CN107848972B - 用于制备n-(4-氟苄基)-n-(1-甲基哌啶-4-基)-n’-(4-(2-甲基丙氧基)苯基甲基)脲及其酒石酸盐和多晶型c的方法 - Google Patents

用于制备n-(4-氟苄基)-n-(1-甲基哌啶-4-基)-n’-(4-(2-甲基丙氧基)苯基甲基)脲及其酒石酸盐和多晶型c的方法 Download PDF

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CN107848972B
CN107848972B CN201680040273.6A CN201680040273A CN107848972B CN 107848972 B CN107848972 B CN 107848972B CN 201680040273 A CN201680040273 A CN 201680040273A CN 107848972 B CN107848972 B CN 107848972B
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pimavanserin
group
substituted
formula
unsubstituted
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CN107848972A (zh
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马龙·卡洛斯
萨冈·坦德尔
R·奥尔森
米卡尔·希尔格伦
马修·J·弗莱明
安德烈亚斯·菲利普·布迪耶
贝亚特·T·韦伯
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Acadia Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • 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
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/98—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201680040273.6A 2015-07-20 2016-07-19 用于制备n-(4-氟苄基)-n-(1-甲基哌啶-4-基)-n’-(4-(2-甲基丙氧基)苯基甲基)脲及其酒石酸盐和多晶型c的方法 Active CN107848972B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562194725P 2015-07-20 2015-07-20
US62/194,725 2015-07-20
PCT/US2016/042933 WO2017015272A1 (en) 2015-07-20 2016-07-19 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

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CN107848972A CN107848972A (zh) 2018-03-27
CN107848972B true CN107848972B (zh) 2021-06-18

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US (4) US10597363B2 (enExample)
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CA (1) CA2992728A1 (enExample)
DK (1) DK3325444T3 (enExample)
ES (1) ES2890492T3 (enExample)
HU (1) HUE055763T2 (enExample)
IL (1) IL256998B (enExample)
PL (1) PL3325444T3 (enExample)
PT (1) PT3325444T (enExample)
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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2890492T3 (es) * 2015-07-20 2022-01-20 Acadia Pharm Inc Métodos para preparar N-(4-fluorobencil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloxi)fenilmetil)carbamida y su sal de tartrato y forma polimórfica C
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2018118626A1 (en) 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
EP3615028A1 (en) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
CN107200707B (zh) * 2017-05-16 2020-10-02 河北科技大学 一种匹莫范色林的制备方法
WO2019008595A1 (en) * 2017-07-03 2019-01-10 Jubilant Generics Limited (Formerly A Division Of Jubilant Life Sciences Limited) PROCESS FOR THE PREPARATION OF 1- (4-FLUOROBENZYL) -3- (4-ISOBUTOXYBENZYL) -1- (1-METHYLPIPERIDIN-4-YL) UREA AND ITS SALTS
WO2019040106A2 (en) * 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, RELATED SALTS AND METHODS FOR THE TREATMENT OF DISEASES
WO2019040104A2 (en) * 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, RELATED SALTS AND METHODS OF TREATING DISEASES
SG11202001062XA (en) 2017-08-21 2020-03-30 Acadia Pharm Inc Compounds, salts thereof and methods for treatment of diseases
EP3675827A1 (en) 2017-08-30 2020-07-08 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
CN110054583A (zh) * 2018-01-19 2019-07-26 广东东阳光药业有限公司 一种制备哌马色林或其盐的方法
CN112119058A (zh) * 2018-04-26 2020-12-22 欧伦股份公司 制备哌马色林碱的方法
CN110894186B (zh) * 2018-09-12 2022-05-24 浙江京新药业股份有限公司 匹莫范色林及其中间体的制备方法
US20220016101A1 (en) 2018-10-30 2022-01-20 Acadia Pharmaceuticals Inc. Methods of treating depression, anxiety and sexual dysfunction using the compound pimavanserin
CN111320569B (zh) * 2018-12-17 2022-03-08 江苏艾立康医药科技有限公司 一种哌马色林固态中间体的制备方法
US20220288048A1 (en) 2019-07-22 2022-09-15 Acadia Pharmaceuticals Inc. Pimavanserin for treating schizophrenia or for treating psychosis secondary to neurodegenerative disorders or depressive disorder
