ES2124167B1 - Nuevos derivados del bencimidazol con actividad antihistaminica. - Google Patents
Nuevos derivados del bencimidazol con actividad antihistaminica.Info
- Publication number
- ES2124167B1 ES2124167B1 ES09601236A ES9601236A ES2124167B1 ES 2124167 B1 ES2124167 B1 ES 2124167B1 ES 09601236 A ES09601236 A ES 09601236A ES 9601236 A ES9601236 A ES 9601236A ES 2124167 B1 ES2124167 B1 ES 2124167B1
- Authority
- ES
- Spain
- Prior art keywords
- new derivatives
- benzmidazole
- group
- antihistamine activity
- ethyl
- 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 - Fee Related
Links
- 230000000694 effects Effects 0.000 title abstract 3
- 230000001387 anti-histamine Effects 0.000 title abstract 2
- 239000000739 antihistaminic agent Substances 0.000 title abstract 2
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 title 1
- -1 ISOPROPYL Chemical class 0.000 abstract 2
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical class C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- 210000000748 cardiovascular system Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
- ORGHESHFQPYLAO-UHFFFAOYSA-N vinyl radical Chemical class C=[CH] ORGHESHFQPYLAO-UHFFFAOYSA-N 0.000 abstract 1
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)
- 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)
Priority Applications (29)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES09601236A ES2124167B1 (es) | 1996-06-04 | 1996-06-04 | Nuevos derivados del bencimidazol con actividad antihistaminica. |
ZA9704893A ZA974893B (en) | 1996-06-04 | 1997-06-03 | New benzimidazole derivatives with antihistaminic activity. |
SI9730652T SI0818454T1 (en) | 1996-06-04 | 1997-06-03 | Benzimidazole derivatives with antihistaminic activity |
DE122011000006C DE122011000006I1 (de) | 1996-06-04 | 1997-06-03 | Benzimidazol-Derivate mit antihistaminischer Wirkung |
AT97500099T ATE264317T1 (de) | 1996-06-04 | 1997-06-03 | Benzimidazol-derivate mit antihistaminischer wirkung |
DE69728608T DE69728608T2 (de) | 1996-06-04 | 1997-06-03 | Benzimidazol-Derivate mit antihistaminischer Wirkung |
EP97500099A EP0818454B1 (en) | 1996-06-04 | 1997-06-03 | Benzimidazole derivatives with antihistaminic activity |
NO19972525A NO313195B1 (no) | 1996-06-04 | 1997-06-03 | Nye benzimidazolderivater med antihistaminaktivitet og farmasöytisk preparat inneholdende disse |
PT97500099T PT818454E (pt) | 1996-06-04 | 1997-06-03 | Derivados de benzimidazole com actividade anti-histaminica |
AU24672/97A AU725700B2 (en) | 1996-06-04 | 1997-06-03 | New benzimidazole derivatives with antihistaminic activity |
CA002206754A CA2206754C (en) | 1996-06-04 | 1997-06-03 | Benzimidazole derivatives with antihistaminic activity |
HR970307A HRP970307B1 (en) | 1996-06-04 | 1997-06-03 | New benzimidazole derivatives with antihistaminic activity |
RU97108980/04A RU2182150C2 (ru) | 1996-06-04 | 1997-06-03 | Производные бензимидазола, антигистаминная фармацевтическая композиция и способ лечения аллергических заболеваний |
DK97500099T DK0818454T3 (da) | 1996-06-04 | 1997-06-03 | Benzimidazolderivater med antihistamin-aktivitet |
MXPA97004127A MXPA97004127A (es) | 1996-06-04 | 1997-06-04 | Nuevos derivados de bencimidazol con actividad antihistaminica. |
BR9703276-0A BR9703276A (pt) | 1996-06-04 | 1997-06-04 | Novos derivados de benzimidazol com atividade anti-histamìnica |
IN1498DE1997 IN186319B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 1996-06-04 | 1997-06-04 | |
