JP2012512885A5 - - Google Patents
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- Publication number
- JP2012512885A5 JP2012512885A5 JP2011542413A JP2011542413A JP2012512885A5 JP 2012512885 A5 JP2012512885 A5 JP 2012512885A5 JP 2011542413 A JP2011542413 A JP 2011542413A JP 2011542413 A JP2011542413 A JP 2011542413A JP 2012512885 A5 JP2012512885 A5 JP 2012512885A5
- Authority
- JP
- Japan
- Prior art keywords
- ethyl
- benzyloxyimino
- azetidine
- cyclohexyl
- benzyl
- 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
Links
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 239000013078 crystal Substances 0.000 claims 8
- -1 4- {1-[(E) -4-cyclohexyl-3-trifluoromethyl-benzyloxyimino] -ethyl} -2-ethyl-benzyl Chemical group 0.000 claims 6
- KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 claims 5
- 150000003892 tartrate salts Chemical class 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 229940049920 malate Drugs 0.000 claims 2
- 150000003891 oxalate salts Chemical class 0.000 claims 2
- WWXCDQQTHJKXBQ-GKMOJYNQSA-N Cl.CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 Chemical compound Cl.CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 WWXCDQQTHJKXBQ-GKMOJYNQSA-N 0.000 claims 1
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- 150000004701 malic acid derivatives Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20305108P | 2008-12-18 | 2008-12-18 | |
| US61/203,051 | 2008-12-18 | ||
| PCT/US2009/068352 WO2010080455A1 (en) | 2008-12-18 | 2009-12-17 | New salts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012512885A JP2012512885A (ja) | 2012-06-07 |
| JP2012512885A5 true JP2012512885A5 (enExample) | 2012-11-22 |
Family
ID=42316715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011542413A Pending JP2012512885A (ja) | 2008-12-18 | 2009-12-17 | 新規な塩 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US8486930B2 (enExample) |
| EP (1) | EP2379499B1 (enExample) |
| JP (1) | JP2012512885A (enExample) |
| KR (1) | KR20110101159A (enExample) |
| CN (2) | CN102256941A (enExample) |
| AU (1) | AU2009335887A1 (enExample) |
| BR (1) | BRPI0922466A2 (enExample) |
| CA (1) | CA2747558A1 (enExample) |
| ES (1) | ES2478842T3 (enExample) |
| MX (1) | MX2011006622A (enExample) |
| RU (1) | RU2011129229A (enExample) |
| WO (1) | WO2010080455A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013535480A (ja) * | 2010-08-05 | 2013-09-12 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ２−［２−［［（４−メトキシ−２，６−ジメチルフェニル）スルホニル］−（メチル）アミノ］エトキシ］−ｎ−メチル−ｎ−［３−（４−メチルピペラジン−１−イル）シクロヘキシル］アセトアミドの酸付加塩及びそのブラジキニンｂ１受容体アンタゴニストとしての使用 |
| HRP20191842T1 (hr) | 2011-01-07 | 2019-12-27 | Novartis Ag | Formulacije imunosupresiva |
| WO2012095853A1 (en) | 2011-01-10 | 2012-07-19 | Novartis Pharma Ag | Modified release formulations comprising sip receptor modulators |
| CA2973540A1 (en) | 2015-02-26 | 2016-09-01 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| US20190047951A1 (en) | 2016-01-04 | 2019-02-14 | Auspex Pharmaceuticals, Inc. | Azetidine modulators of the sphingosine 1-phosphate receptor |
| US11958805B2 (en) * | 2017-03-09 | 2024-04-16 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| US11434200B2 (en) | 2017-03-09 | 2022-09-06 | Novartis Ag | Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| CN111405897A (zh) | 2017-09-27 | 2020-07-10 | 雷迪博士实验室有限公司 | 辛波莫德、其盐及其固态形式的制备方法 |
| EP3687530A1 (en) | 2017-09-29 | 2020-08-05 | Novartis AG | Dosing regimen of siponimod |
| WO2019064217A1 (en) | 2017-09-29 | 2019-04-04 | Novartis Ag | DOSAGE DIAGRAM OF SIPONIMOD |
| EP3743405B1 (en) | 2018-01-22 | 2023-11-15 | Teva Pharmaceuticals International GmbH | Crystalline siponimod fumaric acid and polymorphs thereof |
| CN110776450B (zh) * | 2018-07-27 | 2022-09-27 | 广东东阳光药业有限公司 | 一种辛波莫德晶型及其制备方法 |
| CN113631554B (zh) | 2019-03-28 | 2024-06-21 | 第一生物治疗股份有限公司 | 苯并噻唑化合物的药用盐、多晶型物及其制备方法 |
| EP3972954A1 (en) | 2019-05-21 | 2022-03-30 | Synthon B.V. | Siponimod maleic acid and fumaric acid salt |
| MX2022005014A (es) | 2019-10-31 | 2022-05-16 | Idorsia Pharmaceuticals Ltd | Combinacion de un antagonista de cxcr7 con un modulador del receptor s1p1. |
| US11135197B2 (en) | 2020-02-07 | 2021-10-05 | Argentum Pharmaceuticals Llc | Dosage regimen of an S1P receptor modulator |
| WO2022064007A1 (en) | 2020-09-25 | 2022-03-31 | Synthon B.V. | Siponimod salts and cocrystals |
| CN112402610A (zh) * | 2020-11-20 | 2021-02-26 | 睿阜隆(杭州)生物医药有限公司 | 1-磷酸鞘氨醇受体调节剂在制备治疗糖尿病的药物中的新用途 |
| 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 (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL86632A0 (en) | 1987-06-15 | 1988-11-30 | Ciba Geigy Ag | Derivatives substituted at methyl-amino nitrogen |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| TW225528B (enExample) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| AU687727B2 (en) | 1992-10-28 | 1998-03-05 | Genentech Inc. | Vascular endothelial cell growth factor antagonists |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| EP0817775B1 (en) | 1995-03-30 | 2001-09-12 | Pfizer Inc. | Quinazoline derivatives |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| ATE212993T1 (de) | 1995-07-06 | 2002-02-15 | Novartis Erfind Verwalt Gmbh | Pyrolopyrimidine und verfahren zu ihrer herstellung |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| EP0892789B2 (en) | 1996-04-12 | 2009-11-18 | Warner-Lambert Company LLC | Irreversible inhibitors of tyrosine kinases |
| DE69734513T2 (de) | 1996-06-24 | 2006-07-27 | Pfizer Inc. | Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten |
| WO1998002441A2 (en) | 1996-07-12 | 1998-01-22 | Ariad Pharmaceuticals, Inc. | Non immunosuppressive antifungal rapalogs |
| DE19638745C2 (de) | 1996-09-11 | 2001-05-10 | Schering Ag | Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR) |
| AU4342997A (en) | 1996-09-13 | 1998-04-02 | Sugen, Inc. | Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| TW557297B (en) | 1997-09-26 | 2003-10-11 | Abbott Lab | Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same |
| GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
| CN1152031C (zh) | 1998-08-11 | 2004-06-02 | 诺瓦提斯公司 | 具有血管生成抑制活性的异喹啉衍生物 |
| UA71587C2 (uk) | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
| GB9824579D0 (en) | 1998-11-10 | 1999-01-06 | Novartis Ag | Organic compounds |
| ATE300957T1 (de) | 1998-12-22 | 2005-08-15 | Genentech Inc | Antagonisten von vaskular-endothelialen zellwachstumsfaktoren und ihre anwendung |
| PT1165085E (pt) | 1999-03-30 | 2006-10-31 | Novartis Ag | Derivados de ftalazina para tratar doencas inflamatorias |
| EP1212331B1 (en) | 1999-08-24 | 2004-04-21 | Ariad Gene Therapeutics, Inc. | 28-epirapalogs |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| CN1791395B (zh) * | 2003-05-19 | 2012-09-26 | Irm责任有限公司 | 免疫抑制剂化合物及组合物 |
| CN102600472A (zh) * | 2004-11-29 | 2012-07-25 | 诺瓦提斯公司 | S1p受体激动剂的剂量方案 |
| GT200600350A (es) * | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
| GB0612721D0 (en) | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
-
2009
- 2009-12-17 CA CA2747558A patent/CA2747558A1/en not_active Abandoned
- 2009-12-17 ES ES09793424.4T patent/ES2478842T3/es active Active
- 2009-12-17 CN CN2009801504811A patent/CN102256941A/zh active Pending
- 2009-12-17 KR KR1020117013936A patent/KR20110101159A/ko not_active Withdrawn
- 2009-12-17 MX MX2011006622A patent/MX2011006622A/es not_active Application Discontinuation
- 2009-12-17 WO PCT/US2009/068352 patent/WO2010080455A1/en not_active Ceased
- 2009-12-17 CN CN2013101141799A patent/CN103204794A/zh active Pending
- 2009-12-17 US US13/140,490 patent/US8486930B2/en active Active
- 2009-12-17 BR BRPI0922466A patent/BRPI0922466A2/pt not_active IP Right Cessation
- 2009-12-17 AU AU2009335887A patent/AU2009335887A1/en not_active Abandoned
- 2009-12-17 EP EP09793424.4A patent/EP2379499B1/en active Active
- 2009-12-17 JP JP2011542413A patent/JP2012512885A/ja active Pending
- 2009-12-17 RU RU2011129229/04A patent/RU2011129229A/ru not_active Application Discontinuation
-
2013
- 2013-04-03 US US13/856,371 patent/US8697682B2/en active Active
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