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1. WO1999033789 - αSUBSTITUTED β-ALANINES

Publication Number WO/1999/033789
Publication Date 08.07.1999
International Application No. PCT/GB1998/003859
International Filing Date 23.12.1998
Chapter 2 Demand Filed 20.07.1999
IPC
C07C 275/42 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
275Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
42being further substituted by carboxyl groups
C07D 207/27 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18having one double bond between ring members or between a ring member and a non-ring member
22with 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
24Oxygen or sulfur atoms
262-Pyrrolidones
263with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
27with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
CPC
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
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 35/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
04specific for metastasis
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
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applicants
  • AVENTIS PHARMA LIMITED [GB]/[GB] (AllExceptUS)
  • ASTLES, Peter, Charles [GB]/[GB] (UsOnly)
  • HARRIS, Neil, Victor [GB]/[GB] (UsOnly)
  • MORLEY, Andrew, David [GB]/[GB] (UsOnly)
Inventors
  • ASTLES, Peter, Charles
  • HARRIS, Neil, Victor
  • MORLEY, Andrew, David
Agents
  • CAFFIN, Lee
Priority Data
60/092,60213.07.1998US
9727532.523.12.1997GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) αSUBSTITUTED β-ALANINES
(FR) β-ALANINES SUBSTITUEES
Abstract
(EN)
The invention is directed to physiologically active compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 [where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group -L1-(CH2)n-C(=O)-N(R4)-CH2-CH2-Y]; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4(α4β1).
(FR)
L'invention concerne des composés physiologiquement actifs de la formule générale (I) dans laquelle R1 représente hydrogène, halogène, alkyle inférieur ou alcoxy inférieur, X1, X2 et X6 représentent indépendamment N ou CR2; et X3, X4 ou X5 représente CR3 et les autres représentent indépendamment N ou CR2[où R2 représente hydrogène, halogène, alkyle inférieur ou alcoxy inférieur; et R3 représente un groupe -L1-(CH2)n-C(=O)-N(R4)-CH2-CH2-Y]; et leurs promédicaments, ainsi que des sels et solvates acceptables pharmaceutiquement de ces composés et leurs promédicaments. Ces composés présentent des propriétés pharmaceutiques de valeur, notamment la capacité de réguler l'interaction de VCAM -1 et la fibronectine avec l'intégrine VAL-4(α4β1).
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