CZ19971723A CZ289278B6 (cs) | 1996-06-04 | 1997-06-04 | Benzimidazolové deriváty s antihistaminickou aktivitou |
CN97114905A CN1105716C (zh) | 1996-06-04 | 1997-06-04 | 具有抗组胺的新苯并咪唑衍生物 |
HU9700997A HU227598B1 (en) | 1996-06-04 | 1997-06-04 | Benzimidazole derivatives and antihistaminic pharmaceutical compositions containing them |
US08/868,743 US5877187A (en) | 1996-06-04 | 1997-06-04 | Benzimidazole derivatives with antihistaminic activity |
TR97/00464A TR199700464A3 (tr) | 1996-06-04 | 1997-06-04 | Antihistaminik etkili yeni benzimidazole türevleri. |
JP16201097A JP4218991B2 (ja) | 1996-06-04 | 1997-06-04 | 抗ヒスタミン活性を有する新規ベンズイミダゾール誘導体 |
PL97320358A PL188908B1 (pl) | 1996-06-04 | 1997-06-04 | Nowe pochodne benzimidazolu i ich zastosowanie dowytwarzania leków do leczenia stanów alergicznych |
ARP970102441A AR008386A1 (es) | 1996-06-04 | 1997-06-05 | DERIVADOS DE BENZIMIDAZOL CON ACTIVIDAD ANTIHISTAMINICA Y COMPOSICIoN FARMACÉUTICA ANTIHISTAMINICA QUE LOS CONTIENE. |
TW086110371A TW438794B (en) | 1996-06-04 | 1997-07-22 | New benzimidazole derivatives with antihistaminic activity |
LU91798C LU91798I2 (fr) | 1996-06-04 | 2011-03-22 | Bilastine |
NO2011008C NO2011008I2 (no) | 1996-06-04 | 2011-05-24 | Bilastine eller et addisjonssalt derav |
FR11C0023C FR11C0023I2 (fr) | 1996-06-04 | 2011-07-08 | Derives de benzimidazole a activite antihistaminique |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES09601236A ES2124167B1 (es) | 1996-06-04 | 1996-06-04 | Nuevos derivados del bencimidazol con actividad antihistaminica. |
Publications (2)
Publication Number | Publication Date |
---|---|
ES2124167A1 ES2124167A1 (es) | 1999-01-16 |
ES2124167B1 true ES2124167B1 (es) | 1999-09-16 |
Family
ID=8295035
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES09601236A Expired - Fee Related ES2124167B1 (es) | 1996-06-04 | 1996-06-04 | Nuevos derivados del bencimidazol con actividad antihistaminica. |
Country Status (27)
Families Citing this family (44)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL345247A1 (en) | 1998-07-01 | 2001-12-03 | Takeda Chemical Industries Ltd | Retinoid-associated receptor regulators |
PL196367B1 (pl) | 1998-11-27 | 2007-12-31 | Basf Ag | Podstawione benzimidazole, ich zastosowanie jako inhibitorów PARP oraz środek leczniczy |
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 |
CZ305162B6 (cs) | 2002-04-19 | 2015-05-27 | Faes Farma, S.A. | Polymorf 1 bilastinu, způsob jeho přípravy a lékařské aplikace a farmaceutický přípravek s jeho obsahem |
EP1511482B1 (en) * | 2002-06-13 | 2006-11-15 | 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 COMPOUNDS |
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 |
JP6284616B2 (ja) * | 2013-03-15 | 2018-02-28 | ハーキュリーズ・インコーポレーテッドHercules Incorporated | 沈着特性が改善されたパーソナルケア組成物を生成する組成物及び方法 |
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 |
ES2874577T3 (es) * | 2015-07-24 | 2021-11-05 | Urquima Sa | Formas cristalinas de bilastina y procedimientos para su preparación |
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 |
US11642309B2 (en) | 2017-10-16 | 2023-05-09 | Faes Farma, S.A. | Aqueous compositions comprising bilastine and mometasone |
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 |
ES2773756R1 (es) | 2017-12-18 | 2021-04-12 | Tiefenbacher Alfred E Gmbh & Co Kg | Composición farmacéutica en comprimido que comprende la forma 3 de bilastina y una carga soluble en agua |
