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    Heterocyclic ethers of piperazine n alkanols
    1.
    发明授权
    Heterocyclic ethers of piperazine n alkanols 失效
    哌嗪N醇的杂环化合物

    公开(公告)号：US3787411A

    公开(公告)日：1974-01-22

    申请号：US3787411D

    申请日：1970-09-08

    Applicant: HOECHST AG

    Inventor： MOHLER W ,  GOEBEL A ,  RUSCHIG H ,  SCHMITT K ,  LINDNER E

    IPC: C07D237/14 ,  C07D213/64 ,  C07D215/22 ,  C07D237/30 ,  C07D239/34 ,  C07D239/72 ,  C07D241/18 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D295/04 ,  C07D295/067 ,  C07D295/185 ,  C07D51/70

    CPC classification number: C07D213/64 ,  C07D241/18 ,  C07D295/067 ,  C07D295/185 ,  Y10S514/921

    Abstract: A HECTEROCYCLIC ETHER OF THE FORMULA

    1-(R1-O-A-),4-(R2-)-PIPERAZINE

    IN WHICH R1 IS 3-, 4- OR 6-ALKOXY-PYRIDYL-(2); 2-, 4- 5OR 6-ALKOXY-PYRIDYL-(3); 2- OR 3-ALKOXY-PYRIDYL-(4) WHICH HAVE 1-4 CARBON AOMS IN THE ALKOXY RADICAL: 3-, 4-, 5OR 6-METHYL-PYRIDYL-(2); 6 - ETHYL - PYRIDYL - (4)-; 2,6-DIMETHYL-PYRIDYL-(4); R2 IS PHENYL, O-TOLYL, M-TOLYL, P-TOLYL, O-AANISYL, M-ANISYL, P-ANISYL, O-CHLOROPHENYL, M-CHLOROPHENYL, P-CHLOROPHENYL, PYRIDYL (2), PYRIDYL (3), PYRIDYL (4); 2-CHLORO-4-METHYL-PHENYL, 2-CHLORO - 4 - METHOXYPHENYL AND 2-METHOXY-4 - METHYL - PHENYL, 6 - METHOXYPYRIDYL (2), 2-METHYL-PYRIDYL (4), 4,6-DIMETHYL-PYRIDYL (2) OR THEIR POSITION ISOMERS, AND A IS ALKYLENE HAVING FROM 2 TO 6 CARBON ATOMS WHEREIN THE SAME IS ETHYLENE, TRIMETHYLENE, 2-METHYL-ETHYLENE, 3-METHYL-ETHYLENE, TETRAMETHYLENE, 3-METHYL-TRIMETHYLENE, 2 - ETHYL - ETHYLENE, 1ETHYL-ETHYLENE, PENTAMETHYLENE, 4 - METHYL - TETRAMETHYLENE, 3-ETHYL-TRIMETHYLENE, 1-PROPYL - ETHYLENE, 1 - ISOPROPYL-ETHYLENE, 1,2-DIMETHYL - ETHYLENE, 1 HEXAMETHYLENE, 5METHYL-PETAMETHYLENE, 4 - ETHYL - TETRAMETHYLENE, 3 - PROPYL-TRIMETHYLENE, 2-BUTYL-ETHYLENE, 1 - BUTYL - ETHYLENE OR 1-METHYL-3-ETHYL-TRIMETHYLENE; AND PHYSIOLOGICALLY TOLERABLE ACID ADDITION SALTS THEREOF; THESE COMPOUNDS HAVE AN A-SYMPATHOLYTIC ACTION AND ARE USEFUL IN THE TREATMENT OF SHOCKS, MIGRAINE, HYPERTONIA AND BLOOD CIRCULATION DISORDERS OF THE EXTREMITIES.

    N-(benzoyl)-n'-(piperazin-1-yl)alkyl)ureas
    2.
    发明授权
    N-(benzoyl)-n'-(piperazin-1-yl)alkyl)ureas 失效
    N-（苯甲酰基）-N' - （哌嗪-1-基）烷基）脲

    公开(公告)号：US3823144A

    公开(公告)日：1974-07-09

    申请号：US26474772

    申请日：1972-06-21

    Applicant: HOECHST AG

    Inventor： SCHMITT K ,  HOFFMANN I

    IPC: C07D295/13 ,  C07D51/70

    CPC classification number: C07D295/13 ,  Y10S514/906

    Abstract: BENZOYL UREAS OF THE FORMULA

    1-((R1-PHENYL)-CO-NH-CO-NH-A-),4-(R2-PHENYL)-PIPERAZINE

    AND SALTS THEREOF WITH PHYSIOLOGICALLY ACCEPTABLE ACIDS, USEFUL AS PSYCHOPHARMACOLOGICAL AGENTS, WHEREIN R1 IS ONE OR MORE OF HYDROGEN, HALOGEN, ALKYL HAVING 1 TO 6 CARBON ATOMS, ALKYL HAVING 3 TO 6 CARBON ATOMS, CYCLOALKYL OF 3 TO 7 CARBON ATOMS, CYCLOALKENYL OF 4 TO 7 CARBON ATOMS, ARALKYL HAVING 1 TO 4 ALKYLENE CARBON ATOMS, PHENYL, HYDROXY, ACYLOXY, ALKOXY HAVING 1 TO 6 CARBON ATOMS, ALKENYLOXY HAVING 3 TO 6 CARBON ATOMS, ARALKOXY HAVING 1 TO 4 ALKYLENE CARBON ATOMS, ARYLOXY, TRIFLUORO, OR NITRO, IN ANY POSITION,OR REPRESENTS TWO VICINAL SUBSTITUENTS WICH ARE MEMBERS IF A CONDENSED 5- TO 7MEMBERED CARBOCYCLIC RING; R2 IS HYDRGEN, HALOGEN, ALKYL HAVING 1 TO 4 CARBON ATOMS, OR ALKOXY HAVING 1 TO 4 CARBON ATOMS; AND A IS ALKYLENE HAVING 2 TO 6 CARBON ATOMS.

    2-amino-4,4-di-substituted-4h-3,1-benzoxazines
    3.
    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。

    6.
    发明专利
    未知

    公开(公告)号：SE330170B

    公开(公告)日：1970-11-09

    申请号：SE626567

    申请日：1967-05-03

    Applicant: HOECHST AG

    Inventor： EHRHART G ,  SCHMITT K ,  HOFFMAN I ,  OTT H

    IPC: C07D217/02 ,  C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  C07D35/10

    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.

    10.
    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.

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