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    Pipecolinic acid derivatives, method of manufacturing the same and therapeutic agents containing these compounds
    31.
    发明申请
    Pipecolinic acid derivatives, method of manufacturing the same and therapeutic agents containing these compounds 审中-公开
    哌啶酸衍生物，其制备方法和含有这些化合物的治疗剂

    公开(公告)号：US20010056184A1

    公开(公告)日：2001-12-27

    申请号：US09852704

    申请日：2001-05-11

    发明人： Atsushi Noda ,  Yoshinori Kobayashi ,  Tsuyoshi Tomiyama

    IPC分类号： C07D45/02 ,  C07D41/02 ,  C07D211/68 ,  C07D211/80

    CPC分类号： C07D401/12 ,  C07D211/96 ,  C07D409/12

    摘要： The present invention provides a compound of the general formula (I) or a pharmaceutical salt thereof, 1 wherein, when R1 and R2 are the same they are represented by nullO, nullN, nullOR9 (where R9 is hydrogen, lower alkyl or benzyl), when R1 and R2 are different and one of R1 and R2 is represented by hydrogen, the other is represented by nullR5nullR6null, (where R5 is nullOnull, nullNHnull, nullNHCOnull, or nullNHSO2null, and where R6 is hydrogen, lower alkyl, nullPhnullR7, null(CH2)nnullOnullPhnullR7, (where nnull1-6, R7 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or pyridyloxy), indolyl, N-oxidepyridyl, phthalimide, thienyl, or pyridyl); R3 represents nullCOOH, nullCOOEt, nullCOOMe, nullCH2N(OH)CHO, or nullCONHOH; R4 represents lower alkyl, thienyl, nullPhnullR8 (where R9 represents hydroxy, lower alkyl, lower alkoxy, nitro, halogen, pyridyloxy, or phenyl group substituted hydrogen, lower alkyl, lower alkoxy, hydroxy, and halogen), and methods of making compounds within the class of the general formula (I).

    摘要翻译： 本发明提供通式（I）的化合物或其药用盐，其中当R 1和R 2相同时，它们由= O，= N，-OR 9（其中R 9为氢，低级烷基或苄基 ），当R 1和R 2不同并且R 1和R 2之一由氢表示时，另一个由-R 5 -R 6 - （其中R 5是-O-，-NH-，-NHCO-或-NHSO 2 - ，其中R6为氢，低级烷基，-Ph-R7， - （CH2）nO-Ph-R7（其中n = 1-6，R7为氢，羟基，低级烷基，低级烷氧基，卤素，硝基或 吡啶氧基），吲哚基，N-氧化吡啶基，邻苯二甲酰亚胺，噻吩基或吡啶基）; R3表示-COOH，-COOEt，-COOMe，-CH2N（OH）CHO或-CONHOH; R 4表示低级烷基，噻吩基，-Ph-R 8（其中R 9表示羟基，低级烷基，低级烷氧基，硝基，卤素，吡啶氧基或苯基取代的氢，低级烷基，低级烷氧基，羟基和卤素） 使化合物在通式（I）的类别内。

    N-aminoalkyl-2-anthraquinonecarboxamides: new dopamine receptor subtype specific ligands
    33.
    发明授权
    N-aminoalkyl-2-anthraquinonecarboxamides: new dopamine receptor subtype specific ligands 失效
    N-氨基烷基-2-蒽醌甲酰胺：新的多巴胺受体亚型特异性配体

    公开(公告)号：US5922879A

    公开(公告)日：1999-07-13

    申请号：US995971

    申请日：1997-12-22

    申请人： Xi Chen ,  Jan William Francis Wasley

    发明人： Xi Chen ,  Jan William Francis Wasley

    IPC分类号： C07D295/12 ,  A61K31/44 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D211/70 ,  C07D215/40 ,  C07D295/13 ,  C07D211/06 ,  C07D211/68 ,  C07D211/80

    CPC分类号： C07D295/13 ,  C07D211/70 ,  C07D215/40

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy; --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.8 is hydrogen or lower alkyl;X represents an optionally substituted alkylene group; andY represents a mono-, di- or trisubsituted cyclic amino group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

    摘要翻译： 公开了下式的化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6和R7相同或不同，代表氢，卤素，烷基，烷氧基，羟基，氰基， 硝基，三氟甲基，三氟甲氧基; -O2CR'， - NHCOR'， - COR'，-SOmR'，其中R'是C1-C6烷基，其中m是0,1或2; 或R 1，R 2，R 3，R 4，R 5，R 6和R 7独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R8是氢或低级烷基; X表示任选取代的亚烷基; Y代表单，二或三取代的环状氨基，该化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的疾病 例如药物滥用和强迫症。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

    Polyalkylpiperidine containing acetic acid and 3-amino-acrylic acid derivatives
    37.
    发明授权
    Polyalkylpiperidine containing acetic acid and 3-amino-acrylic acid derivatives 失效
    含有乙酸的聚烷基哌啶和3-氨基 - 丙烯酸衍生物

    公开(公告)号：US5624981A

    公开(公告)日：1997-04-29

    申请号：US313107

    申请日：1994-10-07

    申请人： Martin Holderbaum ,  Alexander Aumueller ,  Hubert Trauth

    发明人： Martin Holderbaum ,  Alexander Aumueller ,  Hubert Trauth

    IPC分类号： C07D211/46 ,  C07D211/58 ,  C07D211/94 ,  C07D401/12 ,  C08F20/34 ,  C08K5/3432 ,  C08K5/3435 ,  C09D7/12 ,  C07D211/68 ,  C07D211/08 ,  C07D401/00 ,  C08K5/34

