RU98105169A - DERIVATIVES 8-AZABICYCLO [3.2.1] OCT-2-ENA, THEIR RECEIVING AND APPLICATION - Google Patents

DERIVATIVES 8-AZABICYCLO [3.2.1] OCT-2-ENA, THEIR RECEIVING AND APPLICATION

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Publication number
RU98105169A
RU98105169A RU98105169/04A RU98105169A RU98105169A RU 98105169 A RU98105169 A RU 98105169A RU 98105169/04 A RU98105169/04 A RU 98105169/04A RU 98105169 A RU98105169 A RU 98105169A RU 98105169 A RU98105169 A RU 98105169A
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RU
Russia
Prior art keywords
disorder
disease
azabicyclo
oct
disorders
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Application number
RU98105169/04A
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Russian (ru)
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RU2157372C2 (en
Inventor
Петер Мольдт
Йорген Шеел-Крюгер
Гуннар М. Ольсен
Эльсебет Эстергорд Нильсен
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Нюросерч А/С
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Publication of RU98105169A publication Critical patent/RU98105169A/en
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Claims (11)

1. Соединение, имеющее формулу
Figure 00000001

или любой из его энантиомеров либо любая их смесь, или его фармацевтически приемлемая соль,
где R представляет собой водород, алкил, алкенил, алкинил, циклоалкил, циклоалкилалкил или 2-гидроксиэтил;
R4 представляет собой фенил, который может быть замещен одним или более чем одним заместителем, выбранным из группы, состоящей из галогена, CF3, CN, алкоксила, циклоалкоксила, алкила, циклоалкила, алкенила, алкинила, аминогруппы, нитрогруппы, гетероарила и арила; 3,4-метилендиоксифенил; бензил, который может быть замещен одним или более чем одним заместителем, выбранным из группы, состоящей из галогена, CF3, CN, алкоксила, циклоалкоксила, алкила, циклоалкила, алкенила, алкинила, аминогруппы, нитрогруппы, гетероарила и арила; гетероарил, который может быть замещен одним или более чем одним заместителем, выбранным из группы, состоящей из галогена, СF3, CN, алкоксила, циклоалкоксила, алкила, циклоалкила, алкенила, алкинила, аминогруппы, нитрогруппы, гетероарила и арила; или нафтил, который может быть замещен одним или более чем одним заместителем, выбранным из группы, состоящей из галогена, CF3, CN, алкоксила, циклоалкоксила, алкила, циклоалкила, алкенила, алкинила, аминогруппы, нитрогруппы, гетероарила и арила.1. The compound having the formula
Figure 00000001

