JP2012508215A5 - - Google Patents
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- JP2012508215A5 JP2012508215A5 JP2011535129A JP2011535129A JP2012508215A5 JP 2012508215 A5 JP2012508215 A5 JP 2012508215A5 JP 2011535129 A JP2011535129 A JP 2011535129A JP 2011535129 A JP2011535129 A JP 2011535129A JP 2012508215 A5 JP2012508215 A5 JP 2012508215A5
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- JP
- Japan
- Prior art keywords
- salt
- salt according
- optionally
- degrees
- ray powder
- 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.)
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- 150000003839 salts Chemical class 0.000 claims 15
- 239000013078 crystal Substances 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims 3
- 206010052779 Transplant rejections Diseases 0.000 claims 3
- 230000004968 inflammatory condition Effects 0.000 claims 3
- 210000000056 organ Anatomy 0.000 claims 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- YPFDHNVEDLHUCE-UHFFFAOYSA-N propane-1,3-diol Chemical compound OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims 2
- 229940095064 tartrate Drugs 0.000 claims 2
- -1 4-octylphenyl Chemical group 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- 159000000021 acetate salts Chemical group 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 150000001558 benzoic acid derivatives Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 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
- 229960000556 fingolimod Drugs 0.000 claims 1
- 150000003893 lactate salts Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000003891 oxalate salts Chemical class 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 150000003892 tartrate salts Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Claims (15)
- 酒石酸塩、乳酸塩、安息香酸塩、琥珀酸塩、マロン酸塩、酢酸塩およびプロピオン酸塩から選択され、場合によって、結晶性である、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）の塩。
- 酒石酸塩、乳酸塩、琥珀酸塩およびマロン酸塩から選択され、場合によって、結晶性である、請求項１に記載の塩。
- 約３．１、１９．３、２１．７、９．６、１７．２、６．４、２２．６および２０．８度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、酒石酸塩である、請求項２に記載の塩。
- 約４．３、８．７、２０．８、１３．１、１０．３、１８．８、８．１、２１．６、２１．９および１９．６度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、乳酸塩である、請求項２に記載の塩。
- 約３．７、７．５、１８．７、１９．８、１５．２、１９．４、１９．９、６．０および２１．９度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、安息香酸塩である、請求項２に記載の塩。
- 約３．２、１９．８、２０．７、２３．３、２６．２、９．８、１９．４、２４．５、３３．４、２６．６および２２．６度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、琥珀酸塩である、請求項２に記載の塩。
- 約２．５、５．２、８．０、１６．２、１７．０および２０．４度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、マロン酸塩である、請求項２に記載の塩。
- 約４．８、８．４、１０．１、１１．５、１５．２、１７．７、１９．３、２０．１、２１．５、２１．９、２４．０、２５．４および３０．８度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、酢酸塩である、請求項１に記載の塩。
- 約４．８、８．４、９．８、１４．７、１６．８、１７．６、１９．７、２０．２、２２．６、２４．８、２９．８度の２θにピークを有するＸ線粉末回折パターンを特徴とする結晶形を場合によって含む、プロピオン酸塩である、請求項１に記載の塩。
- 実質的に純粋な結晶形である、請求項１から９のいずれかに記載の塩。
- 治療で使用される、請求項１から１０のいずれかに記載の塩。
- 臓器または組織移植拒絶、自己免疫疾患または炎症状態の治療または予防に使用する、請求項１から１０のいずれかに記載の塩。
- 薬学的に許容される担体または賦形剤と一緒に請求項１から１０のいずれかに記載の塩を含む医薬組成物。
- 臓器または組織移植拒絶、自己免疫疾患または炎症状態の治療または予防のための医薬の製造のための、請求項１から１０のいずれかに記載の塩の使用。
- 請求項１から１０のいずれかに記載の治療有効量の塩を含む、患者の臓器または組織移植拒絶、自己免疫疾患または炎症状態の治療または予防用医薬組成物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08168862 | 2008-11-11 | ||
| EP08168862.4 | 2008-11-11 | ||
| PCT/EP2009/064889 WO2010055027A2 (en) | 2008-11-11 | 2009-11-10 | Organic compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015089480A Division JP2015178503A (ja) | 2008-11-11 | 2015-04-24 | 有機化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012508215A JP2012508215A (ja) | 2012-04-05 |
| JP2012508215A5 true JP2012508215A5 (ja) | 2012-12-20 |
Family
ID=42062355
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535129A Withdrawn JP2012508215A (ja) | 2008-11-11 | 2009-11-10 | 有機化合物 |
| JP2015089480A Withdrawn JP2015178503A (ja) | 2008-11-11 | 2015-04-24 | 有機化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015089480A Withdrawn JP2015178503A (ja) | 2008-11-11 | 2015-04-24 | 有機化合物 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US8680146B2 (ja) |
| EP (1) | EP2358660A2 (ja) |
| JP (2) | JP2012508215A (ja) |
| KR (1) | KR20110086142A (ja) |
| CN (2) | CN102256933A (ja) |
| AU (1) | AU2009315735B2 (ja) |
| BR (1) | BRPI0921533A2 (ja) |
| CA (1) | CA2741974A1 (ja) |
| CL (1) | CL2011001041A1 (ja) |
| CO (1) | CO6382154A2 (ja) |
| EC (1) | ECSP11011121A (ja) |
| IL (1) | IL212073A0 (ja) |
| MA (1) | MA32877B1 (ja) |
| MX (1) | MX2011004924A (ja) |
| NZ (1) | NZ591999A (ja) |
| PE (1) | PE20120012A1 (ja) |
| RU (1) | RU2543621C2 (ja) |
| TN (1) | TN2011000187A1 (ja) |
| WO (1) | WO2010055027A2 (ja) |
| ZA (1) | ZA201102272B (ja) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006249866B2 (en) | 2005-05-26 | 2011-10-13 | Aldeyra Therapeutics, Inc. | Compositions and methods of treating retinal disease |
| EP2358660A2 (en) * | 2008-11-11 | 2011-08-24 | Novartis AG | Salts of fingolimod |
| EP2456752A2 (en) | 2009-07-24 | 2012-05-30 | ratiopharm GmbH | Process for producing fingolimod salts |
| 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 |
| EP2505589A1 (en) | 2011-04-01 | 2012-10-03 | Johann Wolfgang Goethe-Universität Frankfurt am Main | Novel sphingolipid heterocyclic compounds as modulators of sphingolipid signaling and uses thereof |
| AR085749A1 (es) | 2011-04-01 | 2013-10-23 | Novartis Ag | Formulaciones |
| 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 |
| 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 |
| US10675254B2 (en) | 2013-10-11 | 2020-06-09 | Teikoku Seiyaku Co., Ltd. | Sphingosine-1-phosphate receptor agonist iontophoretic devices and methods of using the same |
| JP6401257B2 (ja) | 2013-10-11 | 2018-10-10 | テイコク ファーマ ユーエスエー インコーポレーテッド | 局所用スフィンゴシン−１−リン酸受容体アゴニスト製剤及びその使用方法 |
| US9925138B2 (en) | 2015-01-20 | 2018-03-27 | Handa Pharmaceuticals, Llc | Stable solid fingolimod dosage forms |
| MX2018013472A (es) | 2016-05-09 | 2019-02-28 | Aldeyra Therapeutics Inc | Tratamiento de combinacion de trastornos y enfermedades inflamatorios oculares. |
| SG11201810704WA (en) | 2016-05-31 | 2018-12-28 | Taiho Pharmaceutical Co Ltd | Sulfonamide compound or salt thereof |
| 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 |
| CN111356451A (zh) | 2017-10-10 | 2020-06-30 | 奥尔德拉医疗公司 | 炎性病症的治疗 |
| US20210261528A1 (en) * | 2018-06-29 | 2021-08-26 | Forma Therapeutics, Inc. | Salts of (s)-(5-cyclobutoxy-2-methyl-6-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)-3,4-dihydroquinolin-1(2h)-yl)(cyclopropyl)methanone and solid forms thereof |
| WO2020033344A1 (en) * | 2018-08-06 | 2020-02-13 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| 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 (16)
