FI118034B - Serotoniiniantagonistien (5HT3) käyttö fibromyalgian hoitoon - Google Patents
Serotoniiniantagonistien (5HT3) käyttö fibromyalgian hoitoon Download PDFInfo
- Publication number
- FI118034B FI118034B FI964004A FI964004A FI118034B FI 118034 B FI118034 B FI 118034B FI 964004 A FI964004 A FI 964004A FI 964004 A FI964004 A FI 964004A FI 118034 B FI118034 B FI 118034B
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- FI
- Finland
- Prior art keywords
- alkyl
- methyl
- hydrogen
- formula
- pain
- Prior art date
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- 208000001640 Fibromyalgia Diseases 0.000 title claims abstract description 12
- 229940082988 antihypertensives serotonin antagonists Drugs 0.000 title description 2
- 239000003420 antiserotonin agent Substances 0.000 title description 2
- 239000003369 serotonin 5-HT3 receptor antagonist Substances 0.000 claims abstract description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 34
- 229910052739 hydrogen Inorganic materials 0.000 claims description 19
- 239000001257 hydrogen Substances 0.000 claims description 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 150000002431 hydrogen Chemical group 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 7
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 5
- 125000003884 phenylalkyl group Chemical group 0.000 claims description 5
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
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- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
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Classifications
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- Life Sciences & Earth Sciences (AREA)
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- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
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- Physical Education & Sports Medicine (AREA)
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- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Heart & Thoracic Surgery (AREA)
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Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9406857A GB9406857D0 (en) | 1994-04-07 | 1994-04-07 | Improvements in or relating to organic compounds |
| GB9406857 | 1994-04-07 | ||
| EP9501264 | 1995-04-06 | ||
| PCT/EP1995/001264 WO1995027490A1 (en) | 1994-04-07 | 1995-04-06 | Use of serotonin antagonists (5ht3) for treating fibromyalgia |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI964004A0 FI964004A0 (fi) | 1996-10-04 |
| FI964004L FI964004L (fi) | 1996-11-29 |
| FI118034B true FI118034B (fi) | 2007-06-15 |
Family
ID=10753131
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI964004A FI118034B (fi) | 1994-04-07 | 1996-10-04 | Serotoniiniantagonistien (5HT3) käyttö fibromyalgian hoitoon |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US5773436A (cs) |
| EP (1) | EP0804196B1 (cs) |
| JP (1) | JP2818303B2 (cs) |
| KR (1) | KR100415181B1 (cs) |
| CN (1) | CN1084618C (cs) |
| AT (1) | ATE225176T1 (cs) |
| AU (1) | AU706279B2 (cs) |
| CA (1) | CA2186844C (cs) |
| CZ (1) | CZ290359B6 (cs) |
| DE (1) | DE69528475T2 (cs) |
| DK (1) | DK0804196T3 (cs) |
| ES (1) | ES2184797T3 (cs) |
| FI (1) | FI118034B (cs) |
| GB (1) | GB9406857D0 (cs) |
| HU (1) | HU226892B1 (cs) |
| MX (1) | MX9604589A (cs) |
| NO (1) | NO312745B1 (cs) |
| PL (1) | PL316658A1 (cs) |
| PT (1) | PT804196E (cs) |
| RU (1) | RU2165760C2 (cs) |
| SK (1) | SK281603B6 (cs) |
| WO (1) | WO1995027490A1 (cs) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6069162A (en) * | 1996-05-27 | 2000-05-30 | Fujisawa Pharmaceutical Co., Ltd. | Indolyl and benzofuranyl carboxamides as inhibitors of nitric oxide production |
| US6696495B2 (en) | 1998-12-02 | 2004-02-24 | Snowden Pharmaceuticals, Llc | Treatment of disorders secondary to organic impairments |
| US6323242B1 (en) | 1998-12-02 | 2001-11-27 | Peter Sterling Mueller | Treatment of disorders secondary to organic impairments |
| AU2672500A (en) | 1999-02-18 | 2000-09-04 | Novartis Ag | Systemic use of 5-ht3 receptor antagonists against rheumatic inflammatory processes |
| JP2002537245A (ja) * | 1999-02-18 | 2002-11-05 | ノバルティス アクチエンゲゼルシャフト | ５−ｈｔ３レセプターアンタゴニストの使用 |
| TW518218B (en) * | 1999-05-27 | 2003-01-21 | Merck Patent Gmbh | Pharmaceutical compositions comprising 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl)piperazine or its physiologically acceptable salts for use in the treatment of sub-type anxiety disorders |
| GB9918425D0 (en) * | 1999-08-04 | 1999-10-06 | Novartis Ag | Organic compounds |
| US20040048874A1 (en) * | 2001-05-22 | 2004-03-11 | Bardsley Hazel Judith | New therapeutic use of 4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D]pyrimidine |
| GB0216027D0 (en) * | 2002-07-10 | 2002-08-21 | Arachnova Therapeutics Ltd | New therapeutic use |
| AR036040A1 (es) | 2001-06-12 | 2004-08-04 | Upjohn Co | Compuestos de heteroarilo multiciclicos sustituidos con quinuclidinas y composiciones farmaceuticas que los contienen |
| AR036041A1 (es) | 2001-06-12 | 2004-08-04 | Upjohn Co | Compuestos aromaticos heterociclicos sustituidos con quinuclidina y composiciones farmaceuticas que los contienen |
| JP4371811B2 (ja) | 2001-10-02 | 2009-11-25 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 疾患治療のためのアザ二環式置換縮合ヘテロアリール化合物 |
| JP2005510482A (ja) * | 2001-10-16 | 2005-04-21 | アストラゼネカ・アクチエボラーグ | 線維筋痛症候群の治療方法 |
| US6849620B2 (en) | 2001-10-26 | 2005-02-01 | Pfizer Inc | N-(azabicyclo moieties)-substituted hetero-bicyclic aromatic compounds for the treatment of disease |
| JP2005523287A (ja) | 2002-02-19 | 2005-08-04 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 疾患治療用アザビシクロ化合物 |
| JP2005523288A (ja) | 2002-02-19 | 2005-08-04 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 疾病治療用の縮合した二環式−ｎ−架橋−複素環式芳香族カルボキサミド |
| AU2003237657A1 (en) * | 2002-05-24 | 2003-12-12 | Epidauros Biotechnologie Ag | Means and methods for improved treatment using "setrones" |
| SK288115B6 (sk) | 2002-09-25 | 2013-09-03 | Memory Pharmaceuticals Corporation | Indazoles, pharmaceutical compositions comprising them and their use |
| WO2004062624A2 (en) * | 2003-01-13 | 2004-07-29 | Dynogen Pharmaceuticals, Inc. | Method of treating nausea, vomiting, retching or any combination thereof |
| EP1558081A4 (en) * | 2003-01-13 | 2006-06-14 | Dynogen Pharmaceuticals Inc | METHOD FOR THE TREATMENT OF FUNCTIONAL ENDURANCE DISEASES |
| PT1697378E (pt) | 2003-12-22 | 2008-02-28 | Memory Pharm Corp | Indoles, 1h-indazoles, 1,2-benzisoxazoles e 1,2-benzisotiazoles, sua preparação e utilizações |
| TW200533348A (en) * | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| RU2417225C2 (ru) | 2004-03-25 | 2011-04-27 | Мемори Фармасьютиклз Корпорейшн | Индазолы, бензотиазолы, бензоизотиазолы, бензизоксазолы и их получение и применение |
| US7728006B2 (en) * | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| US8309575B2 (en) | 2004-04-07 | 2012-11-13 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| TWI351282B (en) * | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| ATE487716T1 (de) * | 2004-04-22 | 2010-11-15 | Memory Pharm Corp | Indole, 1h-indazole, 1,2-benzisoxazole, 1,2- benzoisothiazole, deren herstellung und verwendungen |
