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    ANTHRANILIC ACID ANALOGS
    2.
    发明公开
    ANTHRANILIC ACID ANALOGS 审中-公开
    ANTHRANILIC ACID类似物

    公开(公告)号：EP1003713A1

    公开(公告)日：2000-05-31

    申请号：EP98938221.3

    申请日：1998-08-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： LENNOX, Joseph, Richard ,  ANTANE, Schuyler, Adam ,  BUTERA, John, Anthony

    IPC分类号： C07C233/63 ,  C07D263/34 ,  C07D261/18 ,  A61K31/16 ,  A61K31/42

    CPC分类号： C07D263/34 ,  C07C233/63 ,  C07C2601/10 ,  C07D261/18

    摘要： Compounds of formula (I) wherein: R1, R2 and R3 are, independently, hydrogen, nitro, cyano, C1-10 haloalkoxy, amino, C1-10 alkylamino, sulfo, sulfamoyl, C1-10 alkylsulfonamido, C2-10 alkylcarboxamido C2-10 alkanoyl, C1-10 alkylsulfonyl, C1-10 haloalkylsulfonyl, C1-10 carboxyl, C1-10 haloalkyl and C6-12 aryl; with the provisos: (1) that R1, R2 and R3 may not all simultaneously be hydrogen, and (2) when R1 and R2 are hydrogen, R3 may not be meta-CF3; R4, R5 and R6 are, independently , hydrogen, halogen, nitro, cyano, C1-10 carboalkoxy, C1-10 haloalkoxy, amino C1-10 alkylamino, sulfo, sulfamoyl, C1-10 alkylsulfonamido, C2-10 alkylcarboxamido C2-10 alkanoyl, C1-10 alkylsulfonyl, C1-10 haloalkylsulfonyl, C1-10 carboxyl, C1-10 haloalkyl, C1-10 alkyl and C6-12 aryl; R7 is hydrogen , metal cation, acetylamido, alkoxyacetoyl or a related moiety which delivers the carboxylate in vivo; and X, Y and Z may form a C3-13 carbocyclic ring, oxazole, isoxazole, thiazole, isothiazole, furan, thiophene, 2H-pyrrole, pyrrole, 2-pyrroline, 3-pyrroline, imidazole, pyrazole, 1,2,3-oxadiazole or 1,2,3-triazole bound to the carbon skeleton; or pharmaceutically acceptable salts thereof useful in the treatment of disorders associated with smooth muscle contraction via potassium channel and chloride channel modulation.

    摘要翻译： 其中：R1，R2和R3独立地为氢，硝基，氰基，C1-10卤代烷氧基，氨基，C1-10烷基氨基，磺基，氨磺酰基，C1-10烷基磺酰氨基，C2-10烷基甲酰氨基C2- 10链烷酰基，C1-10烷基磺酰基，C1-10卤代烷基磺酰基，C1-10羧基，C1-10卤代烷基和C6-12芳基; （1）R 1，R 2和R 3可能不全都是氢，并且（2）当R 1和R 2是氢时，R 3可能不是间位-CF 3; R4，R5和R6独立地为氢，卤素，硝基，氰基，C1-10烷氧基羰基，C1-10卤代烷氧基，氨基C1-10烷基氨基，磺基，氨磺酰基，C1-10烷基磺酰氨基，C2-10烷基甲酰氨基C2-10烷酰基 C1-10烷基磺酰基，C1-10卤代烷基磺酰基，C1-10羧基，C1-10卤代烷基，C1-10烷基和C6-12芳基; R7是氢，金属阳离子，乙酰胺基，烷氧基乙酰基或在体内递送羧酸酯的相关部分; 并且X，Y和Z可以形成C3-13碳环，恶唑，异恶唑，噻唑，异噻唑，呋喃，噻吩，2H-吡咯，吡咯，2-吡咯啉，3-吡咯啉，咪唑，吡唑，1,2,3 - 恶二唑或1,2,3-三唑与碳骨架结合; 或其药学上可接受的盐，其可用于通过钾通道和氯化物通道调节治疗与平滑肌收缩相关的病症。

    ANTHRANILIC ACID ANALOGS
    4.
    发明公开
    ANTHRANILIC ACID ANALOGS 审中-公开
    ANTHRANILIC ACID类似物

    公开(公告)号：EP1003712A1

    公开(公告)日：2000-05-31

    申请号：EP98938288.2

    申请日：1998-08-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： LENNOX, Joseph, Richard ,  ANTANE, Schuyler, Adam ,  BUTERA, John, Anthony

