CN101778821A - 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)脲及其酒石酸盐以及晶型的合成 - Google Patents
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)脲及其酒石酸盐以及晶型的合成 Download PDFInfo
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- CN101778821A CN101778821A CN200880021061A CN200880021061A CN101778821A CN 101778821 A CN101778821 A CN 101778821A CN 200880021061 A CN200880021061 A CN 200880021061A CN 200880021061 A CN200880021061 A CN 200880021061A CN 101778821 A CN101778821 A CN 101778821A
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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
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- 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
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/20—Hypnotics; Sedatives
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Hospice & Palliative Care (AREA)
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- Child & Adolescent Psychology (AREA)
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- Hydrogenated Pyridines (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/749,115 | 2007-05-15 | ||
| US11/749,115 US7790899B2 (en) | 2004-09-27 | 2007-05-15 | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
| PCT/US2008/063555 WO2008144326A2 (en) | 2007-05-15 | 2008-05-13 | Synthesis of n-(4-fluorobenzyl)-n-(l-methylpiperidin-4-yl)-n'-(4- (2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101778821A true CN101778821A (zh) | 2010-07-14 |
Family
ID=39595699
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200880021061A Pending CN101778821A (zh) | 2007-05-15 | 2008-05-13 | 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)脲及其酒石酸盐以及晶型的合成 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7790899B2 (https=) |
| EP (1) | EP2146960A2 (https=) |
| JP (1) | JP2010527371A (https=) |
| CN (1) | CN101778821A (https=) |
| AU (1) | AU2008254238A1 (https=) |
| CA (1) | CA2692001A1 (https=) |
| WO (1) | WO2008144326A2 (https=) |
Cited By (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| CN105153016A (zh) * | 2015-10-12 | 2015-12-16 | 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 |
| CN105418460A (zh) * | 2014-08-11 | 2016-03-23 | 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 |
| 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 |
| 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 |
| CN105820110A (zh) * | 2016-05-09 | 2016-08-03 | 杭州科巢生物科技有限公司 | 匹莫范色林新合成方法 |
| CN105859608A (zh) * | 2016-05-27 | 2016-08-17 | 成都百裕制药股份有限公司 | 一种制备哌马色林半酒石酸盐晶型b的方法 |
| CN106008323A (zh) * | 2016-05-30 | 2016-10-12 | 成都百裕制药股份有限公司 | 一种制备哌马色林半酒石酸盐晶型c的方法 |
| CN106916098A (zh) * | 2017-03-07 | 2017-07-04 | 江苏艾立康药业股份有限公司 | 一种哌马色林单酒石酸盐半水合物及制备方法 |
| CN107011137A (zh) * | 2017-04-10 | 2017-08-04 | 杭州科耀医药科技有限公司 | 一种匹莫范色林中间体的合成方法 |
| CN107216271A (zh) * | 2017-06-02 | 2017-09-29 | 沈阳药科大学 | 酒石酸匹莫范色林杂质及其制备方法 |
| WO2020020064A1 (zh) * | 2018-07-26 | 2020-01-30 | 丽珠集团新北江制药股份有限公司 | 利用三光气安全制备匹莫范色林及其酒石酸盐的方法 |
| CN111132976A (zh) * | 2017-08-21 | 2020-05-08 | 阿卡蒂亚药品公司 | 化合物、其盐和用于治疗疾病的方法 |
| CN111479803A (zh) * | 2017-11-06 | 2020-07-31 | 欧伦股份公司 | 匹莫范色林半酒石酸盐的无定形形式 |
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| DK2009000T3 (da) | 2003-01-16 | 2011-09-05 | Acadia Pharm Inc | Selektive serotonin 2A/2C-receptor invers-agonister som terapeutika for neurodegenerative sygdomme |
| 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 |
| CA2580129A1 (en) * | 2004-09-27 | 2006-04-06 | Acadia Pharmaceuticals Inc. | Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation |
| WO2014085362A1 (en) | 2012-11-27 | 2014-06-05 | Acadia Pharmaceuticals Inc. | Methods for the treatment of parkinson's disease psychosis using pimavanserin |
| WO2016141003A1 (en) | 2015-03-02 | 2016-09-09 | Teva Pharmaceutical Industries Ltd. | Processes and intermediates for the preparation of pimavanserin |
| 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 |
| CN106588753B (zh) * | 2015-10-19 | 2021-07-09 | 重庆医药工业研究院有限责任公司 | 一种制备匹马色林的方法 |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
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| CN109563036A (zh) * | 2016-05-19 | 2019-04-02 | 上海诚妙医药科技有限公司 | 匹莫范色林酒石酸盐的新晶型及其制备方法和用途 |
| HU231097B1 (hu) * | 2016-07-08 | 2020-08-28 | Egis Gyógyszergyár Zrt. | Gyógyászati készítmény előállítására alkalmazható pimavanserin sók |
| 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 |
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| CN109734652A (zh) * | 2019-03-07 | 2019-05-10 | 夸克侠医药科技(辽宁)有限公司 | 一种高纯度匹莫范色林的制备方法 |
| ES2908812T3 (es) | 2019-04-17 | 2022-05-04 | Zakl Farmaceutyczne Polpharma S A | Proceso para la preparación de un agente farmacéutico |
| ES2906868T3 (es) | 2019-05-22 | 2022-04-20 | Zakl Farmaceutyczne Polpharma S A | Intermedio farmacéutico para preparar pimavanserina |
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Also Published As
| Publication number | Publication date |
|---|---|
| US20070260064A1 (en) | 2007-11-08 |
| AU2008254238A1 (en) | 2008-11-27 |
| WO2008144326A3 (en) | 2009-03-26 |
| WO2008144326A2 (en) | 2008-11-27 |
| EP2146960A2 (en) | 2010-01-27 |
| CA2692001A1 (en) | 2008-11-27 |
| JP2010527371A (ja) | 2010-08-12 |
| US7790899B2 (en) | 2010-09-07 |
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