JP2004504376A5 - - Google Patents
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- JP2004504376A5 JP2004504376A5 JP2002514087A JP2002514087A JP2004504376A5 JP 2004504376 A5 JP2004504376 A5 JP 2004504376A5 JP 2002514087 A JP2002514087 A JP 2002514087A JP 2002514087 A JP2002514087 A JP 2002514087A JP 2004504376 A5 JP2004504376 A5 JP 2004504376A5
- Authority
- JP
- Japan
- Prior art keywords
- receptor
- ht2c
- pharmaceutical composition
- antagonist
- disease
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
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- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 description 10
- 108010072553 5-HT2C Serotonin Receptor Proteins 0.000 description 9
- 239000000018 receptor agonist Substances 0.000 description 7
- 229940044601 receptor agonist Drugs 0.000 description 7
- 201000010099 disease Diseases 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 108091005435 5-HT6 receptors Proteins 0.000 description 5
- 239000003751 serotonin 6 antagonist Substances 0.000 description 5
- 229940116892 5 Hydroxytryptamine 2B receptor antagonist Drugs 0.000 description 2
- 208000030814 Eating disease Diseases 0.000 description 2
- 208000019454 Feeding and Eating disease Diseases 0.000 description 2
- 208000010412 Glaucoma Diseases 0.000 description 2
- 101150104779 HTR2A gene Proteins 0.000 description 2
- 206010046543 Urinary incontinence Diseases 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 208000015114 central nervous system disease Diseases 0.000 description 2
- 235000014632 disordered eating Nutrition 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 101150075901 htr2 gene Proteins 0.000 description 2
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 description 1
- 102000006969 5-HT2B Serotonin Receptor Human genes 0.000 description 1
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 description 1
- 102100024956 5-hydroxytryptamine receptor 2B Human genes 0.000 description 1
- PBIZLLBVGQBNJU-UHFFFAOYSA-N C1CC2=NC=CC=CC2=C2C1CCN2 Chemical class C1CC2=NC=CC=CC2=C2C1CCN2 PBIZLLBVGQBNJU-UHFFFAOYSA-N 0.000 description 1
- 101150013372 Htr2c gene Proteins 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- -1 piperazinylpyrazine compound Chemical class 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- ISZIQZCZKOFSBT-UHFFFAOYSA-N pyrrolo[2,3-g][1]benzazepine Chemical group N1=CC=CC=C2C3=NC=CC3=CC=C21 ISZIQZCZKOFSBT-UHFFFAOYSA-N 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Description
【特許請求の範囲】
【請求項１】 ５−ＨＴ２Ｃレセプターアゴニストと５−ＨＴ６レセプターアンタゴニスト、または当該アゴニストおよび／またはアンタゴニストの塩、エナンチオマーまたはプロドラッグ形態の組み合わせの有効量と、所望により薬学的に許容される担体とを含む医薬組成物。
【請求項２】 該５−ＨＴ２Ｃレセプターアゴニストが、５−ＨＴ２Ａレセプター、５−ＨＴ２Ｂレセプターおよび５−ＨＴ６レセプターそれぞれに対して、少なくとも約１０、好ましくは少なくとも約２０の、５−ＨＴ２Ｃレセプターについての選択性を有する、請求項１の医薬組成物。
【請求項３】 該５−ＨＴ６レセプターアンタゴニストが、５−ＨＴ２Ａレセプター、５−ＨＴ２Ｂレセプターおよび５−ＨＴ２Ｃレセプターそれぞれに対して少なくとも約１０、好ましくは少なくとも約２０の、５−ＨＴ６レセプターについての選択性を有する、請求項１または２の医薬組成物。
【請求項４】 該５−ＨＴ２Ｃレセプターアゴニストがアリールピペラジン化合物、例えばピペラジニルピラジン化合物である、請求項１、２または３の医薬組成物。
【請求項５】 該５−ＨＴ６レセプターアンタゴニストが、アゼピノインドール、例えば、アリールスルホン置換ヘキサヒドロアゼピノインドール、およびアリールスルホニルインドールから選択される、請求項１ないし４のいずれかの医薬組成物。
【請求項６】 組み合わせ治療的量の５−ＨＴ２Ｃレセプターアゴニストと５−ＨＴ６レセプターアンタゴニストが、薬学的に許容される担体と十分に混合される、請求項１ないし５のいずれかの医薬組成物を製造する方法。
【請求項７】 ５−ＨＴ２Ｃレセプターと５−ＨＴ６レセプターに関連する疾患の治療での、同時、分離または逐次的使用のための、組み合わせ調製品としての、５−ＨＴ２Ｃレセプターアゴニストと５−ＨＴ６レセプターアンタゴニストとを含む製品。
【請求項８】 該疾患が、喫食障害、ＣＮＳ障害、尿失禁および緑内障から選択される、請求項７の製品。
【請求項９】 該疾患が体重超過または肥満である、請求項８の製品。
【請求項１０】 ５−ＨＴ２Ｃレセプターと５−ＨＴ６レセプターに関連する疾患の処置のための医薬の製造のための、５−ＨＴ２Ｃレセプターアゴニストと５−ＨＴ６レセプターアンタゴニストの使用。
【請求項１１】 該疾患が、喫食障害、ＣＮＳ障害、尿失禁および緑内障から選択される、請求項１０の使用。
【請求項１２】 該疾患が体重超過または肥満である、請求項１１の使用。
[Claims]
An effective amount of a combination of a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist, or a salt, enantiomer or prodrug form of said agonist and / or antagonist, and optionally a pharmaceutically acceptable carrier. A pharmaceutical composition comprising:
2. The 5-HT2C receptor agonist, wherein said 5-HT2C receptor agonist has at least about 10, preferably at least about 20, relative to each of the 5-HT2A, 5-HT2B and 5-HT6 receptors. The pharmaceutical composition according to claim 1, which has properties.
3. The selectivity for the 5-HT6 receptor, wherein the 5-HT6 receptor antagonist is at least about 10, preferably at least about 20, for each of the 5-HT2A, 5-HT2B and 5-HT2C receptors. The pharmaceutical composition according to claim 1, comprising:
4. The pharmaceutical composition according to claim 1, 2 or 3, wherein said 5-HT2C receptor agonist is an arylpiperazine compound, for example a piperazinylpyrazine compound.
5. The pharmaceutical composition according to claim 1, wherein said 5-HT6 receptor antagonist is selected from azepinoindoles, such as arylsulfone-substituted hexahydroazepinoindoles and arylsulphonylindoles.
6. The pharmaceutical composition according to claim 1, wherein the combined therapeutic amounts of the 5-HT2C receptor agonist and the 5-HT6 receptor antagonist are thoroughly mixed with a pharmaceutically acceptable carrier. How to make.
7. A 5-HT2C receptor agonist and a 5-HT6 receptor as a combined preparation for simultaneous, separate or sequential use in the treatment of a disease associated with the 5-HT2C receptor and the 5-HT6 receptor. A product comprising an antagonist.
8. The product of claim 7, wherein said disease is selected from eating disorders, CNS disorders, urinary incontinence and glaucoma.
9. The product of claim 8, wherein said disease is overweight or obese.
10. Use of a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist for the manufacture of a medicament for the treatment of a disease associated with the 5-HT2C receptor and the 5-HT6 receptor.
11. The use according to claim 10, wherein said disease is selected from eating disorders, CNS disorders, urinary incontinence and glaucoma.
