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1.发明公开MEDICINES FOR THE PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISEASES 审中-公开EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN EN
公开(公告)号：EP1295883A1
公开(公告)日：2003-03-26
申请号：EP01936958.6
申请日：2001-06-12
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/444 , A61P25/00 , A61P25/28 , A61P25/18
CPC分类号： C07D471/04 , A61K31/4375 , A61K31/444
摘要： Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of neurodegeneration due to hypofunction of glutamic acid receptor and which contain as an active ingredient 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives of the formula (I):
wherein Het is oxadiazolyl; R 1 is hydrogen, lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, etc.; and R 2 is hydrogen, lower alkyl, cyclo-lower alkyl, substituted or unsubstituted aryl, etc., or physiologically acceptable acid addition salts thereof.摘要翻译： 通过延迟或抑制谷氨酸受体功能低下的神经退行性疾病，预防和治疗神经变性疾病如阿尔茨海默氏病和哺乳动物（包括人类）的精神分裂症药物，并含有作为活性成分的5-取代-3-恶二唑基 （I）的-1,6-萘啶-2（1H） - 酮衍生物：其中Het是恶二唑基; R 1是氢，低级烷基，环低级烷基，低级烯基，低级烷氧基，取代或未取代的芳基，取代或未取代的杂芳基等; R 2为氢，低级烷基，环低级烷基，取代或未取代的芳基等，或其生理上可接受的酸加成盐。
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2.发明授权2-ARYL-8-OXODIHYDROPURINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME, AND INTERMEDIATES THEREOF 有权2-芳基-8-氧代二氢嘌呤衍生物，其制备方法，它们作为药物成分和其中间体使用
公开(公告)号：EP1036794B1
公开(公告)日：2003-08-27
申请号：EP98955937.2
申请日：1998-11-26
IPC分类号： C07D473/00 , A61K31/52
CPC分类号： C07D473/00
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3.发明授权ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效乙酰胺衍生物，PROCESS其医疗和化合物含有这种
公开(公告)号：EP0826673B1
公开(公告)日：2002-11-20
申请号：EP96909327.7
申请日：1996-04-10
发明人： MURATA, Teruya , HINO, Katsuhiko , FURUKAWA, Kiyoshi , OKA, Makoto , ITOH, Mari
IPC分类号： C07D239/34 , C07D239/42 , A61K31/505 , C07D239/70 , C07D239/91 , C07D239/94 , C07D403/12 , C07D405/12 , C07D401/12 , C07D401/04 , C07D403/14
CPC分类号： C07D239/42 , C07D239/34 , C07D239/36 , C07D239/91 , C07D239/94 , C07D403/12 , Y02P20/55
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4.发明公开ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME 失效乙酰胺衍生物，PROCESS其医疗和化合物含有这种
公开(公告)号：EP0826673A1
公开(公告)日：1998-03-04
申请号：EP96909327.7
申请日：1996-04-10
发明人： MURATA, Teruya , HINO, Katsuhiko , FURUKAWA, Kiyoshi , OKA, Makoto , ITOH, Mari
IPC分类号： C07D239/34 , C07D239/42 , A61K31/505
CPC分类号： C07D239/42 , C07D239/34 , C07D239/36 , C07D239/91 , C07D239/94 , C07D403/12 , Y02P20/55
摘要： Acetamide derivatives represented by general formula (I) and physiologically acceptable acid-addition salts thereof, wherein X represents -O- or -NR 4 ; R 1 represents H, lower alkyl, lower alkenyl or cycloalkyl(lower)alkyl; R 2 represents lower alkyl, cycloalkyl, optionally substituted phenyl, etc.; R 3 represents H, lower alkyl or hydroxy(lower)alkyl; R 4 represents H, lower alkyl, etc.; R 5 represents H, lower alkyl, lower alkenyl, hydroxy(lower)alkyl, etc.; R 6 represents H, lower alkyl, CF 3 or optionally substituted phenyl, or R 5 and R 6 together form -(CH 2 ) n -; R 7 represents H, halogeno, lower alkyl, lower alkoxy, CF 3 , OH, NH 2 , etc.; and R 8 represents H, halogeno, lower alkyl or lower alkoxy. The compounds act selectively on the peripheral BZ ω3 receptor and exhibit excellent pharmocological effects, which makes them useful as a remedy and preventive for central diseases, for example, diseases associated with anxiety, depression and epilepsy, etc.
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5.发明授权5-SUBSTITUTED-3-OXADIAZOLYL-1,6-NAPHTHYRIDIN-2(1H)-ONE DERIVATIVES 失效IN 5-取代的3-恶二唑基-1,6-萘啶-2（1H） - 酮衍生物
公开(公告)号：EP1010699B1
公开(公告)日：2005-06-15
申请号：EP98931076.8
申请日：1998-07-14
发明人： OHNO, Kazunori , ODAI, Osamu , MASUMOTO, Kaoru , FURUKAWA, Kiyoshi , OKA, Makoto
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Novel 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives represented by general formula (I) wherein Het represents oxadiazolyl; R1 represents H, lower alkyl, lower cycloalkyl, lower alkenyl, lower alkoxy, optionally substituted aryl, optionally substituted heteroaryl, etc.; and R2 represents H, lower alkyl, lower cycloalkyl, optionally substituted aryl, etc. Because of having high affinities selectively with benzodiazepine receptors, these compounds are useful as benzodiazepine receptor agonists, in particular, inverse agonists thereof, for example, brain activators and remedies for memory disorders associating senile dementia, Alzheimer's disease, etc.
