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41. 发明专利

MY118897A CHROMANONE AND THIOCHROMANONE DERIVATIVES 未知
公开(公告)号：MY118897A
公开(公告)日：2005-02-28
申请号：MYPI9901329
申请日：1999-04-07
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , NUSSBAUMER PETER , SCHREINER ERWIN , SCHUSTER INGEBORG
IPC分类号： C07D311/22 , A61K31/35 , A61K31/352 , A61K31/382 , A61P5/28 , A61P5/32 , A61P13/08 , A61P15/00 , A61P17/08 , A61P17/14 , A61P35/00 , A61P43/00 , C07D335/06
摘要： THE INVENTION CONCERNS THE COMPOUNDS OF FORMULA I (FORMULA I)WHEREINRL 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; ANDR4 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; ANDR4 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.

42. 发明专利

PT1230227E 未知
公开(公告)号：PT1230227E
公开(公告)日：2004-10-29
申请号：PT00981270
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： A61K31/423 , A61K31/428 , A61P1/04 , A61P3/10 , A61P5/14 , A61P5/28 , A61P5/32 , A61P9/00 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/08 , A61P17/10 , A61P17/14 , A61P19/02 , A61P21/04 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D263/56 , C07D263/57 , C07D277/64 , C07D413/06 , C07D417/06
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.

43. 发明专利

DE69903143T2 未知
公开(公告)号：DE69903143T2
公开(公告)日：2003-06-05
申请号：DE69903143
申请日：1999-04-07
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH
发明人： BILLICH ANDREAS , NUSSBAUMER PETER , SCHREINER ERWIN , SCHUSTER INGEBORG
IPC分类号： A61K31/352 , A61K31/382 , A61P5/28 , A61P5/32 , A61P13/08 , A61P15/00 , A61P17/08 , A61P17/14 , A61P35/00 , A61P43/00 , C07D311/22 , C07D335/06 , A61K31/35
摘要： The invention concerns the compounds of formula IwhereinR1 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; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; or is 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; andR4 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; andR4 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.

44. 发明专利

HK1049329A1 Benzoxa-and benzothiazolyl sulfamates and their use as steroid sulfatase inhibitors. 未知
公开(公告)号：HK1049329A1
公开(公告)日：2003-05-09
申请号：HK02109307
申请日：2002-12-23
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , SCHREINER ERWIN PAUL , WOLFF-WINISKI BARBARA
IPC分类号： A61K31/423 , A61K31/428 , A61P1/04 , A61P3/10 , A61P5/14 , A61P5/28 , A61P5/32 , A61P9/00 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/08 , A61P17/10 , A61P17/14 , A61P19/02 , A61P21/04 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D263/56 , C07D263/57 , C07D277/64 , C07D413/06 , C07D , A61K , A61P
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.

45. 发明专利

AT224885T 未知
公开(公告)号：AT224885T
公开(公告)日：2002-10-15
申请号：AT99917963
申请日：1999-04-07
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH
发明人： BILLICH ANDREAS , NUSSBAUMER PETER , SCHREINER ERWIN , SCHUSTER INGEBORG
IPC分类号： A61K31/352 , A61K31/382 , A61P5/28 , A61P5/32 , A61P13/08 , A61P15/00 , A61P17/08 , A61P17/14 , A61P35/00 , A61P43/00 , C07D311/22 , C07D335/06 , A61K31/35
摘要： The invention concerns the compounds of formula IwhereinR1 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; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; or is 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; andR4 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; andR4 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.

46. 发明专利

PE10122001A1 BENZOXA Y BENZOTIAZOLES COMO INHIBIDORES DE SULFATASA DE ESTEROIDE 未知
公开(公告)号：PE10122001A1
公开(公告)日：2001-10-02
申请号：PE0012332000
申请日：2000-11-17
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , WOLFF-WINISKI BARBARA , SCHREINER ERWIN PAUL
IPC分类号： A61K31/423 , A61K31/428 , A61P1/04 , A61P3/10 , A61P5/14 , A61P5/28 , A61P5/32 , A61P9/00 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/08 , A61P17/10 , A61P17/14 , A61P19/02 , A61P21/04 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D263/56 , C07D263/57 , C07D277/64 , C07D413/06 , C07D417/06
CPC分类号： C07D263/56 , C07D263/57 , C07D277/64 , C07D413/06
摘要： SE REFIERE A BENZOXA O BENZOTIAZOLES SUSTITUDOS EN POSICION 2 Y CON UN ESTER DEL ACIDO SULFAMICO ENLAZADO POR OXIGENO AL FENILO DEL COMPUESTO DE FORMULA I; DONDE X ES O, S; R1 Y R2 SON H, ALQUILO; O UNO ES H Y EL OTRO ES ACILO, ALCOXICARBONILO; R3 ES ALQUILO, ALQUENILO, ALQUINILO, CICLOALQUILO, ENTRE OTROS. UN COMPUESTO PREFERIDO ES 2-(ADAMANTAN-2-ILIDENMETIL)BENZOXAZOL-6-IL-ESTER DEL ACIDO SULFAMICO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION, A COMPUESTOS INTERMEDIOS. EL COMPUESTO I INHIBE A ESTEROIDE SULFATASA REDUCIENDO LOS NIVELES ENDOGENOS DE ANDROGENOS, ESTROGENOS EN LA PIEL Y PUEDE SER UTIL EN EL TRATAMIENTO DEL ACNE, SEBORREA, ALOPECIA ANDROGENICA, HIRSUTISMO, CARCINOMA DE CELULAS ESCAMOSAS

47. 发明专利

ES2463490T3 Amidas como inhibidores de la esfingomielina 未知
公开(公告)号：ES2463490T3
公开(公告)日：2014-05-28
申请号：ES07801793
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 , A61K31/185 , A61K31/433 , A61K31/662 , A61P19/00 , A61P31/00 , C07C309/24 , C07D285/10
摘要： Un compuesto de la fórmula en donde **Fórmula** A es hidrógeno o (C1-4) alquilo, R1 es un grupo Y-R2, Y no está presente o es (C1-4) alquileno, cuyo alquileno opcionalmente, está sustituido, por halógeno, R2 es -P (O) (OH) (OH), o un grupo de la fórmula X es un grupo de la fórmula el anillo A es (C5-12) cicloalquileno, (C5-12) cicloalquenileno o fenileno, y el anillo B es (C5-12) cicloalquilo no sustituido, (C5-12) cicloalquenilo o (C6-12) arilo, o (C5-12) cicloalquilo, (C5-12) cicloalquenilo o (C6-12) arilo sustituido por R5, en donde R5 es halógeno, halo (C1-4) alquilo, halo (C1-4) alquiloxi, carboxilo, nitro, amino, un grupo que contiene fósforo, un grupo que contiene azufre, o acilo o aciloxi que comprende de 1 a 12 átomos de carbono al lado del grupo de CO, o R5 es un grupo -ZR6, en donde Z no está presente o es NH, O u S, y R6 es hidrógeno si Z está presente, o R6 es, si Z está presente o no, (C3-12) cicloalquilo, (C5-12) cicloalquenilo, (C6-12) arilo, o heterociclilo, incluyen heterociclilo aromático y alifático que comprende 3 a 12 miembros de anillo, y 1 a 4 heteroátomos seleccionados de N, O u S, o (C1-22) alquilo, (C2-22) alquenilo, o (C2-22) alquinilo, cuyo alquilo, alquenilo o alquinilo es no sustituido o sustituido por (C6-12) arilo.

48. 发明专利

AT555790T 未知
公开(公告)号：AT555790T
公开(公告)日：2012-05-15
申请号：AT06791989
申请日：2006-09-12
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , STUETZ ANTON
IPC分类号： A61K31/505 , A61K9/00 , A61K9/70 , A61K31/44 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/538
摘要： A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof.

49. 发明专利

BRPI0615881A2 未知
公开(公告)号：BRPI0615881A2
公开(公告)日：2011-05-31
申请号：BRPI0615881
申请日：2006-09-12
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , STUETZ ANTON
IPC分类号： A61K31/505 , A61K9/70 , A61K31/44 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/538 , A61P17/00 , A61P17/06 , A61P17/10
摘要： A composition comprising a VEGF receptor inhibitor and a penetration enhancer and uses thereof.

50. 发明专利

SG165371A1 COMBINATIONS COMPRISING A VEGF RECEPTOR INHIBITOR AND A PENETRATION ENHANCER 未知
公开(公告)号：SG165371A1
公开(公告)日：2010-10-28
申请号：SG2010066090
申请日：2006-09-12
申请人： NOVARTIS AG
发明人： BILLICH ANDREAS , STUETZ ANTON
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. (No suitable figure)

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