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    4.
    发明专利
    未知

    公开(公告)号：DE2460990A1

    公开(公告)日：1976-07-01

    申请号：DE2460990

    申请日：1974-12-21

    Applicant: HOECHST AG

    Inventor： BECK GERHARD DR ,  LERCH ULRICH DR ,  SEEGER KARL DR ,  TEUFEL HERMANN DR

    IPC: C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07F9/38 ,  C07F9/40 ,  C07C177/00 ,  A61K31/20

    Abstract: Prostaglandin analogues of formula (I) in the natural, optically active configuration or as racemic cpds.: (where R1 + R2 is O, or one of R1 and R2 is H and the other is OH; one of R3 and R4 is H and the other is OH; is 1-5C straight or branched alkyl, or phenyl or benzyl opt. mono- di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy; R5, when X is 1-5C alkyl, is a diphenyl ether gp. opt. mono- di- or tri-substd. in either or both nuclei by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy or a phenoxy-(2-5 C straight chain or 3-6C branched chain alkyl) opt. mono-di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy, or, when X is opt. substd. phenyl, a benzyl residue opt. mono- di- or tri-substd. in the nucleus by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy, or, when X is opt. substd. benzyl, a phenyl residue opt. mono-, di- or tri-substd. by halogen, CF3, OH, 1-4C alkyl and/or 1-4C alkoxy; and the C-atoms in the 5- and 6-positions and the 13- and 14-positions are all linked by single bonds or all linked by double bonds), e.g. 9-oxo-11 alpha, 15-dihydroxy-16-methyl-16-(3-chloro-4-(4-chlorophenoxy)-phenoxy)-- 5-cis-13-trans-tetranorprostadienoci acid, their physiologically tolerable salts with organic and inorganic bases, and their esters with 1-8C aliphatic, cycloaliphatic and araliphatic alcohols are new. (I) can be used as pharmaceuticals with hypotensive, diuretic, antithrombotic labour-inducing, abortifacient, contraceptive, gastric secretion inhibiting, antiulcer and antiasthmatic activity. They are particularly useful as contraceptives for use in humans and as agents for synchronising oestrus in various animal species. They are more potent and longer-acting than natural prostaglandins.

    CEPHALOSPORIN DERIVATIVES AND PROCESS FOR THEIR PREPARATION
    5.
    发明专利
    CEPHALOSPORIN DERIVATIVES AND PROCESS FOR THEIR PREPARATION 未知

    公开(公告)号：DE3377714D1

    公开(公告)日：1988-09-22

    申请号：DE3377714

    申请日：1983-12-21

    Applicant: HOECHST AG

    Inventor： DURCKHEIMER WALTER DR ,  LATTRELL RUDOLF DR ,  SEEGER KARL DR

    IPC: A01N20060101 ,  A01N43/82 ,  A01N43/836 ,  A01N43/86 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/20 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

    Abstract: 1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LU, LI, NL, SE) A cephem derivative of the formula I see diagramm : EP0111934,P10,F3 and physiologically acceptable acid addition salts thereof in which R**1 denotes C1 -C2 -alkyl, R**2 denotes a pyridinium radical see diagramm : EP0111934,P10,F4 which is substituted by 2 alkyl groups in the ortho-position which are linked to form a trimethylene to pentamethylene ring in which one carbon atom can be replaced by an oxygen atom, or denotes a 1-quinolinium radical or a 2-isoquinolinium radical and in which the R**1 O group is in the syn-position. 1. Claims (for the Contracting State AT) A process for the preparation of a cephem derivative of the formula I see diagramm : EP0111934,P11,F4 and physiologically acceptable acid addition salts thereof in which R**1 denotes C1 -C2 -alkyl, R**2 denotes a pyridinium radical see diagramm : EP0111934,P12,F1 which is substituted by 2 alkyl groups in the ortho-position which are linked to form a trimethylene to pentamethylene ring in which one carbon atom can be replaced by an oxygen atom, or denotes a 1-quinolinium radical or a 2-isoquinolinium radical in which the R**1 O group is in the syn-position which comprises a) reacting a compound of the general formula II see diagramm : EP0111934,P12,F2 or salts thereof or a reactive derivative of the compound II in which R**1 has the meaning mentioned above and R**7 denotes an amino group or a protected amino group and R**8 denotes a group which can be replaced by the pyridine, quinoline or isoquinoline derivatives corresponding to the radicals R**2 of the formula I, with these pyridine, quinoline or isoquinoline derivatives, and alpha) splitting off a protective group which may be present and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt, or b) reacting a 7-aminocephem compound of the general formula III see diagramm : EP0111934,P12,F3 or acid addition salts thereof in which R**2 has the abovementioned meaning and in which the amino group can also be present in the form of a reactive derivative, with a 2-(5-amino-1,2,4-thiadiazol-3-yl)-2-synoximinoacetic acid of the general formula IV see diagramm : EP0111934,P12,F4 in which R**1 and R**7 have the meaning mentioned above, or with an activated derivative of this compound, and alpha) splitting off a protective group which may be present, and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt.

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