HK1247555A1 - 用於預防和治療與神經變性疾病相關的幻覺的作為5-ht2a血清素受體的調節劑的二芳基脲和芳基雜芳基脲衍生物 - Google Patents

用於預防和治療與神經變性疾病相關的幻覺的作為5-ht2a血清素受體的調節劑的二芳基脲和芳基雜芳基脲衍生物

Info

Publication number
HK1247555A1
HK1247555A1 HK18106917.7A HK18106917A HK1247555A1 HK 1247555 A1 HK1247555 A1 HK 1247555A1 HK 18106917 A HK18106917 A HK 18106917A HK 1247555 A1 HK1247555 A1 HK 1247555A1
Authority
HK
Hong Kong
Prior art keywords
diaryl
prophylaxis
modulators
treatment
neurodegenerative disease
Prior art date
Application number
HK18106917.7A
Other languages
English (en)
Inventor
Lawrence Tim Friedhoff
Shankar Ramaswamy
Yandong Wen
Original Assignee
Axovant Sciences Gmbh
Lawrence Tim Friedhoff
Shankar Ramaswamy
Yandong Wen
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, Lawrence Tim Friedhoff, Shankar Ramaswamy, Yandong Wen filed Critical Axovant Sciences Gmbh
Publication of HK1247555A1 publication Critical patent/HK1247555A1/zh

Links

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
    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
HK18106917.7A 2015-07-15 2018-05-28 用於預防和治療與神經變性疾病相關的幻覺的作為5-ht2a血清素受體的調節劑的二芳基脲和芳基雜芳基脲衍生物 HK1247555A1 (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562192939P 2015-07-15 2015-07-15
US201562236618P 2015-10-02 2015-10-02
US201562261381P 2015-12-01 2015-12-01
PCT/US2016/042556 WO2017011767A2 (en) 2015-07-15 2016-07-15 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

Publications (1)

Publication Number Publication Date
HK1247555A1 true HK1247555A1 (zh) 2018-09-28

Family

ID=57757714

Family Applications (1)

Application Number Title Priority Date Filing Date
HK18106917.7A HK1247555A1 (zh) 2015-07-15 2018-05-28 用於預防和治療與神經變性疾病相關的幻覺的作為5-ht2a血清素受體的調節劑的二芳基脲和芳基雜芳基脲衍生物

Country Status (14)

Country Link
US (3) US10034859B2 (zh)
EP (1) EP3322415A4 (zh)
JP (2) JP2018520187A (zh)
KR (1) KR20180064373A (zh)
CN (1) CN108472285A (zh)
AU (1) AU2016291673A1 (zh)
BR (1) BR112018000728A2 (zh)
CA (1) CA2992518A1 (zh)
HK (1) HK1247555A1 (zh)
IL (1) IL256831A (zh)
MX (1) MX2018000465A (zh)
RU (1) RU2018103338A (zh)
TW (1) TW201720439A (zh)
WO (1) WO2017011767A2 (zh)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY141862A (en) 2003-07-22 2010-07-16 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
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
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
EP2364142B1 (en) 2008-10-28 2018-01-17 Arena Pharmaceuticals, Inc. Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto
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
EP3307260A4 (en) 2015-06-12 2019-02-13 Axovant Sciences GmbH DIARYL AND ARYLHETEROARYL UREA DERIVATIVES FOR PROPHYLAXIS AND TREATMENT OF SLEEP BEHAVIORAL DISORDERS IN THE REM PHASE
RU2018103338A (ru) 2015-07-15 2019-08-15 Аксовант Сайенсиз Гмбх Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием
EP3325444B1 (en) 2015-07-20 2021-07-07 Acadia Pharmaceuticals Inc. Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form 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
WO2017172757A1 (en) * 2016-03-29 2017-10-05 Acadia Pharmaceuticals Inc. 5-ht2a serotonin receptor inverse agonists or antagonists for use in reducing amyloid-beta peptides and accumulation of amyloid plaques
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
WO2019033068A1 (en) * 2017-08-10 2019-02-14 Axovant Sciences Gmbh USE OF INVERSE AGONISTS OF 5 HT2A FOR THE TREATMENT OF PSYCHOSES
US20210077479A1 (en) 2017-08-30 2021-03-18 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
US11622970B2 (en) 2020-04-28 2023-04-11 Prelude Therapeutics Incorporation BCL-2 inhibitors and their use as pharmaceuticals
WO2022061196A1 (en) * 2020-09-18 2022-03-24 Mydecine Innovations Group Inc. Novel formulations of psilocybin and psilocin compounds as serotonin agonists in combination with 3,4 methylenedioxymethamphetamine (mdma)
USD980157S1 (en) * 2021-02-26 2023-03-07 The Goodyear Tire & Rubber Company Tire

