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    34.
    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.

    BENZOYL UREAS AND PROCESS FOR THEIR MANUFACTURE
    35.
    发明专利
    BENZOYL UREAS AND PROCESS FOR THEIR MANUFACTURE 未知

    公开(公告)号：ZA724294B

    公开(公告)日：1973-03-28

    申请号：ZA724294

    申请日：1972-06-22

    Applicant: HOECHST AG

    Inventor： SCHMITT K ,  HOFFMANN I

    IPC: C07D295/13 ,  C07D

    Abstract: 1368699 Benzoyl ureas FARBWERK HOECHST AG 23 June 1972 [23 June 1971] 29563/72 Heading C2C Novel compounds (I) and their salts in which R 1 represents one or more substituents selected from hydrogen, halogen, C 1-6 alkyl, C 3-6 alkenyl, C 3-7 cycloalkyl, C 4-7 cycloalkenyl, aralkyl (having 1 to 4 C atoms in the alkyl moiety), phenyl, hydroxyl, acyloxy C 1-6 alkoxy, C 3-6 alkenyloxy, aralkoxy or araloxyalkoxy (having 1 to 4 C atoms in the alkyl moiety), aryloxy, trifluoromethyl and nitro and wherein two adjacent substituents R 1 may form a carbocyclic ring having 5 to 7 ring members or an alkylene-dioxy group, R 2 represents one or more substituents selected from hydrogen, halogen, C 1-4 alkyl and C 1-4 alkoxy and A is a C 2-6 alkylene radical are prepared by (1) reaction of an R 1 substituted benzoyl-isocyanate, -carbamate, -carbamoyl halide, -thiocarbamate, -urea, -semicarbazide, or -semicarbazone with an amine of Formula II (2) an R 1 substituted benzamide is reacted with an isocyanate, carbamate, thiocarbamate, carbamoyl halide or urea each substituted by a group of Formula V (3) a correspondingly substituted benzoylisourea ether or ester, benzoyl-isothiourea ether, benzoyl-parabanic acid or benzoylhaloformic acid amidine is hydrolysed; (4) water is added to a correspondingly substituted benzoylcarbodi-imide; (5) a correspondingly substituted benzoyl-thiourea, thiobenzoyl urea or thiobenzoyl-thiourea is treated with a heavy metal oxide, heavy metal salt or an oxidizing agent to replace the sulphur atom by an oxygen atom; (6) an R 1 substituted benzoic acid or halide ester or anhydride thereof is reacted with a urea substituted by the group of Formula (V); (7) a compound IV is reacted with a piperazine VII (8) a compound VI in which B represents a radical of Formula VIII is reacted with R 2 substituted aniline; (9) a compound VI in which B is an R 2 substituted phenyl group, preferably in the form of its reactive ester is reacted with an amine of Formula IX Preferred compounds are N-(4-methoxy-benzoyl)- N 1 - [3 - (4 - m - tolyl - piperazin - 1 - yl) - propyl]- urea; N - (5 - chloro - 2 - methoxy - benzoyl) - N 1 - [3 - (4 - m - tolyl - piperazin - 1 - yl) - propyl]- urea and its hydrochloride; N-(3,4-methylenedioxy - benzoyl) - N 1 - [3 - (4 - m - tolyl - piperazine- 1-yl)-propyl] urea dihydrochloride; N-(2,5-dimethylbenzoyl) - N 1 - [3 - (4 - m - tolyl - piperazin- 1 - yl) - propyl] urea; N - (1 - naphthoyl) - N 1 - [3 - (4 - m - tolyl - piperazin - 1 - yl) - propyl]- urea; N - (5,6,7,8 - tetrahydro - 1 - naphthoyl)- N 1 - [3 - (4 - m - tolyl - piperazin - 1 - yl) - propyl]- urea. Compounds I are tranquillizers and form with a suitable carrier a pharmaceutical preparation which may be administered orally or parenterally.

    39.
    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.

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