JP2004509961A5 - - Google Patents
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- Publication number
- JP2004509961A5 JP2004509961A5 JP2002531121A JP2002531121A JP2004509961A5 JP 2004509961 A5 JP2004509961 A5 JP 2004509961A5 JP 2002531121 A JP2002531121 A JP 2002531121A JP 2002531121 A JP2002531121 A JP 2002531121A JP 2004509961 A5 JP2004509961 A5 JP 2004509961A5
- Authority
- JP
- Japan
- Prior art keywords
- thiazolidine
- pyridyl
- ethoxy
- benzyl
- amino
- 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
- 239000000203 mixture Substances 0.000 description 22
- 201000010099 disease Diseases 0.000 description 20
- SUFUKZSWUHZXAV-BTJKTKAUSA-N rosiglitazone maleate Chemical compound [H+].[H+].[O-]C(=O)\C=C/C([O-])=O.C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O SUFUKZSWUHZXAV-BTJKTKAUSA-N 0.000 description 17
- 239000003814 drug Substances 0.000 description 15
- PVNIIMVLHYAWGP-UHFFFAOYSA-N nicotinic acid Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 14
- 206010022489 Insulin resistance Diseases 0.000 description 13
- 206010003210 Arteriosclerosis Diseases 0.000 description 12
- 208000002705 Glucose Intolerance Diseases 0.000 description 12
- 206010062060 Hyperlipidaemia Diseases 0.000 description 12
- 206010020772 Hypertension Diseases 0.000 description 12
- 208000008589 Obesity Diseases 0.000 description 12
- 208000001132 Osteoporosis Diseases 0.000 description 12
- 235000020824 obesity Nutrition 0.000 description 12
- 201000010065 polycystic ovary syndrome Diseases 0.000 description 12
- 239000008194 pharmaceutical composition Substances 0.000 description 11
- 210000002381 Plasma Anatomy 0.000 description 10
- 239000000243 solution Substances 0.000 description 9
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 8
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 8
- 229920001268 Cholestyramine Polymers 0.000 description 7
- GMRWGQCZJGVHKL-UHFFFAOYSA-N Colestipol Chemical compound ClCC1CO1.NCCNCCNCCNCCN GMRWGQCZJGVHKL-UHFFFAOYSA-N 0.000 description 7
- 229920002911 Colestipol Polymers 0.000 description 7
- FYPMFJGVHOHGLL-UHFFFAOYSA-N Probucol Chemical compound C=1C(C(C)(C)C)=C(O)C(C(C)(C)C)=CC=1SC(C)(C)SC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 FYPMFJGVHOHGLL-UHFFFAOYSA-N 0.000 description 7
- HGMSJMJPXGGEBP-UHFFFAOYSA-N [4-[3-(4-ethylphenyl)butyl]phenyl]-trimethylazanium Chemical compound C1=CC(CC)=CC=C1C(C)CCC1=CC=C([N+](C)(C)C)C=C1 HGMSJMJPXGGEBP-UHFFFAOYSA-N 0.000 description 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 7
- 229960002604 colestipol Drugs 0.000 description 7
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 7
- 229960003512 nicotinic acid Drugs 0.000 description 7
- 235000001968 nicotinic acid Nutrition 0.000 description 7
- 239000011664 nicotinic acid Substances 0.000 description 7
- 229960003912 probucol Drugs 0.000 description 7
- 201000010874 syndrome Diseases 0.000 description 7
- 208000008787 Cardiovascular Disease Diseases 0.000 description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 6
- 206010012289 Dementia Diseases 0.000 description 6
- 208000002249 Diabetes Complications Diseases 0.000 description 6
- 206010012601 Diabetes mellitus Diseases 0.000 description 6
