JP2018035160A5 - - Google Patents
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- JP2018035160A5 JP2018035160A5 JP2017172276A JP2017172276A JP2018035160A5 JP 2018035160 A5 JP2018035160 A5 JP 2018035160A5 JP 2017172276 A JP2017172276 A JP 2017172276A JP 2017172276 A JP2017172276 A JP 2017172276A JP 2018035160 A5 JP2018035160 A5 JP 2018035160A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- hydrate
- composition according
- substantially pure
- crystalline form
- 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
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- 238000000634 powder X-ray diffraction Methods 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- YPFDHNVEDLHUCE-UHFFFAOYSA-N 1,3-Propanediol Chemical compound OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims 1
- -1 2- (4-octylphenyl) ethyl Chemical group 0.000 claims 1
- 206010003816 Autoimmune disease Diseases 0.000 claims 1
- KKGQTZUTZRNORY-UHFFFAOYSA-N Fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960000556 fingolimod Drugs 0.000 claims 1
- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 210000000056 organs Anatomy 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 238000004566 IR spectroscopy Methods 0.000 description 1
- 238000002065 inelastic X-ray scattering Methods 0.000 description 1
- 150000003839 salts Chemical group 0.000 description 1
Description
本発明の実施形態において、本発明の様々な結晶塩形は、実質的に純粋な結晶形である。本明細書で使用される「実質的に純粋な」という用語は、例えばＸ線粉末回折、ラマン分光法またはＩＲ分光法により求められる多形純度が、９０％以上、より好ましくは９５％以上、より好ましくは９６％以上、より好ましくは９７％以上、より好ましくは９８％以上、より好ましくは９９％以上である、結晶形に関する基準を含む。
Claims (4)
- ２−アミノ−２−（２−（４−オクチルフェニル）エチル）プロパン−１，３−ジオール（ＦＴＹ７２０）の結晶性塩酸塩水和物を含む医薬組成物であって、
前記水和物は、２．９、１７．２、３０．６、２８．２、２４．４、８．６および２５．９度±０．２度の２θのピークを含むＸ線粉末回折パターンを特徴とし、
前記水和物中の水含有率は５．２〜５．９％である、医薬組成物。 - 前記水和物は、実質的に純粋な結晶形であり、
前記実質的に純粋とは、多形純度が９０％以上である結晶形に関する基準を含む、請求項１に記載の医薬組成物。 - 臓器移植もしくは組織移植の拒絶、自己免疫疾患または炎症状態の治療または予防において使用するための、請求項１または２に記載の医薬組成物。
- 薬学的に許容される担体または賦形剤をさらに含む、請求項１から３のいずれかに記載の医薬組成物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08168865 | 2008-11-11 | ||
| EP08168865.7 | 2008-11-11 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015173474A Division JP2016028056A (ja) | 2008-11-11 | 2015-09-03 | 有機化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018035160A JP2018035160A (ja) | 2018-03-08 |
| JP2018035160A5 true JP2018035160A5 (ja) | 2019-01-31 |
Family
ID=40521487
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535130A Withdrawn JP2012508216A (ja) | 2008-11-11 | 2009-11-10 | 有機化合物 |
| JP2014020950A Withdrawn JP2014139179A (ja) | 2008-11-11 | 2014-02-06 | 有機化合物 |
| JP2015173474A Withdrawn JP2016028056A (ja) | 2008-11-11 | 2015-09-03 | 有機化合物 |
| JP2017172276A Pending JP2018035160A (ja) | 2008-11-11 | 2017-09-07 | 有機化合物 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535130A Withdrawn JP2012508216A (ja) | 2008-11-11 | 2009-11-10 | 有機化合物 |
