JP2006525360A - Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートおよびＨＭＧ−ＣｏＡ還元酵素阻害剤を含む併用 - Google Patents
Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートおよびＨＭＧ−ＣｏＡ還元酵素阻害剤を含む併用 Download PDFInfo
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- JP2006525360A JP2006525360A JP2006514221A JP2006514221A JP2006525360A JP 2006525360 A JP2006525360 A JP 2006525360A JP 2006514221 A JP2006514221 A JP 2006514221A JP 2006514221 A JP2006514221 A JP 2006514221A JP 2006525360 A JP2006525360 A JP 2006525360A
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- hmg
- coa reductase
- reductase inhibitor
- ethylbutyl
- cyclohexyl
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Landscapes
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
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| US46741803P | 2003-05-02 | 2003-05-02 | |
| US47149503P | 2003-05-16 | 2003-05-16 | |
| US47737203P | 2003-06-10 | 2003-06-10 | |
| US53485604P | 2004-01-08 | 2004-01-08 | |
| PCT/US2004/013633 WO2004098583A1 (en) | 2003-05-02 | 2004-04-30 | Combination comprising s-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate and an hmg coa reductase inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| JP2011284636A Division JP2012107018A (ja) | 2003-05-02 | 2011-12-27 | Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートおよびＨＭＧ−ＣｏＡ還元酵素阻害剤を含む併用 |
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| JP2006525360A true JP2006525360A (ja) | 2006-11-09 |
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| JP2006514221A Pending JP2006525360A (ja) | 2003-05-02 | 2004-04-30 | Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートおよびＨＭＧ−ＣｏＡ還元酵素阻害剤を含む併用 |
| JP2011284636A Pending JP2012107018A (ja) | 2003-05-02 | 2011-12-27 | Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートおよびＨＭＧ−ＣｏＡ還元酵素阻害剤を含む併用 |
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Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20050020668A1 (enExample) |
| EP (3) | EP2289501A1 (enExample) |
| JP (2) | JP2006525360A (enExample) |
| CN (1) | CN102512679A (enExample) |
| AR (1) | AR044155A1 (enExample) |
| PE (1) | PE20050148A1 (enExample) |
| TW (2) | TWI393560B (enExample) |
| WO (1) | WO2004098583A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015515498A (ja) * | 2012-04-30 | 2015-05-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規製剤 |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7879840B2 (en) * | 2005-08-25 | 2011-02-01 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| US20040229781A1 (en) * | 2000-05-10 | 2004-11-18 | Marks Andrew Robert | Compounds and methods for treating and preventing exercise-induced cardiac arrhythmias |
| US6489125B1 (en) * | 2000-05-10 | 2002-12-03 | The Trustees Of Columbia University In The City Of New York | Methods for identifying chemical compounds that inhibit dissociation of FKBP12.6 binding protein from type 2 ryanodine receptor |
| US20040048780A1 (en) * | 2000-05-10 | 2004-03-11 | The Trustees Of Columbia University In The City Of New York | Method for treating and preventing cardiac arrhythmia |
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| US20060293266A1 (en) * | 2000-05-10 | 2006-12-28 | The Trustees Of Columbia | Phosphodiesterase 4D in the ryanodine receptor complex protects against heart failure |
| US8022058B2 (en) | 2000-05-10 | 2011-09-20 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| US7718644B2 (en) * | 2004-01-22 | 2010-05-18 | The Trustees Of Columbia University In The City Of New York | Anti-arrhythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) and uses thereof |
| US7544678B2 (en) * | 2002-11-05 | 2009-06-09 | The Trustees Of Columbia University In The City Of New York | Anti-arrythmic and heart failure drugs that target the leak in the ryanodine receptor (RyR2) |
| HRP20050696B1 (en) | 2003-01-14 | 2008-10-31 | Arena Pharmaceuticals Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
| AU2004220548A1 (en) | 2003-03-07 | 2004-09-23 | The Trustees Of Columbia University, In The City Of New York | Type 1 ryanodine receptor-based methods |
| JP2006520810A (ja) * | 2003-03-17 | 2006-09-14 | 日本たばこ産業株式会社 | Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートの経口吸収性を増加させる方法 |
| US7132426B2 (en) | 2003-07-14 | 2006-11-07 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| US8710045B2 (en) * | 2004-01-22 | 2014-04-29 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the ryanodine receptors |
| MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
| US7704990B2 (en) * | 2005-08-25 | 2010-04-27 | The Trustees Of Columbia University In The City Of New York | Agents for preventing and treating disorders involving modulation of the RyR receptors |
| MX2013003184A (es) | 2010-09-22 | 2013-06-07 | Arena Pharm Inc | Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo. |
| WO2014154606A1 (en) | 2013-03-27 | 2014-10-02 | F. Hoffmann-La Roche Ag | Genetic markers for predicting responsiveness to therapy |
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| US11007175B2 (en) | 2015-01-06 | 2021-05-18 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
| BR112017027656B1 (pt) | 2015-06-22 | 2023-12-05 | Arena Pharmaceuticals, Inc. | Hábito cristalino de placa livre de sal de l-arginina de ácido (r)-2-(7-(4- ciclopentil-3-(trifluorometil)benzilóxi)- 1,2,3,4-tetra-hidrociclo-penta[b]indol-3- il)acético, composição farmacêutica que o compreende, seus usos e método de preparação do mesmo |
| CA3053418A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| BR112020024762A2 (pt) | 2018-06-06 | 2021-03-23 | Arena Pharmaceuticals, Inc. | métodos de tratamento de condições relacionadas ao receptor s1p1 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH1149743A (ja) * | 1997-02-12 | 1999-02-23 | Japan Tobacco Inc | Ｃｅｔｐ活性阻害剤として有効な化合物 |
| WO2000038722A1 (en) * | 1998-12-23 | 2000-07-06 | G.D. Searle & Co. | COMBINATIONS OF CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS AND HMG CoA REDUCTASE INHIBITORS FOR CARDIOVASCULAR INDICATIONS |
| WO2002013797A2 (en) * | 2000-08-15 | 2002-02-21 | Pfizer Products Inc. | Therapeutic combination of a cetp inhibitor and atorvastatin |
Family Cites Families (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3576830A (en) * | 1966-08-12 | 1971-04-27 | Sumitomo Chemical Co | Amides containing sulfur |
| US4117158A (en) * | 1977-09-27 | 1978-09-26 | American Cyanamid Company | 4-(monoalkylamino)benzonitriles useful as anti-atherosclerotic agents |
| US4177158A (en) * | 1978-02-13 | 1979-12-04 | Chevron Research Company | Method for producing an attrition-resistant adsorbent for sulfur dioxide, the resulting composition and a process using same |
| US4346277A (en) * | 1979-10-29 | 1982-08-24 | Eaton Corporation | Packaged electrical heating element |
| US4444784A (en) * | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| US5354772A (en) * | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| US4681893A (en) * | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| USRE36481E (en) * | 1986-06-23 | 2000-01-04 | Merck & Co., Inc. | HMG-CoA reductase inhibitors |
| US4940727A (en) * | 1986-06-23 | 1990-07-10 | Merck & Co., Inc. | Novel HMG-CoA reductase inhibitors |
| US4740438A (en) * | 1986-12-10 | 1988-04-26 | Eastman Kodak Company | Organic disulfides as image dye stabilizers |
| US4853319A (en) * | 1986-12-22 | 1989-08-01 | Eastman Kodak Company | Photographic silver halide element and process |
| JP2569746B2 (ja) * | 1987-08-20 | 1997-01-08 | 日産化学工業株式会社 | キノリン系メバロノラクトン類 |
| GB8729994D0 (en) * | 1987-12-23 | 1988-02-03 | Glaxo Group Ltd | Chemical compounds |
| US5030447A (en) * | 1988-03-31 | 1991-07-09 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions having good stability |
| US5180589A (en) * | 1988-03-31 | 1993-01-19 | E. R. Squibb & Sons, Inc. | Pravastatin pharmaceuatical compositions having good stability |
| US5118583A (en) * | 1988-10-12 | 1992-06-02 | Mitsubishi Paper Mills Limited | Processing composition for printing plate |
| FI94339C (fi) * | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| US5622985A (en) * | 1990-06-11 | 1997-04-22 | Bristol-Myers Squibb Company | Method for preventing a second heart attack employing an HMG CoA reductase inhibitor |
| FR2665450B1 (fr) * | 1990-08-01 | 1994-04-08 | Rhone Poulenc Chimie | Procede de preparation de dispersions aqueuses de copolymeres. |
| JP2648897B2 (ja) * | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| HU9203780D0 (en) * | 1991-12-12 | 1993-03-29 | Sandoz Ag | Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them |
| WO1993011782A1 (en) * | 1991-12-19 | 1993-06-24 | Southwest Foundation For Biomedical Research | Cetp inhibitor polypeptide, antibodies against the synthetic polypeptide and prophylactic and therapeutic anti-atherosclerosis treatments |
| US5519001A (en) * | 1991-12-19 | 1996-05-21 | Southwest Foundation For Biomedical Research | CETP inhibitor polypeptide antibodies against the synthetic polypeptide and prophylactic and therapeutic anti-atherosclerosis treatments |
| US5217859A (en) * | 1992-04-16 | 1993-06-08 | Eastman Kodak Company | Aqueous, solid particle dispersions of dichalcogenides for photographic emulsions and coatings |
| US5219721A (en) * | 1992-04-16 | 1993-06-15 | Eastman Kodak Company | Silver halide photographic emulsions sensitized in the presence of organic dichalcogenides |
| SG45369A1 (en) * | 1993-01-19 | 1998-10-16 | Warner Lambert Co | Stable oral ci-981 formulation and process of preparing same |
| US5350667A (en) * | 1993-06-17 | 1994-09-27 | Eastman Kodak Company | Photographic elements containing magenta couplers and process for using same |
| IL110151A (en) * | 1993-06-30 | 1998-10-30 | Sankyo Co | Amide derivatives and pharmaceutical compositions containing them |
| US5776951A (en) * | 1993-06-30 | 1998-07-07 | Glaxo Wellcome Inc. | Anti-atherosclerotic diaryl compounds |
| US5446207A (en) * | 1993-09-01 | 1995-08-29 | Harbor Branch Oceanographic Institution, Inc. | Anti-dyslipidemic agents |
| US5459154A (en) * | 1993-11-08 | 1995-10-17 | American Home Products Corporation | N-hydroxyureas as 5-lipoxygenase inhibitors and inhibitors of oxidative modification of low density lipoprotein |
| US5405969A (en) * | 1993-12-10 | 1995-04-11 | Eastman Kodak Company | Manufacture of thioether compounds |
| JP3304189B2 (ja) * | 1994-03-18 | 2002-07-22 | マツダ株式会社 | 加硫スクラップゴムを含有する成形用ゴム組成物及びその製造方法 |
| US5654134A (en) * | 1994-05-18 | 1997-08-05 | Fuji Photo Film Co., Ltd. | Silver halide emulsion |
| DE4428457C1 (de) * | 1994-08-11 | 1995-10-05 | Bayer Ag | Geformte, paraffinhaltige Mastiziermittel |
| KR100204738B1 (ko) * | 1994-11-12 | 1999-06-15 | 성재갑 | 콜레스테릴 에스테르 전달 단백질 저해 펩티드 및 이를 포함하는 동맥경화증 예방 및 치료제 |
| US5698564A (en) * | 1994-12-16 | 1997-12-16 | Nisshin Flour Milling Co., Ltd. | Diphenyl disulfide compounds |
| DE69634054T2 (de) * | 1995-07-17 | 2005-12-08 | Warner-Lambert Co. | Kristalline (R-(R*, R*))-2-(4-Fluorophenyl)-β, δ-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-((Phenylamino)Carbonyl)-1H-Pyrrol-1-Heptancarbonsäure Hemi Calcium Salz (Atorvastatin) |
| DE19610932A1 (de) * | 1996-03-20 | 1997-09-25 | Bayer Ag | 2-Aryl-substituierte Pyridine |
| DE19627431A1 (de) * | 1996-07-08 | 1998-01-15 | Bayer Ag | Heterocyclisch kondensierte Pyridine |
| US6207671B1 (en) * | 1996-07-08 | 2001-03-27 | Bayer Aktiengesellschaft | Cycloalkano-pyridines |
| HRP970330B1 (en) * | 1996-07-08 | 2004-06-30 | Bayer Ag | Cycloalkano pyridines |
| US6093573A (en) * | 1997-06-20 | 2000-07-25 | Xoma | Three-dimensional structure of bactericidal/permeability-increasing protein (BPI) |
| US5908859A (en) * | 1997-08-11 | 1999-06-01 | Eli Lilly And Company | Benzothiophenes for inhibiting hyperlipidemia |
| DE19741051A1 (de) * | 1997-09-18 | 1999-03-25 | Bayer Ag | Hetero-Tetrahydrochinoline |
| MA24643A1 (fr) * | 1997-09-18 | 1999-04-01 | Bayer Ag | Tetrahydro-naphtalenes substitues et composes analogues |
| US5916595A (en) * | 1997-12-12 | 1999-06-29 | Andrx Pharmaceutials, Inc. | HMG co-reductase inhibitor |
| US6080778A (en) * | 1998-03-23 | 2000-06-27 | Children's Medical Center Corporation | Methods for decreasing beta amyloid protein |
| US6147089A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6140342A (en) * | 1998-09-17 | 2000-10-31 | Pfizer Inc. | Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines |
| US6147090A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6197786B1 (en) * | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
| GT199900147A (es) * | 1998-09-17 | 1999-09-06 | 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas. | |
| DE19917233A1 (de) * | 1999-04-16 | 2000-10-19 | Aventis Pharma Gmbh | Kristalline Formen des Natriumsalzes des 5-Chlor-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonyl-phenyl)-ethyl)- benzamids |
| US6458849B1 (en) * | 1999-09-23 | 2002-10-01 | G.D. Searle & Co. | use of substituted N,N-disubstituted mercapto amino compounds for inhibiting cholesteryl ester transfer protein activity |
| US20010018446A1 (en) * | 1999-09-23 | 2001-08-30 | G.D. Searle & Co. | Substituted N-Aliphatic-N-Aromatictertiary-Heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity |
| HN2000000203A (es) * | 1999-11-30 | 2001-06-13 | Pfizer Prod Inc | Procedimiento para la obtencion de 1,2,3,4-tetrahidroquinolinas 4-carboxiamino-2- sustituidas. |
| US6242003B1 (en) * | 2000-04-13 | 2001-06-05 | Novartis Ag | Organic compounds |
| US20020013334A1 (en) * | 2000-06-15 | 2002-01-31 | Robl Jeffrey A. | HMG-CoA reductase inhibitors and method |
| US7115279B2 (en) * | 2000-08-03 | 2006-10-03 | Curatolo William J | Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors |
| US7049283B2 (en) * | 2000-12-06 | 2006-05-23 | Novartis Ag | Pharmaceutical compositions for the oral delivery of pharmacologically active agents |
| EE200400024A (et) * | 2001-06-21 | 2004-06-15 | Pfizer Products Inc. | Kolesterüülestri ülekandevalgu inhibiitorite iseemulgeeruvad formulatsioonid |
| US20040053842A1 (en) * | 2002-07-02 | 2004-03-18 | Pfizer Inc. | Methods of treatment with CETP inhibitors and antihypertensive agents |
| US7071210B2 (en) * | 2002-07-02 | 2006-07-04 | Pfizer Inc. | CETP inhibitors in combination with antihypertensive agents and uses thereof |
| ATE534381T1 (de) * | 2003-03-17 | 2011-12-15 | Japan Tobacco Inc | Pharmazeutische cetp-inhibitor-zusammensetzungen |
| JP2006520810A (ja) * | 2003-03-17 | 2006-09-14 | 日本たばこ産業株式会社 | Ｓ−［２−（［［１−（２−エチルブチル）シクロヘキシル］カルボニル］アミノ）フェニル］２−メチルプロパンチオエートの経口吸収性を増加させる方法 |
| BRPI0413363A (pt) * | 2003-08-04 | 2006-10-10 | Pfizer Prod Inc | formas de dosagem fornecendo liberação controlada de inibidores de proteìna de transferência de ésteres de colesterila e liberação imediata de inibidores de hmg-coa redutase |
-
2004
- 2004-04-23 TW TW093111373A patent/TWI393560B/zh not_active IP Right Cessation
- 2004-04-23 TW TW101105603A patent/TWI494102B/zh not_active IP Right Cessation
- 2004-04-30 EP EP10011298A patent/EP2289501A1/en not_active Withdrawn
- 2004-04-30 CN CN2011104212299A patent/CN102512679A/zh active Pending
- 2004-04-30 PE PE2004000438A patent/PE20050148A1/es not_active Application Discontinuation
- 2004-04-30 AR ARP040101498A patent/AR044155A1/es unknown
- 2004-04-30 EP EP10011299.4A patent/EP2289502B1/en not_active Expired - Lifetime
- 2004-04-30 WO PCT/US2004/013633 patent/WO2004098583A1/en not_active Ceased
- 2004-04-30 EP EP04751157A patent/EP1638545A1/en not_active Withdrawn
- 2004-04-30 US US10/835,916 patent/US20050020668A1/en not_active Abandoned
- 2004-04-30 JP JP2006514221A patent/JP2006525360A/ja active Pending
-
2011
- 2011-12-27 JP JP2011284636A patent/JP2012107018A/ja active Pending
-
2013
- 2013-05-03 US US13/887,032 patent/US20140121229A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH1149743A (ja) * | 1997-02-12 | 1999-02-23 | Japan Tobacco Inc | Ｃｅｔｐ活性阻害剤として有効な化合物 |
| WO2000038722A1 (en) * | 1998-12-23 | 2000-07-06 | G.D. Searle & Co. | COMBINATIONS OF CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS AND HMG CoA REDUCTASE INHIBITORS FOR CARDIOVASCULAR INDICATIONS |
| WO2002013797A2 (en) * | 2000-08-15 | 2002-02-21 | Pfizer Products Inc. | Therapeutic combination of a cetp inhibitor and atorvastatin |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015515498A (ja) * | 2012-04-30 | 2015-05-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規製剤 |
Also Published As
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|---|---|
| EP2289502B1 (en) | 2015-07-22 |
| US20140121229A1 (en) | 2014-05-01 |
| PE20050148A1 (es) | 2005-05-19 |
| AR044155A1 (es) | 2005-08-24 |
| TW201231043A (en) | 2012-08-01 |
| TWI494102B (zh) | 2015-08-01 |
| US20050020668A1 (en) | 2005-01-27 |
| JP2012107018A (ja) | 2012-06-07 |
| HK1154780A1 (en) | 2012-05-04 |
| EP2289501A1 (en) | 2011-03-02 |
| TWI393560B (zh) | 2013-04-21 |
| EP1638545A1 (en) | 2006-03-29 |
| EP2289502A1 (en) | 2011-03-02 |
| CN102512679A (zh) | 2012-06-27 |
| WO2004098583A1 (en) | 2004-11-18 |
| TW200507831A (en) | 2005-03-01 |
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