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    2-amino-4,4-di-substituted-4h-3,1-benzoxazines
    1.
    发明授权
    2-amino-4,4-di-substituted-4h-3,1-benzoxazines 失效
    2-氨基-4,4-二取代的4H-3,1-苯并恶唑

    公开(公告)号：US3725404A

    公开(公告)日：1973-04-03

    申请号：US3725404D

    申请日：1971-06-09

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

    IPC: C07D265/18 ,  C07D87/20

    CPC classification number: C07D265/18

    Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

    Abstract translation: 2-氨基-4,4-二取代苯并恶嗪衍生物及其与生理上相容的酸的盐对中枢神经系统具有作用。 这些苯并恶嗪具有下式：其中R是氢，1-4个碳原子的烷基，环己基，苯基或苄基，R1是氢，卤素，三氟甲基，R2是1-4个碳原子的烷基，R3是苯基或卤代苯基。

    2.
    发明专利
    未知

    公开(公告)号：NO130685C

    公开(公告)日：1975-01-22

    申请号：NO17066667

    申请日：1967-11-23

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

    IPC: A61K31/00 ,  C07D93/08

    Abstract: 1,214,000. Benzothiazine derivatives. FARBWERKE HOECHST A.G. 27 Nov., 1967 [26 Nov., 1966], No. 53960/67. Heading C2C. Compounds of the general formula (R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-, A representing an alkylene group that may be interrupted by O, S, methylimino or benzylimino; R 1 = H, halogen, OMe, CF 3 or NO 2 ; R 2,3 = alkyl, cycloalkyl, phenylalkyl or phenyl, in which the phenyl group or the phenyl residue of the phenylalkyl group may be substituted by one or more substituents selected from halogen, OMe, CF 3 and NO 2 ) and their acid addition salts are prepared by (a) reacting a compound of the formula (X = Cl, Br, OH, SH, alkoxy, alkylthio or alkanoyloxy) or a salt thereof with (R values identical or different) or R.NCS or a compound capable of forming such an isothiocyanate, if necessary or desired in the presence of an acid and/or a dehydrating agent, (b) reacting a compound of the formula or a functional derivative thereof with an inorganic sulphide or, if X = SH or alkylthio, with a dehydrating agent, if necessary or desired in the presence of an acid, (c) reacting a compound of the formula (R 4 = Cl, Br, amino, SH or alkylthio) with R 1 NH 2 (R 1 = R other than H) or a salt thereof, or (d) reducing with a complex metal hydride or saponifying a compound of the formula (R 11 = alkyl, alkenyl, aryl, aralkyl, haloalkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-), the compound being reacted, before or after reduction of the acyl group, with a dialkylamine or an appropriate cyclic amine in cases where R 11 = haloalkyl, optionally followed in each case by salt formation. The, lower dialkylaminoalkyl and aminoalkyl groups (excluding any interrupting methylimino or benzylimino group in the latter case) contain up to ten carbon atoms. The isolation of intermediate thiourea derivatives in process (a) is described. The above compounds possess a depressive effect on the central nervous system, a stimulating, tranquillizing and narcosis-prolonging activity and analgesic and spasmolytic activity. They may be administered in the form of pharmaceutical preparations containing them in association with a carrier.

    4.
    发明专利
    未知

    公开(公告)号：SE329620B

    公开(公告)日：1970-10-19

    申请号：SE1601767

    申请日：1967-11-22

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

    IPC: C07D265/18 ,  C07D87/20

    Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

    5.
    发明专利
    未知

    公开(公告)号：NO119681B

    公开(公告)日：1970-06-22

    申请号：NO16327566

    申请日：1966-06-02

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SEIDL G ,  HOFFMANN I

    IPC: B02C18/06 ,  C07D219/02 ,  C07D219/04 ,  C07D219/06 ,  C07D219/14 ,  C07D265/18 ,  C07D265/38

    Abstract: (A) 3,1-Benzothiazines and 3,1-benzoxazines of gen. formula (I), where A = O or S R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl aryl, aralkyl, or lower dialkylaminoalkyl in which the dialkylamino group can also be cyclized via O, S, or methyl- or benzylimino, R1 = H, halogen, methoxy, CF3, NO2 R2 = alkyl, aralkyl, or aryl, in which the benzene rings of the last two can be substituted by halogen, methoxy, CF3, NO2. (B) Salts of I formed with organic and inorganic acids. Compounds (1) combine valuable pharmacological properties with very low toxicity. They are central depressants, as well as stimulants, sedatives, noradrenaline potentiators, analgesics and spasmolytics, and they prolong narcosis. They are useful in the treatment of mental diseases, e.g. depression, psychioneuroses, disturbances and anxiety states of neurotic and psychotic patients.

    6.
    发明专利
    未知

    公开(公告)号：FI48595B

    公开(公告)日：1974-07-31

    申请号：FI316967

    申请日：1967-11-24

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

    IPC: C07D265/18 ,  C07D87/20

    Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

    9.
    发明专利
    未知

    公开(公告)号：NO130685B

    公开(公告)日：1974-10-14

    申请号：NO17066667

    申请日：1967-11-23

    Applicant: HOECHST AG

    Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

    IPC: A61K31/00 ,  C07D93/08

    Abstract: 1,214,000. Benzothiazine derivatives. FARBWERKE HOECHST A.G. 27 Nov., 1967 [26 Nov., 1966], No. 53960/67. Heading C2C. Compounds of the general formula (R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-, A representing an alkylene group that may be interrupted by O, S, methylimino or benzylimino; R 1 = H, halogen, OMe, CF 3 or NO 2 ; R 2,3 = alkyl, cycloalkyl, phenylalkyl or phenyl, in which the phenyl group or the phenyl residue of the phenylalkyl group may be substituted by one or more substituents selected from halogen, OMe, CF 3 and NO 2 ) and their acid addition salts are prepared by (a) reacting a compound of the formula (X = Cl, Br, OH, SH, alkoxy, alkylthio or alkanoyloxy) or a salt thereof with (R values identical or different) or R.NCS or a compound capable of forming such an isothiocyanate, if necessary or desired in the presence of an acid and/or a dehydrating agent, (b) reacting a compound of the formula or a functional derivative thereof with an inorganic sulphide or, if X = SH or alkylthio, with a dehydrating agent, if necessary or desired in the presence of an acid, (c) reacting a compound of the formula (R 4 = Cl, Br, amino, SH or alkylthio) with R 1 NH 2 (R 1 = R other than H) or a salt thereof, or (d) reducing with a complex metal hydride or saponifying a compound of the formula (R 11 = alkyl, alkenyl, aryl, aralkyl, haloalkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-), the compound being reacted, before or after reduction of the acyl group, with a dialkylamine or an appropriate cyclic amine in cases where R 11 = haloalkyl, optionally followed in each case by salt formation. The, lower dialkylaminoalkyl and aminoalkyl groups (excluding any interrupting methylimino or benzylimino group in the latter case) contain up to ten carbon atoms. The isolation of intermediate thiourea derivatives in process (a) is described. The above compounds possess a depressive effect on the central nervous system, a stimulating, tranquillizing and narcosis-prolonging activity and analgesic and spasmolytic activity. They may be administered in the form of pharmaceutical preparations containing them in association with a carrier.

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