JP5286254B2 - 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 - Google Patents

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 Download PDF

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JP5286254B2
JP5286254B2 JP2009511063A JP2009511063A JP5286254B2 JP 5286254 B2 JP5286254 B2 JP 5286254B2 JP 2009511063 A JP2009511063 A JP 2009511063A JP 2009511063 A JP2009511063 A JP 2009511063A JP 5286254 B2 JP5286254 B2 JP 5286254B2
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alkyl
salt
crystalline form
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JP2009537544A (ja
JP2009537544A5 (enExample
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タウフィーク ガルバウイ，
ディパンジャン セングプタ，
アッシュウィン エム． クリシュナン，
ナイネシュ シャー，
マーク マシアス，
ライアン エム． ハート，
エドワード エー． ラリー，
ジョナサン ジェイ． ダッフィールド，
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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
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
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  • Addiction (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2009511063A 2006-05-18 2007-05-17 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 Expired - Fee Related JP5286254B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US80178906P 2006-05-18 2006-05-18
US60/801,789 2006-05-18
US92131807P 2007-04-02 2007-04-02
US60/921,318 2007-04-02
PCT/US2007/011810 WO2007136689A2 (en) 2006-05-18 2007-05-17 Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor

Publications (3)

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JP2009537544A JP2009537544A (ja) 2009-10-29
JP2009537544A5 JP2009537544A5 (enExample) 2011-06-30
JP5286254B2 true JP5286254B2 (ja) 2013-09-11

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US (4) US8481535B2 (enExample)
EP (2) EP2018372B1 (enExample)
JP (1) JP5286254B2 (enExample)
KR (1) KR101514846B1 (enExample)
CN (1) CN102827081A (enExample)
AU (1) AU2007254255B2 (enExample)
BR (1) BRPI0712030A2 (enExample)
CA (1) CA2646081C (enExample)
EA (1) EA016675B1 (enExample)
ES (1) ES2543718T3 (enExample)
IL (2) IL193822A (enExample)
MX (2) MX2008014622A (enExample)
MY (1) MY154962A (enExample)
NZ (2) NZ571829A (enExample)
SG (1) SG171681A1 (enExample)
WO (1) WO2007136689A2 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ544331A (en) 2003-07-22 2010-03-26 Arena Pharm Inc Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
PE20061130A1 (es) 2004-11-19 2007-01-05 Arena Pharm Inc Derivados de 3-fenil-pirazol como moduladores del receptor de serotonina 5-ht2a
EP2027119A2 (en) 2006-05-18 2009-02-25 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
US8148417B2 (en) 2006-05-18 2012-04-03 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
NZ571829A (en) 2006-05-18 2011-10-28 Arena Pharm Inc Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor
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
ES2421237T7 (es) 2007-08-15 2013-09-30 Arena Pharmaceuticals, Inc. Derivados de imidazo[1,2-a]piridin como moduladores del receptor serotoninérgico 5ht2a en el tratamiento de trastornos relacionados con el mismo
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
TR201805216T4 (en) 2008-10-28 2018-06-21 Arena Pharm Inc COMPOSITIONS OF A USEFUL 5-HT2A SEROTONINE RECEPTOR MODULATOR FOR THE TREATMENT OF RELATED DISORDERS
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
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
EP2563759B1 (en) * 2010-04-27 2022-04-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
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
CN108472285A (zh) 2015-07-15 2018-08-31 阿速万科学有限责任公司 用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物

Family Cites Families (97)

