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    Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system
    1.
    发明授权
    Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system 失效
    哌嗪取代的1,4-苯并恶嗪衍生物及其在治疗中枢神经系统疾病中的应用

    公开(公告)号：US5229383A

    公开(公告)日：1993-07-20

    申请号：US748221

    申请日：1991-08-20

    申请人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    发明人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    IPC分类号： C07D265/36 ,  C07D279/16 ,  C07D471/10

    CPC分类号： C07D471/10 ,  C07D265/36 ,  C07D279/16

    摘要： The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.

    摘要翻译： 本发明涉及具有下式（I）的化合物：其中X表示-O-或-S-; R和R 1各自独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基，硝基或三卤代-C 1 -C 6烷基; R 2和R 3各自独立地是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基-C 1 -C 6烷基; 或R 2和R 3与它们所连接的氮原子一起形成任选含有另外选自氧，硫和氮的杂原子的未取代或取代的6元饱和的杂单环; R 4和R 5各自独立地是氢，卤素，硝基，氨基或三卤代-C 1 -C 6烷基; 及其药学上可接受的盐。 本发明的化合物可用于作为主要镇静剂的治疗，例如在精神病性障碍的治疗中。

    2-(piperidinylmethyl)-4-phenyl-2,3-dihydro-4H-1,4-benzoxazines useful as antipsychotics
    2.
    发明授权
    2-(piperidinylmethyl)-4-phenyl-2,3-dihydro-4H-1,4-benzoxazines useful as antipsychotics 失效
    2-（哌啶基甲基）-4-苯基-2,3-二氢-4H-1,4-苯并恶唑作为抗生素有用

    公开(公告)号：US5084454A

    公开(公告)日：1992-01-28

    申请号：US434689

    申请日：1989-10-11

    申请人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    发明人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    IPC分类号： A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61K31/5415 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  C07D265/36 ,  C07D279/16 ,  C07D413/04 ,  C07D417/04 ,  C07D471/10

    CPC分类号： C07D471/10 ,  C07D265/36 ,  C07D279/16

    摘要： The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.

    摘要翻译： PCT No.PCT / EP89 / 00130 Sec。 371日期：1989年10月11日 102（e）日期1989年10月11日PCT提交1989年2月13日PCT公布。 出版物WO89 / 07596 日本1989年8月24日。本发明涉及具有下式（I）的化合物：其中X表示-O-或-S-; R和R 1各自独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基，硝基或三卤代-C 1 -C 6烷基; R 2和R 3各自独立地是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基-C 1 -C 6烷基; 或R 2和R 3与它们所连接的氮原子一起形成任选含有另外选自氧，硫和氮的杂原子的未取代或取代的6元饱和的杂单环; R 4和R 5各自独立地是氢，卤素，硝基，氨基或三卤代-C 1 -C 6烷基; 及其药学上可接受的盐。 本发明的化合物可用于作为主要镇静剂的治疗，例如在精神病性障碍的治疗中。

    Substituted (arylalkoxybenzyl)aminopropanamide derivatives and process for their preparation
    3.
    发明授权
    Substituted (arylalkoxybenzyl)aminopropanamide derivatives and process for their preparation 失效
    取代（芳基烷氧基苄基）氨基丙酰胺衍生物及其制备方法

    公开(公告)号：US5446066A

    公开(公告)日：1995-08-29

    申请号：US215628

    申请日：1994-03-22

    申请人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    发明人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    IPC分类号： A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07C231/10 ,  C07C237/00 ,  C07C237/06 ,  C07C233/04

    CPC分类号： C07C237/00

    摘要： The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

    摘要翻译： 本发明提供新的式（I）化合物其中，条件是n为0或1〜3的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或任选被羟基取代的C 1 -C 4烷基; R 3和R 4各自独立地是氢或C 1 -C 4烷基; 或其药学上可接受的盐; 和式（IA）的化合物（IA）其中R5是氢，卤素，三氟甲基或C1-C4烷氧基，或其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的并且可以用于治疗 作为抗癫痫药，抗帕金森综合征，神经保护药，抗抑郁药，抗痉挛药和催眠药。

    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation
    7.
    发明授权
    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
    取代的（芳基烷基氨基苄基）氨基丙酰胺衍生物及其制备方法

    公开(公告)号：US5449692A

    公开(公告)日：1995-09-12

    申请号：US215694

    申请日：1994-03-22

    申请人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    发明人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    IPC分类号： A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07C231/10 ,  C07C237/06 ,  C07C233/05

    CPC分类号： C07C237/06

    摘要： The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

    摘要翻译： 本发明提供新的式（I）化合物其中n为1至4的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或C1-C4烷基; 及其药学上可接受的盐; 并且其中当R同时为氢时，R 1为氢或卤素且n为1，则R 2为氢或甲基; 和式（IA）其中R 3是卤素的式（IA）及其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的，可用于治疗作为抗癫痫药，抗帕金森病， 神经保护，抗抑郁药，抗痉挛药和催眠药。