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MX2017016413A - Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamineto de un trastorno conductual del sueño rem. - Google Patents

Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamineto de un trastorno conductual del sueño rem.

Info

Publication number
MX2017016413A
MX2017016413A MX2017016413A MX2017016413A MX2017016413A MX 2017016413 A MX2017016413 A MX 2017016413A MX 2017016413 A MX2017016413 A MX 2017016413A MX 2017016413 A MX2017016413 A MX 2017016413A MX 2017016413 A MX2017016413 A MX 2017016413A
Authority
MX
Mexico
Prior art keywords
treatment
derivatives
arilheteroaril
diaril
profilaxis
Prior art date
Application number
MX2017016413A
Other languages
English (en)
Other versions
MX388281B (es
Inventor
Tim Friedhoff Lawrence
Ramaswamy Shankar
Wen Yandong
Original Assignee
Axovant Sciences Gmbh
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 Axovant Sciences Gmbh filed Critical Axovant Sciences Gmbh
Publication of MX2017016413A publication Critical patent/MX2017016413A/es
Publication of MX388281B publication Critical patent/MX388281B/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a ciertos derivados de pirazol de fórmula (I) y composiciones farmacéuticamente de los mismos, que modulan la actividad del receptor de serotonina 5-HT2a y sus usos para el tratamiento del trastorno conductual del sueño REM.
MX2017016413A 2015-06-12 2016-06-10 Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamiento de un trastorno conductual del sueño rem. MX388281B (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201562174983P 2015-06-12 2015-06-12
US201562194084P 2015-07-17 2015-07-17
US201562236562P 2015-10-02 2015-10-02
US201562263967P 2015-12-07 2015-12-07
US201662278198P 2016-01-13 2016-01-13
PCT/US2016/037090 WO2016201373A1 (en) 2015-06-12 2016-06-10 Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder

Publications (2)

Publication Number Publication Date
MX2017016413A true MX2017016413A (es) 2018-08-01
MX388281B MX388281B (es) 2025-03-11

Family

ID=57504273

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017016413A MX388281B (es) 2015-06-12 2016-06-10 Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamiento de un trastorno conductual del sueño rem.

Country Status (15)

Country Link
US (3) US10022355B2 (es)
EP (2) EP3307260A4 (es)
JP (2) JP2018516992A (es)
KR (1) KR20180022792A (es)
CN (1) CN109562085A (es)
AU (2) AU2016276966A1 (es)
CA (1) CA2989343A1 (es)
HK (1) HK1245660A1 (es)
IL (1) IL256231A (es)
MX (1) MX388281B (es)
NO (1) NO20180040A1 (es)
RU (1) RU2017145976A (es)
TW (1) TW201717939A (es)
WO (1) WO2016201373A1 (es)
ZA (1) ZA201800186B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9034911B2 (en) 2008-10-28 2015-05-19 Arena Pharmaceuticals, Inc. Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
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
MX388281B (es) * 2015-06-12 2025-03-11 Axovant Sciences Gmbh Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamiento de un trastorno conductual del sueño rem.
CA2992518A1 (en) 2015-07-15 2017-01-19 Axovant Sciences Gmbh 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
SI3325444T1 (sl) 2015-07-20 2021-11-30 Acadia Pharmaceuticals Inc. Postopki za pripravo N-(4-fluorobenzil)-N-(1-metilpiperidin-4-il)-N'- (4-(2-metilpropiloksi)fenilmetil)karbamida in njegove tartratne soli in polimorfne oblike C
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
WO2018118626A1 (en) * 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
WO2018148737A1 (en) * 2017-02-13 2018-08-16 Axovant Sciences Gmbh 5-ht2a serotonin receptor serotonin receptor inverse agonists useful for the prophylaxis and treatment of parkinsonian symptoms associated with a neurodegenerative disease
US11135211B2 (en) 2017-04-28 2021-10-05 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
US11478467B2 (en) 2017-05-04 2022-10-25 Sreenivasarao Vepachedu Targeted drug rescue with novel compositions, combinations, and methods thereof
EP3675827A1 (en) 2017-08-30 2020-07-08 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
US20220339143A1 (en) * 2019-09-13 2022-10-27 Takeda Pharmaceutical Company Limited Tak-925 for use in treating narcolepsy
CN116354925B (zh) * 2021-12-27 2025-09-09 江苏恩华药业股份有限公司 吡唑衍生物及其应用

Family Cites Families (263)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1643310A1 (de) 1966-12-29 1971-06-03 Dow Chemical Co 4-Alkyl-2,5-dimethoxy-alpha-methyl-phenaethylamin und seine pharmakologisch vertraeglichen Salze
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
US4366158A (en) 1979-11-30 1982-12-28 Burroughs Wellcome Co. 1-(8-Quinolyl)-2-pyrrolidone and its pharmaceutical compositions
IL61721A (en) 1980-12-16 1984-03-30 Blank Izhak Nitroglycerin preparations
US4555399A (en) 1983-11-18 1985-11-26 Key Pharmaceuticals, Inc. Aspirin tablet
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
IT1227626B (it) 1988-11-28 1991-04-23 Vectorpharma Int Farmaci supportati aventi velocita' di dissoluzione aumentata e procedimento per la loro preparazione
JPH02262627A (ja) 1988-12-08 1990-10-25 Japan Synthetic Rubber Co Ltd 有機非線形光学素子
EP0412798A3 (en) 1989-08-08 1992-07-01 Merck Sharp & Dohme Ltd. Substituted pyridines, their preparation, formulations and use in dementia
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.
