AU2007254255B2 - Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor - Google Patents

Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor Download PDF

Info

Publication number
AU2007254255B2
AU2007254255B2 AU2007254255A AU2007254255A AU2007254255B2 AU 2007254255 B2 AU2007254255 B2 AU 2007254255B2 AU 2007254255 A AU2007254255 A AU 2007254255A AU 2007254255 A AU2007254255 A AU 2007254255A AU 2007254255 B2 AU2007254255 B2 AU 2007254255B2
Authority
AU
Australia
Prior art keywords
compound
formula
salt
crystalline form
reacting
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.)
Ceased
Application number
AU2007254255A
Other languages
English (en)
Other versions
AU2007254255A1 (en
Inventor
Jonathan J. Duffield
Tawfik Gharbaoui
Ryan M. Hart
Ashwin M. Krishnan
Edward A. Lally
Mark Macias
Dipanjan Sengupta
Nainesh Shah
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Arena Pharmaceuticals Inc
Original Assignee
Arena Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Publication of AU2007254255A1 publication Critical patent/AU2007254255A1/en
Application granted granted Critical
Publication of AU2007254255B2 publication Critical patent/AU2007254255B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • A61P25/22—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2007254255A 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 Ceased AU2007254255B2 (en)

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 (2)

Publication Number Publication Date
AU2007254255A1 AU2007254255A1 (en) 2007-11-29
AU2007254255B2 true AU2007254255B2 (en) 2013-03-07

Family

ID=38590318

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007254255A Ceased AU2007254255B2 (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

Country Status (16)

Country Link
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
EP1558582B1 (en) 2003-07-22 2005-12-21 Arena Pharmaceuticals, 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
USRE45336E1 (en) 2006-05-18 2015-01-13 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
EA016675B1 (ru) 2006-05-18 2012-06-29 Арена Фармасьютикалз, Инк. Способы получения фенилпиразолов и кристаллическая форма производного фенилпиразола
WO2007136680A2 (en) 2006-05-18 2007-11-29 Arena Pharmaceuticals, Inc. 3-pyraz0lyl-benzamide-4-ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
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
US9567327B2 (en) 2007-08-15 2017-02-14 Arena Pharmaceuticals, Inc. Imidazo[1,2-a]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
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
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
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
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
EP2563759B1 (en) * 2010-04-27 2022-04-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
HK1245660A1 (zh) 2015-06-12 2018-08-31 Axovant Sciences Gmbh 有用於预防和治疗rem睡眠行为障碍的二芳基脲和芳基脲衍生物
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

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
FI973205L (fi) 1995-02-02 1997-10-01 Smithkline Beecham Plc Indolijohdannaisia 5-HT-reseptoriantagonisteina
EP0809492A4 (en) 1995-02-17 2007-01-24 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
WO1997003967A1 (en) 1995-07-22 1997-02-06 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
JP4073489B2 (ja) 1996-05-24 2008-04-09 ニューロサーチ・アクティーゼルスカブ 酸性基を有するフエニル誘導体、その製造方法及びそれをクロライドチャンネル遮断剤として使用する方法
PL330849A1 (en) 1996-06-27 1999-06-07 Smithkline Beecham Corp Antagonists of il-8 receptors
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
CN1118462C (zh) 1997-04-22 2003-08-20 神经研究公司 取代的苯基衍生物、其制备方法以及用途
AU8673198A (en) 1997-07-29 1999-02-22 Smithkline Beecham Corporation Il-8 receptor antagonists
NZ503407A (en) 1997-10-31 2002-08-28 Aventis Pharma Ltd Anilide derivatives useful for treating inflammatory diseases
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
EP1049664B1 (en) 1997-12-22 2005-03-16 Bayer Pharmaceuticals Corporation Inhibition of raf kinase using symmetrical and unsymmetrical substituted diphenyl ureas
WO1999032463A1 (en) 1997-12-22 1999-07-01 Bayer Corporation INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS
AU764766B2 (en) 1998-04-14 2003-08-28 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
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
SK5222001A3 (en) 1998-10-22 2002-05-09 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
ES2345921T3 (es) 1999-03-26 2010-10-06 Euro-Celtique S.A. Pirazoles, imidazoles, oxazoles, tiazoles y pirroles sustituidos con arilo y su uso.
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
DE10146119C1 (de) * 2001-09-19 2002-12-19 Krone Gmbh Zugentlastung für einen Steckverbinder in der Kommunikations- und Datentechnik
EP1427415B1 (en) 2001-09-21 2009-08-12 Brystol-Myers Squibb Company Lactam-containing compounds and derivatives thereof as factor xa inhibitors
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
AU2003275093A1 (en) 2002-09-24 2004-04-19 Arena Pharmaceuticals, Inc. Process of making phenylpyrazoles useful as selective 5ht2a modulators and intermediates thereof
WO2004045118A2 (en) 2002-11-08 2004-05-27 Interdigital Technology Corporation Composite channel quality estimation techniques for wireless receivers
WO2004058722A1 (en) 2002-12-24 2004-07-15 Arena Pharmaceuticals, Inc. Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
WO2004071426A2 (en) 2003-02-11 2004-08-26 Kemia Inc. Compounds for the treatment of viral infection
WO2004085433A2 (en) 2003-03-28 2004-10-07 Pharmacia & Upjohn Company Llc Positive allosteric modulators of the nicotinic acetylcholine receptor
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
EP1558582B1 (en) 2003-07-22 2005-12-21 Arena Pharmaceuticals, 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
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
CA2584485C (en) 2004-10-20 2013-12-31 Resverlogix Corp. Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
US20090239841A1 (en) 2004-10-27 2009-09-24 Hutchison Alan J Diaryl Ureas as CB1 Antagonists
WO2006049734A2 (en) 2004-10-29 2006-05-11 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
WO2006060654A2 (en) 2004-12-01 2006-06-08 Divergence, Inc. Pesticidal compositions and methods
GB0426313D0 (en) 2004-12-01 2005-01-05 Merck Sharp & Dohme Therapeutic agents
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
WO2006070394A1 (en) 2004-12-28 2006-07-06 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
CN101160127A (zh) 2005-01-19 2008-04-09 艾尼纳制药公司 用于预防或治疗进行性多灶性白质脑病而作为5-ht2a血清素受体调节剂的二芳基和芳基杂芳基脲衍生物
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
MX2007009092A (es) 2005-01-27 2007-09-12 Janssen Pharmaceutica Nv Derivados de tetrahidrofurano tetraciclicos heterociclicos como inhibidores de 5ht2 en el tratamiento de trastornos del sistema nervioso central.
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
ES2340066T3 (es) 2005-04-26 2010-05-28 Hypnion, Inc. Compuestos de benzisoxazol piperidina y procedimiento de uso de los mismos.
EP1734039A1 (en) 2005-06-13 2006-12-20 Esbatech AG Aryl urea compounds as BETA-secretase inhibitors
WO2007002563A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Imidazole based lxr modulators
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
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
WO2007136680A2 (en) 2006-05-18 2007-11-29 Arena Pharmaceuticals, Inc. 3-pyraz0lyl-benzamide-4-ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
USRE45336E1 (en) * 2006-05-18 2015-01-13 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
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
EA016675B1 (ru) 2006-05-18 2012-06-29 Арена Фармасьютикалз, Инк. Способы получения фенилпиразолов и кристаллическая форма производного фенилпиразола
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
US9567327B2 (en) 2007-08-15 2017-02-14 Arena Pharmaceuticals, Inc. Imidazo[1,2-a]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

