CN109563036A - 匹莫范色林酒石酸盐的新晶型及其制备方法和用途 - Google Patents

匹莫范色林酒石酸盐的新晶型及其制备方法和用途 Download PDF

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Publication number
CN109563036A
CN109563036A CN201780031372.2A CN201780031372A CN109563036A CN 109563036 A CN109563036 A CN 109563036A CN 201780031372 A CN201780031372 A CN 201780031372A CN 109563036 A CN109563036 A CN 109563036A
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CN
China
Prior art keywords
methyl
disease
luorobenzyl
base
propoxyl group
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Pending
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CN201780031372.2A
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English (en)
Inventor
孟晓明
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Shanghai Begreat Pharmatech
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Shanghai Begreat Pharmatech
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Publication of CN109563036A publication Critical patent/CN109563036A/zh
Pending legal-status Critical Current

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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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • 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

Abstract

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]脲酒石酸盐的新多晶型III及其制备方法和药用用途。与现有晶型相比，新晶型在溶解度、稳定性和制备工艺方面具有明显优势。

Description

PCT国内申请，说明书已公开。

Claims (5)

  1. PCT国内申请，权利要求书已公开。
CN201780031372.2A 2016-05-19 2017-05-19 匹莫范色林酒石酸盐的新晶型及其制备方法和用途 Pending CN109563036A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016103477793 2016-05-19
CN201610347779 2016-05-19
PCT/CN2017/084983 WO2018049836A1 (zh) 2016-05-19 2017-05-19 匹莫范色林酒石酸盐的新晶型及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN109563036A true CN109563036A (zh) 2019-04-02

Family

ID=61619042

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780031372.2A Pending CN109563036A (zh) 2016-05-19 2017-05-19 匹莫范色林酒石酸盐的新晶型及其制备方法和用途

Country Status (3)

Country Link
US (1) US10513495B2 (zh)
CN (1) CN109563036A (zh)
WO (1) WO2018049836A1 (zh)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101031548A (zh) * 2004-09-27 2007-09-05 阿卡蒂亚药品公司 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)脲的盐及其制备
CN101500568A (zh) * 2006-05-15 2009-08-05 阿卡蒂亚药品公司 匹莫范色林的药物制剂
CN104961672A (zh) * 2015-05-20 2015-10-07 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
CN104961671A (zh) * 2014-09-05 2015-10-07 苏州晶云药物科技有限公司 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)脲半酒石酸盐的晶型及其制备方法
CN105523993A (zh) * 2015-12-28 2016-04-27 重庆两江药物研发中心有限公司 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)脲酒石酸盐晶型c及制备应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US10343993B2 (en) * 2015-03-02 2019-07-09 Pliva Hrvatska D.O.O. Processes and intermediates for the preparation of Pimavanserin

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101031548A (zh) * 2004-09-27 2007-09-05 阿卡蒂亚药品公司 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)脲的盐及其制备
CN101500568A (zh) * 2006-05-15 2009-08-05 阿卡蒂亚药品公司 匹莫范色林的药物制剂
CN104961671A (zh) * 2014-09-05 2015-10-07 苏州晶云药物科技有限公司 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)脲半酒石酸盐的晶型及其制备方法
CN104961672A (zh) * 2015-05-20 2015-10-07 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
CN105523993A (zh) * 2015-12-28 2016-04-27 重庆两江药物研发中心有限公司 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)脲酒石酸盐晶型c及制备应用

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Publication number Publication date
WO2018049836A1 (zh) 2018-03-22
US20190084935A1 (en) 2019-03-21
US10513495B2 (en) 2019-12-24

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