| JP2014020950A Withdrawn JP2014139179A (ja) | 2008-11-11 | 2014-02-06 | 有機化合物 |
| JP2015173474A Withdrawn JP2016028056A (ja) | 2008-11-11 | 2015-09-03 | 有機化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8530522B2 (ja) |
| EP (1) | EP2356090B1 (ja) |
| JP (4) | JP2012508216A (ja) |
| KR (2) | KR20130109254A (ja) |
| CN (3) | CN104788325A (ja) |
| AU (1) | AU2009315736B2 (ja) |
| BR (1) | BRPI0921826A2 (ja) |
| CA (1) | CA2743232C (ja) |
| ES (1) | ES2643161T3 (ja) |
| MX (1) | MX2011004962A (ja) |
| PL (1) | PL2356090T3 (ja) |
| PT (1) | PT2356090T (ja) |
| RU (2) | RU2549899C2 (ja) |
| WO (1) | WO2010055028A2 (ja) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2621889B1 (en) | 2010-10-01 | 2019-07-17 | Synthon BV | Process for making fingolimod hydrochloride crystals |
| PL2632889T3 (pl) | 2010-10-28 | 2019-04-30 | Mapi Pharma Ltd | Związki pośrednie i sposób wytwarzania fingolimodu |
| WO2012071524A1 (en) | 2010-11-24 | 2012-05-31 | Ratiopharm Gmbh | Arylsulfonate salts of fingolimod and processes for preparation thereof |
| WO2012070059A1 (en) | 2010-11-25 | 2012-05-31 | Shilpa Medicare Limited | Fingolimod polymorphs and their processes |
| ES2746016T3 (es) | 2010-12-28 | 2020-03-04 | Synthon Bv | Procedimiento para la preparación de cristales de clorhidrato de fingolimod |
| WO2012097330A2 (en) * | 2011-01-14 | 2012-07-19 | University Of Washington | Compositions and methods for treating degenerative muscle conditions |
| EP2702034A4 (en) | 2011-04-29 | 2015-03-25 | Reddys Lab Ltd Dr | PREPARATION OF FINGOLIMOD AND ITS SALTS |
| ES2581482T3 (es) | 2011-05-26 | 2016-09-06 | Jado Technologies Gmbh | Derivados de amino y amonio hidroxi-sustituidos y su uso médico |
| DK2809648T3 (da) | 2011-05-26 | 2019-06-17 | Gri Bio Inc | Oxygenberigede amino- eller ammonium-holdige sulfonsyrederivater og disses medicinske anvendelse |
| EP2809318B1 (en) | 2011-05-26 | 2019-05-08 | GRI Bio, Inc. | Ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use |
| WO2013019872A1 (en) | 2011-08-01 | 2013-02-07 | Teva Pharmaceutical Industries Ltd. | Process for preparing pharmaceutical compositions comprising fingolimod |
| WO2013091704A1 (en) * | 2011-12-22 | 2013-06-27 | Synthon Bv | Pharmaceutical composition comprising fingolimod |
| CN102887829B (zh) * | 2012-09-05 | 2014-07-02 | 中国科学院上海药物研究所 | 芬戈莫德粘酸盐及其晶体的制备方法和用途 |
| NZ630290A (en) * | 2013-01-17 | 2016-09-30 | Shilpa Medicare Ltd | Process for preparation of fingolimod and its salts |
| CA2903708C (en) | 2013-03-05 | 2021-07-13 | Biocon Limited | A process for the preparation of 2-amino-1,3-propane diol compounds and salts thereof |
| CA2920758A1 (en) | 2013-07-29 | 2015-02-05 | Aizant Drug Research Solutions Pvt Ltd | Pharmaceutical compositions of fingolimod |
| WO2016042493A1 (en) | 2014-09-19 | 2016-03-24 | Aizant Drug Research Pvt. Ltd | Pharmaceutical compositions of fingolimod |
