CN102600472A - S1p受体激动剂的剂量方案 - Google Patents
S1p受体激动剂的剂量方案 Download PDFInfo
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- CN102600472A CN102600472A CN2012100846463A CN201210084646A CN102600472A CN 102600472 A CN102600472 A CN 102600472A CN 2012100846463 A CN2012100846463 A CN 2012100846463A CN 201210084646 A CN201210084646 A CN 201210084646A CN 102600472 A CN102600472 A CN 102600472A
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- agonist
- daily dose
- receptor modulators
- alkyl
- receptor
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Classifications
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- A—HUMAN NECESSITIES
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| JP2008509931A (ja) | 2004-08-13 | 2008-04-03 | プレーシス ファーマスーティカルズ インコーポレイテッド | スフィンゴシン−１−ホスフェート（ｓ１ｐ）レセプター活性を調節するための方法および組成物 |
| KR20130041385A (ko) * | 2004-11-29 | 2013-04-24 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| CA2620554C (en) * | 2005-09-09 | 2013-12-17 | Novartis Ag | Treatment of autoimmune diseases |
| GB0612721D0 (en) * | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
| KR101526835B1 (ko) | 2007-05-04 | 2015-06-05 | 노파르티스 아게 | Ｓ1ｐ 수용체 조절제의 용도 |
| KR101718639B1 (ko) | 2008-03-17 | 2017-03-21 | 액테리온 파마슈티칼 리미티드 | 선별적 ｓ1ｐ₁ 수용체 작동약에 대한 투약 섭생 |
| RU2505288C2 (ru) * | 2008-05-20 | 2014-01-27 | Киорин Фармасьютикал Ко., Лтд. | Средства поддержания индуцированной ремиссии |
| US9149459B2 (en) * | 2008-07-23 | 2015-10-06 | Novartis Ag | Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation |
| RU2523281C2 (ru) * | 2008-08-18 | 2014-07-20 | Новартис Аг | Соединения для лечения периферических невропатий |
| CN103204794A (zh) * | 2008-12-18 | 2013-07-17 | 诺瓦提斯公司 | 新的盐 |
| RU2011129230A (ru) * | 2008-12-18 | 2013-01-27 | Новартис Аг | Новая полиморфная форма 1-[4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил]азетидин-3-карбоновой кислоты |
| KR20170062554A (ko) * | 2008-12-18 | 2017-06-07 | 노파르티스 아게 | 1-［4-［1-(4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸］-2-에틸-벤질］-아제티딘-3-카르복실산의 헤미푸마레이트 염 |
| JP5657565B2 (ja) * | 2008-12-22 | 2015-01-21 | ノバルティス アーゲー | Ｓ１ｐ受容体アゴニストの投与レジメン |
| HRP20151190T1 (hr) * | 2008-12-22 | 2016-01-01 | Novartis Ag | Režim doziranja za fingolimod u lijeäśenju multiple skleroze |
| AU2015275246B2 (en) * | 2008-12-22 | 2018-02-01 | Novartis Ag | Dosage regimen for a S1P receptor agonist |
| US20120264719A1 (en) * | 2009-09-29 | 2012-10-18 | Craig Boulton | Dosage regimen of an s1p receptor modulator |
| US20110124605A1 (en) * | 2009-11-20 | 2011-05-26 | Shreeram Aradhye | Use of an S1P Receptor Agonist |
| US8791100B2 (en) | 2010-02-02 | 2014-07-29 | Novartis Ag | Aryl benzylamine compounds |
| EP2566473B1 (en) * | 2010-05-06 | 2016-01-06 | Novartis AG | Dosage regimen of diaryl sulfide derivatives |
| BR112013017302B1 (pt) | 2011-01-07 | 2021-12-07 | Novartis Ag | Composição farmacêutica em fase sólida |
| MX2014004813A (es) * | 2011-10-21 | 2014-05-20 | Novartis Ag | Regimen de dosificacion para un modulador o agonista del receptor s1p. |
| SI2885266T1 (sl) | 2012-08-17 | 2020-10-30 | Actelion Pharmaceuticals Ltd | Postopek za pripravo (2Z,5Z)-5-(3-kloro-4-((R)-2,3-dihidroksipropoksi) benziliden)-2-(propilimino)-3-(O-tolil)tiazolidin-4-on in v omenjenem postopku uporabljena vmesna spojina |
| 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 |
| WO2015053878A1 (en) | 2013-10-11 | 2015-04-16 | Teikoku Pharma Usa, Inc. | Topical sphingosine-1-phosphate receptor agonist formulations and methods of using the same |
| 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 |
| WO2016091996A1 (en) | 2014-12-11 | 2016-06-16 | Actelion Pharmaceuticals Ltd | Dosing regimen for a selective s1p1 receptor agonist |
| MA41139A (fr) | 2014-12-11 | 2017-10-17 | Actelion Pharmaceuticals Ltd | Combinaison pharmaceutique comportant un agoniste sélectif du récepteur sip1 |
