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1. 发明申请

WO2004099206A1 ISOQUINOLINE-3-CARBOXYLIC ACID AMIDES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：异喹啉-3-羧酸酰胺及其药物用途
公开(公告)号：WO2004099206A1
公开(公告)日：2004-11-18
申请号：PCT/EP2004/005042
申请日：2004-05-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SEILER, Max, Peter
发明人： SEILER, Max, Peter
IPC分类号： C07D471/08
CPC分类号： C07D453/02
摘要： The present invention relates to novel isoquinoline-3-carboxylic acid amides having α7 nicotinic acetylcholine receptor agonistic activity, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
摘要翻译：本发明涉及具有α7烟碱乙酰胆碱受体激动活性的新型异喹啉-3-羧酸酰胺，它们的制备，它们作为药物的用途和含有它们的药物组合物。

2. 发明申请

WO2002076946A2 PYRIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物
公开(公告)号：WO2002076946A2
公开(公告)日：2002-10-03
申请号：PCT/EP2002/003332
申请日：2002-03-25
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , CULSHAW, Andrew, James , GULL, Peter , HALLETT, Allan , KIM, Hong-Yong , SEILER, Max, Peter , ZIMMERMANN, Kaspar , LIU, Yugang , PRASHAD, Mahavir
发明人： CULSHAW, Andrew, James , GULL, Peter , HALLETT, Allan , KIM, Hong-Yong , SEILER, Max, Peter , ZIMMERMANN, Kaspar , LIU, Yugang , PRASHAD, Mahavir
IPC分类号： C07D211/00
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula I (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，及其制备。式I化合物是人类香草素受体1（hVR1）的功能阻断剂，可用作药物; 特别是用于治疗疼痛。

3. 发明申请

WO1986006717A1 3-AMINOPROPYLOXYPHENYL DERIVATIVES THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：他们的制备和含有它们的药物组合物的3-氨基丙烯酰基衍生物
公开(公告)号：WO1986006717A1
公开(公告)日：1986-11-20
申请号：PCT/AU1986000133
申请日：1986-05-13
申请人： LOUIS, William, John , BERTHOLD, Richard , SEILER, Max-Peter , STOLL, André
IPC分类号： C07D209/08
CPC分类号： C07D333/38 , C07D209/08 , C07D209/34 , C07D209/42 , C07D231/56 , C07D307/24 , C07D307/68 , C07D333/24
摘要： Compounds of formula (I), characterised in that R signifies optionally substituted heteroaryl-, heteroarylalkyl or heteroarylalkenyl, R1 signifies hydrogen or a substituent, R2 is hydroxy or a group -Z-(CH2)n-Y-R3 wherein R3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxygen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or imino, and X signifies a bond or imino, and their physiologically hydrolysable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Process for the preparation of the compounds are also disclosed.

4. 发明申请

WO02076946A3 FUSED PYRIDINE DERIVATIVES FOR USE AS VANILLOID RECEPTOR ANTAGONISTS FOR TREATING PAIN. 审中-公开
标题翻译：用于治疗疼痛的VANILLOID受体拮抗剂的氟化吡啶衍生物。
公开(公告)号：WO02076946A3
公开(公告)日：2002-12-27
申请号：PCT/EP0203332
申请日：2002-03-25
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , CULSHAW ANDREW JAMES , GULL PETER , HALLETT ALLAN , KIM HONG-YONG , SEILER MAX PETER , ZIMMERMANN KASPAR , LIU YUGANG , PRASHAD MAHAVIR
发明人： CULSHAW ANDREW JAMES , GULL PETER , HALLETT ALLAN , KIM HONG-YONG , SEILER MAX PETER , ZIMMERMANN KASPAR , LIU YUGANG , PRASHAD MAHAVIR
IPC分类号： A61K31/519 , A61K31/522 , A61K45/00 , A61P1/04 , A61P1/18 , A61P7/00 , A61P7/10 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/14 , A61P13/10 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P35/00 , A61P37/08 , C07D471/04 , C07D495/14
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I) wherein R , R , R , R and R are as defined in the description, and the preparation thereof. The compounds of formula I are functional blockers of the human vanilloid receptor 1 (hVR1) and are useful as pharmaceuticals; in particular for treating pain.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，及其制备。式I化合物是人类香草素受体1（hVR1）的功能阻断剂，可用作药物; 特别是用于治疗疼痛。

5. 发明申请

WO1998001444A1 BENZO[g]QUINOLINE DERIVATIVES 审中-公开
标题翻译：苯并[g]喹啉衍生物
公开(公告)号：WO1998001444A1
公开(公告)日：1998-01-15
申请号：PCT/EP1997003582
申请日：1997-07-07
申请人： NOVARTIS AG , GULL, Peter , MARKSTEIN, Rudolf , SEILER, Max, Peter
发明人： NOVARTIS AG
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D473/00 , C07D513/04
摘要： The invention provides a compound of formula (I) wherein A, B, X, Y and R are as defined in the description, and a process for preparing them. The compounds of formula (I) are useful as pharmaceuticals for the treatment of glaucoma and myopia.
摘要翻译：本发明提供式（I）化合物，其中A，B，X，Y和R如描述中所定义，及其制备方法。式（I）化合物可用作治疗青光眼和近视的药物。

6. 发明申请

WO2008034600A1 PYRROLE DERIVATIVES USEFUL FOR THE TREATMENT OF CYTOKINE-MEDIATED DISEASES 审中-公开
标题翻译：用于治疗细胞因子介导性疾病的微量元素衍生物
公开(公告)号：WO2008034600A1
公开(公告)日：2008-03-27
申请号：PCT/EP2007/008153
申请日：2007-09-19
申请人： NOVARTIS AG , HENG, Richard , KOCH, Guido , SCHLAPBACH, Achim , SEILER, Max, Peter
发明人： HENG, Richard , KOCH, Guido , SCHLAPBACH, Achim , SEILER, Max, Peter
IPC分类号： C07D405/14 , C07D403/04 , C07D401/14 , C07D401/04 , A61K31/506 , A61K31/444 , A61K31/4439 , A61P37/00
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D403/04
摘要： A compound of Formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R1-R6 and A are as defined in the specification.
摘要翻译：式（I）的化合物或其药学上可接受的盐或前药酯，其中基团R 1 -R 6和A如说明书中所定义。

7. 发明申请

WO1997003054A1 BENZO[g]QUINOLINE DERIVATIVES 审中-公开
标题翻译：苯并[g]喹啉衍生物
公开(公告)号：WO1997003054A1
公开(公告)日：1997-01-30
申请号：PCT/EP1996002969
申请日：1996-07-05
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , NEUMANN, Peter , PFAEFFLI, Paul , SEILER, Max, Peter , SWOBODA, Robert
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.
IPC分类号： C07D221/08
CPC分类号： C07D401/12 , C07D221/08 , C07D265/34 , C07D279/14
摘要： The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and a process for preparing them. The compounds of formula (I) are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中X，Y，R 1，R 2，R 3和R 4如说明书中所定义，及其制备方法。式（I）的化合物可用作药物。

8. 发明申请

WO1985004403A1 3-AMINOPROPYLOXYPHENYL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 3-氨基戊酰氧基衍生物，其制备和含有它们的药物组合物
公开(公告)号：WO1985004403A1
公开(公告)日：1985-10-10
申请号：PCT/AU1985000063
申请日：1985-03-28
申请人： SANDOZ LTD. , LOUIS, William, John , SEILER, Max-Peter , STOLL, André
发明人： SANDOZ LTD.
IPC分类号： C07D309/08
CPC分类号： C07D309/08
摘要： Formula (I), wherein A) R is O(CH2)2O-R3 and (a) R1 and R5 are hydrogen and R3 is n-propyl, isobutyl, cyclopentylmethyl, benzyl or 2-(p-fluorophenyl)ethyl; (b) R1 is fluorine and R5 is hydrogen and R3 is n-propyl; (c) R1 is methyl and R5 is hydrogen and R3 is cyclopropylmethyl; (d) R1 is cyano and R5 is hydrogen and R3 is n-propyl; (e) R1 is hydrogen, R5 is methyl and R3 is alkyl of 2 to 5 carbon atoms, cycloalkylmethyl of 5 to 7 carbon atoms in the cycloalkyl part thereof or -(CH2)n-R' wherein n is 0, 1 or 2 and R' is phenyl or monofluorophenyl; or B) R is hydroxy, R1 is fluorine and R5 is hydrogen, and their physiologically hydrolysable derivatives, in which at least one hydroxy group is in esterified form, and their salts, elicit highly cardioselective beta 1 adrenoceptor blockade, and in most cases cardiospecific blockade, and relevant cardiotonic activity. These compounds can be used as therapeutic agents. One obtains these compounds by 3-amino-2-oxypropylation of the respective substituted phenol.
摘要翻译：式（I）其中A）R是O（CH 2）2 O-R 3和（a）R 1和R 5是氢，R 3是正丙基，异丁基，环戊基甲基，苄基或2-（对氟苯基）乙基; （b）R1是氟，R5是氢，R3是正丙基; （c）R1是甲基，R5是氢，R3是环丙基甲基; （d）R1是氰基，R5是氢，R3是正丙基; （e）R 1为氢，R 5为甲基，R 3为2〜5个碳原子的烷基，环烷基部分为5〜7个碳原子的环烷基甲基或 - （CH 2）n R'，其中n为0,1或2，R '是苯基或单氟苯基; 或B）R是羟基，R 1是氟并且R 5是氢，以及它们的生理上可水解的衍生物，其中至少一个羟基是酯化形式，及其盐引起高度心脏选择性的β1肾上腺素能受体阻断，并且在大多数情况下是心脏特异性的封锁和相关的强心活动。这些化合物可以用作治疗剂。通过相应的取代苯酚的3-氨基-2-氧丙基化得到这些化合物。

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