公开(公告)号：EP0787011A1

公开(公告)日：1997-08-06

申请号：EP95937005.0

申请日：1995-10-25

申请人： Novartis AG ,  SANDOZ-PATENT-GMBH ,  SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H.

发明人： COTTENS, Sylvain ,  HAEBERLIN, Barbara ,  SEDRANI, Richard ,  VONDERSCHER, Jacky

IPC分类号： A61K ,  A61K47 ,  A61K9 ,  A61K31 ,  A61K38 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37

CPC分类号： A61K9/0019 ,  A61K9/1075 ,  A61K9/4858 ,  A61K31/436 ,  A61K38/13 ,  A61K47/12

摘要： This invention provides a microemulsion pre-concentrate comprising a difficultly soluble active agent and a carrier medium comprising: 1) a hydrophilic phase which comprises dimethylisosorbide and/or a lower alkyl alkanoic ester, 2) a lipophilic phase, and 3) a surfactant. The active agent may be a cyclosporin or a macrolide. In another aspect, this invention provides a pharmaceutical composition for enteral or parenteral administration comprising a macrolide and an acid.

公开(公告)号：EP0663916A1

公开(公告)日：1995-07-26

申请号：EP93920822.0

申请日：1993-09-24

申请人： SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H. ,  SANDOZ-PATENT-GMBH ,  SANDOZ LTD.

发明人： COTTENS, Sylvain ,  SEDRANI, Richard

IPC分类号： A61K31 ,  A61K38 ,  A61K39 ,  A61P11 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D498 ,  C07F7

CPC分类号： C07D498/18

摘要： Novel O-alkylated derivatives of rapamycin of formula (I), especially 40-O-alkylated derivatives, are found to have pharmaceutical utility, particularly as immunosuppressants.

公开(公告)号：EP0734389A1

公开(公告)日：1996-10-02

申请号：EP95903810.0

申请日：1994-12-16

申请人： SANDOZ LTD. ,  SANDOZ-PATENT-GMBH ,  SANDOZ-ERFINDUNGEN Verwaltungsgesellschaft m.b.H.

发明人： COTTENS, Sylvain ,  SEDRANI, Richard

IPC分类号： A61K31 ,  A61P37 ,  C07D498 ,  C07F7

CPC分类号： C07D498/18 ,  C07F7/1852

摘要： Novel demethoxy derivatives of rapamycin of formula (I) are found to have pharmaceutical utility, particularly as an immunosuppressants. In formula (I) R2 = formula (II) or formula (III), X, Y, R1, R3, R3, R4, R5 are as defined in the application.

公开(公告)号：EP1692095A1

公开(公告)日：2006-08-23

申请号：EP04819639.8

申请日：2004-11-30

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： SELLNER, Holger ,  GROSS, Gerhard ,  MAIBAUM, Juergen, Klaus ,  COTTENS, Sylvain

IPC分类号： C07C237/22 ,  A61K31/165

CPC分类号： C07C237/22

摘要： The invention relates to novel δ-amino-Ϝ-hydroxy-ω-aryl-alkanoic acid amides of formula (I), or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP1337527A1

公开(公告)日：2003-08-27

申请号：EP01993604.6

申请日：2001-11-05

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： ALBERT, Rainer ,  COOKE, Nigel, Graham ,  COTTENS, Sylvain ,  EHRHARDT, Claus ,  EVENOU, Jean-Pierre ,  SEDRANI, Richard ,  VON MATT, Peter ,  WAGNER, Jürgen ,  ZENKE, Gerhard

IPC分类号： C07D403/04 ,  C07D403/14 ,  A61K31/404 ,  A61P29/00 ,  A61P37/06

CPC分类号： C07D403/14 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10

摘要： Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

公开(公告)号：EP0663916B1

公开(公告)日：1998-11-25

申请号：EP93920822.9

申请日：1993-09-24

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： COTTENS, Sylvain ,  SEDRANI, Richard

IPC分类号： C07D498/18 ,  C07F7/18 ,  A61K31/435

CPC分类号： C07D498/18

摘要： Novel O-alkylated derivatives of rapamycin of formula (I), especially 40-O-alkylated derivatives, are found to have pharmaceutical utility, particularly as immunosuppressants.

公开(公告)号：EP2007788A2

公开(公告)日：2008-12-31

申请号：EP07781535.5

申请日：2007-04-09

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： COTTENS, Sylvain ,  EHRHARDT, Claus ,  FU, Jiping ,  PARKER, David Thomas ,  PATANE, Michael ,  RADETICH, Branko ,  RAMAN, Prakash ,  RANDL, Stefan Andreas ,  RIGOLLIER, Pascal ,  SEEPERSAUD, Mohindra ,  SIMIC, Oliver ,  WAN, Dongpeng

IPC分类号： C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  A61K38/00 ,  A61P31/14

CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/0808 ,  C07K5/1016

摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

公开(公告)号：EP1007033B1

公开(公告)日：2008-04-23

申请号：EP98951317.1

申请日：1998-08-26

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BAUER, Wilfried ,  COTTENS, Sylvain ,  GEYL, Dieter ,  WEITZ-SCHMIDT, Gabriele ,  KALLEN, Jörg ,  HOMMEL, Ulrich

IPC分类号： A61K31/365 ,  A61K31/22 ,  A61K31/19 ,  A61K31/44 ,  C07D309/10 ,  C07D309/30 ,  C07D319/06 ,  C07D213/64

CPC分类号： C07D213/64 ,  A61K31/00 ,  A61K31/222 ,  A61K31/366 ,  C07C219/24 ,  C07C235/30 ,  C07C237/18 ,  C07C237/22 ,  C07C2601/08 ,  C07C2602/28 ,  C07D207/16 ,  C07D295/13 ,  C07D295/145 ,  C07D295/205 ,  C07D307/52 ,  C07D309/10 ,  C07D309/30 ,  C07D405/12 ,  C07D491/10

摘要： The present invention relates to compounds which bind to all or parts of the active binding 'south pole pocket' of the LFA-1 I-domain and their uses as LFA-1 antagonists.

公开(公告)号：EP1836163A2

公开(公告)日：2007-09-26

申请号：EP05825434.3

申请日：2005-12-21

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BREITENSTEIN, Werner ,  COTTENS, Sylvain ,  EHRHARDT, Claus ,  JACOBY, Edgar ,  LORTHIOIS, Edwige, Liliane, Jeanne ,  MAIBAUM, Juergen, Klaus ,  OSTERMANN, Nils ,  SELLNER, Holger ,  SIMIC, Oliver

IPC分类号： C07D207/09 ,  C07D207/14 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  C07D409/12 ,  C07D207/08 ,  C07D413/12 ,  C07D417/12 ,  C07D491/10 ,  A61K31/40 ,  A61K31/41 ,  A61K31/435 ,  A61K31/54 ,  A61P9/00

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D207/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/10

摘要： Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel inter­mediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as described in the specificacion.

公开(公告)号：EP1154988B1

公开(公告)日：2004-08-11

申请号：EP00916832.9

申请日：2000-02-14

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BAENTELI, Rolf ,  BAUER, Wilfried ,  COTTENS, Sylvain ,  EHRHARDT, Claus ,  HOMMEL, Ulrich ,  KALLEN, Jörg ,  MEINGASSNER, Josef, Gottfried ,  NUNINGER, François ,  WEITZ-SCHMIDT, Gabriele

IPC分类号： C07C235/26 ,  C07C237/18 ,  C07C235/30 ,  C07C237/20 ,  C07D211/76 ,  C07D265/24 ,  C07D401/06 ,  A61K31/4402 ,  A61K31/45 ,  A61K31/4545 ,  A61K31/535 ,  A61P9/10 ,  A61P3/06 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07C271/12 ,  C07C235/26 ,  C07C235/30 ,  C07C237/18 ,  C07C2602/28 ,  C07D211/76 ,  C07D265/10

摘要： Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.