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1. 发明申请

WO2005092856A8 TETRAHYDROCARBAZOLES AND DERIVATIVES 审中-公开
标题翻译：四氯化碳和衍生物
公开(公告)号：WO2005092856A8
公开(公告)日：2006-12-21
申请号：PCT/EP2005002869
申请日：2005-03-17
申请人： HOFFMANN LA ROCHE , DEHMLOW HENRIETTA , KUHN BERND , MASCIADRI RAFFAELLO , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
发明人： DEHMLOW HENRIETTA , KUHN BERND , MASCIADRI RAFFAELLO , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
IPC分类号： A61K31/40 , C07D209/70 , C07D209/86 , C07D209/88 , C07D401/12 , C07D403/06 , C07D403/12 , C07D411/06 , C07D411/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04
CPC分类号： C07D413/06 , C07D209/70 , C07D209/88 , C07D403/12 , C07D413/14 , C07D417/06
摘要： The present invention relates to compounds of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 , X 2 , X 3 , X 4 , n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXRa and/or LXRß agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4，其中，R 5，X 5，X 1，X 2，X 3，X 4， SUP，n和k在说明书和权利要求书中被定义，以及其药学上可接受的盐和/或其药学上可接受的酯。该化合物可用于治疗和预防由LXRα和/或LXRβ激动剂调节的疾病，包括增加脂质和胆固醇水平，特别是低HDL-胆固醇，高LDL-胆固醇，动脉粥样硬化疾病，糖尿病，特别是非胰岛素依赖性糖尿病，代谢综合征，血脂异常，阿尔茨海默氏病，败血症，炎性疾病如结肠炎，胰腺炎，胆汁淤积/肝纤维化，以及具有炎性成分如阿尔茨海默病和受损/可改善的认知功能的疾病。

2. 发明申请

WO2008080844A9 AZASPIRO DERIVATIVES 审中-公开
标题翻译： AZASPIRO衍生物
公开(公告)号：WO2008080844A9
公开(公告)日：2009-10-08
申请号：PCT/EP2007064183
申请日：2007-12-19
申请人： HOFFMANN LA ROCHE , BISSANTZ CATERINA , GRUNDSCHOBER CHRISTOPHE , MASCIADRI RAFFAELLO , RATNI HASANE , ROGERS-EVANS MARK , SCHNIDER PATRICK
发明人： BISSANTZ CATERINA , GRUNDSCHOBER CHRISTOPHE , MASCIADRI RAFFAELLO , RATNI HASANE , ROGERS-EVANS MARK , SCHNIDER PATRICK
IPC分类号： C07D491/20 , A61K31/438 , A61P9/12 , A61P25/24
CPC分类号： C07D491/20
摘要： The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新型吲哚-3-基 - 羰基 - 氮杂螺哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑和抑郁症等疾病。特别地，本发明涉及通式（I）的化合物，其中R 1至R 6，U，V，W，X，Y和Z如说明书中所定义。

3. 发明申请

WO2008077810A3 SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译： SPIRO-PIPERIDINE衍生物
公开(公告)号：WO2008077810A3
公开(公告)日：2008-09-25
申请号：PCT/EP2007063879
申请日：2007-12-13
申请人： HOFFMANN LA ROCHE , BISSANTZ CATERINA , GRUNDSCHOBER CHRISTOPHE , MASCIADRI RAFFAELLO , RATNI HASANE , ROGERS-EVANS MARK , SCHNIDER PATRICK
发明人： BISSANTZ CATERINA , GRUNDSCHOBER CHRISTOPHE , MASCIADRI RAFFAELLO , RATNI HASANE , ROGERS-EVANS MARK , SCHNIDER PATRICK
IPC分类号： C07D211/16 , A61K31/4355 , A61K31/437 , A61K31/438 , A61P9/00 , C07D471/10 , C07D491/10
CPC分类号： C07D491/107 , C07D211/16 , C07D221/20 , C07D401/06 , C07D405/06 , C07D471/10
摘要： The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with the general formula (I), wherein R 1 to R 5 , R 5' , R 7 to R 9 , R 7' , R 8' , X and Y are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新型螺 - 哌啶衍生物，它们的制造方法，含有它们的药物组合物以及它们作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑症和抑郁症以及其他疾病。用通式（I）描述本发明的化合物，其中R 1至R 5，R 5，R 5，R 5，R 5，R 5， R 7，R 8，R 8，X和Y如说明书中所定义。

4. 发明申请

WO2006128802A3 3-METHANESULFONYLQUINOLINES AS GABA-B ENHANCERS 审中-公开
标题翻译：作为GABA-B增强剂的3-甲磺酰基胆碱
公开(公告)号：WO2006128802A3
公开(公告)日：2007-04-12
申请号：PCT/EP2006062514
申请日：2006-05-23
申请人： HOFFMANN LA ROCHE , MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
发明人： MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
IPC分类号： C07C225/22 , A61K31/47 , A61K31/4709 , C07D215/36 , C07D215/38 , C07D215/42 , C07D265/22 , C07D401/04
CPC分类号： C07D265/22 , C07D215/36 , C07D215/38 , C07D215/42 , C07D401/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined hereinabove which are active at the GABA B receptor and which can be used for the preparation of medicaments useful in the control or prevention of CNS disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3如上所定义，其在 GABA B 受体，其可用于制备可用于控制或预防CNS障碍的药物。

