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421 条记录 (耗时 0.028 秒)

    Process for the chemical resolution of 5-alkoxy-substituted (+)-1,3-dimethyloxindolylethylamines
    91.
    发明授权
    Process for the chemical resolution of 5-alkoxy-substituted (+)-1,3-dimethyloxindolylethylamines 失效
    5-烷氧基取代的（+） - 1,3-二甲基氧基二乙胺的化学拆分方法

    公开(公告)号：US5387695A

    公开(公告)日：1995-02-07

    申请号：US022605

    申请日：1993-02-17

    申请人： Thomas B. K. Lee ,  George S. K. Wong

    发明人： Thomas B. K. Lee ,  George S. K. Wong

    IPC分类号： C07B57/00 ,  C07D209/34

    CPC分类号： C07D209/34

    摘要： A process for chemically resolving a mixture of enantiomers of primary amines, such as enantiomers of 1,3-dimethyl-5-methoxyoxindolylethylamine, provides one of the enantiomers in the form of a tartaric acid salt. In carrying out the process, an enantiomeric mixture is contacted with a chiral acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The resulting precipitate can then be recovered. The chiral acid is selected from the group consisting of dibenzoyl-D-tartaric acid, dibenzoyl-L-tartaric acid, ditoluoyl-D-tartaric acid, and ditoluoyl-L-tartaric acid. The precipitates can be used in the synthesis of stereospecific forms of physostigmine.

    摘要翻译： 用于化学拆分伯胺对映异构体如1,3-二甲基-5-甲氧基吲哚基乙胺的对映异构体的混合物的方法提供酒石酸盐形式的一种对映异构体。 在进行该方法时，将对映异构体混合物与手性酸接触，其量足以优先沉淀手性酸盐和其中一种对映异构体。 然后可以回收所得沉淀。 手性酸选自二苯甲酰基-D-酒石酸，二苯甲酰基-L-酒石酸，二甲氧基-D-酒石酸和二甲酰基-L-酒石酸。 沉淀物可用于立体特异性形式的毒扁豆碱合成。

    3-<4-substituted-4-piperazinyl)buty]-4-thiazolidinone and related compounds
    93.
    发明授权
    3-<4-substituted-4-piperazinyl)buty]-4-thiazolidinone and related compounds 失效
    3- [4-取代-4-哌嗪基]丁基] -4-噻唑烷酮及相关化合物

    公开(公告)号：US5371087A

    公开(公告)日：1994-12-06

    申请号：US85273

    申请日：1993-06-29

    申请人： Nicholas J. Hrib ,  John G. Jurcak

    发明人： Nicholas J. Hrib ,  John G. Jurcak

    IPC分类号： A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D277/14 ,  C07D277/60 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  A61K31/50 ,  C07D401/00 ,  C07D403/00

    CPC分类号： C07D277/60 ,  C07D277/14 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14

    摘要： There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

    摘要翻译： 公开了下式的化合物，其中n为0,1或2; 其中每次出现的X独立为氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; Y在每次出现时独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基氰基，三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢，低级烷基，低级或芳基，除了当R 1是芳基或芳基时，R 2是氢，或者R 1 + R 2与它们所连接的碳原子一起形成环戊烷，环己烷 ，环庚烷，吡喃，噻喃，茚满或哌啶环; R3和R4独立地是氢或低级烷基，或者R3 + R4与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，吡咯烷或哌啶环，术语表示未取代的苯基的芳基 或被1,2或3个取代基取代的苯基，各自独立地为低级烷基，低级烷氧基，羟基，卤素，低级烷硫基，氰基，氨基或三氟甲基，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。

    Heteroaryl-8-azabicyclo[3,2,1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin
    95.
    发明授权
    Heteroaryl-8-azabicyclo[3,2,1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin 失效
    杂芳基-8-氮杂双环[3,2,1]辛烷作为抗精神病药，5-HT3受体拮抗剂和5-羟色胺再摄取抑制剂

    公开(公告)号：US5334599A

    公开(公告)日：1994-08-02

    申请号：US37134

    申请日：1993-03-25

    申请人： Edward J. Glamkowski ,  David M. Fink ,  Barbara E. Kurys ,  Yulin Chiang

    发明人： Edward J. Glamkowski ,  David M. Fink ,  Barbara E. Kurys ,  Yulin Chiang

    IPC分类号： C07D451/02 ,  C07D401/04 ,  A61K31/46 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D451/02

    摘要： This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifiuoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifiuoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.

