RU2015111229A - Кристаллические формы гидрохлорида финголимода - Google Patents
Кристаллические формы гидрохлорида финголимода Download PDFInfo
- Publication number
- RU2015111229A RU2015111229A RU2015111229/04A RU2015111229A RU2015111229A RU 2015111229 A RU2015111229 A RU 2015111229A RU 2015111229/04 A RU2015111229/04 A RU 2015111229/04A RU 2015111229 A RU2015111229 A RU 2015111229A RU 2015111229 A RU2015111229 A RU 2015111229A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline
- salt
- fty720
- octylphenyl
- theta
- Prior art date
Links
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims abstract 12
- 229960000556 fingolimod Drugs 0.000 claims abstract 8
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 8
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims abstract 6
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract 4
- 230000004968 inflammatory condition Effects 0.000 claims abstract 4
- 238000000034 method Methods 0.000 claims abstract 4
- 210000000056 organ Anatomy 0.000 claims abstract 4
- -1 2- (4-octylphenyl) ethyl Chemical group 0.000 claims abstract 3
- SWZTYAVBMYWFGS-UHFFFAOYSA-N fingolimod hydrochloride Chemical compound Cl.CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 SWZTYAVBMYWFGS-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
- C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08168865.7 | 2008-11-11 | ||
| EP08168865 | 2008-11-11 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011123371/04A Division RU2549899C2 (ru) | 2008-11-11 | 2009-11-10 | Кристаллические формы гидрохлорида финголимода |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2015111229A true RU2015111229A (ru) | 2015-11-20 |
| RU2015111229A3 RU2015111229A3 (enExample) | 2018-11-08 |
Family
ID=40521487
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011123371/04A RU2549899C2 (ru) | 2008-11-11 | 2009-11-10 | Кристаллические формы гидрохлорида финголимода |
| RU2015111229/04A RU2015111229A (ru) | 2008-11-11 | 2009-11-10 | Кристаллические формы гидрохлорида финголимода |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011123371/04A RU2549899C2 (ru) | 2008-11-11 | 2009-11-10 | Кристаллические формы гидрохлорида финголимода |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8530522B2 (enExample) |
| EP (1) | EP2356090B1 (enExample) |
| JP (4) | JP2012508216A (enExample) |
| KR (2) | KR20130109254A (enExample) |
| CN (3) | CN102209705A (enExample) |
| AU (1) | AU2009315736B2 (enExample) |
| BR (1) | BRPI0921826A2 (enExample) |
| CA (1) | CA2743232C (enExample) |
| ES (1) | ES2643161T3 (enExample) |
| MX (1) | MX2011004962A (enExample) |
| PL (1) | PL2356090T3 (enExample) |
| PT (1) | PT2356090T (enExample) |
| RU (2) | RU2549899C2 (enExample) |
| WO (1) | WO2010055028A2 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2746939T3 (es) * | 2010-10-01 | 2020-03-09 | Synthon Bv | Procedimiento para la preparación de cristales de clorhidrato de fingolimod |
| MX2013004649A (es) | 2010-10-28 | 2013-06-05 | Mapi Pharma Ltd | Compuestos intermedios y proceso para la preparacion de fingolimod. |
| 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 |
| US9216943B2 (en) | 2011-04-29 | 2015-12-22 | Dr. Reddy's Laboratories Ltd. | Preparation of fingolimod and its salts |
| US9751834B2 (en) | 2011-05-26 | 2017-09-05 | Gri Bio, Inc. | Oxygenated amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives and their medical use |
| WO2012160188A1 (en) | 2011-05-26 | 2012-11-29 | Jado Technologies Gmbh | Hydroxy-substituted amino and ammonium derivatives and their medical use |
| DK2809318T3 (da) | 2011-05-26 | 2019-07-22 | Gri Bio Inc | Ammoniumholdige sulfonsyre-, phosphonsyre- og carboxylsyrederivater og disses medicinske anvendelse |
| EA028950B1 (ru) | 2011-08-01 | 2018-01-31 | Тева Фармасьютикал Индастриз Лтд. | Способ получения фармацевтических композиций, содержащих финголимод |
| 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 |
| EP2945927A4 (en) * | 2013-01-17 | 2017-01-18 | Shilpa Medicare Limited | Process for preparation of fingolimod and its salts |
| JP6484567B2 (ja) | 2013-03-05 | 2019-03-13 | バイオコン・リミテッドＢｉｏｃｏｎ Ｌｉｍｉｔｅｄ | ２−アミノ−１，３−プロパンジオール化合物およびその塩の製造のための方法 |
| US20160128951A1 (en) | 2013-07-29 | 2016-05-12 | 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 |
| 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 |
| 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 |
| 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 |
