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    PROCESS FOR PREPARATION OF CYCLOPENANE DERIVATIVES
    1.
    发明授权
    PROCESS FOR PREPARATION OF CYCLOPENANE DERIVATIVES 失效

    公开(公告)号：KR790001361B1

    公开(公告)日：1979-09-28

    申请号：KR740002787

    申请日：1974-06-15

    Applicant: HOECHST AG

    Inventor： BECK GERHARD ,  MILOS BABEJ ,  LERCH ULRICH ,  BARTMANN WILHELM

    Abstract: Title compds. (I; R1,R2 = O; R3,R4 = C1-5 alkyl ; R5 = tetrahydropyranyl, H ; U = (CH2)0-5, cis- or trans-alkyl = c-alkyl; V = simple bond, O, furan, benzyl ; W = alkyl-C-alkyl; X = (CH2)0-4), similar in structure to natural prostaglandine, having strong antiprostaglandine activity were prepd. by reaction of II and in aprotic solvent. Thus, 3.66g (5RS,3'RS)-2-oxo-5 3'-(2"-tetrahydropyranyloxy) -trans-1'-octenyl -cyclopentane-carboxylic ester in C6H5CH3 were stirred with 1.35g potassium-t-butylate followed by reaction with 4g 7-iodo-heptanophosphoric ethyl ester to give I.

    PROCESS FOR PREPARING THIENYL-PROSTAGLANDINS
    4.
    发明公开
    PROCESS FOR PREPARING THIENYL-PROSTAGLANDINS 失效

    公开(公告)号：KR830000208A

    公开(公告)日：1983-03-30

    申请号：KR760000522

    申请日：1976-03-04

    Applicant: HOECHST AG

    Inventor： BARTMANN WILHELM ,  REUSCHLING DIETER ,  TEUFEL HERMANN ,  BECK GERHARD ,  SEEGAR KARL

    IPC: A61K31/557 ,  C07D333/16 ,  C07C177/00

    Abstract: Title compds. I(R1,R2 = H, OH; R3 = α- or β-thienyl, α- or β-thienylmethyl, benzo[b thiophene, cyclopentano[b thiopene, cyclohexano[b thiopene; X = C1-7 straight-or sidechain alkylene, C2-8 alkoxyalkylene), exhibiting a hypotension activity and a urination activity, were prepd. by the reaction of lactol (II) and 4-carboxy-butyl-triphenylphosphonium bromide in NaH-dissolved dimethylsulfoxide in the presence of inert gas to give formula acid(II), which was acid hydrolyzed to give compds. I or their esters by eliminating tetrahydropyranyl protecting group.

    Bisammonium compounds and process for preparing them
    5.
    发明授权
    Bisammonium compounds and process for preparing them 失效
    BISAMMONIUM化合物及其制备方法

    公开(公告)号：US3661966A

    公开(公告)日：1972-05-09

    申请号：US3661966D

    申请日：1969-08-04

    Applicant: HOECHST AG

    Inventor： BARTMANN WILHELM ,  DUWEL DIETER ,  GEORGI VOLKMAR ,  WOLF ERHARD ,  BEERMANN CLAUS ,  LANDAUER FRANZ

    IPC: A61K31/14 ,  C07C233/00 ,  C07C125/06

    CPC classification number: A61K31/14 ,  C07C233/00

    Abstract: BIS-AMMONIUM COMPOUNDS OF THE FORMULA

    R1-OC-N(-CH2-N(+)(-R2)(-R4)-R3))2 2X(-)

    WHEREIN R1 IS ALKYL HAVING 1 TO 6 C-ATOMS, ALKOXY HAVING 1 TO 25 CARBON ATOMS, ALKENYOXY HAVING 3 TO 18 C-ATOMS, CYCLOALKOXY HAVING 4 TO 8 C-ATOMS, CYCLOALKYLALKOXY OR ALCKYLCYCLOALKOXY EACH HAVING 5 TO 8 C-ATOMS, AND HALOGENO-ALKOXY OR ALKOXYALKOXY EACH HAVING 1 TO 6 C-ATOMS, R2 IS ALKYL HAVING 1 TO 3 C-ATOMS, R3 IS ALKYL HAVING 1 TO 25 C-ATOMS, ALKENYL HAVING 3 TO 18 C-ATOMS, CYCLOALKYL HAVING 4 TO 8 C-ATOMS OR PHENALKYL HAVING 1 TO 2 C-ATOMS IN THE ALKYLENE RADICAL AND OPTIONALLY ONE CHLORINE ATOM OR A NITRO GROUP IN THE PHENYL NUCLEUS, R4 IS ALKYL HAVING 6 TO 25 C-ATOMS OR ALKENYL HAVING 5 TO 25 C-ATOMS, AND X- IS AN ANION OF A NON-TOXIC ACID AND A PROCESS FOR PREPARING THEM ARE DESCRIBED. THE COMPOUNDS HAVE VALUABLE ENTHELMINTIC PROPERTIES.

    7-SUBSTITUTED DERIVATIVES OF 3,5-DIHYDROXYHEPT-6-YNOIC ACID, A PROCESS FOR THE PREPARATION THEREOF, THE USE THEREOF AS PHARMACEUTICALS, AND INTERMEDIATES
    8.
    发明专利
    7-SUBSTITUTED DERIVATIVES OF 3,5-DIHYDROXYHEPT-6-YNOIC ACID, A PROCESS FOR THE PREPARATION THEREOF, THE USE THEREOF AS PHARMACEUTICALS, AND INTERMEDIATES 未知

    公开(公告)号：CA1340047C

    公开(公告)日：1998-09-15

    申请号：CA612496

    申请日：1989-09-22

    Applicant: HOECHST AG

    Inventor： KESSELER KURT ,  BARTMANN WILHELM ,  WESS GUENTHER ,  GRANZER ERNOLD

    IPC: A61K31/215 ,  A61K31/34 ,  A61K31/35 ,  A61K31/351 ,  A61K31/365 ,  A61K31/366 ,  A61K31/38 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/496 ,  A61K31/50 ,  A61K31/505 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C33/48 ,  C07C45/30 ,  C07C47/222 ,  C07C47/24 ,  C07C51/367 ,  C07C59/42 ,  C07C59/46 ,  C07C59/48 ,  C07C59/56 ,  C07C59/76 ,  C07C67/31 ,  C07C69/606 ,  C07C69/732 ,  C07C69/734 ,  C07D207/08 ,  C07D207/32 ,  C07D207/333 ,  C07D207/337 ,  C07D213/48 ,  C07D213/55 ,  C07D213/62 ,  C07D213/63 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D261/08 ,  C07D275/02 ,  C07D309/30 ,  C07D405/06

    Abstract: 7-Substituted derivatives of 3,5-dihydroxyhept-6-ynoic acid, a process for the preparation thereof, the use thereof as pharmaceuticals, and intermediates 7-Substituted 3,5-dihydroxyhept-6-ynoic acids and the derivatives thereof of the formula I (see fig. I) as well as the corresponding lactones of the formula II (see fig. II) in which R denotes a) a radical of the formula a (see fig. III) in which R1 and R2 are, independently of one another, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms or phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having up to 4 carbon atoms and hydroxyl, and X=Y-Z is a group of the formula CR3=CR4-CR5, N=CR4-CR5, N=N-CR5, N=CR4-N, in which R3, R4, R5 are, independently of one another, hydrogen, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cycllc hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having up to 4 carbon atoms and hydroxyl, b) a radical of the formula b in which R6 and R7 are, independently of one another, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms, a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen and alkoxy having up to 4 carbon atoms, and U-V-W is a group of the formula C-NR9-CR8, C-O-CR8, C-S-CR8, C-NR9-N , C-O-N (= C-N-O ), C-S-N ( = C-N-S ), N-CR10=CR8 , N-N=CR8 or N-CR10=N, in which R8 is hydrogen, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated eyclic hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having 1-4 carbon atoms and hydroxyl, and R9, R10 are, independently of one another, a straight-chain or branched alkyl or alkenyl radical having up to 6 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 identical or different radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen and alkoxy having up to 4 carbon atoms, or e) a radical of the formula c in which A-B is a group of the formula CH-CH or C=C, and R11, R12, R13 are, independently of one another, a straight-chain or branched alkyl or alkenyl radical having up to 20 carbon atoms, a saturated or up to doubly unsaturated cyclic hydrocarbon radical having 3-6 carbon atoms or a phenyl radical which is optionally substituted by 1-3 radicals selected from the group comprising straight-chain or branched alkyl having up to 4 carbon atoms, halogen, alkoxy having up to 4 carbon atoms and hydroxyl, and R~ denotes hydrogen, a straight-chain or branched alkyl radical having up to 6 carbon atoms, alkali metal or ammonium, a process for the preparation of these compounds, the use thereof as pharmaceuticals and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.

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