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    Hindered N-oxide esters of rapamycin
    1.
    发明授权
    Hindered N-oxide esters of rapamycin 失效
    受阻的雷帕霉素的N-氧化物酯

    公开(公告)号：US5491231A

    公开(公告)日：1996-02-13

    申请号：US345972

    申请日：1994-11-28

    申请人： Frances C. Nelson ,  Guy A. Schiehser

    发明人： Frances C. Nelson ,  Guy A. Schiehser

    IPC分类号： A61K31/435 ,  A61P9/00 ,  A61P29/00 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06 ,  C07D498/18 ,  A61K31/395 ,  C07D491/06

    CPC分类号： C07D498/18

    摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl , or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

    摘要翻译： 结构的化合物，其中R和R 1各自独立地是氢或氢; R 2和R 3各自独立地为烷基，芳基烷基，或者R 2和R 3可以一起形成环烷基环; R4是杂环N-氧化物基团，其可任选被取代; R5是烷基或芳基烷基; R 6和R 7一起形成饱和的N-烷基 - 杂环N-氧化物，其可任选被取代; k = 0-1，m = 0-1; n = 1-6; 条件是R和R 1不是氢，它们可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

    Rapamycin hydroxyesters
    2.
    发明授权
    Rapamycin hydroxyesters 失效
    雷帕霉素羟基酯

    公开(公告)号：US5362718A

    公开(公告)日：1994-11-08

    申请号：US229261

    申请日：1994-04-18

    申请人： Jerauld S. Skotnicki ,  Christina L. Leone ,  Guy A. Schiehser

    发明人： Jerauld S. Skotnicki ,  Christina L. Leone ,  Guy A. Schiehser

    IPC分类号： C07D487/18 ,  A61K31/00 ,  A61K31/435 ,  A61K31/436 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06 ,  C07D498/18 ,  A61K31/695 ,  A61K31/395 ,  C07D498/16 ,  C07D7/04

    CPC分类号： C07D498/18

    摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3 R.sup.4).sub.b (CR.sup.5 R.sup.6).sub.d CR.sup.7 R.sup.8 R.sup.9 ;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or --F;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.5 and R.sup.6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f 0R.sup.10 ;R.sup.7 is hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11 ;R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.8 and R.sup.9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f OR.sup.10 ;R.sup.10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;R.sup.11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;b=0-6;d=0-6; andf=0-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen and further provided that either R.sup.1 or R.sup.2 contains at least one --(CR.sup.3 R.sup.4).sub.f OR.sup.10, X, or --(CR.sup.3 R.sup.4).sub.f OR.sup.10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

    摘要翻译： 其中R 1和R 2各自独立地是氢或-CO（CR 3 R 4）b（CR 5 R 6）d CR 7 R 8 R 9的结构化合物 R 3和R 4各自独立地为氢，烷基，烯基，炔基，三氟甲基或-F; R 5和R 6各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 5和R 6可以一起形成X或环烷基环， 用 - （CR 3 R 4）f O R 10单取代，二取代或三取代; R 7是氢，烷​​基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11; R 8和R 9各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 8和R 9可以一起形成X或环烷基环， 用 - （CR 3 R 4）fOR 10单取代，二取代或三取代; R 10是氢，烷基，烯基，炔基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基，氯乙基或四氢吡喃基; R11是氢，烷基，烯基，炔基或苯基烷基; X是5-（2,2-二烷基）[1,3]二烷基，5-（2,2-二环烷基）[1,3]二氧杂环己基，4-（2,2-二烷基）[1,3] 4-（2,2-二环烷基）[1,3]二烷基，4-（2,2-二烷基）[1,3]二氧戊环基或4-（2,2-二环烷基）[1,3]二氧戊环基; b = 0-6; d = 0-6; 并且f = 0-6，条件是R 1和R 2都不是氢，并且进一步规定R1或R2含有至少一个 - （CR 3 R 4）fOR 10，X或 - （CR 3 R 4）fOR 10取代的环烷基，或药学上 其可接受的盐可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

    Phospholipase A2 inhibitors
    3.
    发明授权
    Phospholipase A2 inhibitors 失效
    磷脂酶A2抑制剂

    公开(公告)号：US4933365A

    公开(公告)日：1990-06-12

    申请号：US301937

    申请日：1989-01-25

    申请人： Lisa A. Marshall ,  Kurt E. Steiner ,  Guy A. Schiehser

    发明人： Lisa A. Marshall ,  Kurt E. Steiner ,  Guy A. Schiehser

    IPC分类号： A61K31/335

    CPC分类号： A61K31/335

    摘要： There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals which comprises administering to a mammal so afflicated an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms;X is ##STR2## A is --CH.sub.2 --, --O-- or --S--; m is 0-8;n is 0-7, with the proviso that m+n.ltoreq.8;or a pharmacologically acceptable salt thereof.

