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1. WO1992016504 - NEW LEUKOTRIENE B4 DERIVATIVES, METHOD FOR PREPARING THEM AND THEIR USE AS DRUGS

Publication Number WO/1992/016504
Publication Date 01.10.1992
International Application No. PCT/DE1992/000151
International Filing Date 24.02.1992
IPC
C07C 33/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
33Unsaturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
05Alcohols containing rings other than six-membered aromatic rings
12containing five-membered rings
C07C 59/46 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
59Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40Unsaturated compounds
42containing hydroxy or O-metal groups
46containing rings other than six-membered aromatic rings
C07C 69/007 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
007Esters of unsaturated alcohols having the esterified hydroxy group bound to an acyclic carbon atom
C07C 69/732 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxyl 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
73of unsaturated acids
732of unsaturated hydroxy carboxylic acids
C07C 405/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
405Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 33/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
33Unsaturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
05Alcohols containing rings other than six-membered aromatic rings
12containing five-membered rings
C07C 405/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
405Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
Applicants
  • SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN [DE]/[DE] (AllExceptUS)
  • SKUBALLA, Werner [DE]/[DE] (UsOnly)
  • BUCHMANN, Bernd [DE]/[DE] (UsOnly)
  • HEINDL, Josef [DE]/[DE] (UsOnly)
  • FRÖHLICH, Wolfgang [DE]/[DE] (UsOnly)
  • EKERDT, Roland [DE]/[DE] (UsOnly)
  • GIESEN, Claudia [DE]/[DE] (UsOnly)
Inventors
  • SKUBALLA, Werner
  • BUCHMANN, Bernd
  • HEINDL, Josef
  • FRÖHLICH, Wolfgang
  • EKERDT, Roland
  • GIESEN, Claudia
Priority Data
P 41 08 351.212.03.1991DE
Publication Language German (de)
Filing Language German (DE)
Designated States
Title
(DE) NEUE LEUKOTRIEN-B4-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL
(EN) NEW LEUKOTRIENE B4 DERIVATIVES, METHOD FOR PREPARING THEM AND THEIR USE AS DRUGS
(FR) NOUVEAUX DERIVES DE LEUCOTRIENES B4, LEUR PROCEDE DE PREPARATION ET LEUR UTILISATION COMME MEDICAMENTS
Abstract
(DE) Leukotrien-B4-Derivate der Formel (I) werden beschrieben, worin R1 CH2OH, CH3, CF3, COOR5, CONR6R7, oder R1 gemeinsam mit R2 eine Carbonylgruppe bedeutet, R2 und R3 gleich oder verschieden H oder ein organischer Säurerest mit 1-15 C-Atomen darstellen, R4 H, C1-C10 gegebenenfalls einfach oder mehrfach durch Chlor oder Brom substituierter Alkyl, C3-C10-Cycloalkyl, gegebenenfalls unabhängig voneinander einfach oder mehrfach durch Chlor, Brom, Phenyl, C1-C4-Alkyl, C1-C4-Alkoxy, Fluormethyl, Chlormethyl, Trifluormethyl, Carboxy oder Hydroxy substituierter C6-C10-Arylrest oder ein 5-6 gliedriger aromatischer heterocyclischer Ring mit wenigstens 1 Heteroatom symbolisieren, R5 Wasserstoff, C1-C10 Alkyl, C3-C10 Cycloalkyl, gegebenenfalls durch 1-3 Chlor, Brom, Phenyl, C1-C4-Alkyl, C1-C4-Alkoxy, Fluormethyl, Chlormethyl, Trifluormethyl, Carboxy oder Hydroxy substituierter C6-C10 Arylrest, CH2-CO-(C6-C10) Aryl oder ein 5-6 gliedriger Ring mit weinigstens 1 Heteroatom bedeutet, A eine trans,trans-CH=CH-CH=CH, eine -CH2CH2-CH=CH- oder eine Tetramethylengruppe, B eine C1-C10 gerad- oder verzweigtkettige Alkylengruppe, die gegebenenfalls durch Fluor substituiert sein kann oder die Gruppe (a), symbolisiert, D eine Direktbindung, Sauerstoff, Schwefel, -C=C-, -CH=CR8, oder gemeinsam mit B auch eine Direktbindung bedeuten können, R6 und R7 gleich oder verschieden sind und H oder C1-C4-Alkyl oder R7 H und R6 C1-C10-Alkanoyl oder C1-C10 Alkansulfonyl darstellen, R8 H, C1-C5 Alkyl, Chlor, Brom bedeutet, n 3-5 ist sowie, wenn R5 Wasserstoff bedeutet, deren Salze mit physiologisch verträglichen Basen und deren Cyclodextrinclathrate.