US20220323429A1 (en) 2019-08-15 2022-10-13 Acadia Pharmaceuticals Inc. Pimavanserin for treating neurodegenerative diseases
WO2022094230A1 (en) 2020-11-02 2022-05-05 Acadia Pharmaceuticals Inc. Compounds for treating psychosis or depression
CN116496496B (zh) * 2023-04-27 2024-11-05 中国石油大学(华东) 一种基于三嗪共价框架材料（CTFs）制备单位点催化剂的制备方法

Family Cites Families (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE794333A (fr) 1972-01-20 1973-07-19 Wyeth John & Brother Ltd Composes heterocycliques azotes therapeutiques
GB1507462A (en) 1974-03-21 1978-04-12 Gallardo Antonio Sa N-heterocyclic substituted benzamides methods for their preparation and compositions containing them
US3983234A (en) 1974-07-04 1976-09-28 Sandoz Ltd. Treatment of dyskinesias
JPS5152176A (enExample) 1974-10-12 1976-05-08 Yoshitomi Pharmaceutical
JPS5285174A (en) 1976-01-05 1977-07-15 Yoshitomi Pharmaceut Ind Ltd Novel urea or thiourea derivatives
GB1586468A (en) 1976-10-29 1981-03-18 Anphar Sa Piperidine derivatives
CA1140119A (en) 1978-04-03 1983-01-25 Joseph Torremans N-heterocyclyl-4-piperidinamines
US4255432A (en) 1979-09-06 1981-03-10 Syntex (U.S.A.) Inc. 8-[2-3-Indolyl)ethyl]-1-oxa-3-,8-diazaspiro[4.5]decan-2-ones, pharmaceutical compositions thereof and methods of use thereof
US4332804A (en) 1981-03-23 1982-06-01 Syntex (U.S.A.) Inc. 9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones
US4353900A (en) 1981-10-19 1982-10-12 Syntex (U.S.A.) Inc. 9-(Arylalkyl or aroylalkyl)-1-oxa-4,9-diazaspiro(5.5)undecan-3-ones
US4353901A (en) 1981-10-19 1982-10-12 Syntex (U.S.A.) Inc. 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones
GB8527052D0 (en) 1985-11-02 1985-12-04 Beecham Group Plc Compounds
GB8621892D0 (en) 1986-09-11 1986-10-15 Lundbeck & Co As H Organic compound
FR2642069B1 (fr) 1989-01-20 1991-04-12 Rhone Poulenc Sante Nouveaux derives du benzopyranne, leur preparation et les compositions pharmaceutiques qui les contiennent
US5214055A (en) 1990-05-18 1993-05-25 Adir Et Compagnie Aminopiperidine 4-oxo-4H-chromen-2-yl compounds
US5216165A (en) 1990-10-03 1993-06-01 American Home Products Corporation N-substituted aminoquinolines as analgesic agents
IT1252227B (it) 1991-12-17 1995-06-05 Ciba Geigy Spa Composti tetrametilpiperidinici atti all'impiego come stabilizzanti per materiali organici
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
CA2123728A1 (en) 1993-05-21 1994-11-22 Noriyoshi Sueda Urea derivatives and their use as acat inhibitors
AU6971794A (en) 1993-05-26 1994-12-20 Smithkline Beecham Laboratoires Pharmaceutiques Novel compounds
IL110298A (en) 1993-07-13 1999-04-11 Brann Mark Robert Identification of ligands by selective amplification of cells transfected with receptors
DE4404183A1 (de) 1994-02-10 1995-08-17 Merck Patent Gmbh 4-Amino-1-piperidylbenzoylguanidine
US5795894A (en) 1995-05-02 1998-08-18 Schering Corporation Piperazino derivatives as neurokinn antagonists
BR9610277A (pt) 1995-08-31 1999-07-06 Schering Corp Derivados de piperazino como antagonistas de neurowuinina
WO1997011940A1 (en) 1995-09-29 1997-04-03 Eli Lilly And Company Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation
IL124536A (en) 1995-12-07 2001-03-19 Daniel C Javitt Pharmaceutical compositions containing a glycine uptake antagonist
CA2249601A1 (en) 1996-04-03 1997-10-23 Thorsten E. Fisher Inhibitors of farnesyl-protein transferase
WO1997038984A1 (en) 1996-04-17 1997-10-23 Du Pont Pharmaceuticals Company N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-one derivatives as factor xa inhibitors
US5869488A (en) 1996-05-01 1999-02-09 Schering Corporation Piperazino derivatives as neurokinin antagonists
US5877173A (en) 1996-08-28 1999-03-02 Washington University Preventing neuronal degeneration in Alzheimer's disease
DK0927192T3 (da) 1996-09-10 2004-09-13 Boehringer Ingelheim Pharma Modificerede aminosyrer, lægemidler indeholdende disse forbindelser og fremgangsmåder til deres fremstilling
