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    Benzo-fused heterocyclic compounds
    3.
    发明公开
    Benzo-fused heterocyclic compounds 失效
    苯并稠合的杂环化合物

    公开(公告)号：EP0081955A3

    公开(公告)日：1983-12-21

    申请号：EP82306432

    申请日：1982-12-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Schiehser, Guy Alan ,  Strike, Donald Peter

    IPC分类号： C07D275/06 ,  C07D209/50 ,  C07D417/12 ,  A61K31/425 ,  A61K31/40

    CPC分类号： C07D275/06 ,  C07D209/46 ,  C07D209/50 ,  C07D277/04 ,  C07D295/096 ,  C07D307/52 ,  C07D417/12

    摘要： The invention concerns compounds of the formula:
    wherein R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 5-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.
    and A is amine selected from
    wherein R 1 is hydrogen or R 2 CH 2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweral- kyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R 3 is (1-piperidinyl)methyl, R 1 is hydrogen; n is 1 to 4 and the pharmacologically acceptable salts thereof; which inhibit gastric acid secretion. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.

    Benzo-fused heterocyclic compounds
    4.
    发明公开
    Benzo-fused heterocyclic compounds 失效
    Benzo-Kondensierte杂种衍生物。

    公开(公告)号：EP0081955A2

    公开(公告)日：1983-06-22

    申请号：EP82306432.4

    申请日：1982-12-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Schiehser, Guy Alan ,  Strike, Donald Peter

    IPC分类号： C07D275/06 ,  C07D209/50 ,  C07D417/12 ,  A61K31/425 ,  A61K31/40

    CPC分类号： C07D275/06 ,  C07D209/46 ,  C07D209/50 ,  C07D277/04 ,  C07D295/096 ,  C07D307/52 ,  C07D417/12

    摘要： The invention concerns compounds of the formula:
    wherein R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 5-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.
    and
    A is amine selected from


    wherein R 1 is hydrogen or R 2 CH 2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweral- kyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R 3 is (1-piperidinyl)methyl, R 1 is hydrogen; n is 1 to 4 and the pharmacologically acceptable salts thereof; which inhibit gastric acid secretion. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.

    摘要翻译： 本发明涉及下式的化合物：其中R是单 - 或二卤代，氨基，硝基，氰基，羟基，三氟甲基，巯基，低级烷基，低级烷氧基，烷酰基，5-7个碳原子的环烷基，羧基， ，一或二低级烷基取代的氨基，烷酰基氨基，低级烷基硫代，低级烷基磺酰基，氨磺酰基，低级烷基取代的氨磺酰基，苯基或被卤素，低级烷基，低级烷氧基，三氟甲基，羟基，氨基，氰基或硝基取代的苯基。 X是SO 2，SO，S或C = O; 并且A是选自的胺，其中R 1是氢或R 2 CH2，其中R 2是单或二低级烷基氨基，一或二-N-低级烷基氨基低级烷基，（2-呋喃基）甲基氨基， 苄基氨基，低级环烷基氨基，1-吡咯烷基，1-哌啶基，1-六氢氮杂基，1-八氢吖嗪基，3-噻唑烷基，4-吗啉基或4-硫代吗啉基; R 3是氢或（1-哌啶基）甲基，条件是当R 3是（1-哌啶基）甲基时，R 1是氢; n为1〜4及其药理学上可接受的盐; 其抑制胃酸分泌。 还公开了用于制备含有它们的化合物和药物组合物的方法。

    N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase
    5.
    发明公开
    N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase 失效
    N，N'，N'-三取代-5,5-二氨基亚甲基-1,3-二恶烷-4,6-二酮α酰-CoA：胆固醇 - 酰基转移酶。

    公开(公告)号：EP0471493A1

    公开(公告)日：1992-02-19

    申请号：EP91307196.5

    申请日：1991-08-06

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Fobare, William Floyd ,  Strike, Donald Peter

    IPC分类号： C07D319/06 ,  A61K31/335 ,  C07D405/12 ,  C07F7/18 ,  A61K31/445 ,  A61K31/695

    CPC分类号： C07D405/12 ,  C07D319/06 ,  C07F7/1852

    摘要： The compounds of the formula:

    in which X, and Y are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R₁ is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethylphenethyl, 1-(t-butyl)dimenthylsilyloxy methylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R₁ is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R₂ is alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.

    摘要翻译： 下式的化合物：其中X和Y独立地是氢，卤素，羟基，硝基，氰基，羧基，三氟甲基，苯基，氨基，烷基氨基，二烷基氨基，烷基，烷氧基或苯基烷氧基; R1是氢，烷基，羟基烷基，烯基，环烷基，苯基环烷基，1-羟基甲基苯乙基，1-（叔丁基）二甲基甲硅烷氧基甲基苯乙基，1-（叔丁基）二甲基甲硅烷氧基甲基异戊基，1-羟基甲基异戊基，苯基，苄基或取代的苯基或苄基， 其中取代基是烷基，烷氧基，卤素，氰基，三氟甲基，氨基，烷基氨基，二烷基氨基，硝基或苯基，苄基，苯乙基或R 1是噻吩基，咪唑基，噻唑基，吡啶基，嘧啶基，吡嗪基，苯并咪唑基，苯基烷基哌啶基或吗啉代; R2是烷基，环烷基，苯基，苄基或取代的苯基或苄基，其中所述取代基是烷基，烷氧基，卤素，氰基，三氟甲基氨基，硝基，烷基氨基或二烷基氨基; 及其药学上可接受的盐; 是ACAT抑制剂，其中一些具有抗氧化性质。

