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51.发明授权4-Hydroxy-2-benzimidazoline-thione compounds and pharmaceutical compositions containing them 失效4-羟基-2-苯并咪唑啉 - 硫酮化合物和含有它们的药物组合物
公开(公告)号：US4215134A
公开(公告)日：1980-07-29
申请号：US2129
申请日：1979-01-09
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , C07D235/02 , C07D235/28 , C07D303/22
CPC分类号： C07D235/02 , C07D235/28 , C07D303/22
摘要： Novel 4-hydroxy-2-benzimidazoline-thione compound of the formula: ##STR1## wherein R is lower alkyl;R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or lower straight-chained or branched alkyl orR.sub.1 and R.sub.2 together represent alkylene; andR.sub.3 is a hydrogen atom or an acyl radical;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译： 下式的新型4-羟基-2-苯并咪唑啉 - 硫酮化合物：其中R是低级烷基; R 1和R 2可以相同或不同，为氢或低级直链或支链烷基或R 1和R 2一起表示亚烷基; 并且R 3是氢原子或酰基; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。
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公开(公告)号：US07235574B2
公开(公告)日：2007-06-26
申请号：US11073227
申请日：2005-03-04
IPC分类号： A61K31/422 , C07D413/02
CPC分类号： C07D413/12 , C07D413/10
摘要： The present invention provides the compounds of formula I-A their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明提供式IA化合物其药学上可接受的盐或酯，对映异构体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法以及使用上述 控制或预防疾病如癌症的化合物。
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公开(公告)号：US07205325B2
公开(公告)日：2007-04-17
申请号：US10808935
申请日：2004-03-25
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Bernhard Goller , Matthias Rueth , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Bernhard Goller , Matthias Rueth , Edgar Voss
IPC分类号： A61K31/4192 , C07D249/04
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention 1 includes compounds of formula (I), and their pharmaceutically acceptable salts. These compounds are useful in the control or prevention of cancer.
摘要翻译： 本发明1包括式（I）的化合物，
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公开(公告)号：US07005526B2
公开(公告)日：2006-02-28
申请号：US11132082
申请日：2005-05-18
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
IPC分类号： C07D263/32 , C07D249/04 , A61K31/422 , A61K31/4192
CPC分类号： C07D413/12
摘要： Objects of the present invention are the compounds of formula (I) formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明的目的是式（I）式（I）的化合物，化学式id =“CHEM-US-00001”num =“000
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公开(公告)号：US20050222228A1
公开(公告)日：2005-10-06
申请号：US11096286
申请日：2005-03-31
IPC分类号： A61K31/422 , C07D413/14 , C07D413/02
CPC分类号： C07D413/14
摘要： The present invention provides compounds of formula (I): their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明提供式（I）化合物：其药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法以及上述用途 用于控制或预防癌症等疾病的化合物。
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公开(公告)号：US20050197370A1
公开(公告)日：2005-09-08
申请号：US11073227
申请日：2005-03-04
IPC分类号： C07D413/10 , C07D413/12 , A61K31/422 , C07D413/02
CPC分类号： C07D413/12 , C07D413/10
摘要： The present invention provides the compounds of formula I-A their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明提供式IA化合物其药学上可接受的盐或酯，对映异构体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法以及使用上述 控制或预防疾病如癌症的化合物。
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公开(公告)号：US06887864B2
公开(公告)日：2005-05-03
申请号：US10383111
申请日：2003-03-06
IPC分类号： A61K31/55 , A61P35/00 , A61P43/00 , C07D223/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/12 , C07D223/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.
摘要翻译： 本发明提供了根据通式（I）的新型氮杂环庚烷衍生物或其药学上可接受的盐，其中符号在说明书中定义，以及其制备方法。 根据本发明的化合物具有抗细胞增殖活性并显示出增加的血浆稳定性。
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公开(公告)号：US06506755B2
公开(公告)日：2003-01-14
申请号：US09767306
申请日：2001-01-23
IPC分类号： C07D27720
CPC分类号： C07D277/20 , C07D417/12 , C07D417/14
摘要： 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.
摘要翻译： 符号R1，R2，A，A1和A2具有在描述中给出的用于治疗癌症疾病的药物的含义的式Iin的5-亚芳基-4-氧代-2-硫代-3-噻唑烷羧酸。
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![Use of thiadiazolo[4,3-a]pyridine derivatives](/abs-image/US/2001/12/04/US06326378B1/abs.jpg.150x150.jpg)
公开(公告)号：US06326378B1
公开(公告)日：2001-12-04
申请号：US09622325
申请日：2000-10-05
IPC分类号： A61K31437
CPC分类号： A61K31/437
摘要： The present invention relates to the method of treating leukemia, lymphoma or inhibiting the proliferation of cells with a compound of formula I.
摘要翻译： 本发明涉及用式I化合物治疗白血病，淋巴瘤或抑制细胞增殖的方法。
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公开(公告)号：US6121322A
公开(公告)日：2000-09-19
申请号：US198722
申请日：1998-11-24
IPC分类号： C07D295/08 , A61K31/015 , A61K31/16 , A61K31/357 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/662 , A61P29/00 , C07C239/20 , C07C259/06 , C07C271/60 , C07D233/02 , C07D257/06 , C07D295/088 , C07D295/12 , C07D295/185 , C07D295/20 , C07D317/22 , C07D317/30 , C07F9/38 , C07F9/40 , A61K31/185 , C07C229/28
CPC分类号： C07D295/185 , C07C259/06 , C07C271/60 , C07D295/088 , C07D317/22 , C07F9/3808 , C07F9/4006 , C07C2102/30
摘要： The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.
摘要翻译： 本发明提供了通式I的新颖的薁衍生物，其中R 1至R 6具有本说明书给出的含义，以及它们的互变异构体，对映异构体，非对映异构体，外消旋物和生理上相容的盐或酯和物质，其在体内水解或代谢为化合物 本发明还涉及制备上述化合物的方法和中间体，含有这些化合物的药物组合物以及这些化合物在治疗炎性病症中的用途。
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