Isoquinoline derivatives and their therapeutical use
AssigneeSmithKline Beecham Corporation
InventorsSteven Coulton, Roderick Alan Porter, Mervyn Thompson
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Abstract
Novel isoquinoline derivatives and methods of using them to treat various neurological indications are disclosed.
Claims8
A compound of formula (I) or pharmaceutically acceptable salt thereof:
- where X and Q are independently a bond, methylene or ethylene groups such the ring structure Z is a five or six membered ring,
- R1 is hydrogen or C1-6 alkyl,
- R2 is hydrogen or up to four substituents independently selected from halogen, CF3, NO2, CN, N3, C1-6 alkylO—, C1-6 alkylS—, C1-6 alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3CO—, CF3O, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-,
- or —NR4R5 where R4 is hydrogen or C1-4 alkyl, and
- R5 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl, and
- R3 is hydrogen or up to two C1-6 alkyl groups.
A process for the preparation of compounds of formula (I), which comprises reacting a compound of formula (II)
- where R1A is R1 as defined for formula (I) or a group convertible to R1,
- with a compound of formula (III)
- where X, Q and Z are as defined for formula (I), and R2A,R3A are R2, R3 as defined for formula (I) or a group or groups convertible to R2, R3
- and where required converting a R1A, R2A or R3A group to a R1, R2 or R3 group, converting one R1, R2 or R3 group to another R1, R2 or R3 group, converting a salt product to the free base or another salt which is pharmaceutically acceptable, or converting a free base product to a pharmaceutically acceptable salt.
A pharmaceutical composition for use in the treatment and/or prophylaxis of disorders treatable and/or preventable with anti-convulsive agents, epilepsy, post-traumatic epilepsy, migraine, neuralgia, trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, which comprises a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier.
A method of treatment and/or prophylaxis of disorders treatable and/or preventable with anti-convulsive agents, epilepsy, post-traumatic epilepsy, migraine, neuralgia, trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, comprising administering to the sufferer in need thereof an effective or prophylactic amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.