    Imidazo[4,5-c]pyridines as antiosteoporotic agents
    7.
    发明公开
    Imidazo[4,5-c]pyridines as antiosteoporotic agents 失效
    咪唑（4,5-c）吡啶als Mittel gegen骨质疏松。

    公开(公告)号：EP0434405A1

    公开(公告)日：1991-06-26

    申请号：EP90313945.9

    申请日：1990-12-19

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Santilli, Arthur Attilio ,  Scotese, Anthony Carmen ,  Strike, Donald Peter

    IPC分类号： C07D471/04 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： The invention describes compounds of formula (I)

    or tautomer thereof, wherein R¹, R², R³, R⁴ and R⁵ are independently selected from hydrogen, lower alkyl containing 1 to 6 carbon atoms, hydroxy, lower alkyloxy containing 1 to 6 carbon atoms, halogen, trifluoromethyl, trifluoromethoxy, nitro, cyano, phenoxy, benzyloxy, acetamido -S(O) p -CH₃ or any two adjacent groups are joined to form methylenedioxy; m is 0 to 2; n is 1 to 3; p is 0 to 2, and pharmaceutically acceptable salts and hydrates thereof which are useful as antiosteoporotic agents

    摘要翻译： 本发明描述了式（I）的化合物或其互变异构体，其中R 1，R 2，R 3，R 4和R 5独立地选自氢，低级烷基 1至6个碳原子，羟基，含有1至6个碳原子的低级烷氧基，卤素，三氟甲基，三氟甲氧基，硝基，氰基，苯氧基，苄氧基，乙酰氨基-S（O）p-CH 3或任何两个相邻基团连接形成亚甲二氧基 ; m为0〜2; n为1〜3; p为0〜2，以及其可用作抗骨质疏松剂的药学上可接受的盐和水合物

    Fused heterocyclic compounds
    9.
    发明公开
    Fused heterocyclic compounds 失效
    Kondensierte heterzyklische Verbindungen。

    公开(公告)号：EP0120585A1

    公开(公告)日：1984-10-03

    申请号：EP84301026.5

    申请日：1984-02-17

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： Schiehser, Guy Alan ,  Strike, Donald Peter

    IPC分类号： C07D513/04 ,  A61K31/425 ,  A61K31/445

    CPC分类号： C07D209/48 ,  C07D295/096 ,  C07D307/52 ,  C07D495/04 ,  C07D513/04

    摘要： The invention concerns compounds of the formula
    wherein B is a moiety having the formula:
    the dotted line represents a bond which is present when B is formula Id or If and absent when B isformula le, R is hydrogen, mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lowercycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkamoylamino, lower alkyl thio, loweralkyl-sulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy,trifluoromethyl, hydroxy, amino, cyano or nitro; X is SO 2 , SO, S or C=O and A is an amine of formula:


    wherein n is 1 to 4; R' is hydrogen or R 2 CH2 wherein R 2 is mono- or diloweralkylamino, mono- or di-N-lower- alkylamino lower alkyl, (2-furyl)methylamino, benzylamino, lower cycloalkylamino of 5 to 7 carbon atoms, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl,4-morpholinyl or4-thiomorpholinyl; R 3 is hydrogen or (1-piperidinyl)-methyl with the proviso that when R 3 is (1-piperidinyl)-methyl, then R' is hydrogen; and the pharmacologically acceptable salts thereof which inhibit gastic acid secretion. Processes for preparing the compounds and pharmaceutical compositions containing them are also disclosed.

    摘要翻译： 本发明涉及式CHEM的化合物，其中B是具有下式的部分：虚线表示当B是式Id时存在​​的键或如果B是式Ie，R是氢时不存在， 单或二卤代，氨基，硝基，氰基，羟基，三氟甲基，巯基，低级烷基，低级烷氧基，烷酰基，低级环烷基，羧基，烷氧基羰基，一或二低级烷基取代的氨基，烷酰氨基，低级烷基硫代，低级烷基 - ，氨磺酰基，低级烷基取代的氨磺酰基，苯基或被卤素，低级烷基，低级烷氧基，三氟甲基，羟基，氨基，氰基或硝基取代的苯基。 X是SO 2，SO，S或C = O，A是下式的胺：其中n为1至4; R 1是氢或R 2 CH2，其中R 2是单或二低级烷基氨基，一或二-N-低级烷基氨基低级烷基，（2-呋喃基）甲基氨基，苄基氨基，5-7碳的低级环烷基氨基 1-吡咯烷基，1-哌啶基，1-六氢氮杂基，1-八氢吖嗪基，3-噻唑烷基，4-吗啉基或4-硫代吗啉基; R 3为氢或（1-哌啶基） - 甲基，条件是当R 3为（1-哌啶基） - 甲基时，R 1为氢; 及其抑制胃酸分泌的药理学上可接受的盐。 还公开了用于制备含有它们的化合物和药物组合物的方法。