CN108472285A - 用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物 - Google Patents

用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物 Download PDF

Info

Publication number
CN108472285A
CN108472285A CN201680050628.XA CN201680050628A CN108472285A CN 108472285 A CN108472285 A CN 108472285A CN 201680050628 A CN201680050628 A CN 201680050628A CN 108472285 A CN108472285 A CN 108472285A
Authority
CN
China
Prior art keywords
hallucinations
dementia
group
disease
treatment
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201680050628.XA
Other languages
English (en)
Chinese (zh)
Inventor
劳伦斯·蒂姆·弗里德霍夫
尚卡尔·拉马斯瓦米
文延东
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sio Gene Therapies Inc
Original Assignee
Axovant Sciences Ltd
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 Ltd filed Critical Axovant Sciences Ltd
Publication of CN108472285A publication Critical patent/CN108472285A/zh
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic 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
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (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)
CN201680050628.XA 2015-07-15 2016-07-15 用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物 Pending CN108472285A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201562192939P 2015-07-15 2015-07-15
US62/192,939 2015-07-15
US201562236618P 2015-10-02 2015-10-02
US62/236,618 2015-10-02
US201562261381P 2015-12-01 2015-12-01
US62/261,381 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
CN108472285A true CN108472285A (zh) 2018-08-31

Family

ID=57757714

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680050628.XA Pending CN108472285A (zh) 2015-07-15 2016-07-15 用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物

Country Status (14)

Country Link
US (3) US10034859B2 (enExample)
EP (1) EP3322415A4 (enExample)
JP (2) JP2018520187A (enExample)
KR (1) KR20180064373A (enExample)
CN (1) CN108472285A (enExample)
AU (1) AU2016291673A1 (enExample)
BR (1) BR112018000728A2 (enExample)
CA (1) CA2992518A1 (enExample)
HK (1) HK1247555A1 (enExample)
IL (1) IL256831A (enExample)
MX (1) MX391031B (enExample)
RU (1) RU2018103338A (enExample)
TW (1) TW201720439A (enExample)
WO (1) WO2017011767A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116354925A (zh) * 2021-12-27 2023-06-30 江苏恩华药业股份有限公司 吡唑衍生物及其应用

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412263B1 (pt) 2003-07-22 2019-10-15 Arena Pharmaceuticals, Inc. Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
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
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
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
CA2741731A1 (en) 2008-10-28 2010-06-03 Arena Pharmaceuticals, Inc. Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto
EP4119141A1 (en) 2015-06-12 2023-01-18 Axovant Sciences GmbH Nelotanserin for the prophylaxis and treatment of rem sleep behavior disorder
EP3322415A4 (en) 2015-07-15 2019-03-13 Axovant Sciences GmbH DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR FOR PROPHYLAXIS AND TREATMENT OF HALLUCINATIONS RELATED TO A NEUROGENERATIVE DISEASE
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
EP3436010B1 (en) * 2016-03-29 2021-03-10 Acadia Pharmaceuticals Inc. 5-ht2a serotonin receptor inverse agonists or antagonists for use in reducing amyloid-beta peptides and accumulation of amyloid plaques
US11464768B2 (en) 2016-12-20 2022-10-11 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
WO2021222174A1 (en) * 2020-04-28 2021-11-04 Prelude Therapeutics Incorporated Bcl-2 inhibitors and their use as pharmaceuticals
US20230346811A1 (en) * 2020-09-18 2023-11-02 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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014085362A1 (en) * 2012-11-27 2014-06-05 Acadia Pharmaceuticals Inc. Methods for the treatment of parkinson's disease psychosis using pimavanserin
WO2015085004A1 (en) * 2013-12-03 2015-06-11 Intra-Cellular Therapies, Inc. Novel methods

Family Cites Families (266)

