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    1.
    发明专利
    未知

    公开(公告)号：FI58920B

    公开(公告)日：1981-01-30

    申请号：FI181974

    申请日：1974-06-14

    Applicant: HOECHST AG

    Inventor： MOHLER WERNER ,  JAYME MANFRED ,  KOMAREK JAROMIR

    IPC: A61K31/52 ,  A61K31/522 ,  A61P7/02 ,  A61P9/08 ,  C07D473/06

    Abstract: Compounds of general formula (I) wherein one of the groups R1 and R3 is a straight-chain or branched oxoalkyl group consisting from 5 to 8 carbon atoms and the oxygen atom is attached to a non-terminal carbon atom and is separated from the nearest ring nitrogen atom by at least 3 carbon atoms in ( omega -1)-oxoalkyl groups and by at least 4 carbon atoms in oxoalkyl groups in which the oxygen atom is separated from the terminal carbon atom by more than one carbon atom, R2 and the other one of groups R1 and R3 are straight chain or branched alkyl groups containing from 1 to 12 carbon atoms but wherein that group R1 or R3 which is other than an oxoalkyl group may also be hydrogen, one nitrogen-bound substituent being hydrogen or alkyl containing more than 1 carbon atom, and physiologically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions containing said compounds.

    XANTHINE DERIVATIVES
    3.
    发明专利
    XANTHINE DERIVATIVES 未知

    公开(公告)号：CA1075692A

    公开(公告)日：1980-04-15

    申请号：CA320437

    申请日：1977-12-07

    Applicant: HOECHST AG

    Inventor： MOHLER WERNER ,  JAYME MANFRED ,  KOMAREK JAROMIR

    IPC: C07D473/06

    Abstract: This invention relates to a process for the preparation of the compounds of general formula (I) wherein R1 is an (.omega.-1)-oxoalkyl group containing from 5 to 7 carbon atoms, R2 is methyl and R3 is propyl, and physiologically acceptable acid addition salts thereof, which comprisesa) reacting an alkali metal salt of a 3-methyl-7-alkyl xanthine with a substance selected from the group consisting of a 1) a compound of formula (III) wherein A is an alkylene group containing from 3 to 5 carbon atoms and Hal is a halogen atom; b 1) an acetal, c 1) ketal and d 1) thioketal therefrom and subsequently hydrolysing the product orb) reacting an alkali metal salt of 1-(.omega.-1)-oxoalkyl-3-methyl-xanthine wherein the oxoalkyl radical has from 5 to 7 carbon atoms with a propylating compound selected from the group consisting of propyl halides and a propyl sulphate in the presence of a solvent,c) reacting a compound of formula (IV) herein X is an alkylene group containing from 3 to 5 carbon atoms and Hal is a halogen atom with an alkali metal salt of an acetoacetate and subsequently subjecting the reaction product to ketone splitting to obtain a product of general formula (I) as defined above, ord) oxidation of a compound of formula (V) wherein R2 and R3 have the meaning as defined above and Y is an(.omega.-1)-hydroxy-alkyl group having from 5 to 7 carbon atoms, and wherein the product obtained is isolated per se or reacted with an acid to form a physiologically compatible acid addition salt thereof. It also relates to the products of this process which are useful in the treatment of diseases involving deficiencies in the blood vascular system.

    4.
    发明专利
    未知

    公开(公告)号：CH612969A5

    公开(公告)日：1979-08-31

    申请号：CH123978

    申请日：1974-06-14

    Applicant: HOECHST AG

    Inventor： MOHLER WERNER ,  JAYME MANFRED ,  KOMAREK JAROMIR

    IPC: A61K31/52 ,  A61K31/522 ,  A61P7/02 ,  A61P9/08 ,  C07D473/06 ,  C07D473/04

    Abstract: Compounds of general formula (I) wherein one of the groups R1 and R3 is a straight-chain or branched oxoalkyl group consisting from 5 to 8 carbon atoms and the oxygen atom is attached to a non-terminal carbon atom and is separated from the nearest ring nitrogen atom by at least 3 carbon atoms in ( omega -1)-oxoalkyl groups and by at least 4 carbon atoms in oxoalkyl groups in which the oxygen atom is separated from the terminal carbon atom by more than one carbon atom, R2 and the other one of groups R1 and R3 are straight chain or branched alkyl groups containing from 1 to 12 carbon atoms but wherein that group R1 or R3 which is other than an oxoalkyl group may also be hydrogen, one nitrogen-bound substituent being hydrogen or alkyl containing more than 1 carbon atom, and physiologically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions containing said compounds.

