公开(公告)号：EP1611104A1

公开(公告)日：2006-01-04

申请号：EP04722563.6

申请日：2004-03-23

申请人： Actelion Pharmaceuticals Ltd.

发明人： AISSAOUI, Hamed ,  CLOZEL, Martine ,  WELLER, Thomas ,  KOBERSTEIN, Ralf ,  SIFFERLEN, Thierry ,  FISCHLI, Walter

IPC分类号： C07D217/02 ,  C07D217/18 ,  C07D217/20 ,  C07D405/06 ,  C07D217/04 ,  C07D217/16 ,  A61P3/04 ,  A61P25/20 ,  A61K31/472

CPC分类号： C07D217/02 ,  C07D217/04 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D405/06

摘要： The invention relates to novel acetamide derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.

摘要翻译： 本发明涉及式（I）的新型乙酰胺衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及相关方面，包括制备这些化合物的方法，含有一种或多种这些化合物的药物组合物，特别是它们作为食欲素受体拮抗剂的用途。

公开(公告)号：EP1554239A2

公开(公告)日：2005-07-20

申请号：EP03785607.7

申请日：2003-10-06

申请人： Actelion Pharmaceuticals Ltd.

发明人： AISSAOUI, Hamed ,  CLOZEL, Martine ,  WELLER, Thomas ,  KOBERSTEIN, Ralf ,  SIFFERLEN, Thierry ,  FISCHLI, Walter,ACTELION Pharmaceuticals Ltd.

IPC分类号： C07C311/13 ,  C07C311/20 ,  C07C311/21 ,  C07D207/335 ,  C07D209/14 ,  C07D213/76 ,  C07D213/75 ,  C07D215/36 ,  C07D215/38 ,  C07D217/04 ,  C07D217/12 ,  C07D231/56 ,  C07D233/61 ,  C07D277/28

CPC分类号： C07C311/21 ,  A61K31/18 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/473 ,  C07C311/13 ,  C07C311/20 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/323 ,  C07D209/14 ,  C07D213/40 ,  C07D213/53 ,  C07D213/71 ,  C07D213/74 ,  C07D213/75 ,  C07D215/12 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D231/56 ,  C07D233/64 ,  C07D277/28 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12

摘要： The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.

摘要翻译： 本发明涉及新型磺酰基氨基 - 乙酸衍生物及其在制备药物组合物中作为活性成分的用途。 本发明还涉及包括制备这些化合物的方法，包含一种或多种这些化合物的药物组合物，特别是其作为食欲素受体拮抗剂的用途的相关方面。

公开(公告)号：EP1448189A2

公开(公告)日：2004-08-25

申请号：EP02790352.5

申请日：2002-11-11

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BREIMER, Lars, Holger ,  DHINGRA, Kapil ,  DHINGRA, Urvashi Hooda ,  RITLAND, Steve

IPC分类号： A61K31/404 ,  A61K31/7068 ,  A61P35/00

CPC分类号： A61K31/404 ,  A61K31/7068 ,  A61K31/7072 ,  A61K2300/00

摘要： The present invention relates to the use of a pharmaceutical combination comprising as a active ingredients a) a component consisting of pharmaceutical composition comprising a compound of formula (I) as defined in the description and claims and b) a component consisting of pharmaceutical composition comprising as an active ingredient gemcitabine for the preparation of a medicament for the treatment of patients suffering with cancer.

公开(公告)号：EP1434870A1

公开(公告)日：2004-07-07

申请号：EP02779375.1

申请日：2002-09-19

申请人： F. HOFFMANN-LA ROCHE AG

发明人： BLEICHER, Konrad ,  BORTHWICK, Scott ,  IDING, Hans ,  ROGERS-EVANS, Mark ,  SCHMID, Stefan ,  TONG, Han, Min ,  WIRZ, Beat

IPC分类号： C12P13/04 ,  C12P11/00 ,  C07C323/63

CPC分类号： C12P13/04 ,  C07C323/59 ,  C07C323/63 ,  C07D285/36 ,  C12P11/00 ,  C12P41/005

摘要： The compounds of formula (I) are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor). The present invention relates to a new process for the preparation compounds of formula (I), wherein R?1, R2, R3¿ and n are as described in the description which process comprises reacting compounds of formula (II), wherein R?1, R2, R3¿, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent.

公开(公告)号：EP1417202A2

公开(公告)日：2004-05-12

申请号：EP02732512.5

申请日：2002-03-21

申请人： F. HOFFMANN-LA ROCHE AG

发明人： EDLIN, Christopher, David ,  REDSHAW, Sally ,  SMITH, Ian, Edward, David ,  WALTER, Daryl, Simon

IPC分类号： C07D401/14 ,  C07D401/06 ,  A61K31/445 ,  A61P31/18

CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D401/14 ,  C07D491/10

摘要： The invention is concerned with novel aminopiperidine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of Formula (I) prevent the human immunodeficiency virus (HIV) from entering cells by blocking interaction of the viral envelope protein gp120 with a chemokine receptor on the cell surface. Consequently the compounds of this invention may be advantageously used as therapeutic agents for the treatment of diseases mediated by the human immunodeficiency virus (HIV), either alone or in combination with other inhibitors of HIV viral replication or with pharmacoenhancers. Disclosed are compounds of general formula (I) wherein R?1, R2, R3¿, X and A are as defined in the description.

公开(公告)号：EP0966464B1

公开(公告)日：2003-05-28

申请号：EP98913585.0

申请日：1998-02-24

申请人： Basilea Pharmaceutica AG

发明人： GUERRY, Philippe ,  HUBSCHWERLEN, Christian ,  JOLIDON, Synèse ,  SPECKLIN, Jean-Luc ,  WYSS, Pierre-Charles

IPC分类号： C07D403/10 ,  A61K31/505 ,  C07D405/14 ,  C07D403/14 ,  C07D401/14

CPC分类号： C07D403/10 ,  C07D403/14 ,  C07D405/14

摘要： The invention is concerned with compounds of general formula (I), wherein R1 signifies lower-alkoxy, R2 signifies hydroxy or lower-alkoxy, R3 signifies hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aralkyl, aryl-Q-alkyl, heterocyclalkyl or a group of the formula -(CH¿2?)n-, Q signifies -SO-; R?4, R4'? each independently signify hydrogen, alkyl, aryl or heterocyclalkyl, R?5¿ signifies hydrogen, alkyl, alkoxy, aryl or heterocycyl, or R?4 and R5¿ together can form a group -(CH¿2?)n-, and n is a whole number of 2 to 5, as well as pharmaceutically usable salts thereof; the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable salts and intermediates for their manufacture.