公开(公告)号：EP1390063B1

公开(公告)日：2004-11-17

申请号：EP02748680.2

申请日：2002-04-29

申请人： F. HOFFMANN-LA ROCHE AG

发明人： INFELD, Martin, Howard ,  PHUAPRADIT, Wantanee ,  SHAH, Navnit, Hargovindas ,  ZHANG, Lin

IPC分类号： A61K38/55 ,  A61K9/20 ,  A61P31/12 ,  A61P31/18

CPC分类号： A61K31/472 ,  A61K9/146 ,  A61K9/2031

摘要： A solid unit oral pharmaceutical dosage form of amorphous nelfinavir mesylate is provided comprising amorphous nelfinavir mesylate, and a pharmaceutically acceptable, water soluble, non-ionic synthetic block copolymer of ethylene oxide and propylene oxide, said copolymer having a melting point of at least 40°C. A hot melt granulation process for making the dosage form is provided.

公开(公告)号：EP1390063A2

公开(公告)日：2004-02-25

申请号：EP02748680.2

申请日：2002-04-29

申请人： F. HOFFMANN-LA ROCHE AG

发明人： INFELD, Martin, Howard ,  PHUAPRADIT, Wantanee ,  SHAH, Navnit, Hargovindas ,  ZHANG, Lin

IPC分类号： A61K38/55 ,  A61K9/20 ,  A61P31/12 ,  A61P31/18

CPC分类号： A61K31/472 ,  A61K9/146 ,  A61K9/2031

摘要： A solid unit oral pharmaceutical dosage form of amorphous nelfinavir mesylate is provided comprising amorphous nelfinavir mesylate, and a pharmaceutically acceptable, water soluble, non-ionic synthetic block copolymer of ethylene oxide and propylene oxide, said copolymer having a melting point of at least 40°C. A hot melt granulation process for making the dosage form is provided.

摘要翻译： 提供了无定形奈非那韦甲磺酸盐的固体单位口服药物剂型，其包含无定形奈非那韦甲磺酸盐和环氧乙烷和环氧丙烷的药学上可接受的水溶性非离子合成嵌段共聚物，所述共聚物的熔点为至少40° C。 提供了制备该剂型的热熔造粒方法。

公开(公告)号：EP1067133B1

公开(公告)日：2003-09-17

申请号：EP00114219.9

申请日：2000-07-03

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Kienzle, Frank ,  Lalonde, Michel ,  Schmid, Rudolf ,  Wang, Shaoning

IPC分类号： C07F9/53 ,  C07B55/00 ,  C07B57/00 ,  C07F9/50

CPC分类号： C07F9/5329 ,  C07F9/5054

公开(公告)号：EP1315736A2

公开(公告)日：2003-06-04

申请号：EP01976128.7

申请日：2001-08-21

申请人： F. HOFFMANN-LA ROCHE AG

发明人： DEVOS, Rene ,  DYMOCK, Brian William ,  HOBBS, Christopher John ,  JIANG, Wen-Rong ,  MARTIN, Joseph Armstrong ,  MERRETT, John Herbert ,  NAJERA, Isabel ,  SHIMMA, Nobuo ,  TSUKUDA, Takuo

IPC分类号： C07H19/06 ,  C07H19/16 ,  A61K31/7064 ,  A61K31/7076 ,  A61P31/14

CPC分类号： C07H19/06 ,  C07H19/16

摘要： Use of compounds of formula (I), wherein R1 is hydrogen, hydroxy, alkyl, hydroxyalkyl, alkoxy, halogen, cyano, isocyano or azido; R2 is hydrogen, hydroxy, alkoxy, chlorine, bromine or iodine; R3 is hydrogen; or R?2 and R3¿ together represent =CH¿2?; or R?2 and R3¿ represent fluorine; X is O, s or CH¿2?; a, b, c, d denoting asymmetric carbon atoms each of which is substituted with 4 different substituents; and B signifies a purine base B1 which is connected through the 9-nitrogen of formula (B1), wherein R?4¿ is hydrogen, hydroxyl, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR7R8, halogen or SH; R5 is hydrogen, hydroxy, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR?7R8, NHOR9, NHNR7R8¿ or SH; R6 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR7R8, halogen, SH or cyano; R?7 and R8¿ are independently of each other hydrogen, alkyl, aryl, hydroxyalkyl, alkenylalkyl, alkynylalkyl, cycloalkyl or acyl; R9 is hydrogen, alkyl or aryl; or B signifies an oxidised purine base B2 which is connected through the 9-nitrogen of formula (B2), wherein R?4, R5 and R6¿ are as defined above; or B signifies a purine base B3 which is connected through the 9-nitrogen of formula (B3), wherein R?4 and R6¿ are as defined above; R10 is hydrogen, alkyl or aryl; Y is O, S or NR11; R11 is hydrogen, hydroxy, alkyl, OR9, heterocyclyl or NR?7R8; R7, R8 and R9¿ are as defined above; or B signifies a pyrimidine base B4 which is connected through the 1-nitrogen of formula (B4), wherein Z is O or S; R12 is hydrogen, hydroxy, alkyl, alkoxy, haloalkyl, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR?7R8, NHOR9, NHNR7R8¿ or SH; R13 is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl or halogen; R?7, R8 and R9¿ are as defined above; or B signifies a pyrimidine base B5 which is connected through the 1-nitrogen of formula (B5), wherein Y, Z, R10 are as defined above for the treatment of diseases mediated by the Hepatitis C Virus (HIV) or for the preparation of a medicament for such treatment. The invention is concerned with novel and known purine and pyrimidine nucleoside derivatives, their use as inhibitors of subgenomic Hepatitis C Virus (HCV) RNA replication and pharmaceutical compositions of such compounds.