Family Cites Families (268)

* 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
WO2010037398A1 (en) 2008-10-03 2010-04-08 H. Lundbeck A/S Oral formulation
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
JPH04334357A (ja) 1991-05-02 1992-11-20 Fujirebio Inc 酵素阻害作用を有するアシル誘導体
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
DE69411176T2 (de) 1993-08-20 1998-11-12 Smithkline Beecham Plc Amide und harnstoffderivate als 5ht1d rezeptor antagonisten
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
AU3577995A (en) 1994-10-04 1996-04-26 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
HU223601B1 (hu) 1995-02-02 2004-10-28 Smithkline Beecham P.L.C. 5-HT receptor antagonista indolszármazékok
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
CA2218486A1 (en) 1995-04-20 1996-10-24 Vectorpharma - Eon N.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
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
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
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
WO1997045111A1 (en) 1996-05-24 1997-12-04 Neurosearch A/S Phenyl derivatives useful as blockers of chloride channels
CZ425698A3 (cs) 1996-06-27 1999-06-16 Smithkline Beecham Corporation Antagonista IL-8 receptoru
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
US6110498A (en) 1996-10-25 2000-08-29 Shire Laboratories, Inc. Osmotic drug delivery system
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
US20010051719A1 (en) 1996-12-19 2001-12-13 Smithkline Beecham P.L.C. Novel compounds
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
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
US6696475B2 (en) 1997-04-22 2004-02-24 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
NZ335822A (en) 1997-04-22 2001-05-25 Neurocrine Biosciences Inc Preparation and use of 2-methyl-4-dipropylamino-8(2',4'-dichlorophenyl)-quinoline and 2-methyl-4-(N-propyl-N-cyclopropanemethyl)amino-8(2',4'-dichlorophenyl)-quinoline for treating corticotropin-releasing factor related diseases
TR199902593T2 (xx) 1997-04-22 2000-03-21 Neurosearch A/S �kame edilmi� fenil t�revleri, bunlar�n haz�rlanmas� ve kullan�m�.
IL133009A0 (en) 1997-05-28 2001-03-19 Aventis Pharm Prod Inc Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
US6103905A (en) 1997-06-19 2000-08-15 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
KR20010014030A (ko) 1997-06-19 2001-02-26 더글라스이.리디치 퀴놀린-인돌 항균제, 이들의 용도 및 조성물
BR9810991A (pt) 1997-07-11 2000-08-08 Smithkline Beecham Plc Novos compostos
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
CA2294064A1 (en) 1997-07-29 1999-02-11 Smithkline Beecham Corporation Il-8 receptor antagonists
JP2001513563A (ja) 1997-08-27 2001-09-04 ヘキサル アーゲー 溶解性および生物学的利用能の改良されたメロキシカムの医薬組成物
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
ES2153809T3 (es) 1997-12-22 2005-07-16 Bayer Pharmaceuticals Corporation Inhibicion de la cinasa raf por uso de difnil-ureas sustituidas simetrica y asimetricamente.
CA2315715C (en) 1997-12-22 2010-06-22 Bayer Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
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
AU764766B2 (en) 1998-04-14 2003-08-28 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
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
GB9819384D0 (en) 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds II
GB9819382D0 (en) 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds I
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
BR9914638A (pt) 1998-10-22 2001-07-03 Neurosearch As Composto, método para a preparação do mesmo, composição farmacêutica, uso de um composto, e, método para o tratamento de um distúrbio ou doença de um corpo de animal vivo
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
DE60044395D1 (de) 1999-03-26 2010-06-24 Euro Celtique Sa Arylsubstituierte pyrazole, imidazole, oxazole, thiazole und pyrrole, sowie deren verwendung
US6413982B1 (en) 1999-03-29 2002-07-02 Neurogen Corporation 4-substituted quinoline derivatives
