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    Intermediates for 5-substituted-3-oxadiazolyl-1,6-Naphthyridin-2(1H)-one derivatives
    1.
    发明授权
    Intermediates for 5-substituted-3-oxadiazolyl-1,6-Naphthyridin-2(1H)-one derivatives 失效
    5-取代-3-恶二唑基-1,6-萘啶-2（1H） - 酮衍生物的中间体

    公开(公告)号：US06277993B1

    公开(公告)日：2001-08-21

    申请号：US09654782

    申请日：2000-09-01

    申请人： Kazunori Ohno ,  Osamu Odai ,  Kaoru Masumoto ,  Kiyoshi Furukawa ,  Makoto Oka

    发明人： Kazunori Ohno ,  Osamu Odai ,  Kaoru Masumoto ,  Kiyoshi Furukawa ,  Makoto Oka

    IPC分类号： C07D47104

    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, R1 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 R2 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 hetero-aromatic 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，R2是H，低级烷基，环低级烷基，环低级烷基甲基， ，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，并且特别用作苯二氮卓反相激动剂， 例如，作为精神无菌药物或用于治疗老年痴呆或阿尔茨海默病的失聪症的药物。

    5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives
    2.
    发明授权
    5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives 失效
    5-取代-3-恶二唑基-1,6-二氮杂萘-2（1H） - 酮衍生物

    公开(公告)号：US06172079B2

    公开(公告)日：2001-01-09

    申请号：US09462412

    申请日：2000-01-10

    申请人： Kazunori Ohno ,  Osamu Odai ,  Kaoru Masumoto ,  Kiyoshi Furukawa ,  Makoto Oka

    发明人： Kazunori Ohno ,  Osamu Odai ,  Kaoru Masumoto ,  Kiyoshi Furukawa ,  Makoto Oka

    IPC分类号： A61K31435

    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, R1 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 R2 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，R2是H，低级烷基，环低级烷基，环低级烷基甲基， ，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，并且特别用作苯二氮卓反相激动剂，例如 作为精神无菌药物或用于治疗老年痴呆或阿尔茨海默氏症的失聪症的药物。

    Production on 3-oxadiazolyl-1,6-naphthyridine derivatives
    3.
    发明授权
    Production on 3-oxadiazolyl-1,6-naphthyridine derivatives 失效
    3-恶二唑基-1,6-二氮杂萘衍生物的制备

    公开(公告)号：US5424434A

    公开(公告)日：1995-06-13

    申请号：US260835

    申请日：1994-06-16

    申请人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    发明人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    IPC分类号： A61K31/4245 ,  A61K31/435 ,  A61K31/4375 ,  C07D271/02 ,  C07D271/06 ,  C07D271/10 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： 3-Oxadiazolyl-5,6,7,8-tetrahydro-1,6-naphthyridine derivative of the formula (I): ##STR1## wherein Het is an oxadiazole ring, R.sub.1 is hydrogen atom, an acyl group, a lower alkyl group or a group of the formula: --CH.sub.2 R.sub.1 ' (in which R.sub.1 ' is a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, benzyl group, aryl group or a heteroaromatic group), R.sub.2 is a lower alkyl group, a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, aryl group, a heteroaromatic group, a halogeno-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkoxy group, a lower alkenyloxy group, a phenoxy group or a lower alkylthio group, or a pharmaceutically acceptable acid addition salt thereof, which are useful as benzodiazepine receptor agonist.

    摘要翻译： 式（I）的3-恶二唑基-5,6,7,8-四氢-1,6-萘啶衍生物：其中Het是恶二唑环，R 1是氢原子，酰基， 低级烷基或式-CH 2 R 1'（其中R 1'为环低级烷基，低级烯基，低级炔基，苄基，芳基或杂芳族基团）的基团，R 2为 低级烷基，低级烷基，低级烯基，低级炔基，芳基，杂芳基，卤代低级烷基，低级烷氧基 - 低级烷基，低级烷氧基，低级烷基 烯氧基，苯氧基或低级烷硫基，或其药学上可接受的酸加成盐，可用作苯并二氮杂受体激动剂。

    3-oxadiazolyl-1,6-naphthyridine derivatives
    4.
    发明授权
    3-oxadiazolyl-1,6-naphthyridine derivatives 失效
    3-恶二唑基-1,6-二氮杂萘衍生物

    公开(公告)号：US5367078A

    公开(公告)日：1994-11-22

    申请号：US112660

    申请日：1993-08-27

    申请人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    发明人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    IPC分类号： A61K31/4245 ,  A61K31/435 ,  A61K31/4375 ,  C07D271/02 ,  C07D271/06 ,  C07D271/10 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： 3-Oxadiazolyl-5,6,7,8-tetrahydro-1,6-naphthyridine derivative of the formula (I): ##STR1## wherein Het is an oxadiazole ring, R.sub.1 is hydrogen atom, an acyl group, a lower alkyl group or a group of the formula: --CH.sub.2 R.sub.1 ' (in which R.sub.1 ' is a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, benzyl group, aryl group or a heteroaromatic groups), R.sub.2 is a lower alkyl group, a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, aryl group, a heteroaromatic group, a halogeno-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkoxy group, a lower alkenyloxy group, a phenoxy group, or a lower alkylthio group, or a pharmaceutically acceptable acid addition salt thereof, which are useful as benzodiazedine receptor agonist.

