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1. 发明授权

US07517888B2 A1 adenosine receptor antagonists 有权
标题翻译： A1腺苷受体拮抗剂
公开(公告)号：US07517888B2
公开(公告)日：2009-04-14
申请号：US11119305
申请日：2005-04-28
申请人： Gloria Cristalli
发明人： Gloria Cristalli
IPC分类号： C07D473/34 , A61K31/52 , A61P13/12
CPC分类号： C07D473/34
摘要： Disclosed are A1 adenosine receptor antagonists having the general formula The compounds are useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.
摘要翻译：公开了具有通式的A1腺苷受体拮抗剂。该化合物可用于治疗各种疾病状态，特别是利尿剂治疗适合的疾病状态。

2. 发明授权

US07163928B2 Partial and full agonists of A1 adenosine receptors 有权
标题翻译： A1腺苷受体的部分和全部激动剂
公开(公告)号：US07163928B2
公开(公告)日：2007-01-16
申请号：US10770542
申请日：2004-02-02
申请人： Gloria Cristalli , Venkata Palle , Jeff Zablocki
发明人： Gloria Cristalli , Venkata Palle , Jeff Zablocki
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/22 , C07H19/167
CPC分类号： C07D473/00
摘要： Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.
摘要翻译：公开了可用于治疗各种疾病状态，特别是心动过速和心房扑动，心绞痛和心肌梗死的部分和全部A 1 N 2腺苷受体激动剂的新化合物。

3. 发明授权

US5593975A Adenosine derivatives having A.sub.2 agonist activity 失效
标题翻译：具有A2激动剂活性的腺苷衍生物
公开(公告)号：US5593975A
公开(公告)日：1997-01-14
申请号：US325201
申请日：1995-01-30
申请人： Gloria Cristalli
发明人： Gloria Cristalli
IPC分类号： C07H19/19 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/08 , A61P25/20 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16
摘要： Adenosine A.sub.2 agonists of the formula ##STR1## wherein R is hydrogen, alkyl, cycloalkyl or phenylalkyl;R.sub.1 is selected from the group consisting ofa) optionally substituted phenyl or naphthyl;b) --(CH.sub.2).sub.m --Het wherein m is 0-3 and Het is a 5 or 6 membered heterocyclic aromatic or non-aromatic ring, optionally benzocondensed;c) cycloalkyl optionally containing unsaturations or alkenyl; and ##STR2## wherein n is 0-4; R.sub.2 is hydrogen, methyl or phenyl;R.sub.5 is hydrogen, alkyl, cycloalkyl, cycloalkenyl or phenylalkyl; or R.sub.2 and R.sub.5 form a 5 or 6-membered carbocyclic ring; or R.sub.5 is hydrogen and R.sub.2 and R.sub.4 form an oxo group or a corresponding acetalic derivative;R.sub.4 is OH, NH.sub.2, dialkylamino, halogen or cyano; andR.sub.3 is alkyl, cycloalkyl, phenyl or benzyl; provided that when R is different from hydrogen or when R is hydrogen and R.sub.3 is phenyl or benzyl, R.sub.1 can also be alkyl, useful in the treatment of cardiovascular pathologies and nervous system diseases, a process for the preparation thereof and pharmaceutical compositions containing them are disclosed.
摘要翻译： PCT No.PCT / EP93 / 00972 Sec。 371日期1995年1月30日 102（e）日期1995年1月30日PCT 1993年4月21日PCT PCT。公开号WO93 / 22328 日期：11月11日，具有式（IMAGE）的腺苷A2激动剂，其中R是氢，烷基，环烷基或苯基烷基; R1选自a）任选取代的苯基或萘基; b） - （CH 2）m -Het，其中m为0-3，Het为5或6元杂环芳族或非芳香环，任选苯并稠合; c）任选地含有不饱和键或烯基的环烷基; 乙基或苯基; R5是氢，烷基，环烷基，环烯基或苯基烷基; 或R 2和R 5形成5或6元碳环; 或R5是氢，R2和R4形成氧代基或相应的缩醛衍生物; R4是OH，NH2，二烷基氨基，卤素或氰基; 和R3是烷基，环烷基，苯基或苄基; 条件是当R不同于氢时，或当R为氢且R3为苯基或苄基时，R1也可为烷基，可用于治疗心血管病变和神经系统疾病，其制备方法和含有它们的药物组合物为披露

