PROCESS FOR THE PREPARATION OF 2,4-11-DEOXYPGE SERIES PROSTAGLANDIN

    公开(公告)号:KR820000509B1

    公开(公告)日:1982-04-10

    申请号:KR780003626

    申请日:1978-11-30

    Applicant: HOECHST AG

    Abstract: Title compds.(I; R1 = H, C1-10 hydrocarbon, ammonium ion; R2 = C1-6 aliphatic hydrocarbon) were prepd. by the hydrolysis of IV(R3 = protecting group; Z = CH2 or -C(CH3)2 group) obtained from the reaction of II and III (R4 = C1-4 alkyl or phenyl). Thus, 111.2 g 3-carbomethoxy-2-propenyl-2-triphenyl-phosphonium bromide and 71.6 g methyl-γ-bromo-crotonate were stirred at 26oC for 1.5 hr to give I.

    NEW PEPTIDE AMIDES AND PROCESS FOR THEIR MANUFACTURE

    公开(公告)号:ZA805151B

    公开(公告)日:1981-08-26

    申请号:ZA805151

    申请日:1980-08-21

    Applicant: HOECHST AG

    Abstract: New peptide amides of the formula I H-Tyr-D-Lys(For)-Gly-X (I) wherein For is formyl, X is alkylamino, dehydro-Phe or Phe-alkylamido having up to 6 carbon atoms in the alkyl moiety, which moiety may be substituted by hydroxy and/or phenyl, Phe-cycloalkylamide or Phe-cycloalkylene amide having up to 8 carbon atoms in the cycloalkyl or cyclalkylene moiety, 1 to 2 CH2 groups being optionally replaced by -NH-, -O-, -S- or -CO-, Phe-alkylene-cycloalkylamide having from 5 to 6 ring carbon atoms, which amide may be substituted by carbonamido,N-alkylcarbonamido or alkyl and 1 carbon atom whereof may be replaced by nitrogen, Phe-endo- or exo-norbornylamide or Phe-thiazolamide or Phe-thiazolidine-carboxylic acid amide, which may be substituted by 1 to 4 methyl groups each, and process for their manufacture are disclosed. These peptide amides are distinguished by an analgetic activity and suppress the motility of the ileum of the guinea pig.

    MEŠANI DIAMIDI PIRIDIN - 2,4 I 2,5 DIKARBOKSILNIH KISELINA I POSTUPAK ZA NJIHOVO DOBIJANJE

    公开(公告)号:YU48156B

    公开(公告)日:1997-05-28

    申请号:YU24692

    申请日:1992-03-12

    Applicant: HOECHST AG

    Abstract: MESANI DIAMIDI PIRIDIN - 2,4 I 2,5 DIKARBOKSILNIH KISELINA I POSTUPAK ZA NJIHOVO DOBIJANJE formule I u kojoj R1 znaci C1 - C12 - alkil, C2 - C12 - alkenil ili C2 - C12 - alkihil, koji su nesupstituisani ili jednom, ili u primeru C2 - C12 - alkila, C2 - C12 - alkehila i C2 - C12 - alkihila vise puta supstituisani, halogenom, hidroksi, cijano, amino, karboksilom, alkoks, alkoksikarbonilom, alkikarboniloksi, alkil - ili dialkilamino, pri cemu alkilni ostaci sadrze 1 - 4 atoma C, ili indolinom ili fenilom, koji su nesupstituisan ili 1,2 ili 3 puta supstituisan halogenom, nitro C1 - C4 - alkilom ili C1 - C4 alkoksi, pri cemu mogu u slucaju visekratnih supstitucija supstituenti biti nezavisno razliciti, ili R1 znaci zasicen C5 - C7 - cikloalkil, koji je u datom primeru benzaneliran ili R1 znaci aril ili heteroaril, koji je nesupstituisan ili posebno 1,2 ili 3 puta supstituisan halogenom, nitro, cijano, C1 - C4 -alkilom ili C1 - C4 alkoksi, pri cemu mogu u slucaju visekratnih supstitucija supstituenti biti nezavisno razliciti ili R1 u slucaju da je R2 H, iznad amino, koji je nesupstituisan ili mono - ili disupstituisan sa C1 - C4 - alkilom, fenilom ili C1 - C3 - alkilkarbonilom, i R1 znaci vodonik ili R1, pri cemu su R2 i R1 jednaki ili se razlikuju, ili pri cemu ostaci R1 i R2 zajedno sa atomom azota cine ostatak sa formulom u kojoj n znaci 1-3 x znaci O, S, CH2 ili N-R3 pri cemu R3 znaci vodonik, fenil ili C1-C6 - alkil, C2 - C6 - alkenil ili C2 - C6 - alkinil, pri cemu su ti fenilni, alkilni, alkenilni i alkinilni ostaci nesupstituisani ili jednom ili vise puta supstituisani fenolom, koji je sa svoje strane nesupstituisan ili jedan put ili vise puta supstituisan jednom ili sa vise supstituenata, odabranim izmedju halogena, nitro, cijano, karboksi, hidroksi, metila, etila, metoksi, etoksi i triflurmetila il N(R4), pri cemu R4 znaci vodonik ili C1 - C3 - alkil ili COOR5, pri cemu R5 znaci vodonik ili C1 - C3 - alkil, ili CON (R6)2 ili CONHR6, pri cemu R6 znaci H ili C1 - C3, alkil, ili pri cemu (R6)2 predstavlja C4 - C6 - alkilensi lanac, u kojoj nije nijedna ili je jedna CH2 grupa, koja ne stoji neposredno uz atom azota, zamenjena sa O, S ili N - R4, ili pri cemu R3 znaci C1 - C4 - alkoksi-karbonil ili C3 - C7 - cikloalkil, kao i fiziolosko podnosljive soli. - Prijava sadrzi jos 1 nezavisan i 2 zavisna zahteva.

    NEW PEPTIDE AMIDES AND PROCESS FOR THEIR MANUFACTURE

    公开(公告)号:AU6162080A

    公开(公告)日:1981-04-09

    申请号:AU6162080

    申请日:1980-08-21

    Applicant: HOECHST AG

    Abstract: New peptide amides of the formula I H-Tyr-D-Lys(For)-Gly-X (I) wherein For is formyl, X is alkylamino, dehydro-Phe or Phe-alkylamido having up to 6 carbon atoms in the alkyl moiety, which moiety may be substituted by hydroxy and/or phenyl, Phe-cycloalkylamide or Phe-cycloalkylene amide having up to 8 carbon atoms in the cycloalkyl or cyclalkylene moiety, 1 to 2 CH2 groups being optionally replaced by -NH-, -O-, -S- or -CO-, Phe-alkylene-cycloalkylamide having from 5 to 6 ring carbon atoms, which amide may be substituted by carbonamido,N-alkylcarbonamido or alkyl and 1 carbon atom whereof may be replaced by nitrogen, Phe-endo- or exo-norbornylamide or Phe-thiazolamide or Phe-thiazolidine-carboxylic acid amide, which may be substituted by 1 to 4 methyl groups each, and process for their manufacture are disclosed. These peptide amides are distinguished by an analgetic activity and suppress the motility of the ileum of the guinea pig.

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