    摘要翻译： 公开了一种用于治疗哺乳动物的免疫炎症状况，如过敏，过敏反应，哮喘和炎症的方法，其包括向受影响的哺乳动物施用有效量的具有下式的化合物：其中R1和R2各自为 独立地是氢，羟基，低级烷基，低级烷氧基，卤代低级烷基，卤代烷基磺酰基，卤素或硝基; R3是7-12个碳原子的氢，低级烷基或芳基; X是-CH 2 - ， - O-或-S-; m为0-8; n为0-7，条件是m + n = 8; 或其药理学上可接受的盐。

    Gem-distributed esters of rapamycin
    4.
    发明授权
    Gem-distributed esters of rapamycin 失效
    雷公藤分泌的酯

    公开(公告)号：US5385910A

    公开(公告)日：1995-01-31

    申请号：US156334

    申请日：1993-11-22

    申请人： Timothy D. Ocain ,  Guy A. Schiehser

    发明人： Timothy D. Ocain ,  Guy A. Schiehser

    IPC分类号： C07D498/18 ,  A61K31/445 ,  C07D471/04

    CPC分类号： C07D498/18

    摘要： Compounds of the structure ##STR1## R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;with the proviso that R and R.sup.1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, and ##STR3## R.sup.1 is ##STR4## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;or a pharmaceutically acceptable salt thereof which are useful as immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agents.

    摘要翻译： 结构式I R和R 1的化合物各自独立地为氢，或者R 2和R 3各自独立地为烷基，芳基烷基，或者可以一起形成环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 条件是R和R 1不是氢或其药学上可接受的盐，而R 2和R 3各自独立地为氢，烷基，芳基烷基，或者可以一起形成 环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

    Fluorinated esters of rapamycin
    5.
    发明授权
    Fluorinated esters of rapamycin 失效
    雷帕霉素氟化酯

    公开(公告)号：US5100883A

    公开(公告)日：1992-03-31

    申请号：US682793

    申请日：1991-04-08

    申请人： Guy A. Schiehser

    发明人： Guy A. Schiehser

    IPC分类号： C07D498/18

    CPC分类号： C07D498/18

    摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## R.sup.3 is a mono-, di-, poly-, or per-fluorinated alkyl group with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.

    摘要翻译： 结构的化合物，其中R 1和R 2各自独立地是氢或R 3是单 - ，二 - ，多 - 或全氟化烷基，条件是R 1和R 2都不是 氢，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病; 由于其抗肿瘤活性可用于治疗实体瘤; 并且由于其抗真菌活性可用于治疗真菌感染。

    Fused heterotricyclic imides with psychotropic activity and intermedrates thereof
    6.
    发明授权
    Fused heterotricyclic imides with psychotropic activity and intermedrates thereof 失效
    融合的异三环酰亚胺具有精神活性及其中间体

    公开(公告)号：US5053508A

    公开(公告)日：1991-10-01

    申请号：US491143

    申请日：1990-03-09

    申请人： Guy A. Schiehser ,  Magid A. Abou-Gharbia ,  Charles Lin

    发明人： Guy A. Schiehser ,  Magid A. Abou-Gharbia ,  Charles Lin

    IPC分类号： C07D307/93 ,  C07D495/04 ,  C07D498/08

    CPC分类号： C07D495/04 ,  C07D307/93

    摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## R.sup.3 and R.sup.4 are hydrogen; R.sup.5 is 2-pyridinyl, 2-pyrazinyl, 2-pyrimidinyl, 3-pyridazinyl or any of the foregoing R.sup.5 moieties substituted by lower alkyl, lower alkoxy, halo lower alkyl, cyano, nitro or halo;X, Y and Z are, independently, N, S, O, NR.sup.6, SO, SO.sub.2, CR.sup.6 or CH.sub.2 ;A is lower alkylene, O or S;R.sup.6 is hydrogen, lower alkyl, aryl, aralkyl;m is 3-7;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/-anxiolytic agents having a low liability for extrapyramidal side effects.

