CA2724181 IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES

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Application Number 2724181

Application Date 13.05.2009

Publication Number 2724181

Publication Date 19.11.2009

Publication Kind A1

IPC

CPC

Applicants SHIRE LLC

Inventors GOLDING, BERNARD
FRANKLIN, RICHARD
MACLEOD, ANGUS

Priority Data 0808944.3 16.05.2008 GB

Title

(EN) IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES

(FR) DERIVES D'IMIDAZOQUINAZOLINE EN TANT QU'ANALOGUES D'ANAGRELIDE POUR LE TRAITEMENT DE SYNDROMES MYELOPROLIFERATIFS 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 treat-ment 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 utili-ty as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

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 or 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
02	Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

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 or 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

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1. CA2724181 - IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES