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    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    3.
    发明授权
    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
    环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药

    公开(公告)号：US06518272B2

    公开(公告)日：2003-02-11

    申请号：US10107866

    申请日：2002-03-27

    Applicant: Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    Inventor： Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    IPC: A61K3150

    CPC classification number: C07D239/42 ,  C07D209/08 ,  C07D211/22 ,  C07D213/74 ,  C07D217/22 ,  C07D277/82 ,  C07D295/125 ,  C07D295/13 ,  C07D319/20

    Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1-C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是 从整数1到5中选择; R 1是任选取代的芳基或单或双环杂芳基，条件是杂芳基不是噻二唑; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; R 4是H，烷基，烯基，炔基，芳基，单或双环杂芳基，芳烷基和单或双环杂芳烷基，其中芳基或杂芳基任选被取代; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。

    Use of aryl- and heteroaryl piperazinyl carboxamides in the treatment of various central nervous system disorders
    6.
    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

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

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

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

    CPC classification number: C07D239/42 ,  C07D209/42 ,  C07D295/13

    Abstract: 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.

    Abstract translation: 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。

    Branched adamantyl and noradamantyl aryl-and aralkylpiperazines with serotonin 5-HT1A activity
    7.
    发明授权
    Branched adamantyl and noradamantyl aryl-and aralkylpiperazines with serotonin 5-HT1A activity 失效
    分支金刚烷基和去甲月桂酰基芳基 - 和芳烷基哌嗪与5-羟色胺5-HT1A活性

    公开(公告)号：US06828324B2

    公开(公告)日：2004-12-07

    申请号：US10783109

    申请日：2004-02-20

    Applicant: Wayne E. Childers, Jr. ,  Horace Fletcher, III ,  Magid A. Abou-Gharbia ,  John P. Yardley

    Inventor： Wayne E. Childers, Jr. ,  Horace Fletcher, III ,  Magid A. Abou-Gharbia ,  John P. Yardley

    IPC: A61K31495

    CPC classification number: C07D239/42 ,  A61K31/496 ,  C07D295/13

    Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection. The compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明提供了使用它们提供神经保护并预防或限制哺乳动物（包括阿尔茨海默氏病，亨廷顿病，帕金森病，艾滋病痴呆，视网膜疾病，糖尿病性周围神经病，多发性硬化，中风，急性血栓栓塞性中风等）的神经退行性进程的化合物和方法。 局灶缺血，全身缺血，短暂性脑缺血发作，手术导致的局部缺血，头部外伤，脊柱创伤，缺氧，胎儿缺氧和神经保护。 具有以下结构的化合物：其中X为-CH 2 - 或键; Y是 - （CH 2）m - 或 - （CH 2）-O-（CH 2） - ; m 0或1; n为0或1; R 1和R 2独立地选自任选取代的芳基或杂芳基; 光学异构体及其药学上可接受的盐。

    Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity
    10.
    发明授权
    Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity 失效
    具有中枢神经系统活性的芳基和杂芳基哌嗪基甲酰胺

    公开(公告)号：US5380725A

    公开(公告)日：1995-01-10

    申请号：US91495

    申请日：1993-07-14

    Applicant: Magid A. Abou-Gharbia ,  John P. Yardley ,  Wayne E. Childers, Jr.

    Inventor： Magid A. Abou-Gharbia ,  John P. Yardley ,  Wayne E. Childers, Jr.

    IPC: C07D209/42 ,  C07D239/42 ,  C07D295/13 ,  A61K31/495 ,  C07D295/145 ,  C07D403/12

    CPC classification number: C07D239/42 ,  C07D209/42 ,  C07D295/13

    Abstract: There are disclosed 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 and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, 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; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.

    Abstract translation: 公开了式（I）的化合物其中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 和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是未取代或取代的苯基，苄基，吡啶基，嘧啶基或吡嗪基，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; m是2至5的整数; 及其药学上可接受的盐。

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