AU725700B2 - New benzimidazole derivatives with antihistaminic activity - Google Patents

New benzimidazole derivatives with antihistaminic activity Download PDF

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Publication number
AU725700B2
AU725700B2 AU24672/97A AU2467297A AU725700B2 AU 725700 B2 AU725700 B2 AU 725700B2 AU 24672/97 A AU24672/97 A AU 24672/97A AU 2467297 A AU2467297 A AU 2467297A AU 725700 B2 AU725700 B2 AU 725700B2
Authority
AU
Australia
Prior art keywords
ethyl
benzimidazole
compound
piperidine
accordance
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
Application number
AU24672/97A
Other languages
English (en)
Other versions
AU2467297A (en
Inventor
Maravillas Bordell
Aurelio Orjales
Victor Rubio
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Faes Farma SA
Original Assignee
Fabrica Espanola de Productos Quimicos y Farmaceuticos FAES SA
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
Application filed by Fabrica Espanola de Productos Quimicos y Farmaceuticos FAES SA filed Critical Fabrica Espanola de Productos Quimicos y Farmaceuticos FAES SA
Publication of AU2467297A publication Critical patent/AU2467297A/en
Application granted granted Critical
Publication of AU725700B2 publication Critical patent/AU725700B2/en
Assigned to FAES FARMA S.A. reassignment FAES FARMA S.A. Request to Amend Deed and Register Assignors: FABRICA ESPANOLA DE PRODUCTOS QUIMICOS Y FARMACEUTICOS S.A.(FAES)
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU24672/97A 1996-06-04 1997-06-03 New benzimidazole derivatives with antihistaminic activity Expired AU725700B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES09601236A ES2124167B1 (es) 1996-06-04 1996-06-04 Nuevos derivados del bencimidazol con actividad antihistaminica.
ESP9601236 1996-06-04

Publications (2)

Publication Number Publication Date
AU2467297A AU2467297A (en) 1997-12-11
AU725700B2 true AU725700B2 (en) 2000-10-19

Family

ID=8295035

Family Applications (1)

Application Number Title Priority Date Filing Date
AU24672/97A Expired AU725700B2 (en) 1996-06-04 1997-06-03 New benzimidazole derivatives with antihistaminic activity

Country Status (27)

Country Link
US (1) US5877187A (enExample)
EP (1) EP0818454B1 (enExample)
JP (1) JP4218991B2 (enExample)
CN (1) CN1105716C (enExample)
AR (1) AR008386A1 (enExample)
AT (1) ATE264317T1 (enExample)
AU (1) AU725700B2 (enExample)
BR (1) BR9703276A (enExample)
CA (1) CA2206754C (enExample)
CZ (1) CZ289278B6 (enExample)
DE (2) DE69728608T2 (enExample)
DK (1) DK0818454T3 (enExample)
ES (1) ES2124167B1 (enExample)
FR (1) FR11C0023I2 (enExample)
HR (1) HRP970307B1 (enExample)
HU (1) HU227598B1 (enExample)
IN (1) IN186319B (enExample)
LU (1) LU91798I2 (enExample)
MX (1) MXPA97004127A (enExample)
NO (2) NO313195B1 (enExample)
PL (1) PL188908B1 (enExample)
PT (1) PT818454E (enExample)
RU (1) RU2182150C2 (enExample)
SI (1) SI0818454T1 (enExample)
TR (1) TR199700464A2 (enExample)
TW (1) TW438794B (enExample)
ZA (1) ZA974893B (enExample)

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WO2000001679A1 (en) 1998-07-01 2000-01-13 Takeda Chemical Industries, Ltd. Retinoid-associated receptor regulators
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ES2151442B1 (es) * 1999-01-11 2001-07-01 Espanola Prod Quimicos Nuevo derivado del bencenoetanol.
US6826561B2 (en) 2000-05-22 2004-11-30 Broadcom Corporation Method and apparatus for performing a binary search on an expanded tree
CA2484460C (en) 2002-04-19 2009-09-29 Faes Farma, S.A. Polymorph of 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazole-2-yl]-1-piperidinyl]ethyl]-.alpha..alpha. dimethyl-benzeneacetic acid
RU2288917C2 (ru) * 2002-04-19 2006-12-10 Фаэс Фарма, С.А. Полиморф 4-[2-[4-[1-(2-этоксиэтил)-1h-бензимидазол-2-ил]-1-пиперидинил]этил]-альфа, альфа-диметилбензолуксусной кислоты, способ его получения, фармацевтический препарат на его основе и его применение
AU2003245442B2 (en) * 2002-06-13 2009-02-05 Vertex Pharmaceuticals Incorporated 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase IV inhibitors for the treatment of bacterial infections
US20070188330A1 (en) * 2006-01-24 2007-08-16 Morhard Robert C System and method for detecting, monitoring, tracking and identifying explosive materials using ID marks
US7247623B2 (en) * 2005-08-19 2007-07-24 Inspire Pharmaceuticals, Inc. Method of treating dry eye disease with non-drying antihistamines
EP2240464A4 (en) * 2008-02-12 2011-09-14 Yuhan Corp PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE PRODUCTS
JP2010013472A (ja) * 2009-09-09 2010-01-21 Faes Farma Sa ４−［２−［１−（２−エトキシエチル）−１Ｈ−ベンズイミダゾール−２−イル］−１−ピペリジニル］エチル］−α，α−ジメチルベンゼノ酢酸の多形体
CN102675101B (zh) * 2012-05-16 2014-01-29 王蕾 2-(4-卤乙基)苯基-2-甲基丙酸酯的制备方法及合成比拉斯汀的方法
CZ307500B6 (cs) 2012-08-15 2018-10-24 Zentiva, K.S. Způsob přípravy derivátu 2-methyl-2´-fenylpropionové kyseliny využívající nové intermediáty
EP2969019A1 (en) * 2013-03-15 2016-01-20 Hercules Incorporated Composition and method of producing personal care compositions with improved deposition properties
CN103214454A (zh) * 2013-03-30 2013-07-24 北京万全德众医药生物技术有限公司 一种比拉斯汀晶型及制备方法
CN103214455B (zh) * 2013-03-30 2018-08-31 北京万全德众医药生物技术有限公司 一种比拉斯汀的制备方法
WO2014188453A2 (en) * 2013-05-24 2014-11-27 Msn Laboratories Private Limited Novel process for the preparation of 2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl}ethyl) phenyl]-2-methylpropanoic acid
CN103351380B (zh) * 2013-06-30 2019-01-22 北京万全德众医药生物技术有限公司 一种制备比拉斯汀的方法
CN104447683A (zh) * 2013-09-12 2015-03-25 天津市汉康医药生物技术有限公司 一种稳定的比拉斯汀化合物
CN103896915A (zh) * 2014-04-01 2014-07-02 中国药科大学 苯并咪唑类衍生物、其制备方法及其在医药上的应用
EP3040334A1 (en) 2014-12-29 2016-07-06 Faes Farma, S.A. New benzimidazole derivatives as antihistamine agents
CN106349214B (zh) * 2015-07-13 2020-11-03 南京长澳医药科技有限公司 一种比拉斯汀杂质的制备方法
SI3327012T1 (sl) * 2015-07-24 2021-10-29 Urquima Sa Kristalinične oblike bilastina in postopki za pripravo le-teh
CN105272977A (zh) * 2015-09-19 2016-01-27 万全万特制药江苏有限公司 一种制备比拉斯汀中间体的方法
EP3170817A1 (en) 2015-11-20 2017-05-24 Faes Farma, S.A. Co-crystals of benzimidazole compounds
EP3170816A1 (en) 2015-11-20 2017-05-24 Faes Farma, S.A. Supersaturated compositions of benzimidazole compounds
WO2017167949A1 (en) 2016-04-01 2017-10-05 Krka, D.D., Novo Mesto Crystalline forms of bilastine
EP3452462A4 (en) * 2016-05-05 2019-10-23 MSN Laboratories Private Limited, R&D Center Solid state forms of 2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid and process for preparation thereof
CN107365298A (zh) * 2017-03-14 2017-11-21 罗欣生物科技（上海）有限公司 一种2‑甲基‑2’‑苯基丙酸衍生物的制备方法
CN109456316A (zh) * 2017-09-06 2019-03-12 万全万特制药江苏有限公司 一种比拉斯汀杂质的制备方法
ES2813561T3 (es) 2017-09-07 2021-03-24 Tiefenbacher Alfred E Gmbh & Co Kg Composición farmacéutica en comprimido que comprende bilastina
PL3681475T3 (pl) 2017-10-16 2021-07-05 Faes Farma, S.A. Wodne kompozycje zawierające bilastynę i mometazon
EP3470062B1 (en) 2017-12-18 2020-10-28 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising bilastine polymorphic form 3 and magnesium aluminometasilicate
PL3641735T3 (pl) 2017-12-18 2021-09-06 Alfred E. Tiefenbacher (Gmbh & Co. Kg) Kompozycja farmaceutyczna tabletki zawierająca bilastynę w postaci 3 i rozpuszczalny w wodzie wypełniacz
EA202091725A1 (ru) 2018-01-18 2020-10-12 Фаэс Фарма С.А. Офтальмические композиции, содержащие биластин, бета-циклодекстрин и по крайней мере одно желатинирующее вещество
CN109081827A (zh) * 2018-11-06 2018-12-25 北京天弘天达医药科技股份有限公司 一种比拉斯汀的制备方法及应用
EP3725298A1 (en) 2019-04-16 2020-10-21 Faes Farma, S.A. Stable and preserved pharmaceutical compositions of bilastine
EP4188339A1 (en) 2020-07-30 2023-06-07 Faes Farma, S.A. Decongestant drug delivery system
CN112110893A (zh) * 2020-10-28 2020-12-22 山东齐环医药科技有限公司 一种比拉斯汀的制备方法
ES3058094T3 (en) 2020-11-18 2026-03-06 Biopharma Synergies S L Orodispersible powder composition comprising an antihistamine compound
CA3200779A1 (en) 2020-12-23 2022-06-30 Strusi ORAZIO LUCA A non-micronized bilastine composition
JP2025508704A (ja) 2022-02-17 2025-04-10 ファエス・ファルマ・ソシエダッド・アノニマ １日１回非経口投与のためのビラスチン組成物
WO2024224308A1 (en) * 2023-04-27 2024-10-31 Leiutis Pharmaceuticals Llp Liquid parenteral formulations of bilastine free of cyclodextrins
WO2024224326A1 (en) * 2023-04-27 2024-10-31 Leiutis Pharmaceuticals Llp Liquid parenteral formulations of bilastine
WO2026104388A1 (en) 2024-11-12 2026-05-21 Faes Farma, S.A. Decongestant controlled release drug delivery system