公开(公告)号：EP3982967A1

公开(公告)日：2022-04-20

申请号：EP20733908.6

申请日：2020-06-10

申请人： Actelion Pharmaceuticals Ltd.

发明人： PREISS, Ralph, T. ,  BRUDERER, Shirin ,  CLOZEL, Martine ,  YANNOULIS ARCEDA, Natalia, Catalina

IPC分类号： A61K31/4965 ,  A61P9/12

公开(公告)号：EP3592391A1

公开(公告)日：2020-01-15

申请号：EP18711258.6

申请日：2018-03-07

申请人： Actelion Pharmaceuticals Ltd

发明人： HELLERBRAND, Klaus ,  SCHLICKER-SPAIN, Alexandra

IPC分类号： A61K47/10 ,  A61K9/19 ,  A61K31/4965 ,  A61P17/02 ,  A61P9/12

公开(公告)号：EP1993557B1

公开(公告)日：2015-11-11

申请号：EP07763188.5

申请日：2007-02-02

申请人： Actelion Pharmaceuticals Ltd.

发明人： PALEPU, Nagesh R.

IPC分类号： A61K31/557 ,  A61K31/5585 ,  A61K9/08 ,  A61K47/18 ,  A61K47/02 ,  A61K9/19 ,  A61K47/26 ,  A61K9/00

CPC分类号： A61K9/19 ,  A61K9/0019 ,  A61K31/557 ,  A61K31/5585 ,  A61K47/183 ,  A61K47/26

公开(公告)号：EP1611104B1

公开(公告)日：2009-07-01

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.

公开(公告)号：EP2007717A1

公开(公告)日：2008-12-31

申请号：EP07735447.0

申请日：2007-04-10

申请人： Actelion Pharmaceuticals Ltd.

发明人： AISSAOUI, Hamed ,  BOSS, Christoph ,  GUDE, Markus ,  KOBERSTEIN, Ralf ,  SIFFERLEN, Thierry ,  ZUMBRUNN ACKLIN, Cornelia

IPC分类号： C07C311/29 ,  C07D213/40 ,  C07D231/12 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D275/04 ,  C07D277/28 ,  C07D285/12 ,  C07D417/12 ,  A61K31/18 ,  A61P25/00

CPC分类号： C07C311/29 ,  C07C2601/02 ,  C07D213/40 ,  C07D213/61 ,  C07D213/64 ,  C07D231/12 ,  C07D231/16 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D275/04 ,  C07D277/28 ,  C07D285/12 ,  C07D417/12

摘要： The invention relates to sulfonamide compounds of formula (I), where A, B, R3 and R4 are as defined in the claims, and their use as orexin receptor antagonists in the prevention and treatment of eating and drinking disorders, all types of sleep disorders, all kinds of cognitive dysfunctions in the healthy population and psychiatric and neurologic disorders. Formula (I).

摘要翻译： 本发明涉及式（I）的新型磺酰胺化合物及其作为食欲素受体拮抗剂的用途。

公开(公告)号：EP1347967B1

公开(公告)日：2007-12-19

申请号：EP01988048.3

申请日：2001-12-19

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： C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D267/14 ,  C07D223/16 ,  C07D243/14 ,  C07D285/36 ,  C07D401/12 ,  A61K31/55

CPC分类号： C07D223/16 ,  A61K31/55 ,  C07D243/14 ,  C07D267/14 ,  C07D281/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention relates to novel benzazepines and related heterocyclic derivatives (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 the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.