GB9300147D0 (en) 1993-01-06 1993-03-03 Minnesota Mining & Mfg Photothermographic materials
GB9311790D0 (en) 1993-06-08 1993-07-28 Minnesota Mining & Mfg Photothermographic materials
JPH09504004A (ja) 1993-08-20 1997-04-22 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 5ht1dレセプター拮抗薬用アミドおよび尿素誘導体
US5596001A (en) 1993-10-25 1997-01-21 Pfizer Inc. 4-aryl-3-(heteroarylureido)quinoline derivatves
DK122693D0 (da) 1993-10-29 1993-10-29 Hempels Skibsfarve Fab J C Marin struktur
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
WO1996010559A1 (en) 1994-10-04 1996-04-11 Fujisawa Pharmaceutical Co., Ltd. Urea derivatives and their use as acat-inhibitors
CA2135253A1 (en) 1994-11-07 1996-05-08 Michael Dennis Compound screening based on a window of chemical-messenger-independent activity
US6540981B2 (en) 1997-12-04 2003-04-01 Amersham Health As Light imaging contrast agents
PL184490B1 (pl) 1995-02-02 2002-11-29 Smithkline Beecham Plc Nowe pochodne indolu jako antagonista receptora T
US5576338A (en) 1995-02-15 1996-11-19 Merck Frosst Canada, Inc. Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis
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
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU5658496A (en) 1995-04-20 1996-11-07 Vectorpharma International S.P.A. Composite with sodium starch glycolate as a support material and products thereof
US5861431A (en) 1995-06-07 1999-01-19 Iotek, Inc. Incontinence treatment
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
AUPN842196A0 (en) 1996-03-05 1996-03-28 Fujisawa Pharmaceutical Co., Ltd. New compound
GB9607219D0 (en) 1996-04-04 1996-06-12 Smithkline Beecham Plc Novel compounds
CA2255858C (en) 1996-05-24 2007-09-11 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
JP2000510862A (ja) 1996-05-24 2000-08-22 ニューロサーチ・アクティーゼルスカブ クロライドチャンネル遮断剤として有用なフエニル誘導体
BR9709938A (pt) 1996-06-27 1999-08-10 Smithkline Beecham Corp Antagonistas dos receptores de il-8
EP0932401A1 (en) 1996-07-01 1999-08-04 Sepracor, Inc. Methods and compositions for treating urinary incontinence using enantiomerically enriched (r,r)-glycopyrrolate
US6063808A (en) 1996-07-01 2000-05-16 Sepracor Inc. Methods and compositions for treating urinary incontinence using enantiomerically enriched (S,S)-glycopyrrolate
FR2750988B1 (fr) 1996-07-11 1998-09-18 Adir Nouveaux derives de 2-(1h)-quinoleinone, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP4863534B2 (ja) 1996-10-25 2012-01-25 スパーナス ファーマシューティカルズ インコーポレイテッド 可溶形態浸透用量送達システム
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
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
US20010051719A1 (en) 1996-12-19 2001-12-13 Smithkline Beecham P.L.C. Novel compounds
EP0867477B1 (de) 1997-03-25 2002-05-02 Ciba SC Holding AG Polycyclische Verbindungen
US6420541B1 (en) 1998-04-14 2002-07-16 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
US6541209B1 (en) 1997-04-14 2003-04-01 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
JP2002501492A (ja) 1997-04-22 2002-01-15 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Crfアンタゴニストのキノ−及びキナゾリン類
CA2285424A1 (en) 1997-04-22 1998-10-29 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
US6696475B2 (en) 1997-04-22 2004-02-24 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
ES2235331T3 (es) 1997-05-28 2005-07-01 Aventis Pharmaceuticals Inc Compuestos quinolina y quinoxalina que inhiben el factor de crecimiento derivado de plaquetas y/o tirosina quinasas p561ck.