    PROCESS FOR PREPARING O-ALKYLATED HYDROXYLAMINES
    7.
    发明专利
    PROCESS FOR PREPARING O-ALKYLATED HYDROXYLAMINES 未知

    公开(公告)号：HU176533B

    公开(公告)日：1981-03-28

    申请号：HUHO002024

    申请日：1977-11-08

    Applicant: HOECHST AG

    Inventor： THORWART WERNER ,  KOMAREK JAROMIR ,  CARTHEUSER CARL ,  GEBERT ULRICH

    IPC: A61K31/395 ,  A61K31/13 ,  A61K31/24 ,  A61P9/12 ,  C07C215/30 ,  C07C239/12 ,  C07C239/20 ,  C07C255/53 ,  C07C255/54 ,  C07C319/14 ,  C07C323/12 ,  C07D207/06 ,  C07D211/00 ,  C07D211/14 ,  C07D233/60 ,  C07D233/74 ,  C07D235/06 ,  C07D295/06 ,  C07D295/08 ,  C07D295/088 ,  C07D295/12 ,  C07D473/08 ,  C07D521/00 ,  C07C83/04 ,  C07C93/02 ,  C07D227/04 ,  C07D247/00 ,  C07D249/00

    Abstract: A compound of general formula (I) wherein X represents a radical selected from the group consisting of one of the formulae in which R1 represents a radical selected from the group (a) a hydrogen atom, (b) an amino group, when X represents an -OR1 moiety, (c) an alkyl group having from 1 to 6 carbon atoms (d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; and R2 and R3, which may be the same or different, each represents a radical selected from the group (a) a hydrogen atom, (b) an alkyl group having from 1 to 6 carbon atoms, an unsubstituted cycloalkyl group having from 3 to 7 carbon atoms, such cycloalkyl group substituted by at most 3 substituents of the group hydroxy groups and alkoxycarbonyl groups having 1 to 4 carbon atoms, (c) an aralkyl group, a diaralkyl group each having 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted in at least one of the radicals in the alkyl moiety by hydroxy groups, and in the aryl moieties by at most 3 substituents selected from the group consisting of alkoxy groups having from 1 to 4 carbon atoms and halogen atoms, (d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents selected from the group consisting of alkyl, alkoxy, halogenoalkyl groups each having up to 4 carbon atoms and halogen atoms, (e) a hydroxy group when the other of R2 and R3 is hydrogen, (f) R2 and R3, together with the nitrogen atom to which they are attached, represent a 5- to 7-membered ring selected from the group consisting of an unsubstituted ring, a ring being substituted by an alkyl group having from 1 to 4 carbon atoms, and a ring being interrupted by a heteroatom selected from the group consisting of oxygen, sulphur and further nitrogen atom, and (g) R2 and R3 together with the nitrogen atom to which they are attached, represent a ring from the group a 5-membered heteroaromatic ring containing up to 4 nitrogen atoms and such a ring being anelled to a benzene- or uracil-ring, and physiologically acceptable acid addition salts thereof, a process for their preparation and a pharmaceutical composition containing them.

    XANTHINE DERIVATIVES
    8.
    发明专利
    XANTHINE DERIVATIVES 未知

    公开(公告)号：CA1075691A

    公开(公告)日：1980-04-15

    申请号：CA320436

    申请日：1977-12-07

    Applicant: HOECHST AG

    Inventor： MOHLER WERNER ,  JAYME MANFRED ,  KOMAREK JAROMIR

    IPC: C07D473/06

    Abstract: This invention relates to a process for the preparation of the compounds of general formula (I) wherein R1 is a straight-chain 5-oxohexyl group, R2 is alkyl having at most 2 carbon atoms and R3 is a straight-chain or branched alkyl group containing from 2 to 4 carbon atoms, and physiologically acceptable acid addition salts thereof, which comprisesa) reacting an alkali metal salt of a 3-methyl- or 3-ethyl-7-alkyl-xanthine with a substance selected from the group consisting of a 1) a compound of formula (III) wherein A is an alkylene group containing 4 carbon atoms and Hal is a halogen atom; b 1) an acetal, c 1) ketal and d 1) thioketal therefrom and subsequently hydrolysing the product, orb) reacting an alkali metal salt of 1-(5-oxohexyl)-3-methyl- or 3-ethyl-xanthine with an alkylating compound selected from the group consisting of alkyl halides and a dialkyl sulphate wherein the alkyl group or groups contain 2 to 4 carbon atoms in the presence of a solvent, orc) reacting a compound of formula (IV) wherein X is an alkylene group containing 3 carbon atoms and Hal is a halogen atom with an alkali metal salt of an acetoacetate and subsequently subjecting the reaction product to ketone splitting to obtain a product of general formula (I) as defined above, ord) oxidation of a compound of formula (V) wherein R2 and R3 have the meaning as defined above and Y is a 5-hydroxyhexyl group; and wherei.n the product obtained is isolated per se or reacted with an acid to form a physiologically compatible acid addition salt thereof. It also relates to the products of this process which are useful in the treatment of diseases involving deficiencies in the blood vascular system.

