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1. 发明公开

CN101065362A 2－烷氧基－3,4,5－三羟基－烷基酰胺、它们的制备、含有它们的组合物与用途失效
公开(公告)号：CN101065362A
公开(公告)日：2007-10-31
申请号：CN200580040746.4
申请日：2005-11-25
申请人：艾文蒂斯药品公司
发明人： J·张 , N·巴特纳加 , J·M·鲁瑟
IPC分类号： C07D223/12 , A61K31/55 , A61P35/00
CPC分类号： C07D223/12 , C07D205/085 , C07D207/273 , C07D207/277 , C07D211/76 , C07D215/38 , C07D223/16 , C07D243/08 , C07D281/06 , C07D281/08 , C07D417/06 , C07D471/04
摘要： 2－烷氧基－3，4，5－三羟基－烷基酰胺，它们的制备，含有它们的组合物与用途。本发明特别涉及2－烷氧基－3，4，5－三羟基－烷基酰胺，它们的制备，含有它们的组合物以及作为药品，特别作为抗癌剂的用途。

2. 发明公开

CN1279669A 芳族砜异羟肟酸金属蛋白酶抑制剂无效
公开(公告)号：CN1279669A
公开(公告)日：2001-01-10
申请号：CN98811130.6
申请日：1998-11-12
申请人： G·D·瑟尔公司
发明人： T·E·巴塔 , D·P·贝克 , T·L·贝姆 , G·A·德克雷森佐 , C·I·维拉米尔 , J·J·麦唐纳德 , J·N·弗雷斯科斯 , D·P·格特曼
IPC分类号： C07D211/66 , C07D309/08 , A61K31/445 , A61K31/35 , A61K31/16 , C07C317/44 , C07D335/02 , C07D405/12 , C07D409/12 , C07D211/94 , C07D405/14 , C07D239/04 , C07D417/12 , C07D407/12
CPC分类号： C07D231/12 , A61K31/19 , A61K31/4166 , A61K31/421 , A61K31/426 , C07C317/44 , C07D207/48 , C07D211/54 , C07D211/66 , C07D211/86 , C07D211/94 , C07D211/96 , C07D225/02 , C07D233/56 , C07D239/04 , C07D249/08 , C07D263/06 , C07D265/06 , C07D279/06 , C07D281/08 , C07D309/08 , C07D309/28 , C07D319/06 , C07D325/00 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要：公开治疗方法,该方法包括给予患有与病理性基质金属蛋白酶活性有关的疾病的宿主有效量的芳族砜异羟肟酸,所述异羟肟酸对一种或多种基质金属蛋白酶(MMP)如MMP－2、MMP－9和MMP－13显示极好的抑制活性,而对MMP－1基本上不显示抑制活性。所述给予的酶抑制剂或其药学上可接受的盐相应于下面式Ⅰ的结构,在式Ⅰ中R1和R2均为氢,或者R1和R2与它们所连接的原子一起形成在所述环中含有一个、两个或三个杂原子的5－8元环,所述杂原子为氧、硫或氮。式(Ⅰ)中的R3为任选取代的芳基或任选取代的杂芳基。也公开具有选择性活性的金属蛋白酶抑制剂化合物、这些化合物的生产方法以及使用抑制剂的药用组合物。

3. 发明公开

CN1031082A 萘并噻唑品衍生物和其制备方法失效
公开(公告)号：CN1031082A
公开(公告)日：1989-02-15
申请号：CN88104589
申请日：1988-07-23
申请人：田辺制药株式会社
发明人：井上博纯 , 我伊野三德 , 长尾拓 , 村田栄
IPC分类号： C07D281/10 , A61K31/55
CPC分类号： C07D281/08 , H01L2224/50 , H01L2924/00012
摘要：一种新颖的结构式为：的萘并噻唑品衍生物或其一种药物学上可接受的酸加成盐，其中R1为一种低级烷氧基基团，R2为氢原子或一种低级链烷酰基团，且R3和R4为相同或不相同的，并为氢原子或一种低级烷基基团。所述的衍生物(I)和其一种盐是用来作为低血压和/或冠状血管舒张剂或大脑血管舒张剂的。

4. 发明授权

CN1017151B 萘并硫杂氮衍生物的制备方法失效
公开(公告)号：CN1017151B
公开(公告)日：1992-06-24
申请号：CN88104589
申请日：1988-07-23
申请人：田辺制药株式会社
发明人：井上博纯 , 我伊野三德 , 长尾拓 , 村田栄
IPC分类号： C07D281/10 , A61K31/55
CPC分类号： C07D281/08 , H01L2224/50 , H01L2924/00012
摘要：一种新颖的结构式为：的萘并硫杂氟杂衍生物或其一种药物学上可接受的酸加成盐，其中R1为一种低级烷氧基基团，R2为氢原子或一种低级链烷酰基团，且R3和R4为相同或不相同的，并为氢原子或一种低级烷基基团。所述的衍生物(I)和其一种盐是用来作为降血压和/或冠状血管舒张剂或大脑血管舒张剂的。

5. 发明公开

CN1038639A 旋光的萘并硫氮杂类的制备方法无效
公开(公告)号：CN1038639A
公开(公告)日：1990-01-10
申请号：CN89103605.9
申请日：1989-05-23
申请人：霍夫曼-拉罗奇有限公司
发明人：戴维·卢埃林·科芬 , 普拉迪普·巴尔克里什纳·马丹 , 艾伦·许瓦兹
IPC分类号： C07C323/63 , C07D281/10 , C07D303/32
CPC分类号： C07D281/08 , C07C319/20 , C07C2601/14 , C07D281/10 , C07C323/56
摘要：通过水解化合物(III)制备化合物(I)的方法，式中R1和R2各自独立地是氢，C1—4烷基，C1—4烷氧基，卤素，三氟甲基或硝基，或R1和R2和与它们相连的苯环一起成为萘，Ar是未取代的或由一至三个下述取代基取代的苯基，这些取代基是C1—4烷基、C1—4烷氧基和卤素。本发明方法制备的化合物(I)可和于制造式(II)的硫氮杂-4(5H)-酮及其类似物，它们具有钙通道阻断剂活性，因此可作为降血压药和治疗局部缺血药。

6. 发明授权

US4652561A Naphtho[1,2-b]-1,4-thiazepinones 失效
标题翻译：萘并[1,2-b] -1,4-噻二酮
公开(公告)号：US4652561A
公开(公告)日：1987-03-24
申请号：US834178
申请日：1986-02-26
申请人： Erno Mohacsi , Jay P. O'Brien
发明人： Erno Mohacsi , Jay P. O'Brien
IPC分类号： C07D281/10 , A61K31/55 , A61K31/554 , A61P3/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D281/08 , C07D281/02
CPC分类号： C07D281/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups or 1 to 3 halogens; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.
摘要翻译：式Ⅰ的化合物，其中R1是被1〜3个低级烷氧基或1〜3个卤素取代的苯基; R2是羟基，低级烷氧基，低级烷酰氧基，低级环烷基羰氧基; R3和R4独立地是低级烷基，苯基低级烷基或一起形成哌啶或吡咯烷环; n为2〜4; m为1〜2; 或其药学上可接受的酸加成盐。式I的化合物具有作为钙通道阻断剂的活性，因此可用作降低血压的药剂和作为治疗缺血的药剂。

7. 发明授权

EP0683773B1 HYPOLIPIDAEMIC CONDENSED 1,4-THIAZEPINES 失效
标题翻译：降血脂，浓缩1,4-硫氮杂
公开(公告)号：EP0683773B1
公开(公告)日：1997-09-17
申请号：EP94906323.4
申请日：1994-02-15
申请人： THE WELLCOME FOUNDATION LIMITED
发明人： BRIEADDY, Lawrence, Edward , HODGSON, Gordon, Lewis, Jr.
IPC分类号： C07D281/10 , C07D281/08 , C07D417/04 , C07D513/04 , A61K31/55
CPC分类号： C07D417/04 , C07D281/08 , C07D281/10 , C07D513/04
摘要： The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R1 is hydrogen or C¿1-6?alkyl; R?2¿ is an atom or group selected from hydrogen, C¿1-6?alkyl (including cycloalkyl and cycloalkylalkyl), C1-4alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R?3¿ is hydrogen, OH, C¿1-6?alkyl, C1-6alkoxy or -OC1-6acyl; R?4¿ is a group independently selected from C¿1-6?alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl, and C2-6alkynyl which groups are optionally substituted; R?5¿ is a group independently selected from C¿2-6?alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl and C2-6alkynyl, which groups are optionally substituted; or R?4 and R5¿, together with the carbon atom to which they are attached, form a C¿3-7?spiro cycloalkyl group which is optionally substituted; R?6 and R7¿ are independently selected from hydrogen and C¿1-6?alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds.