US6103905A (en) 1997-06-19 2000-08-15 Sepracor, Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
US6172084B1 (en) 1997-06-19 2001-01-09 Sepracor, Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
US6376670B1 (en) 1997-06-19 2002-04-23 Sepracor Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
ATE296811T1 (de) 1997-07-11 2005-06-15 Smithkline Beecham Plc Sulfonamid-derivate als 5-ht6 receptor antagonisten und verfahren zu ihrer herstellung
US6028083A (en) 1997-07-25 2000-02-22 Hoechst Marion Roussel, Inc. Esters of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol
AU8673198A (en) 1997-07-29 1999-02-22 Smithkline Beecham Corporation Il-8 receptor antagonists
WO1999009988A1 (en) 1997-08-27 1999-03-04 Hexal Ag New pharmaceutical compositions of meloxicam with improved solubility and bioavailability
PL340261A1 (en) 1997-10-31 2001-01-29 Aventis Pharma Ltd Substituted amilides
JPH11183942A (ja) 1997-12-19 1999-07-09 Nippon Mitsubishi Oil Corp エレクトロクロミック素子
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
DE69829412T2 (de) 1997-12-22 2005-07-28 Bayer Pharmaceuticals Corp., West Haven Hemmung der raf-kinase unter verwendung von symmetrisch und unsymmetrisch substituierten harnstoffen
PT1042305E (pt) 1997-12-22 2005-10-31 Bayer Pharmaceuticals Corp Inibicao de quinase p38 utilizando difenilureias simetricas e assimetricas
GB9801392D0 (en) 1998-01-22 1998-03-18 Smithkline Beecham Plc Novel compounds
GB9803411D0 (en) 1998-02-18 1998-04-15 Smithkline Beecham Plc Novel compounds
US6100291A (en) 1998-03-16 2000-08-08 Allelix Biopharmaceuticals Inc. Pyrrolidine-indole compounds having 5-HT6 affinity
US6107324A (en) 1998-04-14 2000-08-22 Arena Pharmaceuticals Inc. 5-HT2A receptor inverse agonists
US6251893B1 (en) 1998-06-15 2001-06-26 Nps Allelix Corp. Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
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
GB9818916D0 (en) 1998-08-28 1998-10-21 Smithkline Beecham Plc Use
GB9819382D0 (en) 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds I
GB9819384D0 (en) 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds II
GB9820113D0 (en) 1998-09-15 1998-11-11 Merck Sharp & Dohme Therapeutic agents
US6358698B1 (en) 1998-10-07 2002-03-19 Acadia Pharmacueticals Inc. Methods of identifying inverse agonists of the serotonin 2A receptor
NZ510098A (en) 1998-10-22 2003-09-26 Neurosearch As Substituted phenyl derivatives, pharmaceuticals thereof and their use as blockers of the chloride channel
US6403808B1 (en) 1999-12-10 2002-06-11 Virginia Commonwealth University Selective 5-HT6 receptor ligands
US6150393A (en) 1998-12-18 2000-11-21 Arena Pharmaceuticals, Inc. Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
EP1147094A1 (en) 1999-01-15 2001-10-24 Novo Nordisk A/S Non-peptide glp-1 agonists
US6180138B1 (en) 1999-01-29 2001-01-30 Abbott Laboratories Process for preparing solid formulations of lipid-regulating agents with enhanced dissolution and absorption
BR0009322A (pt) 1999-03-26 2002-04-30 Euro Celtique Sa Pirazóis, imidazóis, oxazóis, tiazóis e pirróis substituìdos com arila e o uso dos mesmos
EP1165542B1 (en) 1999-03-29 2003-08-20 Neurogen Corporation 4-substituted quinoline derivatives as nk-3 and/or gaba(a) receptor ligands
ATE375990T1 (de) 1999-04-21 2007-11-15 Nps Allelix Corp Piperidin-indol derivate mit 5-ht6 affinität
GB9909409D0 (en) 1999-04-24 1999-06-23 Zeneca Ltd Chemical compounds
AU4802500A (en) 1999-04-26 2000-11-10 Neurogen Corporation 2-aminoquinolinecarboxamides: neurokinin receptor ligands
US6469006B1 (en) 1999-06-15 2002-10-22 Bristol-Myers Squibb Company Antiviral indoleoxoacetyl piperazine derivatives
IT1312115B1 (it) 1999-06-24 2002-04-04 Nicox Sa Composti amorfi e relative composizioni farmaceutiche
JP4829449B2 (ja) 1999-07-28 2011-12-07 アベンティス・ファーマスーティカルズ・インコーポレイテツド 置換オキソアザヘテロシクリル化合物
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
MY125942A (en) 1999-09-07 2006-09-29 Upjohn Co Aminoalkoxy carbazoles for the treatment of cns diseases
WO2001021160A2 (en) 1999-09-23 2001-03-29 Axxima Pharmaceuticals Aktiengesellschaft Carboxymide and aniline derivatives as selective inhibitors of pathogens
WO2001032660A1 (en) 1999-11-05 2001-05-10 Nps Allelix Corp. Compounds having 5-ht6 receptor antagonist activity
GB9926302D0 (en) 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
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
UA75055C2 (uk) 1999-11-30 2006-03-15 Пфайзер Продактс Інк. Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі
EP1108720A1 (en) 1999-12-08 2001-06-20 Basf Aktiengesellschaft Herbicidal 2-Pyrazolyl-6-Aryloxy-Pyri(mi)dines
US20020025967A1 (en) 1999-12-16 2002-02-28 Smith Miles P. N-alkylpiperdine analogs and uses thereof in treating addictions
JP2003518107A (ja) 1999-12-20 2003-06-03 ニューロメド テクノロジーズ, インコーポレイテッド 部分飽和カルシウムチャネルブロッカー
WO2001064676A2 (en) 2000-02-28 2001-09-07 Scios, Inc. INHIBITORS OF p38-α KINASE
US6310212B1 (en) 2000-03-28 2001-10-30 Neurogen Corporation 4-substituted quinoline derivatives
PE20020063A1 (es) 2000-06-20 2002-01-30 Upjohn Co Bis-arilsulfonas como ligandos del receptor de 5-ht
FR2810979B1 (fr) 2000-06-29 2002-08-23 Adir Nouveaux derives de diphenyluree, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
SE0002754D0 (sv) 2000-07-21 2000-07-21 Pharmacia & Upjohn Ab New pharmaceutical combination formulation and method of treatment with the combination
GB0021450D0 (en) 2000-08-31 2000-10-18 Smithkline Beecham Plc Novel compounds
US6576644B2 (en) 2000-09-06 2003-06-10 Bristol-Myers Squibb Co. Quinoline inhibitors of cGMP phosphodiesterase
GB0021885D0 (en) 2000-09-06 2000-10-18 Fujisawa Pharmaceutical Co New use
EP1332133B1 (en) 2000-10-02 2008-07-09 Janssen Pharmaceutica N.V. Metabotropic glutamate receptor antagonists
EP1326830A1 (en) 2000-10-20 2003-07-16 Biovitrum Ab 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy
DE10053813A1 (de) 2000-10-30 2002-05-08 Bayer Ag Neue Verwendung von Sulfonamiden
AU2002220051B2 (en) 2000-11-02 2007-05-24 Wyeth 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands
AU2002223492A1 (en) 2000-11-14 2002-05-27 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
EP1341783A1 (en) 2000-11-21 2003-09-10 Smithkline Beecham Plc Isoquinoline derivatives useful in the treatment of cns disorders
JP2004517072A (ja) 2000-11-24 2004-06-10 スミスクライン ビーチャム パブリック リミテッド カンパニー Cns障害の治療において有用な化合物
ES2188344B1 (es) 2000-11-29 2004-09-16 Laboratorios Vita, S.A. Compuestos derivados de benzotiofeno, su procedimiento de obtencion y utilizacion de los mismos.
