公开(公告)号：WO2008005956A2

公开(公告)日：2008-01-10

申请号：PCT/US2007/072697

申请日：2007-07-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  MASTALERZ, Harold ,  WITTMAN, Mark D. ,  ZIMMERMANN, Kurt ,  SAULNIER, Mark G. ,  VELAPARTHI, Upender ,  VYAS, Dolatrai M. ,  ZHANG, Guifen ,  JOHNSON, Walter Lewis ,  FRENNESSON, David B. ,  SANG, Xiaopeng ,  LIU, Peiying ,  LANGLEY, David R.

Inventor： MASTALERZ, Harold ,  WITTMAN, Mark D. ,  ZIMMERMANN, Kurt ,  SAULNIER, Mark G. ,  VELAPARTHI, Upender ,  VYAS, Dolatrai M. ,  ZHANG, Guifen ,  JOHNSON, Walter Lewis ,  FRENNESSON, David B. ,  SANG, Xiaopeng ,  LIU, Peiying ,  LANGLEY, David R.

IPC: C07D487/04 ,  A61K31/53 ,  A61P35/00 ,  A61P25/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

Abstract translation: 本发明提供式I化合物[其中的化学结构]（I）及其药学上可接受的盐。 式I化合物抑制酪氨酸激酶活性，从而使它们用作抗癌剂和治疗阿尔茨海默氏病。

公开(公告)号：WO2012009510A1

公开(公告)日：2012-01-19

申请号：PCT/US2011/043962

申请日：2011-07-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  VELAPARTHI, Upender ,  FRENNESSON, David B. ,  SAULNIER, Mark G. ,  AUSTIN, Joel F. ,  HUANG, Audris ,  BALOG, James Aaron ,  VYAS, Dolatrai M.

Inventor： VELAPARTHI, Upender ,  FRENNESSON, David B. ,  SAULNIER, Mark G. ,  AUSTIN, Joel F. ,  HUANG, Audris ,  BALOG, James Aaron ,  VYAS, Dolatrai M.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR 4 or N; and R 1 , R 2 , R 3 , and R 4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract translation: 公开了式（I）的氮杂咔唑化合物或其药学上可接受的盐，其中W是CR 4或N; 并且R 1，R 2，R 3和R 4在本文中定义。 还公开了使用这些化合物治疗至少一种CYP17相关病症例如癌症的方法，以及包含这些化合物的药物组合物。

公开(公告)号：WO2007005708A1

公开(公告)日：2007-01-11

申请号：PCT/US2006/025768

申请日：2006-06-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  MASTALERZ, Harold ,  TRAINOR, George, L. ,  VYAS, Dolatrai, M. ,  GAVAI, Ashvinikumar, V.

Inventor： MASTALERZ, Harold ,  TRAINOR, George, L. ,  VYAS, Dolatrai, M. ,  GAVAI, Ashvinikumar, V.

IPC: C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.

Abstract translation: 本发明涉及至少一种吡咯并三嗪衍生物，至少一种包含至少一种吡咯并三嗪衍生物的药物组合物和至少一种使用至少一种吡咯并三嗪衍生物以治疗至少一种激酶相关病症的方法。

公开(公告)号：WO2012051405A1

公开(公告)日：2012-04-19

申请号：PCT/US2011/056124

申请日：2011-10-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  SAULNIER, Mark G. ,  VYAS, Dolatrai M. ,  LANGLEY, David R. ,  FRENNESSON, David B.

Inventor： SAULNIER, Mark G. ,  VYAS, Dolatrai M. ,  LANGLEY, David R. ,  FRENNESSON, David B.

IPC: C07K1/113 ,  C07K1/107 ,  C07D277/42

CPC classification number: C07K7/64 ,  C07D277/42 ,  C07D417/04 ,  C07K1/1136 ,  C07K5/123 ,  C07K5/126

Abstract: The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.

Abstract translation: 本发明提供了制备大环化合物包括大环稳定肽（MSP）的方法。 根据由适当取代的2-氨基 - 噻唑-5-基甲醇产生的亚氨基喹喔啉型中间体的亲核捕获制备大环和MSP。 在大环化合物的情况下，优选的亲核试剂可以选自富含电子的芳族部分，在MSP的情况下，至少一个氨基酸包含富电子的芳族部分。 此外，该概念可以扩展到其它相关的5元杂环体系代替噻唑，例如咪唑或恶唑。 产生相应的亚氨基喹喔啉型中间体的条件可以与用于2-氨基 - 噻唑-5-基甲醇的条件相似或不同。

公开(公告)号：WO2009111531A1

公开(公告)日：2009-09-11

申请号：PCT/US2009/035975

申请日：2009-03-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  VELAPARTHI, Upender ,  VYAS, Dolatrai M.

Inventor： VELAPARTHI, Upender ,  VYAS, Dolatrai M.

IPC: C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式I化合物抑制蛋白激酶活性，从而使其成为抗癌剂。

公开(公告)号：WO2008005956A3

公开(公告)日：2008-03-06

申请号：PCT/US2007072697

申请日：2007-07-03

Applicant: SQUIBB BRISTOL MYERS CO ,  MASTALERZ HAROLD ,  WITTMAN MARK D ,  ZIMMERMANN KURT ,  SAULNIER MARK G ,  VELAPARTHI UPENDER ,  VYAS DOLATRAI M ,  ZHANG GUIFEN ,  JOHNSON WALTER LEWIS ,  FRENNESSON DAVID B ,  SANG XIAOPENG ,  LIU PEIYING ,  LANGLEY DAVID R

Inventor： MASTALERZ HAROLD ,  WITTMAN MARK D ,  ZIMMERMANN KURT ,  SAULNIER MARK G ,  VELAPARTHI UPENDER ,  VYAS DOLATRAI M ,  ZHANG GUIFEN ,  JOHNSON WALTER LEWIS ,  FRENNESSON DAVID B ,  SANG XIAOPENG ,  LIU PEIYING ,  LANGLEY DAVID R

IPC: C07D487/04 ,  A61K31/53 ,  A61P25/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention provides compounds of formula I [INSERT CHEMICAL STRUCTURE HERE] (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.

Abstract translation: 本发明提供了式I化合物[插入其中的化学结构]（I）及其药学上可接受的盐。 式I化合物抑制酪氨酸激酶活性，从而使它们可用作抗癌剂并用于治疗阿尔茨海默氏病。

公开(公告)号：WO2006007468A1

公开(公告)日：2006-01-19

申请号：PCT/US2005/022059

申请日：2005-06-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  GAVAI, Ashvinikumar, V. ,  MASTALERZ, Harold ,  DARIS, Jean-Paul ,  DEXTRAZE, Pierre ,  LAPOINTE, Philippe ,  RUEDIGER, Edward, H. ,  VYAS, Dolatrai, M. ,  ZHANG, Guifen

Inventor： GAVAI, Ashvinikumar, V. ,  MASTALERZ, Harold ,  DARIS, Jean-Paul ,  DEXTRAZE, Pierre ,  LAPOINTE, Philippe ,  RUEDIGER, Edward, H. ,  VYAS, Dolatrai, M. ,  ZHANG, Guifen

IPC: C07D253/10

CPC classification number: C07D487/04

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 本发明的化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使它们用作抗增殖剂。 所述化合物还可用于治疗与通过生长因子受体作用的信号转导途径相关的其它疾病。