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    6-PHENOXYMETHYL-4-HYDROXYTETRAHYDROPYRAN-2-ONES,A PROCESS FOR THEIR PREPARATION,THEIR USE AS MEDICAMENTS,PHARMACEUTICAL PRODUCTS AND INTERMEDIATES
    11.
    发明专利
    6-PHENOXYMETHYL-4-HYDROXYTETRAHYDROPYRAN-2-ONES,A PROCESS FOR THEIR PREPARATION,THEIR USE AS MEDICAMENTS,PHARMACEUTICAL PRODUCTS AND INTERMEDIATES 未知

    公开(公告)号：PH23860A

    公开(公告)日：1989-11-23

    申请号：PH34188

    申请日：1986-08-27

    Applicant: HOECHST AG

    Inventor： WESS GUNTHER ,  GRANZER ERNOLD ,  BECK GERHARD ,  LAU HANS-HERMANN

    IPC: A61K31/365 ,  C07D309/10 ,  C07D309/30 ,  C07F7/18 ,  A61K31/35

    Abstract: 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE A 6-phenoxymethyl-4-hydroxytetrahydropyran-2-one of the general formula I see diagramm : EP0216127,P57,F1 in which R**1 and R**5 are identical or different and denote a) halogen, b) cycloalkyl having 4-8 carbon atoms, or a phenyl radical which can be substituted in the nucleus once to 3 times by halogen, trifluoromethyl, and/or alkyl or alkoxy each having 1-4 carbon atoms, or c) a straight-chain or branched alkyl radical having 1 to 18 carbon atoms, or a straight-chain or branched alkenyl radical having 2 to 18 carbon atoms, it being possible for the alkyl and alkenyl radicals in turn to be substituted 1-3 times by alpha) straight-chain or branched alkoxy radicals having up to 10 carbon atoms, or cycloalkyl radicals having 3 to 7 carbon atoms, or straight-chain or branched alkenyloxy or alkynyloxy radicals having 3 to 6 carbon atoms, beta) halogen, hydroxyl, cycloalkyl having 3-7 carbon atoms, unsubstituted phenyl or alpha- or beta-thienyl radicals, or phenyl or alpha- or beta-thienyl radicals which in turn are substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1-4 carbon atoms, gamma) unsubstituted phenoxy, benzyloxy, alpha- or beta-thienyloxy radicals, or phenoxy, benzyloxy, alpha- or beta-thienyloxy radicals which in turn are substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1 to 4 carbon atoms, delta) the group see diagramm : EP0216127,P57,F2 R**6 denoting : a straight-chain or branched alkyl or alkenyl radical having up to 8 carbon atoms, or a cycloalkyl or cycloalkenyl radical each having 3-8 carbon atoms, or an unsubstituted phenyl radical, or a phenyl radical which in turn is substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1-4 carbon atoms, or a 3-pyridyl radical, R**2 and R**4 denote hydrogen, and R**3 is alkyl or alkenyl having up to 4 carbon atoms, halogen or alkoxy having 1-4 carbon atoms, and the corresponding open-chain dihydroxy carboxylic acid, their pharmacologically tolerated salts with bases, and their pharmacologically tolerated esters. 1. Claims for the Contracting State : AT A process for the preparation of a 6-phenoxymethyl-4-hydroxytetrahydropyran-2-one of the general formula I see diagramm : EP0216127,P62,F1 in which R**1 and R**5 are identical or different and denote a) halogen, b) cycloalkyl having 4-8 carbon atoms, or a phenyl radical which can be substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy each having 1-4 carbon atoms, or c) a straight-chain or branched alkyl radical having 1 to 18 carbon atoms, or a straight-chain or branched alkenyl radical having 2 to 18 carbon atoms, it being possible for the alkyl and alkenyl radicals in turn to be substituted 2-3 times by alpha) straight-chain or branched alkoxy radicals having up to 10 carbon atoms, or cycloalkoxy radicals having 3 to 7 carbon atoms, or straight-chain or branched alkenyloxy or alkynyloxy radicals having 3 to 6 carbon atoms, beta) halogen, hydroxyl, cycloalkyl having 3-7 carbon atoms, unsubstituted phenyl or alpha- or beta-thienyl radicals, or phenyl or alpha- or beta-thienyl radicals which in turn are substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1-4 carbon atoms, gamma) unsubstituted phenoxy, benzyloxy, alpha- or beta-thienyloxy radicals, or phenoxy, benzyloxy, alpha- or beta-thienyloxy radicals which in turn are substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1 to 4 carbon atoms, delta) the group see diagramm : EP0216127,P62,F2 R**6 denoting : a straight-chain or branched alkyl or alkenyl having up to 8 carbon atoms, or a cycloalkyl or cycloalkenyl radical each having 3-8 carbon atoms, or an unsubstituted phenyl radical, or a phenyl radical which in turn is substituted in the nucleus once to 3 times by halogen, trifluoromethyl and/or alkyl or alkoxy having 1-4 carbon atoms, or a 3-pyridyl radical, R**2 and R**4 denote hydrogen, and R**3 is alkyl or alkenyl having up to 4 carbon atoms, halogen or alkoxy having 1-4 carbon atoms, and the corresponding open-chain dihydroxy carboxylic acid, their pharmacologically tolerated salts with bases, and their pharmacologically tolerated esters, which comprises a) conversion of an appropriately substituted phenol of the formula II see diagramm : EP0216127,P62,F3 in which R**1 , R**2 , R**3 , R**4 and R**5 have the indicated meanings, with the chiral iodide of the formula III see diagramm : EP0216127,P63,F1 in which R**10 denotes a protective group which is stable to bases and weak acids, into an ether of the formula IV see diagramm : EP0216127,P63,F2 in which R**1 to R**5 have the meanings indicated for formula I and R**10 has the meanings indicated for formula III, b) hydrolysis of the ether of the formula IV to give the corresponding hemiacetal of the formula V see diagramm : EP0216127,P63,F3 in which R**1 to R**5 and R**10 have the meanings indicated for formula I or III, c) oxidation of the hemiacetal of the formula V to give the corresponding lactone of the formula VI see diagramm : EP0216127,P64,F1 in which R**1 to R**5 have the meanings indicated for formula I and R**10 has the meanings indicated for formula III, and d) conversion of the protected hydroxylactone of the formula VI into the 6-phenoxymethyl-4-hydroxytetrahydropyran-2-one of the formula I see diagramm : EP0216127,P64,F2 where appropriate the compound of the formula I which has been obtained being converted into the corresponding open-chain dihydroxy carboxylic acid of the formula VII see diagramm : EP0216127,P64,F3 its salt or its ester, where appropriate a salt or ester which has been obtained being converted into the free dihydroxy carboxylic acid or, where appropriate, the free carboxylic acid being converted into the salt or ester.