AR035521A1 (es) 2000-12-22 2004-06-02 Lundbeck & Co As H Derivados de 3-indolina y composicion farmaceutica que los comprende
JP2004520347A (ja) 2001-01-15 2004-07-08 グラクソ グループ リミテッド Ldl−受容体発現のインデューサーとしてのアリールピペリジンおよびピペラジン誘導体
WO2002076464A1 (en) 2001-03-22 2002-10-03 Arena Pharmaceuticals, Inc. Anti-psychosis combination
DK1379239T3 (da) 2001-03-29 2008-01-07 Lilly Co Eli N(2-aryl-ethyl)-benzyl-aminer som antagonister af 5 HT6 receptoren
GB0111186D0 (en) 2001-05-08 2001-06-27 Smithkline Beecham Plc Novel compounds
DE60218037T2 (de) 2001-06-07 2007-08-23 F. Hoffmann-La Roche Ag Neue indolderivate mit affinität zum 5-ht6-rezeptor
BR0210411A (pt) 2001-06-15 2004-08-17 Hoffmann La Roche Derivados 4-piperazinilindol com afinidade para o receptor 5-ht6
ITRM20010356A1 (it) 2001-06-21 2002-12-23 Sigma Tau Ind Farmaceuti "5-alogeno derivati della triptamina utili come ligandi del recettore5-ht6 e/o 5-ht7 della serotonina.
ATE377413T1 (de) 2001-06-29 2007-11-15 Eurand Pharmaceuticals Ltd Verfahren für die thermodynamische aktivierung von wasserlöslichen arzneimitteln, die in vernetzten polymeren geladen sind
MXPA04001089A (es) 2001-08-03 2004-05-20 Upjohn Co 5-arilsulfonil indoles que tienen afinidad por el receptor de 5-ht.
JP2005527463A (ja) 2001-08-07 2005-09-15 スミスクライン ビーチャム パブリック リミテッド カンパニー Cns疾患を治療するための5−ht6受容体アフィニティーを有する3−アリールスルホニル−7−ピペラジニル−インドール、−ベンゾフランおよび−ベンゾチオフェン
IL159880A0 (en) 2001-08-10 2004-06-20 Hoffmann La Roche Arylsulfonyl derivatives with 5-ht6 receptor affinity
JP4733877B2 (ja) 2001-08-15 2011-07-27 富士通セミコンダクター株式会社 半導体装置
ES2370634T3 (es) 2001-08-31 2011-12-21 Novartis Ag Isómeros ópticos de un metabolito de iloperidona.
UA78232C2 (uk) 2001-09-21 2007-03-15 Брістол-Майерс Сквібб Компані Лактамвмісні сполуки та їх похідні як інгібітори фактора ха
JP2005506368A (ja) 2001-10-23 2005-03-03 ビオヴィトルム・アクチボラゲット 肥満の処置におけるまたは食物摂取の減少のためのインドールおよびインドリン誘導体の使用
SE0103649D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic quinoline compounds
JP2005518414A (ja) 2001-12-21 2005-06-23 スミスクライン ビーチャム パブリック リミテッド カンパニー ドーパミン受容体のモジュレーターとしての7−スルホニル−3−ベンゾアゼピン誘導体およびcns障害の治療のためのその使用
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
WO2003066056A1 (en) 2002-02-05 2003-08-14 Glaxo Group Limited Method of promoting neuronal growth
GB0202679D0 (en) 2002-02-05 2002-03-20 Glaxo Group Ltd Novel compounds
US20050090485A1 (en) 2002-02-13 2005-04-28 Bromidge Steven M. 7-Arylsulfonamido-2,3,4,5-tetrahydro-1h-benzo'diazepine derivatives with 5ht6 receptor affinity for the reatment of cns disorders
CA2476173A1 (en) 2002-02-22 2003-09-04 Ruth E. Tenbrink Arylsulfone derivatives
US6743864B2 (en) 2002-03-12 2004-06-01 Basell Poliolefine Italia S.P.A. Polyolefin compositions having high tenacity
PT1956004E (pt) 2002-03-27 2012-08-31 Glaxo Group Ltd Derivados de quinolina e sua utilização como ligandos 5-ht6
EP1497291B1 (en) 2002-03-27 2006-11-22 Glaxo Group Limited Quinoline and aza-indole derivatives and their use as 5-ht6 ligands
KR100636475B1 (ko) 2002-05-13 2006-10-18 에프. 호프만-라 로슈 아게 5-ht6 조절제로서 벤족사진 유도체 및 이의 용도
WO2004034963A2 (en) 2002-05-17 2004-04-29 Eisai Co., Ltd. Methods and compositions using cholinesterase inhibitors
JP4390698B2 (ja) 2002-06-05 2009-12-24 エフ.ホフマン−ラ ロシュ アーゲー Cns障害の処置のための5−ht6レセプターモジュレーターとしての1−スルホニル−4−アミノアルコキシインドール誘導体
NZ536600A (en) 2002-06-20 2007-08-31 Biovitrum Ab Substituted sulphone and sulphonamide compounds useful for the treatment of obesity, type II diabetes and CNS disorders
US7943639B2 (en) 2002-06-20 2011-05-17 Proximagen Limited Compounds
ATE362469T1 (de) 2002-09-17 2007-06-15 Hoffmann La Roche 2,7-disubstituierteindole und ihre verwendung als 5-ht6 modulatoren