* 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
AU3577995A (en) 1994-10-04 1996-04-26 Fujisawa Pharmaceutical Co., Ltd. Urea derivatives and their use as acat-inhibitors
NZ301265A (en) 1995-02-02 1998-12-23 Smithkline Beecham Plc Indole derivatives as 5ht receptor antagonists, preparation and pharmaceutical compositions thereof
JPH11503110A (ja) 1995-02-17 1999-03-23 スミスクライン・ビーチャム・コーポレイション Ｉｌ−８受容体拮抗剤
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
WO1997045111A1 (en) 1996-05-24 1997-12-04 Neurosearch A/S Phenyl derivatives useful as blockers of chloride channels
EP0906273B1 (en) 1996-05-24 2002-10-16 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
WO1997049286A1 (en) 1996-06-27 1997-12-31 Smithkline Beecham Corporation Il-8 receptor antagonists
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�.
JP2001512096A (ja) 1997-07-29 2001-08-21 スミスクライン・ビーチャム・コーポレイション Ｉｌ−８レセプターアンタゴニスト
DK1027328T3 (da) 1997-10-31 2006-11-13 Aventis Pharma Ltd Substituerede anilider
ATE291011T1 (de) 1997-12-22 2005-04-15 Bayer Pharmaceuticals Corp Hemmung der raf-kinase unter verwendung von symmetrisch und unsymmetrisch substituierten harnstoffen
DE69830513T2 (de) 1997-12-22 2006-03-16 Bayer Pharmaceuticals Corp., West Haven HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
US6107324A (en) 1998-04-14 2000-08-22 Arena Pharmaceuticals Inc. 5-HT2A receptor inverse agonists
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
EP1514867A3 (en) 1998-10-22 2005-03-23 NeuroSearch A/S 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
IL145508A0 (en) 1999-03-26 2002-06-30 Euro Celtique Sa Aryl substituted pyrazole, imidazole, oxazole, thiazole and pyrrole derivatives and pharmaceutical compositions containing the same
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
AU2002223492A1 (en) 2000-11-14 2002-05-27 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
US20020156068A1 (en) 2001-03-22 2002-10-24 Behan Dominic P. Anti-psychosis combination
DE10146119C1 (de) * 2001-09-19 2002-12-19 Krone Gmbh Zugentlastung für einen Steckverbinder in der Kommunikations- und Datentechnik
AU2002341693B2 (en) 2001-09-21 2008-05-29 Bristol-Myers Squibb Holdings Ireland Unlimited Company Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
EP1509505A2 (en) 2002-01-23 2005-03-02 Arena Pharmaceuticals, Inc. SMALL MOLECULE MODULATORS OF THE 5−HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
AU2003275093A1 (en) 2002-09-24 2004-04-19 Arena Pharmaceuticals, Inc. Process of making phenylpyrazoles useful as selective 5ht2a modulators and intermediates thereof
TWI258934B (en) 2002-11-08 2006-07-21 Interdigital Tech Corp Composite channel quality estimation techniques and systems for wireless receivers
WO2004058722A1 (en) 2002-12-24 2004-07-15 Arena Pharmaceuticals, Inc. 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
JP2006521345A (ja) 2003-03-28 2006-09-21 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 ニコチン性アセチルコリン受容体の正のアロステリック調節剤
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
NZ544331A (en) 2003-07-22 2010-03-26 Arena Pharm Inc Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
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
CN1926114B (zh) 2004-03-23 2011-08-24 艾尼纳制药公司 用于制备经取代n-芳基-n′-′3-(1h-吡唑-5-基)苯基脲及其中间体的方法
WO2006004722A2 (en) 2004-06-30 2006-01-12 Biomol Research Laboratories, Inc. Compositions and methods for selectively activating human sirtuins
US20080261952A1 (en) 2004-08-16 2008-10-23 Jason Bloxham Aryl Urea Derivatives for Treating Obesity
US20060063754A1 (en) 2004-09-21 2006-03-23 Edgar Dale M Methods of treating a sleep disorder
US7846915B2 (en) 2004-10-20 2010-12-07 Resverlogix Corporation Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
CA2575764A1 (en) 2004-10-27 2006-05-11 Neurogen Corporation Diaryl ureas as cb1 antagonists
US7563785B2 (en) 2004-10-29 2009-07-21 Hypnion, Inc. Quetiapine analogs and methods of use thereof
PE20061130A1 (es) * 2004-11-19 2007-01-05 Arena Pharm Inc Derivados de 3-fenil-pirazol como moduladores del receptor de serotonina 5-ht2a
GB0426313D0 (en) 2004-12-01 2005-01-05 Merck Sharp & Dohme Therapeutic agents
AR051978A1 (es) 2004-12-01 2007-02-21 Divergence Inc Composiciones plaguicidas y metodos
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
ES2465469T3 (es) 2005-01-14 2014-06-05 Gilead Connecticut, Inc. Diaril ureas 1,3-sustituidas como moduladores de la actividad quinasa
CA2594563A1 (en) 2005-01-19 2006-07-27 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
US7915249B2 (en) 2005-01-27 2011-03-29 Janssen Pharmaceutical 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
ATE461925T1 (de) 2005-04-26 2010-04-15 Hypnion Inc Benzisoxazolpiperidinverbindungen und verfahren zu deren anwendung
EP1734039A1 (en) 2005-06-13 2006-12-20 Esbatech AG Aryl urea compounds as BETA-secretase inhibitors
KR101363278B1 (ko) 2005-06-27 2014-02-21 엑셀리시스 페이턴트 컴퍼니 엘엘씨 이미다졸계 ｌｘｒ 변조제
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
TWI329641B (en) 2005-08-31 2010-09-01 Otsuka Pharma Co Ltd (benzo[b]thiophen-4-yl)piperazine compounds, pharmaceutical compositions comprising the same, uses of the same and processes for preparing the same
EP2004627A2 (en) 2006-04-10 2008-12-24 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
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
US8148417B2 (en) * 2006-05-18 2012-04-03 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
EP2027119A2 (en) * 2006-05-18 2009-02-25 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
NZ571829A (en) 2006-05-18 2011-10-28 Arena Pharm Inc Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor
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
ES2421237T7 (es) 2007-08-15 2013-09-30 Arena Pharmaceuticals, Inc. Derivados de imidazo[1,2-a]piridin como moduladores del receptor serotoninérgico 5ht2a en el tratamiento de trastornos relacionados con el mismo
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
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

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NZ571829A (en) 2011-10-28
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US20160272591A1 (en) 2016-09-22
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CA2646081A1 (en) 2007-11-29
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MX2008014622A (es) 2008-11-28
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