    3-DEMETHYLMEVALONIC ACID DERIVATIVES
    12.
    发明专利
    3-DEMETHYLMEVALONIC ACID DERIVATIVES 未知

    公开(公告)号：AU583943B2

    公开(公告)日：1989-05-11

    申请号：AU6202886

    申请日：1986-08-28

    Applicant: HOECHST AG

    Inventor： BECK GERHARD ,  KEREKJARTO BELA VON ,  LAU HANS-HERMANN ,  WESS GUNTHER

    IPC: C07D409/06 ,  A61K31/35 ,  A61K31/351 ,  A61K31/365 ,  A61K31/366 ,  A61K31/38 ,  A61K31/381 ,  A61P3/06 ,  A61P9/10 ,  C07C51/00 ,  C07C51/09 ,  C07C57/30 ,  C07C57/58 ,  C07C59/48 ,  C07C59/54 ,  C07C59/56 ,  C07C59/64 ,  C07C59/72 ,  C07C67/00 ,  C07C67/08 ,  C07C69/66 ,  C07C69/732 ,  C07C69/734 ,  C07D309/10 ,  C07D309/30 ,  C07D333/00 ,  C07D333/16 ,  C07D333/24 ,  C07D409/10 ,  C07F7/18 ,  C07F9/54 ,  C07D407/10 ,  C07D405/10 ,  C07D307/54 ,  C07D213/55 ,  C07D213/61 ,  C07D307/56 ,  C07D333/28 ,  C07F7/10

