CN104761498B - 5‑ht2a血清素受体的调节剂 - Google Patents

5‑ht2a血清素受体的调节剂 Download PDF

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Publication number
CN104761498B
CN104761498B CN201510030389.9A CN201510030389A CN104761498B CN 104761498 B CN104761498 B CN 104761498B CN 201510030389 A CN201510030389 A CN 201510030389A CN 104761498 B CN104761498 B CN 104761498B
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compound
phenyl
methyl
yls
pyrazole
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Expired - Fee Related
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CN104761498A (zh
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布拉德利·蒂加登
丹尼斯·查普曼
马克·德凯尔
彼得·I·多莎
康拉德·费什廷吉
洪纳帕·贾亚库马尔
索尼娅·斯特拉-普莱内特
翠英·陈
徐静东
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Arena Pharmaceuticals Inc
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Arena Pharmaceuticals Inc
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    • 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
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201510030389.9A 2006-05-18 2007-05-17 5‑ht2a血清素受体的调节剂 Expired - Fee Related CN104761498B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US80169906P 2006-05-18 2006-05-18
US60/801,699 2006-05-18
CNA2007800148473A CN101479261A (zh) 2006-05-18 2007-05-17 3-吡唑基-苯甲酰胺-4-醚、其仲胺及其衍生物作为5-ht2a血清素受体的调节剂用于治疗与其相关的病症

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CNA2007800148473A Division CN101479261A (zh) 2006-05-18 2007-05-17 3-吡唑基-苯甲酰胺-4-醚、其仲胺及其衍生物作为5-ht2a血清素受体的调节剂用于治疗与其相关的病症

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CN104761498A CN104761498A (zh) 2015-07-08
CN104761498B true CN104761498B (zh) 2017-12-26

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CN201510030389.9A Expired - Fee Related CN104761498B (zh) 2006-05-18 2007-05-17 5‑ht2a血清素受体的调节剂
CN2013101857262A Pending CN103396412A (zh) 2006-05-18 2007-05-17 5-ht2a血清素受体的调节剂
CNA2007800148473A Pending CN101479261A (zh) 2006-05-18 2007-05-17 3-吡唑基-苯甲酰胺-4-醚、其仲胺及其衍生物作为5-ht2a血清素受体的调节剂用于治疗与其相关的病症

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CN2013101857262A Pending CN103396412A (zh) 2006-05-18 2007-05-17 5-ht2a血清素受体的调节剂
CNA2007800148473A Pending CN101479261A (zh) 2006-05-18 2007-05-17 3-吡唑基-苯甲酰胺-4-醚、其仲胺及其衍生物作为5-ht2a血清素受体的调节剂用于治疗与其相关的病症

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US (7) US8148418B2 (https=)
EP (2) EP2027119A2 (https=)
JP (2) JP5389642B2 (https=)
CN (3) CN104761498B (https=)
AU (1) AU2007254244C1 (https=)
CA (1) CA2646076C (https=)
WO (1) WO2007136680A2 (https=)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1558582E (pt) 2003-07-22 2006-05-31 Arena Pharm Inc Derivados de diaril- e aril-heteroaril-ureia como moduladores do receptor de serotonina 5-ht2a uteis para a profilaxia e tratamento de desordens relacionadas com o mesmo
CA2559038C (en) * 2004-03-23 2013-09-10 Arena Pharmaceuticals, Inc. Processes for preparing substituted n-aryl-n'-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof
SA05260357B1 (ar) * 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
CA2646076C (en) 2006-05-18 2015-06-30 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
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
JP5286254B2 (ja) 2006-05-18 2013-09-11 アリーナ ファーマシューティカルズ， インコーポレイテッド ５−ｈｔ２ａセロトニンレセプター活性のモジュレーターとして有用なフェニルピラゾールの結晶形態および調製方法
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
WO2009023253A2 (en) 2007-08-15 2009-02-19 Arena Pharmaceuticals Inc. IMIDAZO[L,2-α]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
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
WO2010062321A1 (en) 2008-10-28 2010-06-03 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
CN104739829B (zh) 2008-10-28 2018-11-06 艾尼纳制药公司 用于治疗5-ht2a5-羟色胺受体相关障碍的5-ht2a5-羟色胺受体调节剂组合物
WO2010130124A1 (zh) * 2009-05-12 2010-11-18 上海泺安医药技术有限公司 含砜基脂肪胺的制备新工艺及其新盐
CN101885694B (zh) * 2009-05-12 2014-05-14 上海泺安医药技术有限公司 一种含砜基脂肪胺及其盐的制备工艺
EP2269600A1 (en) * 2009-07-02 2011-01-05 Sanofi-Aventis Treatment of sleep disorders using eplivanserin in COPD patients
WO2011075596A1 (en) 2009-12-18 2011-06-23 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
KR20180011843A (ko) 2015-06-11 2018-02-02 바실리어 파마슈티카 인터내셔널 리미티드 유출-펌프 억제제 및 이의 치료적 용도
WO2016201373A1 (en) 2015-06-12 2016-12-15 Axovant Sciences Ltd. Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder
WO2017011767A2 (en) 2015-07-15 2017-01-19 Axovant Sciences Ltd. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease
GB2559500B (en) 2015-09-10 2022-02-23 American Science & Eng Inc Backscatter characterization using interlinearly adaptive electromagnetic x-ray scanning
EP3684463B1 (en) 2017-09-19 2025-05-14 Neuroenhancement Lab, LLC Method and apparatus for neuroenhancement
US11717686B2 (en) 2017-12-04 2023-08-08 Neuroenhancement Lab, LLC Method and apparatus for neuroenhancement to facilitate learning and performance
US11478603B2 (en) 2017-12-31 2022-10-25 Neuroenhancement Lab, LLC Method and apparatus for neuroenhancement to enhance emotional response
US12280219B2 (en) 2017-12-31 2025-04-22 NeuroLight, Inc. Method and apparatus for neuroenhancement to enhance emotional response
US11364361B2 (en) 2018-04-20 2022-06-21 Neuroenhancement Lab, LLC System and method for inducing sleep by transplanting mental states
CN113382683A (zh) 2018-09-14 2021-09-10 纽罗因恒思蒙特实验有限责任公司 改善睡眠的系统和方法
US11193898B1 (en) 2020-06-01 2021-12-07 American Science And Engineering, Inc. Systems and methods for controlling image contrast in an X-ray system
WO2022093849A1 (en) * 2020-10-27 2022-05-05 Arena Pharmaceuticals, Inc. Pyrimidine derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
US20240376090A1 (en) * 2020-10-27 2024-11-14 Arena Pharmaceuticals, Inc. Isoxazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disordered related thereto
WO2022147318A1 (en) * 2020-12-31 2022-07-07 Arena Pharmaceuticals, Inc. Methods of treatment
WO2024122617A1 (ja) * 2022-12-08 2024-06-13 塩野義製薬株式会社 セロトニン受容体結合活性を有する含窒素複素環および炭素環誘導体
WO2025121409A1 (ja) * 2023-12-07 2025-06-12 シオノギ－アプニメッド スリープ サイエンス、エルエルシー セロトニン受容体結合活性を有する含窒素芳香族複素環および芳香族炭素環誘導体

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062206A2 (en) * 2002-01-23 2003-07-31 Arena Pharmaceuticals, Inc. Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
US20050080124A1 (en) * 2003-07-22 2005-04-14 Bradley Teegarden Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto

Family Cites Families (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4099012A (en) 1975-08-28 1978-07-04 Ciba-Geigy Corporation 2-pyrazolyl-benzophenones
DE2926517A1 (de) 1979-06-30 1981-01-15 Beiersdorf Ag Substituierte 3-aryl-pyrazole und 5-aryl-isoxazole und verfahren zu ihrer herstellung
DE2928485A1 (de) 1979-07-14 1981-01-29 Bayer Ag Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen
US4985352A (en) 1988-02-29 1991-01-15 The Trustees Of Columbia University In The City Of New York DNA encoding serotonin 1C (5HT1c) receptor, isolated 5HT1c receptor, mammalian cells expressing same and uses thereof
US5661024A (en) * 1989-10-31 1997-08-26 Synaptic Pharmaceutical Corporation DNA encoding a human serotonic (5-HT2) receptor and uses thereof
US5077409A (en) 1990-05-04 1991-12-31 American Cyanamid Company Method of preparing bis-aryl amide and urea antagonists of platelet activating factor
US5128351A (en) 1990-05-04 1992-07-07 American Cyanamid Company Bis-aryl amide and urea antagonists of platelet activating factor
FR2682379B1 (fr) * 1991-10-09 1994-02-11 Rhone Poulenc Agrochimie Nouveaux phenylpyrazoles fongicides.
FR2690440B1 (fr) 1992-04-27 1995-05-19 Rhone Poulenc Agrochimie Arylpyrazoles fongicides.
US5905080A (en) * 1993-08-20 1999-05-18 Smithkline Beecham, P.L.C. Amide and urea derivatives as 5HT1D receptor antagonists
US5739135A (en) 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
FR2722369B1 (fr) 1994-07-13 1998-07-10 Rhone Poulenc Agrochimie Compositions fongicides a base de derives 3-phenyl-pyrazoles pour le traitement du materiel vegetal de multiplication, nouveaux derives 3-phenyl-pyrazoles et leurs applications fongicides
EP0784612A1 (en) 1994-10-04 1997-07-23 Fujisawa Pharmaceutical Co., Ltd. Urea derivatives and their use as acat-inhibitors
RO115522B1 (ro) * 1995-02-02 2000-03-30 Smithkline Beecham P.L.C. Derivaţi de indolină, procedee pentru prepararea acestora, compoziţii farmaceutice care îi conţin şi metodă de tratament
EP0809492A4 (en) * 1995-02-17 2007-01-24 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
AU6526896A (en) 1995-07-22 1997-02-18 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
US6054472A (en) 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US6005008A (en) 1996-02-16 1999-12-21 Smithkline Beecham Corporation IL-8 receptor antagonists
GB9607219D0 (en) 1996-04-04 1996-06-12 Smithkline Beecham Plc Novel compounds
AU2962297A (en) 1996-05-24 1998-01-05 Neurosearch A/S Phenyl derivatives useful as blockers of chloride channels
US6417393B1 (en) 1996-05-24 2002-07-09 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
CZ425698A3 (cs) 1996-06-27 1999-06-16 Smithkline Beecham Corporation Antagonista IL-8 receptoru
JP2001508767A (ja) 1996-12-02 2001-07-03 藤沢薬品工業株式会社 ５―ｈｔ拮抗作用を有するインドール―ウレア誘導体
US5760246A (en) * 1996-12-17 1998-06-02 Biller; Scott A. Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
US6541209B1 (en) * 1997-04-14 2003-04-01 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
US6696475B2 (en) * 1997-04-22 2004-02-24 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
TR199902593T2 (xx) 1997-04-22 2000-03-21 Neurosearch A/S �kame edilmi� fenil t�revleri, bunlar�n haz�rlanmas� ve kullan�m�.
CA2294064A1 (en) 1997-07-29 1999-02-11 Smithkline Beecham Corporation Il-8 receptor antagonists
BR9813331A (pt) 1997-10-31 2000-08-22 Aventis Pharma Ltd Composto, uso do mesmo, composição farmacêutica, processo para o tratamento de um paciente humano ou animal não humano que sofra ou esteja sujeito a condições que possam ser melhoradas pela administração de um inibidor da adesão celular mediada pela a4b1, e, resina
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