- 206010012655 Diabetic complications Diseases 0.000 description 6
- 206010058108 Dyslipidaemia Diseases 0.000 description 6
- 206010018364 Glomerulonephritis Diseases 0.000 description 6
- 206010061989 Glomerulosclerosis Diseases 0.000 description 6
- 206010018429 Glucose tolerance impaired Diseases 0.000 description 6
- MNQZXJOMYWMBOU-UHFFFAOYSA-N Glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 description 6
- 208000009576 Hypercholesterolemia Diseases 0.000 description 6
- 206010021972 Inflammatory bowel disease Diseases 0.000 description 6
- 208000001083 Kidney Disease Diseases 0.000 description 6
- 108010028554 LDL Cholesterol Proteins 0.000 description 6
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N Leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 description 6
- 102000016267 Leptin Human genes 0.000 description 6
- 108010092277 Leptin Proteins 0.000 description 6
- 206010061227 Lipid metabolism disease Diseases 0.000 description 6
- 206010068871 Myotonic dystrophy Diseases 0.000 description 6
- 206010029149 Nephropathy Diseases 0.000 description 6
- 206010029151 Nephropathy Diseases 0.000 description 6
- 206010029164 Nephrotic syndrome Diseases 0.000 description 6
- 108009000551 Nephrotic syndrome Proteins 0.000 description 6
- 206010033645 Pancreatitis Diseases 0.000 description 6
- 206010038428 Renal disease Diseases 0.000 description 6
- 206010038932 Retinopathy Diseases 0.000 description 6
- 206010038923 Retinopathy Diseases 0.000 description 6
- 206010048214 Xanthoma Diseases 0.000 description 6
- 239000003288 aldose reductase inhibitor Substances 0.000 description 6
- 201000001320 atherosclerosis Diseases 0.000 description 6
- 201000011510 cancer Diseases 0.000 description 6
- 230000003920 cognitive function Effects 0.000 description 6
- 201000008739 coronary artery disease Diseases 0.000 description 6
- 235000014113 dietary fatty acids Nutrition 0.000 description 6
- -1 excipient Substances 0.000 description 6
- 239000000194 fatty acid Substances 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 6
- 239000008103 glucose Substances 0.000 description 6
- 201000001421 hyperglycemia Diseases 0.000 description 6
- 230000001631 hypertensive Effects 0.000 description 6
- 229940039781 leptin Drugs 0.000 description 6
- 201000009925 nephrosclerosis Diseases 0.000 description 6
- 230000001991 pathophysiological Effects 0.000 description 6
- 201000004681 psoriasis Diseases 0.000 description 6
- 150000003626 triacylglycerols Chemical class 0.000 description 6
- WQZGKKKJIJFFOK-VFUOTHLCSA-N β-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 6
- 210000002889 Endothelial Cells Anatomy 0.000 description 5
- 230000020411 cell activation Effects 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 108010069201 VLDL Cholesterol Proteins 0.000 description 4
- 238000001816 cooling Methods 0.000 description 4
- 238000001914 filtration Methods 0.000 description 4
- 238000010438 heat treatment Methods 0.000 description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-L maleate(2-) Chemical group [O-]C(=O)\C=C/C([O-])=O VZCYOOQTPOCHFL-UPHRSURJSA-L 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- VJYJKNKXBSOHFP-ODZAUARKSA-N O=C1CSC(=O)N1.OC(=O)\C=C/C(O)=O Chemical compound O=C1CSC(=O)N1.OC(=O)\C=C/C(O)=O VJYJKNKXBSOHFP-ODZAUARKSA-N 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