    摘要翻译： 公开了下式的化合物：其中R 1和R 2一起代表R 3和R 4是氢; R5是2-吡啶基，2-吡嗪基，2-嘧啶基，3-哒嗪基或由低级烷基，低级烷氧基，卤代低级烷基，氰基，硝基或卤素取代的前述R5部分中的任何一个; X，Y和Z独立地是N，S，O，NR6，SO，SO2，CR6或CH2; A是低级亚烷基，O或S; R6是氢，低级烷基，芳基，芳烷基; m为3-7; 及其药学上可接受的盐，以及它们作为对锥体束外副作用具有低负荷的抗精神病药/溶血性药物的用途。

    Piperazinoisothiazolones with psychotropic activity
    7.
    发明授权
    Piperazinoisothiazolones with psychotropic activity 失效
    哌嗪异噻唑啉酮具有精神活性

    公开(公告)号：US4732984A

    公开(公告)日：1988-03-22

    申请号：US893507

    申请日：1986-08-05

    申请人： Magid A. Abou-Gharbia ,  Guy A. Schiehser ,  Scott J. Childress

    发明人： Magid A. Abou-Gharbia ,  Guy A. Schiehser ,  Scott J. Childress

    IPC分类号： C07D417/14 ,  C07D275/02 ,  C07D275/03 ,  C07D275/04 ,  C07D275/06 ,  C07D417/12 ,  C07D513/04 ,  C07D513/14

    CPC分类号： C07D275/03 ,  C07D275/04 ,  C07D275/06 ,  C07D417/12 ,  C07D513/04 ,  C07D513/14

    摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --O--, --NH--, ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.7 is 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl or phenyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, trifluoromethyl, cyano, nitro or halo, with the proviso that when R.sup.1 and R.sup.2 taken together represent ##STR3## then R.sup.7 is other than 2-pyridinyl, 2-pyrimidinyl or substituted pyrimidin-2-yl;Z is --(CH.sub.2).sub.n --, vinylene, --O--, or ##STR4## X is lower alkylene, vinylene, O or NH; m is 2-5;n is 0-4;o is 1-3;p is 1-4;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.

    摘要翻译： 公开了下式的化合物，其中R 1和R 2各自独立地是氢，低级烷基，芳基或卤素，或者R 1和R 2一起代表-CH 2 - ， - CH 2 CH 2 - ， - 其中虚线表示可选双键; + TR R 3，R 4，R 5和R 6各自独立地为氢，低级烷基，芳基或卤素; R7是2-吡啶基，2-嘧啶基，2-吡嗪基，3-哒嗪基或苯基或被低级烷基，三氟甲基，氰基，硝基或卤素取代的任何前述R 7部分，条件是当R 1和R 2一起代表 那么R 7不是2-吡啶基，2-嘧啶基或取代的嘧啶-2-基; Z是 - （CH 2）n - ，亚乙烯基，-O-或X是低级亚烷基，亚乙烯基，O或NH; m为2-5; n为0-4; o是1-3; p为1-4; 及其药学上可接受的盐，以及它们作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。

    N-alkylated benzo- and hetero-fused antisecretory agents
    8.
    发明授权
    N-alkylated benzo- and hetero-fused antisecretory agents 失效
    N-烷基化苯并 - 和异融合抗分泌剂

    公开(公告)号：US4595757A

    公开(公告)日：1986-06-17

    申请号：US681169

    申请日：1984-12-13

    申请人： Guy A. Schiehser ,  Susan T. Nielsen ,  Donald P. Strike

    发明人： Guy A. Schiehser ,  Susan T. Nielsen ,  Donald P. Strike

    IPC分类号： C07D275/06 ,  C07D295/096 ,  C07D317/58 ,  C07D513/04 ,  C07D405/12 ,  C07D417/12

    CPC分类号： C07D275/06 ,  C07D295/096 ,  C07D317/58 ,  C07D513/04

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## wherein B is a moiety having the formula ##STR3## R is H, mono- or dihalo, amino, nitro, cyano, hydroxy, trifuoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lowercycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;X is SO.sub.2, SO, S or C.dbd.O; andR.sup.2 is phenyl or 1,3-benzodioxol-5-yl;and the pharmacologically acceptable salts thereof, which are (H.sup.+ +K.sup.+)ATPase inhibitors exhibiting a cytoprotective action, are useful in the treatment of conditions where there is hypersecretion of gastric acid, such as gastric and peptic ulceration, as well as in conditions such as stress ulceration.

    摘要翻译： 其中R 1是其中B是具有式R 1的部分的式的化合物是H，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，低级烷氧基，三氟甲基，羟基 ，氨基，氰基或硝基; X是SO 2，SO，S或C = O; 并且R 2是苯基或1,3-苯并间二氧杂环戊烯-5-基; 和其药理学上可接受的盐，其是表现出细胞保护作用的（H ++ K +）ATP酶抑制剂，可用于治疗胃酸过多分泌的病症，例如胃和消化性溃疡，以及在这些病症 作为应激性溃疡。