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1. 发明授权

US5972946A Acetamide derivative, process for preparing the same, and a pharmaceutical composition containing the same 失效
标题翻译：乙酰胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5972946A
公开(公告)日：1999-10-26
申请号：US930604
申请日：1997-10-14
申请人： Teruya Murata , Katsuhiko Hino , Kiyoshi Furukawa , Makoto Oka , Mari Itoh
发明人： Teruya Murata , Katsuhiko Hino , Kiyoshi Furukawa , Makoto Oka , Mari Itoh
IPC分类号： A61K31/505 , A61K31/506 , A61P25/08 , A61P37/02 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/90 , C07D239/91 , C07D239/94 , C07D403/12
CPC分类号： C07D239/42 , C07D239/34 , C07D239/36 , C07D239/91 , C07D239/94 , C07D403/12 , Y02P20/55
摘要： An acetamide derivative of the formula (I): ##STR1## wherein X is --0-- or --NR.sub.4 --, R.sub.1 is H, lower alkyl, lower alkenyl or cyclolalkyl-lower-alkyl, R.sub.2 is lower alkyl, cycloalkyl, substituted or unsubstituted phenyl, etc., R.sub.3 is H, lower alkyl or hydroxy-lower alkyl, R.sub.4 is H, lower alkyl, etc., R.sub.5 is H, lower alkyl, lower alkenyl, hydroxy-lower alkyl, etc., R.sub.6 is H, lower alkyl, CF.sub.3, substituted or unsubstituted phenyl, or R.sub.5 and R.sub.6 may optionally combine to form --(CH.sub.2)n--, R.sub.7 is H, halogen, lower alkyl, lower alkoxy, CF.sub.3, OH, NH.sub.2, etc., R.sub.8 is H, halogen, lower alkyl or lower alkoxy, or a pharmaceutically acceptable acid addition salt thereof. The compounds of the present invention selectively act on the peripheral-type BZ.omega..sub.3 -receptor, and show excellent pharmacological activities, and hence, they are useful in the prophylaxis or treatment of central nervous disorders such as anxiety-related diseases, depression, epilepsy, etc.
摘要翻译： PCT No.PCT / JP96 / 00977 Sec。 371日期1997年10月14日第 102（e）日期1997年10月14日PCT 1996年4月10日PCT PCT。公开号WO96 / 32383 日期：1996年10月17日一种式（I）的乙酰胺衍生物：其中X为-O-或-NR4-，R1为H，低级烷基，低级烯基或环烷基 - 低级烷基，R2为低级烷基，环烷基，或未取代的苯基等，R3为H，低级烷基或羟基 - 低级烷基，R4为H，低级烷基等，R5为H，低级烷基，低级烯基，羟基 - 低级烷基等，R6为H ，低级烷基，CF 3，取代或未取代的苯基，或R 5和R 6可以任选地结合形成 - （CH 2）n - ，R 7是H，卤素，低级烷基，低级烷氧基，CF 3，OH，NH 2等，R 8是 H，卤素，低级烷基或低级烷氧基，或其药学上可接受的酸加成盐。本发明化合物选择性地作用于外周型BZω-3受体，显示优异的药理活性，因此可用于预防或治疗焦虑相关疾病，抑郁症，癫痫等中枢神经疾病等等

2. 发明授权

US06372740B1 2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof 失效
标题翻译： 2-芳基-8-氧代二氢嘌呤衍生物，其制备方法，含有它们的药物组合物及其中间体
公开(公告)号：US06372740B1
公开(公告)日：2002-04-16
申请号：US09555490
申请日：2000-06-01
申请人： Teruya Murata , Kaoru Masumoto , Katsunori Kondo , Kiyoshi Furukawa , Makoto Oka
发明人： Teruya Murata , Kaoru Masumoto , Katsunori Kondo , Kiyoshi Furukawa , Makoto Oka
IPC分类号： C02D47300
CPC分类号： C07D473/00
摘要： 2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted phenyl; X is H, lower alkyl, cycloalkyl-lower alkyl, substituted or unsubstituted phenyl-lower alkyl, lower alkenyl, carbamoyl, di-lower alkylcarbamoyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); Y is H, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, lower alkenyl, substituted or unsubstituted phenyl-lower alkyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); A is substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; provided that when one of X and Y of the above formula (I) is the group of the formula (Q), then the other is the same groups for X or Y as described above except for the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof. These compounds are useful for the prophylaxis or treatment of central nervous disorders such as anxiety-related diseases (neurosis, somatoform disorders, anxiety disorders, and others), depression, epilepsy, etc., or circulatory organs disorders such as angina pectoris, hypertension.
摘要翻译：下式（I）的2-芳基-8-氧代二氢嘌呤衍生物：其中W是H，低级烷基，卤素，低级烷氧基，氨基，一或二低级烷基氨基或取代或未取代的苯基; X为H，低级烷基，环烷基 - 低级烷基，取代或未取代的苯基 - 低级烷基，低级烯基，氨基甲酰基，二低级烷基氨基甲酰基或式（Q）基团：-CH（R3）CON（R1） R2）; Y为H，低级烷基，环烷基，环烷基 - 低级烷基，低级烯基，取代或未取代的苯基 - 低级烷基或式（Q）基团：-CH（R3）CON（R1）（R2） A是取代或未取代的苯基，或取代或未取代的杂芳基; 条件是当上述式（I）的X和Y之一是式（Q）的基团时，另一个是与上述相同的X或Y基团，除了式（Q），或其药学上可接受的酸加成盐。这些化合物可用于预防或治疗诸如焦虑相关疾病（神经症，躯体形式障碍，焦虑障碍等），抑郁症，癫痫等中枢神经障碍或循环器官疾病如心绞痛，高血压。

3. 发明授权

US06620817B1 [5-CHLORO-6-PHENYL-2-(4-TRIFLUOROMETHYLPHENYL)-4-PYRIMIDINYLAMINO]ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATE OF THESE COMPOUNDS 失效
标题翻译： [5-氯代-2-（4-三氟甲基苯基）-4-嘧啶基]氨基]乙酰胺衍生物，其制备方法，含有该化合物的药物组合物和这些化合物的中间体
公开(公告)号：US06620817B1
公开(公告)日：2003-09-16
申请号：US10130151
申请日：2002-05-13
申请人： Teruya Murata , Kazunori Ohno , Masayasu Tanaka , Mari Itoh
发明人： Teruya Murata , Kazunori Ohno , Masayasu Tanaka , Mari Itoh
IPC分类号： C07D23942
CPC分类号： C07D239/42
摘要： A [5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4-pyrimidinyl-amino]acetamide derivative of the formula (I): wherein R1 is a methyl group or a cyclopropyl group, and a pharmaceutical composition containing the same. Said compounds exhibit a potent anti-rheumatoid activity and show low toxicity, and hence, they are useful as an agent for prophylaxis or treatment of immuno inflammatory diseases such as rheumatoid diseases (e.g., rheumatoid arthritis, Behcet disease, ankylosing spondylitis, etc.) and autoimmune diseases (e.g., multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, etc.).
摘要翻译：式（I）的[5-氯-6-苯基-2-（4-三氟甲基苯基）-4-嘧啶基 - 氨基]乙酰胺衍生物：其中R1是甲基或环丙基，以及含有相同。所述化合物显示出有效的抗类风湿活性并显示低毒性，因此它们可用作预防或治疗免疫炎性疾病如类风湿病（例如类风湿性关节炎，白塞病，强直性脊柱炎等）和自身免疫性疾病（例如，多发性硬化，系统性红斑狼疮，Sjögren综合征等）。

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