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1. WO2009138796 - IMIDAZO [2,1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS

Publication Number WO/2009/138796
Publication Date 19.11.2009
International Application No. PCT/GB2009/050517
International Filing Date 13.05.2009
Chapter 2 Demand Filed 12.02.2010
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
5025
ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C07D 487/04 (2006.01)
A61K 31/5025 (2006.01)
A61P 7/02 (2006.01)
CPC
C07D 487/04
Applicants
  • SHIRE LLC [US/US]; 9200 Brookfield Court Florence, Kentucky 41042, US (AllExceptUS)
  • GOLDING, Bernard, T. [GB/GB]; GB (UsOnly)
  • FRANKLIN, Richard [GB/GB]; GB (UsOnly)
  • MACLEOD, Angus [GB/GB]; GB (UsOnly)
  • CICALA, Peter [US/US]; US (UsOnly)
Inventors
  • GOLDING, Bernard, T.; GB
  • FRANKLIN, Richard; GB
  • MACLEOD, Angus; GB
  • CICALA, Peter; US
Agents
  • HARRISON GODDARD FOOTE; Belgrave Hall Belgrave Street Leeds West Yorkshire LS2 8DD, GB
Priority Data
0808947.616.05.2008GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) IMIDAZO [2,1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS
(FR) QUINAZOLINES SUBSTITUÉS
Abstract
(EN)
This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below where the substituents have the meanings defined in claim (I) and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
(FR)
La présente invention concerne la découverte d’analogues substitués de l’agent permettant la réduction sélective du nombre de plaquettes, l’anagrélide, présentant un potentiel de survenue d’effets secondaires cardio-vasculaires réduit et susceptible d’entraîner une amélioration de l’observance du traitement et de la sécurité du patient, dans le cadre du traitement de maladies myéloprolifératives. Plus spécifiquement, la présente invention porte sur certains dérivés imidoazoquinazoline présentant la formule générale indiquée ci-dessous, dans laquelle les substituants présentent des significations telles que définies à la revendication 1 et présentant une utilité en tant qu’agent permettant la réduction du nombre de plaquettes chez l’humain. Les composés de la présente invention agissent par inhibition de la mégacaryocytopoïèse et, par conséquent, de la formation des plaquettes sanguines.
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