[go: up one dir, main page]

ZA200702349B - Synthesis of N- (4 - fluorobenzyl) - N - (1 - methylpiperidin - 4 yl) - N' - (4- (2 - methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms - Google Patents

Synthesis of N- (4 - fluorobenzyl) - N - (1 - methylpiperidin - 4 yl) - N' - (4- (2 - methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms

Info

Publication number
ZA200702349B
ZA200702349B ZA200702349A ZA200702349A ZA200702349B ZA 200702349 B ZA200702349 B ZA 200702349B ZA 200702349 A ZA200702349 A ZA 200702349A ZA 200702349 A ZA200702349 A ZA 200702349A ZA 200702349 B ZA200702349 B ZA 200702349B
Authority
ZA
South Africa
Prior art keywords
methylpropyloxy
methylpiperidin
carbamide
fluorobenzyl
phenylmethyl
Prior art date
Application number
ZA200702349A
Other languages
English (en)
Inventor
Thygesen Mikkel
Tolf Bo-Ragnar
Blatter Fritz
Schlienger Nathalie
Carl-Magnus A Andersson
Berghausen Joerg
Original Assignee
Acadia Pharm Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35539440&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200702349(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Acadia Pharm Inc filed Critical Acadia Pharm Inc
Publication of ZA200702349B publication Critical patent/ZA200702349B/xx

Links

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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
ZA200702349A 2004-09-27 2007-03-20 Synthesis of N- (4 - fluorobenzyl) - N - (1 - methylpiperidin - 4 yl) - N' - (4- (2 - methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms ZA200702349B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US61401404P 2004-09-27 2004-09-27

Publications (1)

Publication Number Publication Date
ZA200702349B true ZA200702349B (en) 2008-10-29

Family

ID=35539440

Family Applications (3)

Application Number Title Priority Date Filing Date
ZA200702349A ZA200702349B (en) 2004-09-27 2007-03-20 Synthesis of N- (4 - fluorobenzyl) - N - (1 - methylpiperidin - 4 yl) - N' - (4- (2 - methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
ZA200702345A ZA200702345B (en) 2004-09-27 2007-03-20 Salts on N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy) phenylmethyl)carbamide and their preparation
ZA201000714A ZA201000714B (en) 2004-09-27 2010-01-29 Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and their preparation

Family Applications After (2)

Application Number Title Priority Date Filing Date
ZA200702345A ZA200702345B (en) 2004-09-27 2007-03-20 Salts on N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy) phenylmethyl)carbamide and their preparation
ZA201000714A ZA201000714B (en) 2004-09-27 2010-01-29 Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and their preparation

Country Status (17)

