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21 条记录 (耗时 0.025 秒)

    Process for producing triazolylbenzophenone derivatives
    3.
    发明授权
    Process for producing triazolylbenzophenone derivatives 失效
    生产三唑并苯酮衍生物的方法

    公开(公告)号：US4143048A

    公开(公告)日：1979-03-06

    申请号：US861009

    申请日：1977-12-15

    申请人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07D249/14

    CPC分类号： C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00 ,  Y10S514/906

    摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n --X--R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen, nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.

    Triazolylbenzophenone derivatives and production thereof
    7.
    发明授权
    Triazolylbenzophenone derivatives and production thereof 失效
    三唑基二苯甲酮衍生物及其制备

    公开(公告)号：US4147700A

    公开(公告)日：1979-04-03

    申请号：US861011

    申请日：1977-12-15

    申请人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07D249/14

    CPC分类号： C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00 ,  Y10S514/906

    摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n --X--R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen, nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.

    摘要翻译： 下式的三唑基二苯甲酮衍生物：其中R表示氢，C1-C6烷基，C1-C6卤代烷基，基团 - （CH2）nX-R5或基团R5表示氢，C1-C6 烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 6 -C 10芳基或C 2 -C 8酰基; X表示硫或氧; n表示0,1,2或3; R 6和R 7各自表示氢或C 1 -C 6 烷基;或者“IMAGE”代表吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基; R1代表氢或卤素; R2代表卤素，硝基或三氟甲基; R3代表C1-C6烷基，C1-C6卤代烷基，C1 -C 6叠氮基 - 烷基，C 6 -C 10芳基，C 2 -C 8酰基或者R 4和R 8各自表示氢，C 1 -C 6烷基或C 7 -C 10芳烷基; R 9表示氢或C 1 -C 6烷基; R 10 表示氢，C1-C6烷基，C7-C10芳烷基或C2-C11α-氨基酰基;或者“IMAGE”代表苯二甲酰亚氨基，吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基）及其药学上可接受的 酸加成盐，可用作抗焦虑剂，镇静剂，催眠药，抗惊厥药，肌肉松弛剂，抗抑郁药，其合成中间体及其制备。

    Heteroaromatic derivatives having an inhibitory activity against HIV integrase
    8.
    发明授权
    Heteroaromatic derivatives having an inhibitory activity against HIV integrase 有权
    对HIV整合酶具有抑制活性的杂芳族衍生物

    公开(公告)号：US07098201B2

    公开(公告)日：2006-08-29

    申请号：US10463816

    申请日：2003-06-18

    申请人： Toshio Fujishita ,  Tomokazu Yoshinaga ,  Akihiko Sato

    发明人： Toshio Fujishita ,  Tomokazu Yoshinaga ,  Akihiko Sato

    IPC分类号： A61K31/33

    CPC分类号： C07D403/06 ,  C07D333/24 ,  C07D333/34

    摘要： A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

    摘要翻译： 式（I）的化合物：其中X是羟基，保护的羟基或任选取代的氨基; Y是-COOR A A，其中R A是氢或酯残基，其中R 1，R 2， 各自独立地为氢或酰胺残基，任选取代的芳基或任选取代的杂芳基; 且A 1是任选取代的杂芳基; 不包括其中Y和/或A 1是任选取代的吲哚-3-基的化合物，其互变异构体，前药，药学上可接受的盐或其水合物对整合酶具有抑制活性 。

    Heteroaromatic derivatives having an inhibitory activity against HIV integrase
    9.
    发明授权
    Heteroaromatic derivatives having an inhibitory activity against HIV integrase 失效
    对HIV整合酶具有抑制活性的杂芳族衍生物

    公开(公告)号：US06645956B1

    公开(公告)日：2003-11-11

    申请号：US10288380

    申请日：2002-11-06

    申请人： Toshio Fujishita ,  Tomokazu Yoshinaga ,  Akihiko Sato

    发明人： Toshio Fujishita ,  Tomokazu Yoshinaga ,  Akihiko Sato

    IPC分类号： A61K3133

    CPC分类号： C07D403/06 ,  C07D333/24 ,  C07D333/34

    摘要： A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteoaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

    摘要翻译： 式（I）的化合物：其中X是羟基，保护的羟基或任选取代的氨基; Y是-COOR A，其中R A是氢或酯残基，-CONR R C，其中R B和R C各自独立地是氢或酰胺残基，任选取代的芳基或任选的 取代的杂芳基; 并且A 1是任选取代的杂芳基; 除了其中Y和/或A 1是任选取代的吲哚-3-基的化合物被排除，其互变异构体，前药，药学上可接受的盐或其水合物对整合酶具有抑制活性。

    Indole derivatives with antiviral activity
    10.
    发明授权
    Indole derivatives with antiviral activity 失效
    具有抗病毒活性的吲哚衍生物

    公开(公告)号：US06333323B1

    公开(公告)日：2001-12-25

    申请号：US09622543

    申请日：2000-08-18

    申请人： Toshio Fujishita ,  Tomokazu Yoshinaga

    发明人： Toshio Fujishita ,  Tomokazu Yoshinaga

    IPC分类号： A61K31535

    CPC分类号： C07D403/06 ,  C07D209/12 ,  C07D209/18 ,  C07D209/20 ,  C07D209/22

    摘要： A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.

    摘要翻译： 下式的化合物：其中R 1是氢，低级烷基或任选取代的芳基磺酰基等，R 2是氢，低级烷基或任选取代的芳烷基等，R 3，R 4，R 5和R 6各自独立地是氢 ，卤素，三卤代低级烷基等，X为羟基或任选取代的氨基，Y为COOR R为氢或酯残基），任选取代的芳基或任选取代的杂芳基，具有整合酶抑制活性，可用作 抗艾滋病药物。