(EN) The invention discloses new leukotriene B4 derivatives of formula (I), wherein R1 stands for CH2OH, CH3, CF3, COOR5, CONR6R7, or R1 together with R2 stands for a carbonyl group, R2 and R3 are the same or different and stand for H or an organic acid residue containing 1 to 15 carbon atoms, R4 stands for H, C1-C10 alkyl, possibly substituted one or more times by chlorine or bromine, C3-C10 cycloalkyl, a C6-C10 aryl residue possibly substituted one or more times by chlorine, bromine or phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, or a 5- or 6-membered aromatic heterocyclic ring with at least one heteroatom, R5 stands for hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, a C6-C10 aryl residue possibly substituted one to three times by chlorine, bromine or phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxy or hydroxy, CH2-CO-(C6-C10) aryl or a 5- or 6-membered ring with at least one heteroatom, A stands for a trans,trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B stands for a C1-C10 straight-chain or branched-chain alkylene group, possibly substituted by fluorine, or the group of formula (a), D stands for a direct bond, oxygen, sulphur, -C=C-, -CH=CR8 or, together with B, for a direct bond, R6 and R7 are the same or different and stand for H or C1-C4 alkyl or R7 stands for H and R6 stands for C1-C10 alkanoyl or C1-C10 alkanesulphonyl, R8 stands for H, C1-C5 alkyl, chlorine or bromine, n is equal to 3 to 5 and, when R5 stands for hydrogen, their salts with physiologically tolerable bases and their cyclodextrin clathrates.
(FR) Des dérivés de leucotriènes B4 ont la formule (I), dans laquelle R1 désigne CH2OH, CH3, CF3, COOR5, CONR6R7, ou R1 désigne avec R2 un groupe carbonyle; R2 ou R3 sont identiques ou différents et désignent H ou un résidu acide organique ayant 1 à 15 atomes de carbone; R4 désigne H, alkyle C1-C10 éventuellement substitué une ou plusieurs fois par chlore ou brome, cycloalkyle C3-C10, un résidu aryle C6-C10 éventuellement substitué une ou plusieurs fois par chlore, brome, phényle, alkyle C1-C4, alcoxy C1-C4, fluorométhyle, chlorométhyle, trifluorométhyle, carboxy ou hydroxy, ou un composé hétérocyclique aromatique penta- ou hexagonal ayant au moins un hétéroatome; R5 désigne hydrogène, alkyle C1-C10, cycloalkyle C3-C10. un résidu aryle C6-C10 éventuellement substitué par 1 à 3 chlores, bromes, phényles, alkyles C1-C4, alcoxys C1-C4, fluorométhyles, chlorométhyles, trifluorométhyles, carboxys ou hydroxys, aryle CH2-CO-(C6-C10) ou un composé cyclique penta- ou hexagonal ayant au moins 1 hétéroatome; A désigne un groupe trans, trans-CH=CH-CH=CH, -CH2CH2-CH=CH- ou tétraméthylène; B désigne un groupe alkylène C1-C10 à chaîne droite ou ramifiée, qui peut le cas échéant être substitué par du fluor, ou B désigne le groupe (a); D désigne une liaison directe, oxygène, soufre, -C=C-, -CH=CR8 ou peut désigner ensemble avec B une liaison directe également; R6 et R7 sont identiques ou différents et désignent H ou alkyle C1-C4, ou R7 désigne H et R6 désigne alcanoyle C1-C10 ou alcansulfonyle C1-C10, R8 désigne H, alkyle C1-C5, chlore, brome; n est compris entre 3 et 5, et lorsque R5 désigne hydrogène, les sels de ces dérivés avec des bases physiologiquement tolérables et leur clathrates de cyclodextrine.
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