- 230000002194 synthesizing Effects 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 229940096700 plain lipid modifying drugs Fibrates Drugs 0.000 description 2
- 229940096701 plain lipid modifying drugs HMG CoA reductase inhibitors Drugs 0.000 description 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN805CH2000 | 2000-09-26 | ||
| PCT/US2001/029896 WO2002026737A1 (fr) | 2000-09-26 | 2001-09-25 | Nouvelles formes polymorphes de 5-[4-[2-[n-methyl-n-(2-pyridyl)amino]ethoxy]benzyl] thiazolidine-2,4-dione maleate et procede de preparation associe |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004509961A JP2004509961A (ja) | 2004-04-02 |
| JP2004509961A5 true JP2004509961A5 (fr) | 2008-11-06 |
Family
ID=29266775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002531121A Pending JP2004509961A (ja) | 2000-09-26 | 2001-09-25 | ５−［４−［２−［ｎ−メチル−ｎ−（２−ピリジル）アミノ］エトキシ］ベンジル］チアゾリジン−２，４−ジオンマレイン酸塩の新規の多型形態およびそれらの調製方法 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP1322647A1 (fr) |
| JP (1) | JP2004509961A (fr) |
| AU (1) | AU9123201A (fr) |
| BR (1) | BR0114196A (fr) |
| CA (1) | CA2426117A1 (fr) |
| CZ (1) | CZ2003864A3 (fr) |
| HU (1) | HUP0301161A3 (fr) |
| IL (1) | IL155036A0 (fr) |
| MX (1) | MXPA03002580A (fr) |
| NO (1) | NO324968B1 (fr) |
| NZ (1) | NZ525498A (fr) |
| PL (1) | PL360661A1 (fr) |
| SK (1) | SK3752003A3 (fr) |
| WO (1) | WO2002026737A1 (fr) |
| ZA (1) | ZA200303223B (fr) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6664278B2 (en) | 1997-12-16 | 2003-12-16 | Smithkline Beecham P.L.C. | Hydrate of 5-[4-[2-(N-methyl-N-(2-pyridil)amino)ethoxy]benzyl]thiazolidine-2,4-dione maleic acid salt |
| US20020137940A1 (en) | 1997-12-16 | 2002-09-26 | Smithkline Beecham P.L.C. | 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2, 4-dione, maleic acid salt, hydrate as pharmaceutical |
| GB9726563D0 (en) | 1997-12-16 | 1998-02-11 | Smithkline Beecham Plc | Novel pharmaceutical |
| US20040248945A1 (en) | 1999-04-23 | 2004-12-09 | Smithkline Beecham P.L.C. | Thiazolidinedione derivative and its use as antidiabetic |
| NZ515168A (en) | 1999-04-23 | 2004-02-27 | Smithkline Beecham Plc | Polymorph of 5-[4-[2- (n-methyl-n-( 2-pyridyl)amino) ethoxy]benzyl] thiazolidine-2,4-dione, maleic acid salt |
| AU765498B2 (en) | 1999-04-23 | 2003-09-18 | Smithkline Beecham Plc | Novel pharmaceutical |
| WO2004062667A1 (fr) * | 2003-01-08 | 2004-07-29 | Dr. Reddy's Laboratories Limited | Forme amorphe du maleate de rosiglitazone et procede de preparation |
| GB0307259D0 (en) * | 2003-03-28 | 2003-05-07 | Glaxo Group Ltd | Process |
| EP1468997A3 (fr) * | 2003-04-18 | 2004-11-03 | CHEMI S.p.A. | Formes polymorphes de maléate de rosiglitatone |
| GB2405403A (en) * | 2003-08-29 | 2005-03-02 | Cipla Ltd | Rosiglitazone maleate of particular polymorphic forms and methods of preparing rosiglitazone free base |
| UA83504C2 (en) | 2003-09-04 | 2008-07-25 | Селджин Корпорейшн | Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione |
| AR047541A1 (es) * | 2004-02-13 | 2006-01-25 | Sandoz Ag | Fosfato de 5-[[4-[2-metil-2-piridinil-amino-etoxi]fenil]metil]-2,4 tiazolidinadiona (rosiglitazona) y sus formas polimorficas |