8. 发明申请

US20180208589A1 LMP7 INHIBITORS 审中-公开
公开(公告)号：US20180208589A1
公开(公告)日：2018-07-26
申请号：US15320155
申请日：2015-06-18
申请人： PRINCIPIA BIOPHARMA INC.
发明人： Timothy Owens , Kenneth Albert Brameld
IPC分类号： C07D417/12 , C07D261/14 , C07C237/20 , C07D249/08 , C07D413/12 , C07D277/34
CPC分类号： C07D417/12 , C07C237/20 , C07D249/08 , C07D261/14 , C07D277/24 , C07D277/32 , C07D277/34 , C07D281/08 , C07D413/12
摘要： The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

9. 发明申请

US20070244087A1 2-ALKOXY-3,4,5-TRIHYDROXY-ALKYLAMIDES, PREPARATION THEREOF, COMPOSITIONS CONTAINING THEM AND USE THEREOF 失效
标题翻译： 2-烷氧基-3,4,5-三羟基烷基亚胺，其制备方法，包含它们的组合物及其用途
公开(公告)号：US20070244087A1
公开(公告)日：2007-10-18
申请号：US11753160
申请日：2007-05-24
申请人： Jidong ZHANG , Neerja BHATNAGAR , Jean-Marie RUXER
发明人： Jidong ZHANG , Neerja BHATNAGAR , Jean-Marie RUXER
IPC分类号： A61K31/554 , A61K31/553 , A61K31/5513 , A61K31/4704 , A61K31/397
CPC分类号： C07D223/12 , C07D205/085 , C07D207/273 , C07D207/277 , C07D211/76 , C07D215/38 , C07D223/16 , C07D243/08 , C07D281/06 , C07D281/08 , C07D417/06 , C07D471/04
摘要： The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
摘要翻译：本发明特别涉及2-烷氧基-3,4,5-三羟基 - 烷基酰胺，其制备方法，含有它们的组合物及其作为药物的用途，特别是作为抗癌剂。

10. 发明授权

US5817652A Hypolipidaemic condensed 1,4-thiazepines 失效
公开(公告)号：US5817652A
公开(公告)日：1998-10-06
申请号：US505232
申请日：1995-08-15
申请人： Lawrence Edward Brieaddy , Gordon Lewis Hodgson, Jr.
发明人： Lawrence Edward Brieaddy , Gordon Lewis Hodgson, Jr.
IPC分类号： A61K31/55 , A61K31/554 , A61P3/06 , A61P9/10 , C07D281/08 , C07D281/10 , C07D285/10 , C07D417/04 , C07D513/04
CPC分类号： C07D417/04 , C07D281/08 , C07D281/10 , C07D513/04
摘要： The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is an atom or group selected from hydrogen, C.sub.1-4 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-4 alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R.sup.3 is hydrogen, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or --O C.sub.1-6 acyl; R.sup.4 is a group independently selected from C.sub.1-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl, and C.sub.2-6 -alkynyl which groups are optionally substituted; R.sup.5 is a group independently selected from C.sub.2-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl and C.sub.2-6 alkynyl, which groups are optionally substituted; or R.sup.4 and R.sup.5, together with the carbon atom to which they are attached, form a C.sub.3-7 spiro cycloalkyl group which is optionally substituted; R.sup.6 and R.sup.7 are independently selected from hydrogen and C.sub.1-6 alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur, or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds. ##STR1##

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