ES2291024T4 (es) 1999-04-21 2009-03-01 Nps Allelix Corp. Compuestos de piperidina-indol con afinidad con 5-ht6.
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
PL354998A1 (en) 1999-07-28 2004-03-22 Aventis Pharmaceuticals Products Inc. Substituted oxoazaheterocyclyl compounds
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
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
AU1542201A (en) 1999-11-05 2001-05-14 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
CA2395075A1 (en) 1999-12-16 2001-06-21 Miles P. Smith 1,3,4-substituted piperidine analogs and uses thereof in treating addictions
CA2397681C (en) 1999-12-20 2011-03-15 Neuromed Technologies, Inc. Partially saturated calcium channel blockers
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
ES2309095T3 (es) 2000-10-02 2008-12-16 Janssen Pharmaceutica Nv Antagonistas de los receptores metabotropicos de glutamato.
IL154685A0 (en) 2000-10-20 2003-09-17 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
CN1222511C (zh) 2000-11-02 2005-10-12 惠氏公司 作为5-羟色胺-6配体的1-芳基-或1-烷基磺酰基-杂环基吲哚
AU2002223492A1 (en) 2000-11-14 2002-05-27 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
JP2004517826A (ja) 2000-11-21 2004-06-17 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イソキノリン誘導体
AU2002220715A1 (en) 2000-11-24 2002-06-03 Smithkline Beecham Plc Indolsulfonyl compounds useful in the treatment of cns disorders
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
EP1351936A1 (en) 2001-01-15 2003-10-15 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
US20020156068A1 (en) 2001-03-22 2002-10-24 Behan Dominic P. Anti-psychosis combination
PL220721B1 (pl) 2001-03-29 2015-12-31 Lilly Co Eli Związki będące pochodnymi N-(indolilo-2-etylo) benzyloaminy, kompozycja farmaceutyczna oraz zastosowanie
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
ATE331707T1 (de) 2001-06-15 2006-07-15 Hoffmann La Roche 4 piperazinylindolderivate mit affinität zum 5- ht6-rezeptor
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.
DK1414414T3 (da) 2001-06-29 2008-03-03 Eurand Pharmaceuticals Ltd Fremgangsmåde til termodynamisk aktivering af vand-uoplöselige lægemidler hvormed tværbundne polymerer er ladet
US6565829B2 (en) 2001-08-03 2003-05-20 Pharmacia & Upjohn Company 5-arylsulfonyl indoles useful for treating disease
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
NZ530742A (en) 2001-08-10 2007-07-27 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
US20050020632A1 (en) 2001-08-31 2005-01-27 Dominique Grimler Optical isomers of an iloperidone metabolite
BRPI0212726B8 (pt) 2001-09-21 2021-05-25 Bristol Myers Squibb Co compostos contendo lactamas, e derivados dos mesmos, composição farmacêutica que os compreende e seus usos
DE60218194T2 (de) 2001-10-23 2007-10-31 Biovitrum Ab Verwendung von indol- und indolin-derivaten bei der behandlung von adipositas oder zur reduzierung der nahrungsaufnahme
SE0103649D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic quinoline compounds
EP1456178A1 (en) 2001-12-21 2004-09-15 Smithkline Beecham Plc 7-sulfonyl-3-benzazepine derivatives as modulators of the dopamine receptor and their use for the treatment of cns disorders
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
GB0202679D0 (en) 2002-02-05 2002-03-20 Glaxo Group Ltd Novel compounds
US20070270432A1 (en) 2002-02-05 2007-11-22 James Hagan Novel Method
ES2260607T3 (es) 2002-02-13 2006-11-01 Glaxo Group Limited Derivados de 7-arilsulfonamido-2,3,4,5-tetrahidro-1h-benzo-diazepina con afinidad por los receptores 5-ht6 para el tratamiento de trastornos del snc.
WO2003072558A2 (en) 2002-02-22 2003-09-04 Pharmacia & Upjohn Company Arylsulfone derivatives
DK1497266T3 (da) 2002-03-27 2008-10-06 Glaxo Group Ltd Quinolinderivater og deres anvendelse som 5HT6-ligander
DE60309852T2 (de) 2002-03-27 2007-06-06 Glaxo Group Ltd., Greenford Chinolin- und aza-indolderivate und deren verwendung als 5-ht6 liganden
