公开(公告)号：EP1848435A4

公开(公告)日：2010-09-29

申请号：EP06719652

申请日：2006-01-25

申请人： SYNTA PHARMACEUTICALS CORP

发明人： SUN LIJUN ,  CHEN SHOUJUN ,  JIANG JUN ,  YU CHIH-YI

IPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61P29/00 ,  A61P37/00 ,  C07D239/02 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

CPC分类号： C07D241/20 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

公开(公告)号：EP1606266A4

公开(公告)日：2008-06-25

申请号：EP04757813

申请日：2004-03-18

申请人： SMITHKLINE BEECHAM CORP

发明人： ALBERTI MICHAEL J ,  DREWRY DAVID HAROLD ,  MILLER D ,  BAMBOROUGH P

IPC分类号： A61K20060101 ,  C07D241/02 ,  C07D401/00 ,  C07D403/00 ,  C07D403/04 ,  C07D405/00 ,  C07D409/00 ,  C07D409/14 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D403/04 ,  C07D409/14 ,  C07D473/00 ,  C07D487/04

摘要： The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity.

摘要翻译： 本发明涉及氨基吡嗪衍生物，含有其的组合物和药物，以及制备和使用这些化合物，组合物和药物的方法。 这种氨基吡嗪衍生物可用于治疗与不适当的酪氨酸和/或丝氨酸/苏氨酸激酶活性相关的疾病。

公开(公告)号：EP1603570A4

公开(公告)日：2008-05-21

申请号：EP04715001

申请日：2004-02-26

申请人： SUGEN INC

发明人： CUI JINGJONG JEAN ,  ZHANG JENNIFER ,  HANAU CATHLEEN ELIZABETH ,  BHUMRALKAR DILIP ,  BOTROUS IRINY ,  CHU JI YU ,  FUNK LEE A ,  HARRIS JR G DAVIS ,  JIA LEI ,  JOHNSON JOANNE ,  KOLODZIEJ STEPHEN A ,  KUNG PEI-PEI ,  LI XIAOYUAN SHARON ,  LIN JASON QISHEN ,  MENG JERRY JIALUN ,  NAMBU MITCHELL DAVID ,  NELSON CHRISTOPHER G ,  PAIRISH MASON ALAN ,  SHEN HONG ,  TRAN-DUBE MICHELLE

IPC分类号： C07D213/73 ,  A61K20060101 ,  A61K31/44 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61P35/00 ,  C07D20060101 ,  C07D211/72 ,  C07D401/00 ,  C07D401/12 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D413/12 ,  C07D417/00 ,  C07D419/00

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D401/12 ,  C07D413/12

摘要： Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET.

公开(公告)号：EP1817285A2

公开(公告)日：2007-08-15

申请号：EP05856976.5

申请日：2005-11-18

申请人： Merck & Co., Inc.

发明人： DEVITA, Robert, J. ,  MILLS, Sander, G. ,  EID, Ronsar ,  YOUNG, Jonathan, R.

IPC分类号： C07D211/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

CPC分类号： C07D401/06 ,  C07D211/46 ,  C07D401/08

摘要： The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

公开(公告)号：EP1725535A2

公开(公告)日：2006-11-29

申请号：EP05724616.7

申请日：2005-03-04

申请人： Merck & Co., Inc.

发明人： MORRISSETTE, Matthew, M. ,  WILLIAMS, Peter, D. ,  WAI, John, S. ,  FISHER, Thorsten, E. ,  LYLE, Terry, A.

IPC分类号： C07D221/18 ,  C07D211/08 ,  C07D211/68 ,  C07D211/80 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07D231/02

CPC分类号： C07D471/04 ,  C07D471/10

摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式I化合物为HIV整合酶抑制剂和HIV复制抑制剂：（I）其中Z，R1，R2，R3，R4，R5，R6，R7，R8和R9如本文所定义。 这些化合物可用于预防和治疗HIV感染以及预防，延缓艾滋病的发作和治疗。 这些化合物本身作为化合物或以药学上可接受的盐的形式用于抗HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：EP1715867A1

公开(公告)日：2006-11-02

申请号：EP05713111.2

申请日：2005-02-09

申请人： Merck & Co., Inc.

