JP2010530897A5 - - Google Patents
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- Publication number
- JP2010530897A5 JP2010530897A5 JP2010513457A JP2010513457A JP2010530897A5 JP 2010530897 A5 JP2010530897 A5 JP 2010530897A5 JP 2010513457 A JP2010513457 A JP 2010513457A JP 2010513457 A JP2010513457 A JP 2010513457A JP 2010530897 A5 JP2010530897 A5 JP 2010530897A5
- Authority
- JP
- Japan
- Prior art keywords
- deuterium
- compound
- positions represented
- compound according
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 9
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrugs Drugs 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000007614 solvation Methods 0.000 claims 1
- 0 *C(C=C1)=CN(c2ccccc2)C1=O Chemical compound *C(C=C1)=CN(c2ccccc2)C1=O 0.000 description 1
Claims (7)
- 構造式Ｉを有する化合物、またはその医薬上許容し得る塩、溶媒和物もしくはプロドラッグ；
（Ｉ）
式中：
Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ５、Ｒ６、Ｒ７、Ｒ８、Ｒ９、Ｒ１０、およびＲ１１は、水素および重水素からなる群から独立して選択され、
Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ５、Ｒ６、Ｒ７、Ｒ８、Ｒ９、Ｒ１０、およびＲ１１のうちの少なくとも１つは、重水素であり、
Ｒ７、Ｒ８、Ｒ９、Ｒ１０、およびＲ１１が重水素である場合、Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ５、およびＲ６のうちの少なくとも一つは重水素である。 - 前記化合物は、
またはその医薬上許容し得る塩、溶媒和物、もしくはプロドラッグからなる群から選択される、請求項１に記載の化合物。 - Ｄとして表される前記位置のそれぞれは、少なくとも９８％の重水素濃縮を有する、請求項２に記載の化合物。
- Ｄとして表される前記位置のそれぞれは、少なくとも９０％の重水素濃縮を有する、請求項２に記載の化合物。
- Ｄとして表される前記位置のそれぞれは、少なくとも５０％の重水素濃縮を有する、請求項２に記載の化合物。
- Ｄとして表される前記位置のそれぞれは、少なくとも１％の重水素濃縮を有する、請求項２に記載の化合物。
- 前記化合物は、
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94513607P | 2007-06-20 | 2007-06-20 | |
| US60/945,136 | 2007-06-20 | ||
| PCT/US2008/067732 WO2008157786A1 (en) | 2007-06-20 | 2008-06-20 | Substituted n-aryl pyridinones as fibrotic inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010530897A JP2010530897A (ja) | 2010-09-16 |
| JP2010530897A5 true JP2010530897A5 (ja) | 2011-08-04 |
| JP5587184B2 JP5587184B2 (ja) | 2014-09-10 |
Family
ID=39731521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010513457A Active JP5587184B2 (ja) | 2007-06-20 | 2008-06-20 | 繊維症阻害剤としての置換ｎ−アリールピリジノン |
Country Status (13)
| Country | Link |
|---|---|
| US (6) | US8383823B2 (ja) |
| EP (1) | EP2170828B1 (ja) |
| JP (1) | JP5587184B2 (ja) |
| KR (2) | KR101767849B1 (ja) |
| CN (2) | CN101842355A (ja) |
| AU (1) | AU2008265595B2 (ja) |
| CA (1) | CA2691379C (ja) |
| DK (1) | DK2170828T3 (ja) |
| ES (1) | ES2400026T3 (ja) |
| HK (1) | HK1214251A1 (ja) |
| IL (1) | IL202840A (ja) |
| NZ (1) | NZ599643A (ja) |
| WO (1) | WO2008157786A1 (ja) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080051332A1 (en) * | 2005-11-18 | 2008-02-28 | Nastech Pharmaceutical Company Inc. | Method of modulating hematopoietic stem cells and treating hematologic diseases using intranasal parathyroid hormone |
| KR101767849B1 (ko) | 2007-06-20 | 2017-08-11 | 오스펙스 파마슈티칼스, 인코포레이티드 | 섬유증 저해제로서의 치환된 ｎ-아릴 피리디논 |
| MX2007009796A (es) | 2007-08-14 | 2009-02-25 | Cell Therapy And Technology S | Gel conteniendo pirfenidona. |
| WO2009035598A1 (en) * | 2007-09-10 | 2009-03-19 | Concert Pharmaceuticals, Inc. | Deuterated pirfenidone |
| JP5627574B2 (ja) | 2008-06-03 | 2014-11-19 | インターミューン， インコーポレイテッド | 炎症性および線維性疾患を治療するための化合物および方法 |