| MXPA06012880A (es) * | 2004-05-07 | 2007-01-26 | Memory Pharm Corp | 1h-indazoles, benzotiazoles, 1,2-benzoisoxazoles, 1,2-benzoisotiazoles y cromonas y preparacion y usos de los mismos. |
| ES2332808T3 (es) * | 2004-11-05 | 2010-02-12 | Theravance, Inc. | Compuestos agonistas del receptor 5-ht4. |
| ES2327142T3 (es) * | 2004-11-05 | 2009-10-26 | Theravance, Inc. | Compuestos de quinolinona-carboxamida. |
| BRPI0517494A (pt) | 2004-12-22 | 2008-10-14 | Memory Pharm Corp | composto, composição farmacêutica, método de ativação/estimulação seletiva de receptores nicotìnicos de a-7 em um paciente em que tal ativação/estimulação tem um efeito terapêutico, método de tratamento de um paciente que sofre de uma doença psicótica, uma doença neurodegenerativa que envolve uma disfunção do sistema colinérgico, e/ou uma condição de debilitação da memória e/ou da cognição, método de tratamento de um paciente que sofre de demência e/ou uma outra condição com perda da memória, método de tratamento de um paciente que sofre de debilitação da memória devido à debilitação cognitiva suave devido ao envelhecimento, mal de alzheimer, esquizofrenia, mal de parkinson, mal de huntington, mal de pick, mal de creutzfeldt-jakob, depressão, envelhecimento, trauma na cabeça, acidente vascular cerebral, hipoxia do snc, senilidade cerebral, demência de multiinfarto, hiv e/ou doença cardiovascular, método de tratamento e/ou prevenção da demência em um paciente com o mal de alzheimer, método de tratamento de um paciente para cortar o vìcio do álcool ou o tratamento de um paciente com a terapia anti-intoxicação, método de tratamento de um paciente para propiciar neuroproteção contra os danos associados com acidentes vasculares cerebrais e isquemia e excitotoxicidade induzida por glutamatos, método de tratamento de um paciente que sofre do vìcio da nicotina, dor, tontura do fuso horário, obesidade e/ou diabetes, método de indução do ato de parar fumar em um paciente, método de tratamento de um paciente que sofre de debilitação cognitiva suave (mci), demência vascular (vad), declìnio cognitivo associado com a idade (aacd), amnésia associada com a cirurgia com o coração aberto, parada cardìaca, anestesia geral, deficiências da memória devido à exposição a agentes anestésicos, debilitação cognitiva induzida pela privação do sono, sìndrome de fadiga crÈnica, narcolepsia, demência relacionada com a aids, debilitação cognitiva relacionada com a epilepsia, sìndrome de down, demência relacionada ao alcoolismo, debilitações da memória induzidas por drogas/substáncias, demência pugilìstica (sìndrome do boxeador), ou demência animal, método para o tratamento da perda da memória, método para o tratamento de um paciente que sofre de debilitação da memória, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da disfunção da transmissão do receptor nicotìnico de acetilcolina em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante de receptores nicotìnicos de acetilcolina defeituosos ou funcionando mal em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da transmissão suprimida do receptor nicotìnico de acetilcolina em um paciente, método para o tratamento ou a profilaxia de uma doença ou de uma condição resultante da perda de sinapses colinérgicas em um paciente, método para a proteção dos neurÈnios em um paciente com neurotoxicidade induzi |
| WO2006069125A1 (en) * | 2004-12-22 | 2006-06-29 | Theravance, Inc. | Indazole-carboxamide compounds |
