公开(公告)号：EP1070059A1

公开(公告)日：2001-01-24

申请号：EP99917963.3

申请日：1999-04-07

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

发明人： BILLICH, Andreas ,  NUSSBAUMER, Peter ,  SCHREINER, Erwin ,  SCHUSTER, Ingeborg

IPC分类号： C07D311/22 ,  C07D335/06 ,  A61K31/35

CPC分类号： C07D335/06 ,  C07D311/22

摘要： The invention concerns compounds of formula (I), wherein R1 and R2 independently are hydrogen, acyl, alkoxycarbonyl or alkyl; either the sulfamoyloxy side chain is bound to the 6 position; R3 is alkyl; alkenyl; alkinyl; a cycloalkyl moiety optionally substituted by alkyl, alkoxy or halogen; arylalkyl; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; a heteroaryl moiety optionally substituted by alkyl, alkoxy or halogen; or is heteroarylalkyl; and R4 is hydrogen; alkyl; hydroxy; or alkoxy; or the sulfamoyloxy side chain is bound to the 7 position; R3 has the significance indicated above for R4; and R4 has the significance indicated above for R3; X is O or S; and the symbol --- is a single or a double bond; in free form or salt form. They can be prepared by sulfamoylation of corresponding hydroxylated compounds, by reduction and/or by N-substitution. They are indicated for use as pharmaceuticals, particularly in the prophylactic or curative treatment of illnesses responsive to steroid sulfatase inhibition.

公开(公告)号：EP1070059B1

公开(公告)日：2002-09-25

申请号：EP99917963.3

申请日：1999-04-07

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

发明人： BILLICH, Andreas ,  NUSSBAUMER, Peter ,  SCHREINER, Erwin ,  SCHUSTER, Ingeborg

IPC分类号： C07D311/22 ,  C07D335/06 ,  A61K31/35

CPC分类号： C07D335/06 ,  C07D311/22

公开(公告)号：EP1805170B1

公开(公告)日：2010-04-14

申请号：EP05798257.1

申请日：2005-10-19

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BILLICH, Andreas ,  LEHR, Philipp ,  GSTACH, Hubert

IPC分类号： C07D413/04 ,  C07D265/18 ,  A61K31/535 ,  A61P29/00

CPC分类号： C07D265/18 ,  C07D413/04 ,  C07F7/1856

摘要： 3,4-dihydro-benzo[e][1,3]oxazin-2-ones which are substituted at the nitrogen atom by unsubstituted or substituted (C3-8)cycloalkyl, (C1-4)alkyl(C3-8)cycloalkyl, (C6-18)aryl or (C6­-18)aryl(C1-4)alkyl and their use as pharmaceuticals.

公开(公告)号：EP2257291A2

公开(公告)日：2010-12-08

申请号：EP09713747.5

申请日：2009-02-19

申请人： Xenon Pharmaceuticals Inc. ,  Novartis AG

发明人： BILLICH, Andreas ,  WINTHER, Michael, D. ,  GOLDBERG, Yigal, Paul ,  WINZENBURG, Gesine ,  RAPP, Karin ,  FRITZE, Andreas

IPC分类号： A61K31/501 ,  A61P17/00 ,  A61P17/08 ,  A61P17/10 ,  A61K9/00 ,  A61K47/08 ,  A61K47/10 ,  A61K47/32

CPC分类号： A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00

摘要： Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human, including administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R
2 , R
3 , R
4 , R
5 , R
6 , R
6a , R
7 , R
7a , R
8 , R
8a , R
9 and R
9a are defined herein, and compositions including a compound of formula (I).

公开(公告)号：EP1230227B1

公开(公告)日：2004-06-23

申请号：EP00981270.2

申请日：2000-11-17

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BILLICH, Andreas ,  SCHREINER, Erwin, Paul ,  WOLFF-WINISKI, Barbara

IPC分类号： C07D263/56 ,  C07D277/64 ,  C07D413/06 ,  C07D417/06 ,  A61K31/423 ,  A61K31/428 ,  A61P17/00 ,  A61P35/00

CPC分类号： C07D263/56 ,  C07D263/57 ,  C07D277/64 ,  C07D413/06

公开(公告)号：EP1945217B1

公开(公告)日：2012-05-02

申请号：EP06791989.4

申请日：2006-09-12

申请人： Novartis AG

发明人： BILLICH, Andreas ,  STÜTZ, Anton

IPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/538 ,  A61K31/501 ,  A61K31/44 ,  A61K9/00 ,  A61K9/70 ,  A61K9/48 ,  A61K47/10 ,  A61K47/20 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10

CPC分类号： A61K9/0014 ,  A61K9/4858 ,  A61K31/44 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/538 ,  A61K47/10 ,  A61K47/20

摘要： A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof , for the treatment of dermatological diseases selected from psoriasis, atopic dermatitis and acne, are disclosed

