公开(公告)号：EP0983243B1

公开(公告)日：2004-06-16

申请号：EP98910350.2

申请日：1998-03-13

申请人： SMITHKLINE BEECHAM CORPORATION ,  CEPHALON, INC.

发明人： DAINES, Robert, A. ,  KINGSBURY, William, D. ,  PENDRAK, Israil ,  MALLAMO, John, P.

IPC分类号： C07D215/52 ,  C07D401/12 ,  C07D401/06 ,  C07D401/10 ,  A61K31/47

CPC分类号： C07D215/50 ,  C07D215/22 ,  C07D215/52 ,  C07D221/18 ,  C07D401/06 ,  C07D401/10

摘要： Pharmaceutical compositions and methods of inhibiting calpain using novel quinoline- or naphthalenecarboxamides are disclosed.

公开(公告)号：EP1005445B1

公开(公告)日：2004-05-26

申请号：EP98945235.4

申请日：1998-08-13

申请人： F. HOFFMANN-LA ROCHE AG

发明人： CHEN, Li ,  GUTHRIE, Robert, William ,  HUANG, Tai-Nang ,  HULL, Kenneth, G. ,  SIDDURI, Achytharao ,  TILLEY, Jefferson, Wright

IPC分类号： C07C233/87 ,  C07C235/52 ,  C07C237/36 ,  C07C317/50 ,  C07C323/39 ,  C07D215/50 ,  C07D233/32 ,  C07D295/088 ,  C07D487/04 ,  A61K31/165 ,  A61K31/33

CPC分类号： C07D213/82 ,  C07C233/87 ,  C07C235/52 ,  C07C237/36 ,  C07C311/17 ,  C07C311/21 ,  C07C317/44 ,  C07C323/62 ,  C07D211/64 ,  C07D215/30 ,  C07D215/50 ,  C07D233/32 ,  C07D233/36 ,  C07D239/28 ,  C07D249/06 ,  C07D261/18 ,  C07D277/56 ,  C07D295/15 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

摘要： Compounds of formula (1) as well as their salts and esters are disclosed wherein X, X', Z and Y are as described in the specification and which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

摘要翻译： 公开了式（1）化合物及其盐和酯，其中X，X'，Z和Y如说明书中所述并且具有作为VCAM-1与表达VLA-4的细胞之间结合的抑制剂的活性。 此类化合物可用于治疗其症状和/或损伤与VCAM-1与表达VLA-4的细胞的结合相关的疾病。

公开(公告)号：EP1385839A1

公开(公告)日：2004-02-04

申请号：EP02761911.3

申请日：2002-04-11

申请人： GlaxoSmithKline S.p.A.

发明人： FARINA, Carlo ,  GAGLIARDI, Stefania ,  GIARDINA, Giuseppe, Arnaldo, Maria ,  MARTINELLI, Marisa

IPC分类号： C07D401/06 ,  C07D409/14 ,  C07D215/16 ,  C07D215/52 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/00 ,  A61P25/00

CPC分类号： C07D215/50 ,  C07D215/16 ,  C07D215/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/06 ,  C07D487/04

摘要： A compound forula (I) below or a pharmaceuticaly acceptable salt or solvate thereof: wherein R1 is H or alkyl; R2 is aryl or cycloalkyl or heteroaryl; R3 is H or alkyl, wherein the alkyl group may be optionally substituted by one or more fluorine atoms; R4 is H, hydroxyalkyl, dihydroxyalkyl or hydroxyalkoxyalkyl; R5 is branched or linear alkyl, cycloalkyl, cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: alkyl, alkenyl, aryl, alkoxy, hydroxy, halo, nitro, cyano, carboxy, carboxamido, sulphonamido, trifluoromethyl, or amino or mono- or di-alkylamino; R7 is H or halo; R¿8= is H or =O; and any of R¿2? and R5 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy, oxo, alkyl, alkenyl, aryl, alkoxy, carboxamido, sulphonamido, trifluoromethyl, or mono- or di- alkylamino; with the proviso that said compound of formula (I) is not a compound selected from the list according to claim 1.

公开(公告)号：EP1359915A1

公开(公告)日：2003-11-12

申请号：EP02702068.4

申请日：2002-01-25

申请人： Smithkline Beecham

发明人： DHANAK, Dashyant ,  KNIGHT, Steven, D. ,  WARREN, Gregory, L.

IPC分类号： A61K31/47 ,  A61K31/4709 ,  C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  A61P9/00

CPC分类号： C07D215/38 ,  C07D215/50 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

摘要： The present invention relates to quinolines, pharmaceutical compositions containing them and their use as antagonists of urotensin II.

摘要翻译： 本发明涉及喹啉，含有它们的药物组合物以及它们作为尾加压素II的拮抗剂的用途。

公开(公告)号：EP1353913A2

公开(公告)日：2003-10-22

申请号：EP02729622.7

申请日：2002-01-15

申请人： AstraZeneca AB

发明人： CHAPDELAINE, Marc,AstraZeneca Wilmington ,  DAVENPORT, Timothy,AstraZeneca Wilmington ,  HAEBERLEIN, Markus ,  HORCHLER, Carey,AstraZeneca Wilmington ,  MCCAULEY, John,AstraZeneca Wilmington ,  PIERSON, Edward,AstraZeneca Wilmington ,  SOHN, Daniel

IPC分类号： C07D311/24 ,  C07D311/74 ,  C07D405/14 ,  C07D417/14 ,  C07D215/233 ,  C07D215/48 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/497

CPC分类号： C07D231/12 ,  A61K31/495 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D215/50 ,  C07D233/56 ,  C07D249/08 ,  C07D311/24 ,  C07D311/58 ,  C07D401/04 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D417/12

摘要： Provided herein is a compound having the formula (I) wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.

公开(公告)号：EP1340744A2

公开(公告)日：2003-09-03

申请号：EP03011749.3

申请日：1994-10-07

申请人： Agouron Pharmaceuticals, Inc.

发明人： Dressman, Bruce A. ,  Fritz, James E. ,  Hammond, Marlys ,  Hornback, William J. ,  Kaldor, Stephen W. ,  Kalish, Vincent J. ,  Munroe, John E. ,  Reich, Siegfried Heinz ,  Tatlock, John H. ,  Shepherd, Timothy A. ,  Rodriguez, Michael J. ,  Jungheim, Louis N.

IPC分类号： C07D207/16 ,  A61K31/47 ,  A61P31/18 ,  C07D211/60 ,  C07D215/50 ,  C07D217/26 ,  C07D401/06 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62 ,  C07C323/60 ,  C07D209/08 ,  C07D215/48 ,  C07D217/02 ,  C07C237/42

CPC分类号： C07D401/06 ,  C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62

摘要： HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

摘要翻译： 可通过化学合成获得的HIV蛋白酶抑制剂抑制或阻断HIV蛋白酶的生物学活性，导致HIV病毒的复制终止。 这些化合物以及含有这些化合物和任选的其它抗病毒剂作为活性成分的药物组合物适用于治疗已知导致AIDS的HIV病毒感染的患者或宿主。

公开(公告)号：EP1332133A1

公开(公告)日：2003-08-06

申请号：EP01974298.0

申请日：2001-09-25

申请人： JANSSEN PHARMACEUTICA N.V.

发明人： MABIRE, Dominique, Jean-PierreJanssen-Cilag S.A. ,  VENET, Marc, GastonJanssen-Cilag S.A. ,  COUPA, SophieJanssen-Cilag S.A. ,  PONCELET, Alain, PhilippeJanssen-Cilag S.A. ,  LESAGE,Anne,Simone,J.Janssen Pharmaceutica N.V.

IPC分类号： C07D215/18 ,  C07D215/22 ,  C07D215/14 ,  C07D215/38 ,  C07F7/10 ,  C07D215/48 ,  C07D409/04 ,  C07D471/04 ,  C07D215/36 ,  C07D405/04 ,  C07D409/12 ,  C07D401/12 ,  C07D491/04 ,  C07D495/04 ,  A61K31/47

CPC分类号： C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D221/10 ,  C07D221/12 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D417/04 ,  C07D453/06 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07F7/0812

摘要： The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C¿1-6?alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R?2¿ represents hydrogen; halo; C¿1-6?alkyl or amino; R?3 and R4¿ each independently represent hydrogen or C¿1-6?alkyl; or R?2 and R3¿ may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z¿4?-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR?11¿ wherein R11 is C¿1-6?alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R?3 and R4¿ may be taken together to form a bivalent radical of formula -CH¿2?-CH2-CH2-CH2- ; R?5¿ represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

