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1. 发明授权

US5679673A Aralkyl bridged diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基桥连二氮杂双环烷烃衍生物
公开(公告)号：US5679673A
公开(公告)日：1997-10-21
申请号：US344304
申请日：1994-11-21
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D453/02 , C07D487/08 , A61K31/55 , C07D471/08
CPC分类号： C07D487/08 , C07D453/02
摘要： Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.9 is selected from hydrido, loweralkyl, benzyl and haloloweralkyl; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothiophenyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中R，R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R10至R13各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中R8和R9各自选自氢，低级烷基，苄基和卤代低级烷基; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

2. 发明授权

US5430169A Method for preparation of sphingoid bases 失效
标题翻译：鞘氨醇碱的制备方法
公开(公告)号：US5430169A
公开(公告)日：1995-07-04
申请号：US195815
申请日：1994-02-14
申请人： Ahcene Boumendjel , Stephen P. F. Miller
发明人： Ahcene Boumendjel , Stephen P. F. Miller
IPC分类号： C07F9/09 , C07F9/113
CPC分类号： C07F9/091 , C07F9/113
摘要： The present invention provides a series of non-toxic compounds which function to inhibit the activity of S-1-P aldolase in respect to its cleavage of S-1-P. These inhibitors are described by the compounds of formula I ##STR1## wherein R is a radical containing 1 to 15 carbon atoms, a halogen, or hydrocarbon, R' is an organic radical or hydrogen, and R" is --NH.sub.3.sup.+ or --NH--NH .sup.+, with the proviso that, when R is CH.sub.3 (CH).sub.12 (CH.dbd.CH) and R' is hydrogen, R" is --NH--NH.sub.3.sup.+.A method for preparing such compounds, which may generally be described as 1-phosphate derivatives of compounds which include a 2-amino-1,3-alcohol radical is also disclosed.
摘要翻译：本发明提供一系列无毒化合物，其功能是抑制S-1-P醛缩酶在其切割S-1-P时的活性。这些抑制剂由式I化合物（I）描述，其中R是含有1至15个碳原子的基团，卤素或烃，R'是有机基团或氢，R“是-NH 3 + 或-NH-NH +，条件是当R为CH 3（CH）12（CH = CH）且R'为氢时，R“为-NH-NH 3 +。还公开了制备这种化合物的方法，其通常可以被描述为包括2-氨基-1,3-醇基的化合物的1-磷酸酯衍生物。

3. 发明授权

US07175838B2 Use of a promoter of T-cell expansion and an inducer of CD40 stimulation in the treatment or prevention of a pathologic state 有权
标题翻译：使用T细胞扩增启动子和CD40刺激诱导剂治疗或预防病理状态
公开(公告)号：US07175838B2
公开(公告)日：2007-02-13
申请号：US10226959
申请日：2002-08-23
申请人： William J. Murphy , Robert Wiltrout , Bruce Blazar , Susan E. Wilson
发明人： William J. Murphy , Robert Wiltrout , Bruce Blazar , Susan E. Wilson
IPC分类号： A61K39/395 , A61K38/20
CPC分类号： A61K38/2013 , A61K39/395 , A61K2039/505 , A61K2300/00
摘要： The invention provides a method of treating or preventing a pathologic state in a mammal. The method comprises administering to the mammal a promoter of T-cell expansion and an inducer of CD40 stimulation, wherein CD40 is stimulated on cells of the immune system. The promoter of T-cell expansion and inducer of CD40 stimulation are administered in synergistically effective amounts to treat or prevent the pathologic state in the mammal. The invention also provides a method of assessing the effectiveness of treatment of a pathologic state in a mammal, wherein the mammal has been administered a promoter of T-cell expansion and an inducer of CD40 stimulation, wherein CD40 is stimulated on cells of the immune system. The method comprises measuring the level of at least one antibody in a test sample obtained from the mammal, which at least one antibody is specific for an antigen that is known to be associated with the pathologic state, and wherein the level of the at least one antibody is indicative of the effectiveness of treatment of the pathologic state in the mammal.
摘要翻译：本发明提供了治疗或预防哺乳动物病理状态的方法。所述方法包括向哺乳动物施用T细胞扩增的启动子和CD40刺激的诱导物，其中CD40在免疫系统的细胞上被刺激。以协同有效量施用T细胞扩增的启动子和CD40刺激诱导物，以治疗或预防哺乳动物的病理状态。本发明还提供了评估哺乳动物病理状态治疗有效性的方法，其中哺乳动物已经给予T细胞扩增启动子和CD40刺激诱导剂，其中CD40在免疫系统的细胞上被刺激。该方法包括测量从哺乳动物获得的测试样品中至少一种抗体的水平，至少一种抗体对于已知与病理状态相关的抗原是特异性的，并且其中至少一种抗体指示治疗哺乳动物病理状态的有效性。

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