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RU2003105900A - 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES WITH CB1-ANTAGONISTIC ACTIVITY - Google Patents

4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES WITH CB1-ANTAGONISTIC ACTIVITY

Info

Publication number
RU2003105900A
RU2003105900A RU2003105900/04A RU2003105900A RU2003105900A RU 2003105900 A RU2003105900 A RU 2003105900A RU 2003105900/04 A RU2003105900/04 A RU 2003105900/04A RU 2003105900 A RU2003105900 A RU 2003105900A RU 2003105900 A RU2003105900 A RU 2003105900A
Authority
RU
Russia
Prior art keywords
compound
formula
disease
compounds according
phenyl
Prior art date
Application number
RU2003105900/04A
Other languages
Russian (ru)
Other versions
RU2281941C2 (en
Inventor
Йозефус Х. М. Ланге
Корнелис Г. Крюсе
Якобус ТИПКЕР
Ян ХОГЕНДОРН
Original Assignee
Солвей Фармасьютикалс Б.В.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Солвей Фармасьютикалс Б.В. filed Critical Солвей Фармасьютикалс Б.В.
Publication of RU2003105900A publication Critical patent/RU2003105900A/en
Application granted granted Critical
Publication of RU2281941C2 publication Critical patent/RU2281941C2/en

Links

Claims (8)

1. Энантиомер, имеющий S-конфигурацию в положении 4 своего 4,5-дигидропиразольного кольца, соединения формулы (I)1. An enantiomer having an S configuration at position 4 of its 4,5-dihydropyrazole ring, a compound of formula (I) в которой R и R1, одинаковые или различные, представляют 3-пиридил или 4-пиридил, или фенил, который может быть замещен галогеном или метоксигруппой;in which R and R 1 , the same or different, are 3-pyridyl or 4-pyridyl, or phenyl, which may be substituted with a halogen or methoxy group; R2 и R3, одинаковые или различные, представляют водород, алкил (1-3 С) или диметиламино;R 2 and R 3 , the same or different, represent hydrogen, alkyl (1-3 C) or dimethylamino; R4 представляет фенил, который может быть замещен 1, 2 или 3 заместителями, выбранными из группы, включающей атомы галогена, трифторметил, метоксигруппу и алкил (1-3 С),R 4 represents phenyl which may be substituted by 1, 2 or 3 substituents selected from the group consisting of halogen atoms, trifluoromethyl, methoxy and alkyl (1-3 C), а также его таутомеры, пролекарства и соли.as well as its tautomers, prodrugs and salts. 2. Соединение, имеющее формулу (I) по п.1, в котором R представляет 4-хлорфенилгруппу, R1 представляет фенил, R2 представляет водород, R3 представляет метил, а R4 представляет 4-хлорфенил, а также его соли.2. The compound having formula (I) according to claim 1, in which R represents a 4-chlorophenyl group, R 1 represents phenyl, R 2 represents hydrogen, R 3 represents methyl, and R 4 represents 4-chlorophenyl, as well as its salts. 3. Фармацевтическая композиция, содержащая по меньшей мере одно соединение по п.1 в качестве активного компонента.3. A pharmaceutical composition comprising at least one compound according to claim 1 as an active component. 4. Способ получения фармацевтических композиций, отличающийся тем, что соединение по п.1 имеет форму, одходящую для введения.4. A method of obtaining pharmaceutical compositions, characterized in that the compound according to claim 1 has a form suitable for administration. 5. Способ получения соединений формулы I, отличающийся тем, что рацемическую смесь соединения формулы I, разделяют на левовращающие и правовращающие энантиомеры.5. A method of obtaining compounds of formula I, characterized in that the racemic mixture of a compound of formula I is divided into levorotatory and dextrorotatory enantiomers. 6. Способ лечения психиатрических расстройств, таких как психоз, тревога, депрессия, дефицит внимания, нарушения памяти и аппетита, ожирение, неврологические расстройства, такие как болезнь Паркинсона, слабоумие, дистония, болезнь Альцгеймера, эпилепсия, болезнь Гентингтона, синдром Туретта, ишемия, боль и другие заболевания ЦНС, включая каннабиноидную нейротрансмиссию, отличающийся тем, что используют соединения по п.1.6. A method of treating psychiatric disorders such as psychosis, anxiety, depression, attention deficit, memory and appetite disorders, obesity, neurological disorders such as Parkinson’s disease, dementia, dystonia, Alzheimer's disease, epilepsy, Huntington’s disease, Tourette’s syndrome, ischemia, pain and other diseases of the central nervous system, including cannabinoid neurotransmission, characterized in that the compounds according to claim 1 are used. 7. Способ лечения желудочно-кишечных заболеваний включая каннабиноидную нейротрансмиссию, отличающийся тем, что используют соединения по п.1.7. A method of treating gastrointestinal diseases including cannabinoid neurotransmission, characterized in that the compounds according to claim 1 are used. 8. Способ лечения сердечно-сосудистых заболеваний, включая каннабиноидную нейротрансмиссию, отличающийся тем, что используют соединения по п.1.8. A method of treating cardiovascular diseases, including cannabinoid neurotransmission, characterized in that the compounds according to claim 1 are used.
RU2003105900/04A 2001-03-22 2002-03-18 Derivatives of 4,5-dihydro-1h-pyrazole possessing cb1-antagonistic activity RU2281941C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01201062 2001-03-22
EP01201062.5 2001-03-22

Publications (2)

Publication Number Publication Date
RU2003105900A true RU2003105900A (en) 2004-08-20
RU2281941C2 RU2281941C2 (en) 2006-08-20

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Country Status (25)

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EP (1) EP1373216B1 (en)
JP (1) JP4373675B2 (en)
KR (1) KR100846614B1 (en)
CN (1) CN100366614C (en)
AR (1) AR033046A1 (en)
AT (1) ATE284872T1 (en)
AU (1) AU2002256690B2 (en)
BR (1) BR0205602A (en)
CA (1) CA2422708C (en)
CZ (1) CZ2003698A3 (en)
DE (1) DE60202270T2 (en)
ES (1) ES2229132T3 (en)
HU (1) HUP0303148A3 (en)
IL (1) IL153508A (en)
MX (1) MXPA03003534A (en)
NO (1) NO324953B1 (en)
NZ (1) NZ524633A (en)
PL (1) PL363751A1 (en)
PT (1) PT1373216E (en)
RU (1) RU2281941C2 (en)
SI (1) SI1373216T1 (en)
SK (1) SK287592B6 (en)
UA (1) UA74066C2 (en)
WO (1) WO2002076949A1 (en)
ZA (1) ZA200307322B (en)

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