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    Dihydropyridine compounds and pharmaceutical compositions containing them
    1.
    发明授权
    Dihydropyridine compounds and pharmaceutical compositions containing them 失效
    二氢吡啶化合物和含有它们的药物组合物

    公开(公告)号：US4727082A

    公开(公告)日：1988-02-23

    申请号：US908350

    申请日：1986-09-17

    申请人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Yasuo Isomura ,  Masaharu Asano ,  Toichi Takenaka

    发明人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Yasuo Isomura ,  Masaharu Asano ,  Toichi Takenaka

    IPC分类号： C07D211/82 ,  A61K31/44 ,  A61K31/455 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  A61P25/28 ,  C07D211/90 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07C317/00 ,  C07C323/00 ,  C07D211/90

    摘要： A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.CH--), or a ethynylene group (--C.dbd.C--); B represents a single bond or --CH.sub. 2 O--; and m and n, which are the same or different, each represents 0 or an integer of 1 to 5.The compounds are useful for the treatment of various cardiovascular disorders, since they possess both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities.

    摘要翻译： 下列通式（I）的二氢吡啶化合物或其盐：其中R 1和R 2相同或不同，各自表示C1至C10烷基，低级烷基 其被氧原子或被C3-C6脂环族基团取代的低级烷基取代; R 3和R 4相同或不同，各自表示低级烷基; R 5和R 6相同或不同，分别表示氢原子，硝基，卤素原子，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基或低级烷基亚磺酰基 ; R 7和R 8相同或不同，各自表示氢原子，卤素原子，氰基，低级烷氧基或低级烷酰氨基，或者可以与R 8结合形成萘基， 相邻苯基; A表示单键，亚乙烯基（-CH = CH-）或亚乙炔基（-C = C-）; B表示单键或-CH 2 O-; 和m和n相同或不同，各自表示0或1至5的整数。该化合物可用于治疗各种心血管疾病，因为它们具有Ca 2+拮抗剂和肾上腺素能β受体阻断活性。

    Dihydropyridine compounds which process both calcium (2+)-antagonistic and beta receptor blocking activities
    2.
    发明授权
    Dihydropyridine compounds which process both calcium (2+)-antagonistic and beta receptor blocking activities 失效
    二钙二氢化合物（2 +） - 拮抗剂和受体阻断活性

    公开(公告)号：US5110820A

    公开(公告)日：1992-05-05

    申请号：US611340

    申请日：1990-11-13

    申请人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Masaharu Asano ,  Toichi Takenaka

    发明人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Masaharu Asano ,  Toichi Takenaka

    IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P3/00 ,  A61P3/14 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D211/90 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07D211/90

    摘要： Dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The compounds have the formula ##STR1## wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s); R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group; R.sup.2 represents an amino group, ##STR2## R.sup.3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s), or ##STR3## R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a trifluoromethyl group, a cyano group, a lower alkyl group, a lower alkoxy group or a lower alkenyloxy group; R.sup.7 represents a hydrogen atom, a cyano group, a halogen atom, a lower alkoxy group or a lower alkanoyl group; R.sup.8 and R.sup.9, which may be the same or different, each represents a lower alkyl group or an aralkyl group; and n represents an integer of 1 to 2: these symbols, hereafter, have the same significances.

    摘要翻译： 提供二氢吡啶化合物及其盐，其表现出Ca 2+ +拮抗性和肾上腺素能β受体阻断活性，因此可用于治疗缺血性心脏病和高血压。 化合物具有式（I）的化合物，其中A表示可被氧原子间隔的具有1-10个碳原子的直链或支链碳链亚烷基; R 1和R 4可以相同或不同，各自表示低级烷基; R 2表示氨基，R 3表示可被氧原子间隔的具有1〜10个碳原子的直链或支链碳链烷基，或者R 5和R 6 可以相同或不同，分别表示氢原子，硝基，卤素原子，三氟甲基，氰基，低级烷基，低级烷氧基或低级链烯氧基。 R7表示氢原子，氰基，卤素原子，低级烷氧基或低级烷酰基; R 8和R 9可以相同或不同，各自表示低级烷基或芳烷基; n表示1〜2的整数，以下，符号相同。

    Dihydropyridine composition
    3.
    发明授权
    Dihydropyridine composition 失效
    二氢吡啶组成

    公开(公告)号：US5591757A

    公开(公告)日：1997-01-07

    申请号：US418262

    申请日：1995-04-06

    申请人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Masaharu Asano ,  Toichi Takenaka

    发明人： Takashi Fujikura ,  Noriki Ito ,  Yuzo Matsumoto ,  Masaharu Asano ,  Toichi Takenaka

    IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P3/00 ,  A61P3/14 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D211/90 ,  C07D401/12

    CPC分类号： C07D401/12 ,  C07D211/90

    摘要： Pharmaceutical composition of certain dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The pharmaceutical compositions contains either 4-(2-hydroxy-3-phenoxy-propylamino)-butyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or 6-(2-hydroxy-3-phenoxypropylamino) hexyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or their pharmaceutically acceptable salts.

    摘要翻译： 提供某些二氢吡啶化合物及其盐的药物组合物，其表现出Ca 2+拮抗剂和肾上腺素能β受体阻断活性，因此可用于治疗缺血性心脏病和高血压。 药物组合物含有4-（2-羟基-3-苯氧基 - 丙基氨基） - 丁基甲基2,6-二甲基-4-（间硝基苯基）-1,4-二氢吡啶-3,5-二羧酸酯或6-（ 2-羟基-3-苯氧基丙基氨基）己基甲基2,6-二甲基-4-（间硝基苯基）-1,4-二氢吡啶-3,5-二羧酸酯或其药学上可接受的盐。

    Novel fused derivatives of 2-pyridones
    5.
    发明授权
    Novel fused derivatives of 2-pyridones 失效
    2-吡啶酮的新型融合衍生物

    公开(公告)号：US4186200A

    公开(公告)日：1980-01-29

    申请号：US876517

    申请日：1978-02-09

    申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

    发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

    IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/415

    CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

    摘要： Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4##when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, and the pharmacologically acceptable non-toxic salts thereof. The compounds described above are strong analgesic anti-inflammatory agents.

    摘要翻译： 式中，R 1和R 2中的一个表示低级烷基，苯基，卤代苯基或低级烷氧基苯基，另一方表示氢原子，低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子，低级烷基，苯基或苯基低级烷基; X表示氧原子，硫原子，亚氨基或由下式表示的基团，其中m表示1或2，R4表示低级烷基，羟基低级烷基，环烷基或苯基低级烷基 组; Y表示可以被低级烷基，三亚甲基，四亚甲基，可被低级烷基取代的亚乙烯基取代的亚乙基，或者R5表示氢原子的低级烷基 基，三氟甲基或苯基; 说X是所示的组

    Nitrogen-containing heterocyclic compounds
    7.
    发明授权
    Nitrogen-containing heterocyclic compounds 失效
    含氮杂环化合物

    公开(公告)号：US4251533A

    公开(公告)日：1981-02-17

    申请号：US67918

    申请日：1979-08-20

    申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

    发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma ,  Masuo Murakami

    IPC分类号： A61K31/44 ,  C07D213/64 ,  C07D213/74 ,  C07D213/89 ,  C07D455/02 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/435 ,  C07D471/02

    CPC分类号： C07C255/00 ,  C07D213/64 ,  C07D213/89 ,  C07D471/04 ,  C07D513/04

    摘要： Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group; and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## wherein R.sub.5 represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, or a phenyl group; said X is the group shown by ##STR4## when one of said R.sub.1 and R.sub.2 is a lower alkyl group and the other is a hydrogen atom, and said Y is an ethylene group, 1/7and the pharmacologically acceptable non-toxic salts thereof.The compounds described above are strong analgesic anti-inflammatory agents.

