公开(公告)号：EP2271642B1

公开(公告)日：2014-03-05

申请号：EP09731060.1

申请日：2009-04-10

申请人： Genentech, Inc. ,  Curis, Inc.

发明人： GUNZNER, Janet, L. ,  SUTHERLIN, Daniel, P. ,  STANLEY, Mark, S. ,  BAO, Liang ,  CASTANEDO, Georgette ,  LALONDE, Rebecca, L. ,  WANG, Shumei ,  REYNOLDS, Mark, E. ,  SAVAGE, Scott, J. ,  MALESKY, Kimberly ,  DINA, Michael, S.

IPC分类号： C07D403/14 ,  C07D403/06 ,  C07D213/06 ,  A61K31/4418 ,  A61K31/4436 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4439

CPC分类号： C07D213/16 ,  C07D213/06 ,  C07D213/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07F9/582

公开(公告)号：EP2411398A1

公开(公告)日：2012-02-01

申请号：EP09842417.9

申请日：2009-03-24

申请人： Sumitomo Chemical Company, Limited ,  Genentech, Inc.

发明人： MIKI, Takashi ,  SHIMASAKI, Yasuharu ,  BABU, Srinivasan ,  CHENG, Zhigang ,  REYNOLDS, Mark, E. ,  TIAN, Qingping

IPC分类号： C07F5/04

CPC分类号： C07F5/025

摘要： The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by reacting an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel catalyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

公开(公告)号：EP1330430A2

公开(公告)日：2003-07-30

申请号：EP01965996.0

申请日：2001-08-16

申请人： GENENTECH, INC.

发明人： ARTIS, Dean, R. ,  JACKSON, David, Y. ,  RAWSON, Thomas, E. ,  REYNOLDS, Mark, E. ,  SUTHERLIN, Daniel, P. ,  STANLEY, Mark, S.

IPC分类号： C07C237/22 ,  C07C237/20 ,  C07C233/81 ,  C07C233/75 ,  C07C237/04 ,  A61K31/40 ,  A61K31/216 ,  A61K31/196 ,  C07D207/16 ,  C07D207/48 ,  A61P19/02

CPC分类号： C07D403/12 ,  C07C233/25 ,  C07C233/60 ,  C07C233/81 ,  C07C237/04 ,  C07C237/20 ,  C07C237/22 ,  C07C2601/08 ,  C07C2603/18 ,  C07C2603/32 ,  C07D207/16 ,  C07D207/48 ,  C07D209/88 ,  C07D405/12

摘要： Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with α4 integrins or their ligands.

摘要翻译： 提供式（I）的化合物，其中A，Q，W，X，Y，Z，R 1至R 4，m和n如本文所定义。 本发明的化合物结合α4H整联蛋白受体，从而抑制α4A整联蛋白的配体结合，其可用于预防和/或治疗与 α4整联蛋白或其配体。

公开(公告)号：EP2411398B1

公开(公告)日：2014-12-17

申请号：EP09842417.9

申请日：2009-03-24

申请人： Sumitomo Chemical Company, Limited ,  Genentech, Inc.

发明人： MIKI, Takashi ,  SHIMASAKI, Yasuharu ,  BABU, Srinivasan ,  CHENG, Zhigang ,  REYNOLDS, Mark, E. ,  TIAN, Qingping

IPC分类号： C07F5/04

CPC分类号： C07F5/025

公开(公告)号：EP2271642A2

公开(公告)日：2011-01-12

申请号：EP09731060.1

申请日：2009-04-10

申请人： Genentech, Inc. ,  Curis, Inc.

发明人： GUNZNER, Janet, L. ,  SUTHERLIN, Daniel, P. ,  STANLEY, Mark, S. ,  BAO, Liang ,  CASTANEDO, Georgette ,  LALONDE, Rebecca, L. ,  WANG, Shumei ,  REYNOLDS, Mark, E. ,  SAVAGE, Scott, J. ,  MALESKY, Kimberly ,  DINA, Michael, S.

IPC分类号： C07D403/14 ,  C07D403/06 ,  C07D213/06

CPC分类号： C07D213/16 ,  C07D213/06 ,  C07D213/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07F9/582

摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as s therapeutic agent for treating malignancies where the compounds have the general formula (I): where A, X, Y R
1, R
2, R
3, R
4, m and n are as described herein.

摘要翻译： 本发明提供了用作治疗恶性肿瘤的治疗剂的hedgehog信号传导的新型抑制剂，其中化合物具有通式（I）：其中A，X，YR 1，R 2，R 3，R 4，m和n是 如本文所述。

公开(公告)号：EP1347968A1

公开(公告)日：2003-10-01

申请号：EP01997016.9

申请日：2001-11-26

申请人： GENENTECH, INC.

发明人： BURDICK, Daniel, J. ,  GADEK, Thomas, R. ,  MARSTERS James, C., Jr. ,  OARE, David ,  REYNOLDS, Mark, E. ,  STANLEY, Mark, S.

IPC分类号： C07D405/12 ,  C07D417/12 ,  C07D207/16 ,  A61P37/06 ,  A61K31/34 ,  A61K31/425 ,  A61K31/40

CPC分类号： C07D405/12 ,  A61K31/198 ,  A61K31/40 ,  A61K31/44 ,  C07D207/16 ,  C07D277/06 ,  C07D307/54 ,  C07D417/12

摘要： The invention relates to novel compounds having formula (I), wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation