Novel indole derivatives

A process for the preparation of a compound of formula I comprising deprotecting a compound of formula

• 14
• wherein R1 to R4 and n are defined in the specification and PG represents a protecting group.

A method of treatment of a disease modulated by 5-HT2 receptors comprising administration of a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt, solvate or ester thereof to a patient in need of such treatment.

A pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt, solvate or ester thereof and a therapeutically inert carrier.

A method of treatment and of eating disorders and obesity comprising administration of a therapeutically effective amount of a compound of formula I to a patient in need of such treatment.

A method of treatment and prophylaxis of diabetes mellitus, Type I diabetes, Type II diabetes, diabetes secondary to pancreatic disease, diabetes related to steroid use, Type III diabetes, diabetes insipidus, hyperglycaemia, diabetic complications and insulin resistance comprising administration of a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment and prophylaxis of type II diabetes comprising administration of a therapeutically effective amount of a compound of formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment and prophylaxis of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders and sleep apnoea comprising administration of a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment of disorders of the central nervous system selected from the group consisting of depression, atypical depression, bipolar disorders, anxiety disorders, obsessive-compulsive disorders, social phobias or panic states, sleep disorders, sexual dysfunction, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or other pain, raised intracranial pressure, epilepsy, personality disorders, age-related behavioural disorders, behavioural disorders associated with dementia, organic mental disorders, mental disorders in childhood, aggressivity, age-related memory disorders, chronic fatigue syndrome, drug and alcohol addiction, bulimia, anorexia nervosa, premenstrual tension, trauma, stroke, neurode generative diseases, encephalitis and meningitis comprising administration of a therapeutically effective amount of a compound of formula I or a salt, solvate or ester therof to a patient in need of such treatment.

A method of treatment of obesity comprising administering a therapeutically effective amount of (S)-2-(6-ethoxy-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl)-1-methyl-ethylamine or a salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment of type II diabetes comprising administering a therapeutically effective amount of (S)-2-(6-ethoxy-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl)-1-methyl-ethylamine or a salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment of type II diabetes comprising administering a therapeutically effective amount of (S)-2-[6-(3-methoxy-propoxy)-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl]-1-methyl-ethylamine or a salt, solvate or ester thereof to a patient in need of such treatment.

A method of treatment of obesity comprising administering a therapeutically effective amount of (S)-2-[6-(3-methoxy-propoxy)-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl]-1-methyl-ethylamine or a salt, solvate or ester thereof to a patient in need of such treatment.

A pharmaceutical composition comprising a therapeutically effective amount of (S)-2-[6-(3-methoxy-propoxy)-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl]-1-methyl-ethylamine or a salt, solvate or ester thereof and a therapeutically inert carrier.

A pharmaceutical composition comprising a therapeutically effective amount of (S)-2-(6-ethoxy-2,3-dihydro-1H-3a-aza-cyclopenta[a]inden-8-yl)-1-methyl-ethylamine or a salt, solvate or ester thereof and a therapeutically inert carrier.