CA2992728A1 - 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 - Google Patents

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 Download PDF

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Publication number
CA2992728A1
CA2992728A1 CA2992728A CA2992728A CA2992728A1 CA 2992728 A1 CA2992728 A1 CA 2992728A1 CA 2992728 A CA2992728 A CA 2992728A CA 2992728 A CA2992728 A CA 2992728A CA 2992728 A1 CA2992728 A1 CA 2992728A1
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Canada
Prior art keywords
substituted
pimavanserin
group
unsubstituted
formula
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CA2992728A
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English (en)
French (fr)
Inventor
Marlon Carlos
Sagun Tandel
Roger Olsson
Mikael HILLGREN
Matthew J. Fleming
Andreas Philipp Boudier
Beat T. Weber
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Acadia Pharmaceuticals Inc
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Acadia Pharmaceuticals Inc
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Publication of CA2992728A1 publication Critical patent/CA2992728A1/en
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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (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)
CA2992728A 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 Pending CA2992728A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2992728A1 true CA2992728A1 (en) 2017-01-26

Family

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CA2992728A Pending CA2992728A1 (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

Country Status (13)

Country Link
US (4) US10597363B2 (enExample)
EP (1) EP3325444B1 (enExample)
JP (1) JP6850282B2 (enExample)
CN (1) CN107848972B (enExample)
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)
SI (1) SI3325444T1 (enExample)
WO (1) WO2017015272A1 (enExample)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
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

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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
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
EP3558311A1 (en) 2016-12-20 2019-10-30 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
US11135211B2 (en) 2017-04-28 2021-10-05 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
EP3672960A2 (en) * 2017-08-21 2020-07-01 Acadia Pharmaceuticals Inc. Compounds, salts thereof and their use for the treatment of diseases
WO2019040106A2 (en) * 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, RELATED SALTS AND METHODS FOR THE TREATMENT OF DISEASES
MX2020001757A (es) 2017-08-21 2020-09-07 Acadia Pharm Inc Compuestos, sales de los mismos y metodos para el tratamiento de enfermedades.
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. PIMAVANSERIN FORMULATIONS
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
WO2019207494A1 (en) * 2018-04-26 2019-10-31 Olon S.P.A. Method for the preparation of pimavanserin base
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
WO2020092618A1 (en) 2018-10-30 2020-05-07 Acadia Pharmaceuticals Inc. Methods of treating depression, anxiety and sexual dysfunction using the compound primavanserin
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
WO2021016369A1 (en) 2019-07-22 2021-01-28 Acadia Pharmaceuticals Inc. Pimavanserin for trating schizophrenia or for treating psychosis secondary to neurodegenerative disorders or depressive disorder
WO2021030607A1 (en) 2019-08-15 2021-02-18 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

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