JP3887769B2 (ja) 1997-12-22 2007-02-28 バイエル コーポレイション 対称および非対称ジフェニル尿素を用いるｐ３８キナーゼの阻害
BR9814375A (pt) 1997-12-22 2002-05-21 Bayer Ag Inibição de raf cinase usando difenil uréias substituìdas simétricas e assimétricas
MXPA00010060A (es) 1998-04-14 2004-04-23 Arena Pharm Inc Receptores de serotonina humana constitutivamente activados, no endogenos y moduladores de molecula pequenos de los mismos.
US6140509A (en) * 1998-06-26 2000-10-31 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
GB9816263D0 (en) 1998-07-24 1998-09-23 Merck Sharp & Dohme Therapeutic agents
OA11665A (en) 1998-10-22 2004-12-08 Neurosearch As Substituted phenyl derivatives, their preparation and use.
US6150393A (en) 1998-12-18 2000-11-21 Arena Pharmaceuticals, Inc. Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
CA2368631A1 (en) 1999-03-26 2000-10-05 Euro-Celtique S.A. Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof
GB9909409D0 (en) 1999-04-24 1999-06-23 Zeneca Ltd Chemical compounds
WO2001021160A2 (en) 1999-09-23 2001-03-29 Axxima Pharmaceuticals Aktiengesellschaft Carboxymide and aniline derivatives as selective inhibitors of pathogens
US6531291B1 (en) 1999-11-10 2003-03-11 The Trustees Of Columbia University In The City Of New York Antimicrobial activity of gemfibrozil and related compounds and derivatives and metabolites thereof
EP1108720A1 (en) 1999-12-08 2001-06-20 Basf Aktiengesellschaft Herbicidal 2-Pyrazolyl-6-Aryloxy-Pyri(mi)dines
FR2810979B1 (fr) * 2000-06-29 2002-08-23 Adir Nouveaux derives de diphenyluree, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2002039987A2 (en) 2000-11-14 2002-05-23 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
AR035521A1 (es) 2000-12-22 2004-06-02 Lundbeck & Co As H Derivados de 3-indolina y composicion farmaceutica que los comprende
WO2002076464A1 (en) 2001-03-22 2002-10-03 Arena Pharmaceuticals, Inc. Anti-psychosis combination
CA2461202C (en) * 2001-09-21 2011-07-12 Donald Pinto Lactam-containing compounds and derivatives thereof as factor xa inhibitors
EP1562937A2 (en) * 2002-06-24 2005-08-17 Acadia Pharmaceuticals Inc. N-substituted piperidine derivatives as serotonin receptor agents
WO2004028450A2 (en) 2002-09-24 2004-04-08 Arena Pharmaceuticals, Inc. Process of making phenylpyrazoles useful as selective 5ht2a modulators and intermediates thereof
TW200735568A (en) 2002-11-08 2007-09-16 Interdigital Tech Corp Composite channel quality estimation techniques for wireless receivers
US20060229335A1 (en) * 2002-12-24 2006-10-12 Bradley Teegarden Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
US20040248850A1 (en) 2003-02-11 2004-12-09 Kemia, Inc. Compounds for the treatment of HIV infection
WO2004085433A2 (en) 2003-03-28 2004-10-07 Pharmacia & Upjohn Company Llc Positive allosteric modulators of the nicotinic acetylcholine receptor
DE10315571A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
US20050054691A1 (en) * 2003-08-29 2005-03-10 St. Jude Children's Research Hospital Carboxylesterase inhibitors
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
CA2559038C (en) 2004-03-23 2013-09-10 Arena Pharmaceuticals, Inc. Processes for preparing substituted n-aryl-n'-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof
US20060014705A1 (en) * 2004-06-30 2006-01-19 Howitz Konrad T Compositions and methods for selectively activating human sirtuins
JP2008509982A (ja) 2004-08-16 2008-04-03 プロシディオン・リミテッド アリール尿素誘導体
US20060063754A1 (en) 2004-09-21 2006-03-23 Edgar Dale M Methods of treating a sleep disorder
WO2006045010A2 (en) * 2004-10-20 2006-04-27 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
AU2005302669A1 (en) 2004-10-27 2006-05-11 Neurogen Corporation Diaryl ureas as CB1 antagonists
SA05260357B1 (ar) 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
GB0426313D0 (en) 2004-12-01 2005-01-05 Merck Sharp & Dohme Therapeutic agents
WO2006060654A2 (en) 2004-12-01 2006-06-08 Divergence, Inc. Pesticidal compositions and methods
WO2006060762A2 (en) 2004-12-03 2006-06-08 Arena Pharmaceuticals, Inc. Pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EP1831172B1 (en) 2004-12-28 2009-02-18 Council of Scientific and Industrial Research Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors
WO2006076592A1 (en) 2005-01-14 2006-07-20 Cgi Pharmaceuticals, Inc. 1,3 substituted diaryl ureas as modulators of kinase activity
EP1843762A1 (en) 2005-01-19 2007-10-17 Arena Pharmaceuticals, Inc. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis or treatment of progressive multifocal leukoencephalopathy
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
EP1846415B1 (en) 2005-01-27 2012-08-01 Janssen Pharmaceutica NV Heterocyclic tetracyclic tetrahydrofuran derivatives as 5ht2 inhibitors in the treatment of cns disorders
GT200600042A (es) 2005-02-10 2006-09-27 Aventis Pharma Inc Compuestos de bis arilo y heteroarilo sustituido como antagonistas selectivos de 5ht2a
WO2006089871A2 (en) 2005-02-23 2006-08-31 Neurosearch A/S Diphenylurea derivatives useful as erg channel openers for the treatment of cardiac arrhythmias
GB0504828D0 (en) 2005-03-09 2005-04-13 Merck Sharp & Dohme Therapeutic agents
GB0505437D0 (en) 2005-03-17 2005-04-20 Merck Sharp & Dohme Therapeutic agents
GB0505725D0 (en) 2005-03-19 2005-04-27 Merck Sharp & Dohme Therapeutic agents
TWI320783B (en) 2005-04-14 2010-02-21 Otsuka Pharma Co Ltd Heterocyclic compound
JP5049267B2 (ja) 2005-04-26 2012-10-17 ハイプニオン・インコーポレイテッド ベンズイソオキサゾールピペラジン化合物およびその使用方法
JP2008542742A (ja) * 2005-06-03 2008-11-27 ケンブリッジ エンタープライズ リミティッド バイオマーカー
EP1734039A1 (en) 2005-06-13 2006-12-20 Esbatech AG Aryl urea compounds as BETA-secretase inhibitors
US8703805B2 (en) 2005-06-27 2014-04-22 Exelixis Patent Company Llc Modulators of LXR
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
AR055203A1 (es) 2005-08-31 2007-08-08 Otsuka Pharma Co Ltd Derivados de benzotiofeno con propiedades antipsicoticas
WO2007120600A2 (en) 2006-04-10 2007-10-25 Arena Pharmaceuticals, Inc. 3-pyridinyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
GB0608655D0 (en) 2006-05-03 2006-06-14 Merck Sharp & Dohme Therapeutic Treatment
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
EP2051978A2 (en) 2006-05-18 2009-04-29 Arena Pharmaceuticals, Inc. Acetamide derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
JP5286254B2 (ja) 2006-05-18 2013-09-11 アリーナ ファーマシューティカルズ， インコーポレイテッド ５−ｈｔ２ａセロトニンレセプター活性のモジュレーターとして有用なフェニルピラゾールの結晶形態および調製方法
CA2646076C (en) 2006-05-18 2015-06-30 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
JP2010502618A (ja) 2006-08-31 2010-01-28 アリーナ ファーマシューティカルズ， インコーポレイテッド セロトニン５−ｈｔ２ａ受容体のモジュレータとしてのベンゾフラン誘導体
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
WO2008054748A2 (en) 2006-10-31 2008-05-08 Arena Pharmaceuticals, Inc. Indazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
WO2009023253A2 (en) 2007-08-15 2009-02-19 Arena Pharmaceuticals Inc. IMIDAZO[L,2-α]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
JP2009196349A (ja) 2008-01-25 2009-09-03 Canon Finetech Inc バーコード印刷装置およびバーコード印刷方法
WO2011075596A1 (en) 2009-12-18 2011-06-23 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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062206A2 (en) * 2002-01-23 2003-07-31 Arena Pharmaceuticals, Inc. Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
US20050080124A1 (en) * 2003-07-22 2005-04-14 Bradley Teegarden Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto

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