Country Link
US (6) US7868176B2 (fr)
EP (3) EP2289879B1 (fr)
JP (2) JP4996467B2 (fr)
KR (2) KR20070083800A (fr)
CN (3) CN101031548B (fr)
AU (2) AU2005289635A1 (fr)
BR (1) BRPI0516063A (fr)
CA (2) CA2580129A1 (fr)
DK (1) DK1794126T3 (fr)
ES (2) ES2530258T3 (fr)
MX (2) MX2007003433A (fr)
NZ (1) NZ553702A (fr)
PL (2) PL2289879T3 (fr)
RU (2) RU2417986C2 (fr)
SG (2) SG157378A1 (fr)
WO (2) WO2006036874A1 (fr)
ZA (3) ZA200702349B (fr)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL151164A0 (en) * 2000-03-06 2003-04-10 Acadia Pharm Inc Azacyclic compounds for use in the treatment of serotonin related diseases
KR20100008799A (ko) * 2001-12-28 2010-01-26 아카디아 파마슈티칼스 인코포레이티드 모노아민 수용체 조정자로서의 스피로아자사이클릭 화합물
BR0312217A (pt) * 2002-06-24 2005-05-10 Acadia Pharm Inc Compostos, métodos de inibição da atividade/ativação de um receptor monoaminérgico e método de tratamento de condição doentia associada a um receptor de monoaminergético
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
CN101780080B (zh) 2003-01-16 2014-06-04 阿卡蒂亚药品公司 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂
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
ES2530258T3 (es) * 2004-09-27 2015-02-27 Acadia Pharmaceuticals Inc. Síntesis de una forma cristalina de sal tartrato de N-(4-fluorobencil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloxi)fenilmetil)carbamida
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 (fr) * 2006-04-19 2007-11-01 Acadia Pharmaceuticals, Inc. Utilisation de 4-amino-piperidines pour le traitement des troubles du sommeil
CA2652300A1 (fr) * 2006-05-15 2007-11-22 Acadia Pharmaceuticals Inc. Formules pharmaceutiques de pimavanserine
WO2008116024A2 (fr) 2007-03-19 2008-09-25 Acadia Pharmaceuticals Inc. Combinaisons d'agonistes ou antagonistes inverses de 5-ht2a avec antipsychotiques
US20080280886A1 (en) * 2007-05-08 2008-11-13 Auspex Pharmaceuticals, Inc. Substituted ureas
EP2173343A1 (fr) * 2007-05-18 2010-04-14 Acadia Pharmaceuticals Inc. Utilisation de pimavansérine pour le traintemant de la maladie de parkinson et des symptômes associé
CA2700331A1 (fr) * 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Co-administration de pimavanserine avec d'autres agents
WO2009039461A2 (fr) * 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Dérivés de pipéridine n-substitués en tant qu'agents récepteurs de la sérotonine
EP2865678A3 (fr) * 2008-06-30 2015-05-27 Janssen Pharmaceutica NV Forme cristalline hémi-tartrate d'un dérivé de benzoimidazol-2-yl pyrimidine
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 (fr) 2012-11-27 2014-06-05 Acadia Pharmaceuticals Inc. Méthodes pour le traitement de la psychose de la maladie de parkinson à l'aide de pimavansérine
EP3702358A1 (fr) * 2013-06-21 2020-09-02 Intra-Cellular Therapies, Inc. Procédé pour la préparation des sels d'un inhibiteur de pde1
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 (fr) 2015-03-02 2016-09-09 Teva Pharmaceutical Industries Ltd. Procédés et intermédiaires pour la préparation de pimavansérine
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
DK3325444T3 (da) * 2015-07-20 2021-10-04 Acadia Pharm Inc Fremgangsmåder til fremstilling af n-(4-fluorbenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamid og dets tartratsalt og polymorf form 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 (fr) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Association de pimavansérine et de modulateurs du cytochrome p450
EP3436010B1 (fr) 2016-03-29 2021-03-10 Acadia Pharmaceuticals Inc. Agonistes ou antagonistes inverses du récepteur de la sérotonine 5-ht2a destinés à être utilisés dans le but de réduire les peptides bèta-amyloïdes et l'accumulation de plaques amyloïdes
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
CN107868058B (zh) * 2016-09-23 2023-02-14 上海医药集团股份有限公司 一种喹唑啉衍生物的盐、其制备方法及应用
EP3558311A1 (fr) 2016-12-20 2019-10-30 Acadia Pharmaceuticals Inc. Pimavansérine seule ou en association pour une utilisation dans le traitement de la psychose liée à la maladie d'alzheimer
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
EP3615028A1 (fr) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavansérine pour le traitement d'un trouble de contrôle des impulsions
BR112019024817A2 (pt) 2017-05-25 2020-08-18 Glytech Llc. formulações para tratamento de distúrbio de estresse pós-traumático
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
EP3672960A2 (fr) 2017-08-21 2020-07-01 Acadia Pharmaceuticals Inc. Composés, sels associés et méthodes de traitement de maladies
SI3672954T1 (sl) * 2017-08-21 2025-11-28 Acadia Pharmaceuticals Inc. Spojine, njihove soli in njihova uporaba za zdravljenje bolezni
EP3675827A1 (fr) 2017-08-30 2020-07-08 Acadia Pharmaceuticals Inc. Formulations de pimavansérine
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
CN111201218A (zh) * 2017-12-22 2020-05-26 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
EP3741744B1 (fr) * 2019-05-22 2022-01-05 Zaklady Farmaceutyczne "Polpharma" S.A. Intermédiaire pharmaceutique pour la préparation de pimavansérine
WO2021016369A1 (fr) 2019-07-22 2021-01-28 Acadia Pharmaceuticals Inc. Pimavansérine pour le traitement de la schizophrénie ou pour le traitement de la psychose découlant de troubles neuro-dégénératifs ou d'un trouble dépressif
WO2021030607A1 (fr) 2019-08-15 2021-02-18 Acadia Pharmaceuticals Inc. Pimavansérine pour le traitement de maladies neurodégénératives
KR20220099989A (ko) 2019-11-08 2022-07-14 케모센트릭스, 인크. 보체 성분 c5a 수용체의 염 형태
CA3155596A1 (fr) * 2019-11-08 2021-05-14 Rajinder Singh Forme cristalline de base libre d'un recepteur de composant c5a du complement
US11603356B2 (en) 2019-11-08 2023-03-14 Chemocentryx, Inc. Amorphous form of a complement component C5a receptor
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 (fr) 2020-11-02 2022-05-05 Acadia Pharmaceuticals Inc. Composés pour le traitement de la psychose ou de la dépression
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

