CN101031548B - 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 - 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)脲的盐及其制备 Download PDFInfo
- Publication number
- CN101031548B CN101031548B CN2005800326490A CN200580032649A CN101031548B CN 101031548 B CN101031548 B CN 101031548B CN 2005800326490 A CN2005800326490 A CN 2005800326490A CN 200580032649 A CN200580032649 A CN 200580032649A CN 101031548 B CN101031548 B CN 101031548B
- Authority
- CN
- China
- Prior art keywords
- formula
- crystalline
- salt
- acid
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 0 CC(C)COc(cc1)ccc1Cl(C)NC(N(Cc(cc1)ccc1F)C1CC[N+](*)CC1)=O Chemical compound CC(C)COc(cc1)ccc1Cl(C)NC(N(Cc(cc1)ccc1F)C1CC[N+](*)CC1)=O 0.000 description 2
- MLZAYWZRBULEIK-UHFFFAOYSA-O CC(C)COc1ccc(C(C)NC(N(C2CC[NH+](C)CC2)Nc(cc2)ccc2F)=O)cc1 Chemical compound CC(C)COc1ccc(C(C)NC(N(C2CC[NH+](C)CC2)Nc(cc2)ccc2F)=O)cc1 MLZAYWZRBULEIK-UHFFFAOYSA-O 0.000 description 1
- RKEWSXXUOLRFBX-UHFFFAOYSA-N CC(C)COc1ccc(CNC(N(Cc(cc2)ccc2F)C2CCN(C)CC2)=O)cc1 Chemical compound CC(C)COc1ccc(CNC(N(Cc(cc2)ccc2F)C2CCN(C)CC2)=O)cc1 RKEWSXXUOLRFBX-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
-
- 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
- A61P25/18—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
-
- 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
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (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)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61401404P | 2004-09-27 | 2004-09-27 | |
| US60/614,014 | 2004-09-27 | ||
| PCT/US2005/034376 WO2006036874A1 (en) | 2004-09-27 | 2005-09-26 | Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101031548A CN101031548A (zh) | 2007-09-05 |
| CN101031548B true CN101031548B (zh) | 2011-04-06 |
Family
ID=35539440
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800326490A Expired - Lifetime CN101031548B (zh) | 2004-09-27 | 2005-09-26 | 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 |
| CN2005800326503A Expired - Lifetime CN101035759B (zh) | 2004-09-27 | 2005-09-26 | 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 |
| CN201110039289.4A Expired - Lifetime CN102153505B (zh) | 2004-09-27 | 2005-09-26 | 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800326503A Expired - Lifetime CN101035759B (zh) | 2004-09-27 | 2005-09-26 | 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 |
| CN201110039289.4A Expired - Lifetime CN102153505B (zh) | 2004-09-27 | 2005-09-26 | 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 |
Country Status (17)
| Country | Link |
|---|---|
| US (6) | US7868176B2 (https=) |
| EP (3) | EP2289879B1 (https=) |
| JP (2) | JP4996467B2 (https=) |
| KR (2) | KR101260036B1 (https=) |
| CN (3) | CN101031548B (https=) |
| AU (2) | AU2005289635A1 (https=) |
| BR (1) | BRPI0516063A (https=) |
| CA (2) | CA2580136C (https=) |
| DK (1) | DK1794126T3 (https=) |
| ES (2) | ES2412207T3 (https=) |
| MX (2) | MX2007003433A (https=) |
| NZ (1) | NZ553702A (https=) |
| PL (2) | PL2289879T3 (https=) |
| RU (2) | RU2417986C2 (https=) |
| SG (2) | SG157378A1 (https=) |
