EP1509505A2 - Modulateurs a petites molecules du recepteur de serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associes - Google Patents
Modulateurs a petites molecules du recepteur de serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associesInfo
- Publication number
- EP1509505A2 EP1509505A2 EP03705889A EP03705889A EP1509505A2 EP 1509505 A2 EP1509505 A2 EP 1509505A2 EP 03705889 A EP03705889 A EP 03705889A EP 03705889 A EP03705889 A EP 03705889A EP 1509505 A2 EP1509505 A2 EP 1509505A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- phenyl
- methyl
- bromo
- pyrazol
- urea
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/16—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La présente invention concerne certains dérivés de pyrazole de formule (I) et leurs compositions pharmaceutiques qui modulent l'activité du récepteur de sérotonine 5-HT2A. L'invention concerne des composés et leurs compositions pharmaceutiques, utiles dans la prophylaxie ou le traitement visant à faire diminuer l'agrégation plaquettaire, la coronaropathie, l'infarctus du myocarde, l'accident ischémique transitoire, l'angine de poitrine, l'accident vasculaire cérébral, la fibrillation auriculaire, diminuant le risque de formation de caillots sanguins, l'asthme ou les symptômes associés, l'agitation ou un symptôme, les troubles du comportement, la psychose d'origine médicamenteuse, la psychose à forme d'état d'excitation, le syndrome de Gilles de la Tourette, le trouble maniaque, la psychose organique ou NSA, le trouble psychotique, la psychose, la schizophrénie aiguë, la schizophrénie chronique et la schizophrénie NSA et les troubles associés. La présente invention concerne également le procédé de prophylaxie ou de traitement de troubles induits par le récepteur de sérotonine 5-HT2A combiné à un antagoniste du récepteur D2 de dopamine tel que l'halopéridol, administré séparément ou ensemble.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38619802P | 2002-01-23 | 2002-01-23 | |
US386198P | 2002-01-23 | ||
US38638402P | 2002-06-05 | 2002-06-05 | |
US386384P | 2002-06-05 | ||
US40146702P | 2002-08-05 | 2002-08-05 | |
US401467P | 2002-08-05 | ||
PCT/US2003/002059 WO2003062206A2 (fr) | 2002-01-23 | 2003-01-23 | Modulateurs a petites molecules du recepteur de serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associes |
Publications (1)
Publication Number | Publication Date |
---|---|
EP1509505A2 true EP1509505A2 (fr) | 2005-03-02 |
Family
ID=27617596
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP03705889A Pending EP1509505A2 (fr) | 2002-01-23 | 2003-01-23 | Modulateurs a petites molecules du recepteur de serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associes |
Country Status (2)
Country | Link |
---|---|
EP (1) | EP1509505A2 (fr) |
WO (1) | WO2003062206A2 (fr) |
Families Citing this family (49)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE348808T1 (de) | 2000-03-06 | 2007-01-15 | Acadia Pharm Inc | Azacyclische verbindungen zur verwendung in der behandlung von mit serotonin verwandten krankheiten |
EP1461339B1 (fr) | 2001-12-28 | 2010-04-28 | Acadia Pharmaceuticals Inc. | Composes spiroazacycliques utilises comme modulateurs du recepteur de monoamine |
US7538222B2 (en) | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
CA2490397A1 (fr) | 2002-06-24 | 2003-12-31 | Acadia Pharmaceuticals Inc. | Derives de piperidine substitues en n en tant qu'agents recepteurs de la serotonine |
US7253186B2 (en) | 2002-06-24 | 2007-08-07 | Carl-Magnus Andersson | N-substituted piperidine derivatives as serotonin receptor agents |
GB0229618D0 (en) * | 2002-12-19 | 2003-01-22 | Cancer Rec Tech Ltd | Pyrazole compounds |
CN1816524B (zh) | 2003-01-16 | 2012-06-27 | 阿卡蒂亚药品公司 | 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂 |
JP2006522130A (ja) * | 2003-04-03 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換ピラゾール |
EP1695966A1 (fr) * | 2003-07-22 | 2006-08-30 | Arena Pharmaceuticals, Inc. | Dérivés diaryl et arylhétéroaryl de l'urée comme modulateurs du recepteur serotonin 5-HT2a, utiles pour la prophylaxe et le traitment des désordres associées |
DE602004000260T2 (de) * | 2003-07-22 | 2006-08-24 | Arena Pharmaceuticals, Inc., San Diego | Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen |
CA2559038C (fr) * | 2004-03-23 | 2013-09-10 | Arena Pharmaceuticals, Inc. | Methodes de preparation de n-aryl-n'-[3-(1h-pyrazol-5-yl) phenylurees] substituees et leurs intermediaires |
US7820695B2 (en) | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
EP2289879B1 (fr) | 2004-09-27 | 2014-11-12 | Acadia Pharmaceuticals Inc. | Synthèse d'une forme cristalline du sel de tartrate de n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide |
US7790899B2 (en) | 2004-09-27 | 2010-09-07 | Acadia Pharmaceuticals, Inc. | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
PE20061130A1 (es) * | 2004-11-19 | 2007-01-05 | Arena Pharm Inc | Derivados de 3-fenil-pirazol como moduladores del receptor de serotonina 5-ht2a |
US20080015223A1 (en) * | 2004-12-03 | 2008-01-17 | Arena Pharmaceuticals, Inc. | Pyrazole Derivatives as Modulators of the 5-Ht2a Serotonin Receptor Useful for the Treatment of Disorders Related Thereto |
CA2594563A1 (fr) * | 2005-01-19 | 2006-07-27 | Arena Pharmaceuticals, Inc. | Derives de diaryl-uree et d'arylheteroaryl-uree utilises comme modulateurs du recepteur de la serotonine 5-ht2a et utiles pour la prevention ou le traitement de la leucoencephalopathie multifocale progressive |
AR052886A1 (es) * | 2005-01-26 | 2007-04-11 | Arena Pharm Inc | Procedimientos para preparar fenilpirazol ureas sustituidas y para la obtencion de sus intermediarios de sintesis |
TWI370130B (en) | 2005-11-24 | 2012-08-11 | Eisai R&D Man Co Ltd | Two cyclic cinnamide compound |
TWI378091B (en) | 2006-03-09 | 2012-12-01 | Eisai R&D Man Co Ltd | Multi-cyclic cinnamide derivatives |
CA2646081C (fr) | 2006-05-18 | 2017-06-27 | Arena Pharmaceuticals, Inc. | Formes cristallines et procedes de preparation de phenylpyrazoles utiles en tant que modulateurs des recepteurs 5-ht2a de la serotonine |
EP3395816A1 (fr) * | 2006-05-18 | 2018-10-31 | Arena Pharmaceuticals, Inc. | Éthers, amines secondaires et leurs dérivés en tant que modulateurs du récepteur de la sérotonine 5-ht2a utiles pour le traitement de troubles associés |
ES2536762T3 (es) | 2006-05-18 | 2015-05-28 | Arena Pharmaceuticals, Inc. | Aminas primarias y sus derivados como moduladores del receptor de la serotonina 5-HT2A útiles para el tratamiento de trastornos relacionados con este |
EP2019093A4 (fr) * | 2006-05-19 | 2011-02-23 | Eisai R&D Man Co Ltd | Dérivé de cinnamide de type urée |
TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與5-ht2a血清素受體相關聯病症之作為5-ht2a血清素受體之調節劑的吡唑衍生物 |
TW200848054A (en) | 2007-02-28 | 2008-12-16 | Eisai R&D Man Co Ltd | Two cyclic oxomorpholine derivatives |
CA2681506C (fr) | 2007-03-19 | 2016-05-24 | Perry Peters | Combinaisons d'agonistes ou antagonistes inverses de 5-ht2a avec antipsychotiques |
WO2009023253A2 (fr) | 2007-08-15 | 2009-02-19 | Arena Pharmaceuticals Inc. | Dérivés d'imidazo[l,2-α]pyridine utilisés comme modulateurs du récepteur sérotoninergique 5-ht2a dans le traitement des troubles qui lui sont associés |
US7935815B2 (en) | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
MX2010002098A (es) | 2007-08-31 | 2010-03-30 | Eisai R&D Man Co Ltd | Compuesto policiclico. |