DE19643331A1 (de) 1996-10-21 1998-04-23 Thomae Gmbh Dr K 1-(4-Piperidinyl)-piperidinylene, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6057338A (en) 1997-04-04 2000-05-02 Merck & Co., Inc. Somatostatin agonists
HUP0001285A3 (en) 1997-05-08 2000-10-30 Smithkline Beecham Corp Philap Pyrrolidine derivatives as protease inhibitors, process for producing them and pharmaceutical compositions containing them
GB9718833D0 (en) 1997-09-04 1997-11-12 Merck Sharp & Dohme Therapeutic agents
CA2323177A1 (en) 1998-03-11 1999-09-16 Susan Marie Milosovich Composition
JP2003514763A (ja) 1998-04-14 2003-04-22 アリーナ・フアーマシユーチカルズ・インコーポレーテツド 非内在性の構成的に活性化されるヒトセロトニンレセプターおよびその小分子調節物質
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
US6358698B1 (en) 1998-10-07 2002-03-19 Acadia Pharmacueticals Inc. Methods of identifying inverse agonists of the serotonin 2A receptor
CN1198613C (zh) 1998-10-16 2005-04-27 第一三得利制药株式会社 氨基苯氧基乙酸衍生物和含有它们的药用组合物
US6150393A (en) 1998-12-18 2000-11-21 Arena Pharmaceuticals, Inc. Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
EP1013276A1 (en) 1998-12-23 2000-06-28 Pfizer Inc. Aminoazacycloalkanes as CCR5 modulators
EP1178800A4 (en) 1999-03-24 2002-07-31 Univ California Method of treating neurodegenerative disorders using aspartyl protease inhibitors
US6399619B1 (en) 1999-04-06 2002-06-04 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
KR20020014797A (ko) 1999-05-17 2002-02-25 한센 핀 베네드, 안네 제헤르, 웨이콥 마리안느 글루카곤 길항제/역 아고니스트
US20040229908A1 (en) 1999-07-13 2004-11-18 Jodi Nelson Compositions and methods for the treatment of Parkinson's disease and tardive dyskinesias
US20050148018A1 (en) 1999-10-07 2005-07-07 David Weiner Methods of identifying inverse agonists of the serotonin 2A receptor
FR2802206B1 (fr) 1999-12-14 2005-04-22 Sod Conseils Rech Applic Derives de 4-aminopiperidine et leur utilisation en tant que medicament
US7022698B2 (en) 1999-12-28 2006-04-04 U & I Pharmaceuticals, Ltd. Pharmaceutical compositions containing new polymorphic forms of olanzapine and uses thereof
CA2397981C (en) 2000-03-06 2010-12-21 Acadia Pharmaceuticals, Inc. Azacyclic compounds for use in the treatment of serotonin related diseases
GB0011838D0 (en) 2000-05-17 2000-07-05 Astrazeneca Ab Chemical compounds
US20020099076A1 (en) 2000-05-25 2002-07-25 Richard Scheyer D. Use of (+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol or its prodrug in the treatment of symptoms of dementia and dopamine induced psychosis
DE60141752D1 (de) 2000-06-30 2010-05-20 Innogenetics Nv Differentielle diagnose von neurologischen krankheiten
HUP0300810A2 (hu) 2000-07-20 2003-08-28 M.G.V.S. Ltd. Mesterséges értranszplantátum, valamint ennek létrehozása és alkalmazása
IL154363A0 (en) 2000-09-25 2003-09-17 Actelion Pharmaceuticals Ltd Substituted amino-aza-cycloalkanes useful against malaria
AU2002230423A1 (en) 2000-11-08 2002-05-21 Massachusetts Institute Of Technology Serotonergic compositions and methods for treatment of mild cognitive impairment
WO2002076464A1 (en) 2001-03-22 2002-10-03 Arena Pharmaceuticals, Inc. Anti-psychosis combination
GB0108099D0 (en) 2001-03-30 2001-05-23 Hoffmann La Roche Aminopiperidine derivatives
KR100809569B1 (ko) 2001-10-02 2008-03-04 아카디아 파마슈티칼스 인코포레이티드 무스카린 제제로서 벤즈이미다졸리디논 유도체
ATE466014T1 (de) 2001-12-28 2010-05-15 Acadia Pharm Inc Spiroazacyclische verbindungen als monoaminrezeptormodulatoren
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
UY27668A1 (es) 2002-02-20 2003-10-31 Pfizer Prod Inc Composición de ziprasidona y controles sintéticos
GB0208279D0 (en) 2002-04-10 2002-05-22 Glaxo Group Ltd Novel compounds
MXPA04012893A (es) 2002-06-24 2005-03-31 Acadia Pharm Inc Derivados de piperidina n-substituidos como agentes receptores de serotonina.