| US9925138B2 (en) | 2015-01-20 | 2018-03-27 | Handa Pharmaceuticals, Llc | Stable solid fingolimod dosage forms |
| RU2627691C1 (ru) * | 2016-07-06 | 2017-08-10 | Олег Ростиславович Михайлов | Кристаллическая η-модификация 2-амино-2-(2-(4-октилфенил)этил)пропан-1,3-диол гидрохлорида, способ её получения и фармацевтическая композиция на её основе |
| CN106860440A (zh) * | 2017-01-16 | 2017-06-20 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗系统性红斑狼疮脑病药物中的应用 |
| CN106667981B (zh) * | 2017-01-16 | 2019-05-14 | 南京医科大学第二附属医院 | 盐酸芬戈莫德在制备治疗药物性肝损伤药物中的应用 |
| GR1009654B (el) | 2018-08-31 | 2019-11-18 | Φαρματεν Α.Β.Ε.Ε. | Φαρμακευτικο σκευασμα που περιλαμβανει εναν ανοσοτροποποιητικο παραγοντα και μεθοδος για την παρασκευη αυτου |
| WO2020245775A1 (en) * | 2019-06-05 | 2020-12-10 | Biocon Limited | Crystalline forms of 2-amino-2-(2-(4-octylphenyl) ethyl) propane-1,3-diol |
| CN114599363A (zh) | 2019-10-31 | 2022-06-07 | 爱杜西亚药品有限公司 | Cxcr7拮抗剂与s1p1受体调节剂的组合 |
| EP4353709A1 (en) | 2021-05-31 | 2024-04-17 | Shanghai Yonsun Biotechnology Co., Ltd. | Pharmaceutical salt of fingolimod, preparation method therefor, pharmaceutical composition containing same and use thereof |
| EP4212156A1 (en) | 2022-01-13 | 2023-07-19 | Abivax | Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a s1p receptor modulator |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE122011100012I1 (de) * | 1992-10-21 | 2011-10-20 | Mitsubishi Tanabe Pharma Corp | 2-Amino-1, 3-propandiolverbindung und immunosuppressium. |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| JP4079505B2 (ja) * | 1998-04-28 | 2008-04-23 | 田辺三菱製薬株式会社 | ２−アミノ−２−［２−（４−オクチルフェニル）エチル］プロパン−１，３−ジオールの新規な製造法 |
| JP4503184B2 (ja) * | 1998-11-11 | 2010-07-14 | ノヴァルティス アーゲー | ２−アミノ−２−［２−（４−ｃ２−２０−アルキル−フェニル）エチル］プロパン−１，３−ジオール類の製造 |
| DK1031347T3 (da) * | 1999-01-27 | 2002-07-08 | Idea Ag | Transnasal transport/immunisering med meget tilpasselige bærere |
| EP1176140B1 (en) * | 1999-02-10 | 2004-12-29 | Mitsubishi Pharma Corporation | Amide compounds and medicinal use thereof |
| CN1144779C (zh) * | 1999-03-11 | 2004-04-07 | 杭州中美华东制药有限公司 | 制备2-[2-(4-烷基苯基)-乙基]-2-氨基-丙二醇的方法以及其中制得的中间产物 |
| PL364359A1 (en) * | 2001-06-08 | 2004-12-13 | Novartis Ag | Treatment or prophylaxis of insulin-producing cell graft rejection |
| US20030144712A1 (en) * | 2001-12-20 | 2003-07-31 | Jackson Streeter, M.D. | Methods for overcoming organ transplant rejection |
| NZ560662A (en) * | 2002-05-16 | 2009-09-25 | Novartis Ag | Use of EDG receptor binding agents in cancer |
| GB0217152D0 (en) * | 2002-07-24 | 2002-09-04 | Novartis Ag | Organic compounds |
| NZ542622A (en) | 2003-04-08 | 2009-01-31 | Novartis Ag | Solid pharmaceutical compositions comprising a S1P receptor agonist and a sugar alcohol |