发明人： BONNEFOUS, Celine ,  KAMENECKA, Theodore, M. ,  VERNIER, Jean-Michel

IPC分类号： A61K31/4965 ,  A61K31/44 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

CPC分类号： C07D401/12 ,  C07D213/81 ,  C07D241/26 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07F7/0812

摘要： The present invention is directed to novel amides such as those of Formula (I): (I) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel amides and/or compositions containing these compounds.

公开(公告)号：EP1653961A1

公开(公告)日：2006-05-10

申请号：EP04779406.0

申请日：2004-07-28

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： HEERDING, Dirk, A. ,  CLARK, Tammy, J. ,  DREWRY, David, H. ,  LEBER, Jack, Dale ,  SAFONOV, Igor ,  YAMASHITA, Dennis, S.

IPC分类号： A61K31/4965 ,  A61K31/505 ,  A61K31/44 ,  A01N43/54 ,  A01N43/42 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00

CPC分类号： C07D471/04

摘要： Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yI compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

公开(公告)号：EP1606266A2

公开(公告)日：2005-12-21

申请号：EP04757813.3

申请日：2004-03-18

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： ALBERTI, Michael J.,c/o GlaxoSmithKline ,  DREWRY, David, Harold,c/o GlaxoSmithKline ,  MILLER, D.,c/o GlaxoSmithKline Med. Res. Centre ,  BAMBOROUGH, P.,c/o GlaxoSmithKline Med. Res. Ctr.

IPC分类号： C07D241/02 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

CPC分类号： C07D471/04 ,  C07D403/04 ,  C07D409/14 ,  C07D473/00 ,  C07D487/04

摘要： The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity.

摘要翻译： 本发明涉及氨基吡嗪衍生物，含有其的组合物和药物，以及制备和使用这些化合物，组合物和药物的方法。 这种氨基吡嗪衍生物可用于治疗与不适当的酪氨酸和/或丝氨酸/苏氨酸激酶活性相关的疾病。

公开(公告)号：EP1603572A1

公开(公告)日：2005-12-14

申请号：EP04757541.0

申请日：2004-03-17

申请人： Bristol-Myers Squibb Company

发明人： QIAO, Jennifer, X. ,  WANG, Tammy, C. ,  WANG, Gren, Z. ,  GUNGOR, Timur

IPC分类号： A61K31/535 ,  A61K31/445 ,  A61K31/44 ,  C07D413/00 ,  C07D401/00 ,  C07D411/00

CPC分类号： C07D213/64 ,  C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trysin-like serine proteases, specifically factor Xa.

公开(公告)号：EP1436287A4

公开(公告)日：2005-10-26

申请号：EP02773438

申请日：2002-09-18

申请人： CURIS INC

发明人： BAXTER ANTHONY DAVID ,  BOYD EDWARD ANDREW ,  PORTER JEFFERY ,  PRICE STEPHEN ,  RUBIN LEE L ,  STIBBARD JOHN HARRY ALEXANDER ,  FRANK-KAMENETSKY MARIA

IPC分类号： C07D239/90 ,  A61K31/18 ,  A61K31/381 ,  A61K31/422 ,  A61K31/427 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/16 ,  A61P7/00 ,  A61P7/06 ,  A61P11/00 ,  A61P15/08 ,  A61P17/00 ,  A61P17/14 ,  A61P19/08 ,  A61P21/00 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P43/00 ,  C07C317/34 ,  C07C317/38 ,  C07D239/91 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D491/113 ,  C07D409/00 ,  A61K31/27 ,  A61K31/33 ,  A61K31/395 ,  A61K31/415 ,  A61P35/00 ,  C07D327/04 ,  C07D411/00

CPC分类号： A61K31/422 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/50 ,  A61K31/517 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14