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1. WO2003068226 - 2-OXAZOLAMINES AND THEIR USE AS 5-HT2B RECEPTOR ANTAGONISTS

Publication Number WO/2003/068226
Publication Date 21.08.2003
International Application No. PCT/GB2003/000552
International Filing Date 11.02.2003
Chapter 2 Demand Filed 09.09.2003
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
30
having two or three double bonds between ring members or between ring members and non-ring members
34
with 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
48
Nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C07D 263/48 (2006.01)
C07D 413/04 (2006.01)
CPC
C07D 263/48
C07D 413/04
Applicants
  • PHARMAGENE LABORATORIES LIMITED [GB/GB]; 2 Orchard Road Royston Hertfordshire SG8 5HD, GB
Inventors
  • OXFORD, Alexander, William; GB
  • BORMAN, Richard, Anthony; GB
  • COLEMAN, Robert, Alexander; GB
  • CLARK, Kenneth, Lyle; GB
  • HYND, George; GB
  • ARCHER, Janet, Ann; GB
  • ALEY, Amanda; GB
  • HARRIS, Neil, Victor; GB
Agents
  • WATSON, Robert, J. ; Mewburn Ellis York House 23 Kingsway London Greater London WC2B 6HP, GB
Priority Data
0203412.213.02.2002GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 2-OXAZOLAMINES AND THEIR USE AS 5-HT2B RECEPTOR ANTAGONISTS
(FR) 2-OXAZOLAMINES ET LEUR UTILISATION COMME ANTAGONISTES DU RECEPTEUR 5-HT2B
Abstract
(EN)
The present invention relates to compounds of formula (I): wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either:(i) independently selected from H, R, R', SO2R, C(=O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R' is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT2B receptor.
(FR)
La présente invention concerne les composés de la formule (I) où R1 ou R4 est sélectionné dans le groupe constitué de H et alkyle C1-6, cycloalkyle C3-7, cycloalkyle C3-7-alkyle C1-4, et phényle-alkyle C1-4 éventuellement substitués; l'autre R1 ou R4 respectivement restant représentant un groupe aryle C9-14 éventuellement substitué; R2 et R3 sont soit (i) indépendamment sélectionnés parmi H, R, R', SO2R, C(=O)R, (CH2)nNR5R6, où n vaut 1 à 4 et R5 et R6 sont indépendamment sélectionnés parmi H et R, R représentant alkyle C1-4 éventuellement substitué, et R' représentant phényle-C1-4 alkyle éventuellement substitué, soit (ii) ils forment, avec l'atome d'azote auquel ils sont liés, un groupe hétérocyclique C5-7 éventuellement substitué. L'invention concerne également leur utilisation comme produits pharmaceutiques, notamment pour traiter les états atténués par l'antagonisme d'un récepteur 5-HT2B.
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