CA2498946A1 (en) 2002-09-17 2004-04-01 F. Hoffmann-La Roche Ag 2,4-substituted indoles and their use as 5-ht6 modulators
AU2003275093A1 (en) 2002-09-24 2004-04-19 Arena Pharmaceuticals, Inc. Process of making phenylpyrazoles useful as selective 5ht2a modulators and intermediates thereof
US7635709B2 (en) 2002-09-26 2009-12-22 The United States Of America As Represented By The Department Of Veterans Affairs Compositions and methods for bowel care in individuals with chronic intestinal pseudo-obstruction
PL376479A1 (en) 2002-10-18 2005-12-27 F.Hoffmann-La Roche Ag 4-piperazinyl benzenesulfonyl indoles with 5-ht6 receptor affinity
KR100683361B1 (ko) 2002-11-08 2007-02-15 에프. 호프만-라 로슈 아게 치환된 벤즈옥사진온 및 그의 용도
TWI258934B (en) 2002-11-08 2006-07-21 Interdigital Tech Corp Composite channel quality estimation techniques and systems for wireless receivers
JPWO2004046110A1 (ja) 2002-11-15 2006-03-16 アステラス製薬株式会社 メラニン凝集ホルモン受容体拮抗剤
TWI284124B (en) 2002-12-03 2007-07-21 Hoffmann La Roche Aminoalkoxyindoles
US20060229335A1 (en) 2002-12-24 2006-10-12 Bradley Teegarden Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
EP1594512A4 (en) 2003-02-11 2007-07-11 Kemia Inc COMPOUNDS FOR THE TREATMENT OF VIRUS INFECTIONS
MXPA05008441A (es) 2003-02-14 2005-10-19 Wyeth Corp Derivados de heterociclil-3-sulfonilindazol o azaindazol como ligandos de 5-hidroxitriptamina-6.
KR20050101551A (ko) 2003-02-14 2005-10-24 와이어쓰 5-하이드록시트립타민-6 리간드로서의헤테로사이클릴-3-설포닐인다졸
ES2324535T3 (es) 2003-02-14 2009-08-10 Merck Serono Sa Derivados de la piperazina-2-carboxamida.
EP1601358B1 (en) 2003-03-03 2007-12-19 F. Hoffmann-La Roche Ag 2,5-substituted tetrahydroisoquinolines for use as 5-ht6 modulators
TWI289141B (en) 2003-03-11 2007-11-01 Hoffmann La Roche F. Ag. Quinolinone derivatives and uses thereof
GB0305575D0 (en) 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
EP1611128A2 (en) 2003-03-28 2006-01-04 Pharmacia & Upjohn Company LLC Positive allosteric modulators of the nicotinic acetylcholine receptor
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
PL1558582T3 (pl) 2003-07-22 2006-05-31 Arena Pharm Inc Diarylowe i aryloheteroarylowe pochodne mocznika jako modulatory receptora serotoninowego 5-HT2A użyteczne w profilaktyce i w leczeniu zaburzeń związanych z tym receptorem
EP1695966A1 (en) 2003-07-22 2006-08-30 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
AU2004266233A1 (en) 2003-08-13 2005-03-03 Amgen, Inc. Melanin concentrating hormone receptor antagonist
US7091236B1 (en) 2003-08-20 2006-08-15 Sciele Pharma, Inc. Method for increasing the bioavailability of glycopyrrolate
GB0320320D0 (en) 2003-08-29 2003-10-01 Glaxo Group Ltd Novel compounds
US20050054691A1 (en) 2003-08-29 2005-03-10 St. Jude Children's Research Hospital Carboxylesterase inhibitors
WO2005021545A1 (en) 2003-09-03 2005-03-10 Galapagos Nv IMIDAZO[1,5-a]PYRIDINE OR IMIDAZO[1,5-a]PIPERIDINE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEDICAMENT AGAINST 5-HT2A RECEPTOR-RELATED DISORDERS
GB0321473D0 (en) 2003-09-12 2003-10-15 Glaxo Group Ltd Novel compounds
GB0322510D0 (en) 2003-09-25 2003-10-29 Glaxo Group Ltd Novel compounds
PT1667975E (pt) 2003-09-26 2008-02-29 Glaxo Group Ltd Forma polimórfica de 3-fenilsulfonil-8-piperazin-1-il-quinolina
SE0302760D0 (sv) 2003-10-20 2003-10-20 Biovitrum Ab New compounds
WO2005066157A1 (en) 2004-01-02 2005-07-21 Suven Life Sciences 3-(pyrolidin-3-l) indoles as 5-ht6 receptor modulators
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
US20070293539A1 (en) 2004-03-18 2007-12-20 Lansbury Peter T Methods for the treatment of synucleinopathies
ATE548353T1 (de) 2004-03-23 2012-03-15 Arena Pharm Inc Verfahren zur herstellung von substituierte n- aryl-n'-ä3-(1h-pyrazol-5-yl)phenylü-harnstoffe and intermediate davon.
