JP6850282B2 - Ｎ−（４−フルオロベンジル）−ｎ−（１−メチルピペリジン−４−イル）−ｎ’−（４−（２−メチルプロピルオキシ）フェニルメチル）カルバミドならびにその酒石酸塩および多形形態ｃを調製する方法 - Google Patents

Ｎ−（４−フルオロベンジル）−ｎ−（１−メチルピペリジン−４−イル）−ｎ’−（４−（２−メチルプロピルオキシ）フェニルメチル）カルバミドならびにその酒石酸塩および多形形態ｃを調製する方法 Download PDF

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JP6850282B2
JP6850282B2 JP2018502212A JP2018502212A JP6850282B2 JP 6850282 B2 JP6850282 B2 JP 6850282B2 JP 2018502212 A JP2018502212 A JP 2018502212A JP 2018502212 A JP2018502212 A JP 2018502212A JP 6850282 B2 JP6850282 B2 JP 6850282B2
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pimavanserin
substituted
group
tartrate
formula
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JP2018522012A5 (enExample
JP2018522012A (ja
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カルロス，マーロン
タンデル，サグン
オルソン，ロジャー
ヒルグレン，ミカエル
フレミング，マシュー，ジェイ．
ブーディエ，アンドレアス，フィリップ
ウェーバー，ビート，ティー．
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アカディア ファーマシューティカルズ インコーポレーテッド
アカディア ファーマシューティカルズ インコーポレーテッド
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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)
JP2018502212A 2015-07-20 2016-07-19 Ｎ−（４−フルオロベンジル）−ｎ−（１−メチルピペリジン−４−イル）−ｎ’−（４−（２−メチルプロピルオキシ）フェニルメチル）カルバミドならびにその酒石酸塩および多形形態ｃを調製する方法 Active JP6850282B2 (ja)

Applications Claiming Priority (3)

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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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JP2018522012A JP2018522012A (ja) 2018-08-09
JP2018522012A5 JP2018522012A5 (enExample) 2019-08-08
JP6850282B2 true JP6850282B2 (ja) 2021-03-31

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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)

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WO2019040106A2 (en) * 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, RELATED SALTS AND METHODS FOR THE TREATMENT OF DISEASES
US11440884B2 (en) 2017-08-21 2022-09-13 Acadia Pharmaceuticals Inc. Compounds, salts thereof and methods for treatment of diseases
WO2019040107A1 (en) 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, CORRESPONDING SALTS AND METHODS FOR THE TREATMENT OF DISEASES
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
US11319288B2 (en) 2018-04-26 2022-05-03 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
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
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
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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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