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6.发明公开2-ARYL-8-OXODIHYDROPURINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME, AND INTERMEDIATES THEREOF 有权2-ARYL-8-OXODIHYDROPURIN-DERIVATE，IHRE HERSTELLUNG，IHRE VERWENDUNG ALS MEDIKAMENTENKOMPONENTE UND DEREN INTERMEDIATE
公开(公告)号：EP1036794A1
公开(公告)日：2000-09-20
申请号：EP98955937.2
申请日：1998-11-26
IPC分类号： C07D473/00 , A61K31/52
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(R 3 )CON(R 1 )(R 2 ); 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(R 3 )CON(R 1 )(R 2 ); 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为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的CHEM; X是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）的基团：-CH（R 3）CON [R <1>）（R <2>）; Y是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）的基团：-CH（R 3）CON（R 1） （R <2>）; 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中枢神经障碍如焦虑相关疾病（神经症，躯体形式障碍，焦虑障碍等），抑郁症，癫痫等，或循环器官疾病如心绞痛，高血压。
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7.发明公开DEMENTIA REMEDIES CONTAINING 2-ARYL-8-OXODIHYDROPURINE DERIVATIVES AS THE ACTIVE INGREDIENT 审中-公开补救治疗痴呆2-芳氧代二氢嘌呤衍生物为有效ACTIVE CONTAIN
公开(公告)号：EP1306378A1
公开(公告)日：2003-05-02
申请号：EP01951985.9
申请日：2001-07-24
IPC分类号： C07D473/00 , A61K31/522 , A61P25/28
CPC分类号： A61K31/522 , C07D473/00
摘要： Medicines for treatment or prevention of dementia comprising 2-aryl-8-oxodihydropurine derivatives of the formula (I):
wherein W is H, C 1-6 alkyl, halogen, C 1-6 alkoxy, or the like; X is H, C 1-6 alkyl, a group of the formula (Q):-CH(R 3 )CON(R 1 )(R 2 )(wherein R 1 is a C 1-6 alkyl or the like; R 2 is phenyl-substituted C 1-4 alkyl or the like; and R 3 is H or the like); Y is H, C 1-6 alkyl, a group of the above formula (Q), or the like; and A is substituted phenyl or the like, with the proviso that one of X and Y is a group of the formula (Q) and the other is a group selected from those defined for X or Y except the groups (Q), or pharmaceutically acceptable acid addition salts thereof. The above compounds exhibit an extremely potent ameliorating effect on learning disorder and/or dymnesia and thus are useful in the treatment or prevention of Alzheimer-type dementia, cerebrovascular dementia, senile dementia, etc.-
8.发明公开5-SUBSTITUTED-3-OXADIAZOLYL-1,6-NAPHTHYRIDIN-2(1H)-ONE DERIVATIVES 失效5-STELLUNG SUBSTITUIERTE 3-OXADIAZOLYL-1,6-NAPHTHYRIDIN-2（1H）-ON-DERIVATE
公开(公告)号：EP1010699A1
公开(公告)日：2000-06-21
申请号：EP98931076.8
申请日：1998-07-14
发明人： OHNO, Kazunori , ODAI, Osamu , MASUMOTO, Kaoru , FURUKAWA, Kiyoshi , OKA, Makoto
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： A 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivative of the formula (I):
wherein Het is oxadiazolyl, R 1 is H, lower alkyl, cyclo-lower alkyl, trifluoromethyl, lower alkenyl, lower alkynyl, lower alkoxy, lower alkoxy-lower alkyl, hydroxy-lower alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, and R 2 is H, lower alkyl, cyclo-lower alkyl, cyclo-lower alkylmethyl, lower alkenyl, cyclo-lower alkenyl, lower alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, or a pharmaceutically acceptable acid addition salt thereof, which has high selective affinity to benzodiazepine receptor and is useful particularly as a benzodiazepine inverse agonist, for example, as psychoanaleptic drug or a drug for the treatment of dysmnesia in senile dementia or Alzheimer's disease.摘要翻译： 式（I）的5-取代-3-恶二唑基-1,6-二氮杂萘-2（1H） - 酮衍生物：其中Het是恶二唑基，R 1是H，低级烷基，环低级 烷基，三氟甲基，低级烯基，低级炔基，低级烷氧基，低级烷氧基 - 低级烷基，羟基 - 低级烷基，取代或未取代的芳基，或取代或未取代的杂芳基，R 2是H，低级烷基， 烷基，环低级烷基甲基，低级烯基，环低级烯基，低级炔基，取代或未取代的芳基或取代或未取代的杂芳族基团或其药学上可接受的酸加成盐，其对苯并二氮杂受体具有高选择性亲和力，并且是有用的 特别是作为苯二氮卓类反向激动剂，例如精神无菌药物或用于治疗老年痴呆或阿尔茨海默氏症中的失眠症的药物。
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