| WO (2) | WO2006037043A1 (https=) |
| ZA (3) | ZA200702345B (https=) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2002126554A (ru) * | 2000-03-06 | 2004-03-20 | Акадиа Фармасьютикалз, Инк. (Us) | Азациклические соединения для применения при лечении опосредованных серотонином заболеваний |
| WO2003057698A2 (en) * | 2001-12-28 | 2003-07-17 | Acadia Pharmaceuticals, Inc. | Spiroazacyclic compounds as monoamine receptor modulators |
| CN100509804C (zh) | 2002-06-24 | 2009-07-08 | 阿卡蒂亚药品公司 | N-取代哌啶衍生物作为血清素受体试剂 |
| US7253186B2 (en) * | 2002-06-24 | 2007-08-07 | Carl-Magnus Andersson | N-substituted piperidine derivatives as serotonin receptor agents |
| US7538222B2 (en) | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | 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 |
| PT1587789E (pt) | 2003-01-16 | 2008-12-16 | Acadia Pharm Inc | Agonistas inversos selectivos para receptores 2a/2c da serotonina como agentes terapêuticos para doenças neurodegenerativas |
| 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 |
| 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 |
| JP4996467B2 (ja) * | 2004-09-27 | 2012-08-08 | アカディア ファーマシューティカルズ インコーポレイテッド | 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、並びにその酒石酸塩及び結晶形態の合成 |
| WO2007124136A1 (en) * | 2006-04-19 | 2007-11-01 | Acadia Pharmaceuticals, Inc. | Use of 4-amino-piperidines for treating sleep disorders |
| EP2037918A2 (en) * | 2006-05-15 | 2009-03-25 | Acadia Pharmaceuticals Inc. | Pharmaceutical formulations of pimavanserin |
| HRP20130713T1 (en) | 2007-03-19 | 2013-09-30 | Acadia Pharmaceuticals Inc. | Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics |
| WO2008141057A1 (en) * | 2007-05-08 | 2008-11-20 | Auspex Pharmaceuticals, Inc. | Deuterated pimavanserin 1- (4-flu0r0benzyl) -3- (4-isobutoxybenzyl) -1- ( l-methyl-piperidin-4-yl) -urea |
| AU2008254669A1 (en) * | 2007-05-18 | 2008-11-27 | Acadia Pharmaceuticals Inc. | Use of pimavanserin in the treatment of parkinson and symptoms thereof |
| WO2009039461A2 (en) * | 2007-09-21 | 2009-03-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| JP2010540454A (ja) * | 2007-09-21 | 2010-12-24 | 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 | ピマバンセリンと他の薬剤との併用投与 |
| US20100029942A1 (en) * | 2008-06-30 | 2010-02-04 | Sergio Cesco-Cancian | 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 |
| US9446037B2 (en) | 2012-11-27 | 2016-09-20 | Acadia Pharmaceuticals Inc. | Methods for the treatment of parkinson's disease psychosis using pimavanserin |
| US9630971B2 (en) * | 2013-06-21 | 2017-04-25 | Intra-Cellular Therapies, Inc. | Free base crystals |
| 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 |
| WO2016141003A1 (en) | 2015-03-02 | 2016-09-09 | Teva Pharmaceutical Industries Ltd. | 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 |
| PL3325444T3 (pl) * | 2015-07-20 | 2021-12-06 | Acadia Pharmaceuticals Inc. | Sposoby wytwarzania N-(4-fluorobenzylo)-N-(1-metylopiperydyn-4-ylo)-N'-(4-(2-metylopropyloksy)fenylometylo)karbamidu oraz jego soli winianowej i postaci polimorficznej C |
| 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 |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
| WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | 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 |
| CN105859608B (zh) * | 2016-05-27 | 2018-12-28 | 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 |
| HU231097B1 (hu) * | 2016-07-08 | 2020-08-28 | Egis Gyógyszergyár Zrt. | Gyógyászati készítmény előállítására alkalmazható pimavanserin sók |
| EP3517529B1 (en) * | 2016-09-23 | 2022-03-23 | Shanghai Pharmaceuticals Holding Co., Ltd. | Salt of quinazoline derivative, preparation method therefor and application thereof |
| 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 |
| US20180208556A1 (en) | 2017-01-20 | 2018-07-26 | Sci Pharmtech, Inc. | Method for Preparing Pimavanserin |
| 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 |
| WO2018200977A1 (en) | 2017-04-28 | 2018-11-01 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
| CA3064846A1 (en) | 2017-05-25 | 2018-11-29 | Glytech, Llc | Combined therapy for nmdar antagonist-responsive neuropsychiatric disorders |
| CN107216271B (zh) * | 2017-06-02 | 2018-11-13 | 沈阳药科大学 | 酒石酸匹莫范色林杂质及其制备方法 |
| MX393950B (es) | 2017-06-12 | 2025-03-24 | Glytech Llc | Composicion y metodo para el tratamiento de la depresion y psicosis en humanos |
| SG11202001062XA (en) * | 2017-08-21 | 2020-03-30 | Acadia Pharm Inc | Compounds, salts thereof and methods for treatment of diseases |
| WO2019040104A2 (en) | 2017-08-21 | 2019-02-28 | Acadia Pharmaceuticals Inc. | COMPOUNDS, RELATED SALTS AND METHODS OF TREATING DISEASES |
| WO2019046167A1 (en) | 2017-08-30 | 2019-03-07 | Acadia Pharmaceuticals Inc. | PIMAVANSERIN FORMULATIONS |
| JP2018035199A (ja) * | 2017-12-07 | 2018-03-08 | 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 |
| WO2019120250A1 (zh) * | 2017-12-22 | 2019-06-27 | 广东东阳光药业有限公司 | 一种哌马色林半酒石酸盐的新晶型及其制备方法 |
| IT201800003736A1 (it) | 2018-03-19 | 2019-09-19 | Lundbeck Pharmaceuticals Italy S P A | Processo per la produzione di Pimavanserin |
| IT201800009690A1 (it) | 2018-10-23 | 2020-04-23 | Lundbeck Pharmaceuticals Italy Spa | Processo per la produzione di pimavanserina |
| US20220016101A1 (en) | 2018-10-30 | 2022-01-20 | Acadia Pharmaceuticals Inc. | Methods of treating depression, anxiety and sexual dysfunction using the compound pimavanserin |
| CN111320568B (zh) * | 2018-12-15 | 2021-12-07 | 浙江京新药业股份有限公司 | 一种匹莫范色林的新晶型及其制备方法 |
| ES2906868T3 (es) * | 2019-05-22 | 2022-04-20 | Zakl Farmaceutyczne Polpharma S A | Intermedio farmacéutico para preparar pimavanserina |
| US20220288048A1 (en) | 2019-07-22 | 2022-09-15 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating schizophrenia or for treating psychosis secondary to neurodegenerative disorders or depressive disorder |
| US20220323429A1 (en) | 2019-08-15 | 2022-10-13 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating neurodegenerative diseases |
| CN114867473A (zh) | 2019-11-08 | 2022-08-05 | 凯莫森特里克斯股份有限公司 | 补体成分c5a受体的盐形式 |
| US11603356B2 (en) * | 2019-11-08 | 2023-03-14 | Chemocentryx, Inc. | Amorphous form of a complement component C5a receptor |