| 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. |
| ECSP951461A (es) | 1995-06-07 | 1998-04-07 | SINTESIS DE 3- {4-(2- AMINOETOXI) BENZOIL]-2-ARIL-6- HIDROXIBENZO {b] TIOFENOS (CASO X- 9295B) | |
| ECSP972265A (es) | 1997-09-23 | 1998-11-30 | Dihidrato de d-olanzapina | |
| FR2785607B1 (fr) | 1998-11-09 | 2001-02-09 | Rhodia Chimie Sa | Procede de preparation de tris(ether-amine) |
| 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 |
| JP4627356B2 (ja) * | 1999-06-30 | 2011-02-09 | 松森 昭 | ウイルス性心筋炎の予防または治療薬剤 |
| PL364359A1 (en) * | 2001-06-08 | 2004-12-13 | Novartis Ag | Treatment or prophylaxis of insulin-producing cell graft 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 |
| EA012266B1 (ru) * | 2004-12-21 | 2009-08-28 | Лаборатуар Сероно С.А. | Сульфониламиноциклические соединения и их применение |
| GT200600350A (es) | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
| AU2006297130B2 (en) * | 2005-09-30 | 2009-12-24 | Novartis Ag | DPP IV inhibitor for use in the treatment of autoimmune diseases and graft rejection |
| EP2046315B1 (en) * | 2006-06-02 | 2013-04-10 | The Ohio State University Research Foundation | Therapeutic agents for the treatment of mantle cell lymphoma |
| US7985586B2 (en) * | 2008-02-04 | 2011-07-26 | Georgia Health Sciences University | Oligodendrocyte precursor cell composition and methods of use |
| EP2358660A2 (en) * | 2008-11-11 | 2011-08-24 | Novartis AG | Salts of fingolimod |
-
2009
- 2009-11-10 EP EP09752168A patent/EP2358660A2/en not_active Withdrawn
- 2009-11-10 KR KR1020117013304A patent/KR20110086142A/ko not_active Application Discontinuation
- 2009-11-10 US US13/128,832 patent/US8680146B2/en not_active Expired - Fee Related
- 2009-11-10 CN CN2009801448205A patent/CN102256933A/zh active Pending
- 2009-11-10 AU AU2009315735A patent/AU2009315735B2/en not_active Ceased
- 2009-11-10 PE PE2011000987A patent/PE20120012A1/es not_active Application Discontinuation
- 2009-11-10 CA CA2741974A patent/CA2741974A1/en not_active Abandoned
- 2009-11-10 NZ NZ591999A patent/NZ591999A/xx not_active IP Right Cessation
- 2009-11-10 JP JP2011535129A patent/JP2012508215A/ja not_active Withdrawn
- 2009-11-10 CN CN201510547567.5A patent/CN105198760A/zh active Pending
- 2009-11-10 BR BRPI0921533A patent/BRPI0921533A2/pt not_active IP Right Cessation
- 2009-11-10 RU RU2011123365/04A patent/RU2543621C2/ru not_active IP Right Cessation
- 2009-11-10 MX MX2011004924A patent/MX2011004924A/es active IP Right Grant
- 2009-11-10 WO PCT/EP2009/064889 patent/WO2010055027A2/en active Application Filing
-
2011
- 2011-03-28 ZA ZA2011/02272A patent/ZA201102272B/en unknown
- 2011-03-31 IL IL212073A patent/IL212073A0/en unknown
- 2011-04-19 TN TN2011000187A patent/TN2011000187A1/fr unknown
- 2011-05-10 CL CL2011001041A patent/CL2011001041A1/es unknown
- 2011-05-12 CO CO11058592A patent/CO6382154A2/es not_active Application Discontinuation
- 2011-06-03 MA MA33910A patent/MA32877B1/fr unknown
- 2011-06-10 EC EC2011011121A patent/ECSP11011121A/es unknown
-
2014
- 2014-02-13 US US14/179,807 patent/US20140235722A1/en not_active Abandoned
-
2015
- 2015-04-24 JP JP2015089480A patent/JP2015178503A/ja not_active Withdrawn
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