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1. WO1997023465 - NEW BARBITURIC ACID DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL AGENTS CONTAINING THESE COMPOUNDS

Publication Number WO/1997/023465
Publication Date 03.07.1997
International Application No. PCT/EP1996/005766
International Filing Date 20.12.1996
Chapter 2 Demand Filed 23.05.1997
IPC
C07D 239/62 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
60Three or more oxygen or sulfur atoms
62Barbituric acids
C07D 401/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
A61P 27/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
A61P 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
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)
Applicants
  • BOEHRINGER MANNHEIM GMBH [DE]/[DE] (AllExceptUS)
  • BOSIES, Elmar [DE]/[DE] (UsOnly)
  • ESSWEIN, Angelika [DE]/[DE] (UsOnly)
  • GRAMS, Frank [DE]/[DE] (UsOnly)
  • KRELL, Hans-Willi [AT]/[DE] (UsOnly)
  • MENTA, Ernesto [IT]/[IT] (UsOnly)
Inventors
  • BOSIES, Elmar
  • ESSWEIN, Angelika
  • GRAMS, Frank
  • KRELL, Hans-Willi
  • MENTA, Ernesto
Common Representative
  • BOEHRINGER MANNHEIM GMBH
Priority Data
195 48 624.223.12.1995DE
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NEW BARBITURIC ACID DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL AGENTS CONTAINING THESE COMPOUNDS
(FR) NOUVEAUX DERIVES D'ACIDE BARBITURIQUE, LEURS PROCEDES DE PRODUCTION ET SUBSTANCES PHARMACEUTIQUES CONTENANT LESDITS DERIVES
Abstract
(EN)
Compounds of formula (I) in which X, Y and Z are independently of one another oxygen, sulphur or NH; R1 represents a group W-V: W is a valence dash or a straight-chained or branched C1-C8 alkyl or a C2-C8 alkenyl group which is optionally once or several times substituted, V is an optionally substituted monocycle or bicycle which can contain one or several heteroatoms, or W-V is a C1-C20 alkyl group which can be interrupted by heteroatoms, one or several carbon atoms are optionally substituted; R2 and R3 represent hydrogen or one of the two represents lower alkyl or lower acyl; R4 and R5 denote independently of each other for A-D, wherein A represents a dash alkyl, alkenyl, acyl, alkylsulfonyl, sulfonyl, alkylaminocarbonyl, aminocarbonyl, alkoxycarbonyl, oxy-carbonyl, alkylaminothiocarbonyl, aminothio-carbonyl which is optionally once or several times substituted; D represents a hydrogen, monocycle or bicycle, the monocycle or bicycle is optionally once or several times interrupted by heteroatoms and the monocycle or bicycle is once or several times substituted, or R4 and R5 together with the adjacent N atom form a ring; pharmacologically acceptable salts and prodrugs thereof and optically active forms, processes for their production and pharmaceutical agents which contain these compounds having a matrix metalloprotease-inhibitory action.
(FR)
L'invention concerne des composés de formule (I) et leurs sels pharmaceutiquement acceptables ainsi que leurs promédicaments et des formes optiquement actives. Dans la formule (I), X, Y et Z représentent indépendamment l'un de l'autre oxygène, soufre ou NH; R1 représente un groupe W-V, W représentant un trait de valence ou un alkyle C1-C8 linéaire ou ramifié ou un groupe alcényle C2-C8 éventuellement substitué une ou plusieurs fois; V représentant un monocycle ou un bicycle éventuellement substitué pouvant contenir au moins un hétéroatome, ou W-V représentant un groupe alkyle C1-C20 pouvant être interrompu par des hétéroatomes, au moins un atome de carbone éventuellement substitué; R2 et R3 représentent hydrogène ou l'un des deux représente alkyle inférieur ou acyle inférieur; R4 et R5 représentent indépendamment l'un de l'autre A-D, A représentant l'un des radicaux suivants à valence libre et éventuellement substitués une ou plusieurs fois: alkyle, alcényle, acyle, alkylsulfonyle, sulfonyle, alkylaminocarbonyle, aminocarbonyle, alcoxycarbonyle, oxycarbonyle, alkylaminothiocarbonyle, aminothiocarbonyle; D représentant un hydrogène, un monocycle ou un bicycle, ces deux derniers étant éventuellement interrompus une ou plusieurs fois par des hétéroatomes et substitués une ou plusieurs fois, ou R4 et R5 conjointement avec l'atome de N adjacent forment un noyau. L'invention concerne également des procédés de production desdits composés ainsi que des substances pharmaceutiques contenant ces composés présentant un effet d'inhibition de la métalloprotéase matricielle.
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