RU96121561A - APPLICATION OF SEROTONIN ANTAGONISTS (5HT3) FOR TREATMENT OF FIBROMYALGIA - Google Patents

APPLICATION OF SEROTONIN ANTAGONISTS (5HT3) FOR TREATMENT OF FIBROMYALGIA

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Publication number
RU96121561A
RU96121561A RU96121561/14A RU96121561A RU96121561A RU 96121561 A RU96121561 A RU 96121561A RU 96121561/14 A RU96121561/14 A RU 96121561/14A RU 96121561 A RU96121561 A RU 96121561A RU 96121561 A RU96121561 A RU 96121561A
Authority
RU
Russia
Prior art keywords
alkyl
antagonist
fibromyalgia
treatment
cycloalkyl
Prior art date
Application number
RU96121561/14A
Other languages
Russian (ru)
Other versions
RU2165760C2 (en
Inventor
Вольфганг МЮЛЛЕР
Томас Штрац
Original Assignee
Новартис Аг
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
Priority claimed from GB9406857A external-priority patent/GB9406857D0/en
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU96121561A publication Critical patent/RU96121561A/en
Application granted granted Critical
Publication of RU2165760C2 publication Critical patent/RU2165760C2/en

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Claims (7)

1. Применение 5-НТ3 антагониста для лечения фибромиалгии.1. The use of 5-HT 3 antagonist for the treatment of fibromyalgia. 2. Применение по п.1, отличающееся тем, что 5-НТ3 антагонист представлен формулой I
Figure 00000001

в которой R1 представляет собой водород, галоген, гидрокси, алкокси(1-4С), амино, алкил(1-4С)амино или диалкил(1-4С)амино;
R2 представляет собой водород, алкил(1-7С), алкенил(3-6С), алкинил(3-10С), циклоалкил(3-7С), циклоалкил(3-7С)алкил(1-4С), фенил, фенилалкил(1-3С), алкил(1-6С)карбонил, алкил(1-6С)оксикарбонил, карбамил, сульфамил или моно- или диалкил(1-6С)карбамил или сульфамил;
Х представляет собой СН или N;
Y представляет собой NR3 или О, при этом R3 является водородом или алкилом(1-6С), или Х+Y вместе представляют собой С-А-N или С-А-СН, в которых А обозначает СН=СН или -(СН2)m-, при этом m равняется 2 или 3;
n равняется 0, 1 или 2;
Z представляет собой радикал формулы (а)
Figure 00000002

в которой о равняется 0;
p принимает значения 0, 1 или 2;
q принимает значения 0, 1 или 2, или о равняется 1, p равняется 0, и q принимает значения 0 или 1;
R4 представляет собой водород, алкил(1-7С), циклоалкил(3-6С), фенилалкил(1-4С), необязательно моно- или дизамещенный галогеном, алкил(1-4С) или алкокси(1-4С),
или радикал формулы (b)
Figure 00000003

в которой o' принимает значения 1, 2 или 3;
p' принимает значения 0 или 1;
q' является 0 или 1,
или радикалом формулы (с) или (d)
Figure 00000004

в которых один из R5, R6 и R7 представляет собой водород, алкил(1-6С), циклоалкил(3-7С), алкенил(2-6С), фенил или фенилалкил(1-3С), а два других независимо представляют собой водород или алкил(1-6С), при условии, что Z не является (d), когда n равно 0 и Y представляет собой NR3 или (c X) N-A-C,
в свободной форме или в форме фармацевтически приемлемой соли, или в форме комплекса.2. The use according to claim 1, characterized in that the 5-HT 3 antagonist is represented by formula I
Figure 00000001

in which R 1 represents hydrogen, halogen, hydroxy, alkoxy (1-4C), amino, alkyl (1-4C) amino or dialkyl (1-4C) amino;
R 2 represents hydrogen, alkyl (1-7C), alkenyl (3-6C), alkynyl (3-10C), cycloalkyl (3-7C), cycloalkyl (3-7C) alkyl (1-4C), phenyl, phenylalkyl (1-3C), alkyl (1-6C) carbonyl, alkyl (1-6C) hydroxycarbonyl, carbamyl, sulfamyl or mono- or dialkyl (1-6C) carbamyl or sulfamyl;
X represents CH or N;
Y represents NR 3 or O, wherein R 3 is hydrogen or alkyl (1-6C), or X + Y together represent C-A-N or C-A-CH, in which A is CH = CH or - (CH 2 ) m -, wherein m is 2 or 3;
n is 0, 1 or 2;
Z represents a radical of formula (a)
Figure 00000002