| JP2022554019A (ja) | 2019-11-08 | 2022-12-27 | ケモセントリックス,インコーポレイティド | 補体成分C5a受容体の遊離塩基結晶形態 |
| CN113214231B (zh) * | 2020-01-21 | 2022-04-08 | 瀚远医药有限公司 | 5ht2a受体拮抗剂及其医疗应用 |
| WO2022094230A1 (en) | 2020-11-02 | 2022-05-05 | Acadia Pharmaceuticals Inc. | Compounds for treating psychosis or depression |
| CN112920108A (zh) * | 2021-01-29 | 2021-06-08 | 北京诺康达医药科技股份有限公司 | 酒石酸匹莫范色林晶型a的制备方法 |
| CN114874103B (zh) * | 2022-05-11 | 2024-09-06 | 合肥立方制药股份有限公司 | 一种匹莫范色林中间体4-异丁氧基苄胺的连续合成方法 |
| JP7406285B1 (ja) | 2023-03-09 | 2023-12-27 | 国立大学法人島根大学 | ビリルビン誘発性神経機能障害、黄疸を伴う精神疾患、又はビリルビンudp-グルクロン酸転移酵素遺伝子変異に起因する精神疾患を治療、予防又は管理するための医薬組成物 |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE794333A (fr) | 1972-01-20 | 1973-07-19 | Wyeth John & Brother Ltd | Composes heterocycliques azotes therapeutiques |
| GB1507462A (en) * | 1974-03-21 | 1978-04-12 | Gallardo Antonio Sa | N-heterocyclic substituted benzamides methods for their preparation and compositions containing them |
| US3983234A (en) * | 1974-07-04 | 1976-09-28 | Sandoz Ltd. | Treatment of dyskinesias |
| GB1586468A (en) | 1976-10-29 | 1981-03-18 | Anphar Sa | Piperidine derivatives |
| CA1140119A (en) | 1978-04-03 | 1983-01-25 | Joseph Torremans | N-heterocyclyl-4-piperidinamines |
| US4255432A (en) * | 1979-09-06 | 1981-03-10 | Syntex (U.S.A.) Inc. | 8-[2-3-Indolyl)ethyl]-1-oxa-3-,8-diazaspiro[4.5]decan-2-ones, pharmaceutical compositions thereof and methods of use thereof |
| US4332804A (en) * | 1981-03-23 | 1982-06-01 | Syntex (U.S.A.) Inc. | 9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones |
| US4353900A (en) | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(Arylalkyl or aroylalkyl)-1-oxa-4,9-diazaspiro(5.5)undecan-3-ones |
| US4353901A (en) | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones |
| GB8527052D0 (en) | 1985-11-02 | 1985-12-04 | Beecham Group Plc | Compounds |
| GB8621892D0 (en) | 1986-09-11 | 1986-10-15 | Lundbeck & Co As H | Organic compound |
| FR2642069B1 (fr) * | 1989-01-20 | 1991-04-12 | Rhone Poulenc Sante | Nouveaux derives du benzopyranne, leur preparation et les compositions pharmaceutiques qui les contiennent |
| US5214055A (en) * | 1990-05-18 | 1993-05-25 | Adir Et Compagnie | Aminopiperidine 4-oxo-4H-chromen-2-yl compounds |
| US5216165A (en) | 1990-10-03 | 1993-06-01 | American Home Products Corporation | N-substituted aminoquinolines as analgesic agents |
| IT1252227B (it) | 1991-12-17 | 1995-06-05 | Ciba Geigy Spa | Composti tetrametilpiperidinici atti all'impiego come stabilizzanti per materiali organici |
| US5595872A (en) * | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| CA2123728A1 (en) | 1993-05-21 | 1994-11-22 | Noriyoshi Sueda | Urea derivatives and their use as acat inhibitors |
| JPH09501404A (ja) | 1993-05-26 | 1997-02-10 | スミスクライン・ビーチャム・ラボラトワール・ファルマソーティク | 新規化合物 |
| IL110298A (en) | 1993-07-13 | 1999-04-11 | Brann Mark Robert | Identification of ligands by selective amplification of cells transfected with receptors |
| DE4404183A1 (de) | 1994-02-10 | 1995-08-17 | Merck Patent Gmbh | 4-Amino-1-piperidylbenzoylguanidine |
| US5795894A (en) * | 1995-05-02 | 1998-08-18 | Schering Corporation | Piperazino derivatives as neurokinn antagonists |
