WO2003016259A3 - Milchsäureelemente enthaltende verbindungen, deren herstellung sowie deren verwendung als pharmazeutische wirkstoffe - Google Patents

Milchsäureelemente enthaltende verbindungen, deren herstellung sowie deren verwendung als pharmazeutische wirkstoffe Download PDF

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Publication number
WO2003016259A3
WO2003016259A3 PCT/AT2002/000247 AT0200247W WO03016259A3 WO 2003016259 A3 WO2003016259 A3 WO 2003016259A3 AT 0200247 W AT0200247 W AT 0200247W WO 03016259 A3 WO03016259 A3 WO 03016259A3
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WO
WIPO (PCT)
Prior art keywords
lactic acid
acid elements
group
general formula
active substance
Prior art date
Application number
PCT/AT2002/000247
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English (en)
French (fr)
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WO2003016259A2 (de
Inventor
Christian R Noe
Jens Kruse
Bodo Lachmann
Regina Lauer
Original Assignee
Pharmacon Forschung & Beratung Gmbh
Christian R Noe
Jens Kruse
Bodo Lachmann
Regina Lauer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharmacon Forschung & Beratung Gmbh, Christian R Noe, Jens Kruse, Bodo Lachmann, Regina Lauer filed Critical Pharmacon Forschung & Beratung Gmbh
Priority to AU2002325614A priority Critical patent/AU2002325614A1/en
Publication of WO2003016259A2 publication Critical patent/WO2003016259A2/de
Publication of WO2003016259A3 publication Critical patent/WO2003016259A3/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/25—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/612—Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a six-membered aromatic ring in the acid moiety
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/675—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
    • C07C69/68—Lactic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Die Erfindung betrifft Milchsäureelemente enthaltende Verbindungen der allgemeinen Formel (I), worin n gleich 1-16 und die Bezeichnung * das Chiralitätszentrum der Milchsäureelemente bedeuten, wobei die Milchsäureelemente entweder mit einheitlicher oder mit unterschiedlicher Konfiguration am Chiralitätszentrum, gegebenenfalls in Form diastereomerer Mischungen vorliegen, worin R1 entweder die Acylgruppe eines unter sauren Bedingungen reaktionsfähigen Wirkstoffes darstellt, wobei in diesem Fall X für Sauerstoff und R2 für Wasserstoff oder einen geradkettigen oder verzweigten Alkylrest mit 1 bis 8 Kohlenstoffatomen stehen, oder worin R1 Wasserstoff für den Fall, dass X gleich Sauerstoff oder NR' ist, und R2 einen Wirkstoff mit einer mit dem Milchsäureelement veresterten Hydroxylgruppe (X gleich Sauerstoff) oder einen Wirkstoff mit einer mit dem Milchsäureelement amidierten Aminogruppe (X gleich NR') bedeuten, wobei R' für Wasserstoff bei Wirkstoffen vom Typ eines primären Amins und bei Wirkstoffen vom Typ eines sekundären Amins, im Falle eines nicht zyklischen sekundären Amins, für den Rest an der Aminogruppe des Wirkstoffes, im Fall eines zyklischen sekundären Amins für die kovalente Bindung von Stickstoff zu R2 steht, wobei für diesen Fall durch die allgemeine Formel (i) ein zyklisches sekundäres Amin definiert ist. Die Verbindung der allgemeinen Formel (I) können in einfach durchführbarer Weise aus Milchsäureoligomeren bzw. dimeren hergestellt werden. Die Erfindung betrifft weiters Arzneistoffe, insbesondere Prodrugs, welche zumindest eine Verbindung der allgemeinen Formel (I) zusammen mit einem pharmazeutisch verträglichen Träger enthalten.
PCT/AT2002/000247 2001-08-16 2002-08-16 Milchsäureelemente enthaltende verbindungen, deren herstellung sowie deren verwendung als pharmazeutische wirkstoffe WO2003016259A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002325614A AU2002325614A1 (en) 2001-08-16 2002-08-16 Compounds containing lactic acid elements, method for the production and use thereof as pharmaceutically active substances

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ATA1288/01 2001-08-16
AT12882001 2001-08-16

Publications (2)

Publication Number Publication Date
WO2003016259A2 WO2003016259A2 (de) 2003-02-27
WO2003016259A3 true WO2003016259A3 (de) 2003-09-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/AT2002/000247 WO2003016259A2 (de) 2001-08-16 2002-08-16 Milchsäureelemente enthaltende verbindungen, deren herstellung sowie deren verwendung als pharmazeutische wirkstoffe

Country Status (2)

