RU2478384C2 - Курс лечения с использованием агониста рецептора s1p - Google Patents
Курс лечения с использованием агониста рецептора s1p Download PDFInfo
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- RU2478384C2 RU2478384C2 RU2007124327/15A RU2007124327A RU2478384C2 RU 2478384 C2 RU2478384 C2 RU 2478384C2 RU 2007124327/15 A RU2007124327/15 A RU 2007124327/15A RU 2007124327 A RU2007124327 A RU 2007124327A RU 2478384 C2 RU2478384 C2 RU 2478384C2
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- Prior art keywords
- alkyl
- dose
- agonist
- fty720
- treatment
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Landscapes
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
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| US63148304P | 2004-11-29 | 2004-11-29 | |
| US60/631,483 | 2004-11-29 | ||
| PCT/US2005/043044 WO2006058316A1 (en) | 2004-11-29 | 2005-11-28 | Dosage regimen of an s1p receptor agonist |
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| RU2012141951/15A Division RU2012141951A (ru) | 2004-11-29 | 2012-10-02 | Курс лечения с использованием агониста рецептора sip |
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| RU2007124327A RU2007124327A (ru) | 2009-01-10 |
| RU2478384C2 true RU2478384C2 (ru) | 2013-04-10 |
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| RU2007124327/15A RU2478384C2 (ru) | 2004-11-29 | 2005-11-28 | Курс лечения с использованием агониста рецептора s1p |
| RU2012141951/15A RU2012141951A (ru) | 2004-11-29 | 2012-10-02 | Курс лечения с использованием агониста рецептора sip |
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| RU2012141951/15A RU2012141951A (ru) | 2004-11-29 | 2012-10-02 | Курс лечения с использованием агониста рецептора sip |
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| EP (3) | EP2359821A1 (enExample) |
| JP (4) | JP2008521827A (enExample) |
| KR (4) | KR20140095109A (enExample) |
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| PT (1) | PT1819326E (enExample) |
| RU (2) | RU2478384C2 (enExample) |
| SG (2) | SG158096A1 (enExample) |
| TN (1) | TNSN07209A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US7241812B2 (en) | 2004-08-13 | 2007-07-10 | Praecis Pharmaceuticals, Inc. | Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity |
| KR20140095109A (ko) * | 2004-11-29 | 2014-07-31 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| ES2357426T3 (es) * | 2005-09-09 | 2011-04-26 | Novartis Ag | Tratamiento de enfermedades autoinmunes. |
| GB0612721D0 (en) * | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
| CN104337808A (zh) | 2007-05-04 | 2015-02-11 | 诺华股份有限公司 | S1p受体调节剂的用途 |
| LT2278960T (lt) * | 2008-03-17 | 2017-02-10 | Actelion Pharmaceuticals Ltd. | S1p1 receptoriaus selektyvaus agonisto dozavimo režimas |
| CA2724592A1 (en) * | 2008-05-20 | 2009-11-26 | Kyorin Pharmaceutical Co., Ltd. | Agent for maintenance of induced remission |
| KR101608108B1 (ko) * | 2008-07-23 | 2016-03-31 | 노파르티스 아게 | 스핑고신 1 포스페이트 수용체 조절제 및 근육 염증을 치료하기 위한 그의 용도 |
| SG193803A1 (en) * | 2008-08-18 | 2013-10-30 | Novartis Ag | Compounds for the treatment of peripheral neuropathies |
| BRPI0922457A2 (pt) * | 2008-12-18 | 2015-12-15 | Novartis Ag | forma polimórfica de ácido 1-(4-{1-[(e)-4-ciclo-hexil-3-trifluormetil-benziloxi-imino]-etil)-2-etil-benzil)-azetidino-3-carboxílico" |
| MX2011006622A (es) * | 2008-12-18 | 2011-07-12 | Novartis Ag | Sales novedosas. |
| HRP20131106T1 (hr) * | 2008-12-18 | 2013-12-20 | Novartis Ag | Hemifumaratna sol od 1-[4-[1-(4-cikloheksil-3-trifluorometil-benziloksiimino)-etil]-2-etil-benzil]-azetidin-3-karboksilne kiseline |