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
WO2004039322A2 (en) 2002-10-29 2004-05-13 Miicro, Inc. Novel combination therapy for schizophrenia focused on improved cognition: 5-ht-2a/d2 blockade with adjunctive blockade of prefrontal da reuptake
US7601740B2 (en) 2003-01-16 2009-10-13 Acadia Pharmaceuticals, Inc. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
EP1589974A2 (en) 2003-01-23 2005-11-02 Acadia Pharmaceuticals Inc. Use of n-desmethylclozapine to treat human neuropsychiatric disease
CA2547639A1 (en) 2003-12-02 2005-06-16 B&B Beheer Nv Use of d4 and 5-ht2a antagonists, inverse agonists or partial agonists
EP1576985A1 (en) 2004-03-18 2005-09-21 B&B Beheer NV Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists
PL1696931T3 (pl) 2003-12-22 2009-10-30 Acadia Pharm Inc Aminopodstawione analogi diarylo[A,D]cykloheptenowe jako agoniści receptorów muskarynowych i sposoby leczenia chorób neuropsychiatrycznych
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
US20050261278A1 (en) 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
US7790899B2 (en) * 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
DK1794126T3 (da) 2004-09-27 2013-06-24 Acadia Pharm Inc Krystallinsk form af N-(-4-fluorbenzyl)-N-(1-methylpiperidn-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamid-hemitartrat
WO2006096439A2 (en) 2005-03-04 2006-09-14 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for the treatment and/or prevention of schizophrenia and related diseases
JP2008534593A (ja) 2005-03-30 2008-08-28 メルク エンド カムパニー インコーポレーテッド グルカゴン受容体アンタゴニスト化合物、そのような化合物を含む組成物、及びその使用方法
US20080051429A1 (en) 2006-04-19 2008-02-28 Van Kammen Daniel Use of 4-amino-piperidines for treating sleep disorders
WO2007124136A1 (en) * 2006-04-19 2007-11-01 Acadia Pharmaceuticals, Inc. Use of 4-amino-piperidines for treating sleep disorders
CA2652300A1 (en) 2006-05-15 2007-11-22 Acadia Pharmaceuticals Inc. Pharmaceutical formulations of pimavanserin
ES2423485T3 (es) 2007-03-19 2013-09-20 Acadia Pharmaceuticals Inc. Asociaciones de agonistas y antagonistas inversos 5-HT2A con antipsicóticos
WO2008141057A1 (en) 2007-05-08 2008-11-20 Auspex Pharmaceuticals, Inc. Deuterated pimavanserin 1- (4-flu0r0benzyl) -3- (4-isobutoxybenzyl) -1- ( l-methyl-piperidin-4-yl) -urea
AU2008254669A1 (en) 2007-05-18 2008-11-27 Acadia Pharmaceuticals Inc. Use of pimavanserin in the treatment of parkinson and symptoms thereof
WO2009035473A2 (en) 2007-09-13 2009-03-19 Sanfilippo Louis C Method of treating binge eating disorder, obesity resulting from binge eating behavior and depressive disorders
WO2009039461A2 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
SI2200610T1 (en) 2007-09-21 2018-06-29 Acadia Pharmaceuticals Inc. Co-administration of pimavanserin with other agents
WO2010111353A1 (en) 2009-03-25 2010-09-30 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
US8927553B2 (en) 2009-08-10 2015-01-06 Daljit Singh Dhanoa Deuterium-enriched alkyl sulfonamides and uses thereof
CA2777843A1 (en) 2009-10-16 2011-04-21 University Of South Florida Treatment of suicidal ideation or behavior using inhibitors of nicotinic acetylcholine receptors
US7816383B1 (en) 2009-12-04 2010-10-19 Intermune, Inc. Methods of administering pirfenidone therapy
WO2011085216A2 (en) 2010-01-08 2011-07-14 Ironwood Pharmaceuticals, Inc. Use of faah inhibitors for treating parkinson's disease and restless legs syndrome
