Use of cysteine derivatives for the preparation of a...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/4985 (2006.01)

Patent

CA 2336846

The invention relates to the use of cysteine derivatives for preparing a medicament intended to treat diseases which result from the formation of the heterotrimeric G protein. These diseases include in particular diseases linked to the following biological functions or disorders: smell, taste, perception of the light, neurotransmission, neurodegeneration, endocrine and exocrine gland functions, autocrine and paracrine regulation, arterial tension, embryogenesis, benign cell proliferation, oncogenesis, viral infection, immunological functions, diabetes, obesity, and benign and malign proliferative diseases. Said cysteine derivatives include in particular: - bis-1,1'-[7-(2-amino-1-oxo-3-thiopropyl)-8-(cyclohexylmethyl)-2-(2- methoxyphenyl)- 5,6,7,8-tetrahydroimidazo[1.2a]pyrazine disulphide (I), and - bis-1,1'-7-(2-amino-1-oxo-3-thiopropyl-(2-(1-naphtyl)-8-(2-methylpropyl)- 5,6,7,8- tetrahydroimidazo[1.2a]pyrazin-7-yl) disulphide (II).

L'invention concerne l'utilisation de dérivés de la cystéine pour préparer un médicament destiné à traiter des maladies qui résultent de la formation de la protéine G hétérotrimérique. Ces maladies comprennent en particulier des maladies liées aux fonctions biologiques ou désordres suivants: odorat, goût, perception de la lumière, neurotransmission, neurodégénérescence, fonctionnement des glandes endocrines et exocrines, régulation autocrine et paracrine, tension artérielle, embryogénèse, prolifération cellulaire bénigne, oncogénèse, infection virale, fonctions immunologiques, diabète, obésité, et maladies prolifératives bénignes et malignes. Lesdits dérivés de la cystéine comprennent en particulier: le disulfure de bis-1,1'-[7-(2-amino-1-oxo-3-thiopropyl)-8-(cyclohexylméthyl)-2-(2-méthoxyphényl)-5,6,7,8-tétrahydroimidazo[1,2a]pyrazine (I); et le disulfure de bis-1,1'-[7- (2-amino- 1-oxo-3-thiopropyl- (2-(1-naphtyl)-8- (2-méthylpropyl)- 5,6,7,8- tétrahydroimidazo [1,2a]pyrazin-7-yle) (II).

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