5. 发明申请

WO9616046A2 NOVEL BENZYL PYRIMIDINES 审中-公开
标题翻译：新颖的苄基吡啶
公开(公告)号：WO9616046A2
公开(公告)日：1996-05-30
申请号：PCT/EP9504451
申请日：1995-11-13
申请人： HOFFMANN LA ROCHE , GUERRY PHILIPPE , JOLIDON SYNESE , MASCIADRI RAFFAELLO , STALDER HENRI , THEN RUDOLF
发明人： GUERRY PHILIPPE , JOLIDON SYNESE , MASCIADRI RAFFAELLO , STALDER HENRI , THEN RUDOLF
IPC分类号： A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/675 , A61K31/695 , A61P31/04 , C07C255/37 , C07D215/56 , C07D239/48 , C07D239/49 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D417/10 , C07D471/04 , C07F7/10 , C07F7/18 , C07F9/6512
CPC分类号： C07D239/49 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D471/04 , C07F7/1856 , C07F9/65122
摘要： Substituted 5-benzyl-2,4-diaminopyrimidines of general formula (I) in which R represents lower alkoxy, R represents bromine or lower alkoxy and R represents aryl, heteroaryl or a group -Q-R , wherein Q signifies ethylene, vinylene or ethynylene and R signifies aryl, heteroaryl, lower alkoxy-carbonyl or carbamoyl, as well as readily hydrolyzable esters of carboxylic acids of formula I and pharmaceutically acceptable salts of these compounds can be used in the control or prevention of infectious diseases.
摘要翻译：取代的通式（I）的5-苄基-2,4-二氨基嘧啶，其中R 1表示低级烷氧基，R 2表示溴或低级烷氧基，R 3表示芳基，杂芳基或基团-QR 30>，其中Q表示乙烯，亚乙烯基或亚乙炔基，R 30表示芳基，杂芳基，低级烷氧基 - 羰基或氨基甲酰基，以及式I的羧酸的易水解的酯和这些化合物的药学上可接受的盐在控制或预防传染病方面。

6. 发明申请

WO0240487A3 BENZODIAZEPINE DERIVATIVES AS GABA A RECEPTOR MODULATORS 审中-公开
标题翻译：作为GABA受体调节剂的苯二氮卓衍生物
公开(公告)号：WO0240487A3
公开(公告)日：2002-09-26
申请号：PCT/EP0112887
申请日：2001-11-08
申请人： HOFFMANN LA ROCHE
发明人： MASCIADRI RAFFAELLO , THOMAS ANDREW WILLIAM , WICHMANN JUERGEN
IPC分类号： A61K31/55 , A61K31/5517 , A61P25/00 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to compounds of formula (I), wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, trifluoromethyl, trifluoromethoxy or lower alkylthio; R is -C(O)O-lower alkyl, isoxazol, 1,2,4-oxadiazol-3-yl or 1,2,4-oxadiazol-5-yl, which rings may be substituted by lower alkyl, trifluoromethyl or cycloalkyl; R is hydrogen, lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-halogen, -(CH2)n-pyridin-4-yl, or -(CH2)n-phenyl, wherein the phenyl ring may be substituted by one or two substituents selected from the group consisting of lower alkoxy, halogen, -SO2CH3, phenyl, OCF3, nitro, CF3, -NR2, or is -(CH2)n-indolyl, optionally substituted by lower alkyl or lower alkoxy, or is pyrrolidinyl-5-oxo, -C(O)-NR2, -(CH2)n-OH, -(CH2)n-NR2 or -(CH2)n-benzo[1,3]dioxole; R is hydrogen or lower alkyl; and n is 0, 1, 2 or 3; and to their pharmaceutically acceptable acid addition salts. These compounds have a good affinity to the GABA A alpha 5 receptor and they are therefore useful for the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，卤素，低级烷基，低级烷氧基，羟基，氰基，三氟甲基，三氟甲氧基或低级烷硫基; R 2是-C（O）O-低级烷基，异恶唑，1,2,4-恶二唑-3-基或1,2,4-恶二唑-5-基，该环可以被低级烷基取代，三氟甲基或环烷基; （CH 2）n - 卤素， - （CH 2）n - 吡啶-4-基或 - （CH 2）n - 苯基，其中苯基环可以被一个或两个选自低级烷氧基，卤素，-SO 2 CH 3，苯基，OCF 3，硝基，CF 3，-NR 2或是 - （CH 2）n - 吲哚基的取代基取代，任选被低级烷基或低级烷氧基或吡咯烷基-5-氧代-C（O）-NR2， - （CH2）n-OH， - （CH2）n-NR2或 - （CH2）n-苯并[1,3] R是氢或低级烷基; 并且n为0,1,2或3; 及其药学上可接受的酸加成盐。这些化合物对GABA Aα5受体具有良好的亲和力，因此它们可用于治疗与该受体有关的疾病。

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