KR101260036B1 - N-(4-플루오로벤질)-n-(1-메틸피페리딘-4-일)-n'-(4-(2-메틸프로필옥시)페닐메틸)카르바미드와그의 타르트레이트염 및 결정형의 합성 - Google Patents
N-(4-플루오로벤질)-n-(1-메틸피페리딘-4-일)-n'-(4-(2-메틸프로필옥시)페닐메틸)카르바미드와그의 타르트레이트염 및 결정형의 합성 Download PDFInfo
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- KR101260036B1 KR101260036B1 KR1020077009394A KR20077009394A KR101260036B1 KR 101260036 B1 KR101260036 B1 KR 101260036B1 KR 1020077009394 A KR1020077009394 A KR 1020077009394A KR 20077009394 A KR20077009394 A KR 20077009394A KR 101260036 B1 KR101260036 B1 KR 101260036B1
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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
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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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
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61401404P | 2004-09-27 | 2004-09-27 | |
| US60/614,014 | 2004-09-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20070083799A KR20070083799A (ko) | 2007-08-24 |
| KR101260036B1 true KR101260036B1 (ko) | 2013-05-06 |
Family
ID=35539440
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020077009394A Active KR101260036B1 (ko) | 2004-09-27 | 2005-09-26 | N-(4-플루오로벤질)-n-(1-메틸피페리딘-4-일)-n'-(4-(2-메틸프로필옥시)페닐메틸)카르바미드와그의 타르트레이트염 및 결정형의 합성 |
| KR1020077009395A Withdrawn KR20070083800A (ko) | 2004-09-27 | 2005-09-26 | N-(4-플루오로벤질)-n-(1-메틸피페리딘-4-일)-n'-(4-(2-메틸프로필옥시)페닐메틸)카르바미드의염류 및 이들의 제조 방법 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020077009395A Withdrawn KR20070083800A (ko) | 2004-09-27 | 2005-09-26 | N-(4-플루오로벤질)-n-(1-메틸피페리딘-4-일)-n'-(4-(2-메틸프로필옥시)페닐메틸)카르바미드의염류 및 이들의 제조 방법 |
Country Status (17)
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|---|---|
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| EP (3) | EP2289879B1 (enExample) |
| JP (2) | JP4996467B2 (enExample) |
| KR (2) | KR101260036B1 (enExample) |
| CN (3) | CN102153505B (enExample) |
| AU (2) | AU2005289635A1 (enExample) |
| BR (1) | BRPI0516063A (enExample) |
| CA (2) | CA2580136C (enExample) |
| DK (1) | DK1794126T3 (enExample) |
| ES (2) | ES2530258T3 (enExample) |
| MX (2) | MX2007003433A (enExample) |
| NZ (1) | NZ553702A (enExample) |
| PL (2) | PL1794126T3 (enExample) |
| RU (2) | RU2417986C2 (enExample) |
| SG (2) | SG161221A1 (enExample) |
| WO (2) | WO2006036874A1 (enExample) |
| ZA (3) | ZA200702349B (enExample) |
Families Citing this family (73)
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| MXPA02008770A (es) * | 2000-03-06 | 2004-09-10 | Acadia Pharm Inc | Compuestos azaciclicos para uso en el tratamiento de enfermedades relacionadas con la serotonina. |
| MXPA04006280A (es) | 2001-12-28 | 2004-09-27 | Acadia Pharm Inc | Compuestos espiroazaciclicos como moduladores de receptor de monoamina. |
| 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 |
| MY139563A (en) * | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| US7601740B2 (en) * | 2003-01-16 | 2009-10-13 | Acadia Pharmaceuticals, Inc. | Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases |
| US20050261278A1 (en) * | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US7820695B2 (en) | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
| CN102153505B (zh) * | 2004-09-27 | 2014-10-22 | 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)脲及其酒石酸盐的合成和晶形 |
| 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 |
| WO2007124136A1 (en) * | 2006-04-19 | 2007-11-01 | Acadia Pharmaceuticals, Inc. | Use of 4-amino-piperidines for treating sleep disorders |
| WO2007133802A2 (en) * | 2006-05-15 | 2007-11-22 | Acadia Pharmaceuticals Inc. | Pharmaceutical formulations of pimavanserin |
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| NO2200610T3 (enExample) * | 2007-09-21 | 2018-06-09 | ||
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| TW201018668A (en) * | 2008-06-30 | 2010-05-16 | Janssen Pharmaceutica Nv | Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| AR091507A1 (es) * | 2012-06-21 | 2015-02-11 | Intra Cellular Therapies Inc | SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA |
| WO2014085362A1 (en) | 2012-11-27 | 2014-06-05 | Acadia Pharmaceuticals Inc. | Methods for the treatment of parkinson's disease psychosis using pimavanserin |
| EP3702358A1 (en) * | 2013-06-21 | 2020-09-02 | Intra-Cellular Therapies, Inc. | Process for preparing salts of a known pde1 inhibitor |
| JP2015117192A (ja) * | 2013-12-17 | 2015-06-25 | 東和薬品株式会社 | シロドシンγ型結晶及びその製造方法 |
| CN104961671B (zh) * | 2014-09-05 | 2018-01-02 | 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 |
| 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 |
| CN107848972B (zh) | 2015-07-20 | 2021-06-18 | 阿卡蒂亚药品公司 | 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 |
| CZ2015601A3 (cs) | 2015-09-02 | 2017-03-15 | Zentiva, K.S. | Způsob výroby 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)močoviny a jejích deuterovaných analog neobsahujících dimerické nečistoty |
| 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 |
| CZ2015688A3 (cs) | 2015-10-02 | 2017-04-12 | Zentiva, K.S. | Způsob výroby 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)močoviny a jeho deuterovaných analogů |
| 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 |
| 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 |
| CN106699637A (zh) * | 2015-11-17 | 2017-05-24 | 重庆医药工业研究院有限责任公司 | 一种匹马色林单酒石酸盐晶型及其制备方法 |
| CN105924381B (zh) * | 2015-12-18 | 2019-04-16 | 重庆两江药物研发中心有限公司 | 一种哌马色林晶型c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 |
| 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 |
| CN107021917B (zh) * | 2016-02-02 | 2020-08-04 | 江苏恩华药业股份有限公司 | 哌马色林半酒石酸盐的新晶型及其制备方法 |
| 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 |
| 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 |
| 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 |
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| CA3067162A1 (en) | 2017-06-12 | 2018-12-20 | Glytech Llc. | Treatment of depression with nmda antagonists and d2/5ht2a or selective 5ht2a antagonists |
| RS67273B1 (sr) * | 2017-08-21 | 2025-10-31 | Acadia Pharm Inc | Jedinjenja, njihove soli i njihova upotreba u lečenju bolesti |
| WO2019040104A2 (en) | 2017-08-21 | 2019-02-28 | Acadia Pharmaceuticals Inc. | COMPOUNDS, RELATED SALTS AND METHODS OF TREATING DISEASES |
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