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1. (WO2009138789) SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2009/138789 International Application No.: PCT/GB2009/050509
Publication Date: 19.11.2009 International Filing Date: 13.05.2009
Chapter 2 Demand Filed: 11.02.2010
IPC:
C07D 471/14 (2006.01) ,A61K 31/519 (2006.01) ,A61P 7/00 (2006.01) ,C07D 487/14 (2006.01) ,C07D 495/14 (2006.01) ,C07D 491/147 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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
12
in which the condensed system contains three hetero rings
14
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
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
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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic 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
12
in which the condensed system contains three hetero rings
14
Ortho-condensed systems
147
the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
Applicants:
GOLDING, Bernard [GB/GB]; GB (UsOnly)
FRANKLIN, Richard [GB/GB]; GB (UsOnly)
HIRST, Kim [GB/GB]; GB (UsOnly)
SHIRE LLC [US/US]; 9200 Brookfield Court Florence, Kentucky 41042, US (AllExceptUS)
Inventors:
GOLDING, Bernard; GB
FRANKLIN, Richard; GB
HIRST, Kim; GB
Agent:
HARRISON GODDARD FOOTE; Belgrave Hall Belgrave Street Leeds West Yorkshire LS2 8DD, GB
Priority Data:
0808950.016.05.2008GB
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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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)