US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
ES2666324T3 (es) | 2008-10-28 | 2018-05-04 | Arena Pharmaceuticals, Inc. | Composiciones de un modulador del receptor de serotonina 5-HT2A útiles para el tratamiento de trastornos relacionados con el mismo |
WO2010062321A1 (fr) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Procédés utiles pour la préparation de 1-[3-(4-bromo-2-méthyl-2h-pyrazol-3-yl)-4-méthoxy-phényl]-3-(2,4-difluoro‑phényl)-urée, et formes cristallines associées |
US8980891B2 (en) | 2009-12-18 | 2015-03-17 | Arena Pharmaceuticals, Inc. | Crystalline forms of certain 3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto |
JP6155187B2 (ja) | 2010-03-30 | 2017-06-28 | ヴァーセオン コーポレイション | トロンビンの阻害剤としての多置換芳香族化合物 |
US9156837B2 (en) | 2011-07-29 | 2015-10-13 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
CN108354933A (zh) | 2013-03-15 | 2018-08-03 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物的制药用途 |
MX2015011567A (es) * | 2013-03-15 | 2016-04-25 | Verseon Corp | Halogeno-pirazoles como inhibidores de trombina. |
CA2960790A1 (fr) | 2014-09-17 | 2016-03-24 | Verseon Corporation | Composes de pyridone substituee par pyrazolyl en tant qu'inhibiteurs de serine protease |
LT3261639T (lt) | 2015-02-27 | 2022-11-25 | Verseon International Corporation | Pakaitiniai pirazolo junginiai kaip serino proteazės inhibitoriai |
JP2018516992A (ja) | 2015-06-12 | 2018-06-28 | アクソファント サイエンシーズ ゲーエムベーハーAxovant Sciences Gmbh | レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体 |
RU2018103338A (ru) | 2015-07-15 | 2019-08-15 | Аксовант Сайенсиз Гмбх | Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием |
PT3325444T (pt) | 2015-07-20 | 2021-09-22 | Acadia Pharm Inc | Métodos para preparar n-(4-fluorobenzil)-n-(1-metilpiperidina-4-il)-n'-(4-(2-metilpropiloxi)fenilmetil)carbamida e o seu sal de tartarato e forma polimórfica c |
US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
WO2017165635A1 (fr) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Association de pimavansérine et de modulateurs du cytochrome p450 |
EP3558311A1 (fr) | 2016-12-20 | 2019-10-30 | Acadia Pharmaceuticals Inc. | Pimavansérine seule ou en association pour une utilisation dans le traitement de la psychose liée à la maladie d'alzheimer |
EP3615028A1 (fr) | 2017-04-28 | 2020-03-04 | Acadia Pharmaceuticals Inc. | Pimavansérine pour le traitement d'un trouble de contrôle des impulsions |
US20210077479A1 (en) | 2017-08-30 | 2021-03-18 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
WO2023236920A1 (fr) * | 2022-06-07 | 2023-12-14 | Sironax Ltd. | Modulateurs de sarm1, leurs préparations et leurs utilisations |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5281571A (en) * | 1990-10-18 | 1994-01-25 | Monsanto Company | Herbicidal benzoxazinone- and benzothiazinone-substituted pyrazoles |
WO1998024785A1 (fr) * | 1996-12-02 | 1998-06-11 | Fujisawa Pharmaceutical Co., Ltd. | Derives d'indole-uree presentant des proprietes d'antagonistes de 5-ht |
AU764766B2 (en) * | 1998-04-14 | 2003-08-28 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof |
US20020156068A1 (en) * | 2001-03-22 | 2002-10-24 | Behan Dominic P. | Anti-psychosis combination |
-
2003
- 2003-01-23 EP EP03705889A patent/EP1509505A2/fr active Pending
- 2003-01-23 WO PCT/US2003/002059 patent/WO2003062206A2/fr not_active Application Discontinuation
Non-Patent Citations (1)
Title |
---|
See references of WO03062206A2 * |
Also Published As
Publication number | Publication date |
---|---|
WO2003062206A2 (fr) | 2003-07-31 |
WO2003062206A3 (fr) | 2004-01-08 |
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