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    21.
    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.

    22.
    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.

    ANTIDEPRESSIVE AGENT
    23.
    发明专利
    ANTIDEPRESSIVE AGENT 未知

    公开(公告)号：AU517779B2

    公开(公告)日：1981-08-27

    申请号：AU3670478

    申请日：1978-05-31

    Applicant: HOECHST AG

    Inventor： SCHMITT K

    IPC: A61K31/47 ,  A61K31/55 ,  A61P25/24 ,  A61P25/26

    Abstract: What is disclosed are medicinal compositions, useful as anti-depressive agents, containing a compound of the formula; (I) in which R1, R3 and R4, which may be identical or different, and represent hydrogen atoms or lower alkyl or aralkyl groups, and R2 and R2', which may be identical or different, represent hydrogen or halogen atoms, hydroxy or trifluoromethyl groups or lower alkyl, alkoxy or aralkoxy groups, it also being possible that two adjacent radicals form an alkylene-dioxy radical, and R5 represents a hydrogen or halogen atom, a hydroxy, trifluoromethyl or nitro group or a lower alkyl, alkoxy or aralkoxy radical, and their salts with acids (active substance A) together with 7-chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4 (3H,5H)-dione (active substance B), and their use as antidepressive agent.

    MEDICINAL COMPOSITIONS AND ITS USE AS ANTIDEPRESSIVE AGENT
    25.
    发明专利
    MEDICINAL COMPOSITIONS AND ITS USE AS ANTIDEPRESSIVE AGENT 未知

    公开(公告)号：ZA783123B

    公开(公告)日：1979-06-27

    申请号：ZA783123

    申请日：1978-05-30

    Applicant: HOECHST AG

    Inventor： STAMMBERGER W ,  HOFFMANN I ,  SCHMITT K ,  FUELBERTH W

    IPC: A61K31/55 ,  A61K31/47 ,  A61P25/24 ,  A61P25/26 ,  A61K

    Abstract: What is disclosed are medicinal compositions, useful as anti-depressive agents, containing a compound of the formula; (I) in which R1, R3 and R4, which may be identical or different, and represent hydrogen atoms or lower alkyl or aralkyl groups, and R2 and R2', which may be identical or different, represent hydrogen or halogen atoms, hydroxy or trifluoromethyl groups or lower alkyl, alkoxy or aralkoxy groups, it also being possible that two adjacent radicals form an alkylene-dioxy radical, and R5 represents a hydrogen or halogen atom, a hydroxy, trifluoromethyl or nitro group or a lower alkyl, alkoxy or aralkoxy radical, and their salts with acids (active substance A) together with 7-chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4 (3H,5H)-dione (active substance B), and their use as antidepressive agent.

    26.
    发明专利
    未知

    公开(公告)号：DK242278A

    公开(公告)日：1978-12-02

    申请号：DK242278

    申请日：1978-05-31

    Applicant: HOECHST AG

    Inventor： SCHMITT K ,  HOFFMANN I ,  SCHACHT U

    IPC: C07D217/18 ,  A61K31/47 ,  A61K31/472 ,  A61P25/24 ,  A61P25/26 ,  C07D217/04 ,  C07D

    Abstract: 4-Phenyl-8-amino-tetrahydroisoquinolines of the formula in which R1 stands for bromine and R2 stands for hydrogen or both R1 and R2 represent chlorine, and their salts with physiologically tolerated acids, pharmaceutical preparations prepared therefrom, process for the manufacture of these preparations and their use for the treatment of depressive conditions.

    28.
    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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