CN1105716C - 具有抗组胺的新苯并咪唑衍生物 - Google Patents

具有抗组胺的新苯并咪唑衍生物 Download PDF

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Publication number
CN1105716C
CN1105716C CN97114905A CN97114905A CN1105716C CN 1105716 C CN1105716 C CN 1105716C CN 97114905 A CN97114905 A CN 97114905A CN 97114905 A CN97114905 A CN 97114905A CN 1105716 C CN1105716 C CN 1105716C
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CN
China
Prior art keywords
ethyl
phenyl
pharmacology
alkali
dimethyl
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
Application number
CN97114905A
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English (en)
Chinese (zh)
Other versions
CN1176964A (zh
Inventor
A·奥加勒斯
V·鲁比奥
M·博德尔
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
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Publication of CN1176964A publication Critical patent/CN1176964A/zh
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Publication of CN1105716C publication Critical patent/CN1105716C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN97114905A 1996-06-04 1997-06-04 具有抗组胺的新苯并咪唑衍生物 Expired - Lifetime CN1105716C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES9601236 1996-06-04
ES09601236A ES2124167B1 (es) 1996-06-04 1996-06-04 Nuevos derivados del bencimidazol con actividad antihistaminica.

Publications (2)

Publication Number Publication Date
CN1176964A CN1176964A (zh) 1998-03-25
CN1105716C true CN1105716C (zh) 2003-04-16

Family

ID=8295035

Family Applications (1)

Application Number Title Priority Date Filing Date
CN97114905A Expired - Lifetime CN1105716C (zh) 1996-06-04 1997-06-04 具有抗组胺的新苯并咪唑衍生物

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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EP1092711A4 (en) 1998-07-01 2002-07-31 Takeda Chemical Industries Ltd RETINOID ASSOCIATED RECEPTOR REGULATORS
CN1184208C (zh) 1998-11-27 2005-01-12 巴斯福股份公司 取代的苯并咪唑及其制备和用途
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
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
BRPI0215703B8 (pt) * 2002-04-19 2021-05-25 Faes Farma Sa polimorfo de ácido 4-[2-[1-(2-etoxietil)-1h-benzidimazol-2-il]-1-piperidinil]etil]-a, a-dimetil-benzenoacético, preparado farmacêutico, e seu uso do polimorfo 1
MXPA04012628A (es) * 2002-06-13 2005-03-23 Patricia Olivershaffer DERIVADOS Y COMPUESTOS RELACIONADOS DEL áCIDO 2-UREIDO-6-HETEROARIL-3H-BENZOIMIDAZOL-4-CARBOXILICO COMO INHIBIDORES DE GIRASA Y/O TOPOISOMERASA IV PARA EL TRATAMIENTO DE INFECCIONES BACTERIALES.
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
CN101952273B (zh) 2008-02-12 2014-11-12 柳韩洋行 2-甲基2’-苯基丙酸衍生物的制备方法和中间体化合物
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
RU2671577C2 (ru) * 2013-03-15 2018-11-02 Геркулес Ллк Состав и способ получения композиций для личной гигиены, обладающих улучшенными характеристиками осаждения
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
EP3327012B1 (en) * 2015-07-24 2021-03-17 Urquima, S.A. Crystalline forms of bilastine and preparation methods thereof
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
EP3453384B1 (en) 2017-09-07 2020-05-27 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising bilastine
BR112020007569A2 (pt) 2017-10-16 2020-09-24 Faes Farma, S.A. composições aquosas de bilastina
EP3641735B1 (en) 2017-12-18 2021-02-24 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising bilastine form 3 and a water-soluble filler
ES2835287T3 (es) 2017-12-18 2021-06-22 Tiefenbacher Alfred E Gmbh & Co Kg Composición farmacéutica de comprimido que comprende la forma polimórfica 3 de bilastina y aluminometasilicato de magnesio
DK3740191T3 (da) 2018-01-18 2021-06-07 Faes Farma Sa Oftalmiske sammensætninger omfattende bilastin, et beta-cyclodextrin og mindst et geleringsmiddel
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
WO2022106923A1 (en) 2020-11-18 2022-05-27 BioPharma Synergies, S. L. Orodispersible powder composition comprising an antihistamine compound
EP4267109A1 (en) 2020-12-23 2023-11-01 Noucor Health S.A. A non-micronized bilastine composition
MX2024009978A (es) 2022-02-17 2024-08-26 Faes Farma Sa Composicion de bilastina para administracion parenteral una vez al dia.
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5322850A (en) * 1992-07-20 1994-06-21 Fabrica Espanola De Productos Quimicos Y Farmaceuticos, S.A. Antiallergic piperidine derivatives of benzimidazole
WO1995000480A1 (en) * 1993-06-25 1995-01-05 Merrell Pharmaceuticals Inc. Novel intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives

Family Cites Families (3)

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GB8904174D0 (en) * 1989-02-23 1989-04-05 British Bio Technology Compounds
EP0525129A4 (en) * 1990-04-13 1993-03-24 Smith-Kline Beecham Corporation Substituted benzimidazoles
DK0701443T4 (da) * 1992-08-03 2000-12-18 Sepracor Inc Terfenadinmetabolitter og deres optisk rene isomerer til behandling af allergiske lidelser

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5322850A (en) * 1992-07-20 1994-06-21 Fabrica Espanola De Productos Quimicos Y Farmaceuticos, S.A. Antiallergic piperidine derivatives of benzimidazole
WO1995000480A1 (en) * 1993-06-25 1995-01-05 Merrell Pharmaceuticals Inc. Novel intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives

Non-Patent Citations (1)

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Title
JOURNAL OF HETEROEYELIE CHEMISTRY,VOL.32 1995-01-01 A.ORJALES ET AL *

Also Published As

Publication number Publication date
HUP9700997A1 (hu) 1999-09-28
TR199700464A3 (tr) 1997-12-21
HRP970307A2 (en) 1998-04-30
DE122011000006I1 (de) 2011-06-16
EP0818454A1 (en) 1998-01-14
FR11C0023I2 (fr) 2012-03-16
BR9703276A (pt) 2004-08-17
FR11C0023I1 (enExample) 2011-08-19
HU227598B1 (en) 2011-09-28
NO2011008I2 (no) 2012-05-14
ZA974893B (en) 1997-12-30
CA2206754A1 (en) 1997-12-04
PL320358A1 (en) 1997-12-08
DK0818454T3 (da) 2004-07-12
JPH1059961A (ja) 1998-03-03
ATE264317T1 (de) 2004-04-15
EP0818454B1 (en) 2004-04-14
SI0818454T1 (en) 2004-08-31
RU2182150C2 (ru) 2002-05-10
AU725700B2 (en) 2000-10-19
PT818454E (pt) 2004-08-31
AU2467297A (en) 1997-12-11
PL188908B1 (pl) 2005-05-31
NO972525D0 (no) 1997-06-03
JP4218991B2 (ja) 2009-02-04
CA2206754C (en) 2007-01-23
CZ289278B6 (cs) 2001-12-12
IN186319B (enExample) 2001-08-04
TR199700464A2 (xx) 1997-12-21
CZ172397A3 (en) 1997-12-17
LU91798I2 (fr) 2011-05-23
ES2124167A1 (es) 1999-01-16
NO2011008I1 (no) 2011-06-06
ES2124167B1 (es) 1999-09-16
HU9700997D0 (en) 1997-07-28
AR008386A1 (es) 2000-01-19
DE69728608T2 (de) 2005-04-21
TW438794B (en) 2001-06-07
US5877187A (en) 1999-03-02
CN1176964A (zh) 1998-03-25
DE69728608D1 (de) 2004-05-19
NO972525L (no) 1997-12-05
NO313195B1 (no) 2002-08-26
HRP970307B1 (en) 2002-02-28
MXPA97004127A (es) 2005-07-25

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Owner name: FAES PHARMA S. A.

Free format text: FORMER NAME OR ADDRESS: FABRICA ESPANOLA DE PRODUCTOS QUIMICOS Y FARMACEUTICOS, S. A.

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Address after: The Spanish

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Patentee before: Fabrica Espanola De productos Quimicos Y Farmaceuticos, S. A.

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