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    • 1. 发明申请
    • NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
    • 新型喹啉衍生物及其药物组合物
    • WO1996020194A1
    • 1996-07-04
    • PCT/JP1995002713
    • 1995-12-27
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.TAKEUCHI, MakotoNAITO, RyoHAYAKAWA, MasahikoOKAMOTO, YoshinoriYONETOKU, YasuhiroIKEDA, KenISOMURA, Yasuo
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D453/02
    • C07D221/12C07D453/02C09K19/3444
    • A quinuclidine derivative represented by general formula (I), a salt, N-oxide or quaternary ammonium salt thereof, and a medicinal composition containing the same, wherein the ring A represents optionally substituted aryl, cycloalkyl, cycloalkenyl, heteroaryl containing 1 to 4 heteroatoms selected from among oxygen, nitrogen and sulfur, or 5- to 7-membered saturated heterocycle; X represents a single bond or methylene; R represents halogeno, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower acyl, mercapto, lower alkylthio, sulfonyl, lower alkylsulfonyl, sulfinyl, lower alkylsulfinyl, sulfonamido, lower alkanesulfonamido, carbamoyl, thio-carbamoyl, mono- or di(lower alkyl)carbamoyl, nitro, cyano, amino, mono- or di(lower alkyl)amino, methylenedioxy, ethylenedioxy or lower alkyl optionally substituted by halogeno, hydroxy, lower alkoxy, amino or mono- or di(lower alkyl)amino; 1 is 0 or 1; m is an integer of 1 to 3; and n is an integer of 1 or 2. The compound has an antagonistic effect on muscarine M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
    • 由通式(I)表示的奎宁环衍生物,其盐,N-氧化物或季铵盐及含有该奎宁环衍生物的药物组合物,其中环A表示任选取代的芳基,环烷基,环烯基,含有1至4个杂原子的杂芳基 选自氧,氮和硫,或5-至7-元饱和杂环; X表示单键或亚甲基; R代表卤代,羟基,低级烷氧基,羧基,低级烷氧基羰基,低级酰基,巯基,低级烷硫基,磺酰基,低级烷基磺酰基,亚磺酰基,低级烷基亚磺酰基,亚磺酰氨基,低级烷烃磺酰胺基,氨基甲酰基,硫代氨基甲酰基, 氨基,硝基,氰基,氨基,一或二(低级烷基)氨基,亚甲二氧基,亚乙二氧基或任选被卤代,羟基,低级烷氧基,氨基或一或二(低级烷基)氨基取代的低级烷基; 1为0或1; m为1〜3的整数。 并且n是1或2的整数。该化合物对毒蕈碱M3受体具有拮抗作用,并且可用作泌尿系统疾病,呼吸系统疾病或消化系统疾病的预防或治疗。
    • 2. 发明申请
    • BENZENESULFONE COMPOUNDS AND SALTS THEREOF
    • 苯并呋喃酮化合物及其盐
    • WO1998008820A1
    • 1998-03-05
    • PCT/JP1997002934
    • 1997-08-25
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.YOKOTA, MasakiKAWAZOE, SouichirouOKAMOTO, YoshinoriKUBOTA, HirokazuNAITO, RyoARAKIDA, Yasuhito
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D215/12
    • C07D215/14
    • Benzenesulfone compounds represented by general formula (I) or pharmaceutically acceptable salts thereof, useful as pharmaceuticals having a combination of leucotriene antagonism with thromboxane A2 antagonism and good oral absorbability, especially as agents for preventing and treating diseases and which leucotriene and thromboxane A2 participate, such as bronchial asthma, wherein B represents an optionally substituted quinolyl group; D represents an optionally substituted phenyl group; E represents a group represented by formulas (a), (b), or (c); one of A and A represents an optionally substituted methylene group or an optionally substituted ethylene group with the other representing a single bond, an optionally substituted methylene group, or an optionally substituted ethylene group, provided that when 1 is 1 and Y represents an optionally substituted phenylene group, each of A and A may represent a single bond; X represents an oxygen atom or a sulfur atom; Y represents an optionally substituted phenylene group, an optionally substituted phenyleneoxy group, or an optionally substituted spirocyclopropinyl group; Z represents a group represented by the formula: -CH=CH-, -CH2-CH2-, -CH2O-, or -O-CH2-; R represents a carboxyl group or tetrazolyl group which may be optionally substituted with an ester residue; 1, n, p, and q, which may be the same or different, are each 0 or 1; and m represents 1, 2, or 3.
    • 通式(I)表示的苯磺酸盐或其药学上可接受的盐,其可用作具有白三烯拮抗作用与血栓素A2拮抗作用的组合和良好的口服吸收性的药物,特别是作为预防和治疗疾病的药物以及白内障和血栓素A2参与的药物 作为支气管哮喘,其中B表示任选取代的喹啉基; D表示任选取代的苯基; E表示由式(a),(b)或(c)表示的基团。 A 1和A 2之一表示任选取代的亚甲基或任选取代的亚乙基,另一个代表单键,任选取代的亚甲基或任选取代的亚乙基,条件是当1为1时 Y表示任意取代的亚苯基,A 1和A 2中的每一个可以表示单键; X表示氧原子或硫原子; Y表示任选取代的亚苯基,任选取代的亚苯基氧基或任选取代的螺环丙基; Z表示由下式表示的基团:-CH = CH-,-CH 2 -CH 2 - , - CH 2 O - 或-O-CH 2 - ; R表示可任选被酯残基取代的羧基或四唑基; 1,n,p和q可以相同或不同,各自为0或1; m表示1,2或3。