JP7168447B2 - ビラスチンの結晶形態及びそれらの調製方法 - Google Patents

ビラスチンの結晶形態及びそれらの調製方法 Download PDF

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JP7168447B2
JP7168447B2 JP2018522878A JP2018522878A JP7168447B2 JP 7168447 B2 JP7168447 B2 JP 7168447B2 JP 2018522878 A JP2018522878 A JP 2018522878A JP 2018522878 A JP2018522878 A JP 2018522878A JP 7168447 B2 JP7168447 B2 JP 7168447B2
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bilastine
crystalline form
temperature
eta
crystalline
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JP2018522945A (ja
JP2018522945A5 (enExample
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リオ ペリカチョ，ホセ ルイス デル
バリェト，マリア クリスティーナ プイグハネル
ロペス，ラファエル プロヘンス
マルチネス，ヨランダ エステール アルレドンド
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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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • 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)
JP2018522878A 2015-07-24 2016-07-22 ビラスチンの結晶形態及びそれらの調製方法 Active JP7168447B2 (ja)

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

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JP2018522945A JP2018522945A (ja) 2018-08-16
JP2018522945A5 JP2018522945A5 (enExample) 2019-08-22
JP7168447B2 true JP7168447B2 (ja) 2022-11-09

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JP2018522878A Active JP7168447B2 (ja) 2015-07-24 2016-07-22 ビラスチンの結晶形態及びそれらの調製方法

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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

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005529120A (ja) 2002-04-19 2005-09-29 ファエス・ファルマ・ソシエダッド・アノニマ 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
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
WO2014026657A2 (en) 2012-08-15 2014-02-20 Zentiva, K.S A process for the preparation of a derivative of 2-methyl-2'-phenylpropionic acid using new intermediates
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
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

Family Cites Families (5)

* 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.
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
SK7066Y1 (sk) * 2014-01-29 2015-03-03 Zentiva Ks Kryštalický dihydrát bilastínu
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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005529120A (ja) 2002-04-19 2005-09-29 ファエス・ファルマ・ソシエダッド・アノニマ 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
WO2014026657A2 (en) 2012-08-15 2014-02-20 Zentiva, K.S A process for the preparation of a derivative of 2-methyl-2'-phenylpropionic acid using new intermediates
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
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
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

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
厚生省医薬安全局審査管理課長，医薬品の残留溶媒ガイドラインについて，医薬審，１９９８年，第３０７号，ｐｐ．１－１１
平山令明，有機化合物結晶作製ハンドブック，２００８年 ７月２５日，ｐ．１７－２３，３７－４０，４５－５１，５７－６５
高田則幸，創薬段階における原薬Ｆｏｒｍスクリーニングと選択，ＰＨＡＲＭ ＳＴＡＧＥ，２００７年 １月１５日，Ｖｏｌ．６， Ｎｏ．１０，ｐ．２０－２５

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Publication number Publication date
CA2993134A1 (en) 2017-02-02
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
ES2600827B9 (es) 2018-03-28
CY1124505T1 (el) 2022-07-22
MX2018000883A (es) 2018-08-15
EP3327012A1 (en) 2018-05-30

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