Tetrahydro-benzthiazoles, the preparation thereof and their use as
intermediate products or as pharmaceuticals
    21.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑,其制备方法及其作为中间产物或药物的用途

    公开(公告)号:US4886812A

    公开(公告)日:1989-12-12

    申请号:US256671

    申请日:1988-10-12

    IPC分类号: A61K31/425 C07D277/82

    CPC分类号: C07D277/82

    摘要: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译: 本发明涉及通式为(I)的新的四氢苯并噻唑,其中R 1表示氢原子,烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而上述苯基核酸 可各自被1或2个卤素原子取代,R2表示氢原子或烷基,R3表示氢原子,烷基,环烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基 基团可以被氟,氯或溴原子取代,R4表示氢原子,烷基,烷基或烯基,或者R3和R4与它们之间的氮原子一起代表吡咯烷子基,哌啶子基, 六亚甲基亚氨基或吗啉代基,其对映异构体及其酸加成盐。 上述通式I的化合物,其中R1或R3基团或R1和R3两个基团之一表示酰基,是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    Tetrahydro-benzthiazoles, the preparation thereof and their use as
intermediate products or as pharmaceuticals
    22.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑,其制备方法及其作为中间产物或药物的用途

    公开(公告)号:US4731374A

    公开(公告)日:1988-03-15

    申请号:US810947

    申请日:1985-12-19

    IPC分类号: A61K31/425 C07D277/82

    CPC分类号: C07D277/82

    摘要: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译: 本发明涉及通式为(I)的新的四氢苯并噻唑,其中R 1表示氢原子,烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而上述苯基核 可各自被1或2个卤素原子取代,R2表示氢原子或烷基,R3表示氢原子,烷基,环烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基 基团可以被氟里酰,氯或溴原子取代,R4表示氢原子,烷基,烷基或烯基,或者R3和R4与它们之间的氮原子一起代表吡咯烷子基,哌啶子基, 六亚甲基亚氨基或吗啉代基,其对映异构体及其酸加成盐。 上述通式I的化合物,其中R1或R3基团或R1和R3两个基团之一表示酰基,是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    Tetrahydro-benzthiazoles, the preparation thereof and their use as
intermediate products or as pharmaceuticals
    23.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑,其制备方法及其作为中间产物或药物的用途

    公开(公告)号:US4843086A

    公开(公告)日:1989-06-27

    申请号:US124197

    申请日:1987-11-23

    IPC分类号: A61K31/425 C07D277/82

    CPC分类号: C07D277/82

    摘要: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms.R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译: 本发明涉及通式为(I)的新的四氢苯并噻唑,其中R 1表示氢原子,烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而上述苯基核 可各自被1或2个卤素原子取代。 R2表示氢原子或烷基,R3表示氢原子,烷基,环烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而苯基核可以被氟取代 ,氯或溴原子,R4表示氢原子,烷基,烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基,哌啶子基,六亚甲基亚氨基或吗啉代基,对映体和酸加成 的盐。 上述通式I的化合物,其中R1或R3基团或R1和R3两个基团之一表示酰基,是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。