or any of its enantiomers, or any mixture thereof, or a pharmaceutically acceptable salt thereof,
where R represents hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl;
R 4 is phenyl, which may be substituted by one or more substituents selected from the group consisting of halogen, CF 3 , CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; 3,4-methylenedioxyphenyl; benzyl, which may be substituted by one or more substituents selected from the group consisting of halogen, CF 3 , CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; heteroaryl, which may be substituted by one or more substituents selected from the group consisting of halogen, CF 3 , CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl; or naphthyl, which may be substituted by one or more substituents selected from the group consisting of halogen, CF 3 , CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl. 2. Соединение по п. 1, которое представляет собой
(+)-3-(3,4-дихлорфенил)-8-метил-8-азабицикло[3.2.1]окт-2-ен,
(+)-3-(4-хлорфенил)-8-метил-8-азабицикло[3.2.1]окт-2-ен или
(+)-3-(3,4-дихлорфенил)-8-азабицикло[3.2.1]окт-2-ен
либо их фармацевтически приемлемая соль присоединения.2. The compound according to claim 1, which is
(+) - 3- (3,4-dichlorophenyl) -8-methyl-8-azabicyclo [3.2.1] oct-2-ene,
(+) - 3- (4-chlorophenyl) -8-methyl-8-azabicyclo [3.2.1] oct-2-ene or
(+) - 3- (3,4-dichlorophenyl) -8-azabicyclo [3.2.1] oct-2-ene
or a pharmaceutically acceptable addition salt thereof. 3. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по п.1 вместе с по меньшей мере одним фармацевтически приемлемым носителем или разбавителем. 3. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1, together with at least one pharmaceutically acceptable carrier or diluent. 4. Способ изготовления лекарственного средства для лечения расстройства или заболевания живого организма, включая человека, причем это расстройство или заболевание является чувствительным к ингибированию обратного захвата моноаминного нейромедиатора в центральной нервной системе, отличающийся тем, что для изготовления используют соединение по п.1. 4. A method of manufacturing a drug for treating a disorder or disease of a living organism, including a human, this disorder or disease is sensitive to inhibiting the reuptake of a monoamine neurotransmitter in the central nervous system, characterized in that the compound according to claim 1 is used for manufacturing. 5. Способ изготовления лекарственного средства для лечения расстройства или заболевания живого организма, включая человека, причем это расстройство или заболевание является чувствительным к ингибированию обратного захвата серотонина в центральной нервной системе, отличающийся тем, что для изготовления используют соединение по п.1. 5. A method of manufacturing a drug for treating a disorder or disease of a living organism, including a human, and this disorder or disease is sensitive to inhibition of serotonin reuptake in the central nervous system, characterized in that the compound according to claim 1 is used for manufacturing. 6. Способ изготовления лекарственного средства для лечения депрессии и родственных расстройств, таких как псевдодеменции или синдром Ганзера, обсессивно-компульсивные расстройства, состояния паники, нарушения памяти, состояние гиперактивности дефицита внимания, ожирение, состояния тревоги и расстройства при приеме пищи, отличающийся тем, что для изготовления используют соединение по п.1. 6. A method of manufacturing a drug for treating depression and related disorders such as pseudodementia or Ganser syndrome, obsessive-compulsive disorders, panic conditions, memory disorders, attention deficit hyperactivity disorder, obesity, anxiety and eating disorders, characterized in for manufacturing use the compound according to claim 1. 7. Способ по пп. 4-6, отличающийся тем, что используемое соединение представляет собой
(+)-3-(3,4-дихлорфенил)-8-метил-8-азабицикло[3.2.1]окт-2-ен,
(+)-3-(4-хлорфенил)-8-метил-8-азабицикло[3.2.1]окт-2-ен или
(+)-3-(3,4-дихлорфенил)-8-азабицикло[3.2.1]окт-2-ен
либо их фармацевтически приемлемую соль присоединения.7. The method according to paragraphs. 4-6, characterized in that the compound used is
(+) - 3- (3,4-dichlorophenyl) -8-methyl-8-azabicyclo [3.2.1] oct-2-ene,
(+) - 3- (4-chlorophenyl) -8-methyl-8-azabicyclo [3.2.1] oct-2-ene or
(+) - 3- (3,4-dichlorophenyl) -8-azabicyclo [3.2.1] oct-2-ene
or their pharmaceutically acceptable salt accession. 8. Способ лечения расстройства или заболевания живого организма, включая человека, причем это расстройство или заболевание является чувствительным к ингибированию обратного захвата моноаминного нейромедиатора, при котором нуждающемуся в таком лечении живому организму, включая человека, вводят терапевтически эффективное количество соединения по п.1. 8. A method of treating a disorder or disease of a living organism, including a human, and this disorder or disease is sensitive to inhibition of the reuptake of a monoamine neurotransmitter, in which a therapeutic effective amount of a compound according to claim 1 is administered to a living organism in need of such treatment. 9. Способ лечения расстройства или заболевания живого организма, включая человека, причем это расстройство или заболевание является чувствительным к ингибированию обратного захвата серотонина, при котором нуждающемуся в таком лечении живому организму, включая человека, вводят терапевтически эффективное количество соединения по п.1. 9. A method of treating a disorder or disease of a living organism, including a human, and this disorder or disease is sensitive to inhibition of serotonin reuptake, in which a living therapeutically effective amount, including a human, is administered a therapeutically effective amount of a compound according to claim 1. 10. Способ по пп. 8 и 9, отличающийся тем, что лечат депрессию и родственные расстройства, такие как псевдодеменции или синдром Ганзера, обсессивно-компульсивные расстройства, состояния паники, нарушения памяти, состояние гиперактивности дефицита внимания, ожирение, состояния тревоги и расстройства при приеме пищи. 10. The method according to paragraphs. 8 and 9, characterized in that they treat depression and related disorders such as pseudodementia or Ganser syndrome, obsessive-compulsive disorders, panic conditions, memory disorders, attention deficit hyperactivity disorder, obesity, anxiety disorders and eating disorders. 11. Способ получения соединений по п.1, при котором дегидратируют соединение, имеющее формулу
Figure 00000002

где R и R4 такие, как определено в п.1, после чего возможно образуют его фармацевтически приемлемую соль присоединения.11. The method of producing compounds according to claim 1, wherein the compound having the formula
Figure 00000002

where R and R 4 are as defined in claim 1, after which it is possible to form its pharmaceutically acceptable addition salt.
RU98105169/04A 1995-10-13 1996-10-11 Derivatives of 8-azabicyclo[3,2,1]oct-2-ene, method of their synthesis, pharmaceutical composition, method of drug preparing, methods of inhibition of reuptake of monoamine neuromediating agent, especially, serotonin RU2157372C2 (en)

Applications Claiming Priority (2)

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DK1156/95 1995-10-13
DK115695 1995-10-13

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US (1) US6100275A (en)
EP (1) EP0859777B1 (en)
JP (1) JP3462505B2 (en)
KR (1) KR100274829B1 (en)
CN (1) CN1083840C (en)
AT (1) ATE362931T1 (en)
AU (1) AU709327B2 (en)
BR (1) BR9610960A (en)
CA (1) CA2233541C (en)
CZ (1) CZ285093B6 (en)
DE (1) DE69637097T2 (en)
DK (1) DK0859777T3 (en)
EE (1) EE03446B1 (en)
HU (1) HUP9802433A3 (en)
IL (1) IL123583A (en)
IS (1) IS4681A (en)
NO (1) NO980919L (en)
NZ (1) NZ320216A (en)
PL (1) PL185357B1 (en)
RU (1) RU2157372C2 (en)
SK (1) SK283425B6 (en)
TR (1) TR199800628T2 (en)
UA (1) UA63894C2 (en)
WO (1) WO1997013770A1 (en)

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