公开(公告)号：EP1003724B1

公开(公告)日：2003-02-12

申请号：EP97915425.9

申请日：1997-03-25

申请人： Aventis Pharma Deutschland GmbH

发明人： KIRSCH, Reinhard ,  KLEIM, Jörg-Peter ,  RIESS, Günther ,  ROSENSTOCK, Bernd ,  RÖSNER, Manfred ,  WINKLER, Irvin

IPC分类号： C07D215/50 ,  A61K31/47 ,  C07D401/12

CPC分类号： C07D215/227 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  C07D215/50 ,  C07D401/12 ,  C07D491/04 ,  C07D491/06

公开(公告)号：EP1077944A1

公开(公告)日：2001-02-28

申请号：EP98945825.2

申请日：1998-09-02

申请人： GUILFORD PHARMACEUTICALS INC.

发明人： LI, Jia-He ,  ZHANG, Jie

IPC分类号： C07D215/50 ,  C07C235/84 ,  A61K31/16 ,  A61K31/47

CPC分类号： C07D257/04 ,  A61K31/16 ,  A61K31/47 ,  C07C233/65 ,  C07C235/84 ,  C07D209/42 ,  C07D215/50 ,  C07D217/24 ,  C07D217/26 ,  C07D221/12 ,  C07D221/18 ,  C07D239/72 ,  C07D307/84 ,  C07D333/68 ,  C07D495/04

摘要： A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof; wherein: Y represents the atoms necessary to form a fused 5-to 6-membered, aromatic or non-aromatic, carbocyclic or N-containing heterocyclic ring, wherein Y and any heteroatom(s) therein are unsubstituted or independently substituted by at least one non-interfering alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, carboxy or halo substituent; X is at the 1-position of ring Y and is -COOR5 or a substituted or unsubstituted moiety selected from the group consisting of (a), (b), (c), (d), (e), (f) and (g) wherein R7 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R1 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R2, R3, R4 and R5 are independently hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl, and are either unsubtsituted or substituted with a moiety selected from the group consisting of alkyl, alkenyl, alkoxy, phenoxy, benzyloxy, cycloalkyl, cycloalkenyl, hydroxy, carboxy, carbonyl, amino, amido, cyano, isocyano, nitro, nitroso, nitrilo, isonitrilo, imino, azo, diazo, sulfonyl, sulfoxy, thio, thiocarbonyl, sulfhydryl, halo, haloalkyl, trifluoromethyl and aryl.

公开(公告)号：EP0831831A1

公开(公告)日：1998-04-01

申请号：EP96918362.0

申请日：1996-06-06

申请人： RHONE-POULENC RORER PHARMACEUTICALS, INC.

发明人： MYERS, Michael, R. ,  SPADA, Alfred, P. ,  MAGUIRE, Martin, P. ,  PERSONS, Paul, E.

IPC分类号： C07D239 ,  A61K31 ,  A61P9 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07C43 ,  C07D213 ,  C07D215 ,  C07D241 ,  C07D265 ,  C07D277 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D471

CPC分类号： C07C43/2055 ,  A61K31/517 ,  A61K31/5377 ,  C07C43/225 ,  C07C43/23 ,  C07D213/30 ,  C07D213/64 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/233 ,  C07D215/50 ,  C07D239/74 ,  C07D239/88 ,  C07D239/91 ,  C07D239/93 ,  C07D239/94 ,  C07D241/42 ,  C07D241/52 ,  C07D265/22 ,  C07D277/64 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D471/04

摘要： This invention relates to a method for the selective treatment of cell growth and differentiation characterized by activity of the human epidermal growth factor receptor type 2 (HER2). More specifically, this invention relates to the use of substituted or unsubstituted mono- or bi-cyclic aryl, heteroaryl, cycloalkyl or heterocycloalkyl compounds in selectively regulating cell growth. Pharmaceutical compositions useful for the selective treatment of cell growth and differentiation are also described.

摘要翻译： 本发明涉及以人表皮生长因子受体2型（HER2）的活性为特征的选择性治疗细胞生长和分化的方法。 更具体地说，本发明涉及取代或未取代的单环或双环芳基，杂芳基，环烷基或杂环烷基化合物在选择性调节细胞生长中的用途。 还描述了用于选择性处理细胞生长和分化的药物组合物。