PL211057B1 (pl) 2002-05-13 2012-04-30 Hoffmann La Roche Pochodne benzoksazyny, sposób ich wytwarzania, środek farmaceutyczny i zastosowanie pochodnych benzoksazyny
WO2004034963A2 (en) 2002-05-17 2004-04-29 Eisai Co., Ltd. Methods and compositions using cholinesterase inhibitors
KR100657056B1 (ko) 2002-06-05 2006-12-13 에프. 호프만-라 로슈 아게 중추 신경계 장애의 치료를 위한 5-ht6-수용체조절제로서 1-설폰일-4-아미노알콕시 인돌 유도체
JP4754821B2 (ja) 2002-06-20 2011-08-24 プロキシマゲン・リミテッド 肥満症、ii型糖尿病およびcns障害の治療に有用な新規化合物
MXPA04012914A (es) 2002-06-20 2005-03-31 Biovitrum Ab Nuevos compuestos utiles para el tratamiento de la obesidad, diabetes tipo ii y desordenes cns.
MXPA05002696A (es) 2002-09-17 2005-05-05 Hoffmann La Roche Indoles 2,7-sustituidos y su uso como moduladores de 5-hidroxitriptamina 6 (5-ht6).
JP4267573B2 (ja) 2002-09-17 2009-05-27 エフ.ホフマン−ラ ロシュ アーゲー 2,4−置換インドールおよびそれらの5−ht6モジュレーターとしての使用
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
WO2004035047A1 (en) 2002-10-18 2004-04-29 F. Hoffmann-La Roche Ag 4-piperazinyl benzenesulfonyl indoles with 5-ht6 receptor affinity
US7016330B2 (en) 2002-11-08 2006-03-21 Interdigital Technology Corporation Composite channel quality estimation techniques for wireless receivers
CN100390157C (zh) 2002-11-08 2008-05-28 弗·哈夫曼-拉罗切有限公司 取代的苯并嗪酮及其用途
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
RU2350602C2 (ru) 2002-12-03 2009-03-27 Ф.Хоффманн-Ля Рош Аг Аминоалкоксииндолы, как лиганды рецептора 5-нт6, для лечения заболеваний цнс
AU2003297441A1 (en) 2002-12-24 2004-07-22 Arena Pharmaceuticals, Inc. Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
US7601740B2 (en) * 2003-01-16 2009-10-13 Acadia Pharmaceuticals, Inc. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
US20040248850A1 (en) 2003-02-11 2004-12-09 Kemia, Inc. Compounds for the treatment of HIV infection
MXPA05008438A (es) 2003-02-14 2005-10-19 Wyeth Corp Heterociclil-3-sulfonilindazoles como ligandos de 5-hidroxitriptamina-6.
TW200418830A (en) 2003-02-14 2004-10-01 Wyeth Corp Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
EP1592389B1 (en) 2003-02-14 2009-04-22 Laboratoires Serono SA Piperazine-2-carboxamide derivatives
CA2517146A1 (en) 2003-03-03 2004-09-16 F. Hoffmann-La Roche Ag 2,5- and 2,6-substituted tetrahydroisoquinolines for use as 5-ht6 modulators
GB0305575D0 (en) 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
TWI289141B (en) 2003-03-11 2007-11-01 Hoffmann La Roche F. Ag. Quinolinone derivatives and uses thereof
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
SI1558582T1 (sl) 2003-07-22 2006-06-30 Arena Pharm Inc Diaril in arilheteroaril secninski derivati kot modulatorji 5-HT2A serotoninskega receptorja, koristnega za profilakso in zdravljenje motenj, ki so znjim povezane
MY141862A (en) 2003-07-22 2010-07-16 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
WO2005019167A2 (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
CA2559038C (en) 2004-03-23 2013-09-10 Arena Pharmaceuticals, Inc. Processes for preparing substituted n-aryl-n'-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof
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
BRPI0511874A (pt) 2004-06-09 2008-01-15 Glaxo Group Ltd derivados da pirrolopiridina
WO2006004722A2 (en) 2004-06-30 2006-01-12 Biomol Research Laboratories, Inc. 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
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
GB0422263D0 (en) 2004-10-07 2004-11-10 Glaxo Group Ltd Novel compounds
US8093273B2 (en) 2004-10-20 2012-01-10 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
JP2008518014A (ja) 2004-10-27 2008-05-29 ニューロゲン コーポレイション Cb1拮抗薬としてのジアリール尿素
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
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
US20080015223A1 (en) 2004-12-03 2008-01-17 Arena Pharmaceuticals, Inc. Pyrazole Derivatives as Modulators of the 5-Ht2a Serotonin Receptor Useful for the Treatment of Disorders Related Thereto
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