| WO2005095390A2 (fr) * | 2004-03-31 | 2005-10-13 | Sandoz Ag | Nouveau co-precipite |
| EP1757603A4 (fr) * | 2004-05-11 | 2008-06-25 | Santen Pharmaceutical Co Ltd | Agent thérapeutique pour une affection de kératoconjonctivite |
| JP2005350451A (ja) * | 2004-05-11 | 2005-12-22 | Santen Pharmaceut Co Ltd | 角結膜障害治療剤 |
| CZ296472B6 (cs) * | 2004-07-27 | 2006-03-15 | Zentiva, A. S | Sul kyseliny stavelové s 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidin-2,4-dionu azpusob její prípravy a její pouzití |
| ITMI20041537A1 (it) * | 2004-07-28 | 2004-10-28 | Chemi Spa | Nuova forma polimorfa del rosiglitazone maleato |
| CZ298424B6 (cs) * | 2005-05-24 | 2007-09-26 | Zentiva, A. S. | Zpusob krystalizace rosiglitazonu a jeho derivátuze smesných rozpouštedel |
| EP2184055A1 (fr) | 2008-11-07 | 2010-05-12 | LEK Pharmaceuticals d.d. | Procédé de préparation de formes galéniques solides de maléate de rosiglitazone |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG59988A1 (en) * | 1987-09-04 | 1999-02-22 | Beecham Group Plc | Substituted thiazolidinedione derivatives |
| GB9218830D0 (en) * | 1992-09-05 | 1992-10-21 | Smithkline Beecham Plc | Novel compounds |
| EP0844997A1 (fr) * | 1996-06-19 | 1998-06-03 | Dr. Reddy's Research Foundation | Nouvelles formes polymorphes de la troglitazone ayant une activite anti-diabetique augmentee et procede pour leur preparation |
| WO1997041120A1 (fr) * | 1996-07-26 | 1997-11-06 | Dr. Reddy's Research Foundation | Composes de thiazolidinedione presentant des proprietes antidiabetiques, hypolipidemiantes, antihypertensives, leur procede de preparation et compositions pharmaceutiques les contenant |
| GB9726566D0 (en) * | 1997-12-16 | 1998-02-11 | Smithkline Beecham Plc | Novel pharmaceutical |
| NZ515168A (en) * | 1999-04-23 | 2004-02-27 | Smithkline Beecham Plc | Polymorph of 5-[4-[2- (n-methyl-n-( 2-pyridyl)amino) ethoxy]benzyl] thiazolidine-2,4-dione, maleic acid salt |
| AU765498B2 (en) * | 1999-04-23 | 2003-09-18 | Smithkline Beecham Plc | Novel pharmaceutical |
-
2001
- 2001-09-25 SK SK375-2003A patent/SK3752003A3/sk not_active Application Discontinuation
- 2001-09-25 MX MXPA03002580A patent/MXPA03002580A/es active IP Right Grant
- 2001-09-25 IL IL15503601A patent/IL155036A0/xx unknown
- 2001-09-25 NZ NZ525498A patent/NZ525498A/en unknown
- 2001-09-25 BR BR0114196-1A patent/BR0114196A/pt not_active Application Discontinuation
- 2001-09-25 CA CA002426117A patent/CA2426117A1/fr not_active Abandoned
- 2001-09-25 HU HU0301161A patent/HUP0301161A3/hu unknown
- 2001-09-25 CZ CZ2003864A patent/CZ2003864A3/cs unknown
- 2001-09-25 WO PCT/US2001/029896 patent/WO2002026737A1/fr active IP Right Grant
- 2001-09-25 JP JP2002531121A patent/JP2004509961A/ja active Pending
- 2001-09-25 AU AU9123201A patent/AU9123201A/xx active Pending
- 2001-09-25 EP EP01971336A patent/EP1322647A1/fr not_active Withdrawn
- 2001-09-25 PL PL01360661A patent/PL360661A1/xx not_active Application Discontinuation
-
2003
- 2003-03-25 NO NO20031356A patent/NO324968B1/no unknown
- 2003-04-24 ZA ZA200303223A patent/ZA200303223B/xx unknown
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