    Abstract: 1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE) A 3-demethylmevalonic acid derivative of the formula I (delta-lactone) or la (corresponding dihydroxy carboxylic acid derivative) see diagramm : EP0217092,P37,F1 see diagramm : EP0217092,P37,F2 in which A-B denotes a radical of the formula -CH=CH- or -CH2 -CH2 -, Z denotes a -CH2 - or -CH2 -CH2 - group, R**1 denotes a cycloaliphatic hydrocarbon radical which has 3 to 7 carbon atoms and is optionally substituted with 1 or 2 methyl groups, R**2 and R**3 denote hydrogen, halogen, trifluoromethyl, alkyl or alkoxy, each having 1-6 carbon atoms, R**4 denotes hydrogen or a straight-chain or branched C1 -C5 -alkyl radical, benzyl, benzyl which is substituted 1-2 times by C1 -C4 -alkyl or halogen, alkali metal or ammonium (NH4-+ ) or ammonium ion which is substituted with C1 -C4 -alkyl or hydroxy-C1 -C4 -alkyl. 1. Claims (for the Contracting State AT) A process for the preparation of 3-demethylmevalonic acid derivatives of the formula I (delta -lactone) and la (corresponding dihydroxy carboxylic acid derivative) see diagramm : EP0217092,P40,F1 see diagramm : EP0217092,P40,F2 in which A-B denotes a radical of the formula -CH=CH- or - CH2 -CH2 Z denotes a -CH2 - or -CH2 -CH2 - group, R**1 denotes a cycloaliphatic hydrocarbon radical which has 3 to 7 carbon atoms and is optionally substituted with 1 or 2 methyl groups, R**2 and R**3 denote hydrogen, halogen, trifluoromethyl, alkyl or alkoxy, each having 1-6 carbon atoms, R**4 denotes hydrogen or a straight-chain or branched C1 -C5 -alkyl radical, benzyl, benzyl which is substituted 1-2 times by C1 -C4 -alkyl or halogen, alkali metal or ammonium (NH4 **+ ) or ammonium ion which is substituted with C1 -C4 -alkyl or hydroxy-C1 -C4 -alkyl, which comprises a) reaction of the phosphonium salts of the formula II see diagramm : EP0217092,P40,F3 in which R**1 , R**2 , R**3 and Z have the meaning indicated for formula I, and X is CI, Br or I, with the chiral aldehyde of the formula III see diagramm : EP0217092,P40,F4 in which R**5 denotes a protective group which is stable to bases and weak acids, to give a compound of the formula see diagramm : EP0217092,P40,F5 in which R**1 , R**2 , R**3 and Z have the meaning given for formula I, R**5 has the meaning given for formula III (and A-B represents the (-CH=CH-) group), b) acid hydrolysis of the methyl acetal group in a compound of the general formula IV to give a lactol of the formula V see diagramm : EP0217092,P41,F1 in which R**1 , R**2 , R**3 and Z have the meaning given for formula I, R**5 has the meaning given for formula III (and A-B represents the (-CH=CH-) group), c) oxidation of the compound of the general formula V to give a lactone of the formula VI see diagramm : EP0217092,P41,F2 in which R**1 , R**2 and R**3 and Z have the meaning given for formula I, R**5 has the meaning given for formula III (and A-B represents the (-CH=CH-) group), d) elimination of the protective group R**5 in a compound of the general formula VI to give a compound of the formula I in which R**1 , R**2 , R**3 and Z have the meanings indicated for formula I, and A-B represents the (-CH=CH-) group, where appropriate hydrogenation of a compound of the general formula I in which A-B represents a (-CH=CH-) group to give a compound of the general formula I in which A-B represents a (-CH2 -CH2 -) group, it also being possible to carry out the hydrogenation on the compounds of the formula IV, V or VI to give corresponding compounds in which A-B represents the (-CH2 -CH2 -) group, where appropriate conversion of a hydroxy lactone I into the corresponding free hydroxy acids la or their salts, or, where appropriate, preparation of the corresponding ester from the free hydroxy acids la or from the hydroxy lactone I.

    13.
    发明专利
    未知

    公开(公告)号：PT99713B

    公开(公告)日：1999-05-31

    申请号：PT9971391

    申请日：1991-12-06

    Applicant: HOECHST AG

    Inventor： KRAMER WERNER ,  MULLNER STEFAN ,  WESS GUNTHER ,  NEUBAUER HORST

    IPC: A61K31/575 ,  A61K31/58 ,  A61P3/06 ,  C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00

    Abstract: The invention relates to bile acid derivatives of the formula I G1-X-G2(I) in which G1 and G2 are bile acid radicals or modified bile acid radicals in the form of the free acids, the esters or amides, the salt forms and also the forms derivatized on the alcohol groups and X is a bridge group or a single covalent bond, it being possible for G1 and G2 to be optionally bonded via X. The compounds according to the invention have a high affinity for the specific bile acid transport system of the small intestine and inhibit bile acid absorption in a concentration-dependent and competitive manner.

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