Family Cites Families (5)

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Publication number Priority date Publication date Assignee Title
GB8904174D0 (en) * 1989-02-23 1989-04-05 British Bio Technology Compounds
JPH05507469A (ja) * 1990-04-13 1993-10-28 スミスクライン・ビーチャム・コーポレイション 置換ベンズイミダゾール
ES2048109B1 (es) * 1992-07-20 1994-12-16 Espanola Prod Quimicos Procedimiento de preparacion de nuevos derivados piperidicos del bencimidazol.
RU2167657C2 (ru) * 1992-08-03 2001-05-27 Сепракор, Инк. Фармацевтическая композиция для лечения аллергических заболеваний, способ антигистаминного лечения, применение композиции для получения лекарственного препарата
CA2362337C (en) * 1993-06-25 2005-08-02 Merrell Pharmaceuticals Inc. Novel intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives

Also Published As

Publication number Publication date
ZA974893B (en) 1997-12-30
NO972525D0 (no) 1997-06-03
JPH1059961A (ja) 1998-03-03
AR008386A1 (es) 2000-01-19
EP0818454A1 (en) 1998-01-14
DE122011000006I1 (de) 2011-06-16
AU2467297A (en) 1997-12-11
FR11C0023I1 (enExample) 2011-08-19
CA2206754A1 (en) 1997-12-04
DE69728608D1 (de) 2004-05-19
HU9700997D0 (en) 1997-07-28
DE69728608T2 (de) 2005-04-21
BR9703276A (pt) 2004-08-17
ES2124167B1 (es) 1999-09-16
EP0818454B1 (en) 2004-04-14
HUP9700997A1 (hu) 1999-09-28
TR199700464A3 (tr) 1997-12-21
NO2011008I1 (no) 2011-06-06
PL320358A1 (en) 1997-12-08
LU91798I2 (fr) 2011-05-23
NO972525L (no) 1997-12-05
MXPA97004127A (es) 2005-07-25
CZ172397A3 (en) 1997-12-17
ATE264317T1 (de) 2004-04-15
FR11C0023I2 (fr) 2012-03-16
HRP970307A2 (en) 1998-04-30
CN1176964A (zh) 1998-03-25
TW438794B (en) 2001-06-07
NO2011008I2 (no) 2012-05-14
RU2182150C2 (ru) 2002-05-10
PL188908B1 (pl) 2005-05-31
CN1105716C (zh) 2003-04-16
DK0818454T3 (da) 2004-07-12
TR199700464A2 (xx) 1997-12-21
ES2124167A1 (es) 1999-01-16
US5877187A (en) 1999-03-02
CZ289278B6 (cs) 2001-12-12
CA2206754C (en) 2007-01-23
IN186319B (enExample) 2001-08-04
PT818454E (pt) 2004-08-31
HU227598B1 (en) 2011-09-28
NO313195B1 (no) 2002-08-26
HRP970307B1 (en) 2002-02-28
JP4218991B2 (ja) 2009-02-04
SI0818454T1 (en) 2004-08-31

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