Family Cites Families (68)

* Cited by examiner, † Cited by third party
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 (fr) 1978-04-03 1983-01-25 Joseph Torremans Nouvelles n-heterocycle-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 (fr) 1993-05-21 1994-11-22 Noriyoshi Sueda Derives de l'uree et leur utilisation comme inhibiteurs de l'acat
WO1994027967A1 (fr) 1993-05-26 1994-12-08 Smithkline Beecham Laboratoires Pharmaceutiques Nouveaux composes
US5707798A (en) 1993-07-13 1998-01-13 Novo Nordisk A/S 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
EP0854869B1 (fr) 1995-09-29 2004-08-25 Eli Lilly And Company Composes spiro comme inhibiteurs de l'agregation de plaquettes dependante du fibrinogene
EP0944388A4 (fr) 1996-04-03 2001-08-16 Merck & Co Inc Inhibiteurs de la farnesyl-proteine transferase
AU2733997A (en) 1996-04-17 1997-11-07 Du Pont Pharmaceuticals 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
US6344449B1 (en) 1996-09-10 2002-02-05 Dr. Karl Thomae Gmbh Modified aminoacids, pharmaceuticals containing these compounds and method for their production
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
CN1255162A (zh) 1997-05-08 2000-05-31 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
CA2291734A1 (fr) * 1997-06-27 1999-01-07 Merck Sharp & Dohme Limited Derives de 3-(benzylamino)piperidine substitues et leur utilisation comme agents therapeutiques
US20020163987A1 (en) * 1997-12-12 2002-11-07 British Nuclear Fuels Plc Monitoring a sample containing a neutron source
DE1071701T1 (de) 1998-04-14 2001-08-23 Arena Pharmaceuticals, Inc. Non-endogene, konstitutiv aktivierte humane serotonin-rezeptoren und kleine molekülmodulatoren davon
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
JP2002527477A (ja) 1998-10-16 2002-08-27 サントリー株式会社 神経細胞保護作用物質としてのアミノフェノキシ酢酸誘導体
US6150393A (en) * 1998-12-18 2000-11-21 Arena Pharmaceuticals, Inc. Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
EP1013276A1 (fr) * 1998-12-23 2000-06-28 Pfizer Inc. Aminoazacycloalcanes comme modulateurs de CCR5
WO2000056335A1 (fr) 1999-03-24 2000-09-28 The Regents Of The University Of California Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease
US6399619B1 (en) 1999-04-06 2002-06-04 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
CN1356977A (zh) 1999-05-17 2002-07-03 诺沃挪第克公司 胰高血糖素拮抗剂/反向激动剂
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
IL151164A0 (en) 2000-03-06 2003-04-10 Acadia Pharm Inc Azacyclic compounds for use in the treatment of serotonin related diseases
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
JP4273965B2 (ja) * 2001-06-05 2009-06-03 東洋紡績株式会社 抗血栓性組成物およびそれを有する医療用具
KR20100008799A (ko) 2001-12-28 2010-01-26 아카디아 파마슈티칼스 인코포레이티드 모노아민 수용체 조정자로서의 스피로아자사이클릭 화합물
KR20040075353A (ko) 2002-01-17 2004-08-27 제너럴 일렉트릭 캄파니 양이온성 개시제로서 약하게 배위된 이미다졸리딘음이온을 포함하는 오늄 염
WO2003062206A2 (fr) 2002-01-23 2003-07-31 Arena Pharmaceuticals, Inc. Modulateurs a petites molecules du recepteur de serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associes
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
BR0312217A (pt) * 2002-06-24 2005-05-10 Acadia Pharm Inc Compostos, métodos de inibição da atividade/ativação de um receptor monoaminérgico e método de tratamento de condição doentia associada a um receptor de monoaminergético
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
WO2004009549A2 (fr) 2002-07-18 2004-01-29 Actelion Pharmaceuticals Ltd Piperidines utiles pour traiter des maladies du systeme nerveux central
WO2004039322A2 (fr) 2002-10-29 2004-05-13 Miicro, Inc. Nouvelle polytherapie pour la schizophrenie, fondee sur une cognition amelioree : blocage de 5-ht-2a/d2 avec blocage auxiliaire du recaptage da prefrontal
CN101780080B (zh) 2003-01-16 2014-06-04 阿卡蒂亚药品公司 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂
EP1589974A2 (fr) 2003-01-23 2005-11-02 Acadia Pharmaceuticals Inc. Utilisation de la n-desmethylclozapine pour le traitement de maladies neuropsychiatriques chez l'homme
DE602004002567T2 (de) 2003-02-17 2007-05-31 F. Hoffmann-La Roche Ag Piperidinbenzolsulfonamidderivate
US7628762B2 (en) 2003-03-19 2009-12-08 Suros Surgical Systems, Inc. Adapter assembly for stereotactic biopsy
MXPA06007244A (es) * 2003-12-22 2006-08-18 Acadia Pharm Inc Analogos amino sustituidos de diaril[a,d]ciclohepteno como agonistas muscarinicos y metodos de tratamiento de trastornos neuropsiquiatricos.
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
ES2530258T3 (es) * 2004-09-27 2015-02-27 Acadia Pharmaceuticals Inc. Síntesis de una forma cristalina de sal tartrato de N-(4-fluorobencil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloxi)fenilmetil)carbamida

Also Published As

Publication number Publication date
EP2289879A1 (fr) 2011-03-02
RU2417986C2 (ru) 2011-05-10
AU2005289444B2 (en) 2012-06-14
KR101260036B1 (ko) 2013-05-06
PL1794126T3 (pl) 2013-08-30
MX2007003433A (es) 2007-08-06
SG161221A1 (en) 2010-05-27
NZ553702A (en) 2010-10-29
ES2530258T3 (es) 2015-02-27
AU2005289635A2 (en) 2006-04-06
ZA201000714B (en) 2010-10-27
EP1794126A1 (fr) 2007-06-13
WO2006037043A1 (fr) 2006-04-06
CN101035759B (zh) 2011-06-15
RU2007115921A (ru) 2008-11-10
JP5154227B2 (ja) 2013-02-27
US7868176B2 (en) 2011-01-11
CN102153505A (zh) 2011-08-17
EP1794126B1 (fr) 2013-03-20
CN102153505B (zh) 2014-10-22
US20110184179A1 (en) 2011-07-28
WO2006036874A1 (fr) 2006-04-06
US20060106063A1 (en) 2006-05-18
CN101031548A (zh) 2007-09-05
KR20070083800A (ko) 2007-08-24
DK1794126T3 (da) 2013-06-24
US20100305329A1 (en) 2010-12-02
SG157378A1 (en) 2009-12-29
KR20070083799A (ko) 2007-08-24
US20060205781A1 (en) 2006-09-14
US7923564B2 (en) 2011-04-12
HK1102397A1 (en) 2007-11-16
JP4996467B2 (ja) 2012-08-08
RU2387643C2 (ru) 2010-04-27
ES2412207T3 (es) 2013-07-10
US20060111399A1 (en) 2006-05-25
US8236960B2 (en) 2012-08-07
AU2005289444A1 (en) 2006-04-06
US20060205780A1 (en) 2006-09-14
EP2289879B1 (fr) 2014-11-12
MX2007003403A (es) 2007-05-07
CN101031548B (zh) 2011-04-06
AU2005289635A1 (en) 2006-04-06
PL2289879T3 (pl) 2015-05-29
ZA200702345B (en) 2010-04-28
CA2580136A1 (fr) 2006-04-06
CA2580136C (fr) 2015-08-18
JP2008514642A (ja) 2008-05-08
CN101035759A (zh) 2007-09-12
CA2580129A1 (fr) 2006-04-06
AU2005289444A2 (en) 2006-04-06
RU2007115886A (ru) 2008-11-10
US7732615B2 (en) 2010-06-08
EP1794125A1 (fr) 2007-06-13
JP2008514627A (ja) 2008-05-08
BRPI0516063A (pt) 2008-08-19

Similar Documents

Publication Publication Date Title
ZA200702349B (en) Synthesis of N- (4 - fluorobenzyl) - N - (1 - methylpiperidin - 4 yl) - N' - (4- (2 - methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
WO2008144326A3 (fr) Synthèse de n-(4-fluorobenzyl)-n-(l-méthylpypéridine-4-yl)-n'-(4-2-méthylpropyloxy)phénylméthyl)carbamide et son sel de tartrate et des formes cristallines
IL190198A0 (en) N-(3-amino-quinoxalin-2-yl)-sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
DK1948608T3 (da) Farmaceutiske salte og polymorfe former af N-(5-chlor-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]-benzoyl]amino]-5-methoxybenzamid, en faktor xa-inhibitor
EP1828224A4 (fr) Compositions contenant des acides amines non naturels et des polypeptides, procedes impliquant ces acides amines non naturels et polypeptides, et utilisations desdits acides amines non naturels et polypeptides
IL189201A0 (en) N-(arylamino)-sulfonamide inhibitors of mek
IL179520A0 (en) N - substituted piperidines and their use as pharmaceuticals
ZA200902469B (en) 4-[4-({[4-Chloro-3(Trifluoromethyl)Phenyl)]Carbamoyl} Amino)-3-Fluorophenoxy]-N-Methylpyridine-2-Carboxamide Monohydrate
IL179389A0 (en) Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
IS7479A (is) Afleiður af N-[fenýl(píperidín-2-ýl)metýl]bensamíð, aðferð við framleiðslu þeirra og notkun í læknismeðferðum
IL186308A (en) A pharmaceutical composition containing metformin hydrochloride and pioglitazone hydrochloride
DE60314013D1 (de) 2-(1h-indazol-6-ylamino)- benzamid-verbindungen als protein kinase inhibitoren und deren verwendung zur behandlung von ophthalmischen krankheiten
TW200716117A (en) Formulations of a SRC/ABL inhibitor
IL213615A0 (en) N-(5-substituted-2-nitrophenyl)amine derivatives and methods for the preparation of 6-substituted-1-methyl-1-h-benzimidazole derivatives utilizing the same
DK1893603T3 (da) Piperidin-4-YL-amidderivater og anvendelsen deraf som SST-receptorundertype 5-antagonister
ATE471315T1 (de) Piperidin- und piperazinacetamide als inhibitoren der 17beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
SI1794126T1 (sl) Kristaln oblika N-(4-flurobenzil)-N-(1-metilpiperidin-4-il)-N'-(4-(2- metilpropiloksi)fenilmetil)karbamid hemi-tartrata
ZA200700651B (en) 3-substituted-5-and 6-aminoalkyl indole-2-carboxylic acid amides and related analogs as inhibitors of casein kinase
HK1102396A (en) Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2- methylpropyloxy)phenylmethyl)carbamide and their preparation
DE602006015309D1 (de) Haar- und/oder kopfhautpflegezusammensetzungen mit amino-oxo-indolyliden-verbindungen
ZA200801443B (en) N-(arylamino)-sulfonamide inhibitors of MEK
IL180336A0 (en) Crystal forms of (3r) -1 - (2 - methylalanyl - d - tryptophyl) - 3 -(phenylmethyl)-3- piperidinecarboxylic acid 1, 2, 2 - trimethylhydrazide
EP1896433A4 (fr) Nouvelles formes cristallines de (s)-n-(1-carboxy-2-methyl-prop-1-yl)-n-pentanoyl-n-[2'-(1h-tetrazol-5-yl)bi-phenyl-4-ylmethyl]-amine
NO20081080L (no) Nytt salt I
DE60304451D1 (de) Verwendung von ceramiden in haarbehandlungsmitteln