| CN102264359A (zh) * | 2008-12-22 | 2011-11-30 | 诺瓦提斯公司 | S1p受体激动剂的给药方案 |
| CA2747992C (en) * | 2008-12-22 | 2017-11-07 | Novartis Ag | Dosage regimen of an s1p receptor agonist |
| AU2015275246B2 (en) * | 2008-12-22 | 2018-02-01 | Novartis Ag | Dosage regimen for a S1P receptor agonist |
| SG10201913361RA (en) * | 2009-09-29 | 2020-03-30 | Novartis Ag | 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 |
| AU2011249789B2 (en) * | 2010-05-06 | 2015-03-19 | Novartis Ag | Dosage regimen of diaryl sulfide derivatives |
| UA114283C2 (uk) | 2011-01-07 | 2017-05-25 | Новартіс Аг | Композиції імуносупресантів |
| SG10201602279PA (en) * | 2011-10-21 | 2016-04-28 | Novartis Ag | Dosage regimen for an s1p receptor modulator or agonist |
| HUE050733T2 (hu) | 2012-08-17 | 2021-01-28 | Actelion Pharmaceuticals Ltd | Eljárás (2Z,5Z)-5-(3-klór-4-((R)-2,3-dihidroxipropoxi)benzilidén)-2-(pro-pilimino)-3-(O-tolil)tiazolidin-4-on elõállítására és ezen eljárásban alkalmazott köztitermék |
| 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 |
| 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 |
| 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 |
| MA41139A (fr) | 2014-12-11 | 2017-10-17 | Actelion Pharmaceuticals Ltd | Combinaison pharmaceutique comportant un agoniste sélectif du récepteur sip1 |
| HRP20220359T8 (hr) | 2014-12-11 | 2022-05-27 | Actelion Pharmaceuticals Ltd | Režim doziranja ponesimoda, selektivnog agonista receptora s1p1 |
| WO2016135644A1 (en) | 2015-02-26 | 2016-09-01 | 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 |
| AU2020372647A1 (en) | 2019-10-31 | 2022-06-16 | Idorsia Pharmaceuticals Ltd | Combination of a CXCR7 antagonist with an S1P1 receptor modulator |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6004565A (en) * | 1997-09-02 | 1999-12-21 | Yoshitomi Pharmaceutical Industries, Ltd. | Compositions and methods of using compositions with accelerated lymphocyte homing immunosuppressive properties |
| EP1431275A1 (en) * | 2001-09-27 | 2004-06-23 | Kyorin Pharmaceutical Co., Ltd. | Diaryl ether derivative, addition salt thereof, and immunosuppressant |
| EP1431284A1 (en) * | 2001-09-27 | 2004-06-23 | Kyorin Pharmaceutical Co., Ltd. | Diaryl sulfide derivative, addition salt thereof, and immunosuppressant |
| WO2004103306A2 (en) * | 2003-05-19 | 2004-12-02 | Irm Llc | Immunosuppressant compounds and compositions |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0627406T3 (da) | 1992-10-21 | 1999-07-12 | Taito Co | 2-Amino-1,3-propandiolforbindelser og immunundertrykkende midler |
| KR100358922B1 (ko) | 1994-08-22 | 2003-01-24 | 미쯔비시 웰 파마 가부시키가이샤 | 벤젠화합물및그의의약으로서의용도 |
| US6121329A (en) * | 1995-12-28 | 2000-09-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Topical administration of 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| US6277888B1 (en) * | 1997-02-27 | 2001-08-21 | Welfide Corporation | Drug composition |
| CN1290819C (zh) | 1997-04-04 | 2006-12-20 | 三菱制药株式会社 | 2－氨基丙烷－1，3－二醇化合物、其作为医药的用途及其合成中间体 |
| 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 |
| BR0112484A (pt) | 2000-07-13 | 2003-09-23 | Sankyo Co | Composto ou um seu sal, éster ou outro derivado farmacologicamente aceitável, composição farmacêutica, uso de um composto ou de um seu sal, éster ou outro derivado farmacologicamente aceitável, e, processo para a preparação do mesmo |
| AU8533101A (en) | 2000-08-31 | 2002-03-13 | Merck & Co Inc | Phosphate derivatives as immunoregulatory agents |
| JP4012823B2 (ja) | 2001-03-26 | 2007-11-21 | ノバルティス アクチエンゲゼルシャフト | ２−アミノ−誘導体 |
