Compound for treatment of erectile dysfunction

The compound for use according to any one of claims 1 and 2, wherein the compound has the structure of formula (Ia);

• or a pharmaceutically acceptable salt thereof.

The compound for use according to any one of the preceding claims, wherein the compound is exo-7-[(8-azabicyclo[3.2.1]octan-3-yl)oxy]-3-methoxy-chromen-2-one or a pharmaceutically acceptable salt thereof.

The compound for use according to any one of the preceding claims wherein the compound is exo-7-[(8-azabicyclo[3.2.1]octan-3-yl)oxy]-3-methoxy-chromen-2-one hydrochloride.

The compound for use according to any one of the preceding claims, wherein the compound of formula I is administered in an amount per individual dose from about 0.5 mg to about 10 mg.

The compound for use according to any one of the preceding claims, wherein the compound of formula I is administered in an amount per individual dose from about 0.1 mg to 20 mg per individual dose, such as about 0.1 mg, such as about 0.2 mg, 0.3 mg, 0.4 mg, 0.5 mg, 0.6 mg, 0.7 mg, 0.8 mg, 0.9 mg, 1 mg, 1.5 mg, 2 mg, 2.5 mg, 3 mg, 3.5 mg, 4 mg, 4.5 mg, 5 mg, 6 mg, 7 mg, 8 mg, 9 mg, or 10 mg per individual dose.

The compound for use according to any one of the preceding claims, wherein the compound of formula I is administered to the subject at about 5 mg per individual dose.

The compound for use according to any one of the preceding claims, wherein the compound of formula I is administered to the subject at 5 mg per individual dose.

The compound for use according to any one of the preceding claims wherein the compound is administered once daily.

The compound for use according to any one of the preceding claims, wherein said compound is administered more than once a day, such as 2 times a day, such as 3 times a day, such as 4 times a day.

The compound for use according to any one of the preceding claims wherein the compound is administered once a week or twice a week.

The compound for use according to any one of the preceding claims wherein the total daily dose of said compound is from about 1 and 10 mg.

The compound for use according to any one of the preceding claims, wherein said compound is administered orally in an amount per individual dose from about 0.035 mg/kg to 0.135 mg/kg, such as from 0.040 mg/kg to 0.110 mg/kg, such as from 0.042 mg/kg to 0.100 mg/kg, such as from 0.0450 mg/kg to 0.100 mg/kg, such as from 0.045 mg/kg to 0.091 mg/kg, such as from 0.050 mg/kg to 0.091 mg/kg.

The compound for use according to any one of the preceding claims, wherein said compound is administered orally in an amount per individual dose from about from 0.075 mg/kg to 0.250 mg/kg, such as from 0.080 mg/kg to 0.222 mg/kg, such as from 0.083 mg/kg to 0.200 mg/kg, such as from 0.091 mg/kg to 0.185 mg/kg, such as from 0.100 mg/kg to 0.185 mg/kg, such as from 0.050 mg/kg to 0.185 mg/kg.

The compound for use according to any one of the preceding claims, wherein said compound is administered to the subject at 5 mg per individual dose, wherein the subject was a weight from about 60 kg to about 115 kg.

The compound for use according to any one of the preceding claims, wherein the erectile dysfunction is organic erectile dysfunction.

The compound for use according to any one of the preceding claims, wherein the erectile dysfunction is lifelong erectile dysfunction or acquired erectile dysfunction.

The compound for use according to any one of the preceding claims, wherein the erectile dysfunction is generalised erectile dysfunction or situational erectile dysfunction.

The compound for use according to any one of the preceding claims, wherein the subject is administered with a further therapeutic agent effective for the treatment of erectile dysfunction.

The compound for use according to any one of the preceding claims, wherein the subject is under another treatment for erectile dysfunction.

The compound for use according to any one of the preceding claims, wherein the subject is a non-responder of treatment for erectile dysfunction with one or more PDE5 inhibitors.

The compound for use according to any one of the preceding claims, wherein the compound is able to produce a central effect initiating erection and/or a peripheral effect potentiating erection.

