RU94022663A - Derivatives of 2-mercaptobenzimidazole having selective anxyolytic activity - Google Patents
Derivatives of 2-mercaptobenzimidazole having selective anxyolytic activityInfo
- Publication number
- RU94022663A RU94022663A RU94022663/04A RU94022663A RU94022663A RU 94022663 A RU94022663 A RU 94022663A RU 94022663/04 A RU94022663/04 A RU 94022663/04A RU 94022663 A RU94022663 A RU 94022663A RU 94022663 A RU94022663 A RU 94022663A
- Authority
- RU
- Russia
- Prior art keywords
- derivatives
- mercaptobenzimidazole
- compounds
- anxyolytic
- activity
- Prior art date
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
FIELD: medicine. SUBSTANCE: desired products have common formulawhere n= 0,2,3; R is allyl, dialkylamino- or nitrogen-containing heterocycles, Rand Rare the same or different and represent H, lower alkyls and alkoxy. Desired derivatives are prepared by alkylation of 2-mercaptobenzimidazoles with appropriate alkylating agent. The process is followed by treatment thus prepared bases with hydrogen chloride. Said derivatives or their pharmaceutically acceptable salts has anxyolytic action and are low toxic. EFFECT: creates novel derivatives of 2-mercaptobenzimidazole having selective anxyolytic activity.
Claims (1)
где n = 0, 2, 3; R - аллил, диалкиламино или азотсодержащие гетероциклы; R1 и R2 - одинаковые или различные, водород, низшие алкилы, алкокси, и их фармацевтически приемлемым солям, обладающим анксиолитической активностью. Целью изобретения является создание новых соединений в ряду 2-меркаптобензимидазола, обладающих селективной анксиолитической активностью при низкой токсичности. Цель достигается синтезом заявляемых соединений путем алкилирования 2-меркаптобензимидазолов соответствующими алкилирующими агентами с последующей обработкой образующихся оснований хлористым водородом. По данным проведенного психофармакологического скрининга по общепринятой схеме заявляемые соединения в широком диапазоне доз обладают выраженным анксиолитическим действием, которое не сопровождается побочными седативным, снотворным, миорелаксантным эффектами. Заявляемые соединения имеют низкую токсичность.The invention relates to new biologically active compounds - derivatives of 2-mercaptobenzimidazole of the General formula
where n = 0, 2, 3; R is allyl, dialkylamino or nitrogen-containing heterocycles; R 1 and R 2 are the same or different, hydrogen, lower alkyls, alkoxy, and their pharmaceutically acceptable salts having anxiolytic activity. The aim of the invention is the creation of new compounds in the series of 2-mercaptobenzimidazole with selective anxiolytic activity with low toxicity. The goal is achieved by the synthesis of the claimed compounds by alkylation of 2-mercaptobenzimidazoles with appropriate alkylating agents, followed by treatment of the resulting bases with hydrogen chloride. According to psychopharmacological screening according to the generally accepted scheme, the claimed compounds in a wide range of doses have a pronounced anxiolytic effect, which is not accompanied by side sedative, hypnotic, muscle relaxant effects. The inventive compounds have low toxicity.
Priority Applications (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU94022663/04A RU2061686C1 (en) | 1994-06-10 | 1994-06-10 | 2-mercaptobenzimidazole derivatives having selective anxiolytic activity |
| DE69528843T DE69528843T2 (en) | 1994-06-10 | 1995-05-11 | PHARMACOLOGICALLY ACTIVE 2-MERCAPTOBENZIMIDAZOLE DERIVATIVES |
| US08/750,369 US6376666B1 (en) | 1994-06-10 | 1995-05-11 | 2-mercaptobenzimidazole derivatives possessing pharmacological activity |
| JP50199296A JP3559045B2 (en) | 1994-06-10 | 1995-05-11 | 2-mercaptobenzimidazole derivatives having pharmacological activity |
| PCT/RU1995/000085 WO1995034304A1 (en) | 1994-06-10 | 1995-05-11 | Pharmacologically active 2-mercaptobenzimidazole derivatives |
| EP95918794A EP0788795B1 (en) | 1994-06-10 | 1995-05-11 | Pharmacologically active 2-mercaptobenzimidazole derivatives |
| KR1019960707153A KR970703765A (en) | 1994-06-10 | 1996-12-10 | 2-MERCAPTOBENZIMIDAZOLE DERIVATIVES POSSESSING THE PHARMACOLOGICAL ACTIVITY |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU94022663/04A RU2061686C1 (en) | 1994-06-10 | 1994-06-10 | 2-mercaptobenzimidazole derivatives having selective anxiolytic activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU94022663A true RU94022663A (en) | 1996-05-27 |
| RU2061686C1 RU2061686C1 (en) | 1996-06-10 |
Family
ID=20157201
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU94022663/04A RU2061686C1 (en) | 1994-06-10 | 1994-06-10 | 2-mercaptobenzimidazole derivatives having selective anxiolytic activity |
Country Status (1)
| Country | Link |
|---|---|
| RU (1) | RU2061686C1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2423200A1 (en) * | 2010-05-26 | 2012-02-29 | Afofarm, Cjsc | Polymorphic forms of 5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole dihydrochloride and processes for their preparation |
| RU2519191C1 (en) * | 2013-02-19 | 2014-06-10 | Общество с ограниченной ответственностью "Научно-производственное объединение "МедФармСинтез" | Medication, possessing anxiolytic activity |
| RU2578412C1 (en) * | 2014-12-02 | 2016-03-27 | Общество С Ограниченной Ответственностью "Валента - Интеллект" | Pharmaceutical composition for treating asthenia and/or chronic fatigue syndrome |
| JP2023526515A (en) | 2020-05-20 | 2023-06-21 | ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティ オブ イリノイ | Methods for treating lysosomal storage diseases with histatin peptides |
-
1994
- 1994-06-10 RU RU94022663/04A patent/RU2061686C1/en active Protection Beyond IP Right Term
Also Published As
| Publication number | Publication date |
|---|---|
| RU2061686C1 (en) | 1996-06-10 |
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