RU2007147371A - 2,8-DIMETHYL-5- [2- (4-R-Phenyl) -ethyl] -1,2,3,4-TETRAHYDRO-1NPIRIDO [4,3-b] INDOLES-MEDICINE SUBSTANCE, PHARMACEUTICAL COMPOSITION, METHODS FOR THEIR PRODUCTION AND APPLICATION FOR THE TREATMENT OF PSYCHOTIC DISEASES - Google Patents

Abstract

1. Medicinal substances with neurotropic activity against α-adrenoceptors, dopamine D and central nervous system serotonin receptors, of the general formula 1 in the form of free bases or in the form of pharmaceutically acceptable salts intended for the treatment and prevention of psychotic diseases,! ! where R represents a hydrogen atom or lower alkyl. ! 2. The medicinal substances according to claim 1, which are 2,8-dimethyl-5-phenethyl-1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.1, its hydrochloride 1.2, 2, 8-dimethyl-5- [2- (4-methylphenyl) ethyl] -1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.3 or its hydrochloride 1.4. ! ! 3. Medicinal substances according to claim 1 or 2, the spectrum of receptor-specific agonistic and / or antagonistic activity of which includes activity against α1A, α1B, α1D, α2A adrenoceptors, dopamine D1, D2L, D2S, D3, D4.2, D4 .4 and D7 receptors and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 receptors. ! 4. The drug substances according to claim 3, the spectrum of receptor-specific agonistic and / or antagonistic activity of which includes at least one receptor from a series of histamine H1, H2 and H3, muscarinic M1, M2 and M3 and imidazoline receptors, as well as sodium and calcium channels and monoamine transporters from the range of norepinephrine transporter NET and dopamine transporter DT. ! 5. A pharmaceutical composition with a wide range of receptor-specific activity for the treatment and / or prevention of psychotic diseases in humans and warm-blooded animals, comprising a pharmaceutically effective amount of a substance of formula 1 or a pharmaceutically acceptable salt thereof. ! 6. The pharmaceutical composition according to claim 5, containing pharmaceutically effective

Claims (11)

1. Medicinal substances with neurotropic activity against α-adrenoceptors, dopamine D and serotonin receptors of the central nervous system, General formula 1 in the form of free bases or in the form of pharmaceutically acceptable salts intended for the treatment and prevention of psychotic diseases,

where R represents a hydrogen atom or lower alkyl. 2. The medicinal substances according to claim 1, which are 2,8-dimethyl-5-phenethyl-1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.1, its hydrochloride 1.2, 2, 8-dimethyl-5- [2- (4-methylphenyl) ethyl] -1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.3 or its hydrochloride 1.4.

3. Drug substances according to claim 1 or 2, the spectrum of receptor-specific agonistic and / or antagonistic activity of which includes activity against α _1A , α _1B , α _1D , α _2A adrenoceptors, dopamine D ₁ , D _2L , D _2S , D ₃ , D _4.2 , D _4.4 and D ₇ receptors and serotonin 5-HT _1A , 5-HT _1B , 5-HT _2A , 5-HT _2B , 5-HT _2C , 5-HT ₆ and 5-HT ₇ receptors. 4. The drug substances according to claim 3, the spectrum of receptor-specific agonistic and / or antagonistic activity of which includes at least one receptor from a number of histamine H ₁ , H ₂ and H ₃ , muscarinic M ₁ , M ₂ and M ₃ and imidazoline receptors as well as sodium and calcium channels and monoamine transporters from the range of norepinephrine transporter NET and dopamine transporter DT. 5. A pharmaceutical composition with a wide range of receptor-specific activity for the treatment and / or prevention of psychotic diseases in humans and warm-blooded animals, comprising a pharmaceutically effective amount of a substance of formula 1 or a pharmaceutically acceptable salt thereof. 6. The pharmaceutical composition according to claim 5, containing a pharmaceutically effective amount of a drug substance of General formula 1.1, or 1.2, or 1.3, or 1.4 according to any one of claims 2 to 4. 7. A method for producing a pharmaceutical composition according to claim 5 or 6 by mixing with an inert excipient and / or solvent of at least one drug substance of formula 1 or a pharmaceutically acceptable salt thereof. 8. A medicinal product comprising a medicinal substance according to any one of claims 1 to 4 or a pharmaceutical composition according to any one of claims 5 or 6, intended for the treatment and / or prevention of psychotic diseases. 9. The drug of claim 8, intended for the prevention and / or treatment of schizophrenia, schizophrenia-like diseases; schizotypal disorders; schizoaffective disorders, including bipolar and depressive types; delusional disorders, including delusions of attitude, persecution, greatness, jealousy, erotomania, as well as hypochondriacal, somatic, mixed and undifferentiated delirium; short-term psychotic disorders; induced psychotic disorders; induced by substances of psychotic disorders, as well as other psychotic disorders. 10. The drug of claim 8, intended for the treatment and / or prevention of simple, hebephrenic, paranoid, hypertoxic (febrile), catatonic, schizoaffective, residual or undifferentiated schizophrenia, and / or forms of schizophrenia, or any other known forms of schizophrenia. 11. A method of treating and / or preventing psychotic diseases by administering to a human or warm-blooded animal a drug substance according to any one of claims 1-4 or a pharmaceutical composition according to claim 5 or 6, or a drug according to any one of claims 8-10.