| CA3156298A1 (en) | 2019-10-31 | 2021-05-06 | Laetitia POUZOL | Combination of a cxcr7 antagonist with an s1p1 receptor modulator |
| JP2024521882A (ja) | 2021-05-31 | 2024-06-04 | 上海雲晟研新生物科技有限公司 | フィンゴリモド薬用塩、製造方法、それを含む医薬組成物及び使用 |
| 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 (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0627406B1 (en) * | 1992-10-21 | 1998-10-28 | Yoshitomi Pharmaceutical Industries, Ltd. | 2-amino-1,3-propanediol compound and immunosuppressant |
| 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 |
| EP1457478B1 (en) * | 1998-11-11 | 2017-07-19 | Novartis AG | Production of 2-amino-2-[2-(4-alkyl-phenyl)ethyl]propane-1,3-diols |
| PT1031347E (pt) * | 1999-01-27 | 2002-09-30 | Idea Ag | Transporte/imunizacao transnasal com veiculos muitissimo adaptaveis |
| CN1230421C (zh) * | 1999-02-10 | 2005-12-07 | 三菱制药株式会社 | 酰胺化合物及其药物用途 |
| 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 |
| PL372103A1 (en) * | 2002-05-16 | 2005-07-11 | Novartis Ag | Use of edg receptor binding agents in cancer |
| GB0217152D0 (en) * | 2002-07-24 | 2002-09-04 | Novartis Ag | Organic compounds |
| NZ592339A (en) * | 2003-04-08 | 2012-09-28 | Novartis Ag | Solid pharmaceutical compositions of S1P receptor agonist with 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 |
| EP1940388A2 (en) * | 2005-09-30 | 2008-07-09 | Novartis AG | Dpp iv inhibtor for use in the treatment of autoimmune diseases and graft rejection |
| 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 |
| US8318812B2 (en) * | 2006-06-02 | 2012-11-27 | The Ohio State University Research Foundation | Therapeutic agents for the treatment of lymphoid malignancies |
| KR20090057399A (ko) * | 2006-09-26 | 2009-06-05 | 노파르티스 아게 | Ｓ１ｐ 조정제를 포함하는 제약 조성물 |
| WO2009155475A1 (en) * | 2008-06-20 | 2009-12-23 | Novartis Ag | Paediatric compositions for treating1 multiple sclerosis |
| ES2746939T3 (es) | 2010-10-01 | 2020-03-09 | Synthon Bv | Procedimiento para la preparación de cristales de clorhidrato de fingolimod |
-
2009
- 2009-11-10 CN CN200980144998XA patent/CN102209705A/zh active Pending
- 2009-11-10 JP JP2011535130A patent/JP2012508216A/ja not_active Withdrawn
- 2009-11-10 RU RU2011123371/04A patent/RU2549899C2/ru active
- 2009-11-10 PT PT97483507T patent/PT2356090T/pt unknown
- 2009-11-10 EP EP09748350.7A patent/EP2356090B1/en active Active
- 2009-11-10 BR BRPI0921826A patent/BRPI0921826A2/pt not_active Application Discontinuation
- 2009-11-10 RU RU2015111229/04A patent/RU2015111229A/ru not_active Application Discontinuation
- 2009-11-10 CN CN201710377640.8A patent/CN107233336A/zh active Pending
- 2009-11-10 AU AU2009315736A patent/AU2009315736B2/en not_active Ceased
- 2009-11-10 MX MX2011004962A patent/MX2011004962A/es active IP Right Grant
- 2009-11-10 WO PCT/EP2009/064891 patent/WO2010055028A2/en not_active Ceased
- 2009-11-10 CN CN201510141353.8A patent/CN104788325A/zh active Pending
- 2009-11-10 KR KR1020137024001A patent/KR20130109254A/ko not_active Withdrawn
- 2009-11-10 KR KR1020117010560A patent/KR101393994B1/ko not_active Expired - Fee Related
- 2009-11-10 PL PL09748350T patent/PL2356090T3/pl unknown
- 2009-11-10 ES ES09748350.7T patent/ES2643161T3/es active Active
- 2009-11-10 US US13/128,825 patent/US8530522B2/en not_active Expired - Fee Related
- 2009-11-10 CA CA2743232A patent/CA2743232C/en active Active
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| CA2743232A1 (en) | 2010-05-20 |
| US20110229501A1 (en) | 2011-09-22 |
| EP2356090A2 (en) | 2011-08-17 |
| WO2010055028A3 (en) | 2010-07-08 |
| MX2011004962A (es) | 2011-05-30 |
| RU2015111229A3 (enExample) | 2018-11-08 |
| CN102209705A (zh) | 2011-10-05 |
| ES2643161T3 (es) | 2017-11-21 |
| JP2014139179A (ja) | 2014-07-31 |
| JP2018035160A (ja) | 2018-03-08 |
| RU2011123371A (ru) | 2012-12-20 |
| JP2016028056A (ja) | 2016-02-25 |
| WO2010055028A2 (en) | 2010-05-20 |
| EP2356090B1 (en) | 2017-07-05 |
| AU2009315736B2 (en) | 2013-08-29 |
| KR20110069156A (ko) | 2011-06-22 |
| CA2743232C (en) | 2015-12-29 |
| CN107233336A (zh) | 2017-10-10 |
| KR20130109254A (ko) | 2013-10-07 |
| CN104788325A (zh) | 2015-07-22 |
| US8530522B2 (en) | 2013-09-10 |
| PT2356090T (pt) | 2017-10-16 |
| JP2012508216A (ja) | 2012-04-05 |
| RU2549899C2 (ru) | 2015-05-10 |
| US20140051766A1 (en) | 2014-02-20 |
| PL2356090T3 (pl) | 2017-12-29 |
| BRPI0921826A2 (pt) | 2016-01-12 |
| AU2009315736A1 (en) | 2010-05-20 |
| KR101393994B1 (ko) | 2014-05-14 |
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