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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
C07D 263/48 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
34with 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
48Nitrogen atoms not forming part of a nitro radical
C07D 413/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61K 31/421
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
4211,3-Oxazoles, e.g. pemoline, trimethadione
A61K 31/422
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 13/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • PHARMAGENE LABORATORIES LIMITED [GB]/[GB]
Inventors
  • OXFORD, Alexander, William
  • BORMAN, Richard, Anthony
  • COLEMAN, Robert, Alexander
  • CLARK, Kenneth, Lyle
  • HYND, George
  • ARCHER, Janet, Ann
  • ALEY, Amanda
  • HARRIS, Neil, Victor
Agents
  • WATSON, Robert, J.
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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