公开(公告)号：EP1351941B1

公开(公告)日：2004-09-29

申请号：EP02717403.6

申请日：2002-01-18

申请人： PHARMACOPEIA, INC.

发明人： GUO, Tao ,  HO, Koc-Kan ,  MCDONALD, Edward ,  DOLLE, Roland, Ellwood ,  SAIONZ, Kurt, W. ,  KULTGEN, Steven, G. ,  LIU, Ruiyan ,  DONG, Guizhen ,  GENG, Peng ,  ADANG, Anton, Egbert, Peter ,  VAN STRATEN, Nicole, Corine, Renee

IPC分类号： C07D241/08 ,  A61K31/495 ,  C07D233/78 ,  C07C271/20 ,  C07C237/22 ,  C07C275/14 ,  C07D233/12 ,  C07D207/26 ,  C07D243/08 ,  A61K31/45 ,  A61K31/55 ,  A61K31/551 ,  A61K31/4166 ,  A61P15/08

CPC分类号： C07D207/273 ,  A61K38/00 ,  C07C237/22 ,  C07C271/22 ,  C07C275/14 ,  C07C2601/02 ,  C07D223/10 ,  C07D233/76 ,  C07D241/08 ,  C07D243/08 ,  C07K5/06078 ,  C07K5/06191

摘要： The invention relates to a bisaryl derivative of the formula I, wherein (R, R) is selected from (H, H), O, (H, CH3), (H, OH) and (H, CN); Ar is substituted phenyl; and A is a group of following formula II, III, IV or V: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.

公开(公告)号：EP1189612A1

公开(公告)日：2002-03-27

申请号：EP00945035.4

申请日：2000-06-30

申请人： Daiichi Pharmaceutical Co., Ltd. ,  PHARMACOPEIA, INC.

发明人： BALDWIN, John, J. ,  MCDONALD, Edward ,  MORIARTY, Kevin, Joseph ,  SARKO, Christopher, Ronald ,  MACHINAGA, Nobuo ,  NAKAYAMA, Atsushi ,  CHIBA, Jun ,  IIMURA, Shin ,  YONEDA, Yoshiyuki

IPC分类号： A61K31/40 ,  A61K31/4025 ,  C07D207/12 ,  C07D207/14 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D207/08 ,  C07C275/42 ,  C07C2601/02 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/22 ,  C07D207/24 ,  C07D209/12 ,  C07D211/26 ,  C07D211/34 ,  C07D211/38 ,  C07D213/55 ,  C07D217/02 ,  C07D277/04 ,  C07D277/28 ,  C07D277/48 ,  C07D295/13 ,  C07D295/185 ,  C07D307/33 ,  C07D311/20 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/06 ,  C07D491/04

摘要： Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by formula (I). As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.

摘要翻译： 公开了选择性抑制配体与α4β1整联蛋白（VLA-4）结合的化合物及其制备方法。 在一个实施方案中，本发明的化合物由式（I）表示。 作为VLA-4介导的细胞粘附的选择性抑制剂，本发明的化合物可用于治疗与这种粘附相关的病症，包括但不限于炎性和自身免疫应答，糖尿病，哮喘，牛皮癣，炎症性疾病 肠病，移植排斥反应和肿瘤转移。 还公开了抑制VLA-4介导的细胞粘附的方法和治疗与LA-4介导的细胞粘附相关的病症的方法。

公开(公告)号：EP1409463A1

公开(公告)日：2004-04-21

申请号：EP02739978.1

申请日：2002-06-25

申请人： Bristol-Myers Squibb Company ,  PHARMACOPEIA, INC.

发明人： MORIARTY, Kevin, J. ,  SHIMSHOCK, Yvonne ,  AHMED, Gulzar ,  WU, Junjun ,  WEN, James ,  LI, Wei ,  ERICKSON, Shawn, D. ,  LETOURNEAU, Jeffrey, J. ,  MCDONALD, Edward ,  LEFTHERIS, Katerina ,  WROBLESKI, Stephen, T. ,  HUSSAIN, Zahid ,  HENDERSON, Ian ,  METZGER, Axel ,  BALDWIN, John, J. ,  DYCKMAN, Alaric

IPC分类号： C07D239/32 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D251/46 ,  C07D251/52 ,  C07D251/54 ,  A61K31/166 ,  A61P29/00 ,  A61P37/08 ,  A61P7/02

摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I). Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-a expression utilizing compounds of the present invention are also disclosed.

摘要翻译： 公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。 在一个实施方案中，本发明的化合物由式（I）表示。 也公开了使用本发明化合物治疗与不适当的p38激酶活性或TNF-α表达有关的病症的方法，药物组合物和方法。

公开(公告)号：EP1409463B1

公开(公告)日：2010-02-24

申请号：EP02739978.1

申请日：2002-06-25

申请人： Bristol-Myers Squibb Company ,  PHARMACOPEIA, INC.

