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：AU5895500A

公开(公告)日：2001-01-31

申请号：AU5895500

申请日：2000-06-28

Applicant: COR THERAPEUTICS INC ,  ORTHO MCNEIL PHARM INC

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

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

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：WO0192250A3

公开(公告)日：2002-04-25

申请号：PCT/US0117667

申请日：2001-06-01

Applicant: KANTER JAMES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  COR THERAPEUTICS INC

Inventor： KANTER JAMES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT

IPC: C07D311/22 ,  C07D311/58

CPC classification number: C07D311/58 ,  C07D311/22

Abstract: Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.

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。

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：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：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：WO0130780A3

公开(公告)日：2001-11-29

申请号：PCT/US0029804

申请日：2000-10-27

Applicant: COR THERAPEUTICS INC ,  SCARBOROUGH ROBERT M ,  MEHROTA MUKUND ,  PANDEY ANJALI ,  SMYTH MARK

Inventor： SCARBOROUGH ROBERT M ,  MEHROTA MUKUND ,  PANDEY ANJALI ,  SMYTH MARK

IPC: A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/551 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D401/04 ,  C07D413/14 ,  C07D471/10 ,  A61K31/438

CPC classification number: C07D401/04 ,  C07D413/14 ,  C07D471/10

Abstract: This invention relates to certain substituted or unsubstituted pyridyl-containing spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

Abstract translation: 本发明涉及用碱性和酸性官能团取代的某些取代或未取代的含吡啶基螺环化合物，其可用于抑制血小板聚集。

公开(公告)号：AU1244001A

公开(公告)日：2001-05-08

申请号：AU1244001

申请日：2000-10-27

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M JR ,  MEHROTA MUKUND ,  PANDEY ANJALI ,  SMYTH MARK

IPC: A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/551 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D401/04 ,  C07D413/14 ,  C07D471/10 ,  A61K31/438 ,  C07D209/00 ,  C07D221/00