| BR9610277A (pt) | 1995-08-31 | 1999-07-06 | Schering Corp | Derivados de piperazino como antagonistas de neurowuinina |
| WO1997011940A1 (en) | 1995-09-29 | 1997-04-03 | Eli Lilly And Company | Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation |
| EP0944388A4 (en) | 1996-04-03 | 2001-08-16 | Merck & Co Inc | INHIBITORS OF FARNESYL PROTEIN TRANSFERASE |
| EP0960104B1 (en) | 1996-04-17 | 2004-06-16 | Bristol-Myers Squibb Pharma Company | N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-one derivatives as factor xa inhibitors |
| US5869488A (en) | 1996-05-01 | 1999-02-09 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5877173A (en) | 1996-08-28 | 1999-03-02 | Washington University | Preventing neuronal degeneration in Alzheimer's disease |
| SK285631B6 (sk) | 1996-09-10 | 2007-05-03 | Dr. Karl Thomae Gmbh | Modifikované aminokyseliny, farmaceutický prostriedok s ich obsahom a ich použitie |
| DE19643331A1 (de) | 1996-10-21 | 1998-04-23 | Thomae Gmbh Dr K | 1-(4-Piperidinyl)-piperidinylene, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US6057338A (en) | 1997-04-04 | 2000-05-02 | Merck & Co., Inc. | Somatostatin agonists |
| TR199902752T2 (xx) | 1997-05-08 | 2000-06-21 | Smithkline Beecham Corporation | Proteaz inhibit�rleri. |
| CA2291734A1 (en) * | 1997-06-27 | 1999-01-07 | Merck Sharp & Dohme Limited | Substituted 3-(benzylamino)piperidine derivatives and their use as therapeutic agents |
| US20020163987A1 (en) * | 1997-12-12 | 2002-11-07 | British Nuclear Fuels Plc | Monitoring a sample containing a neutron source |
| US6107324A (en) * | 1998-04-14 | 2000-08-22 | Arena Pharmaceuticals Inc. | 5-HT2A receptor inverse agonists |
| US6140509A (en) | 1998-06-26 | 2000-10-31 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof |
| US6358698B1 (en) | 1998-10-07 | 2002-03-19 | Acadia Pharmacueticals Inc. | Methods of identifying inverse agonists of the serotonin 2A receptor |
| CA2315050C (en) | 1998-10-16 | 2009-02-03 | Suntory Limited | Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof |
| US6150393A (en) | 1998-12-18 | 2000-11-21 | Arena Pharmaceuticals, Inc. | Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors |
| EP1013276A1 (en) * | 1998-12-23 | 2000-06-28 | Pfizer Inc. | Aminoazacycloalkanes as CCR5 modulators |
| JP2002539260A (ja) | 1999-03-24 | 2002-11-19 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | アスパルチルプロテアーゼインヒビターを使用して神経変性障害を処置する方法 |
| US6399619B1 (en) | 1999-04-06 | 2002-06-04 | Merck & Co., Inc. | Pyrrolidine modulators of chemokine receptor activity |
| DE60023492T2 (de) | 1999-05-17 | 2006-07-20 | Novo Nordisk A/S | Glucagon antagonisten/inverse agonisten |
| US20050148018A1 (en) * | 1999-10-07 | 2005-07-07 | David Weiner | Methods of identifying inverse agonists of the serotonin 2A receptor |
| FR2802206B1 (fr) | 1999-12-14 | 2005-04-22 | Sod Conseils Rech Applic | Derives de 4-aminopiperidine et leur utilisation en tant que medicament |
| US7022698B2 (en) * | 1999-12-28 | 2006-04-04 | U & I Pharmaceuticals, Ltd. | Pharmaceutical compositions containing new polymorphic forms of olanzapine and uses thereof |