    IPC分类号： C07C233/55 ,  C07D213/79

    CPC分类号： C07D213/80 ,  C07C233/55

    摘要： Compounds of formula (I) wherein: R1, R2, R3, R4, R5, R6, R7 and R8 are, independently, hydrogen, COOR15, halogen, nitro, cyano, C1-10 alkoxy, C1-10 haloalkoxy, sulfonic acid, C1-10 alkylsulfonyl, C6-12 arylsulfonyl, C6-12 aralkylsulfonyl, C1-10 alkylsulfinyl, C6-12 arylsufinyl, C6-12 aralkylsulfinyl, sulfamoyl, C1-10 alkylsulfamido, C6-12 arylsulfamido, C1-10 alkanoyl, C6-12 aryloyl, C6-12 aralkanoyl, amino, C1-10 alkylamino, C2-10 dialkylamino, C6-12 arakylamino, C6-12 arylamino, carboxamido, C1-10 alkylcarboxamido, C6-12 arylcarboxamido, C1-10 haloalkyl, C1-10 alkyl, C2-12 alkenyl, C6-12 aryl, C6-12 aralkyl; with the proviso that at least one of R4 and R5 is COOR15; R9 is hydrogen, C1-10 alkyl, and C1-10 haloalkyl; R10 is hydrogen, C1-10 alkyl, C1-10 haloalkyl, or C2-12 alkylidene; R15 is hydrogen, metal cation, acetylamido, alkoxyacetoyl or a related moiety which delivers the carboxylate in vivo; the dotted line is an optional double bond; with the proviso that when R10 is an alkylidene moiety, the double bond is absent; and W is nitrogen or carbon bearing a hydrogen, or R4, R5 or R6 as hereinbefore defined; or pharmaceutical salts thereof, are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel and chloride channel modulation.

    摘要翻译： 其中：R1，R2，R3，R4，R5，R6，R7和R8独立地为氢，COOR15，卤素，硝基，氰基，C1-10烷氧基，C1-10卤代烷氧基，磺酸， C1-10烷基磺酰基，C6-12芳基磺酰基，C6-12芳烷基磺酰基，C1-10烷基亚磺酰基，C6-12芳基磺酰基，C6-12芳烷基亚磺酰基，氨磺酰基，C1-10烷基磺酰氨基，C6-12芳基磺酰氨基，C1-10链烷酰基， 芳酰基，C6-12芳烷酰基，氨基，C1-10烷基氨基，C2-10二烷基氨基，C6-12芳烷基氨基，C6-12芳基氨基，甲酰氨基，C1-10烷基甲酰氨基，C6-12芳基甲酰氨基，C1-10卤代烷基， ，C 2-12烯基，C 6-12芳基，C 6-12芳烷基; 条件是R 4和R 5中的至少一个是COOR 15; R9是氢，C1-10烷基和C1-10卤代烷基; R10为氢，C1-10烷基，C1-10卤代烷基或C2-12亚烷基; R15是氢，金属阳离子，乙酰胺基，烷氧基乙酰基或在体内递送羧酸酯的相关部分; 虚线是可选的双键; 条件是当R 10是亚烷基部分时，双键不存在; W是氮或带有氢的碳，或如上文所定义的R4，R5或R6; 或其药用盐可用于通过钾通道和氯通道调节来治疗与平滑肌收缩相关的病症。

    DIAMINOCYCLOBUTENE-3,4-DIONES
    6.
    发明公开
    DIAMINOCYCLOBUTENE-3,4-DIONES 失效
    DIAMINOCYCLOBUTENE -3,4-二酮

    公开(公告)号：EP0796243A1

    公开(公告)日：1997-09-24

    申请号：EP95935742.0

    申请日：1995-10-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： ANTANE, Madelene, Miyoko ,  BUTERA, John, Anthony ,  HIRTH, Bradford, Hammond ,  ANTANE, Schuyler, Adam

    IPC分类号： A61K31 ,  A61P1 ,  A61P13 ,  A61P15 ,  A61P21 ,  C07C231 ,  C07C233 ,  C07C255 ,  C07C271 ,  C07C311 ,  C07D213 ,  C07D217

