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1. 发明申请

WO0211704A3 USE OF ARYL-SUBSTITUTED 1,1-DIPHOSPHONATES FOR THE TREATMENT OF BONE DISEASES 审中-公开
标题翻译：用于治疗骨髓疾病的ARYL替代的1,1-DipHOSPHONATES的应用
公开(公告)号：WO0211704A3
公开(公告)日：2002-07-18
申请号：PCT/EP0108676
申请日：2001-07-27
申请人： SYMPHAR SA , NIESOR ERIC J , GUYON-GELLIN YVES , BENTZEN CRAIG L , NGUYEN LAN MONG , PHAN HIEU TRUNG
发明人： NIESOR ERIC J , GUYON-GELLIN YVES , BENTZEN CRAIG L , NGUYEN LAN MONG , PHAN HIEU TRUNG
IPC分类号： A61K45/00 , A61K31/00 , A61K31/663 , A61P1/02 , A61P3/14 , A61P5/06 , A61P13/08 , A61P19/08 , A61P19/10 , A61P35/00 , A61P43/00
CPC分类号： A61K31/663
摘要： The invention provides the use of an aryl-substituted 1,1-diphosphonate for the manufacture of a medicament for stimulating bone formation; said aryl-susbtituted 1,1-diphosphonate being a compound of formula (I) in which A is (a) or (b) or (c) where: X is H, an alkyl group having from 1 to 4 carbon atoms; X , X and X are identical or different and are H, a straight or branched alkyl or alkoxy group having from 1 to 8 carbon atoms, X is H, a straight or branched alkyl group having from 1 to 8 carbon atoms, an optionally substituted benzyl group, X is H, a straight or branched alkyl group having from 1 to 8 carbon atoms, X is H or an alkyl group having from 1 to 4 carbon atoms, q is 0 or 1, R , R , R and R are identical or different and are H, a straight, branched or cyclic alkyl group comprising from 1 to 8 carbon atoms, or R , R and R and R may form an alkylidenedioxy ring comprising from 2 to 8 carbon atoms, L is -CH=CH-CH2-, -(CH2)n, -O(CH2)n, -S-, -SO2, -S(CH2)n-, -SO2(CH2)n, where n is an integer from 1 to 7, or together with B, L is (CH=CH)k-(CH2)dCH=where k is 0 or 1 and d is an integrer from 0 to 4, -B is H, an alkyl group having from 1 to 4 carbon atoms, -t is 0 or 1, with the proviso that t is 0 only when L, together with B, is (CH=CH)k-(CH2)d-CH= where k and d are as described above, and with the further proviso that when L is -(CH2)n or -S-, at least one of R , R , R and R is other than hydrogen.
摘要翻译：本发明提供了芳基取代的1,1-二膦酸盐在制备用于刺激骨形成的药物中的用途; 所述芳基 - 取代的1,1-二膦酸酯是其中A为（a）或（b）或（c）的式（I）化合物，其中：X为H，具有1至4个碳原子的烷基原子; X 1，X 2和X 3相同或不同，为H，具有1至8个碳原子的直链或支链烷基或烷氧基，X 4为H，直链或支链烷基具有1至8个碳原子的基团，任选取代的苄基，X 5是H，具有1至8个碳原子的直链或支链烷基，X 6是H或具有1至 4个碳原子，q为0或1，R 1，R 2，R 3和R 4相同或不同，为H，包含1至8个碳原子的直链，支链或环状烷基碳原子或R 1，R 2和R 3和R 4可以形成包含2至8个碳原子的亚烷基二氧基环，L是-CH = CH-CH 2 - ， - （CH 2） n，-O（CH 2）n，-S - ， - SO 2，-S（CH 2）n - ， - SO 2（CH 2）n，其中n是1至7的整数，或与B一起，L是（CH = CH）k-（CH 2）d CH =其中k为0或1，d为0至4的整数，-B为H，具有1至4个碳原子的烷基，-t为0或1，条件是仅当L与B一起为（CH = CH）k-（CH）时，t为0 2）d-CH =其中k和d如上所述，进一步的条件是当L是 - （CH 2）n或-S-时，R 1，R 2， 3>和R 4不是氢。

