Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase

A pharmaceutical composition comprising, as active ingredient, at least one compound of formula (I):

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• wherein
• either Y is (CH2) and X is chosen from the following group:
• O, NH, N-(C1-C4)alkyl, N-benzyl, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 and CHPh;
• or Y is (C═O) and X is chosen from the following group:
• NH, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl and N-5-pyrimidyl;
• wherein the (C1-C4)alkyl contains 1 to 4 carbon atoms in a straight or branched chain;
• or
• a racemic mixture, an enantiomer, a diastereoisomer or a mixture thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof, optionally in combination with a pharmaceutically acceptable carrier.

A process for preparing a compound of formula (I), including a racemic mixture, an enantiomer, a diastereoisomer or a mixture of said enantiomer or said diastereomer, or a tautomer thereof:

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• comprising the step of cyclizing a compound of formula (II) under suitable reaction conditions such that said compound of formula (II) cyclizes to form said compound of formula (I);
• and
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• wherein
• either Y is (CH2) and X is chosen from the following group:
• O, NH, N-(C1-C4)alkyl, N-benzyl, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 and CHPh;
• or Y is (C═O) and X is chosen from the following group:
• NH, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl and N-5-pyrimidyl;
• wherein the (C1-C4)alkyl contains 1 to 4 carbon atoms in a straight or branched chain;
• and
• optionally converting said product into a pharmaceutically acceptable salt.

A method of treating an illness, which involves an abnormal production of nitric oxide (NO) by induction of an inducible NO-synthase (NOS-2), comprising administering to a patient in need of such a treatment a therapeutically effective amount of a compound of formula (I):

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• wherein
• either Y is (CH2) and X is chosen from the following group:
• O, NH, N-(C1-C4)alkyl, N-benzyl, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 and CHPh;
• or Y is (C═O) and X is chosen from the following group:
• NH, N-phenyl, N-(2-pyridyl), N-(3-pyridyl), N-(4-pyridyl), N-2-pyrimidyl and N-5-pyrimidyl;
• wherein the (C1-C4)alkyl contains 1 to 4 carbon atoms in a straight or branched chain;
• or
• a racemic mixture, an enantiomer, a diastereoisomer or a mixture thereof, or a tautomer thereof, or a pharmaceutically acceptable salt thereof, optionally in combination with a pharmaceutically acceptable carrier.