| WO2010065755A1 (en) * | 2008-12-04 | 2010-06-10 | Concert Pharmaceuticals, Inc. | Deuterated pyridinones |
| WO2010132864A1 (en) * | 2009-05-15 | 2010-11-18 | Intermune, Inc. | Methods of treating hiv patients with anti-fibrotics |
| TWI434833B (zh) | 2009-06-03 | 2014-04-21 | Intermune Inc | 用於合成吡非尼酮（ｐｉｒｆｅｎｉｄｏｎｅ）的改良方法 |
| US20110053968A1 (en) * | 2009-06-09 | 2011-03-03 | Auspex Pharmaceuticals, Inc. | Aminopyrimidine inhibitors of tyrosine kinase |
| CN101921225B (zh) * | 2009-06-11 | 2013-04-03 | 北京凯得尔森生物技术有限公司 | 吡啡尼酮类化合物、其制备方法和应用 |
| CN102639700A (zh) | 2009-09-30 | 2012-08-15 | 哈佛大学校长及研究员协会 | 通过调节自噬增强基因产物调节自噬的方法 |
| US10105356B2 (en) | 2011-01-31 | 2018-10-23 | Avalyn Pharma Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
| ES2913095T3 (es) | 2011-01-31 | 2022-05-31 | Avalyn Pharma Inc | Compuestos de pirfenidona y análogos de piridona en aerosol y usos de los mismos |
| CA2828895A1 (en) * | 2011-03-08 | 2012-09-13 | Auspex Pharamaceuticals, Inc. | Substituted n-aryl pyridinones |
| AU2012258575B2 (en) * | 2011-05-25 | 2017-03-02 | Intermune, Inc. | Pirfenidone and anti-fibrotic therapy in selected patients |
| MX2011007675A (es) * | 2011-07-19 | 2012-07-11 | Cell Therapy And Technology S A De C V | Procedimiento para la fabricacion de una composicion farmaceutica en forma de tabletas de liberacion prolongada conteniendo pirfenidona y su aplicacion en la regresion de la insuficiencia renal cronica, contractura capsular mamaria y fibrosis hepatica humanas. |
| CN113956315B (zh) | 2011-09-08 | 2024-08-09 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物、及其用途 |
| US20130150426A1 (en) | 2011-11-22 | 2013-06-13 | Intermune, Inc. | Methods of diagnosing and treating idiopathic pulmonary fibrosis |
| MX346763B (es) | 2012-03-28 | 2017-03-31 | Cell Therapy And Tech S A De C V | Composición tópica semisólida conteniendo pirfenidona y dialil óxido de disulfuro modificado (odd-m) para eliminar o prevenir el acné. |
| US9402821B2 (en) * | 2012-08-13 | 2016-08-02 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for treatment of cystic fibrosis |
| MX356551B (es) | 2012-08-23 | 2018-06-04 | Grupo Medifarma S A De C V Star | Composición antiséptica, antiseborreica y exfoliante para eliminar o prevenir el acné. |
| CA2819967C (en) * | 2012-08-31 | 2016-03-22 | Intermune, Inc. | Use of pirfenidone concomitantly with ciprofloxacin |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| EP3932932A1 (en) | 2013-03-13 | 2022-01-05 | Sage Therapeutics, Inc. | Neuroactive steriods and methods of use thereof |
| MX2015012437A (es) * | 2013-03-13 | 2016-04-15 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones, y usos de los mismos. |
| US9770443B2 (en) | 2014-01-10 | 2017-09-26 | Genoa Pharmaceuticals, Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
| EA201691493A1 (ru) * | 2014-01-24 | 2017-02-28 | Оспекс Фармасьютикалз, Инк. | Замещенные n-арилпиридиноны |
| EP3102190A4 (en) | 2014-02-07 | 2017-09-06 | Auspex Pharmaceuticals, Inc. | Novel pharmaceutical formulations |
| KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
| US20150284327A1 (en) * | 2014-04-04 | 2015-10-08 | Auspex Pharmaceuticals, Inc. | Oxindole inhibitors of tyrosine kinase |
| WO2015171345A1 (en) * | 2014-04-30 | 2015-11-12 | Auspex Pharmaceuticals, Inc. | N-aryl pyridinones modulators of fibrosis and/or collagen infiltration |
| US10259840B2 (en) | 2014-06-18 | 2019-04-16 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US10696712B2 (en) | 2015-07-06 | 2020-06-30 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| CA2991313C (en) | 2015-07-06 | 2023-12-19 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MX2020011449A (es) | 2015-07-06 | 2022-02-28 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| CN105315198A (zh) * | 2015-11-02 | 2016-02-10 | 重庆康乐制药有限公司 | 一种吡非尼酮的晶型及其制备方法 |
| SI3256138T1 (sl) * | 2015-11-25 | 2022-07-29 | Axsome Therapeutics, Inc. | Farmacevtski sestavki, ki obsegajo meloksikam |
| CN105330598B (zh) * | 2015-12-02 | 2017-11-14 | 新发药业有限公司 | 一种吡非尼酮的制备方法 |
| US20190070145A1 (en) * | 2016-03-22 | 2019-03-07 | Mayo Foundation For Medical Education And Research | Using fatty acid synthase inhibitors to treat fibrosis |
| CA2937365C (en) | 2016-03-29 | 2018-09-18 | F. Hoffmann-La Roche Ag | Granulate formulation of 5-methyl-1-phenyl-2-(1h)-pyridone and method of making the same |
| AU2017240157B2 (en) | 2016-04-01 | 2022-10-20 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| KR102442586B1 (ko) | 2016-04-08 | 2022-09-08 | 큐어테크 바이오 에이비 | 고리-융합된 티아졸리노 2-피리돈, 이의 제조 방법 및 결핵의 치료 및/또는 예방에 있어서의 그 용도 |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MD3481846T2 (ro) | 2016-07-07 | 2021-11-30 | Sage Therapeutics Inc | 24-Hidroxisteroli 11-substituiți pentru utilizare în tratamentul stărilor legate de NMDA |
| CA3038900A1 (en) | 2016-09-30 | 2018-04-05 | Sage Therapeutics, Inc. | C7 substituted oxysterols and methods as nmda modulators |
| NZ752732A (en) | 2016-10-18 | 2024-08-30 | Sage Therapeutics Inc | Oxysterols and methods of use thereof |
| AU2017345399B2 (en) | 2016-10-18 | 2022-02-24 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| CN106748984A (zh) * | 2016-11-22 | 2017-05-31 | 斯芬克司药物研发（天津）股份有限公司 | 6‑羟甲基‑1‑苯基吡啶‑2‑酮及其制备方法与应用 |
| EP3661506A4 (en) * | 2017-07-31 | 2021-04-21 | Washington University | PIRFENIDONE DERIVATIVES FOR MODULATION OF B LYMPHOCYTE ACTIVITY AND ORGAN PROTECTION |
| MX366086B (es) | 2017-08-15 | 2019-06-27 | Cell Therapy And Tech S A De C V | Composicion topica semisolida conteniendo un agente antimicrobiano y pirfenidona para el tratamiento de daños cronicos de la piel. |
| CN108285431B (zh) * | 2018-03-23 | 2021-04-09 | 北京康蒂尼药业股份有限公司 | 一种吡非尼酮有关物质及其制备方法和用途 |
| IL312572A (en) * | 2018-09-14 | 2024-07-01 | Puretech Lyt 100 Inc | Deuterium enriched pirfenidone and methods of using it |
| EP4121049A4 (en) * | 2020-03-18 | 2024-04-03 | Puretech Lyt 100, Inc. | METHODS OF TREATING LYMPHOEDEMA WITH DEUPIRFENIDONE |
| WO2022010925A1 (en) * | 2020-07-06 | 2022-01-13 | Puretech Lyt 100, Inc. | Methods of treating diseases and disorders with deupirfenidone |
| CN114957106B (zh) * | 2022-05-23 | 2024-01-30 | 湖北工程学院 | 药物吡非尼酮的流动相自动合成方法 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02215719A (ja) | 1989-02-15 | 1990-08-28 | Yamauchi Akitomo | 線維化病変組織の修復並びに線維化病変の阻止剤 |
| US5310562A (en) * | 1989-11-22 | 1994-05-10 | Margolin Solomon B | Composition and method for reparation and prevention of fibrotic lesions |
| KR20040068613A (ko) | 1994-03-25 | 2004-07-31 | 이소테크니카 인코포레이티드 | 중수소화된 화합물 이를 포함하는 고혈압 치료용 조성물 |
| US6221335B1 (en) * | 1994-03-25 | 2001-04-24 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
| US5962478A (en) * | 1995-09-19 | 1999-10-05 | Margolin; Solomon B. | Inhibition of tumor necrosis factor α |
| US6294350B1 (en) * | 1997-06-05 | 2001-09-25 | Dalhousie University | Methods for treating fibroproliferative diseases |
| US6440710B1 (en) * | 1998-12-10 | 2002-08-27 | The Scripps Research Institute | Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds |
| ES2193921T3 (es) * | 1999-12-03 | 2003-11-16 | Pfizer Prod Inc | Compuestos de sulfamoilheteroaril-pirazol como agentes antinflamatorios/analgesicos. |
| EP1134290A3 (en) * | 2000-03-14 | 2004-01-02 | Pfizer Products Inc. | Pharmacophore models for the identification of the CYP2D6 inhibitory potency of selective serotonin reuptake inhibitors |
| AU2001258825A1 (en) * | 2000-05-29 | 2001-12-11 | Shionogi And Co., Ltd. | Method for labeling with tritium |
| JP2005528082A (ja) * | 2001-12-18 | 2005-09-22 | モンドバイオテック・ラボラトリーズ・アンスタルト | 間質性肺疾患の治療を向上させるためのインターフェロンγ又はパーフェニドンと分子診断薬との新規医薬組成物 |
| OA12771A (en) | 2002-02-14 | 2006-07-04 | Pharmacia Corp | Substituted pyridinones as modulators of P38 map kinase. |
| CA2496577A1 (en) | 2002-08-28 | 2004-03-11 | Intermune, Inc. | Combination therapy for treatment of fibrotic disorders |
| TW200413273A (en) * | 2002-11-15 | 2004-08-01 | Wako Pure Chem Ind Ltd | Heavy hydrogenation method of heterocyclic rings |
| EP1599171A2 (en) | 2003-02-28 | 2005-11-30 | Intermune, Inc. | Combination therapy for treating alphavirus infection and liver fibrosis |
| WO2004105684A2 (en) | 2003-05-16 | 2004-12-09 | Intermune, Inc. | Combination therapy for proliferative disorders |
| WO2005038056A1 (en) | 2003-10-14 | 2005-04-28 | Intermune, Inc. | Combination therapy for the treatment of viral diseases |
| US7407973B2 (en) * | 2003-10-24 | 2008-08-05 | Intermune, Inc. | Use of pirfenidone in therapeutic regimens |
| JP4072623B2 (ja) | 2004-03-09 | 2008-04-09 | 独立行政法人産業技術総合研究所 | ピリジン−ｎ−オキシド類の製造方法 |
| WO2005110478A2 (en) * | 2004-04-13 | 2005-11-24 | Intermune, Inc. | Combination therapy for treating fibrotic disorders |
| SI1928454T1 (sl) * | 2005-05-10 | 2015-01-30 | Intermune, Inc. | Piridonski derivati za moduliranje s stresom aktiviranega protein kinaznega sistema |
| US20080033011A1 (en) * | 2005-07-29 | 2008-02-07 | Concert Pharmaceuticals Inc. | Novel benzo[d][1,3]-dioxol derivatives |
| NZ591443A (en) | 2005-09-22 | 2013-04-26 | Intermune Inc | Granule formation of pirfenidone and pharmaceutically acceptable excipients |
| US20070203202A1 (en) | 2005-12-02 | 2007-08-30 | Robinson Cynthia Y | Methods of reducing adverse events associated with pirfenidone therapy |
| US7750168B2 (en) * | 2006-02-10 | 2010-07-06 | Sigma-Aldrich Co. | Stabilized deuteroborane-tetrahydrofuran complex |
| CA2661404A1 (en) * | 2006-09-05 | 2008-03-13 | Schering Corporation | Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis |
| US20080287508A1 (en) | 2007-05-18 | 2008-11-20 | Intermune, Inc. | Altering pharmacokinetics of pirfenidone therapy |
| KR101767849B1 (ko) | 2007-06-20 | 2017-08-11 | 오스펙스 파마슈티칼스, 인코포레이티드 | 섬유증 저해제로서의 치환된 ｎ-아릴 피리디논 |
| WO2009035598A1 (en) | 2007-09-10 | 2009-03-19 | Concert Pharmaceuticals, Inc. | Deuterated pirfenidone |
| WO2010065755A1 (en) | 2008-12-04 | 2010-06-10 | Concert Pharmaceuticals, Inc. | Deuterated pyridinones |
| AP2011005824A0 (en) | 2009-01-26 | 2011-08-31 | Intermune Inc | Methods for treating acute myocardial infarctions and associated disorders. |
| KR101522924B1 (ko) | 2009-05-25 | 2015-05-26 | 센트럴 사우스 유니버시티 | 1-(치환된 페닐)-5-트리플루오로메틸-2-(1ｈ)피리돈 화합물 및 이것의 염의 제조방법 및 용도 |
| CA2828895A1 (en) | 2011-03-08 | 2012-09-13 | Auspex Pharamaceuticals, Inc. | Substituted n-aryl pyridinones |
| AU2012258575B2 (en) | 2011-05-25 | 2017-03-02 | Intermune, Inc. | Pirfenidone and anti-fibrotic therapy in selected patients |
| EA201691493A1 (ru) | 2014-01-24 | 2017-02-28 | Оспекс Фармасьютикалз, Инк. | Замещенные n-арилпиридиноны |
| WO2015171345A1 (en) | 2014-04-30 | 2015-11-12 | Auspex Pharmaceuticals, Inc. | N-aryl pyridinones modulators of fibrosis and/or collagen infiltration |
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2008
- 2008-06-20 KR KR1020167000072A patent/KR101767849B1/ko active IP Right Grant
- 2008-06-20 ES ES08771632T patent/ES2400026T3/es active Active
- 2008-06-20 JP JP2010513457A patent/JP5587184B2/ja active Active
- 2008-06-20 CN CN200880102512A patent/CN101842355A/zh active Pending
- 2008-06-20 WO PCT/US2008/067732 patent/WO2008157786A1/en active Application Filing
- 2008-06-20 US US12/143,484 patent/US8383823B2/en active Active
- 2008-06-20 KR KR1020107001341A patent/KR101583737B1/ko active IP Right Grant
- 2008-06-20 EP EP08771632A patent/EP2170828B1/en active Active
- 2008-06-20 DK DK08771632.0T patent/DK2170828T3/da active
- 2008-06-20 CN CN201510221701.2A patent/CN104892498A/zh active Pending
- 2008-06-20 AU AU2008265595A patent/AU2008265595B2/en active Active
- 2008-06-20 CA CA2691379A patent/CA2691379C/en active Active
- 2008-06-20 NZ NZ599643A patent/NZ599643A/xx unknown
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2009
- 2009-12-20 IL IL202840A patent/IL202840A/en active IP Right Grant
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2012
- 2012-10-29 US US13/663,188 patent/US8680123B1/en active Active
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2013
- 2013-12-18 US US14/132,528 patent/US8969575B2/en active Active
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2014
- 2014-04-30 US US14/266,048 patent/US9062001B2/en active Active
- 2014-08-08 US US14/455,339 patent/US8969576B2/en active Active
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2015
- 2015-05-21 US US14/718,993 patent/US9504677B2/en active Active
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2016
- 2016-02-24 HK HK16102071.0A patent/HK1214251A1/zh unknown