US7625931B2 (en) 2005-01-14 2009-12-01 Cgi Pharmaceuticals, Inc. Certain substituted diphenyl ureas, as modulators of kinase activity
WO2006078610A1 (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
US20060188569A1 (en) 2005-01-21 2006-08-24 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
EP1846415B1 (en) 2005-01-27 2012-08-01 Janssen Pharmaceutica NV Heterocyclic tetracyclic tetrahydrofuran derivatives as 5ht2 inhibitors in the treatment of cns disorders
GT200600042A (es) 2005-02-10 2006-09-27 Aventis Pharma Inc Compuestos de bis arilo y heteroarilo sustituido como antagonistas selectivos de 5ht2a
WO2006089871A2 (en) 2005-02-23 2006-08-31 Neurosearch A/S Diphenylurea derivatives useful as erg channel openers for the treatment of cardiac arrhythmias
AU2006218403A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
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
DE602006012650D1 (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
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
GB0519765D0 (en) 2005-09-28 2005-11-09 Glaxo Group Ltd Novel compounds
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
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
US20100226855A1 (en) 2006-03-02 2010-09-09 Spherics, Inc. Rate-Controlled Oral Dosage Formulations
WO2007120600A2 (en) 2006-04-10 2007-10-25 Arena Pharmaceuticals, Inc. 3-pyridinyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
GB0608655D0 (en) 2006-05-03 2006-06-14 Merck Sharp & Dohme Therapeutic Treatment
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
EP2018371B1 (en) 2006-05-18 2015-03-04 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
NZ594353A (en) 2006-05-18 2013-02-22 Arena Pharm Inc Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-HT2A serotonin receptor
AU2007254244C1 (en) 2006-05-18 2014-07-31 Arena Pharmaceuticals, Inc. 3-pyrazolyl-benzamide-4-ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
JP2009541423A (ja) 2006-06-23 2009-11-26 ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ コリンエステラーゼ阻害剤と5‐ht6レセプター親和性の化合物との組合せ
WO2008027483A1 (en) 2006-08-31 2008-03-06 Arena Pharmaceuticals, Inc. Benzofuran derivatives as modulators of the 5-ht2a 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
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
CN101679297B (zh) 2006-12-08 2012-01-11 埃克塞利希斯股份有限公司 Lxr和fxr调节剂
ES2389958T3 (es) 2007-03-21 2012-11-05 Glaxo Group Limited Uso de derivados de quinolina en el tratamiento del dolor
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
US20090082388A1 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals Inc. Co-administration of pimavanserin with other agents
WO2009074607A1 (en) 2007-12-12 2009-06-18 Glaxo Group Limited Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline
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
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
EP2364142B1 (en) 2008-10-28 2018-01-17 Arena Pharmaceuticals, Inc. Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto
GB201111712D0 (en) 2011-07-08 2011-08-24 Gosforth Ct Holdings Pty Ltd Pharmaceutical compositions
EP2763676B1 (en) 2011-10-03 2019-12-25 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
US9446037B2 (en) 2012-11-27 2016-09-20 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
AU2014360452C1 (en) * 2013-12-03 2019-05-16 Intra-Cellular Therapies, Inc. Novel methods
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
CA2985370A1 (en) 2015-05-07 2016-11-10 Axovant Sciences Gmbh Compositions and methods of treating a neurodegenerative disease
EP3307260A4 (en) 2015-06-12 2019-02-13 Axovant Sciences GmbH DIARYL AND ARYLHETEROARYL UREA DERIVATIVES FOR PROPHYLAXIS AND TREATMENT OF SLEEP BEHAVIORAL DISORDERS IN THE REM PHASE
RU2018103338A (ru) 2015-07-15 2019-08-15 Аксовант Сайенсиз Гмбх Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием
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
WO2019033068A1 (en) 2017-08-10 2019-02-14 Axovant Sciences Gmbh USE OF INVERSE AGONISTS OF 5 HT2A FOR THE TREATMENT OF PSYCHOSES