GB0407025D0 (en) 2004-03-29 2004-04-28 Glaxo Group Ltd Novel compounds
GB0411421D0 (en) 2004-05-21 2004-06-23 Glaxo Group Ltd Novel compounds
TW200611695A (en) 2004-06-09 2006-04-16 Glaxo Group Ltd Pyrrolopyridine derivatives
US20060014705A1 (en) 2004-06-30 2006-01-19 Howitz Konrad T Compositions and methods for selectively activating human sirtuins
TW200616608A (en) 2004-07-09 2006-06-01 Forest Laboratories Memantine as adjunctive treatment to atypical antipsychotics in schizophrenia patients
US20060172992A1 (en) 2004-08-13 2006-08-03 Eisai Co., Ltd. Therapeutic agent for overactive bladder resulting from cerebral infarction
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
GB0422263D0 (en) 2004-10-07 2004-11-10 Glaxo Group Ltd Novel compounds
EP1838296B1 (en) 2004-10-20 2012-08-08 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
WO2006049941A2 (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
KR101358078B1 (ko) 2004-11-01 2014-02-06 주식회사 유스팜인터내셔널 근위축성 측삭 경화증의 신경퇴행을 감소시키기 위한 방법및 조성물
GB0425548D0 (en) 2004-11-19 2004-12-22 Glaxo Group Ltd Radiolabelled ligands
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
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
DE102004061593A1 (de) 2004-12-21 2006-06-22 Abbott Gmbh & Co. Kg Substituierte N-heterocyclische Verbindungen und ihre therapeutische Verwendung
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
WO2006078948A2 (en) 2005-01-21 2006-07-27 Teva Pharmaceutical Industries Ltd. Stable pharmaceutical formulations of zonisamide and methods for their manufacture
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
ES2391780T3 (es) 2005-01-27 2012-11-29 Janssen Pharmaceutica Nv Derivados de tetrahidrofurano tetracíclicos como inhibidores de 5HT2 en el tratamiento de trastornos de SNC
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
DK1877390T3 (da) 2005-04-26 2010-05-31 Hypnion Inc Benzisoxazol-piperazin-forbindelser og fremgangsmåder til anvendelse deraf
EP1734039A1 (en) 2005-06-13 2006-12-20 Esbatech AG Aryl urea compounds as BETA-secretase inhibitors
ES2525217T3 (es) 2005-06-27 2014-12-19 Exelixis Patent Company Llc Moduladores de LXR basados en imidazol
US7754724B2 (en) 2005-06-30 2010-07-13 Dow Agrosciences Llc N-substituted piperazines
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US7544685B2 (en) 2005-08-17 2009-06-09 H. Lundbeck A/S 2,3-dihydroindole compounds
AR055203A1 (es) 2005-08-31 2007-08-08 Otsuka Pharma Co Ltd Derivados de benzotiofeno con propiedades antipsicoticas
GB0519760D0 (en) 2005-09-28 2005-11-09 Glaxo Group Ltd Novel compounds
GB0519758D0 (en) 2005-09-28 2005-11-09 Glaxo Group Ltd Novel process
GB0519765D0 (en) 2005-09-28 2005-11-09 Glaxo Group Ltd Novel compounds
US20090053306A1 (en) 2005-09-29 2009-02-26 Agarwal Rajesh K Pharmaceutical Compositions of a 5-HT2A Serotonin Receptor Modulator Useful for the Treatment of Disorders Related Thereto
PE20071143A1 (es) 2006-01-13 2008-01-20 Wyeth Corp Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6
WO2007103286A2 (en) 2006-03-02 2007-09-13 Spherics, Inc. Rate-controlled bioadhesive oral dosage formulations
JP2009533442A (ja) 2006-04-10 2009-09-17 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セロトニン受容体関連障害の治療のために有用な5−ht2aセロトニン受容体のモジュレータとしての3−ピリジニル−ピラゾール誘導体
GB0608655D0 (en) 2006-05-03 2006-06-14 Merck Sharp & Dohme Therapeutic Treatment
JP2009537556A (ja) 2006-05-18 2009-10-29 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に関連する障害の処置に有用な5−ht2aセロトニンレセプターのモジュレーターとしてのアセトアミド誘導体
USRE45337E1 (en) 2006-05-18 2015-01-13 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
EA016675B1 (ru) 2006-05-18 2012-06-29 Арена Фармасьютикалз, Инк. Способы получения фенилпиразолов и кристаллическая форма производного фенилпиразола
