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1. 发明授权

EP1651592B1 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： NEW二苯并[b，f]恶-10-羧酸酰胺和它们的药物应用
公开(公告)号：EP1651592B1
公开(公告)日：2009-04-29
申请号：EP04763454.8
申请日：2004-07-23
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
IPC分类号： C07C235/40 , C07D313/14 , C07D267/20 , A61K31/335 , A61K31/395 , A61K31/165 , A61P25/28
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).

2. 发明授权

EP1670803B1 CERTAIN SUBSTITUTED SPIROCYCLIC LACTAMS AND USE THEREOF AS PHARMACEUTICALS 有权
标题翻译：某些取代螺环内酰胺及其用作药物
公开(公告)号：EP1670803B1
公开(公告)日：2008-03-12
申请号：EP04765790.3
申请日：2004-10-04
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4-4]non-7-yl)-propionam ides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.

3. 发明公开

EP1851208A1 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物AS BACE抑制剂
公开(公告)号：EP1851208A1
公开(公告)日：2007-11-07
申请号：EP06701373.0
申请日：2006-01-13
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BETSCHART, Claudia , LERCHNER, Andreas , MACHAUER, Rainer , RÜEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
IPC分类号： C07D273/02
CPC分类号： C07D273/00 , C07D245/04 , C07D273/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/08
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

4. 发明公开

EP1651592A2 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： NEER DIBENZO [B，F] OXEPIN-10-CARBONSÄUREAMIDEUND DEREN PHARMAZEUTISCHE ANWENDUNGEN
公开(公告)号：EP1651592A2
公开(公告)日：2006-05-03
申请号：EP04763454.8
申请日：2004-07-23
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
IPC分类号： C07C235/40 , C07D313/14 , C07D267/20 , A61K31/335 , A61K31/395 , A61K31/165 , A61P25/28
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).
摘要翻译：本发明涉及新型的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β受体相关的神经和血管疾病，淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。

5. 发明公开

EP1838680A2 MACROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物和组合物AS BACE抑制剂
公开(公告)号：EP1838680A2
公开(公告)日：2007-10-03
申请号：EP06706226.5
申请日：2006-01-13
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： LERCHNER, Andreas , MACHAUER, Rainer , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D245/06 , C07D281/00 , A61P25/28 , A61K31/395
CPC分类号： C07D273/02 , C07D245/06 , C07D291/08 , C07D413/04 , C07D413/12 , C07D419/12
摘要： The invention relates to novel macrocyclic compounds of the formula in which R1, R3, V1, V2, X1, X2, Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16, 17 or 18, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

6. 发明公开

EP1670803A1 CERTAIN SUBSTITUTED SPIROCYCLIC LACTAMS AND USE THEREOF AS PHARMACEUTICALS 有权
标题翻译：某些取代螺环内酰胺及其用作药物
公开(公告)号：EP1670803A1
公开(公告)日：2006-06-21
申请号：EP04765790.3
申请日：2004-10-04
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4-4]non-7-yl)-propionam ides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.

7. 发明授权

EP1654241B1 MACROCYCLIC COMPOUNDS HAVING ASPARTIC PROTEASE INHIBITING ACTIVITY AND PHARMACEUTICAL USES THEREOF 有权
标题翻译：万家乐循环连接ASPARAGINPROTEASEHEMMENDER影响和它们的药物用途
公开(公告)号：EP1654241B1
公开(公告)日：2008-03-19
申请号：EP04740596.4
申请日：2004-07-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BETSCHART, Claudia , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D273/02 , C07D291/08 , A61P25/00 , A61K31/33
CPC分类号： C07D285/00 , A61K31/33 , C07D273/02 , C07D291/08
摘要： The present invention relates to macrocyclic compounds of formula (I), wherein R1, is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, hydroxy(C1-6)alkyl, (C1-4)alkylthio(C1-4)alkyl, (C1-6)alkenyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, piperidinyl or pyrrolidinyl, R2 and R4, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7) cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl or heteroaryl(C1-4) alkyl, or R2 and R4, together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R3 is hydrogen or (C1-4)alkyl, X1 is CH2, X2 is CH2, O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C1-4)alkyl, Y is (C1-8)alkylen or (C1-8)alkylenoxy(C1-6)alkylen, (C1-8)alkenylen or (C1-8)alkenylenoxy(C1-6)alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X1, and X2 are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S02, AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation.

8. 发明公开

EP1682521A1 MACROCYCLIC LACTAMS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：大环内酰胺类和它们的药物用途
公开(公告)号：EP1682521A1
公开(公告)日：2006-07-26
申请号：EP04797621.2
申请日：2004-11-04
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/02 , C07D281/00 , C07D255/02 , A61K31/33 , A61P25/00
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula (I) wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

9. 发明公开

EP1654241A1 MACROCYCLIC COMPOUNDS HAVING ASPARTIC PROTEASE INHIBITING ACTIVITY AND PHARMACEUTICAL USES THEREOF 有权
标题翻译：万家乐循环连接ASPARAGINPROTEASEHEMMENDER影响和它们的药物用途
公开(公告)号：EP1654241A1
公开(公告)日：2006-05-10
申请号：EP04740596.4
申请日：2004-07-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BETSCHART, Claudia , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D273/02 , C07D291/08 , A61P25/00 , A61K31/33
CPC分类号： C07D285/00 , A61K31/33 , C07D273/02 , C07D291/08
摘要： The present invention relates to macrocyclic compounds of formula (I), wherein R1, is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, hydroxy(C1-6)alkyl, (C1-4)alkylthio(C1-4)alkyl, (C1-6)alkenyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, piperidinyl or pyrrolidinyl, R2 and R4, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7) cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl or heteroaryl(C1-4) alkyl, or R2 and R4, together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R3 is hydrogen or (C1-4)alkyl, X1 is CH2, X2 is CH2, O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C1-4)alkyl, Y is (C1-8)alkylen or (C1-8)alkylenoxy(C1-6)alkylen, (C1-8)alkenylen or (C1-8)alkenylenoxy(C1-6)alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X1, and X2 are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S02, AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation.

10. 发明授权

EP2663561B1 NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS 有权
标题翻译：恶嗪衍生物及其神经系统疾病的治疗
公开(公告)号：EP2663561B1
公开(公告)日：2016-03-16
申请号：EP12700390.3
申请日：2012-01-11
申请人： Novartis AG
发明人： BADIGER, Sangamesh , CHEBROLU, Murali , HURTH, Konstanze , JACQUIER, Sébastien , LUEOEND, Rainer Martin , MACHAUER, Rainer , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob , VOEGTLE, Markus
IPC分类号： C07D413/14 , C07D471/04 , C07D487/04 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/14 , A61K31/5377 , C07B59/002 , C07B2200/05 , C07D471/04 , C07D487/04 , A61K2300/00

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