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    11.
    发明专利
    未知

    公开(公告)号：NO119743B

    公开(公告)日：1970-06-29

    申请号：NO17066967

    申请日：1967-11-23

    Applicant: HOECHST AG

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

    IPC: 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.

    13.
    发明专利
    未知

    公开(公告)号：SE357563B

    公开(公告)日：1973-07-02

    申请号：SE1614767

    申请日：1967-11-24

    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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