| US20180042895A1 (en) | 2015-02-26 | 2018-02-15 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| US10250466B2 (en) * | 2016-03-29 | 2019-04-02 | Juniper Networks, Inc. | Application signature generation and distribution |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| PH12022551043A1 (en) | 2019-10-31 | 2023-05-03 | Idorsia Pharmaceuticals Ltd | Combination of a cxcr7 antagonist with an s1p1 receptor modulator |
Citations (4)
| 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 |
| WO2003062252A1 (en) * | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Edg receptor agonists |
| WO2003061567A2 (en) * | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| CN1524002A (zh) * | 2001-06-08 | 2004-08-25 | ��˹��ŵ�� | 治疗或预防产胰岛素细胞的移植排斥反应 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996006068A1 (en) | 1994-08-22 | 1996-02-29 | Yoshitomi Pharmaceutical Industries, Ltd. | Benzene compound and medicinal use thereof |
| CA2213989C (en) * | 1995-12-28 | 2007-05-29 | Yoshitomi Pharmaceutical Industries Ltd. | External preparation for topical administration |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| KR20000075745A (ko) * | 1997-02-27 | 2000-12-26 | 가마후라 아키오 | 의약 조성물 |
| IL155065A (en) | 1997-04-04 | 2004-01-04 | Mitsubishi Pharma Corp | History - 2 Aminopropene - 1, 3 - Diol and Pharmaceutical Preparations Containing Them |
| JPH1180026A (ja) * | 1997-09-02 | 1999-03-23 | Yoshitomi Pharmaceut Ind Ltd | 新規免疫抑制剤、その使用方法およびその同定方法 |
| JPH11116479A (ja) * | 1997-10-10 | 1999-04-27 | Sugen Inc | 脳癌のための組み合わせ化学療法処置 |
| CN1267429C (zh) | 2000-07-13 | 2006-08-02 | 三共株式会社 | 氨基醇衍生物 |
| CA2421893A1 (en) | 2000-08-31 | 2002-03-07 | Merck And Co., Inc. | Phosphate derivatives as immunoregulatory agents |
| EP1377593B1 (en) | 2001-03-26 | 2005-12-28 | Novartis AG | 2-amino-propanol derivatives |
| WO2002080902A1 (en) * | 2001-04-02 | 2002-10-17 | Astrazeneca Ab | Solid pharmaceutical composition comprising 4 -cyano-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono- m toluidide and pvp |
| ES2364816T3 (es) * | 2001-04-02 | 2011-09-14 | Genentech, Inc. | Terapia de combinación. |
| JP2002316985A (ja) | 2001-04-20 | 2002-10-31 | Sankyo Co Ltd | ベンゾチオフェン誘導体 |
| US6963012B2 (en) | 2001-09-27 | 2005-11-08 | Kyorin Pharmaceutical Co., Ltd. | Diaryl ether derivative, addition salt thereof, and immunosuppressant |
| CA2461212C (en) * | 2001-09-27 | 2010-08-17 | Kyorin Pharmaceutical Co., Ltd. | Diaryl sulfide derivatives, salts thereof and immunosuppressive agents using the same |
| DE60330047D1 (en) | 2002-01-18 | 2009-12-24 | Merck & Co Inc | "n-(benzyl)aminoalkyl carboxylate, phosphinate, phosphonate und tetrazole als edg rezeptoragonisten" |
| TWI335311B (en) * | 2002-09-24 | 2011-01-01 | Novartis Ag | Organic compounds |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| PE20050158A1 (es) | 2003-05-19 | 2005-05-12 | Irm Llc | Compuestos inmunosupresores y composiciones |
| UA74941C2 (en) | 2004-04-26 | 2006-02-15 | Fos Internat S A | A metal-thermal process for producing magnesium and vacuum induction furnace for realizing the same |
| WO2005113330A1 (en) | 2004-05-05 | 2005-12-01 | Adler, Richard, S. | Systems and methods for protecting ship from attack on the surface or under water |
| WO2006041015A1 (ja) * | 2004-10-12 | 2006-04-20 | Kyorin Pharmaceutical Co., Ltd. | アミノアルコール誘導体とその付加塩及び免疫抑制剤 |
| KR20130041385A (ko) * | 2004-11-29 | 2013-04-24 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| GT200600350A (es) * | 2005-08-09 | 2007-03-28 | Formulaciones líquidas |
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Patent Citations (4)
| 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 |
| CN1524002A (zh) * | 2001-06-08 | 2004-08-25 | ��˹��ŵ�� | 治疗或预防产胰岛素细胞的移植排斥反应 |
| WO2003062252A1 (en) * | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Edg receptor agonists |
| WO2003061567A2 (en) * | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
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