公开(公告)号：EP1542681A2

公开(公告)日：2005-06-22

申请号：EP03774484.4

申请日：2003-09-19

申请人： SCHERING CORPORATION

发明人： COURTNEY, Rachel ,  LAUGHLIN, Mark, A.

IPC分类号： A61K31/4196 ,  C07D249/00 ,  A61P31/10

CPC分类号： A61K31/4178 ,  A61K31/496

摘要： The use of posaconazole for the preparation of a medicament for the treatment or prevention of fungal infections in humans of 12 years and older in need of such treatment or prevention the medicament which comprises an effective amount of posaconazole in divided doses two to four times a day to produce an arithmetic mean steady state average maximum plasma concentration of posaconazole of at least about 300 ng/mL to at least about 550 ng/mL is disclosed.

公开(公告)号：EP1175401B1

公开(公告)日：2005-07-20

申请号：EP00926486.2

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： BAROUDY, Bahige, M. ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  MCCOMBIE, Stuart, W. ,  MCKITTRICK, Brian, A. ,  MILLER, Michael, W. ,  NEUSTADT, Bernard, R. ,  PALANI, Anandan ,  SMITH, Elizabeth, M. ,  STEENSMA, Ruo ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  LAUGHLIN, Mark, A. ,  GILBERT, Eric ,  LABROLI, Marc, A.

IPC分类号： C07D211/58 ,  C07D401/06 ,  C07D405/12 ,  C07D401/10 ,  C07D413/06 ,  C07D409/06 ,  A61K31/496 ,  A61P31/12 ,  A61P19/00

CPC分类号： C07D409/06 ,  A61K31/496 ,  C07D211/58 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D413/06

摘要： The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R?4, R5 and R7¿ are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

公开(公告)号：EP1175224B1

公开(公告)日：2005-02-23

申请号：EP00928604.8

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： LAUGHLIN, Mark, A.

IPC分类号： A61K38/21 ,  A61P31/18

CPC分类号： A61K38/212 ,  A61K2300/00

摘要： The use of a pegylated interferon-alfa and a CCR5 antagonist, further in association with at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with an anti-HIV-1 drug therapy, e.g., HAART, for preparation of a medicament for the treatment of HIV-1 infections as well as HIV-1 infections as well as HIV-1 and HCV co-infections in treatment-naive as well as treatment-experienced adult and pediatric patients are disclosed.

公开(公告)号：EP1175401A1

公开(公告)日：2002-01-30

申请号：EP00926486.2

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： BAROUDY, Bahige, M. ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  MCCOMBIE, Stuart, W. ,  MCKITTRICK, Brian, A. ,  MILLER, Michael, W. ,  NEUSTADT, Bernard, R. ,  PALANI, Anandan ,  SMITH, Elizabeth, M. ,  STEENSMA, Ruo ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  LAUGHLIN, Mark, A. ,  GILBERT, Eric ,  LABROLI, Marc, A.

IPC分类号： C07D211/58 ,  C07D401/06 ,  C07D405/12 ,  C07D401/10 ,  C07D413/06 ,  C07D409/06 ,  A61K31/496 ,  A61P31/12 ,  A61P19/00

CPC分类号： C07D409/06 ,  A61K31/496 ,  C07D211/58 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D413/06

摘要： The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R?4, R5 and R7¿ are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

公开(公告)号：EP1175224A2

公开(公告)日：2002-01-30

申请号：EP00928604.8

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： LAUGHLIN, Mark, A.

IPC分类号： A61K38/21 ,  A61P31/18

CPC分类号： A61K38/212 ,  A61K2300/00

摘要： The use of a pegylated interferon-alfa and a CCR5 antagonist, further in association with at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with an anti-HIV-1 drug therapy, e.g., HAART, for preparation of a medicament for the treatment of HIV-1 infections as well as HIV-1 infections as well as HIV-1 and HCV co-infections in treatment-naive as well as treatment-experienced adult and pediatric patients are disclosed.

公开(公告)号：EP1175402B1

公开(公告)日：2005-07-20

申请号：EP00926487.0

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： BAROUDY, Bahige, M. ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  McCOMBIE, Stuart, W. ,  McKITTRICK, Brian, A. ,  MILLER, Michael, W. ,  NEUSTADT, Bernard, R. ,  PALANI, Anandan ,  STEENSMA, Ruo ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  LAUGHLIN, Mark, A.

IPC分类号： C07D211/58 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4468 ,  A61K31/4523 ,  A61P31/12 ,  A61P19/00

CPC分类号： C07D413/14 ,  C07D211/58 ,  C07D401/14 ,  C07D417/14

摘要： Pharmaceutical compositions for the treatment of HIV are provided comprising compounds of formula (II) or a pharmaceutically acceptable salt or isomer thereof, in combination with specified antiviral agents.

公开(公告)号：EP1263457A2

公开(公告)日：2002-12-11

申请号：EP01922303.1

申请日：2001-03-08

申请人： SCHERING CORPORATION

发明人： LAUGHLIN, Mark, A.

IPC分类号： A61K38/21 ,  A61P37/04 ,  A61P31/12

CPC分类号： A61K38/212

摘要： Use of interferon-alfa, e.g., pegylated interferon alfa-2a or 2b for preparation of a medicament for promotion of an HIV-1 specific immune response, e.g., promotion of HIV-1 specific T-cells, in adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV comprising a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b is disclosed.

公开(公告)号：EP1175402A1

公开(公告)日：2002-01-30

申请号：EP00926487.0

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： BAROUDY, Bahige, M. ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  McCOMBIE, Stuart, W. ,  McKITTRICK, Brian, A. ,  MILLER, Michael, W. ,  NEUSTADT, Bernard, R. ,  PALANI, Anandan ,  STEENSMA, Ruo ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  LAUGHLIN, Mark, A.

IPC分类号： C07D211/58 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4468 ,  A61K31/4523 ,  A61P31/12 ,  A61P19/00

CPC分类号： C07D413/14 ,  C07D211/58 ,  C07D401/14 ,  C07D417/14

摘要： Pharmaceutical compositions for the treatment of HIV are provided comprising compounds of formula (II) or a pharmaceutically acceptable salt or isomer thereof, in combination with specified antiviral agents.