| RU2002126554A (ru) * | 2000-03-06 | 2004-03-20 | Акадиа Фармасьютикалз, Инк. (Us) | Азациклические соединения для применения при лечении опосредованных серотонином заболеваний |
| GB0011838D0 (en) * | 2000-05-17 | 2000-07-05 | Astrazeneca Ab | Chemical compounds |
| GB0108099D0 (en) | 2001-03-30 | 2001-05-23 | Hoffmann La Roche | Aminopiperidine derivatives |
| EP1402871B1 (en) * | 2001-06-05 | 2009-02-18 | Toyo Boseki Kabushiki Kaisha | Antithrombotic compositions and medical instruments containing the same |
| WO2003057698A2 (en) * | 2001-12-28 | 2003-07-17 | Acadia Pharmaceuticals, Inc. | Spiroazacyclic compounds as monoamine receptor modulators |
| KR20040075353A (ko) | 2002-01-17 | 2004-08-27 | 제너럴 일렉트릭 캄파니 | 양이온성 개시제로서 약하게 배위된 이미다졸리딘음이온을 포함하는 오늄 염 |
| EP1509505A2 (en) | 2002-01-23 | 2005-03-02 | Arena Pharmaceuticals, Inc. | SMALL MOLECULE MODULATORS OF THE 5−HT2A SEROTONIN RECEPTOR USEFUL FOR THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO |
| UY27668A1 (es) | 2002-02-20 | 2003-10-31 | Pfizer Prod Inc | Composición de ziprasidona y controles sintéticos |
| GB0208279D0 (en) | 2002-04-10 | 2002-05-22 | Glaxo Group Ltd | Novel compounds |
| 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 |
| CN100509804C (zh) | 2002-06-24 | 2009-07-08 | 阿卡蒂亚药品公司 | N-取代哌啶衍生物作为血清素受体试剂 |
| WO2004009549A2 (en) | 2002-07-18 | 2004-01-29 | Actelion Pharmaceuticals Ltd | Piperidines useful for the treatment of central nervous system disorders |
| AU2003284899A1 (en) | 2002-10-29 | 2004-05-25 | Miicro, Inc. | Novel combination therapy for schizophrenia focused on improved cognition: 5-ht-2a/d2 blockade with adjunctive blockade of prefrontal da reuptake |
| PT1587789E (pt) * | 2003-01-16 | 2008-12-16 | Acadia Pharm Inc | Agonistas inversos selectivos para receptores 2a/2c da serotonina como agentes terapêuticos para doenças neurodegenerativas |
| JP2006515628A (ja) * | 2003-01-23 | 2006-06-01 | 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 | ヒト神経精神疾患を処置するためのn−デスメチルクロザピンの使用 |
| SI1594840T1 (sl) | 2003-02-17 | 2006-12-31 | Hoffmann La Roche | Derivati piperidin-benzensulfonamida |
| US7628762B2 (en) | 2003-03-19 | 2009-12-08 | Suros Surgical Systems, Inc. | Adapter assembly for stereotactic biopsy |
| PT1696931E (pt) * | 2003-12-22 | 2009-06-12 | Acadia Pharm Inc | Análogos diaril[a,d]ciclo-hepteno substituídos com amino utilizados como agonistas muscarínicos e métodos de tratamento de perturbações neuropsiquiátricas |
| US7820695B2 (en) * | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US20050261278A1 (en) * | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
| JP4996467B2 (ja) * | 2004-09-27 | 2012-08-08 | アカディア ファーマシューティカルズ インコーポレイテッド | 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、並びにその酒石酸塩及び結晶形態の合成 |
| 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 |
-
2005
- 2005-09-26 JP JP2007533762A patent/JP4996467B2/ja not_active Expired - Lifetime
- 2005-09-26 PL PL10180395T patent/PL2289879T3/pl unknown
- 2005-09-26 ES ES05805643T patent/ES2412207T3/es active Active
- 2005-09-26 AU AU2005289635A patent/AU2005289635A1/en not_active Abandoned