* 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
JPH03135978A (ja) 1989-08-08 1991-06-10 Merck Sharp & Dohme Ltd 置換ピリジン、その製法、処方並びに痴呆症における使用法
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
US5905080A (en) 1993-08-20 1999-05-18 Smithkline Beecham, P.L.C. Amide and urea derivatives as 5HT1D receptor antagonists
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
EP0784612A1 (en) 1994-10-04 1997-07-23 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
CN1151147C (zh) 1995-02-02 2004-05-26 史密丝克莱恩比彻姆有限公司 作为5-ht受体拮抗剂的吲哚衍生物
US5576338A (en) 1995-02-15 1996-11-19 Merck Frosst Canada, Inc. Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis
EP0809492A4 (en) 1995-02-17 2007-01-24 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
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
WO1997045400A1 (en) 1996-05-24 1997-12-04 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
AU2962297A (en) 1996-05-24 1998-01-05 Neurosearch A/S Phenyl derivatives useful as blockers of chloride channels
KR20000022273A (ko) 1996-06-27 2000-04-25 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 Il-8 수용체 길항제
US6063808A (en) 1996-07-01 2000-05-16 Sepracor Inc. Methods and compositions for treating urinary incontinence using enantiomerically enriched (S,S)-glycopyrrolate
WO1998000016A1 (en) 1996-07-01 1998-01-08 Sepracor, Inc. Methods and compositions for treating urinary incontinence using enantiomerically enriched (r,r)-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
DE69735002T2 (de) 1996-10-25 2006-10-26 Shire Laboratories, Inc. Osmotisches Verabreichungssystem für lösliche Dosen
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.
DE59803962D1 (de) 1997-03-25 2002-06-06 Ciba Sc Holding Ag Polycyclische Verbindungen
US6541209B1 (en) 1997-04-14 2003-04-01 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
US6420541B1 (en) 1998-04-14 2002-07-16 Arena Pharmaceuticals, Inc. Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof
SK282818B6 (sk) 1997-04-22 2002-12-03 Neurosearch A/S Substituované fenylderiváty, ich príprava, použitie a farmaceutický prípravok
PT977737E (pt) 1997-04-22 2004-02-27 Janssen Pharmaceutica Nv Quino- e quinazolinas antagonistas de crf
US6696475B2 (en) 1997-04-22 2004-02-24 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
EP1001945B1 (en) 1997-05-28 2011-03-02 Aventis Pharmaceuticals 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
EP0991623A2 (en) 1997-06-19 2000-04-12 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
WO1999002502A2 (en) 1997-07-11 1999-01-21 Smithkline Beecham Plc Sulphonamide derivatives being 5-ht6 receptor antagonists and process for their preparation
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
EP1007049A1 (en) 1997-08-27 2000-06-14 Hexal AG New pharmaceutical compositions of meloxicam with improved solubility and bioavailability
JP4555468B2 (ja) 1997-10-31 2010-09-29 アベンテイス・フアルマ・リミテツド 置換アニリド
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
EP1042305B1 (en) 1997-12-22 2005-06-08 Bayer Pharmaceuticals Corp. INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS
CA2315646C (en) 1997-12-22 2010-02-09 Bayer Corporation Inhibition of raf kinase using symmetrical and unsymmetrical substituted 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
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
EP1123274B1 (en) 1998-10-22 2004-12-29 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
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
AU3033500A (en) 1999-01-15 2000-08-01 Agouron Pharmaceuticals, Inc. 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
KR20020015308A (ko) 1999-03-26 2002-02-27 추후보정 아릴 치환된 피라졸, 이미다졸, 옥사졸, 티아졸 및 피롤,및 이의 용도
JP2002540203A (ja) 1999-03-29 2002-11-26 ニューロゲン コーポレイション Ｎｋ−３および／またはｇａｂａ（ａ）受容体リガンドとしての４−置換キノリン誘導体
CA2370147C (en) 1999-04-21 2009-07-28 Allelix Biopharmaceuticals Inc. Piperidine-indole compounds having 5-ht6 affinity
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
CZ2002323A3 (cs) 1999-07-28 2002-05-15 Aventis Pharmaceuticals Products Inc. Substituované oxoazaheterocyklylové sloučeniny a farmaceutické prostředky, které je obsahují
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
GB9926302D0 (en) 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
WO2001032660A1 (en) 1999-11-05 2001-05-10 Nps Allelix Corp. Compounds having 5-ht6 receptor antagonist activity
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
AU784848B2 (en) 1999-12-20 2006-07-06 Zalicus Pharmaceuticals Ltd. Partially saturated calcium channel blockers
AU2001241927A1 (en) 2000-02-28 2001-09-12 Scios Inc. Inhibitors of p38-alpha 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
US7115630B2 (en) 2000-10-02 2006-10-03 Janssen Pharmaceutica N.V. Metabotropic glutamate receptor antagonists
NZ524675A (en) 2000-10-20 2004-09-24 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
BR0115102B1 (pt) 2000-11-02 2013-11-26 Compostos 1-aril- ou 1-alquilsulfonil-heterociclilbenzazóis e composição compreendendo os mesmos
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
WO2002041889A2 (en) 2000-11-24 2002-05-30 Smithkline Beecham P.L.C. 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
US20040077654A1 (en) 2001-01-15 2004-04-22 Bouillot Anne Marie Jeanne Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
WO2002076464A1 (en) 2001-03-22 2002-10-03 Arena Pharmaceuticals, Inc. Anti-psychosis combination
KR100894189B1 (ko) 2001-03-29 2009-04-22 일라이 릴리 앤드 캄파니 5-ｈｔ6 수용체의 길항제로서의 ｎ-(2-아릴에틸)벤질아민
GB0111186D0 (en) 2001-05-08 2001-06-27 Smithkline Beecham Plc Novel compounds
YU96103A (sh) 2001-06-07 2006-08-17 F.Hoffmann-La Roche Ag. Novi derivati indola sa afinitetom za 5-ht6 receptor
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.
WO2003002097A1 (en) 2001-06-29 2003-01-09 Eurand Pharmaceuticals Ltd Process of thermodynamical activation of water-insoluble drugs loaded into cross-linked polymers
EP1411925A1 (en) 2001-08-03 2004-04-28 PHARMACIA & UPJOHN COMPANY 5-arylsulfonyl indoles having 5-ht6 receptor affinity
WO2003013510A1 (en) 2001-08-07 2003-02-20 Smithkline Beecham P.L.C. 3-arylsulfonyl-7-piperazinyl- indoles, -benzofurans and -benzothiophenes with 5-ht6 receptor affinity for treating cns disorders
MXPA04001250A (es) 2001-08-10 2004-05-27 Hoffmann La Roche Derivados de arilsulfonilo con afinidad receptora de 5-hidroxitriptamina6 (5-ht6).
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
WO2003020707A1 (en) 2001-08-31 2003-03-13 Novartis Ag Optical isomers of an iloperidone metabolite
ES2329881T3 (es) 2001-09-21 2009-12-02 Bristol-Myers Squibb Company Compuestos que contienen lactama y derivados de los mismos como inhibidores del factor xa.
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
WO2003062205A1 (en) 2001-12-21 2003-07-31 Smithkline Beecham P.L.C. 7-sulfonyl-3-benzazepine derivatives as modulators of the dopamine receptor and their use for the treatment of cns disorders
WO2003062206A2 (en) 2002-01-23 2003-07-31 Arena Pharmaceuticals, Inc. Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
JP2005522432A (ja) 2002-02-05 2005-07-28 グラクソ　グループ　リミテッド ニューロン成長の促進方法
GB0202679D0 (en) 2002-02-05 2002-03-20 Glaxo Group Ltd Novel compounds
DE60304695T2 (de) 2002-02-13 2006-09-21 Glaxo Group Ltd., Greenford 7-arylsulfonamido-2,3,4,5-tetrahydro-1h-benzo[d]azepin-derivate mit 5-hat-6-rezeptor affinität zur behandlung von erkrankungen des zentralnervensystems
BR0307903A (pt) 2002-02-22 2006-04-04 Upjohn Co derivados de arilsulfona
BRPI0308696B8 (pt) 2002-03-27 2021-05-25 Axovant Sciences Gmbh composto derivado de quinolina, seu processo de preparação, sua composição farmacêutica e seus usos
AU2003226724A1 (en) 2002-03-27 2003-10-08 Glaxo Group Limited Quinoline and aza-indole derivatives and their use as 5-ht6 ligands
CA2485136C (en) 2002-05-13 2011-12-20 F. Hoffmann-La Roche Ag Benzoxazine derivatives as 5-ht6 modulators and uses thereof
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
US7943639B2 (en) 2002-06-20 2011-05-17 Proximagen Limited Compounds
SG156524A1 (en) 2002-06-20 2009-11-26 Biovitrum Ab Publ New compounds useful for the treatment of obesity, type ii diabetes and cns disorders
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
ATE362469T1 (de) 2002-09-17 2007-06-15 Hoffmann La Roche 2,7-disubstituierteindole und ihre verwendung als 5-ht6 modulatoren
WO2004028450A2 (en) 2002-09-24 2004-04-08 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
EP1556037B1 (en) 2002-10-18 2006-11-02 F. Hoffmann-La Roche Ag 4-piperazinyl benzenesulfonyl indoles with 5-ht6 receptor affinity
TW200529597A (en) 2002-11-08 2005-09-01 Interdigital Tech Corp Composite channel quality estimation techniques for wireless receivers
JP4401297B2 (ja) 2002-11-08 2010-01-20 エフ．ホフマン−ラ ロシュ アーゲー 置換ベンゾオキサジノン及びその使用
AU2003284402A1 (en) 2002-11-15 2004-06-15 Yamanouchi Pharmaceutical Co., Ltd. Antagonist to melanin-concentrating hormone receptor
NZ539950A (en) 2002-12-03 2007-05-31 Hoffmann La Roche Aminoalkoxyindoles as 5-HT6-receptor ligands for the treatment of CNS-disorders
WO2004058722A1 (en) 2002-12-24 2004-07-15 Arena Pharmaceuticals, Inc. Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
ATE407117T1 (de) * 2003-01-16 2008-09-15 Acadia Pharm Inc Selektive serotonin 2a/2c inverse rezeptoragonisten als therapeutika für neurodegenerative erkrankungen
CA2515544A1 (en) 2003-02-11 2004-08-26 Kemia Inc. Compounds for the treatment of viral infection
BRPI0407253A (pt) 2003-02-14 2006-01-31 Wyeth Corp Heterociclil-3-sulfonilindazóis como ligandos 5-hidroxitriptamina-6 processo de preparação dos mesmos, seus usos na preparação de uma composição farmacêutica e composição farmacêutica compreendendo os referidos compostos
ATE429228T1 (de) 2003-02-14 2009-05-15 Serono Lab Derivate von piperazine-2-carboxamide
JP2006517966A (ja) 2003-02-14 2006-08-03 ワイス ５−ヒドロキシトリプタミン−６リガンドとしてのヘテロサイクリル−３−スルホニルアザインドールまたは−アザインダゾール誘導体
ES2297386T3 (es) 2003-03-03 2008-05-01 F. Hoffmann-La Roche Ag Tetrahidroisoquinolinas 2,5-sustituidas para uso como moduladores de 5-ht6.
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
JP2006521345A (ja) 2003-03-28 2006-09-21 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ニコチン性アセチルコリン受容体の正のアロステリック調節剤
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
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
BRPI0412263B1 (pt) 2003-07-22 2019-10-15 Arena Pharmaceuticals, Inc. Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
MXPA06001636A (es) 2003-08-13 2006-04-28 Amgen Inc Antagonista del receptor de la hormona concentradora de melanina.
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
AU2004268918A1 (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
GB0322629D0 (en) 2003-09-26 2003-10-29 Glaxo Group Ltd Novel compound
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
WO2005103011A1 (en) 2004-03-23 2005-11-03 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
ATE412651T1 (de) 2004-06-09 2008-11-15 Glaxo Group Ltd Pyrrolopyridinderivate
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
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
CA2584485C (en) 2004-10-20 2013-12-31 Resverlogix Corp. Stilbenes and chalcones 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
WO2006049734A2 (en) 2004-10-29 2006-05-11 Hypnion, Inc. Quetiapine analogs and methods of use thereof
DE602005025391D1 (de) 2004-11-01 2011-01-27 Seo Hong Yoo Verfahren und zusammensetzungen zur verringerung der neurodegeneration bei amyotrophischer lateralsklerose
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
GB0425548D0 (en) 2004-11-19 2004-12-22 Glaxo Group Ltd Radiolabelled ligands
WO2006060654A2 (en) 2004-12-01 2006-06-08 Divergence, Inc. Pesticidal compositions and methods
GB0426313D0 (en) 2004-12-01 2005-01-05 Merck Sharp & Dohme Therapeutic agents
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
EP1858877B1 (en) 2005-01-14 2014-03-12 Gilead Connecticut, Inc. 1,3 substituted diaryl ureas as modulators of kinase activity
AU2006206687A1 (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
AU2006206292B2 (en) 2005-01-21 2009-09-03 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
BRPI0607088A2 (pt) 2005-01-27 2009-08-04 Janssen Pharmaceutica Nv derivados de tetrahidrofurano heterocìclico tetracìclico como inibidores de 5ht2 no tratamento de distúrbios cns
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
US7998974B2 (en) 2005-03-03 2011-08-16 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
US7494998B2 (en) 2005-04-26 2009-02-24 Hypnion, Inc. Benzisoxazole piperazine compounds and methods of use thereof
EP1734039A1 (en) 2005-06-13 2006-12-20 Esbatech AG Aryl urea compounds as BETA-secretase inhibitors
EP1910307A1 (en) 2005-06-27 2008-04-16 Exelixis, Inc. Pyrazole based lxr modulators
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
TWI329641B (en) 2005-08-31 2010-09-01 Otsuka Pharma Co Ltd (benzo[b]thiophen-4-yl)piperazine compounds, pharmaceutical compositions comprising the same, uses of the same and processes for preparing the same
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
KR20080055963A (ko) 2005-09-29 2008-06-19 아레나 파마슈티칼스, 인크. 5-ｈｔ2ａ 세로토닌 수용체 조절제와 관련된 장애의 치료에유용한 5-ｈｔ2ａ 세로토닌 수용체 조절제의 제약 조성물
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
EP2027119A2 (en) 2006-05-18 2009-02-25 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
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
CN102827081A (zh) 2006-05-18 2012-12-19 艾尼纳制药公司 用作5-ht2a 血清素受体调节剂的苯基-吡唑的晶型和其制备方法
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
PT2040755E (pt) 2006-06-23 2011-07-08 Esteve Labor Dr Combinação de um inibidor de colinesterase e um composto com afinidade para o receptor 5-ht6
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
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
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
AU2007333194A1 (en) 2006-12-08 2008-06-19 Exelixis, Inc. LXR and FXR modulators
EP2120950B1 (en) 2007-03-21 2012-07-04 Glaxo Group Limited Use of quinoline derivatives in the treatment of pain
EP2190844B3 (en) 2007-08-15 2013-07-17 Arena Pharmaceuticals, Inc. Imidazo[1,2-a]pyridine derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
CA2700331A1 (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
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
US20110178094A1 (en) 2008-10-03 2011-07-21 H. Lundbeck A/S Oral Formulation
CA2741731A1 (en) 2008-10-28 2010-06-03 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
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
EP2858649B1 (en) 2012-06-11 2019-10-23 Psychogenics Inc. Treatment of motor and movement disorder side effects associated with parkinson's disease treatments
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
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
WO2015171547A1 (en) 2014-05-05 2015-11-12 Ovid Therapeutics Inc. Methods of treating cognitive impairment associated with neurodegenerative disorders
MX2017014192A (es) 2015-05-07 2018-08-01 Axovant Sciences Gmbh Composiciones y metodos de tratamiento de una enfermedad neurodegenerativa.
US20160324851A1 (en) 2015-05-07 2016-11-10 Axovant Sciences, Ltd. Methods of treating a neurodegenerative disease
EP4119141A1 (en) 2015-06-12 2023-01-18 Axovant Sciences GmbH Nelotanserin for the prophylaxis and treatment of rem sleep behavior disorder
EP3322415A4 (en) 2015-07-15 2019-03-13 Axovant Sciences GmbH DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR FOR PROPHYLAXIS AND TREATMENT OF HALLUCINATIONS RELATED TO A NEUROGENERATIVE DISEASE
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014085362A1 (en) * 2012-11-27 2014-06-05 Acadia Pharmaceuticals Inc. Methods for the treatment of parkinson's disease psychosis using pimavanserin
WO2015085004A1 (en) * 2013-12-03 2015-06-11 Intra-Cellular Therapies, Inc. Novel methods

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116354925A (zh) * 2021-12-27 2023-06-30 江苏恩华药业股份有限公司 吡唑衍生物及其应用

Also Published As

Publication number Publication date
JP2021185144A (ja) 2021-12-09
US20210177804A1 (en) 2021-06-17
MX391031B (es) 2025-03-21
CA2992518A1 (en) 2017-01-19
RU2018103338A (ru) 2019-08-15
WO2017011767A3 (en) 2017-04-06
EP3322415A2 (en) 2018-05-23
HK1247555A1 (zh) 2018-09-28
KR20180064373A (ko) 2018-06-14
TW201720439A (zh) 2017-06-16
US10034859B2 (en) 2018-07-31
US20170014385A1 (en) 2017-01-19
WO2017011767A2 (en) 2017-01-19
US11304932B2 (en) 2022-04-19
EP3322415A4 (en) 2019-03-13
AU2016291673A1 (en) 2018-01-25
US20190151287A1 (en) 2019-05-23
RU2018103338A3 (enExample) 2019-08-15
BR112018000728A2 (pt) 2018-09-04
MX2018000465A (es) 2018-09-17
JP2018520187A (ja) 2018-07-26
IL256831A (en) 2018-03-29

Similar Documents

Publication Publication Date Title
US11304932B2 (en) 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
US20200397754A1 (en) Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of rem sleep behavior disorder
JP2008527042A (ja) 進行性多病巣性白質脳障害の予防または治療に有用な、５−ｈｔ２ａセロトニン受容体の調節因子としてのジアリールおよびアリールヘテロアリール尿素誘導体
US20160324852A1 (en) Compositions and methods of treating a neurodegenerative disease
JP2010505832A (ja) ５−ｈｔ２ａセロトニン受容体に関連する障害の処置に有用な５−ｈｔ２ａセロトニン受容体の調整因子としてのピラゾール誘導体
US20190343817A1 (en) Method of treating pain
IL269787A (en) Methods and compositions for treating aging-associated impairments using ccr3-inhibitors
US20210128528A1 (en) Use of 5ht2a inverse agonists for treating psychosis
EA021936B1 (ru) Способ лечения острой мании
US20180042922A1 (en) Compositions and methods of treating a neurodegenerative disease
BR112021004893A2 (pt) composições compreendendo um inibidor de crac e um corticosteroide e métodos de uso dos mesmos
RS57133B1 (sr) Kompozicija za tretman poremećaja hipoaktivno umanjenje seksualne želje
KR20100022956A (ko) 급성 조증 치료용 카르바모일-시클로헥산

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
RJ01 Rejection of invention patent application after publication

Application publication date: 20180831

RJ01 Rejection of invention patent application after publication