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    21.
    发明专利
    未知

    公开(公告)号：BR7202216D0

    公开(公告)日：1973-07-17

    申请号：BR221672

    申请日：1972-04-14

    Applicant: HOECHST AG

    Inventor： KUCH H ,  HOFFMANN I

    IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07D53/04 ,  C07F9/28 ,  A61K27/00

    Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

    23.
    发明专利
    未知

    公开(公告)号：AR192762A1

    公开(公告)日：1973-03-14

    申请号：AR24144572

    申请日：1972-04-13

    Applicant: HOECHST AG

    Inventor： KUCH H ,  HOFFMANN I

    IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645

    Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

    25.
    发明专利
    未知

    公开(公告)号：NO121721B

    公开(公告)日：1971-04-05

    申请号：NO16798067

    申请日：1967-05-03

    Applicant: HOECHST AG

    Inventor： ERHART G ,  SCHMITT K ,  HOFFMANN I ,  OTT H

    IPC: C07D217/02 ,  C07D217/04 ,  C07D217/14 ,  C07D217/16

    Abstract: 1,164,192. 4-Phenyl-tetrahydroquinoline derivatives. FARBWERKE HOECHST A.G. 5 May, 1967 [5 May, 1966; 12 Aug., 1966; 15 April, 1967 (2)], No. 21016/67. Heading C2C. Novel compounds of the Formula (I) wherein R is H or alkyl, R 1 is H, acyl of a saturated or unsaturated C 2-6 aliphatic, aromatic or araliphatic carboxylic acid, C 1-5 alkyl, C 7-10 aralkyl; R 2 and R 2 1 may be the same or different and each represent H, halogen, OH, CF 3 , C 1-5 alkyl or alkoxy, C 7-10 aralkoxy, or R 2 and R 2 1 together represent C 1-2 alkylenedioxy; R 3 and R 4 are identical or different and represent H, C 1-5 alkyl, phenyl, or C 7-10 aralkyl, and R 5 is H, halogen, OH, CF 3 , NO 2 , C 1-4 alkyl or alkoxy, or C 7-10 aralkoxy; or a salt thereof, are obtained by (a) effecting ring closure in a compound of the Formula (II) where X is -CHOH, optionally esterified by a sulphonic or carboxylic acid, or a CH-halogen group, by treating it with an acid condensing agent, or (b) treating a compound of the Formula I above (but where R 1 is H and R 4 is not H) with an agent for introducing the acyl radical of a saturated or unsaturated aliphatic carboxylic acid of up to 6 carbon atoms, an aromatic or araliphatic carboxylic acid, or (c) reducing by means of a complex metal hydride, a compound of general Formula IV in which R, R 1 , R 2 , R 2 1, R 4 and R 5 have the meanings given above and R 4 may also represent hydrogen, and, if desired, treating with an alkylating agent a compound of the general Formula I, in which R 1 and/or R 4 represent a hydrogen atom, or by separating in known manner benzyl radicals from a compound of the general Formula I, in which the R 1 and/or R 4 represents benzyl radicals, and/or treating with an ether splitting agent a compound of the general Formula I, in which R 2 , R 2 1 and/or R 5 represent alkoxy or aralkoxy groups, and, if desired, converting the salt obtained into the free base or converting the free base obtained into a physiologically tolerable salt by a treatment with an acid. The following intermediates are also described:- (a) N - (2 - Amino - benzyl) - 1 - phenyl - 2 - methylamino-propanol- (1) is obtained (1) by reducing N - (2 - aminobenzyl) - 2 - methylamino-propiophenone with NaBH 4 , or (ii) by reacting 2-nitrobenzyl chloride with 1-phenyl-2- methylamino-propanol-(1) to yield N-(2-nitrobenzyl) - 1 - phenyl - 2 - methylamino - propanol - (1) and reducing the nitro group with Raney nickel; (b) N - (2 - acetamino - benzyl) - 1 - phenyl - 2 - methylamino - propanol - (1) is obtained by acetylating compound (a) above; (c) 1,2,3,4 - tetrahydro - 2 - methyl - 4 - phenyl - 8-amino -isoquinolone is obtained by condensation of N-methyl-N-(2-aminobenzyl)-mandelic acid amide with H 2 SO 4 ; (d) N - (2 - amino - benzyl) - 1 - (3,4 - dimethylphenyl) - 2 - methylamino - propanol - 1 is obtained by reacting α-bromo-3,4-dimethyl-propiophenone with (2-nitrobenzyl)-methylamine then hydrogenating the NO 2 group and then reducing the CO group; (e) N - (2 - aminobenzyl) - 1 - phenyl - 2 - amino-propanol.(1) is obtained by hydrogenating a mixture of α-acetyl-benzyl alcohol and benzylamine to form 1-phenyl-2-aminopropanol-(1) which is reacted with 2-nitrobenzaldehyde and the product reduced at the nitro and azo-methine groups to form the above compound (e). Pharmaceutical compositions, having a centrally stimulating and thymoleptic action, comprise compounds of Formula I or physiologically tolerable salts thereof, together with a pharmaceutically suitable carrier, in forms suitable for oral or parenteral administration.

    26.
    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.

    27.
    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.

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