公开(公告)号：EP1670807A1

公开(公告)日：2006-06-21

申请号：EP04765669.9

申请日：2004-09-28

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BILLICH, Andreas ,  ETTMAYER, Peter ,  MECHTCHERIAKOVA, Diana ,  NUSSBAUMER, Peter ,  WLACHOS, Alexander

IPC分类号： C07F9/113 ,  C07C215/24 ,  C09B69/00 ,  C12N9/12

CPC分类号： C12N9/1205 ,  C07C219/20 ,  C07C233/71 ,  C07C237/08 ,  C07C237/10 ,  C07C311/41 ,  C07C2603/50 ,  C07D271/12 ,  C07F9/65324 ,  C12Q1/42 ,  C12Q1/485 ,  G01N2500/02

摘要： The present invention relates to a method (assay) for determining the activity of an enzyme selected from the group consisting of a sphingosine kinase and a phosphatase involved in the sphingolipid pathway by use of a labeled sphingosine.

摘要翻译： 本发明涉及一种用于通过使用标记的鞘氨醇来测定选自鞘氨醇激酶和参与神经鞘脂途径的磷酸酶的酶的活性的方法（测定）。

公开(公告)号：EP2081649A2

公开(公告)日：2009-07-29

申请号：EP07821129.9

申请日：2007-10-10

申请人： NOVARTIS AG

发明人： BAUMRUKER, Thomas ,  BILLICH, Andreas ,  MECHTCHERIAKOVA, Diana ,  WLACHOS, Alexander

IPC分类号： A61P37/02 ,  A61K39/00 ,  A61K48/00

CPC分类号： G01N33/564 ,  G01N2800/102 ,  G01N2800/104 ,  G01N2800/285 ,  G01N2800/52

摘要： The use of CD1 B, or CD1 D, respectively as a target for a disorder selected from Systemic Lupus Erythematosus (SLE), Lupus Anticoagulant (LA) Rheumatoid Arthritis (RA) and Idiopathic Thrombocytopenic Purpura, and the use of CD1 D as a target in a disorder which is Multiple Sclerosis (MS), e g as a biomarker, a method for preparing a diagnostic kit and a method for identifying agents that modulates a disorder which is mediated by elevated levels of CD1 B, or CD1 D, respectively, in case of CD1 B, or CD1 D, respectively selected from Systemic Lupus Erythematosus (SLE), Lupus Anticoagulant (LA) Rheumatoid Arthritis (RA) and Idiopathic Thrombocytopenic Purpura, and in case of CD1 D a disorder which is Multiple Sclerosis (MS)

公开(公告)号：EP2057173A1

公开(公告)日：2009-05-13

申请号：EP07801793.6

申请日：2007-08-21

申请人： NOVARTIS AG

发明人： BAUMANN, Karl ,  BILLICH, Andreas ,  OBERHAUSER, Berndt

IPC分类号： C07F9/38 ,  C07D285/10 ,  C07C309/24 ,  A61P31/00 ,  A61P19/00 ,  A61K31/662 ,  A61K31/433 ,  A61K31/185

CPC分类号： C07D285/10 ,  C07F9/3882

摘要： The present invention, relates to compounds of formula (I), wherein A is hydrogen or (C1-4)alkyl, R1 is a group Y-R2, Y is not present or is (C1-4)alkylene, which alkylene optionally is substituted, e.g. one or morefold, by halogen, such as F, R2 is -P(O)(OH)(OH), or a group of formula (a) or (b) or (c), X is a group of formula (d) ring A is (C5-12)cycloalkylene, (C5-12)cycloalkenyIene or phenylene, and ring B is unsubstituted or substituted (C5-12)cycloalkyl, (C5-12)cycloalkenyI or (C6-12)aryl, and their use as pharmaceuticals.

公开(公告)号：EP1230227A1

公开(公告)日：2002-08-14

申请号：EP00981270.2

申请日：2000-11-17

申请人： Novartis AG

发明人： BILLICH, Andreas ,  SCHREINER, Erwin, Paul ,  WOLFF-WINISKI, Barbara

IPC分类号： C07D263/56 ,  C07D277/64 ,  C07D413/06 ,  C07D417/06 ,  A61K31/423 ,  A61K31/428 ,  A61P17/00 ,  A61P35/00

CPC分类号： C07D263/56 ,  C07D263/57 ,  C07D277/64 ,  C07D413/06

摘要： Benzoxa- and benzthiazoles substituted at the 2 position and carrying a sulfamic acid ester group bound via oxygen to the phenyl part of the ring structure, such as the compounds of formula (I) wherein the symbols have various significances, possess interesting pharmacological activity. They can be prepared by sulfamoylation of a corresponding compound carrying a hydroxy group on the phenyl part of the ring structure, or by N-substitution. They are indicated for use as steroid sulfatase inhibitors in the prevention and treatment of illnesses responsive to steroid sulfatase inhibition, such as acne.