发明人： MORIARTY, Kevin, J. ,  SHIMSHOCK, Yvonne ,  AHMED, Gulzar ,  WU, Junjun ,  WEN, James ,  LI, Wei ,  ERICKSON, Shawn, D. ,  LETOURNEAU, Jeffrey, J. ,  MCDONALD, Edward ,  LEFTHERIS, Katerina ,  WROBLESKI, Stephen, T. ,  HUSSAIN, Zahid ,  HENDERSON, Ian ,  METZGER, Axel ,  BALDWIN, John, J. ,  DYCKMAN, Alaric

IPC分类号： C07D239/32 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D251/46 ,  C07D251/52 ,  C07D251/54 ,  A61K31/166 ,  A61P29/00 ,  A61P37/08 ,  A61P7/02

公开(公告)号：EP1242385B1

公开(公告)日：2009-11-25

申请号：EP00988358.8

申请日：2000-12-22

申请人： PHARMACOPEIA, INC. ,  Bristol-Myers Squibb Company

发明人： MORIARTY, Kevin, Joseph ,  SHIMSHOCK, Yvonne ,  AHMED, Gulzar ,  WU, Junjun ,  WEN, James ,  LI, Wei ,  ERICKSON, Shawn, David ,  LETOURNEAU, Jeffrey, John ,  MCDONALD, Edward ,  LEFTHERIS, Katerina ,  WROBLESKI, Stephen, T. ,  HUSSAIN, Zahid

IPC分类号： C07D237/04 ,  A61K31/505 ,  A61P29/00 ,  C07D401/12 ,  A61K31/53 ,  C07D403/04 ,  A61K31/55 ,  C07D403/12

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D251/52 ,  C07D251/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I. Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

公开(公告)号：EP1242385A1

公开(公告)日：2002-09-25

申请号：EP00988358.8

申请日：2000-12-22

申请人： PHARMACOPEIA, INC. ,  Bristol-Myers Squibb Co.

发明人： MORIARTY, Kevin, Joseph ,  SHIMSHOCK, Yvonne ,  AHMED, Gulzar ,  WU, Junjun ,  WEN, James ,  LI, Wei ,  ERICKSON, Shawn, David ,  LETOURNEAU, Jeffrey, John ,  MCDONALD, Edward ,  LEFTHERIS, Katerina ,  WROBLESKI, Stephen, T. ,  HUSSAIN, Zahid

IPC分类号： C07D237/04 ,  A61K31/505 ,  A61P29/00 ,  C07D401/12 ,  A61K31/53 ,  C07D403/04 ,  A61K31/55 ,  C07D403/12

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D251/52 ,  C07D251/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I. Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

公开(公告)号：EP1351941A1

公开(公告)日：2003-10-15

申请号：EP02717403.6

申请日：2002-01-18

申请人： PHARMACOPEIA, INC.

发明人： GUO, Tao ,  HO, Koc-Kan ,  MCDONALD, Edward ,  DOLLE, Roland, Ellwood ,  SAIONZ, Kurt, W. ,  KULTGEN, Steven, G. ,  LIU, Ruiyan ,  DONG, Guizhen ,  GENG, Peng ,  ADANG, Anton, Egbert, Peter ,  VAN STRATEN, Nicole, Corine, Renee

IPC分类号： C07D241/08 ,  A61K31/495 ,  C07D233/78 ,  C07C271/20 ,  C07C237/22 ,  C07C275/14 ,  C07D233/12 ,  C07D207/26 ,  C07D243/08 ,  A61K31/45 ,  A61K31/55 ,  A61K31/551 ,  A61K31/4166 ,  A61P15/08

CPC分类号： C07D207/273 ,  A61K38/00 ,  C07C237/22 ,  C07C271/22 ,  C07C275/14 ,  C07C2601/02 ,  C07D223/10 ,  C07D233/76 ,  C07D241/08 ,  C07D243/08 ,  C07K5/06078 ,  C07K5/06191

摘要： The invention relates to a bisaryl derivative of the formula I, wherein (R, R) is selected from (H, H), O, (H, CH3), (H, OH) and (H, CN); Ar is substituted phenyl; and A is a group of following formula II, III, IV or V: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.

摘要翻译： 本发明涉及式I的二芳基衍生物，其中（R，R）选自（H，H），O，（H，CH 3），（H，OH）和（H，CN）; Ar是取代的苯基; 并且A是下列通式II，III，IV或V的组：本发明的化合物具有FSH受体调节活性，可用于控制生育力，避孕或用于治疗激素依赖性疾病。