RU2007147347A

RU2007147347A - 2,8-DIMETHYL-5- [2 (4-R-Phenyl) -ethyl] 1,2,3,4-tetrahydro-1H-pyrido [4,3-b] INDOLES-MEDICINAL SUBSTANCE, PHARMACEUTICAL COMPOSITION, METHODS FOR THEIR PRODUCTION AND APPLICATIONS FOR TREATMENT OF DISORDERS CAUSED BY CHEMICALS AND DEPENDENCIES ON CHEMICALS

Info

Publication number: RU2007147347A
Application number: RU2007147347/04A
Authority: RU
Inventors: Александр Васильевич Иващенко (US); Александр Васильевич Иващенко; Сергей Евгеньевич Ткаченко (RU); Сергей Евгеньевич Ткаченко; Илья Матусович Окунь (US); Илья Матусович Окунь; Ян Вадимович Лавровский (US); Ян Вадимович Лавровский; Андрей Александрович Иващенко (RU); Андрей Александрович Иващенко; Николай Филиппович Савчук (RU); Николай Филиппович Савчук
Original assignee: Андрей Александрович Иващенко (RU); Андрей Александрович Иващенко; Алла Хем, Ллс (Us); Алла Хем, Ллс
Priority date: 2007-12-21
Filing date: 2007-12-21
Publication date: 2009-06-27

Abstract

1. Лекарственные субстанции, обладающие нейротропной активностью по отношению к α-адреноцепторам, допаминовым D и серотониновым 5-НТ рецепторам, общей формулы 1 в виде свободных оснований или в виде фармацевтически приемлемых солей, предназначенные для лечения и предупреждения расстройств, вызванных химическими веществами и зависимостями от химических веществ. ! ! где R представляет собой атом водорода или низший алкил. ! 2. Лекарственные субстанции по п.1, представляющие собой 2,8-диметил-5-фенетил-1,2,3,4-тетрагидро-1Н-пиридо[4,3-b]индол 1.1 или его гидрохлорид 1.2, 2,8-диметил-5-[2-(4-метилфенил)-этил]-1,2,3,4-тетрагидро-1Н-пиридо[4,3-b] индол 1.3 или его гидрохлорид 1.4. ! ! 3. Лекарственные субстанции по п.1, спектр рецептор-специфичной агонистической и/или антагонистической активности которых включает активность по отношению к α1A, α1B, α1D, α2А адреноцепторам, допаминовым D1, D2L, D2S, D3, D4.2 рецепторам и серотониновым 5-НТ2А, 5-HT2B, 5-HT2C, 5-НТ6 и 5-НТ7 рецепторам. ! 4. Лекарственные субстанции по п.1, спектр рецептор-специфичной агонистической и/или антагонистической активности которых может включать, по крайней мере, один рецептор из ряда гистаминовых и имидазолиновых рецепторов, а также натриевых и кальциевых каналов и моноаминовых транспортеров. ! 5. Фармацевтическая композиция с широким спектром рецептор-специфичной активности для лечения и/или предупреждения расстройств, вызванных химическими веществами и зависимостями от химических веществ, содержащая фармацевтически эффективное количество субстанции общей формулы 1 или ее фармацевтически приемлемой соли. ! 6. Фармацевтическая композиция по п.5, содержащая фармацевтически эффективное количеств1. Medicinal substances with neurotropic activity against α-adrenoceptors, dopamine D and serotonin 5-HT 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 disorders caused by chemicals and addictions from chemicals. ! ! where R represents a hydrogen atom or lower alkyl. ! 2. The drug substance according to claim 1, which is 2,8-dimethyl-5-phenethyl-1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.1 or 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. The drug substances according to claim 1, 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 receptors and serotonin 5 -HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 receptors. ! 4. The drug substances according to claim 1, the spectrum of receptor-specific agonistic and / or antagonistic activity of which may include at least one receptor from a number of histamine and imidazoline receptors, as well as sodium and calcium channels and monoamine transporters. ! 5. A pharmaceutical composition with a wide range of receptor-specific activity for the treatment and / or prevention of disorders caused by chemicals and chemical addiction, containing a pharmaceutically effective amount of a substance of General formula 1 or its pharmaceutically acceptable salt. ! 6. The pharmaceutical composition according to claim 5, containing pharmaceutically effective amounts

Claims

1. Medicinal substances with neurotropic activity against α-adrenoceptors, dopamine D and serotonin 5-HT 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 disorders caused by chemicals and addictions from chemicals.

where R represents a hydrogen atom or lower alkyl.

2. The drug substance according to claim 1, which is 2,8-dimethyl-5-phenethyl-1,2,3,4-tetrahydro-1H-pyrido [4,3-b] indole 1.1 or 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. The drug substances according to claim 1, 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 receptors and serotonin 5-HT _2A , 5-HT _2B , 5-HT _2C , 5-HT ₆ and 5-HT ₇ receptors.

4. The drug substances according to claim 1, the spectrum of receptor-specific agonistic and / or antagonistic activity of which may include at least one receptor from a number of histamine and imidazoline receptors, as well as sodium and calcium channels and monoamine transporters.

5. A pharmaceutical composition with a wide range of receptor-specific activity for the treatment and / or prevention of disorders caused by chemicals and chemical addiction, containing a pharmaceutically effective amount of a substance of General formula 1 or its pharmaceutically acceptable salt.

6. The pharmaceutical composition according to claim 5, containing a pharmaceutically effective amount of a drug substance 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 general formula 1 or a pharmaceutically acceptable salt thereof.

8. A drug in the form of tablets, capsules or injections, placed in a pharmaceutically acceptable package, comprising a drug substance according to any one of claims 1 to 4 or a new pharmaceutical composition according to any one of claims 5 and 6, intended for treatment and / or preventing disorders caused by chemicals and chemical addictions.

9. The drug of claim 8, intended for the prevention and / or treatment of disorders associated with the use of drugs, alcohol, drugs (addiction, substance dependence), pathological cravings (substance craving) and abuse (substance abuse); substance intoxication, withdrawal or withdrawal syndrome, delirium (substance-induced delirium), dementia (substance-induced persisting dementia), amnestic disorder (substance-induced persisting amnesic disorder), psychotic disorder (substance-induced psychotic disorder), substance-induced mood disorder, substance-induced anxiety disorder, substance-induced sexual dysfunction, substance-induced sleep disorder and substance-induced persisting perception disorder, flashbacks).

10. 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 to 4, or a pharmaceutical composition according to claim 5 or 6, or a drug according to claim 8 or 9.