    CPC分类号： C07D401/12 ,  C07D211/46 ,  C07D211/94 ,  C08K5/3435 ,  C09D7/1241

    摘要： Polyalkylpiperidine-containing acetic acid and 3-aminoacrylic acid derivatives I ##STR1## where R.sup.1 is hydrogen, C.sub.1 - to C.sub.6 -alkyl, formyl, C.sub.2 - to C.sub.6 -alkanoyl, C.sub.1 - to C.sub.12 -alkoxy, C.sub.5 - to C.sub.6 -cycloalkoxy, cyanomethyl, hydroxymethyl, 2-hydroxyethyl or a radical of the formula --CR.sup.3 =CH--CO--OR.sup.4, whereR.sup.3 is hydrogen, C.sub.1 -to C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.4 andR.sup.4 is C.sub.1 - to C.sub.20 -alkyl, C.sub.5 - to C.sub.8 -cycloalkyl, C.sub.7 - to C.sub.18 -aralkyl, phenyl, tolyl or a radical of the formula --(CH.sub.2 CH.sub.2 O).sub.n H or --[CH(CH.sub.3)CH.sub.2 O].sub.n H, where n is a number from 1 to 30,X is O, NH or NR.sup.6, whereR.sup.6 is C.sub.1 - to C.sub.12 -alkyl, andY is hydrogen or a group of the formula =CH--NHR.sup.7 or =CH--NR.sup.6 R.sup.7, whereR.sup.7 is phenyl which can be substituted by one to three C.sub.1 - to C.sub.12 -alkyl, C.sub.1 - to C.sub.12 -alkoxy, halogen, cyano, hydroxyl, phenyl or groups of the formula --CO--OR.sup.5, --CO--R.sup.5, --CO--NHR.sup.5, --O--CO--R.sup.5 or --NH--CO--R.sup.5, is a 5- or 6-membered unsaturated or saturated heterocyclic ring having up to three hetero atoms from the group comprising nitrogen, oxygen and sulfur, which can additionally be benzo-fused and substituted by one to three C.sub.1 - to C.sub.12 -alkyl, C.sub.1 - to C.sub.12 -alkoxy, halogen, cyano, hydroxyl, phenyl, phenoxy or C.sub.1 - to C.sub.12 -alkoxycarbonyl are described.

    摘要翻译： PCT No.PCT / EP93 / 00739 Sec。 371日期：1994年10月7日 102（e）日期1994年10月7日PCT 1993年3月26日PCT公布。 公开号WO93 / 20051 日期：1993年10月14日含聚烷基哌啶的乙酸和3-氨基丙烯酸衍生物I其中R1是氢，C1-至C6-烷基，甲酰基，C2-至C6-烷酰基，C1-至C12-烷氧基，C5 - C6-环烷氧基，氰甲基，羟甲基，2-羟乙基或式-CR3 = CH-CO-OR4的基团，其中R3是氢，C1-C6烷基或式-CO-OR4的基团和 R 4是C 1 -C 20烷基，C 5至C 8环烷基，C 7至C 18芳烷基，苯基，甲苯基或式 - （CH 2 CH 2 O）n H或 - [CH（CH 3）CH 2 O] n H基团，其中n 是1至30的数，X是O，NH或NR 6，其中R 6是C 1 -C 12 - 烷基，Y是氢或式= CH-NHR 7或= CH-NR 6 R 7的基团，其中R 7是苯基 可被一至三个C 1至C 12烷基，C 1至C 12 - 烷氧基，卤素，氰基，羟基，苯基或式-CO-OR 5基团，-CO-R 5，-CO-NHR 5 - O-CO-R5或-NH-CO-R5是具有至多三个杂原子的5或6元不饱和或饱和杂环， 可以另外被苯并稠合并被一至三个C 1 -C 12烷基，C 1 -C 12烷氧基，卤素，氰基，羟基，苯基，苯氧基或C 1 -C 12烷氧基羰基取代的氮，氧和硫。 被描述。

    Process of synthesizing acetals
    40.
    发明授权
    Process of synthesizing acetals 失效
    合成缩醛的方法

    公开(公告)号：US5362877A

    公开(公告)日：1994-11-08

    申请号：US64990

    申请日：1993-05-24

    申请人： Atsuhiro Ohkawa

    发明人： Atsuhiro Ohkawa

    IPC分类号： B01J27/122 ,  B01J31/22 ,  C07B61/00 ,  C07D213/70 ,  C07D215/36 ,  C07D217/22 ,  C07D249/12 ,  C07D257/04 ,  C07D271/06 ,  C07D285/08 ,  C07D211/72 ,  C07D211/68 ,  C07D211/78

    CPC分类号： C07D257/04

    摘要： A process of synthetizing an acetal, which comprises reacting,i) a compound represented by formula (I); ##STR1## withii) at least one compound selected from the group consisting of paraformaldehyde, trioxane and compound represented by formula (II); ##STR2## iii) a compound represented by formula (III); ##STR3## in the presence of at least one of a Lewis acid and a metal salt to synthesize the acetal represented by formula (IV); ##STR4## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and X.sub.1 have the same meaning as those in claim (I).

    摘要翻译： 合成缩醛的方法，其包括使i）由式（I）表示的化合物; （I）与ii）至少一种选自多聚甲醛，三恶烷和由式（II）表示的化合物的化合物; （II）iii）由式（III）表示的化合物; （III）在路易斯酸和金属盐中的至少一种的存在下合成由式（IV）表示的缩醛; （IV）其中R1，R2，R3，R4和X1具有与权利要求（I）中相同的含义。