| CN1212308C (zh) * | 2003-07-24 | 2005-07-27 | 漆又毛 | 2－氨基－2－（2－（4－辛基苯基）乙基）－1，3－丙二醇盐酸盐的制备方法 |
| CN1241903C (zh) * | 2003-10-14 | 2006-02-15 | 马启明 | 制备2－对辛基苯乙基－2－氨基丙二醇的方法 |
| TWI418350B (zh) * | 2005-06-24 | 2013-12-11 | Sankyo Co | 含有ｐｐａｒ調節劑之醫藥組成物的用途 |
| AU2006297130B2 (en) * | 2005-09-30 | 2009-12-24 | Novartis Ag | DPP IV inhibitor for use in the treatment of autoimmune diseases and graft rejection |
| ATE534630T1 (de) * | 2005-10-26 | 2011-12-15 | Merck Serono Sa | Sulfonamidderivate und deren verwendung zur modulation von metalloproteinasen |
| CN1310869C (zh) * | 2005-11-22 | 2007-04-18 | 江苏吴中苏药医药开发有限责任公司 | 2－氨基－2－[2－(4－烷基苯基)乙基]－1,3－丙二醇的制备方法 |
| CN100548968C (zh) * | 2006-03-01 | 2009-10-14 | 徐州师范大学 | 一种制备2-对辛基苯乙基-2-氨基丙二醇盐酸盐的方法 |
| EP2046315B1 (en) * | 2006-06-02 | 2013-04-10 | The Ohio State University Research Foundation | Therapeutic agents for the treatment of mantle cell lymphoma |
| CN102579387A (zh) * | 2006-09-26 | 2012-07-18 | 诺瓦提斯公司 | 包含s1p调节剂的药物组合物 |
| KR20160131126A (ko) * | 2008-06-20 | 2016-11-15 | 노파르티스 아게 | 다발성 경화증을 치료하기 위한 소아용 조성물 |
| EP2621889B1 (en) | 2010-10-01 | 2019-07-17 | Synthon BV | Process for making fingolimod hydrochloride crystals |
-
2009
- 2009-11-10 BR BRPI0921826A patent/BRPI0921826A2/pt not_active Application Discontinuation
- 2009-11-10 AU AU2009315736A patent/AU2009315736B2/en not_active Ceased
- 2009-11-10 EP EP09748350.7A patent/EP2356090B1/en active Active
- 2009-11-10 CN CN201510141353.8A patent/CN104788325A/zh active Pending
- 2009-11-10 KR KR1020137024001A patent/KR20130109254A/ko not_active Application Discontinuation
- 2009-11-10 CA CA2743232A patent/CA2743232C/en active Active
- 2009-11-10 US US13/128,825 patent/US8530522B2/en active Active
- 2009-11-10 PL PL09748350T patent/PL2356090T3/pl unknown
- 2009-11-10 RU RU2011123371/04A patent/RU2549899C2/ru active
- 2009-11-10 CN CN200980144998XA patent/CN102209705A/zh active Pending
- 2009-11-10 PT PT97483507T patent/PT2356090T/pt unknown
- 2009-11-10 CN CN201710377640.8A patent/CN107233336A/zh active Pending
- 2009-11-10 JP JP2011535130A patent/JP2012508216A/ja not_active Withdrawn
- 2009-11-10 MX MX2011004962A patent/MX2011004962A/es active IP Right Grant
- 2009-11-10 KR KR1020117010560A patent/KR101393994B1/ko active IP Right Grant
- 2009-11-10 WO PCT/EP2009/064891 patent/WO2010055028A2/en active Application Filing
- 2009-11-10 ES ES09748350.7T patent/ES2643161T3/es active Active
- 2009-11-10 RU RU2015111229/04A patent/RU2015111229A/ru not_active Application Discontinuation
-
2013
- 2013-08-12 US US13/964,817 patent/US20140051766A1/en not_active Abandoned
-
2014
- 2014-02-06 JP JP2014020950A patent/JP2014139179A/ja not_active Withdrawn
-
2015
- 2015-09-03 JP JP2015173474A patent/JP2016028056A/ja not_active Withdrawn
-
2017
- 2017-09-07 JP JP2017172276A patent/JP2018035160A/ja active Pending
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