12. The use according to claim 11, wherein said disease is overweight or obese.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0002754A SE0002754D0 (en) | 2000-07-21 | 2000-07-21 | New pharmaceutical combination formulation and method of treatment with the combination |
| PCT/SE2001/001651 WO2002008178A1 (en) | 2000-07-21 | 2001-07-19 | New combination of serotonin agonist (5ht2) and antagonist (5ht6)as pharmaceutical formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004504376A JP2004504376A (en) | 2004-02-12 |
| JP2004504376A5 true JP2004504376A5 (en) | 2008-07-17 |
Family
ID=20280577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002514087A Withdrawn JP2004504376A (en) | 2000-07-21 | 2001-07-19 | Novel combination of serotonin agonist (5HT2) and antagonist (5HT6) as pharmaceutical preparation |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP1301476A1 (en) |
| JP (1) | JP2004504376A (en) |
| KR (1) | KR100845450B1 (en) |
| CN (1) | CN1221254C (en) |
| AU (2) | AU8273401A (en) |
| BR (1) | BR0112661A (en) |
| CA (1) | CA2411192A1 (en) |
| EA (1) | EA006604B1 (en) |
| HK (1) | HK1057536A1 (en) |
| HU (1) | HUP0301346A3 (en) |
| IL (1) | IL154057A0 (en) |
| MX (1) | MXPA03000548A (en) |
| NO (1) | NO20030304L (en) |
| NZ (1) | NZ523216A (en) |
| PL (1) | PL360309A1 (en) |
| SE (1) | SE0002754D0 (en) |
| WO (1) | WO2002008178A1 (en) |
| YU (1) | YU2603A (en) |
| ZA (1) | ZA200210234B (en) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0115102B1 (en) * | 2000-11-02 | 2013-11-26 | 1-Aryl or 1-alkylsulfonylheterocyclylbenzazoles compounds and composition comprising them | |
| US7034029B2 (en) | 2000-11-02 | 2006-04-25 | Wyeth | 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands |
| CN1321110C (en) * | 2001-06-15 | 2007-06-13 | 弗·哈夫曼-拉罗切有限公司 | 4-piperazinylindole derivatives with 5-HT6 receptor affinity |
| MXPA03011638A (en) * | 2001-06-15 | 2004-04-02 | Hoffmann La Roche | 4-piperazinylindole derivatives with 5-ht6 receptor affinity. |
| US6825198B2 (en) | 2001-06-21 | 2004-11-30 | Pfizer Inc | 5-HT receptor ligands and uses thereof |
| GB0202679D0 (en) * | 2002-02-05 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
| ES2307919T3 (en) | 2002-03-27 | 2008-12-01 | Glaxo Group Limited | DERIVATIVES OF QUINOLINA AND ITS USE AS LIGANDS OF 5-HT6. |
| CL2004000826A1 (en) * | 2003-04-25 | 2005-03-04 | Pfizer | USE OF AN AGONIST FOR THE 5-HT2C RECEPTOR TO PREPARE A USEFUL MEDICINAL PRODUCT IN THE TREATMENT OF URINARY INCONTINENCE CAUSED BY STRESS, WITH THE CONDITION THAT THE AGONIST IS NOT 1- [6-CHLORINE-5- (TRIFLUOROMETIL) -2- PIRIDINIL] PIPERAZINA (ORG-129 |
| DK1558582T3 (en) | 2003-07-22 | 2006-05-08 | Arena Pharm Inc | Diaryl and arylheteroarlurea derivatives as modulators of the activity of the 5-HT2A serotonin receptor useful for the prophylaxis or treatment of disorders related thereto |
| EP2248524A3 (en) | 2004-08-25 | 2011-03-09 | Takeda Pharmaceutical Company Limited | Preventives/remedies for stress urinary incontinence and method of screening the same |
| US7713954B2 (en) | 2004-09-30 | 2010-05-11 | Roche Palo Alto Llc | Compositions and methods for treating cognitive disorders |
| US20100048713A1 (en) * | 2006-01-06 | 2010-02-25 | Aarhus Universitet | Compounds acting on the serotonin transporter |
| JP5528699B2 (en) | 2006-05-16 | 2014-06-25 | 武田薬品工業株式会社 | Fused heterocyclic compounds and uses thereof |
| US20070293475A1 (en) * | 2006-06-20 | 2007-12-20 | Alcon Manufacturing Ltd. | Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma |
| DE602007012080D1 (en) * | 2007-08-01 | 2011-03-03 | Esteve Labor Dr | Combination of at least two 5-HT6 ligands |
| EP2789338A3 (en) | 2007-11-15 | 2015-01-14 | Takeda Pharmaceutical Company Limited | Condensed pyridine derivate and use thereof |
| WO2009074607A1 (en) | 2007-12-12 | 2009-06-18 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| WO2009123714A2 (en) | 2008-04-02 | 2009-10-08 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| US9126946B2 (en) | 2008-10-28 | 2015-09-08 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
| UA100192C2 (en) | 2008-11-11 | 2012-11-26 | УАЙТ ЭлЭлСи | 1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands |
| KR101768234B1 (en) | 2009-06-15 | 2017-08-14 | 다케다 야쿠힌 고교 가부시키가이샤 | Pyrazinooxazepine derivatives |
| EP2510949A4 (en) | 2009-12-11 | 2013-11-13 | Astellas Pharma Inc | Therapeutic agent for fibromyalgia |
| MX2017016413A (en) | 2015-06-12 | 2018-08-01 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder. |
| RU2018103338A (en) | 2015-07-15 | 2019-08-15 | Аксовант Сайенсиз Гмбх | Derivatives of diaryl and arylheteroarylureas for the prevention and treatment of hallucinations associated with a neurodegenerative disease |
| CN107628981B (en) * | 2017-10-31 | 2019-07-30 | 威海市妇女儿童医院 | A kind of cinnamoyl sulfonylindoline compounds and its application for preparing glaucoma medicine |
| JPWO2019131902A1 (en) | 2017-12-27 | 2020-12-10 | 武田薬品工業株式会社 | Remedies for stress urinary incontinence and fecal incontinence |
| CN111269165A (en) * | 2018-12-05 | 2020-06-12 | 中国科学院大连化学物理研究所 | Synthetic method of 3-arylsulfonyl indole derivative |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DZ2376A1 (en) * | 1996-12-19 | 2002-12-28 | Smithkline Beecham Plc | New sulfonamide derivatives process for their preparation and pharmaceutical compositions containing them. |
| GB9803411D0 (en) * | 1998-02-18 | 1998-04-15 | Smithkline Beecham Plc | Novel compounds |
| US6100291A (en) * | 1998-03-16 | 2000-08-08 | Allelix Biopharmaceuticals Inc. | Pyrrolidine-indole compounds having 5-HT6 affinity |
| US6251893B1 (en) * | 1998-06-15 | 2001-06-26 | Nps Allelix Corp. | Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity |
| GB9819035D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Res Ltd | Chemical compounds VII |
-
2000
- 2000-07-21 SE SE0002754A patent/SE0002754D0/en unknown
-
2001
- 2001-07-19 AU AU8273401A patent/AU8273401A/en active Pending
- 2001-07-19 AU AU2001282734A patent/AU2001282734B2/en not_active Ceased
- 2001-07-19 CA CA002411192A patent/CA2411192A1/en not_active Abandoned
- 2001-07-19 EA EA200300183A patent/EA006604B1/en not_active IP Right Cessation
- 2001-07-19 CN CNB018131549A patent/CN1221254C/en not_active Expired - Fee Related
- 2001-07-19 HU HU0301346A patent/HUP0301346A3/en unknown
- 2001-07-19 MX MXPA03000548A patent/MXPA03000548A/en active IP Right Grant
- 2001-07-19 EP EP01961472A patent/EP1301476A1/en not_active Withdrawn
- 2001-07-19 YU YU2603A patent/YU2603A/en unknown
- 2001-07-19 BR BR0112661-0A patent/BR0112661A/en not_active IP Right Cessation
- 2001-07-19 KR KR1020037000321A patent/KR100845450B1/en not_active IP Right Cessation
- 2001-07-19 PL PL36030901A patent/PL360309A1/en not_active Application Discontinuation
- 2001-07-19 JP JP2002514087A patent/JP2004504376A/en not_active Withdrawn
- 2001-07-19 IL IL15405701A patent/IL154057A0/en unknown
- 2001-07-19 NZ NZ523216A patent/NZ523216A/en not_active IP Right Cessation
- 2001-07-19 WO PCT/SE2001/001651 patent/WO2002008178A1/en active IP Right Grant
-
2002
- 2002-12-18 ZA ZA200210234A patent/ZA200210234B/en unknown
-
2003
- 2003-01-20 NO NO20030304A patent/NO20030304L/en not_active Application Discontinuation
-
2004
- 2004-01-15 HK HK04100306A patent/HK1057536A1/en not_active IP Right Cessation
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