CA2993134A1 - Crystalline forms of bilastine and preparation methods thereof - Google Patents

Crystalline forms of bilastine and preparation methods thereof Download PDF

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Publication number
CA2993134A1
CA2993134A1 CA2993134A CA2993134A CA2993134A1 CA 2993134 A1 CA2993134 A1 CA 2993134A1 CA 2993134 A CA2993134 A CA 2993134A CA 2993134 A CA2993134 A CA 2993134A CA 2993134 A1 CA2993134 A1 CA 2993134A1
Authority
CA
Canada
Prior art keywords
bilastine
crystalline form
eta
preparation
alpha
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.)
Pending
Application number
CA2993134A
Other languages
English (en)
French (fr)
Inventor
Jose Luis Del Rio Pericacho
Maria Cristina Puigjaner Vallet
Rafael Prohens Lopez
Yolanda Esther ARREDONDO MARTINEZ
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.)
Disproquima Sa
Urquima SA
Original Assignee
Disproquima Sa
Urquima 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 Disproquima Sa, Urquima SA filed Critical Disproquima Sa
Publication of CA2993134A1 publication Critical patent/CA2993134A1/en
Pending legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2993134A 2015-07-24 2016-07-22 Crystalline forms of bilastine and preparation methods thereof Pending CA2993134A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ES201531103 2015-07-24
ESP201531103 2015-07-24
PCT/ES2016/070560 WO2017017301A1 (es) 2015-07-24 2016-07-22 Formas cristalinas de bilastina y procedimientos para su preparación

Publications (1)

Publication Number Publication Date
CA2993134A1 true CA2993134A1 (en) 2017-02-02

Family

ID=57884122

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2993134A Pending CA2993134A1 (en) 2015-07-24 2016-07-22 Crystalline forms of bilastine and preparation methods thereof

Country Status (13)

Country Link
EP (1) EP3327012B1 (enExample)
JP (1) JP7168447B2 (enExample)
KR (1) KR102657147B1 (enExample)
CN (1) CN107849007B (enExample)
CA (1) CA2993134A1 (enExample)
CY (1) CY1124505T1 (enExample)
ES (2) ES2600827B9 (enExample)
LT (1) LT3327012T (enExample)
MX (1) MX382563B (enExample)
PL (1) PL3327012T3 (enExample)
PT (1) PT3327012T (enExample)
SI (1) SI3327012T1 (enExample)
WO (1) WO2017017301A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP3453384B1 (en) 2017-09-07 2020-05-27 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising bilastine
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
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
BR112021005403A2 (pt) * 2018-09-25 2021-06-15 Glenmark Life Sciences Limited processos para a preparação de forma cristalina 2 de bilastina e para a preparação de solvato de p-xileno de bilastina, e, solvato de p-xileno de bilastina

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2124167B1 (es) * 1996-06-04 1999-09-16 Espanola Prod Quimicos Nuevos derivados del bencimidazol con actividad antihistaminica.
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
CZ307500B6 (cs) * 2012-08-15 2018-10-24 Zentiva, K.S. Způsob přípravy derivátu 2-methyl-2´-fenylpropionové kyseliny využívající nové intermediáty
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
CN104447682A (zh) * 2013-09-12 2015-03-25 天津市汉康医药生物技术有限公司 比拉斯汀化合物
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
SK7066Y1 (sk) * 2014-01-29 2015-03-03 Zentiva Ks Kryštalický dihydrát bilastínu
CN103788062A (zh) * 2014-02-17 2014-05-14 北京博泽德润医药科技开发有限公司 一种比拉斯汀晶型及其制备方法
CN104151290A (zh) * 2014-06-30 2014-11-19 北京万全德众医药生物技术有限公司 一种制备比拉斯汀新晶型的方法
CN104177331B (zh) * 2014-09-10 2016-08-17 北京科莱博医药开发有限责任公司 比拉斯汀的制备方法
CN104530002B (zh) * 2015-01-29 2017-06-09 天津梅花生物医药科技有限公司 比拉斯汀化合物及其制备方法

Also Published As

Publication number Publication date
ES2874577T3 (es) 2021-11-05
CN107849007A (zh) 2018-03-27
WO2017017301A1 (es) 2017-02-02
ES2600827B1 (es) 2017-11-24
MX382563B (es) 2025-03-13
SI3327012T1 (sl) 2021-10-29
EP3327012A4 (en) 2018-12-19
PL3327012T3 (pl) 2021-11-22
JP2018522945A (ja) 2018-08-16
RU2018104258A3 (enExample) 2019-12-25
CN107849007B (zh) 2024-08-09
EP3327012B1 (en) 2021-03-17
LT3327012T (lt) 2021-09-10
BR112018001225A2 (pt) 2018-09-11
KR20180036722A (ko) 2018-04-09
ES2600827A1 (es) 2017-02-10
ES2600827A8 (es) 2017-06-15
RU2018104258A (ru) 2019-08-26
KR102657147B1 (ko) 2024-04-12
PT3327012T (pt) 2021-06-21
JP7168447B2 (ja) 2022-11-09
ES2600827B9 (es) 2018-03-28
CY1124505T1 (el) 2022-07-22
MX2018000883A (es) 2018-08-15
EP3327012A1 (en) 2018-05-30

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