Also Published As

Publication number Publication date
US20180186748A1 (en) 2018-07-05
IL222340A (en) 2014-05-28
WO2007136689A2 (en) 2007-11-29
KR101514846B1 (ko) 2015-04-23
HK1121453A1 (en) 2009-04-24
EA016675B1 (ru) 2012-06-29
MX349156B (es) 2017-07-14
EP2018372B1 (en) 2015-05-13
ES2543718T3 (es) 2015-08-21
US20100234380A1 (en) 2010-09-16
US20160272591A1 (en) 2016-09-22
EP2527329A1 (en) 2012-11-28
MX2008014622A (es) 2008-11-28
CN102827081A (zh) 2012-12-19
IL193822A (en) 2015-11-30
EA200870544A1 (ru) 2009-06-30
AU2007254255A1 (en) 2007-11-29
KR20090009244A (ko) 2009-01-22
WO2007136689A3 (en) 2008-01-10
SG171681A1 (en) 2011-06-29
US9199940B2 (en) 2015-12-01
BRPI0712030A2 (pt) 2012-01-03
JP5286254B2 (ja) 2013-09-11
US20130296321A1 (en) 2013-11-07
US9783502B2 (en) 2017-10-10
JP2009537544A (ja) 2009-10-29
CA2646081A1 (en) 2007-11-29
NZ571829A (en) 2011-10-28
EP2018372A2 (en) 2009-01-28
MY154962A (en) 2015-08-28
NZ594353A (en) 2013-02-22
CA2646081C (en) 2017-06-27
US8481535B2 (en) 2013-07-09

Similar Documents

Publication Publication Date Title
US9783502B2 (en) Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor
JP4740115B2 (ja) 置換ピラゾール
US7285554B2 (en) Pyrazole derivative
KR20210143803A (ko) Tead 전사인자의 신규한 소분자 저해제
KR20150061644A (ko) 지방산 신타아제 저해제로서의 히드로피롤로피롤 유도체
AU2009266756A1 (en) Triazole derivative or salt thereof
TW200536832A (en) Process for producing 5-hydroxy-4-thiomethylpyrazole compound
WO2012020738A1 (ja) 複素環化合物およびその用途
CN102361853A (zh) 甲苯胺磺酰胺及其用途
CN103360317B (zh) 双环取代吡唑酮偶氮类衍生物、其制备方法及用途
JP4833832B2 (ja) ピラゾール化合物
US20080200694A1 (en) Process for Making Phenoxy Benzamide Compounds
CN101479248A (zh) 用作5-ht2a血清素受体调节剂的苯基-吡唑的晶型和其制备方法
HK1177210A (en) Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor
HK1121453B (en) Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor
TW202411213A (zh) 用於治療trpm3介導病症之新型衍生物
CA3190593A1 (en) Urea derivatives as pyruvate kinase activators
EP3560927B1 (en) Azepine derivatives acting as 5-ht7 receptor modulators
JP2019116422A (ja) ［１−（４−｛３−［（２ｒ）−２−メチルピロリジン−１−イル］プロポキシ｝フェニル）−１ｈ−ピラゾール−４−イル］（モルホリン−４−イル）メタノンの結晶の製造方法
MXPA06009117A (en) Indazole derivatives and pharmaceutical compositions containing them

Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: ADD THE CO-INVENTOR DUFFIELD, JONATHAN J.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired