WO1996006601B1 - Utilisation des ligands de 5-ht comme agents antiprurigineux - Google Patents
Utilisation des ligands de 5-ht comme agents antiprurigineuxInfo
- Publication number
- WO1996006601B1 WO1996006601B1 PCT/US1995/010838 US9510838W WO9606601B1 WO 1996006601 B1 WO1996006601 B1 WO 1996006601B1 US 9510838 W US9510838 W US 9510838W WO 9606601 B1 WO9606601 B1 WO 9606601B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- ligand
- antagonist
- agonist
- agonists
- group
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title claims abstract 16
- 239000003908 antipruritic agent Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract 15
- 208000003251 Pruritus Diseases 0.000 claims abstract 8
- 239000005557 antagonist Substances 0.000 claims abstract 5
- 239000000952 serotonin receptor agonist Substances 0.000 claims abstract 4
- 241000124008 Mammalia Species 0.000 claims abstract 3
- 239000000387 serotonin 5-HT4 receptor agonist Substances 0.000 claims abstract 3
- 150000002148 esters Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000002484 serotonin 2C antagonist Substances 0.000 claims 4
- HTEVMLYDEWVIQE-SPIKMXEPSA-N 4-(4-methylpiperazin-1-yl)-7-(trifluoromethyl)pyrrolo[1,2-a]quinoxaline dimaleate Chemical compound [H+].[H+].[H+].[H+].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.C1CN(C)CCN1C1=NC2=CC(C(F)(F)F)=CC=C2N2C1=CC=C2 HTEVMLYDEWVIQE-SPIKMXEPSA-N 0.000 claims 2
- ASXGJMSKWNBENU-UHFFFAOYSA-N 8-OH-DPAT Chemical compound C1=CC(O)=C2CC(N(CCC)CCC)CCC2=C1 ASXGJMSKWNBENU-UHFFFAOYSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 claims 2
- 229960005417 ketanserin Drugs 0.000 claims 2
- XRXDAJYKGWNHTQ-UHFFFAOYSA-N quipazine Chemical compound C1CNCCN1C1=CC=C(C=CC=C2)C2=N1 XRXDAJYKGWNHTQ-UHFFFAOYSA-N 0.000 claims 2
- 229950002315 quipazine Drugs 0.000 claims 2
- WYWNEDARFVJQSG-UHFFFAOYSA-N 2-methylserotonin Chemical compound C1=C(O)C=C2C(CCN)=C(C)NC2=C1 WYWNEDARFVJQSG-UHFFFAOYSA-N 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- -1 spirotraxine Chemical compound 0.000 claims 1
- BYQQRDWZLNYPPA-UHFFFAOYSA-N α-methylserotonin Chemical compound C1=CC(O)=C[C]2C(CC(N)C)=CN=C21 BYQQRDWZLNYPPA-UHFFFAOYSA-N 0.000 claims 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 abstract 2
- 102000014630 G protein-coupled serotonin receptor activity proteins Human genes 0.000 abstract 2
- 239000003420 antiserotonin agent Substances 0.000 abstract 2
- 230000002009 allergenic effect Effects 0.000 abstract 1
- 239000000427 antigen Substances 0.000 abstract 1
- 102000036639 antigens Human genes 0.000 abstract 1
- 108091007433 antigens Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000004031 partial agonist Substances 0.000 abstract 1
- 239000003521 serotonin 5-HT1 receptor agonist Substances 0.000 abstract 1
- 239000003478 serotonin 5-HT2 receptor agonist Substances 0.000 abstract 1
- 239000000198 serotonin 5-HT3 receptor agonist Substances 0.000 abstract 1
- 238000007910 systemic administration Methods 0.000 abstract 1
Abstract
La présente invention est fondée sur la découverte selon laquelle des ligands du récepteur de 5-HT sont utiles dans le traitement de modèles expérimentaux de prurits (démangeaisons) rencontrés cliniquement. Un ligand de 5-HT, utilisé selon la description, est un composé pouvant se fixer, avec une certaine sélectivité, à au moins un site récepteur de 5-HT. L'administration par voie générale d'agonistes et d'antagonistes de 5-HT entraîne une réduction du nombre de réaction de grattage et de lichénification à une provocation occulaire par des antigènes allergéniques. A cet effet, la présente invention concerne un procédé permettant de traiter un prurit par administration par voie générale d'une dose thérapeutiquement efficace d'un agoniste ou d'un antagoniste de 5-HT à un mammifère souffrant dudit prurit. Les ligands de 5-HT peuvent, par exemple, être sélectionnés parmi les agonistes, les agonistes partiels et les antagonistes de 5-HT1, 5-HT2, 5-HT3 et 5-HT4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/298,245 US5521183A (en) | 1994-08-30 | 1994-08-30 | Use of 5-HT ligands as anti-pruritic agents |
| US08/298,245 | 1994-08-30 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO1996006601A1 WO1996006601A1 (fr) | 1996-03-07 |
| WO1996006601B1 true WO1996006601B1 (fr) | 1996-03-21 |
Family
ID=23149684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1995/010838 WO1996006601A1 (fr) | 1994-08-30 | 1995-08-25 | Utilisation des ligands de 5-ht comme agents antiprurigineux |
Country Status (2)
| Country | Link |
|---|---|
| US (1) | US5521183A (fr) |
| WO (1) | WO1996006601A1 (fr) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5869497A (en) * | 1996-03-15 | 1999-02-09 | Eli Lilly And Company | Method of treating or ameliorating the symptoms of common cold or allergic rhinitis |
| BR9708146A (pt) * | 1996-03-15 | 1999-07-27 | Lilly Co Eli | Processo de tratamento de resfriado comum ou de rinite alérgica |
| US5886003A (en) * | 1996-03-25 | 1999-03-23 | Eli Lilly And Company | Methods of treating or ameliorating the symptoms of venomous bites and stings |
| FR2758263B1 (fr) * | 1997-01-16 | 1999-12-17 | Oreal | Utilisation d'un antagoniste ou d'un agoniste de serotonine specifiques respectivement du recepteur 5ht2 et 5ht1d dans une composition cosmetique ou dermatologique pour peaux sensibles et composition obtenue |
| ES2256085T3 (es) * | 1999-11-23 | 2006-07-16 | Janssen Pharmaceutica N.V. | Uso de agonistas de 5ht3 para relajar el fundus. |
| BR0109193A (pt) * | 2000-03-17 | 2003-05-27 | Alcon Inc | Compostos com atividade agonista 5-ht2 e 5-ht1a para tratamento do glaucoma |
| WO2008086069A1 (fr) * | 2007-01-03 | 2008-07-17 | The General Hospital Corporation | Procédé de traitement du prurit |
| WO2009059307A1 (fr) * | 2007-11-01 | 2009-05-07 | Washington University In St. Louis | Compositions et procédés de traitement du prurit |
| US20100048607A1 (en) * | 2008-08-25 | 2010-02-25 | Chandrashekhar Kocherlakota | Formulations comprising palonosetron |
| US8957024B2 (en) | 2011-07-27 | 2015-02-17 | Washington University | Composition and methods for reducing opioid-induced pruritus |
| WO2013154513A1 (fr) | 2012-04-04 | 2013-10-17 | Mi̇lli̇ Savunma Bakanliği | Utilisation d'antagonistes du récepteur 5-ht7 comprenant certains antipsychotiques atypiques en tant qu'antiprurigineux |
| US9198898B2 (en) | 2013-06-24 | 2015-12-01 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| US8906951B1 (en) | 2013-06-24 | 2014-12-09 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| WO2016118632A1 (fr) | 2015-01-20 | 2016-07-28 | The General Hospital Corporation | Prévention et traitement de prurit avec un antagoniste de mrgpr |
| KR20190040298A (ko) * | 2016-08-23 | 2019-04-17 | 뉴림 파머슈티칼스 리미티드 | 소양증 및/또는 가려움증의 치료방법 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH23995A (en) * | 1984-01-09 | 1990-02-09 | Janssen Pharmaceutica Nv | 4((bicycle heterocyclyl)-methyl and hetero)piperidines |
| US4839374A (en) * | 1984-01-09 | 1989-06-13 | Janssen Pharmaceutica, N.V. | 4-((Bicyclic heterocyclyl)-methyl and -hetero)-piperidines |
| GB8515934D0 (en) * | 1985-06-24 | 1985-07-24 | Janssen Pharmaceutica Nv | (4-piperidinomethyl and-hetero)purines |
| FR2605008B1 (fr) * | 1986-10-08 | 1988-12-02 | Synthelabo | Derives d'imidazo (4,5-b)pyridinone-2, leur preparation et leur application en therapeutique |
| US5071846A (en) * | 1987-07-01 | 1991-12-10 | Janssen Pharmaceutica N.V. | Anti-hystaminic [(bicyclic heterocyclyl) methyl and --hetero] substituted hexahydro-1H-azepines and pyrrolidines |
| US5151424A (en) * | 1987-07-01 | 1992-09-29 | Janssen Pharmaceutica N.V. | Pharmacologically active (Bicyclic heterocyclyl)methyl and -hetero) substituted hexahydro-1H-azepines and pyrrolidines |
| GB8900380D0 (en) * | 1989-01-09 | 1989-03-08 | Janssen Pharmaceutica Nv | 2-aminopyrimidinone derivatives |
| PH30434A (en) * | 1989-04-07 | 1997-05-09 | Janssen Pharmaceutica Nv | Hydroxyalkylfuranyl derivatives |
| JPH09502699A (ja) * | 1993-03-26 | 1997-03-18 | ベス、イスラエル、ホスピタル、アソシエーション | バスピロン又はその誘導体の局部的及び全身投与に依る免疫反応性病体の治療 |
| WO1995009167A1 (fr) * | 1993-09-30 | 1995-04-06 | Tokyo Tanabe Company Limited | Derive d'indoline et antagoniste du recepteur 5-ht3 contenant ce derive et utilise comme ingredient actif |
-
1994
- 1994-08-30 US US08/298,245 patent/US5521183A/en not_active Expired - Fee Related
-
1995
- 1995-08-25 WO PCT/US1995/010838 patent/WO1996006601A1/fr active Application Filing
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