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    • 1. 发明授权
    • Benzodiazepine derivative
    • 苯二氮卓衍生物
    • US5776929A
    • 1998-07-07
    • US663304
    • 1996-06-25
    • Sanji HagishitaSusumu KamataKaoru SenoNobuhiro HagaYasunobu Ishihara
    • Sanji HagishitaSusumu KamataKaoru SenoNobuhiro HagaYasunobu Ishihara
    • C07D243/12C07D403/12C07D403/14C07D405/14C07D409/14C07D413/12C07D417/14A61K31/55
    • C07D403/12C07D243/12C07D403/14C07D405/14C07D409/14C07D413/12C07D417/14
    • A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
    • PCT No.PCT / JP94 / 02132 Sec。 371日期1996年6月25日第 102(e)日期1996年6月25日PCT 1994年12月19日PCT PCT。 公开号WO95 / 18110 日期:1995年7月6日一种式(I)的苯并二氮杂衍生物:其中R 1是一个键,-CH 2 - , - CH 2 O-,-SCH 2 - 或下式的基团: 低级烷基,-COOR 5,-CONH(CH 2)n COOR 5,-CONHSO 2 R 5,-SO 2 NHCOR 5或任选取代的杂环基(R 5为氢原子,低级烷基或苄基,n为1至5的整数)。 R3是键,-CO-或-CONH-; 并且R4是任选取代的杂环基,任选取代的低级烷基,任选取代的低级环烷基,任选取代的芳基或低级烷氧基羰基或其药学上可接受的盐,其对胃泌素受体和/或CCK-B受体具有高亲和力 但不适用于CCK-A受体,并且可用于治疗与胃泌素受体和/或CCK-B受体相关的疾病,而不诱导与CCK-A受体相关的副作用。
    • 3. 发明申请
    • Therapeutic Agent for Constipation
    • 便秘治疗剂
    • US20090069363A1
    • 2009-03-12
    • US11792893
    • 2005-12-13
    • Tsutomu SuzukiTakuko SawadaYasunobu Ishihara
    • Tsutomu SuzukiTakuko SawadaYasunobu Ishihara
    • A61K31/485C07D489/00A61P1/10
    • A61K31/485A61K45/06
    • A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid μ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I): (wherein R1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R2 and R3 independently represent hydrogen, hydroxy or the like; R4 is hydrogen, hydroxy or the like; R5 is hydrogen; R4 and R5 may optionally form —O— or the like; R6 represents hydrogen, lower alkyl or the like (wherein X represents —O— or —N(R10)— or the like; R7, R8, R9a and R9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents —CH— or the like; Z represents a crosslinkage composed of 2 to 5 atoms) or a pharmaceutically acceptable salt thereof or a solvate of either.
    • 一种由具有阿片样物质α受体激动剂活性的化合物诱导的便秘的治疗和/或预防剂,该药物包含作为有效成分的具有阿片样物质δ受体拮抗剂活性的化合物,例如式(I)的化合物:其中 R1代表氢,低级烷基,环烷基低级烷基等; R2和R3独立地表示氢,羟基等; R4是氢,羟基等; R5是氢; R4和R5可以任选地形成-O-或 R6表示氢,低级烷基等(其中X表示-O-或-N(R10) - 等; R7,R8,R9a和R9b独立地表示氢,低级烷基,低级烷氧基羰基等; r 表示0〜5的整数,Y表示-CH-等; Z表示2〜5个原子的交联键)或其药学上可接受的盐或其溶剂合物。
    • 4. 发明授权
    • 9-(Substituted thio)-4H-pyrido[1,2,-A]pyrimidin-4-one derivatives
    • 9-(取代的硫代)-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物
    • US4840953A
    • 1989-06-20
    • US206665
    • 1988-06-15
    • Shigeru MatsutaniYukio MizushimaMasami DoteuchiYasunobu Ishihara
    • Shigeru MatsutaniYukio MizushimaMasami DoteuchiYasunobu Ishihara
    • C07D471/04
    • C07D471/04
    • 9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.
    • 9-(取代的硫代)-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物其中n为0或1,R为-COR 1,-CONR 4 R 5或-CH 2 R 6 R1是C1-C5烷基,C3-C7环烷基,烯硫基,苯乙烯基,苯氧基甲基,噻吩基甲基,任选取代的C 6 -C 10芳基,任选取代的苄基,或任选被取代的5或6元杂环基,R 2和R 3各自是氢, C 1 -C 5烷基,羧基,C 2 -C 5烷氧基羰基或任选取代的苄氧基羰基,R 4和R 5各自为氢,C 1 -C 5烷基,C 3 -C 7环烷基或任选取代的苯基,R 8为任选取代的吡啶基或苯基)可用作抗溃疡剂 代理商通过几条路线提供。