Also Published As

Publication number Publication date
WO2017011767A3 (en) 2017-04-06
TW201720439A (zh) 2017-06-16
JP2021185144A (ja) 2021-12-09
US10034859B2 (en) 2018-07-31
KR20180064373A (ko) 2018-06-14
JP2018520187A (ja) 2018-07-26
WO2017011767A2 (en) 2017-01-19
EP3322415A4 (en) 2019-03-13
US20190151287A1 (en) 2019-05-23
US20210177804A1 (en) 2021-06-17
CA2992518A1 (en) 2017-01-19
EP3322415A2 (en) 2018-05-23
IL256831A (en) 2018-03-29
AU2016291673A1 (en) 2018-01-25
RU2018103338A (ru) 2019-08-15
BR112018000728A2 (pt) 2018-09-04
MX2018000465A (es) 2018-09-17
US11304932B2 (en) 2022-04-19
CN108472285A (zh) 2018-08-31
US20170014385A1 (en) 2017-01-19
RU2018103338A3 (zh) 2019-08-15

Similar Documents

Publication Publication Date Title
HK1247555A1 (zh) 用於預防和治療與神經變性疾病相關的幻覺的作為5-ht2a血清素受體的調節劑的二芳基脲和芳基雜芳基脲衍生物
HK1255160A1 (zh) 取代的4-氮雜吲哚以及它們作為glun2b受體調節劑的用途
IL262654A (en) Pharmacy preparation
HRP20190024T1 (hr) Derivati hidroksialkil-piperazina kao modulatori receptora cxcr3
HK1247914A1 (zh) 作為毒蕈鹼性m1受體正向別構調節劑的氟吲哚衍生物
HK1232211A1 (zh) 二甲基吡啶胺衍生物及其醫藥用途
HK1257091A1 (zh) 茚烷衍生物作為mglur7調節劑
IL261780B (en) New immunobiological products
ZA201607353B (en) Bicyclic derivatives and pharmaceutical composition including the same