in which o equals 0;
p is 0, 1 or 2;
q is 0, 1 or 2, or o is 1, p is 0, and q is 0 or 1;
R 4 represents hydrogen, alkyl (1-7C), cycloalkyl (3-6C), phenylalkyl (1-4C), optionally mono- or disubstituted with halogen, alkyl (1-4C) or alkoxy (1-4C),
or a radical of formula (b)
Figure 00000003

in which o 'takes the values 1, 2 or 3;
p 'is 0 or 1;
q 'is 0 or 1,
or a radical of formula (c) or (d)
Figure 00000004

in which one of R 5 , R 6 and R 7 represents hydrogen, alkyl (1-6C), cycloalkyl (3-7C), alkenyl (2-6C), phenyl or phenylalkyl (1-3C), and the other two independently represent hydrogen or alkyl (1-6C), provided that Z is not (d) when n is 0 and Y is NR 3 or (c X) NAC,
in free form or in the form of a pharmaceutically acceptable salt, or in the form of a complex. 3. Применение по п.1, отличающееся тем, что 5-НТ3 антагонист представляет собой индол-3-ил-карбоновая кислота-эндо-8-метил-8-аза-бицикло[3,2,1] -окт-3-ил-сложный эфир в свободной форме или форме фармацевтически приемлемой соли или комплекса.3. The use according to claim 1, characterized in that the 5-HT 3 antagonist is an indol-3-yl-carboxylic acid-endo-8-methyl-8-aza-bicyclo [3,2,1] -oct-3 -yl ester in free or pharmaceutically acceptable salt or complex form. 4. Применение по п.1, отличающееся тем, что 5-НТ3 антагонист представляет собой 1,2,3,9-тетрагидро-9-метил-[(2-метил-1Н-имидазол-1-ил)-метил]-4Н-карбазол-4-он.4. The use according to claim 1, characterized in that the 5-HT 3 antagonist is 1,2,3,9-tetrahydro-9-methyl - [(2-methyl-1H-imidazol-1-yl) methyl] -4H-carbazol-4-one. 5. Применение 5-НТ3 антагониста для производства фармацевтического состава для лечения фибромиалгии.5. The use of a 5-HT 3 antagonist for the manufacture of a pharmaceutical composition for the treatment of fibromyalgia. 6. Способ лечения фибромиалгии у субъекта, нуждающегося в таком лечении, который включает введение указанному субъекту терапевтически эффективного количества 5-НТ3 антагониста.6. A method of treating fibromyalgia in a subject in need of such treatment, which comprises administering to the subject a therapeutically effective amount of a 5-HT 3 antagonist. 7. Фармацевтический состав, который в качестве активного агента включает в себя 5-НТ3 антагонист, предназначенный для лечения фибромиалгии.7. The pharmaceutical composition, which as an active agent includes a 5-HT 3 antagonist, intended for the treatment of fibromyalgia.
RU96121561/14A 1994-04-07 1995-04-06 Serotonin antagonist (5ht3) application method for treating fibromyalgia RU2165760C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9406857.4 1994-04-07
GB9406857A GB9406857D0 (en) 1994-04-07 1994-04-07 Improvements in or relating to organic compounds

Publications (2)

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RU96121561A true RU96121561A (en) 1999-01-10
RU2165760C2 RU2165760C2 (en) 2001-04-27

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US (2) US5773436A (en)
EP (1) EP0804196B1 (en)
JP (1) JP2818303B2 (en)
KR (1) KR100415181B1 (en)
CN (1) CN1084618C (en)
AT (1) ATE225176T1 (en)
AU (1) AU706279B2 (en)
CA (1) CA2186844C (en)
CZ (1) CZ290359B6 (en)
DE (1) DE69528475T2 (en)
DK (1) DK0804196T3 (en)
ES (1) ES2184797T3 (en)
FI (1) FI118034B (en)
GB (1) GB9406857D0 (en)
HU (1) HU226892B1 (en)
MX (1) MX9604589A (en)
NO (1) NO312745B1 (en)
PL (1) PL316658A1 (en)
PT (1) PT804196E (en)
RU (1) RU2165760C2 (en)
SK (1) SK281603B6 (en)
WO (1) WO1995027490A1 (en)

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