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
US20100120747A1 (en) 2006-06-23 2010-05-13 Laboratorios Del Dr. Esteve, S.A. Combination of a cholinesterase inhibitor and a compound with 5-ht6 receptor affinity
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
TW200823204A (en) 2006-10-17 2008-06-01 Arena Pharm Inc Biphenyl sulfonyl and phenyl-heteroaryl sulfonyl modulators of the histamine H3-receptor useful for the treatment of disorders related thereto
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
US8097633B2 (en) 2006-11-15 2012-01-17 Rich Steven A Uses for quaternary ammonium anticholinergic muscarinic receptor antagonists in patients being treated for cognitive impairment or acute delirium
US8969402B2 (en) 2006-11-15 2015-03-03 Steven A. Rich Combined acetylcholinesterase inhibitor and quaternary ammonium antimuscarinic therapy to alter progression of cognitive diseases
US9034890B2 (en) 2006-11-15 2015-05-19 Steven A. Rich Combined acetylcholinesterase inhibitor and quaternary ammonium antimuscarinic therapy to alter progression of cognitive diseases
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
US20100041672A1 (en) 2007-03-21 2010-02-18 Glaxo Group Limited Use of quinoline derivatives in the treatment of pain and irritable bowel syndrome
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
WO2009039460A2 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Co-administration of pimavanserin with other agents
US9084742B2 (en) 2007-12-12 2015-07-21 Axovant Sciences Ltd. Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-Quinoline
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
CN102170884A (zh) 2008-10-03 2011-08-31 H.隆德贝克有限公司 口服制剂
US9034911B2 (en) 2008-10-28 2015-05-19 Arena Pharmaceuticals, Inc. Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
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
GB201111712D0 (en) 2011-07-08 2011-08-24 Gosforth Ct Holdings Pty Ltd Pharmaceutical compositions
EP3718547A1 (en) 2011-10-03 2020-10-07 The University of Utah Research Foundation Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
MX2014015266A (es) 2012-06-11 2015-06-23 Psychogenics Inc Tratamiento de efectos secundarios de trastorno motriz y del movimiento asociados con tratamientos de enfermedad de parkinson.
JO3459B1 (ar) 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
JOP20210047A1 (ar) 2012-10-25 2017-06-16 Otsuka Pharma Co Ltd عامل وقائي و/أو علاجي للأعراض السلوكية والنفسية المصحوبة بمرض تنكسي عصبي أو الأعراض الإندفاعية المصحوبة بمرض ذهني، يحتوي على بريكسبيرازول أو ملحه
WO2014085362A1 (en) 2012-11-27 2014-06-05 Acadia Pharmaceuticals Inc. Methods for the treatment of parkinson's disease psychosis using pimavanserin
KR101472682B1 (ko) 2013-07-23 2014-12-15 고려대학교 산학협력단 메타물질 제조 방법, 이에 의해 제조된 메타물질 구조 필름 및 이를 이용한 광학 이미징 시스템
US9478471B2 (en) 2014-02-19 2016-10-25 Taiwan Semiconductor Manufacturing Company, Ltd. Apparatus and method for verification of bonding alignment
US20150313903A1 (en) * 2014-05-05 2015-11-05 Ovid Therapeutics Inc. Methods of treating cognitive impairment associated with neurodegenerative disorders
US20160324851A1 (en) 2015-05-07 2016-11-10 Axovant Sciences, Ltd. Methods of treating a neurodegenerative disease
JP2018515607A (ja) 2015-05-07 2018-06-14 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 神経変性疾患を処置する組成物および方法
MX388281B (es) * 2015-06-12 2025-03-11 Axovant Sciences Gmbh Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamiento de un trastorno conductual del sueño rem.
CA2992518A1 (en) 2015-07-15 2017-01-19 Axovant Sciences Gmbh 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

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