Country Link
AU (1) AU2002325614A1 (de)
WO (1) WO2003016259A2 (de)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL196384B1 (pl) * 2005-01-11 2007-12-31 Ct Materialow Polimerowych I W Nowe estry niesteroidowych leków przeciwzapalnych i sposób ich wytwarzania
WO2008119518A1 (en) 2007-03-30 2008-10-09 Laccure Ab Use of oligomers of lactic acid in the treatment of gynaecological disorders
US9370502B2 (en) * 2012-07-16 2016-06-21 Laccure Ab Pharmaceutical compositions containing oligomeric lactic acid
EP2810640A1 (de) * 2013-06-03 2014-12-10 Basf Se Ester von Oligohydroxycarbonsäuren und deren Verwendung
AU2016279486B2 (en) * 2015-06-15 2021-04-01 Nmd Pharma A/S Compounds for use in treating neuromuscular disorders
US11147788B2 (en) 2017-12-14 2021-10-19 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11730714B2 (en) 2017-12-14 2023-08-22 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders

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Publication number Priority date Publication date Assignee Title
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US4216224A (en) * 1978-09-22 1980-08-05 Scott Eugene J Van Methods and compositions for treating psoriasis with retinoyl compounds
EP0573253A2 (de) * 1992-06-03 1993-12-08 Unilever Plc Topisches antibakterielles Mittel
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US5401773A (en) * 1990-02-22 1995-03-28 Roussel-Uclaf Lactic acid acylates
JPH0959218A (ja) * 1995-08-25 1997-03-04 Shimadzu Corp Ｌ−乳酸オリゴマー誘導体
WO1997020812A1 (en) * 1995-12-04 1997-06-12 Advanced Polymer Systems, Inc. RETINYL ESTERS OF α-HYDROXY ACIDS FOR TOPICAL IMPROVEMENT OF SKIN FUNCTION AND APPEARANCE
US5880152A (en) * 1995-10-06 1999-03-09 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
US5883123A (en) * 1995-10-06 1999-03-16 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
US5912269A (en) * 1996-04-30 1999-06-15 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
WO2001005750A1 (fr) * 1999-07-19 2001-01-25 Shionogi & Co., Ltd. COMPOSES DE p-TERPHENYLE A CHAINES LATERALES D'ACYLOXYMETHOXYCARBONYLE
WO2002072531A1 (fr) * 2001-03-13 2002-09-19 Amato Pharmaceutical Products, Ltd. Ester d'acide oligolactique a chaine

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2116347A (en) * 1937-08-25 1938-05-03 Dow Chemical Co Alpha-salicylo-aliphatic acid esters
DE1020324B (de) * 1954-12-17 1957-12-05 Boehringer Sohn Ingelheim Verfahren zur Herstellung von esterartigen Milchsaeurederivaten mit definierter Kettenlaenge und endstaendiger Ester-, Amid- oder Nitrilgruppe
US4216224A (en) * 1978-09-22 1980-08-05 Scott Eugene J Van Methods and compositions for treating psoriasis with retinoyl compounds
US5401773A (en) * 1990-02-22 1995-03-28 Roussel-Uclaf Lactic acid acylates
EP0573253A2 (de) * 1992-06-03 1993-12-08 Unilever Plc Topisches antibakterielles Mittel
US5270331A (en) * 1993-01-26 1993-12-14 Pfizer, Inc. Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides
JPH0959218A (ja) * 1995-08-25 1997-03-04 Shimadzu Corp Ｌ−乳酸オリゴマー誘導体
US5880152A (en) * 1995-10-06 1999-03-09 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
US5883123A (en) * 1995-10-06 1999-03-16 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
WO1997020812A1 (en) * 1995-12-04 1997-06-12 Advanced Polymer Systems, Inc. RETINYL ESTERS OF α-HYDROXY ACIDS FOR TOPICAL IMPROVEMENT OF SKIN FUNCTION AND APPEARANCE
US5912269A (en) * 1996-04-30 1999-06-15 Vertex Pharmaceuticals, Inc. Butyrate prodrugs derived from lactic acid
WO2001005750A1 (fr) * 1999-07-19 2001-01-25 Shionogi & Co., Ltd. COMPOSES DE p-TERPHENYLE A CHAINES LATERALES D'ACYLOXYMETHOXYCARBONYLE
WO2002072531A1 (fr) * 2001-03-13 2002-09-19 Amato Pharmaceutical Products, Ltd. Ester d'acide oligolactique a chaine

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AU2002325614A1 (en) 2003-03-03
WO2003016259A2 (de) 2003-02-27

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