WO2012002583A1 (en) 2010-07-02 2012-01-05 Vanderbilt University Method for treating schizophrenia and related diseases with a combination therapy
EP2598159A4 (en) 2010-07-30 2014-01-08 Merck Sharp & Dohme INHIBITION OF THE CYP3A DRUG MIXTURE EXCHANGE
US9737531B2 (en) 2012-07-12 2017-08-22 Glytech, Llc Composition and method for treatment of depression and psychosis in humans
EP2556827A1 (en) 2011-08-11 2013-02-13 Acadia Pharmaceuticals Inc. Treatment of neurodegenerative diseases
WO2014085362A1 (en) 2012-11-27 2014-06-05 Acadia Pharmaceuticals Inc. Methods for the treatment of parkinson's disease psychosis using pimavanserin
CN105418460B (zh) * 2014-08-11 2017-04-12 苏州鹏旭医药科技有限公司 匹莫范色林及其类似化合物中间体，其制备方法和制备匹莫范色林及其类似化合物的方法
EP3271018B1 (en) * 2015-03-02 2020-12-23 Pliva Hrvatska D.O.O. Processes and intermediates for the preparation of pimavanserin
CN104961672B (zh) * 2015-05-20 2017-10-20 沈阳药科大学 一种n‑(4‑氟苄基)‑n‑(1‑甲基哌啶‑4‑基)‑n’‑(4‑异丁氧基苄基)脲的酒石酸盐的合成方法
CN104844502B (zh) * 2015-06-05 2018-07-31 齐鲁师范学院 一种匹莫范色林的制备方法
JP2018516992A (ja) 2015-06-12 2018-06-28 アクソファント サイエンシーズ ゲーエムベーハーＡｘｏｖａｎｔ Ｓｃｉｅｎｃｅｓ Ｇｍｂｈ レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体
WO2017011767A2 (en) 2015-07-15 2017-01-19 Axovant Sciences Ltd. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of hallucinations associated with a neurodegenerative disease
ES2890492T3 (es) 2015-07-20 2022-01-20 Acadia Pharm Inc Métodos para preparar N-(4-fluorobencil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloxi)fenilmetil)carbamida y su sal de tartrato y forma polimórfica C
CN105111135A (zh) * 2015-09-09 2015-12-02 安徽省逸欣铭医药科技有限公司 取代的尿素衍生物制备方法
CN106543072A (zh) 2015-09-21 2017-03-29 天津市汉康医药生物技术有限公司 匹莫范色林化合物
CN105153016B (zh) * 2015-10-12 2017-10-03 北京诺康达医药科技有限公司 一种匹莫范色林的制备方法
CN105481757A (zh) * 2015-12-25 2016-04-13 北京康立生医药技术开发有限公司 一种哌马色林的制备方法
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
US20190117636A1 (en) 2016-03-29 2019-04-25 Acadia Pharmaceuticals Inc. 5-ht2a serotonin receptor inverse agonists or antagonists for use in reducing amyloid-beta peptides and accumulation of amyloid plaques
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
CN105820110B (zh) * 2016-05-09 2018-07-24 杭州科巢生物科技有限公司 匹莫范色林合成方法
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
EP3615028A1 (en) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
EP3675827A1 (en) 2017-08-30 2020-07-08 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
WO2019177973A1 (en) 2018-03-13 2019-09-19 Acadia Pharmaceuticals Inc. Methods for assessing suicidality
US20220016101A1 (en) 2018-10-30 2022-01-20 Acadia Pharmaceuticals Inc. Methods of treating depression, anxiety and sexual dysfunction using the compound pimavanserin
US20220288048A1 (en) 2019-07-22 2022-09-15 Acadia Pharmaceuticals Inc. Pimavanserin for treating schizophrenia or for treating psychosis secondary to neurodegenerative disorders or depressive disorder
US20220323429A1 (en) 2019-08-15 2022-10-13 Acadia Pharmaceuticals Inc. Pimavanserin for treating neurodegenerative diseases
US20210161880A1 (en) 2019-12-02 2021-06-03 Acadia Pharmaceuticals Inc. Methods for treating dementia related psychosis
WO2022094230A1 (en) 2020-11-02 2022-05-05 Acadia Pharmaceuticals Inc. Compounds for treating psychosis or depression

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