AU2019209214B2 (en) | 2018-01-18 | 2023-11-23 | Faes Farma, S.A. | Ophthalmic compositions comprising bilastine, a beta-cyclodextrin and at least one gelling agent |
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 |
JP2023549381A (ja) | 2020-11-18 | 2023-11-24 | バイオファーマ・シナジーズ,エス.エル. | 抗ヒスタミン活性化合物を含む口内分散性粉末組成物 |
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 |
WO2024224326A1 (en) * | 2023-04-27 | 2024-10-31 | Leiutis Pharmaceuticals Llp | Liquid parenteral formulations of bilastine |
WO2024224308A1 (en) * | 2023-04-27 | 2024-10-31 | Leiutis Pharmaceuticals Llp | Liquid parenteral formulations of bilastine free of cyclodextrins |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8904174D0 (en) * | 1989-02-23 | 1989-04-05 | British Bio Technology | Compounds |
AU7759591A (en) * | 1990-04-13 | 1991-11-11 | Smithkline Beecham Corporation | Substituted benzimidazoles |
ES2048109B1 (es) * | 1992-07-20 | 1994-12-16 | Espanola Prod Quimicos | Procedimiento de preparacion de nuevos derivados piperidicos del bencimidazol. |
DE69334145T2 (de) * | 1992-08-03 | 2008-01-24 | Sepracor Inc., Marlborough | Terfenadincarboxylat und die Behandlung von Hautreizung |
CA2362337C (en) * | 1993-06-25 | 2005-08-02 | Merrell Pharmaceuticals Inc. | Novel intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives |
-
1996
- 1996-06-04 ES ES09601236A patent/ES2124167B1/es not_active Expired - Fee Related
-
1997
- 1997-06-03 DE DE69728608T patent/DE69728608T2/de not_active Expired - Lifetime
- 1997-06-03 AU AU24672/97A patent/AU725700B2/en not_active Expired
- 1997-06-03 DK DK97500099T patent/DK0818454T3/da active
- 1997-06-03 EP EP97500099A patent/EP0818454B1/en not_active Expired - Lifetime
- 1997-06-03 HR HR970307A patent/HRP970307B1/xx not_active IP Right Cessation
- 1997-06-03 AT AT97500099T patent/ATE264317T1/de active
- 1997-06-03 CA CA002206754A patent/CA2206754C/en not_active Expired - Lifetime
- 1997-06-03 ZA ZA9704893A patent/ZA974893B/xx unknown
- 1997-06-03 NO NO19972525A patent/NO313195B1/no not_active IP Right Cessation
- 1997-06-03 PT PT97500099T patent/PT818454E/pt unknown
- 1997-06-03 SI SI9730652T patent/SI0818454T1/xx unknown
- 1997-06-03 RU RU97108980/04A patent/RU2182150C2/ru active
- 1997-06-03 DE DE122011000006C patent/DE122011000006I1/de active Pending
- 1997-06-04 JP JP16201097A patent/JP4218991B2/ja not_active Expired - Lifetime
- 1997-06-04 US US08/868,743 patent/US5877187A/en not_active Expired - Lifetime
- 1997-06-04 IN IN1498DE1997 patent/IN186319B/en unknown
- 1997-06-04 MX MXPA97004127A patent/MXPA97004127A/es active IP Right Grant
- 1997-06-04 CZ CZ19971723A patent/CZ289278B6/cs not_active IP Right Cessation
- 1997-06-04 PL PL97320358A patent/PL188908B1/pl unknown
- 1997-06-04 HU HU9700997A patent/HU227598B1/hu active Protection Beyond IP Right Term
- 1997-06-04 TR TR97/00464A patent/TR199700464A3/tr unknown
- 1997-06-04 BR BR9703276-0A patent/BR9703276A/pt not_active IP Right Cessation
- 1997-06-04 CN CN97114905A patent/CN1105716C/zh not_active Expired - Lifetime
- 1997-06-05 AR ARP970102441A patent/AR008386A1/es active IP Right Grant
- 1997-07-22 TW TW086110371A patent/TW438794B/zh not_active IP Right Cessation
-
2011
- 2011-03-22 LU LU91798C patent/LU91798I2/fr unknown
- 2011-05-24 NO NO2011008C patent/NO2011008I2/no unknown
- 2011-07-08 FR FR11C0023C patent/FR11C0023I2/fr active Active
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