    CPC分类号： C07D213/75 ,  C07C233/41 ,  C07C255/60 ,  C07C271/28 ,  C07C311/08 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/42 ,  C07D217/02

    摘要： The compound of formula (I), wherein R1 and R2 are, independent from each other, hydrogen, C1-10 straight chain alkyl, C1-10 branched alkyl, or C3-10 cyclic or bicyclic alkyl; R3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms; A is selected from the group consisting of (a), wherein R4 is hydrogen, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-6 alkylamino, C2-12 dialkylamino, C1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano, carboxyl; or, A is a phenyl group of formula (b), wherein R5 and R6, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, C1-6 alkylamino, C2-12 dialkylamino, sulfamyl, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, arylcarboxamido containing 7 to 13 carbon atoms, C2 to C6 alkanoyl, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

    摘要翻译： 其中R 1和R 2彼此独立地为氢，C 1-10直链烷基，C 1-10支链烷基或C 3-10环状或双环烷基的式（I）化合物; R3是选自甲酰基，2至7个碳原子的烷酰基，3至7个碳原子的烯酰基，1至7个碳原子的烷基磺酰基，7至12个碳原子的芳酰基，9至20个的芳基烯酰基 6-12个碳原子的芳基磺酰基，8-12个碳原子的芳基烷酰基或7-12个碳原子的芳基烷基磺酰基; A选自（a），其中R4是氢，C1-6烷基，C1-6全氟烷基，C1-6烷氧基，C1-6全氟烷氧基，氨基，C1-6烷基氨基，C2-12二烷基氨基，C1 -6烷基亚磺酰氨基，含2-7个碳原子的烷基甲酰胺基，硝基，氰基，羧基; 或者A是式（b）的苯基，其中R5和R6彼此独立地选自：氰基，硝基，氨基，C1-6烷基，C1-6全氟烷基，C1-6烷氧基， C1-6全氟烷氧基，C1-6烷基氨基，C2-12二烷基氨基，氨磺酰基，C1-6烷基磺酰氨基，C6-12芳基磺酰氨基，含2-7个碳原子的烷基甲酰氨基，含7-13个碳原子的芳基甲酰氨基，C2- C6烷基磺酰基，C1-6全氟烷基磺酰基，C6-12芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基或氢; 或其药学上可接受的盐是平滑肌松弛剂。

    N-ARYL AND N-HETEROARYL-1,2-DIAMINOCYCLOBUTENE-3,4-DIONES WITH SMOOTH MUSCLE RELAXING ACTIVITIES
    7.
    发明公开
    N-ARYL AND N-HETEROARYL-1,2-DIAMINOCYCLOBUTENE-3,4-DIONES WITH SMOOTH MUSCLE RELAXING ACTIVITIES 失效
    N-ARYL- UND N-HETEROARYL - 1,2 - 二氨基胆碱酯酶-3,4-二酮麻醉剂麦克风胶原蛋白

    公开(公告)号：EP0789690A1

    公开(公告)日：1997-08-20

    申请号：EP95939108.0

    申请日：1995-10-25

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： BUTERA, John, Anthony ,  ANTANE, Schuyler, Adam ,  HIRTH, Bradford, Hammond

    IPC分类号： C07D239 ,  A61K31 ,  A61P13 ,  A61P15 ,  A61P43 ,  C07C225 ,  C07C255 ,  C07D213 ,  C07D215 ,  C07D217 ,  C07D231 ,  C07D235