4. 发明授权

US07189730B2 A2A adenosine receptor antagonists 失效
标题翻译： A2A腺苷受体拮抗剂
公开(公告)号：US07189730B2
公开(公告)日：2007-03-13
申请号：US10322985
申请日：2002-12-18
申请人： Gloria Cristalli
发明人： Gloria Cristalli
IPC分类号： C07D473/40 , C07D473/16 , C07D473/24 , C07D31/52 , C07D31/522
CPC分类号： C07D217/18 , C07D473/16 , C07D473/18 , C07D473/24
摘要： Disclosed are novel A2A adenosine receptor antagonists of the formula: wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is optionally substituted lower alkyl or optionally substituted cycloalkyl; R3 is hydrogen, halogen, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl; X is —O—, —S—, or —NH—; and Y is optionally substituted alkylene; and the pharmaceutically acceptable salts thereof; which are useful for treating various disease states, for example cardiovascular disorders, including tissue damage due to ischemia, CNS diseases, including Parkinson's disease, depression, and the like.
摘要翻译：公开了下式的新型A 2A腺苷受体拮抗剂：其中：R 1是任选取代的芳基或任选取代的杂芳基; R 2是任选取代的低级烷基或任选取代的环烷基; R 3是氢，卤素，任选取代的烷氧基，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基; X是-O - ， - S-或-NH-; Y是任选取代的亚烷基; 及其药学上可接受的盐; 其可用于治疗各种疾病状态，例如心血管疾病，包括由缺血引起的组织损伤，CNS疾病，包括帕金森病，抑郁症等。

5. 发明申请

US20050245546A1 A1 adenosine receptor antagonists 有权
标题翻译： A1腺苷受体拮抗剂
公开(公告)号：US20050245546A1
公开(公告)日：2005-11-03
申请号：US11119305
申请日：2005-04-28
申请人： Gloria Cristalli
发明人： Gloria Cristalli
IPC分类号： A61K31/52 , C07D473/12 , C07D473/34
CPC分类号： C07D473/34
摘要： Disclosed are A1adenosine receptor antagonists, useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.
摘要翻译：公开了用于治疗各种疾病状态，特别是利尿剂治疗适合的疾病状态的A 1 N 2腺苷受体拮抗剂。

6. 发明授权

US06914053B2 Adenosine A3 receptor agonists 失效
标题翻译：腺苷A3受体激动剂
公开(公告)号：US06914053B2
公开(公告)日：2005-07-05
申请号：US10657762
申请日：2003-09-08
申请人： Gloria Cristalli
发明人： Gloria Cristalli
IPC分类号： A61K31/70 , A61K31/7076 , A61P25/00 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16
摘要： Disclosed are novel adenosine A3 receptor agonists of Formula I: wherein: R is hydrogen or lower alkyl; R1 is optionally substituted lower alkoxy or optionally substituted cycloalkyloxy; R2 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted trialkylsilyl; and R3 is hydroxymethyl or R4R5NC(Q)—; in which R4 and R5 are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl.
摘要翻译：公开了式I的新型腺苷A 3 N 3受体激动剂：其中：R是氢或低级烷基; R 1是任选取代的低级烷氧基或任选取代的环烷氧基; R 2是氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基，任选取代的杂芳基或任选取代的三烷基甲硅烷基; 和R 3是羟甲基或R 4 R 5 NC（Q） - ; 其中R 4和R 5是氢，任选取代的烷基，任选取代的环烷基，任选取代的杂环基，任选取代的芳基或任选取代的杂芳基。

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