C07D295/192 ,  C07D295/22 ,  C07D295/26 ,  C07D307/38 ,  C07D307/52 ,  C07D401/12 ,  A61K31/277 ,  A61K31/501

CPC classification number: C07D213/40 ,  C07C311/16 ,  C07C311/46 ,  C07D217/22 ,  C07D295/192 ,  C07D295/26 ,  C07D307/52 ,  C07D401/12

Abstract: Compounds of the formula A - Y - D - E - G - J - Z - L in which D is a direct link, a substituted or unsubstituted phenyl or naphtyl group or a heterocyclic ring system; Z is a substituted or unsubstituted phenyl or naphthyl 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: 式A-Y-D-E-G-J-Z-L的化合物，其中D是直链，取代或未取代的苯基或萘基或杂环系; Z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，公开了其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：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：WO0071516B1

公开(公告)日：2001-03-01

申请号：PCT/US0014209

申请日：2000-05-24

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M ,  WANG LINGYAN

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 claim 5, formula (I) and formula (II), where A-B is (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 如权利要求5，式（I）和式（II）所述，其中A-B是（1），公开了它们的盐和与其有关的组合物，其具有抗哺乳动物因子Xa的活性。 这些化合物可用于体外或体内用于预防或治疗凝血病症。

公开(公告)号：WO0071516A2

公开(公告)日：2000-11-30

申请号：PCT/US0014209

申请日：2000-05-24

Applicant: COR THERAPEUTICS INC

Inventor： ZHU BING-YAN ,  SCARBOROUGH ROBERT M ,  WANG LINGYAN

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 ,  C07D207/00

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 claim 5, formula (I) and formula (II), where A-B is (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 在其中A-B为（1）的权利要求5所述的式（I）和式（II）中，其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：WO0008137A3

公开(公告)日：2000-03-23

申请号：PCT/US9917594

申请日：1999-08-04

Applicant: COR THERAPEUTICS INC ,  RAMAKRISHNAN VANITHA ,  PHILLIPS DAVID R

Inventor： RAMAKRISHNAN VANITHA ,  PHILLIPS DAVID R

IPC: A01K67/027 ,  C07K14/705 ,  C12N5/10 ,  C12N15/09 ,  C12N15/85 ,  C12Q1/02 ,  C12N15/00 ,  A61K49/00 ,  C12N15/12

CPC classification number: C12N15/8509 ,  A01K67/0276 ,  A01K2217/05 ,  A01K2217/075 ,  A01K2227/105 ,  A01K2267/03 ,  A01K2267/0381 ,  C07K14/705

Abstract: The present invention relates to nonhuman transgenic animals in which the GP V gene has been modified. The invention is also useful for identifying agents that modulate the biological functions of GP V, including the screening and identification of potential therapeutic agents.

Abstract translation: 本发明涉及其中GPV基因已被修饰的非人类转基因动物。 本发明还可用于鉴定调节GPV的生物学功能的试剂，包括筛选和鉴定潜在的治疗剂。