    CPC分类号： C07D213/75 ,  C07C225/20 ,  C07C255/58 ,  C07C255/60 ,  C07C2601/04

    摘要： The compounds of formula (I), wherein R1 is hydrogen, C1-10 straight or branched chain alkyl, C3-10 cyclic or bicyclic alkyl, alkanoyl of 2 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms; R2 is hydrogen, C1-10 straight or branched chain alkyl or C3-10 cyclic or bicyclic alkyl; A is a group of formula (II), wherein R7 and R8, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, sulfonamide, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, C2-6 alkylcarboxamido, C7-12 arylcarboxamido, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, carboalkoxy of 2 to 7 carbon atoms, hydroxyl or hydrogen; or A is Het where Het is selected from (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), (p), wherein R9 is hydrogen, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, C1-6 alkylsulfonamido, C2-6 alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro, iodo; n is an integer from 0 to 6; R3 and R4 are, independent from each other, hydrogen, C1-10 straight or branched chain alkyl, or C3-10 cyclic or bicyclic alkyl; C1-10 perfluoro alkyl, C1-10 hydroxyalkyl, C2-10 alkoxyalkyl, fluoro; or, when taken together, form a spirocyclic ring containing a total of 3-7 carbon atoms; R5 and R6, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-12 mono- or dialkylamino, sulfonamide, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, C2-6 alkylcarboxamido, C7-12 arylcarboxamido, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl, C2-7 carboalkoxy, hydroxyl, or hydrogen; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式（I）化合物或其药学上可接受的盐是平滑肌松弛剂（I）

    INDAZOL-3-ONE-2-YL DERIVATIVES OF BENZOPYRANS
    8.
    发明授权
    INDAZOL-3-ONE-2-YL DERIVATIVES OF BENZOPYRANS 失效
    吲唑-3-酮-2-基苯并吡喃衍生物

    公开(公告)号：EP0639191B1

    公开(公告)日：1996-11-20

    申请号：EP93911065.6

    申请日：1993-05-05

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： BUTERA, John, Anthony ,  ANTANE, Schuyler, Adam

    IPC分类号： C07D405/04 ,  A61K31/415

    CPC分类号： C07D405/04 ,  A61K31/415

    摘要： The compounds of formula (I) wherein R1 is C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C2-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, or C2-12 mono- or di-alkylcarbamoyl; R2 is hydrogen, C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C2-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, or C2-12 mono- or di-alkylcarbamoyl; R3 and R4, independent from each other, are C1-6 alkyl; either R5 is hydrogen, hydroxyl, C2-6 alkanoyloxy, C7-12 aroyloxy, carbamoyloxy, formyloxy, C2-6 alkoxycarbonyloxy, C2-12 mono- or di-alkylcarbamoyloxy, and R6 is hydrogen, or R5 and R6 together are a bond; R7 and R8, independent from each other, are selected from the following: C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C1-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, C2-12 mono- or di-alkylcarbamoyl, or hydrogen; and R9 is hydrogen, C1-6 alkyl, C2-6 alkylcarbonyl or C1-6 alkylsulfonyl; or a pharmaceutically acceptable salt thereof are useful as smooth muscle relaxants, as antihypertensives and K channel activators.

    INDAZOL-3-ONE-2-YL DERIVATIVES OF BENZOPYRANS
    9.
    发明公开
    INDAZOL-3-ONE-2-YL DERIVATIVES OF BENZOPYRANS 失效
    吲唑-3-酮-2-基苯并吡喃衍生物。

    公开(公告)号：EP0639191A1

    公开(公告)日：1995-02-22

    申请号：EP93911065.0

    申请日：1993-05-05

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： BUTERA, John, Anthony ,  ANTANE, Schuyler, Adam

    IPC分类号： A61K31 ,  A61P9 ,  C07D405

    CPC分类号： C07D405/04 ,  A61K31/415

    摘要： The compounds of formula (I) wherein R1 is C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C2-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, or C2-12 mono- or di-alkylcarbamoyl; R2 is hydrogen, C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C2-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, or C2-12 mono- or di-alkylcarbamoyl; R3 and R4, independent from each other, are C1-6 alkyl; either R5 is hydrogen, hydroxyl, C2-6 alkanoyloxy, C7-12 aroyloxy, carbamoyloxy, formyloxy, C2-6 alkoxycarbonyloxy, C2-12 mono- or di-alkylcarbamoyloxy, and R6 is hydrogen, or R5 and R6 together are a bond; R7 and R8, independent from each other, are selected from the following: C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C2-6 alkoxycarbonyl, nitro, cyano, halogeno, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C1-6 alkanoylamino, C2-6 perfluoroalkanoylamino, C1-12 mono- or di-alkylamino, C1-6 alkylsulfonyl, C6-12 arylsulfonyl, carboxyl, C2-12 mono- or di-alkylcarbamoyl, or hydrogen; and R9 is hydrogen, C1-6 alkyl, C2-6 alkylcarbonyl or C1-6 alkylsulfonyl; or a pharmaceutically acceptable salt thereof are useful as smooth muscle relaxants, as antihypertensives and K channel activators.