The compound for use according to any one of the preceding claims, wherein the compound is able to initiate and/or potentiate erection through smooth muscle relaxation.

The compound for use according to any one of the preceding claims, wherein the compound is able to initiate erection by increasing central dopamine and/or a peripheral effect potentiating erection through nitric oxide release.

The compound for use according to any one of the preceding claims, wherein the compound is able to increase the number of erectile events, the duration of erectile events, penile tumescence and/or the penile rigidity.

The compound for use according to any one of the preceding claims, wherein the compound is able to increase the number of erectile events, the duration of erectile events, penile tumescence and/or the penile rigidity in the subject during sexual stimulation.

The compound according to any one of the preceding claims, wherein the subject is a mammal.

The compound according to any one of the preceding claims, wherein the mammal is a human.

The compound according to any one of the preceding claims, wherein the human is male.

The compound for use according to any one of the preceding claims, wherein the subject is male.

The compound for use according to any one of the preceding claims, wherein the subject is an adult male.

The compound for use according to any one of the preceding claims, wherein the subject is a male over the age of 20.

The compound for use according to any one of the preceding claims, wherein the subject has a weight from about 55 kg to about 130 kg, such as 60 kg to about 115 kg.

The compound for use according to any one of the preceding claims, wherein the subject has a body-mass index (BMI) from about 19.5 kg/m2 to about 35.5 kg/m2.

The compound for use according to any one of the preceding claims, wherein the subject prior to treatment had an international index of Erectile Function 5 (IIEF-5) of less than 17, such as between 12 and 16, such as between 8 and 11, such as between 5 and 7.

The compound for use according to any one of the preceding claims, wherein the subject prior to treatment had an international index of Erectile Function 5 (IIEF-5) of less than 12.

The compound for use according to any one of the preceding claims, wherein the compound is able to increase the International Index of Erectile Function in the subject.

The compound for use according to any one of the preceding claims, wherein the administration of the compound is an oral administration.

The compound for use according to any one of the preceding claims, wherein the administration of the compound is parenteral administration, such as cutaneous, mucosal, subcutaneous, intramuscular, intraperitoneal, intravenous or intra-arterial injection.

The compound for use according to any one of the preceding claims, wherein the compound is formulated in a pharmaceutical composition further comprising a pharmaceutically acceptable diluent, carrier and/or excipient.

The compound for use according to any one of the preceding claims, wherein the compound is formulated as a solid dosage form, such as a tablet, a capsule, a pill, granules or a powder.

A solid dosage form comprising a compound of formula I,

• or a pharmaceutically acceptable salt thereof, wherein the compound is present in an amount from about 0.5 mg to about 10 mg.

A composition comprising a compound of formula (I),

• and one or more PDE5 inhibitor(s).

Use of a compound of formula (I),

• for the manufacture of a medicament for the treatment, prevention, reduction or alleviation of erectile dysfunction in a subject in need thereof, wherein said compound is administered in a dose from about 0.001 to about 1 mg/kg mg.

A method of treatment, prevention, reduction or alleviation of erectile dysfunction in a subject in need thereof, the method comprising administering to the subject in need an amount from about 0.001 to about 1 mg/kg of a compound of formula (I),

• or a pharmaceutically acceptable salt thereof.

A method of increasing frequency of erectile responses in a subject, said method comprising administering to the subject an amount from about 0.001 mg/kg to about 1 mg/kg of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

A method of increasing duration of erectile responses in a subject, said method comprising administering to the subject an amount from about 0.001 mg/kg to about 1 mg/kg of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

A method of increasing the magnitude of erectile responses in a subject said method comprising administering to the subject an amount from about 0.001 mg/kg to about 1 mg/kg of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

A method of achieving a mean plasma concentration of a compound of formula (I) from about 1 ng/ml to 50 ng/mL in a subject said method comprising administering to the subject an amount from about 0.001 mg/kg to about 1 mg/kg of the compound of formula (I) or a pharmaceutically acceptable salt thereof.