2. 发明申请

WO2008000643A1 BENZIMIDAZOLE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS FXR AGONISTS AND PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME 审中-公开
标题翻译：苯并咪唑衍生物，其生产方法，它们用作FXR激动剂和含有它的药物制剂
公开(公告)号：WO2008000643A1
公开(公告)日：2008-01-03
申请号：PCT/EP2007/055994
申请日：2007-06-18
申请人： F. HOFFMANN-LA ROCHE AG , BENSON, Gregory Martin , BLEICHER, Konrad , CHUCHOLOWSKI, Alexander , DEHMLOW, Henrietta , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , NIESOR, Eric J. , PANDAY, Narendra , RICHTER, Hans , SCHULER, Franz , WAROT, Xavier Marie , WRIGHT, Matthew , YANG, Minmin
发明人： BENSON, Gregory Martin , BLEICHER, Konrad , CHUCHOLOWSKI, Alexander , DEHMLOW, Henrietta , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer E. , NIESOR, Eric J. , PANDAY, Narendra , RICHTER, Hans , SCHULER, Franz , WAROT, Xavier Marie , WRIGHT, Matthew , YANG, Minmin
IPC分类号： C07D235/18 , C07D409/10 , C07D409/04 , C07D403/04 , C07D403/10 , A61K31/4184 , A61P3/00 , A61P25/00 , A61P35/00
CPC分类号： C07D235/18 , C07D235/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/06
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R 1 to R 8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的苯并咪唑衍生物，其中R 1至R 8如在说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物与FXR结合，可用作药物。

3. 发明申请

WO0211708A3 METHODS FOR INDUCING APOLIPOPROTEIN E SECRETION 审中-公开
标题翻译：诱导青蒿素E分泌的方法
公开(公告)号：WO0211708A3
公开(公告)日：2003-03-13
申请号：PCT/EP0108980
申请日：2001-08-02
申请人： SYMPHAR SA , NIESOR ERIC J , PEREZ ANE , THUILLARD JEAN-LUC , BENTZEN CRAIG L , NGUYEN LAN MONG
发明人： NIESOR ERIC J , PEREZ ANE , THUILLARD JEAN-LUC , BENTZEN CRAIG L , NGUYEN LAN MONG
IPC分类号： G01N33/50 , A61K31/045 , A61K31/08 , A61K31/232 , A61K31/335 , A61K31/336 , A61K31/575 , A61K31/58 , A61K45/00 , A61K45/06 , A61P3/00 , A61P3/10 , A61P25/00 , A61P25/20 , A61P25/28 , A61P27/02 , G01N33/15 , G01N33/53
CPC分类号： A61K45/06 , A61K31/045 , A61K31/335 , A61K31/575 , A61K31/215 , A61K31/08 , A61K2300/00
摘要： The invention provides a method for increasing apolipoprotein E (ApoE) in plasma and in tissues of a mammal by using a combination of an ApoE increasing amount of an activator of the orphan nuclear receptor FXR and an ApoE increasing amount of an activator of the orphan nuclear receptor LXR alpha . Also provided is the use of a combination of an ApoE increasing amount of a FXR activator and of an ApoE increasing amount of a LXR alpha activator, for the manufacture of a medicament for increasing ApoE in plasma and in tissues of a mammal.
摘要翻译：本发明提供了通过使用ApoE增加量的孤儿核受体FXR的活化剂和ApoE增加量的孤儿核激活剂的组合来增加血浆和哺乳动物组织中的载脂蛋白E（ApoE）的方法受体LXRα。还提供使用ApoE增加量的FXR活化剂和ApoE增加量的LXRα激活剂的组合，用于制备用于增加血浆和哺乳动物组织中的ApoE的药物。

4. 发明申请

WO2010069859A1 CYCLOHEXANECARBOXAMIDE DERIVATIVES USEFUL AS INHIBITORS OF CHOLESTERYL ESTER TRANSFER PROTEIN 审中-公开
标题翻译：作为胆固醇转运蛋白的抑制剂的环己基甲酰胺衍生物
公开(公告)号：WO2010069859A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/066863
申请日：2009-12-10
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , KUEHNE, Holger , NIESOR, Eric J. , PFLIEGER, Philippe
发明人： HOFFMANN, Torsten , KUEHNE, Holger , NIESOR, Eric J. , PFLIEGER, Philippe
IPC分类号： C07C323/52 , C07C327/30 , A61K31/167 , A61K31/216 , A61P9/00
CPC分类号： C07C323/52 , C07C327/30 , C07C2601/14
摘要： The invention is concerned with novel compound of formula (I) wherein R, R 2 and Q are as defined in the description and in the claims, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的新化合物，其中R，R 2和Q如说明书和权利要求书中所定义，及其药学上可接受的盐，其制备方法，它们作为药物的用途和包含它们的药物组合物。

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