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1. WO2009138789 - SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS

Publication Number WO/2009/138789
Publication Date 19.11.2009
International Application No. PCT/GB2009/050509
International Filing Date 13.05.2009
Chapter 2 Demand Filed 11.02.2010
IPC
C07D 471/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/519 2006.1
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 7/00 2006.1
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
C07D 487/14 2006.1
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
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 495/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 491/147 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
147the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
CPC
A61P 7/00
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
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
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 487/14
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
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 491/147
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
147the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
Applicants
  • SHIRE LLC [US]/[US] (AllExceptUS)
  • GOLDING, Bernard [GB]/[GB] (UsOnly)
  • FRANKLIN, Richard [GB]/[GB] (UsOnly)
  • HIRST, Kim [GB]/[GB] (UsOnly)
Inventors
  • GOLDING, Bernard
  • FRANKLIN, Richard
  • HIRST, Kim
Agents
  • HARRISON GODDARD FOOTE
Priority Data
0808950.016.05.2008GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS
(FR) QUINAZOLINES SUBSTITUÉES EN TANT QU'AGENTS DE RÉDUCTION DU NOMBRE DES PLAQUETTES SANGUINES
Abstract
(EN) This invention relates to the discovery of 3-and 5-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 (I) shown below wherein the meanings of the substituents are 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 en position 3 et 5 de l'anagrélide, un agent de réduction sélective du nombre des plaquettes, présentant un potentiel réduit d'effets secondaires cardiovasculaires et qui, par conséquent, 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 (I) ci-dessous, dans laquelle les significations des substituants sont 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.
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