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1. WO2003020282 - THIENO-(1,3)-OXAZIN-4-ONES WITH LIPASE INHIBITING ACTIVITY

Publication Number WO/2003/020282
Publication Date 13.03.2003
International Application No. PCT/GB2002/003903
International Filing Date 23.08.2002
Chapter 2 Demand Filed 13.03.2003
IPC
C07D 498/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 498/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
CPC
A61K 31/535
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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 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
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
Applicants
  • ALIZYME THERAPEUTICS LIMITED [GB]/[GB] (AllExceptUS)
  • HODSON, Harold, Francis [GB]/[GB] (UsOnly)
  • DUNK, Christopher, Robert [GB]/[GB] (UsOnly)
  • PALMER, Richard, Michael, John [GB]/[GB] (UsOnly)
  • MITCHELL, Dale, Robert [GB]/[GB] (UsOnly)
  • BIRAULT, Véronique [FR]/[GB] (UsOnly)
  • HUNT, Russell, George [GB]/[GB] (UsOnly)
Inventors
  • HODSON, Harold, Francis
  • DUNK, Christopher, Robert
  • PALMER, Richard, Michael, John
  • MITCHELL, Dale, Robert
  • BIRAULT, Véronique
  • HUNT, Russell, George
Agents
  • CORNISH, Kristina, Victoria, Joy
Priority Data
0121019.430.08.2001GB
0206031.714.03.2002GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) THIENO-(1,3)-OXAZIN-4-ONES WITH LIPASE INHIBITING ACTIVITY
(FR) ACTIVITE D'INHIBITION DE
Abstract
(EN) The use of a compound comprising formula (I), or a salt, ester, amide or prodrug thereof in the treatment of obesity and related disorders. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I): A is an optionally substituted thienyl moiety, Y is O, S, or NR2, R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups and R2 is hydrogen or a group as defined for R1.
(FR) L'invention concerne l'utilisation d'un composé de formule (I), ou d'un sel, d'un ester, d'un amide ou d'un prodrogue dudit composé utile dans le traitement de l'obésité et de troubles associés. L'invention concerne également de nouveaux composés de formule (I), des procédés de préparation de ces composés et des compositions pharmaceutiques les contenant. Dans la formule (I), A représente une fraction thiényl éventuellement substituée, Y représente O, S, ou NR2, R1 est un alkyle réticulé ou non réticulé (éventuellement interrompu par un ou plusieurs atomes d'oxygène), alcényle, alcynyle, cycloalkyle, cycloalcényle, aryle, arylalkyle, arylalkyle réduit, arylalcényle, hétéroaryle, hétéroarylalkyle, hétéroarylalcényle, aryle réduit, hétéroaryle réduit, hétéroarylalkyle réduit ou un dérivé substitué d'un quelconque des groupes précédents, et R2 représente hydrogène ou un groupe comme défini pour R1.
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