Process for producing trans-dibenzoxenopyrrole compound and intermediate therefor
    3.
    发明授权
    Process for producing trans-dibenzoxenopyrrole compound and intermediate therefor 失效
    反式二苯并恶唑并吡咯化合物及其中间体的制备方法

    公开(公告)号:US08288564B2

    公开(公告)日:2012-10-16

    申请号:US12667654

    申请日:2008-07-07

    IPC分类号: C07D491/22

    CPC分类号: C07D313/14 C07D491/044

    摘要: The invention provides a process for production of trans-dibenzoxenopyrrole compounds, in which reduction, leaving group conversion, hydrogenation and methylation are carried out in that order. The process of the invention allows trans-dibenzoxenopyrrole compounds to be produced by a simpler procedure than conventional processes. The invention further provides novel compounds obtained as intermediates in the process, and a process for their production.

    摘要翻译: 本发明提供了制备反式二苯并恶唑并吡咯化合物的方法,其中按顺序进行还原,离去基团转化,氢化和甲基化。 本发明的方法允许通过比常规方法更简单的方法制备反式二苯并恶唑并吡咯化合物。 本发明还提供了在该方法中作为中间体获得的新化合物及其制备方法。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    5.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物,其制备方法及其应用

    公开(公告)号:US07410997B2

    公开(公告)日:2008-08-12

    申请号:US10727644

    申请日:2003-12-05

    IPC分类号: A61K31/335 C07D313/08

    摘要: Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译: 由式(1)表示的化合物,其中X为例如CH,CH 2 CHR(其中R为低级烷基或取代的低级烷基)或CRR'(其中R和 R'与上述定义的R相同); Y是例如CH,CH 2或C-O; Z是例如O,S,S-O或SO 2; U是C或N; R 1至R 4各自独立地为例如氢原子,OR,SR(其中R与上述定义相同),或芳环, 取代的芳环或杂环; R 5和R 8中的至少一个是例如OH,R 5和R 8的剩余部分, SUB>各自独立地为例如氢原子或OH,其光学异构体,其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用,例如气管平滑肌的优异的缓解作用,气道超敏反应的抑制和抑制炎症细胞浸润到气道中,另外还具有高安全性。

    Treatment method using anti-neurodegeneratively active
10-aminoaliphatyl-dibenz �b,f!oxepines
    7.
    发明授权
    Treatment method using anti-neurodegeneratively active 10-aminoaliphatyl-dibenz �b,f!oxepines 失效
    使用抗神经变性活性的10-氨基芳基 - 二苯并[b,f]氧杂七环素的治疗方法

    公开(公告)号:US5780501A

    公开(公告)日:1998-07-14

    申请号:US889769

    申请日:1997-07-08

    CPC分类号: C07D313/14

    摘要: Base-substituted dibenz�b,f!oxepines of formula I ##STR1## wherein alk is a divalent aliphatic radical, R is an amino group that is unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals or disubstituted by divalent aliphatic radicals, and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and pharmaceutically acceptable salts thereof, may be used as anti-neurodegenerative active ingredients of medicaments. The invention relates also to novel compounds of formula I.

    摘要翻译: 式I的碱取代的二苯并[b,f]氧杂七环素其中alk是二价脂族基团,R是未被取代的或被一价脂族和/或芳脂族基团单取代或二取代的氨基 或二价脂族基团二取代,R 1,R 2,R 3和R 4各自独立地为氢,低级烷基,低级烷氧基,卤素或三氟甲基及其药学上可接受的盐,可用作抗神经变性活性成分 的药物。 本发明还涉及式I的新化合物。

    Aminoalkylthiodibenzoxepins and pharmaceutical use
    8.
    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

    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。

    Azatetracyclic carbonitriles
    9.
    发明授权
    Azatetracyclic carbonitriles 失效
    氮四环碳腈

    公开(公告)号:US4492691A

    公开(公告)日:1985-01-08

    申请号:US394368

    申请日:1982-07-01

    摘要: Azatetracyclic carbonitriles of the formula ##STR1## in which R represents hydrogen, lower alkyl, cycloalkyl-lower alkyl having up to 10 carbon atoms, lower alkenyl, lower alkynyl or free, etherified or esterified hydroxy-lower alkyl, and acid addition salts thereof, processes for their manufacture, pharmaceutical compositions that contain such compounds and their use. They are distinguished especially by their central nervous system-depressant, agitation-inhibitory (amphetamine-antagonistic) action. They can therefore be used as tranquillizing, anti-psychotic, agitation-inhibitory compounds for the treatment of agitated states having various causes.

    摘要翻译: 式(I)的氮杂四环碳腈,其中R表示氢,低级烷基,具有至多10个碳原子的环烷基 - 低级烷基,低级烯基,低级炔基或游离的醚化或酯化的羟基 - 低级烷基,和酸加成 其盐,其制备方法,含有这些化合物的药物组合物及其用途。 它们特别受到其中枢神经系统抑制剂,抑制抑制(苯丙胺拮抗)作用。 因此,它们可以用作用于治疗具有各种原因的搅动状态的镇静,抗精神病,抑制激动的化合物。