- 2005-09-26 CA CA2580136A patent/CA2580136C/en not_active Expired - Lifetime
- 2005-09-26 CN CN2005800326490A patent/CN101031548B/zh not_active Expired - Lifetime
- 2005-09-26 EP EP10180395.5A patent/EP2289879B1/en not_active Expired - Lifetime
- 2005-09-26 WO PCT/US2005/034813 patent/WO2006037043A1/en not_active Ceased
- 2005-09-26 RU RU2007115886/04A patent/RU2417986C2/ru active
- 2005-09-26 JP JP2007533699A patent/JP5154227B2/ja not_active Expired - Lifetime
- 2005-09-26 RU RU2007115921/04A patent/RU2387643C2/ru active
- 2005-09-26 EP EP05801891A patent/EP1794125A1/en not_active Withdrawn
- 2005-09-26 SG SG200907436-0A patent/SG157378A1/en unknown
- 2005-09-26 WO PCT/US2005/034376 patent/WO2006036874A1/en not_active Ceased
- 2005-09-26 SG SG201002293-7A patent/SG161221A1/en unknown
- 2005-09-26 AU AU2005289444A patent/AU2005289444B2/en not_active Expired
- 2005-09-26 NZ NZ553702A patent/NZ553702A/en not_active IP Right Cessation
- 2005-09-26 KR KR1020077009394A patent/KR101260036B1/ko not_active Expired - Lifetime
- 2005-09-26 CN CN2005800326503A patent/CN101035759B/zh not_active Expired - Lifetime
- 2005-09-26 US US11/235,381 patent/US7868176B2/en active Active
- 2005-09-26 US US11/235,558 patent/US7732615B2/en active Active
- 2005-09-26 CA CA002580129A patent/CA2580129A1/en not_active Abandoned
- 2005-09-26 CN CN201110039289.4A patent/CN102153505B/zh not_active Expired - Lifetime
- 2005-09-26 MX MX2007003433A patent/MX2007003433A/es active IP Right Grant
- 2005-09-26 DK DK05805643.3T patent/DK1794126T3/da active
- 2005-09-26 KR KR1020077009395A patent/KR20070083800A/ko not_active Withdrawn
- 2005-09-26 BR BRPI0516063-4A patent/BRPI0516063A/pt not_active Application Discontinuation
- 2005-09-26 PL PL05805643T patent/PL1794126T3/pl unknown
- 2005-09-26 MX MX2007003403A patent/MX2007003403A/es not_active Application Discontinuation
- 2005-09-26 ES ES10180395.5T patent/ES2530258T3/es active Active
- 2005-09-26 EP EP05805643A patent/EP1794126B1/en not_active Expired - Lifetime
-
2006
- 2006-05-03 US US11/417,447 patent/US20060205780A1/en not_active Abandoned
- 2006-05-03 US US11/418,341 patent/US20060205781A1/en not_active Abandoned
-
2007
- 2007-03-20 ZA ZA200702345A patent/ZA200702345B/xx unknown
- 2007-03-20 ZA ZA200702349A patent/ZA200702349B/xx unknown
-
2010
- 2010-01-29 ZA ZA201000714A patent/ZA201000714B/en unknown
- 2010-06-07 US US12/795,547 patent/US7923564B2/en not_active Expired - Lifetime
-
2011
- 2011-04-06 US US13/081,427 patent/US8236960B2/en not_active Expired - Lifetime
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101031548B (zh) | 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 | |
| US7790899B2 (en) | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms | |
| CN101772491A (zh) | 基本不含有二聚体杂质的瑞格列奈 | |
| US20240043370A1 (en) | Method for triethylenetetramine purification | |
| CN119859139A (zh) | 双盐酸安罗替尼的固体形式及其制备方法 | |
| HK1102397B (en) | Crystalline form of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl) carbamide hemi-tartrate |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20110406 |