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    Carbamates of rapaycin
    43.
    发明授权
    Carbamates of rapaycin 失效
    高分子化合物的氨基甲酸酯

    公开(公告)号：US5559227A

    公开(公告)日：1996-09-24

    申请号：US449593

    申请日：1995-05-24

    申请人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    发明人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    IPC分类号： A61K31/395 ,  A61K31/44 ,  A61K31/675 ,  C07D491/06 ,  C07D498/04 ,  C07D498/16

    CPC分类号： A61K31/70

    摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12 and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ting may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

    摘要翻译： 结构式II的化合物，其中R 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11或者或者-CONR 3 R 13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R17是或-C 3BOND C-R21; R 18，R 19，R 20和R 21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基，其中该杂环可以任意地含有杂环中的NR 22，并且该环碳可任选地被烷基，芳烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2都不是氢，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。

    Venlafaxine in the inducement of cognition enhancement
    45.
    发明授权
    Venlafaxine in the inducement of cognition enhancement 失效
    文拉法辛诱导认知增强

    公开(公告)号：US5530013A

    公开(公告)日：1996-06-25

    申请号：US442546

    申请日：1995-05-16

    申请人： G. E. Morris Husbands ,  Magid A. Abou-Gharbia ,  John A. Moyer ,  Eric A. Muth

    发明人： G. E. Morris Husbands ,  Magid A. Abou-Gharbia ,  John A. Moyer ,  Eric A. Muth

    IPC分类号： A61K31/135 ,  A61K31/41

    CPC分类号： A61K31/135

    摘要： This invention provides a method of inducing cognition enhancement in a mammal by administering to the mammal experiencing a cognition impairment an effective amount of a hydroxycycloalkanephenethyl amine compound of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## wherein the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl, or alkanol;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3, or 4;or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供了通过向经历认知障碍的哺乳动物施用有效量的以下结构式的羟基环烷基甲苯胺化合物来诱导哺乳动物认知增强的方法：不饱和度; R1是氢或烷基; R2是烷基; R4是氢，烷基，甲酰基或烷醇; R 5和R 6独立地是氢，羟基，烷基，烷氧基，烷酰氧基，氰基，硝基，烷基巯基，氨基，烷基氨基，二烷基氨基，烷酰氨基，卤素，三氟甲基或一起，亚甲基二氧基; R7是氢或烷基; 且n为0,1,2,3或4; 或其药学上可接受的盐。

    Carbamates of rapamycin
    46.
    发明授权
    Carbamates of rapamycin 失效

    公开(公告)号：US5484790A

    公开(公告)日：1996-01-16

    申请号：US448812

    申请日：1995-05-24

    申请人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    发明人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    IPC分类号： A61K31/395 ,  A61K31/44 ,  A61K31/675 ,  C07D491/06 ,  C07D498/04 ,  C07D498/16

    CPC分类号： A61K31/70

    摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

    Carbamates of rapamycin
    47.
    发明授权
    Carbamates of rapamycin 失效
    雷帕霉素的氨基甲酸酯

    公开(公告)号：US5480988A

    公开(公告)日：1996-01-02

    申请号：US284764

    申请日：1994-08-02

    申请人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    发明人： Amedeo A. Failli ,  Oleg I. Bleyman ,  Wenling Kao ,  Magid A. Abou-Gharbia

    IPC分类号： A61K31/395 ,  A61K31/44 ,  A61K31/675 ,  C07D491/06 ,  C07D498/04 ,  C07D498/16

    CPC分类号： A61K31/70

    摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.4 R.sup.5).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## --R.sup.12, or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, p--OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, Tri-(alkyl)silyethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each independently, hydrogen or alkyl; ##STR3## R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyll, arylalkyl, halogen, --CF.sub.3, ---OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, anti inflammatory, antifungal, antiproliferative, and antitumor agent.

