초록 ▼

The new derivatives of vincamine according to this invention may be represented by the general formula [Figure] (I) in which R1 represents a halogen atom and R2 may represent a hydroxy group whereas R3 may represent a hydrogen atom, or R2 may form with R3 an additional bond. The compounds may be use

The new derivatives of vincamine according to this invention may be represented by the general formula [Figure] (I) in which R1 represents a halogen atom and R2 may represent a hydroxy group whereas R3 may represent a hydrogen atom, or R2 may form with R3 an additional bond. The compounds may be used to treat cardio-circulatory, cerebro-vascular and respiratory insufficiencies.

대표청구항 ▼

A process for preparing a compound of the formula [Figure] (I) in which: R1 represents a chlorine atom in the 10-position R2 and R3 represent together an additional carbon-carbon bond which comprises the steps of: (a) reacting tabersonine with hydrochloric acid in solution in an alcohol for 2-4 days

A process for preparing a compound of the formula [Figure] (I) in which: R1 represents a chlorine atom in the 10-position R2 and R3 represent together an additional carbon-carbon bond which comprises the steps of: (a) reacting tabersonine with hydrochloric acid in solution in an alcohol for 2-4 days at room temperature in the presence of a peracid selected from the group consisting of m-chloroperbenzoic acid, perphthalic acid and p-nitroperbenzoic acid, (b) heating the resulting compound of formula I wherein R2 and R3 represent respectively OH and H in formic acid at 99%. A compound of formula I as defined in claim 1 being 10-chloro dehydro-14,15 apovincamine (or 10-chloro D14,15 apovincamine). A pharmaceutical composition for use in human and veterinary medicine in treating cardio circulatory, cerebrovascular and respiratory insufficiencies, containing an effective amount of about 1 to 200 mg of an active ingredient comprising at least the compound of formula I as defined in claim 1 together with a pharmaceutically acceptable carrier. A method of treating cardiocirculatory, cerebrovascular and respiratory insufficiency comprising daily administration to a patient in need of such treatment of a pharmaceutical composition comprising 3 mg to 600 mg daily dosage of the vincamine derivative as defined in claim 1 in its base or salt form together with a pharmaceutically acceptable excipient.