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    • 8. 发明授权
    • Dihydropyridine compounds and pharmaceutical compositions containing them
    • 二氢吡啶化合物和含有它们的药物组合物
    • US4727082A
    • 1988-02-23
    • US908350
    • 1986-09-17
    • Takashi FujikuraNoriki ItoYuzo MatsumotoYasuo IsomuraMasaharu AsanoToichi Takenaka
    • Takashi FujikuraNoriki ItoYuzo MatsumotoYasuo IsomuraMasaharu AsanoToichi Takenaka
    • C07D211/82A61K31/44A61K31/455A61P9/00A61P9/06A61P9/08A61P9/10A61P9/12A61P25/02A61P25/28C07D211/90C07D401/12
    • C07D401/12C07C317/00C07C323/00C07D211/90
    • 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.
    • 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。
    • 9. 发明授权
    • Novel fused derivatives of 2-pyridones
    • 2-吡啶酮的新型融合衍生物
    • US4186200A
    • 1980-01-29
    • US876517
    • 1978-02-09
    • Kazuo KuboNoriki ItoIsao SouzuYasuo IsomuraHiroshige HommaMasuo Murakami
    • Kazuo KuboNoriki ItoIsao SouzuYasuo IsomuraHiroshige HommaMasuo Murakami
    • A61K31/44C07D213/64C07D213/74C07D213/89C07D455/02C07D471/04C07D498/04C07D513/04A61K31/415
    • C07C255/00C07D213/64C07D213/89C07D471/04C07D513/04
    • 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.
    • 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
    • 10. 发明授权
    • Dihydropyridine compounds which process both calcium (2+)-antagonistic
and beta receptor blocking activities
    • 二钙二氢化合物(2 +) - 拮抗剂和受体阻断活性
    • US5110820A
    • 1992-05-05
    • US611340
    • 1990-11-13
    • Takashi FujikuraNoriki ItoYuzo MatsumotoMasaharu AsanoToichi Takenaka
    • Takashi FujikuraNoriki ItoYuzo MatsumotoMasaharu AsanoToichi Takenaka
    • A61K31/4427A61K31/455A61P3/00A61P3/14A61P9/08A61P9/10A61P9/12A61P25/02C07D211/90C07D401/12
    • C07D401/12C07D211/90
    • 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.
    • 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。