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    Aryl-and heteroaryl piperazinyl carboxamides having central nervous system activity
    11.
    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：US5254552A

    公开(公告)日：1993-10-19

    申请号：US852119

    申请日：1992-03-16

    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 ,  C07D401/04 ,  C07D401/14

    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.The compounds of this invention which demonstrate selectivity at the 5-HT.sub.1A and 5-HT.sub.2 versus D.sub.2 receptor binding sites are useful as potential anxiolytic-antidepressant agents.Compounds of this invention with equal high affinity for the 5-HT.sub.1A and D.sub.2 -receptor binding sites are useful as mixed antipsychotic-anxiolytic agents.Compounds of this invention which demonstrate central cholinergic activity are useful in the treatment of senile dementia of the Alzheimer type (SDAT) and Huntingdon's chorea.

    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。 在5-HT1A和5-HT2与D2受体结合位点上证明选择性的本发明化合物可用作潜在的抗焦虑药物 - 抗抑郁剂。 对于5-HT1A和D2-受体结合位点具有相等高亲和力的本发明化合物可用作混合抗精神病药 - 抗焦虑剂。 显示中枢胆碱能活性的本发明化合物可用于治疗老年痴呆型（SDAT）和亨廷顿氏舞蹈病的老年性痴呆。

    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    15.
    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：US06376494B1

    公开(公告)日：2002-04-23

    申请号：US09723478

    申请日：2000-11-28

    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: A61K31496

    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; R1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。

    Aryl- and heteroaryl piperazinyl carboxamides having central nervous system activity
    17.
    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：US5010078A

    公开(公告)日：1991-04-23

    申请号：US493179

    申请日：1990-03-14

    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

    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。

    10,11-dihydro-5-alkyl-12-substituted-10,5-(iminomethano)-5H-d ibenzo[a,d]cycloheptenes as neuroprotectant agents
    18.
    发明授权
    10,11-dihydro-5-alkyl-12-substituted-10,5-(iminomethano)-5H-d ibenzo[a,d]cycloheptenes as neuroprotectant agents 失效
    10,11-二氢-5-烷基-12-取代-10-（亚氨基甲酰基）-5H-二苯并[a，d]环庚烯作为神经保护剂

    公开(公告)号：US4940789A

    公开(公告)日：1990-07-10

    申请号：US418591

    申请日：1989-10-10

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

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

    IPC: A61K31/55 ,  A61P25/28 ,  A61P43/00 ,  C07D471/08

    CPC classification number: C07D471/08

    Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, nitro, halo, trifluoromethyl, amino, alkylamino or dialkylamino; R.sup.2 is alkyl; R.sup.4 is alkyl, phenyl or benzyl; n is 0 or 1; m is one of the integers 0,1,2,3,4,5 or 6; and X is alkyl, alkylamino, dialkylamino, alkanoyl or substituted or unsubstituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolyl, morpholinyl, furyl thienyl, pyrrolyl, tetrahydrofuryl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl or perhydropyridminyl, in which the subsitutent is alkyl, alkoxy, halo, trifluoromethyl, cyano, nitro or hydroxy; or a pharmaceutically acceptable salt thereof; and their use in control of degenerative CNS disease states.

    Abstract translation: 本发明涉及下式的新型神经保护剂：其中R 1和R 3独立地为氢，烷基，烷氧基，羟基，氰基，硝基，卤素，三氟甲基，氨基，烷基氨基或二烷基氨基; R2是烷基; R4是烷基，苯基或苄基; n为0或1; m是整数0,1,2,3,4,5或6之一; X是烷基，烷基氨基，二烷基氨基，烷酰基或取代或未取代的苯基，吡啶基，嘧啶基，吡嗪基，喹啉基，吗啉基，呋喃基噻吩基，吡咯基，四氢呋喃基，四氢噻吩基，吡咯烷基，哌啶基，哌嗪基或全氢吡啶基，其中所述取代基是烷基， 烷氧基，卤素，三氟甲基，氰基，硝基或羟基; 或其药学上可接受的盐; 及其在控制退行性CNS疾病状态中的应用。

    Piperazinylalkylcarboxylic acid adamantylamides
    19.
    发明授权
    Piperazinylalkylcarboxylic acid adamantylamides 失效
    哌嗪基烷基羧酸金刚烷基酰胺

    公开(公告)号：US4921958A

    公开(公告)日：1990-05-01

    申请号：US413407

    申请日：1989-09-27

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

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

    IPC: C07D239/42 ,  C07D295/13 ,  C07D295/15

    CPC classification number: C07D295/13 ,  C07D239/42 ,  C07D295/15

    Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.

    Abstract translation: 下式的化合物：其中Ad是1-金刚烷基，2-金刚烷基或3-降金刚烷基; n为1,2,3,4或5; 烷基，苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，氰基，硝基或三氟甲基; R2是苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代甲基，2-，3-或4-吡啶基，2-，4-或5-嘧啶基或2- 或3-吡嗪基; R 3和R 4独立地是氢，甲基，苯基或苄基; 或其药学上可接受的盐是具有抗精神病活性成分的抗焦虑/抗抑郁药。

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