    摘要翻译： 结构式II的化合物，其中R 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 4 R 5）n（CR 8 R 9）pNR 10 R 11或CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11， 或 -R12或-CONR3R13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，p-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R18，R19，R20和R21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基，其中该杂环可以在杂环中任选地含有NR 22，并且该环碳可任选地被烷基，芳烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2都不是氢，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。

    Use of aryl- and heteroaryl piperazinyl carboxamides in the treatment of various central nervous system disorders
    48.
    发明授权
    Use of aryl- and heteroaryl piperazinyl carboxamides in the treatment of various central nervous system disorders 失效
    芳基和杂芳基哌嗪基甲酰胺在治疗各种中枢神经系统疾病中的应用

    公开(公告)号：US5106849A

    公开(公告)日：1992-04-21

    申请号：US689409

    申请日：1991-04-22

    申请人： Magid A. Abou-Gharbia ,  John P. Yardley ,  Wayne E. Childers, Jr. ,  John A. Moyer

    发明人： Magid A. Abou-Gharbia ,  John P. Yardley ,  Wayne E. Childers, Jr. ,  John A. Moyer

    IPC分类号： C07D209/42 ,  C07D239/42 ,  C07D295/13

    CPC分类号： C07D239/42 ,  C07D209/42 ,  C07D295/13

    摘要： There are disclosed the use of the compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了式（I）化合物（I）的用途，其中R1是1-金刚烷基，3-甲基-1-金刚烷基，3-降金刚烷基，未取代的或取代的-2-吲哚基，3-吲哚基 2-苯并呋喃基或3-苯并呋喃基，其中取代基选自低级烷基，低级烷氧基和卤素; R2是未取代的或取代的苯基，苄基或嘧啶基，其中取代基选自低级烷基，低级烷氧基，三氟甲基和卤素; R3是H或1〜3个碳原子的低级烷基; n是整数0或1; 且m为2至5的整数及其药学上可接受的盐。

    Polycyclic phenalkyl amines as psychotropic agents
    49.
    发明授权
    Polycyclic phenalkyl amines as psychotropic agents 失效
    多环苯烷基胺作为精神药物

    公开(公告)号：US5036070A

    公开(公告)日：1991-07-30

    申请号：US537551

    申请日：1990-06-13

    申请人： Magid A. Abou-Gharbia

    发明人： Magid A. Abou-Gharbia

    IPC分类号： C07D239/42 ,  C07D241/20 ,  C07D295/092 ,  C07D319/20

    CPC分类号： C07D239/42 ,  C07D241/20 ,  C07D295/088 ,  C07D319/20

    摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, or phenyl, or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 -- or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, alkyl, alkoxy, or halo;Z is oxygen, or --N(R.sup.6), where R.sup.6 is hydrogen or alkyl;m is 1-4;n is 0-2; ##STR3## wherein R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl, or diphenylmethyl, where the substituents are selected from the group of alkyl, alkoxy, halo, cyano, nitro and trifluoromethyl;R.sup.8 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, or NHR.sup.9 where R.sup.9 is hydrogen, alkyl, phenyl, tolyl, xylyl, mesityl, methoxyphenyl, or halophenyl with the proviso when Z is oxygen, R.sup.7 is other than phenyl or pyridyl;or a pharmaceutically acceptable salt thereof, which by virtue of high affinity for the dopamine D-2 receptor and the serotonin 5-HT-.sub.1A receptor, are useful as antipsychotic and anxiolytic agents for the treatment of a variety of central nervous system disorders such as paranoia, schizophrenia, anxiety, sleep disorders, and related problems.

    摘要翻译： 公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，烷基或苯基，或者R 1和R 2一起表示 - （CH 2）4 - 或，其中虚线表示任选的 双键; R3是氢，烷基，烷氧基或卤素; Z是氧或-N（R6），其中R6是氢或烷基; m为1-4; n为0-2; 其中R 7为未取代或取代的苯基，2-吡啶基，2-嘧啶基，2-吡嗪基，3-哒嗪基或二苯基甲基，其中取代基选自烷基，烷氧基，卤素，氰基， 硝基和三氟甲基; R8是氢，羟基，氰基，烷基，烷氧基，卤素或NHR9，其中R9是氢，烷基，苯基，甲苯基，二甲苯基，三甲苯基，甲氧基苯基或卤代苯基，条件是Z是氧时，R7不是苯基或吡啶基 ; 或其药学上可接受的盐，其由于对多巴胺D-2受体和5-羟色胺5-HT-1A受体的高亲和力可用作抗精神病药和抗焦虑剂，用于治疗各种中枢神经系统疾病，例如 偏执狂，精神分裂症，焦虑症，睡眠障碍和相关问题。