Pyrimidoindole derivatives and processes for preparation...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2025820

ABSTRACT Compound of the formula: Image wherein R1, R2 and R3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl, R4 is imidazolyl which may have suitable sub- stituent(s) or pyridyl, A is lower alkylene, and ---- is single bond or double bond, and pharma- ceutically acceptable salts thereof. The preparation of these compounds, pharmaceutical compositions containing them and their use as a medicament are also disclosed. These compounds are useful for treating or preventing 5-hydroxytryptamine mediated diseases, for example, central nervous system (CNS) disorders such as psychosis (e.g. schizophrenia, mania, etc.), anxiety, and depression; pains or aches such as headaches (e.g. migraine, cluster headaches, vascular headaches, etc.) and neuralgia (e.g. trigeminal neuralgia, etc.); gastro- intestinal disorders such as symptoms of gastro- intestinal dysfunction such as occur with, for example, dyspepsia, peptic ulcer, reflux oesophagitis and flatulence, and irritable bowel syndrome (IBS); nausea or vomiting, each of which may be associated with cancer therapy; motion sickness; and the like in human being or animals, particularly nausea and vomiting.

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