    摘要翻译： 式中，R 1和R 2中的一个表示低级烷基，苯基，卤代苯基或低级烷氧基苯基，另一方表示氢原子，低级 烷基或苯基低级烷基; 所述R1和R2可以相互结合形成三亚甲基或四亚甲基; R3表示氢原子，低级烷基，苯基或苯基低级烷基; X表示氧原子，硫原子，亚氨基或由下式表示的基团，其中m表示1或2，R4表示低级烷基，羟基低级烷基，环烷基或苯基低级烷基 组; Y表示可以被低级烷基，三亚甲基，四亚甲基，可被低级烷基取代的亚乙烯基取代的亚乙基，或者R5表示氢原子的低级烷基 基，三氟甲基或苯基; 当所述R 1和R 2中的一个为低级烷基且另一个为氢原子，所述Y为亚乙基时，X为所示的基团，其药理学上可接受的无毒性盐 。 上述化合物是强镇痛抗炎剂。

    1-Oxo-1,2-dihydroisoquinoline derivatives
    8.
    发明授权
    1-Oxo-1,2-dihydroisoquinoline derivatives 失效
    1-氧代-1,2-二氢异喹啉衍生物

    公开(公告)号：US4198512A

    公开(公告)日：1980-04-15

    申请号：US925217

    申请日：1978-07-17

    申请人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

    发明人： Kazuo Kubo ,  Noriki Ito ,  Isao Souzu ,  Yasuo Isomura ,  Hiroshige Homma

    IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P25/04 ,  A61P29/00 ,  C07D217/24

    CPC分类号： C07D217/24

    摘要： Novel 1-oxo-1,2-dihydroisoquinoline compounds of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a phenyl lower alkyl group; R.sub.2 represents a lower alkyl group; R.sub.3 represents a hydrogen atom, a lower alkanoyl group, a lower alkyl group or a hydroxy lower alkyl group; and n is 0, 1 or 2 and the pharmacologically acceptable non-toxic salts thereof.The compounds of this invention are strong analgesic anti-inflammatory agents.

    摘要翻译： 新颖的式Ⅰ-1-氧代-1,2-二氢异喹啉化合物，其中R1代表低级烷基或苯基低级烷基; R2表示低级烷基; R3表示氢原子，低级烷酰基，低级烷基或羟基低级烷基; 和n为0,1或2及其药理学上可接受的无毒盐。 本发明的化合物是强镇痛抗炎剂。

    Diurea derivatives useful as medicaments and processes for the preparation thereof
    10.
    发明授权
    Diurea derivatives useful as medicaments and processes for the preparation thereof 失效
    用作药物的二脲衍生物及其制备方法

    公开(公告)号：US5384425A

    公开(公告)日：1995-01-24

    申请号：US64850

    申请日：1993-10-07

    申请人： Noriki Ito ,  Tomoyuki Yasunaga ,  Yuichi Iizumi ,  Tomio Araki

    发明人： Noriki Ito ,  Tomoyuki Yasunaga ,  Yuichi Iizumi ,  Tomio Araki

    IPC分类号： C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C335/14 ,  C07D213/75 ,  C07C69/017

    CPC分类号： C07D213/75 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C335/14 ,  C07C2101/14 ,  C07C2101/18

    摘要： Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.6 is a phenyl substituted by acyloxy.

    摘要翻译： 提供了可由以下通式表示的二脲衍生物及其盐：其中，R 1和R 2相同或不同，各自表示C 1-10烷基，C 3-18环烷基或低级 被环烷基取代的烷基; R 3，R 4，R 5和R 6相同或不同，各自表示氢原子，低级烷基，环烷基，烃基芳烷基，吡啶基或未取代或取代的苯基，苯基 基团选自低级烷基，卤素原子取代的低级烷基，卤原子，硝基，氨基，一或二低级烷基氨基，低级酰基氨基，羟基，低级烷氧基和低级烷基 酰氧基; X表示氧原子或硫原子，n1和n2表示1〜6的整数， 并且其中R 3 -R 6中的至少一个是被酰氧基取代的苯基。