TWI393711B - １-〔３-〔３-（４-氯苯基）丙氧基〕丙基〕哌啶之新穎鹽 - Google Patents

１-〔３-〔３-（４-氯苯基）丙氧基〕丙基〕哌啶之新穎鹽 Download PDF

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Publication number
TWI393711B
TWI393711B TW095104184A TW95104184A TWI393711B TW I393711 B TWI393711 B TW I393711B TW 095104184 A TW095104184 A TW 095104184A TW 95104184 A TW95104184 A TW 95104184A TW I393711 B TWI393711 B TW I393711B
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Taiwan
Prior art keywords
propyl
chlorophenyl
propoxy
piperidine monohydrochloride
crystalline
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TW095104184A
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English (en)
Chinese (zh)
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TW200639157A (en
Inventor
拉葛 馬努耶爾Ｍ.
薩拉爾斯 裘安
古爾雷洛 馬塔
古格利塔 安東尼歐
查理 舒瓦特 尚
麥可 亞瑞格 尚
瑪莉 蕾寇特 珍妮
里內奧 薩威爾
舒納克 瓦特
史塔克 侯格
羅賓 加內林 賈倫
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生物科研公司
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Application filed by 生物科研公司 filed Critical 生物科研公司
Publication of TW200639157A publication Critical patent/TW200639157A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Ophthalmology & Optometry (AREA)
TW095104184A 2005-02-10 2006-02-08 １-〔３-〔３-（４-氯苯基）丙氧基〕丙基〕哌啶之新穎鹽 TWI393711B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05100942A EP1690858B1 (en) 2005-02-10 2005-02-10 Monohydrochloride salt of 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine

Publications (2)

Publication Number Publication Date
TW200639157A TW200639157A (en) 2006-11-16
TWI393711B true TWI393711B (zh) 2013-04-21

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ID=34938687

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TW095104184A TWI393711B (zh) 2005-02-10 2006-02-08 １-〔３-〔３-（４-氯苯基）丙氧基〕丙基〕哌啶之新穎鹽

Country Status (22)

Country Link
US (2) US8207197B2 (https=)
EP (2) EP1690858B1 (https=)
JP (1) JP5072604B2 (https=)
KR (1) KR101344271B1 (https=)
CN (1) CN101155793B (https=)
AR (1) AR054734A1 (https=)
AT (2) ATE391716T1 (https=)
CA (1) CA2597016C (https=)
CY (1) CY1108428T1 (https=)
DE (2) DE602005005941D1 (https=)
DK (1) DK1846384T3 (https=)
ES (1) ES2309948T3 (https=)
HR (1) HRP20080446T3 (https=)
ME (1) ME01103B (https=)
MX (1) MX2007009574A (https=)
PL (1) PL1846384T3 (https=)
PT (1) PT1846384E (https=)
RS (1) RS50624B (https=)
SI (1) SI1846384T1 (https=)
TW (1) TWI393711B (https=)
UY (1) UY29369A1 (https=)
WO (1) WO2006084833A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2167096A4 (en) * 2007-06-13 2010-07-14 Cypress Bioscience Inc IMPROVING TOLERANCE TO MIRTAZAPINE AND A SECOND ACTIVE INGREDIENT BY THE COMBINED USE OF THEM
BRPI1008020A2 (pt) 2009-02-11 2016-03-15 Sunovion Pharmaceuticals Inc antagonistas e agonistas inversos h3 da histamina e métodos de uso dos mesmos
SG176735A1 (en) 2009-06-10 2012-01-30 Sunovion Pharmaceuticals Inc Histamine h3 inverse agonists and antagonists and methods of use thereof
MX2012002898A (es) 2009-09-11 2012-04-02 Sunovion Pharmaceuticals Inc Agonistas y antagonistas inversos de histamina h3 y metodos de uso para los mismos.
WO2014199935A1 (ja) * 2013-06-10 2014-12-18 株式会社エム・エス・エス 小胞体ストレスシグナルを抑制することによる，薬剤の副作用としての体重増加や肥満を防止するために用いられる肥満防止剤
CN103435575A (zh) * 2013-08-06 2013-12-11 中国人民解放军军事医学科学院毒物药物研究所 1-（ 3-（ 3-（ 4-氯苯基）丙氧基）丙基）哌啶盐酸盐的制备方法
CN104447620B (zh) * 2014-11-28 2016-05-04 瑞阳制药有限公司 1-[3-[3-(4-氯苯基)丙氧基]丙基]-哌啶盐酸盐的制备方法
EP3239138A1 (en) 2016-04-25 2017-11-01 Sandoz Ag Hydrogen fumarate salt of 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine
WO2020092604A1 (en) * 2018-10-30 2020-05-07 Concert Pharmaceuticals, Inc. Deuterated pitolisant
IT201900013941A1 (it) 2019-08-05 2021-02-05 Procos Spa PROCESSO PER LA SINTESI DI PITOLISANT HCl
CN110804026B (zh) * 2019-11-18 2022-04-01 苏州永健生物医药有限公司 1- (3- (3-（4-氯苯基）丙氧基)丙基)哌啶盐酸盐的合成方法
US11945788B2 (en) 2021-06-07 2024-04-02 Nuray Chemicals Private Limited Process for preparing pitolisant hydrochloride and solid-state forms thereof
US11623920B2 (en) 2021-06-07 2023-04-11 Nuray Chemicals Private Limited Process for preparing pitolisant hydrochloride and solid-state forms thereof
EP4457219A4 (en) * 2021-12-29 2025-12-10 Biophore India Pharmaceuticals Pvt Ltd SOLID FORMS OF 1-3-[3-(4-CHLOROPHENYL)PROPOXY]PROPYL PIPERIDINE HYDROCHLORIDE AND THEIR PREPARATION PROCESS
US20250281475A1 (en) * 2022-05-04 2025-09-11 Msn Laboratories Private Limited, R & D Center A pharmaceutical composition of pitolisant hydrochloride and their process for the preparation
WO2024084379A1 (en) * 2022-10-17 2024-04-25 Biophore India Pharmaceuticals Pvt. Ltd A NOVEL PROCESS FOR THE PREPARATION OF AMORPHOUS SOLID DISPERSION OF 1-{3-[3-(4-CHLOROPHENYL) PROPOXY] PROPYL} PIPERIDINE, HYDROCHLORIDE WITH HYDROXYPROPYL BETA-CYCLODEXTRIN (HPβCD)
EP4374854A1 (en) * 2022-11-28 2024-05-29 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical mixture comprising amorphous pitolisant
EP4688166A1 (en) 2023-03-31 2026-02-11 BIOPROJET Pharma Polymorph form of pitolisant hydrochloride
WO2025082974A1 (en) 2023-10-16 2025-04-24 Bioprojet Pharma New formulations of pitolisant and methods of use
EP4681704A1 (en) 2024-07-18 2026-01-21 BIOPROJET Pharma New formulations of pitolisant
EP4732903A1 (en) * 2024-10-28 2026-04-29 BIOPROJET Pharma Co-crystals of pitolisant hydrochloride

Citations (1)

* Cited by examiner, † Cited by third party
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EP0982300A2 (en) * 1998-07-29 2000-03-01 Societe Civile Bioprojet Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0982300A2 (en) * 1998-07-29 2000-03-01 Societe Civile Bioprojet Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications

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Publication number Publication date
KR20070101381A (ko) 2007-10-16
EP1690858B1 (en) 2008-04-09
EP1690858A1 (en) 2006-08-16
EP1846384B1 (en) 2008-07-23
UY29369A1 (es) 2006-05-31
CA2597016A1 (en) 2006-08-17
US8354430B2 (en) 2013-01-15
PT1846384E (pt) 2008-10-21
ES2309948T3 (es) 2008-12-16
SI1846384T1 (sl) 2008-12-31
CY1108428T1 (el) 2014-04-09
JP2008530050A (ja) 2008-08-07
CA2597016C (en) 2013-01-15
US8207197B2 (en) 2012-06-26
ATE402154T1 (de) 2008-08-15
KR101344271B1 (ko) 2013-12-26
ME01103B (me) 2013-03-20
CN101155793B (zh) 2015-05-20
JP5072604B2 (ja) 2012-11-14
US20120289546A1 (en) 2012-11-15
RS50624B (sr) 2010-06-30
DK1846384T3 (da) 2008-11-17
PL1846384T3 (pl) 2009-01-30
US20080221162A1 (en) 2008-09-11
EP1846384A1 (en) 2007-10-24
CN101155793A (zh) 2008-04-02
DE602006001938D1 (de) 2008-09-04
WO2006084833A1 (en) 2006-08-17
DE602005005941D1 (de) 2008-05-21
TW200639157A (en) 2006-11-16
MX2007009574A (es) 2007-09-25
AR054734A1 (es) 2007-07-11
ATE391716T1 (de) 2008-04-15
HRP20080446T3 (en) 2008-10-31

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