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1. EP2313410 - IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES

Office
European Patent Office
Application Number 09746111
Application Date 13.05.2009
Publication Number 2313410
Publication Date 27.04.2011
Publication Kind A1
IPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519
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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants SHIRE LLC
Inventors GOLDING BERNARD
FRANKLIN RICHARD
MACLEOD ANGUS
Priority Data 0808944 16.05.2008 GB
Title
(DE) IMIDAZOCHINAZOLINDERIVATE ALS ANAGRELIDANALOGA ZUR BEHANDLUNG MYELOPROLIFERATIVER ERKRANKUNGEN UND THROMBOTISCHER ERKRANKUNGEN
(EN) IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES
(FR) DÉRIVÉS D'IMIDAZOQUINAZOLINE EN TANT QU'ANALOGUES D'ANAGRÉLIDE POUR LE TRAITEMENT DE SYNDROMES MYÉLOPROLIFÉRATIFS ET DE SYNDROMES THROMBOTIQUES
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 wherein the substituents have the meanings defined in claim 1: 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) L'invention concerne la découverte d'analogues substitués de l'anagrélide, un agent de réduction sélective du nombre des plaquettes, présentant un potentiel réduit d'effets secondaires cardiovasculaires et qui devraient conduire à une observance thérapeutique et à une sécurité améliorées dans le traitement de syndromes myéloprolifératifs. Plus spécifiquement, la présente invention concerne certains dérivés d'imidazoquinazoline représentés par la formule générale décrite ci-dessous, dans laquelle les substituants présentent les significations définies dans la revendication 1, et qui présentent une utilité en tant qu'agents de réduction du nombre des plaquettes chez les êtres humains. Les composés de la présente invention agissent en inhibant la mégacaryocytopoïèse et par conséquent la formation des plaquettes sanguines.