    摘要翻译： 本发明涉及式（I）的化合物，其中X是-O - ， - S-或-NH-; Y是氢，卤素和低级烷氧基; p为1或2; n为2,3或4; R是氢，低级烷基，低级烷氧基，羟基，卤素，氨基，低级烷基氨基，硝基，低级烷硫基，三氟甲氧基，氰基，三氟甲基，R1是氢，低级烷基，低级烷氧基，卤素，羟基，羧基，低级烷基氨基，硝基，低级烷硫基，氰基 和三氟甲基; m为1或2; 其药学上可接受的酸加成盐，以及适用的几何和旋光异构体及其外消旋混合物。 本发明的化合物和组合物可用作5-HT 3受体拮抗剂的抗精神病药和5-羟色胺再摄取的抑制剂。

    Process of preparing 2,6-methano-1,3-benzodiazocine compounds
    97.
    发明授权
    Process of preparing 2,6-methano-1,3-benzodiazocine compounds 失效
    制备2,6-亚甲基-1,3-苯并二氮辛腈的方法

    公开(公告)号：US5264575A

    公开(公告)日：1993-11-23

    申请号：US901638

    申请日：1992-06-19

    申请人： Richard C. Allen ,  Marc N. Agnew ,  David M. Fink

    发明人： Richard C. Allen ,  Marc N. Agnew ,  David M. Fink

    IPC分类号： C07D471/08 ,  C07D221/02

    CPC分类号： C07D471/08

    摘要： Novel 2,6-methano-1,3-benzodiazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain and for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease, utilizing compounds or compositions thereof are disclosed.

    摘要翻译： 新颖的2,6-亚甲基-1,3-苯并二氮杂环丁烷，中间体，其制备方法，利用化合物或组合物，减轻疼痛和减轻胆碱能功能降低的各种记忆障碍功能如阿尔茨海默病的方法， 披露

    Alkylamino- and alkylamino alkyl diarylketones and pharmaceutical compositions thereof
    99.
    发明授权
    Alkylamino- and alkylamino alkyl diarylketones and pharmaceutical compositions thereof 失效
    烷基氨基和烷基氨基烷基二芳基酮及其药物组合物

    公开(公告)号：US5177111A

    公开(公告)日：1993-01-05

    申请号：US643631

    申请日：1991-01-22

    申请人： R. Richard L. Hamer ,  Brian Freed ,  Richard C. Allen

    发明人： R. Richard L. Hamer ,  Brian Freed ,  Richard C. Allen

    IPC分类号： C07C45/00 ,  C07C45/45 ,  C07C49/233 ,  C07C49/80 ,  C07C217/86 ,  C07C225/16 ,  C07C225/22

    CPC分类号： C07C225/22 ,  C07C217/86 ,  C07C225/16 ,  C07C45/004 ,  C07C45/455 ,  C07C49/233 ,  C07C49/80

    摘要： This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula ##STR1## where Ar is aryl of the formula ##STR2## where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF.sub.3, NO.sub.2 and u is an integer of 1 to 3; X and Y are independently CH.sub.2 --, --CF.sub.2 -- or --CHF--; Z and W are independently --CH.sub.2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1, R.sub.1 is H or loweralkyl; R.sub.2 and R.sub.3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.

    摘要翻译： 本发明涉及式IMA的烷基氨基和烷基氨基烷基二芳基酮，其中Ar是下式的芳基：其中V是氢，卤素，低级烷基，低级烷氧基，CF 3，NO 2，u是1至3的整数; X和Y独立地是CH 2 + 13，-CF 2 - 或-CHF-; Z和W独立地是-CH 2 - ， - O - ， - CHOH-或-CHF-; m，n，p，q和t分别为0或1，R1为H或低级烷基的整数; R2和R3是低级烷基; 和其药学上可接受的酸加成盐，并且在适用的情况下为其几何和旋光异构体及其外消旋混合物。 本发明的化合物显示出作为镇痛剂的用途，并且作为减轻各种记忆功能障碍的药剂，其特征在于胆碱能功能降低，如阿尔茨海默病。

    Aminoalkylthiodibenzoxepins and pharmaceutical use
    100.
    发明授权
    Aminoalkylthiodibenzoxepins and pharmaceutical use 失效
    氨基烷基硫代二苯并氧氮皮素和药物用途

    公开(公告)号：US5140027A

    公开(公告)日：1992-08-18

    申请号：US522932

    申请日：1990-05-14

    申请人： Helen H. Ong ,  Vernon B. Anderson ,  James A. Profitt

    发明人： Helen H. Ong ,  Vernon B. Anderson ,  James A. Profitt

    IPC分类号： C07D313/14

    CPC分类号： C07D313/14

    摘要： Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.

    摘要翻译： 公开了新的氨基烷基硫代二氧化硫蛋白，其生理上可耐受的酸加成盐，其制备方法，包括其的药物和兽医制剂以及通过施用方法进行治疗。 这些化合物可用作镇痛药，抗抑郁药和抗惊厥药。 还公开了一种通过碱金属在低级烷醇中选择性还原烯烃的方法。