| EA013567B1 (ru) * | 2005-03-02 | 2010-06-30 | Тереванс, Инк. | Хинолиноновые соединения в качестве агонистов рецептора 5-ht |
| WO2006105117A2 (en) * | 2005-03-28 | 2006-10-05 | Dynogen Pharmaceuticals, Inc. | Method of treating disorders and conditions using peripherally-restricted antagonists and inhibitors |
| US8106066B2 (en) * | 2005-09-23 | 2012-01-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
| CN102781436B (zh) | 2009-11-06 | 2014-01-08 | 爱思开生物制药株式会社 | 纤维肌痛综合征的治疗方法 |
| JOP20130213B1 (ar) | 2012-07-17 | 2021-08-17 | Takeda Pharmaceuticals Co | معارضات لمستقبلht3-5 |
| ES2883295T3 (es) | 2014-09-29 | 2021-12-07 | Takeda Pharmaceuticals Co | Forma cristalina de 1-(1-metil-1h-pirazol-4-il)-n-((1r,5s,7s)-9-metil-3-oxa-9-azabiciclo[3.3.1]nonan-7-il)-1h-indol-3-carboxamida |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CY1908A (en) * | 1984-12-20 | 1985-12-13 | Sandoz Ag | Treatment of gastrointestinal disorders using 5-HT3 antagonists |
| EP0498466B1 (en) * | 1985-04-27 | 2002-07-24 | F. Hoffmann-La Roche Ag | Indazole-3-carboxamide and -3-carboxylic acid derivatives |
| GB8623142D0 (en) * | 1986-09-26 | 1986-10-29 | Beecham Group Plc | Compounds |
| US5246942A (en) * | 1988-04-27 | 1993-09-21 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Pharmaceutically useful dibenzofurancarboxamides of specific stereo-configuration |
| US4963689A (en) * | 1989-05-19 | 1990-10-16 | Pfizer Inc. | Heterocyclicguanidines as 5HT3 antagonists |
| GB8928208D0 (en) * | 1989-12-13 | 1990-02-14 | Glaxo Group Ltd | Medicaments |
| EP0517984A1 (en) * | 1991-06-11 | 1992-12-16 | Merrell Dow Pharmaceuticals Inc. | Derivatives of amide analogs of certain methano bridged quinolizines |
-
1994
- 1994-04-07 GB GB9406857A patent/GB9406857D0/en active Pending
-
1995
- 1995-04-06 JP JP7526064A patent/JP2818303B2/ja not_active Expired - Fee Related
- 1995-04-06 SK SK1278-96A patent/SK281603B6/sk not_active IP Right Cessation
- 1995-04-06 US US08/721,988 patent/US5773436A/en not_active Expired - Lifetime
- 1995-04-06 WO PCT/EP1995/001264 patent/WO1995027490A1/en active IP Right Grant
- 1995-04-06 HU HU9602721A patent/HU226892B1/hu not_active IP Right Cessation
- 1995-04-06 MX MX9604589A patent/MX9604589A/es not_active IP Right Cessation
- 1995-04-06 PT PT95916611T patent/PT804196E/pt unknown
- 1995-04-06 EP EP95916611A patent/EP0804196B1/en not_active Expired - Lifetime
- 1995-04-06 DE DE69528475T patent/DE69528475T2/de not_active Expired - Lifetime
- 1995-04-06 CA CA002186844A patent/CA2186844C/en not_active Expired - Fee Related
- 1995-04-06 KR KR1019960705579A patent/KR100415181B1/ko not_active Expired - Fee Related
- 1995-04-06 CN CN95192946A patent/CN1084618C/zh not_active Expired - Fee Related
- 1995-04-06 CZ CZ19962915A patent/CZ290359B6/cs not_active IP Right Cessation
- 1995-04-06 DK DK95916611T patent/DK0804196T3/da active
- 1995-04-06 PL PL95316658A patent/PL316658A1/xx unknown
- 1995-04-06 AT AT95916611T patent/ATE225176T1/de not_active IP Right Cessation
- 1995-04-06 ES ES95916611T patent/ES2184797T3/es not_active Expired - Lifetime
- 1995-04-06 AU AU23052/95A patent/AU706279B2/en not_active Ceased
- 1995-04-06 RU RU96121561/14A patent/RU2165760C2/ru not_active IP Right Cessation
-
1996
- 1996-10-04 FI FI964004A patent/FI118034B/fi not_active IP Right Cessation
- 1996-10-04 NO NO19964236A patent/NO312745B1/no not_active IP Right Cessation
-
1998
- 1998-05-18 US US09/080,605 patent/US5985866A/en not_active Expired - Fee Related
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