| ES2364816T3 (es) * | 2001-04-02 | 2011-09-14 | Genentech, Inc. | Terapia de combinación. |
| HUP0303454A3 (en) * | 2001-04-02 | 2005-12-28 | Astrazeneca Ab | Solid pharmaceutical composition comprising 4-cyano-trifluoro-3(4-fluorophenyl-sulphonyl)-2-hydroxy-2-methylpropiono-m toluidide and pvp |
| JP2002316985A (ja) | 2001-04-20 | 2002-10-31 | Sankyo Co Ltd | ベンゾチオフェン誘導体 |
| NZ529044A (en) * | 2001-06-08 | 2008-03-28 | Novartis Ag | Treatment or prophylaxis of insulin-producing cell graft rejection |
| AU2003207567B2 (en) | 2002-01-18 | 2008-01-24 | Merck Sharp & Dohme Corp. | Edg receptor agonists |
| WO2003061567A2 (en) | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| US7351725B2 (en) | 2002-01-18 | 2008-04-01 | Merck & Co., Inc. | N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as Edg receptor agonists |
| KR20080103117A (ko) * | 2002-09-24 | 2008-11-26 | 노파르티스 아게 | 탈수초성 장애의 치료에 있어서의 스핑고신-1-포스페이트 수용체 아고니스트 |
| ES2467160T3 (es) | 2003-05-19 | 2014-06-12 | Irm Llc | Compuestos y composiciones inmunosupresores |
| 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 |
| JPWO2006041015A1 (ja) * | 2004-10-12 | 2008-05-15 | 杏林製薬株式会社 | アミノアルコール誘導体とその付加塩及び免疫抑制剤 |
| KR20140095109A (ko) * | 2004-11-29 | 2014-07-31 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| GT200600350A (es) * | 2005-08-09 | 2007-03-28 | Formulaciones líquidas |
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- 2005-11-28 EP EP10179081A patent/EP2359821A1/en not_active Withdrawn
- 2005-11-28 SG SG200907947-6A patent/SG158096A1/en unknown
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- 2005-11-28 WO PCT/US2005/043044 patent/WO2006058316A1/en not_active Ceased
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- 2005-11-28 SG SG2013002662A patent/SG187468A1/en unknown
- 2005-11-28 KR KR20157005416A patent/KR20150028858A/ko not_active Ceased
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6004565A (en) * | 1997-09-02 | 1999-12-21 | Yoshitomi Pharmaceutical Industries, Ltd. | Compositions and methods of using compositions with accelerated lymphocyte homing immunosuppressive properties |
| EP1431275A1 (en) * | 2001-09-27 | 2004-06-23 | Kyorin Pharmaceutical Co., Ltd. | Diaryl ether derivative, addition salt thereof, and immunosuppressant |
| EP1431284A1 (en) * | 2001-09-27 | 2004-06-23 | Kyorin Pharmaceutical Co., Ltd. | Diaryl sulfide derivative, addition salt thereof, and immunosuppressant |
| WO2004103306A2 (en) * | 2003-05-19 | 2004-12-02 | Irm Llc | Immunosuppressant compounds and compositions |
Non-Patent Citations (2)
| Title |
|---|
| SKERJANEC A. et al: «Systemic exposure and preliminary efficacy of FTY720 in de novo renal transplant recipients» / Am J Transplant, 2002, vol.2, suppl.3, Abst.964. Введение в исследование потребления лекарственных средств. - Еженедельник «АПТЕКА», 31.05.2004, 442 (21), [Найдено из Интернет 30.10.2009] <URL: http://www.apteka.ua/article/15352>. ОКОРОКОВ А.Н. Лечение аутоиммунного тиреоидита. Лечение болезней внутренних органов. - Витебск, 1998 [Найдено из Интернет 06.05.2011] URL: http//www.rustamsamedov.narod.ru/physlib/thyreoiditauto.html. ВЫШКОВСКИЙ Г.Л. Регистр лекарственных средств России РЛС-Аптекарь. Ежегодный сборник, выпуск 5, 2003, подписано в печать 24.06.2002, стр.1016. МИХАЙЛОВ И.Б. Основы рациональной фармакотерапии. Учебное пособие по клинической фармакологии для студентов педиатрических и лечебных факультетов медицинских высших учебных заведений. - СПб., 1999, стр.32. * |
| ГАЛЕНКО-ЯРОШЕВСКИЙ П.А. Руководство по фармакологии к практическим занятиям. - М., 2000, с.599-600. * |
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