    摘要翻译： 式（I）的3-恶二唑基-5,6,7,8-四氢-1,6-萘啶衍生物：其中Het是恶二唑环，R 1是氢原子，酰基， 低级烷基或式-CH 2 R 1'（其中R 1'为环低级烷基，低级烯基，低级炔基，苄基，芳基或杂芳族基团）的基团，R 2为 低级烷基，低级烷基，低级烯基，低级炔基，芳基，杂芳基，卤代低级烷基，低级烷氧基 - 低级烷基，低级烷氧基，低级烷基 烯氧基，苯氧基或低级烷硫基，或其药学上可接受的酸加成盐，其可用作苯并二嗪二受体激动剂。

    Intermediates for 3-oxadiazoly-1,6-naphthyridine derivatives
    5.
    发明授权
    Intermediates for 3-oxadiazoly-1,6-naphthyridine derivatives 失效
    3-恶二唑-1,6-二氮杂萘衍生物的中间体

    公开(公告)号：US5424433A

    公开(公告)日：1995-06-13

    申请号：US260800

    申请日：1994-06-16

    申请人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    发明人： Kazunori Ohno ,  Osamu Odai ,  Yukio Tominaga ,  Kiyoshi Furukawa ,  Makoto Oka

    IPC分类号： A61K31/4245 ,  A61K31/435 ,  A61K31/4375 ,  C07D271/02 ,  C07D271/06 ,  C07D271/10 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： 3-Oxadiazolyl-5,6,7,8-tetrahydro-1,6-naphthyridine derivative of the formula (I): ##STR1## wherein Het is an oxadiazole ring, R.sub.1 is hydrogen atom, an acyl group, a lower alkyl group or a group of the formula: --CH.sub.2 R.sub.1' (in which R.sub.1' is a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, benzyl group, aryl group or a heteroaromatic group), R.sub.2 is a lower alkyl group, a cyclo-lower alkyl group, a lower alkenyl group, a lower alkynyl group, aryl group, a heteroaromatic group, a halogeno-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkoxy group, a lower alkenyloxy group, a phenoxy group or a lower alkylthio group, or a pharmaceutically acceptable acid addition salt thereof, which are useful as benzodiazepine receptor agonist.

    摘要翻译： 式（I）的3-恶二唑基-5,6,7,8-四氢-1,6-萘啶衍生物：其中Het是恶二唑环，R 1是氢原子，酰基， 低级烷基或式-CH 2 R 1'（其中R 1'为环低级烷基，低级烯基，低级炔基，苄基，芳基或杂芳族基团）的基团，R 2为 低级烷基，低级烷基，低级烯基，低级炔基，芳基，杂芳基，卤代低级烷基，低级烷氧基 - 低级烷基，低级烷氧基，低级烷基 烯氧基，苯氧基或低级烷硫基，或其药学上可接受的酸加成盐，可用作苯并二氮杂受体激动剂。

    2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof
    6.
    发明授权
    2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof 失效
    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。

    Acetamide derivative, process for preparing the same, and a pharmaceutical composition containing the same
    7.
    发明授权
    Acetamide derivative, process for preparing the same, and a pharmaceutical composition containing the same 失效
    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

    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
    9.
    发明授权
    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof 失效
    治疗脑功能不全疾病的药物，新型2-（1-哌嗪基）-4-苯基环烷基嘧啶衍生物及其制备方法

    公开(公告)号：US5185338A

    公开(公告)日：1993-02-09

    申请号：US711894

    申请日：1991-06-07

    申请人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    发明人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    IPC分类号： A61K31/505 ,  C07D239/70

    CPC分类号： C07D239/70 ,  A61K31/505

    摘要： Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: ##STR1## wherein n is 3, 4, 5 or 6; R.sup.1 is hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, hydroxy-C.sub.2 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted aryl-carbonyl-(C.sub.1 -C.sub.6) alkyl, or acyl; R.sup.2 is hydrogen atom, halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or trifluoromethyl; and R.sup.3 is hydrogen atom or C.sub.1 -C.sub.6 alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

    摘要翻译： 用于治疗脑功能不全疾病的药物，其包含下式的化合物作为活性成分：其中n为3,4,5或6;其中n为3,4,5或6; R 1是氢原子，C 1 -C 6烷基，C 3 -C 8环烷基，羟基-C 2 -C 6）烷基，未取代或取代的芳基，杂芳基，未取代或取代的芳基 - （C 1 -C 6）烷基，未取代或取代的芳基 - 羰基 - （ C 1 -C 6）烷基或酰基; R2是氢原子，卤素原子，C1-C6烷基，C1-C6烷氧基或三氟甲基; 和R3是氢原子或C1-C6烷基或其酸加成盐，具有优异的脑功能改善活性的新型2-（1-哌嗪基）-4-苯基 - 环烷基嘧啶衍生物，其制备方法。