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    • 61. 发明申请
    • NOVEL N-(PYRIDYLCARBONYL)BENZAZEPINE DERIVATIVE AND INTERMEDIATE THEREFOR
    • 新型N-(吡咯烷基)苯并噻吩衍生物及其中间体
    • WO1994014796A1
    • 1994-07-07
    • PCT/JP1993001838
    • 1993-12-17
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.MATSUMOTO, YuzoTANAKA, AkihiroMATSUHISA, AkiraKIKUCHI, KazumiSAKAMOTO, Ken-ichiroYATSU, TakeyukiYANAGISAWA, Isao
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D401/06
    • C07D401/06
    • An N-(pyridylcarbonyl)benzazepine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, useful for preventing and treating cardiac failure, hyponatremia, syndrome of inappropriate secretion of vasopressin (SIADH), hypertension, renal failure, edema, water metabolism disorder, and the like on the basis of arginine vasopressin receptor antagonism; and a benzazepinylcarbonylpyridine derivative represented by general formula (II) or a salt thereof, useful as an intermediate for the production of the compound (I) and so forth, wherein R represents hydrogen, lower alkyl, lower alkoxy, halogen, or phenyl which may be substituted by lower alkyl; X represents -NHCO- or -CON(R )-; n represents 0 or 1; and R represents hydrogen or (a) wherein R is as defined above, wherein n is as defined above; and Y represents COOH, activated carboxy, protected carboxy, or optionally protected HN(R )-.
    • 用于预防和治疗心力衰竭,低钠血症,加压素分泌不良综合征(SIADH),高血压,肾衰竭,水肿,水分的通式(I)表示的N-(吡啶基羰基)苯并氮杂衍生物或其药学上可接受的盐 代谢障碍等,基于精氨酸加压素受体拮抗作用; 和由通式(II)表示的苯并氮杂基羰基吡啶衍生物或其盐,可用作制备化合物(I)等的中间体,其中R表示氢,低级烷基,低级烷氧基,卤素或苯基, 被低级烷基取代; X表示-NHCO-或-CON(R 1) - ; n表示0或1; 并且R 1表示氢或(a)其中R如上定义,其中n如上所定义; 和Y代表COOH,活化的羧基,保护的羧基或任选被保护的HN(R 1) - 。
    • 66. 发明申请
    • NOVEL BISHETEROCYCLIC DERIVATIVE OR SALT THEREOF
    • 新型双相异构衍生物或其盐
    • WO1993003021A1
    • 1993-02-18
    • PCT/JP1992000954
    • 1992-07-28
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.NIIGATA, KunihiroTAKAHASHI, TakumiYONEDA, TakashiNOSHIRO, OsamuKOIKE, ReikoSHIMAYA, Akiyoshi
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D263/44
    • C07D263/44C07D277/20C07D277/34C07D493/04Y02P20/55
    • A bisheterocyclic compound represented by general formula (I), stereoisomers thereof, tautomers thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a pharmaceutical composition containing the same, and a process for the production thereof. In formula (I), R and R may be the same or different from each other and each represents (II) or (III), R represents hydrogen or a protective group, X, Y and Y may be the same or different from one another and each represents oxygen or sulfur, B and B represent each phenylene, B represents phenylene, naphthylene, cyclohexylene or furo[3,2-b]furanylene, L and L represent each -(O)n-A-, n represents 0 or 1, and A represents a single bond or lower alkylene, provided that when n is 1, A represents alkylene and the oxygen atom of each of L and L is bonded to B . The above compounds are useful as a hypoglycemic drug based on the activity of enhancing insulin sensitivity.
    • 由通式(I)表示的双杂环化合物,其立体异构体,其互变异构体,其药学上可接受的盐或其药学上可接受的溶剂合物,含有它们的药物组合物及其制备方法。 在式(I)中,R 1和R 2可以彼此相同或不同,并且各自表示(II)或(III),R 3表示氢或保护基,X,Y' 1>和Y 2可以相同或不同,各自表示氧或硫,B 1和B 2表示各个亚苯基,B 3表示亚苯基,亚萘基,亚环己基或呋喃并[3 ,2-b]呋喃,L 1和L 2表示 - (O)n - ,n表示0或1,A表示单键或低级亚烷基,条件是当n为1时,A表示 亚烷基和L 1和L 2各自的氧原子与B 3键合。 基于提高胰岛素敏感性的活性,上述化合物可用作降血糖药物。