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1. WO2001044194 - PROPANOIC ACID DERIVATIVES AS INTEGRIN INHIBITORS

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Publication Number WO/2001/044194
Publication Date 21.06.2001
International Application No. PCT/GB2000/004831
International Filing Date 15.12.2000
Chapter 2 Demand Filed 22.05.2001
IPC
C07D 213/74 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/89 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
89with hetero atoms directly attached to the ring nitrogen atom
C07D 401/12 2006.1
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
12linked by a chain containing hetero atoms as chain links
CPC
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 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 213/74
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/89
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
89with hetero atoms directly attached to the ring nitrogen atom
C07D 401/12
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
12linked by a chain containing hetero atoms as chain links
Applicants
  • CELLTECH R & D LIMITED [GB]/[GB] (AllExceptUS)
  • ALEXANDER, Rikki, Peter [GB]/[GB] (UsOnly)
  • LANGHAM, Barry, John [GB]/[GB] (UsOnly)
  • REUBERSON, James, Thomas [GB]/[GB] (UsOnly)
  • TROWN, Emma, Louise [GB]/[GB] (UsOnly)
  • WARRELLOW, Graham, John [GB]/[GB] (UsOnly)
Inventors
  • ALEXANDER, Rikki, Peter
  • LANGHAM, Barry, John
  • REUBERSON, James, Thomas
  • TROWN, Emma, Louise
  • WARRELLOW, Graham, John
Agents
  • MERCER, Christopher, Paul
Priority Data
9929988.517.12.1999GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROPANOIC ACID DERIVATIVES AS INTEGRIN INHIBITORS
(FR) DERIVES D'ACIDE PROPANOIQUE EN TANT QU'INHIBITEURS D'INTEGRINE
Abstract
(EN) Propanoic acid derivatives of formula (1) are described: Ar-X1-Ar1-Z-R; in which Ar is a nitrogen base containing group; X1 is a linker atom or group; Ar1 is an optionally substituted pyridine or pyridine-N-oxide; Z is a group -CH(R13)CH2- [in which R13 is R13a or Alk1aR13a, R13a is a hydrogen atom or an optionally substituted aliphatic, cycloaliphatic heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group and Alk1a is an optionally substituted C1-3alkylene chain], -C(R12a)(R13)-CH(R12b)- [in which R12a and R12b together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or -C(R13)=CH-; R is a carboxylic acid (-CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
(FR) La présente invention concerne des dérivés d'acide propanoïque de formule (1) Ar-X1-Ar1-Z-R; dans laquelle: Ar est un groupe contenant des bases azotées; X1 est un atome ou groupe de liaison; Ar1 est un pyridine-N-oxyde ou une pyridine éventuellement substituée; Z est un groupe -CH(R13)CH2- [dans lequel R13 est R13a ou Alk1aR13a, R13a est un atome d'hydrogène ou un groupe aliphatique, cycloaliphatique, hétéroaliphatique, hétérocycloaliphatique, aromatique ou hétéroaromatique éventuellement substitué et Alk1a est une chaîne alkylène C1-3 éventuellement substituée], -C(R12a)(R13)-CH(R12b)- [dans lequel R12a et R12b forment avec les atomes de carbone auquels ils sont liés, un groupe cycloalkyle C3-7] ou -C(R13)=CH-; R est un acide carbocyclique (-CO2H) ou un dérivé ou biostère de cet acide; et les sels, solvates, hydrates et N-oxydes desdits dérivés. Les composés permettent d'inhiber la liaison des intégrines à leurs ligands et s'avèrent utiles pour la prévention et le traitement des troubles immunitaires et inflammatoires.
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