    HYDROXYALKYL SUBSTITUTED XANTHINE DERIVATIVES
    9.
    发明专利
    HYDROXYALKYL SUBSTITUTED XANTHINE DERIVATIVES 未知

    公开(公告)号：CA1062709A

    公开(公告)日：1979-09-18

    申请号：CA178591

    申请日：1973-08-10

    Applicant: HOECHST AG

    Inventor： HINZE HEINZ-JOACHIM ,  SOEDER ALFONS ,  POPENDIKER KURT ,  MOHLER WERNER ,  JAYME MANFRED ,  KOMAREK JAROMIR ,  REISER MARIO

    IPC: C07D473/06 ,  C07D473/08 ,  C07D473/10 ,  C07D473/04

    Abstract: Xanthine compounds, and processes for their preparation of formula wherein: R1 represents (a) an .omega.-hydroxyalkyl radical of 4 to 8 carbon atoms or (b) an (.omega.-1)-hydroxyalkyl radical having 4, 5, 7, or 8 carbon atoms; or(c) a 5-hydroxyhexyl group, or (d) an alkyl radical of 1 to 12 carbon atoms, or (e) hydrogen; R2 represents an .omega.- or (.omega.-1) hydroxyalkyl radical of 4 to 8 carbon atoms, or an alkyl radical of 1 to 12 carbon atoms; R3 represents (a) an .omega.-hydroxyalkyl radical of 6 to 8 carbon atoms, or (b) an (.omega.-1) hydroxyalkyl radical of 4 to 8 carbon atoms or (c) an alkyl radical having 4 to 8 carbon atoms, or (d) hydrogen, provided that: (i) at least one of the groups R1, R2, or R3 represents a hydroxyalkyl group as defined above in respect of R1, R2 and R3; (ii) R1 only represents a 5hydroxyhexyl group if at least one of R2 and R3 is an alkyl radical other than methyl, or if R3 is hydrogen; and (iii) at least one of the groups R1, R2 and R3 contains at least 5 carbon atoms, and in which definitions .omega.and(.omega.-1) mean the terminal carbon atom of the group distant from the xanthine ring system, and the carbon atom adjacent to the terminal one, respectively. These compounds find use in medicaments to improve blood circulation.

    10.
    发明专利
    未知

    公开(公告)号：FI773353A

    公开(公告)日：1978-05-10

    申请号：FI773353

    申请日：1977-11-08

    Applicant: HOECHST AG

    Inventor： GEBERT ULRICH ,  THORWART WERNER ,  KOMAREK JAROMIR ,  CARTHEUSER CARL

    IPC: A61K31/395 ,  A61K31/13 ,  A61K31/24 ,  A61P9/12 ,  C07C215/30 ,  C07C239/12 ,  C07C239/20 ,  C07C255/53 ,  C07C255/54 ,  C07C319/14 ,  C07C323/12 ,  C07D207/06 ,  C07D211/00 ,  C07D211/14 ,  C07D233/60 ,  C07D233/74 ,  C07D235/06 ,  C07D295/06 ,  C07D295/08 ,  C07D295/088 ,  C07D295/12 ,  C07D473/08 ,  C07D521/00 ,  C07D

    Abstract: A compound of general formula (I) wherein X represents a radical selected from the group consisting of one of the formulae in which R1 represents a radical selected from the group (a) a hydrogen atom, (b) an amino group, when X represents an -OR1 moiety, (c) an alkyl group having from 1 to 6 carbon atoms (d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; and R2 and R3, which may be the same or different, each represents a radical selected from the group (a) a hydrogen atom, (b) an alkyl group having from 1 to 6 carbon atoms, an unsubstituted cycloalkyl group having from 3 to 7 carbon atoms, such cycloalkyl group substituted by at most 3 substituents of the group hydroxy groups and alkoxycarbonyl groups having 1 to 4 carbon atoms, (c) an aralkyl group, a diaralkyl group each having 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted in at least one of the radicals in the alkyl moiety by hydroxy groups, and in the aryl moieties by at most 3 substituents selected from the group consisting of alkoxy groups having from 1 to 4 carbon atoms and halogen atoms, (d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents selected from the group consisting of alkyl, alkoxy, halogenoalkyl groups each having up to 4 carbon atoms and halogen atoms, (e) a hydroxy group when the other of R2 and R3 is hydrogen, (f) R2 and R3, together with the nitrogen atom to which they are attached, represent a 5- to 7-membered ring selected from the group consisting of an unsubstituted ring, a ring being substituted by an alkyl group having from 1 to 4 carbon atoms, and a ring being interrupted by a heteroatom selected from the group consisting of oxygen, sulphur and further nitrogen atom, and (g) R2 and R3 together with the nitrogen atom to which they are attached, represent a ring from the group a 5-membered heteroaromatic ring containing up to 4 nitrogen atoms and such a ring being anelled to a benzene- or uracil-ring, and physiologically acceptable acid addition salts thereof, a process for their preparation and a pharmaceutical composition containing them.

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