JP2002528490A5 - - Google Patents
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- JP2002528490A5 JP2002528490A5 JP2000579211A JP2000579211A JP2002528490A5 JP 2002528490 A5 JP2002528490 A5 JP 2002528490A5 JP 2000579211 A JP2000579211 A JP 2000579211A JP 2000579211 A JP2000579211 A JP 2000579211A JP 2002528490 A5 JP2002528490 A5 JP 2002528490A5
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- alkyl
- aryl
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- phenyl
- disease
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| DE (1) | DE69940480D1 (https=) |
| WO (1) | WO2000025770A1 (https=) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19923086A1 (de) * | 1999-05-20 | 2000-11-23 | Aventis Pharma Gmbh | Cinnamoylaminoalkyl-substituierte Benzolsulfonamidderivate, Verfahren zu ihrer Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| MY125533A (en) * | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| GB0012214D0 (en) | 2000-05-19 | 2000-07-12 | Merck Sharp & Dohme | Therapeutic agents |
| EP1299362A4 (en) * | 2000-07-05 | 2004-11-03 | Synaptic Pharma Corp | SELECTIVE RECEPTOR ANTAGONISTS OF MELANINE CONCENTRATING HORMON-1 (MCH1) AND THEIR USE |
| CA2436744A1 (en) * | 2001-01-30 | 2002-08-08 | Merck & Co., Inc. | Method for identifying maxi-k channel blockers for use in lowering elevated intraocular pressure using hek-293 cells |
| DE10153346A1 (de) * | 2001-10-29 | 2004-04-22 | Grünenthal GmbH | Substituierte Indole |
| US20040115739A1 (en) * | 2002-01-25 | 2004-06-17 | Garcia Maria L | Method for identifying maxi-k channel blockers for use in lowering elevated intraocular pressure using hek-293 cells |
| TW200307539A (en) * | 2002-02-01 | 2003-12-16 | Bristol Myers Squibb Co | Cycloalkyl inhibitors of potassium channel function |
| US8163726B2 (en) * | 2002-09-18 | 2012-04-24 | University Of Pennsylvania | Method of inhibiting choroidal neovascularization |
| WO2004041161A2 (en) * | 2002-10-30 | 2004-05-21 | Merck & Co., Inc. | Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity |
| MXPA05010824A (es) * | 2003-04-10 | 2005-12-05 | Pfizer | Compuestos biciclicos como antagonistas del receptor nr2b. |
| CA2539324A1 (en) | 2003-09-18 | 2005-03-31 | Macusight, Inc. | Transscleral delivery |
| EP1680411A2 (en) * | 2003-10-08 | 2006-07-19 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters containing cycloalkyl or pyranyl groups |
| JP2007517056A (ja) | 2003-12-29 | 2007-06-28 | セプラコア インコーポレーテッド | ピロール及びピラゾールｄａａｏ阻害剤 |
| US7772232B2 (en) * | 2004-04-15 | 2010-08-10 | Bristol-Myers Squibb Company | Quinazolinyl compounds as inhibitors of potassium channel function |
| US7879839B2 (en) | 2004-07-29 | 2011-02-01 | Merck Sharp & Dohme Corp. | Potassium channel inhibitors |
| US7569589B2 (en) | 2004-07-29 | 2009-08-04 | Merck & Co., Inc. | Potassium channel inhibitors |
| US8663639B2 (en) | 2005-02-09 | 2014-03-04 | Santen Pharmaceutical Co., Ltd. | Formulations for treating ocular diseases and conditions |
| JP4974903B2 (ja) | 2005-02-09 | 2012-07-11 | 参天製薬株式会社 | 疾患または状態を処置するための液体処方物 |
| EP1922311A2 (en) * | 2005-09-09 | 2008-05-21 | Brystol-Myers Squibb Company | Acyclic ikur inhibitors |
| US20070203111A1 (en) * | 2006-01-06 | 2007-08-30 | Sepracor Inc. | Cycloalkylamines as monoamine reuptake inhibitors |
| NZ569608A (en) | 2006-01-06 | 2011-09-30 | Sepracor Inc | Tetralone-based monoamine reuptake inhibitors |
| WO2007092620A2 (en) | 2006-02-09 | 2007-08-16 | Macusight, Inc. | Stable formulations, and methods of their preparation and use |
| PL2001466T3 (pl) | 2006-03-23 | 2016-06-30 | Santen Pharmaceutical Co Ltd | Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń |
| CN101421228B (zh) | 2006-03-31 | 2014-05-21 | 塞普拉柯公司 | 手性酰胺和胺的制备 |
| AR060404A1 (es) * | 2006-04-11 | 2008-06-11 | Novartis Ag | Compuestos organicos utiles como inhibidores de dipeptidil-peptidasa iv |
| US7884124B2 (en) | 2006-06-30 | 2011-02-08 | Sepracor Inc. | Fluoro-substituted inhibitors of D-amino acid oxidase |
| US7801502B2 (en) * | 2006-12-18 | 2010-09-21 | Aai Corporation | Method for implementing continuous radio frequency (RF) alignment in advanced electronic warfare (EW) signal stimulation systems |
| US20130012485A1 (en) * | 2006-12-22 | 2013-01-10 | Baeschlin Daniel Kaspar | Organic compounds |
| US7902252B2 (en) | 2007-01-18 | 2011-03-08 | Sepracor, Inc. | Inhibitors of D-amino acid oxidase |
| CA2688493C (en) | 2007-05-31 | 2016-04-19 | Sepracor Inc. | Phenyl substituted cycloalkylamines as monoamine reuptake inhibitors |
| EP2280941B1 (de) * | 2008-03-27 | 2015-05-06 | Grünenthal GmbH | (hetero-)aryl-cyclohexan-derivate |
| ES2464102T3 (es) | 2008-03-27 | 2014-05-30 | Grünenthal GmbH | Derivados de 4-aminociclohexano sustituidos |
| US8409628B2 (en) | 2010-02-04 | 2013-04-02 | Penguin IP Holdings, Inc. | Methods and compositions for oxygenation of skin to treat skin disorders |
| US8900601B2 (en) | 2010-03-31 | 2014-12-02 | Jennifer Bartels | Permeable mixtures, methods and compositions for the skin |
| AU2011261375B2 (en) | 2010-06-04 | 2016-09-22 | Albany Molecular Research, Inc. | Glycine transporter-1 inhibitors, methods of making them, and uses thereof |
| JP2015501327A (ja) * | 2011-11-04 | 2015-01-15 | シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト | 殺虫化合物 |
| WO2013093508A2 (en) * | 2011-12-22 | 2013-06-27 | Oslo University Hospital Hf | Wnt pathway inhibitors |
| TW201427947A (zh) | 2012-10-12 | 2014-07-16 | Lundbeck & Co As H | 環狀胺 |
| TWI598325B (zh) * | 2012-10-12 | 2017-09-11 | Ｈ 朗德貝克公司 | 苯甲醯胺類 |
| UY36390A (es) | 2014-11-05 | 2016-06-01 | Flexus Biosciences Inc | Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen |
| MX2017005462A (es) * | 2014-11-05 | 2017-07-28 | Flexus Biosciences Inc | Agentes inmunorreguladores. |
| WO2016105448A1 (en) * | 2014-12-22 | 2016-06-30 | Darryl Rideout | Imidazoline receptor type 1 ligands for use as therapeutics |
| WO2021114313A1 (en) * | 2019-12-14 | 2021-06-17 | Shanghai East Hospital | Ion channel antagonists/blockers and uses thereof |
| CN111812243B (zh) * | 2020-07-21 | 2022-06-03 | 中南大学湘雅二医院 | 一种消减全血环孢素测定的基质效应的分析方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL84944A (en) * | 1987-01-19 | 1992-02-16 | Ici Plc | Pharmaceutical compositions containing 1,2-dihydro-3h-indazolone derivatives,some new such compounds and their preparation |
| GB8707123D0 (en) | 1987-03-25 | 1987-04-29 | Pfizer Ltd | Antiarrhythmic agents |
| IL88314A (en) | 1987-11-18 | 1994-05-30 | Tanabe Seiyaku Co | Sulphonylamino indane derivatives, their preparation and pharmaceutical compositions containing them |
| IE903957A1 (en) | 1989-11-06 | 1991-05-08 | Sanofi Sa | Aromatic amine compounds, their method of preparation and¹pharmaceutical compositions in which they are present |
| US5179216A (en) * | 1990-08-16 | 1993-01-12 | American Home Products Corporation | N,n', n'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-coa:cholesterol-acyl transferase |
| EP0472053B1 (en) | 1990-08-20 | 1998-06-17 | Eisai Co., Ltd. | Sulfonamide derivatives |
| ZA96211B (en) | 1995-01-12 | 1996-07-26 | Teva Pharma | Compositions containing and methods of using 1- aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives |
| CA2253502A1 (en) * | 1996-05-06 | 1997-11-13 | Stephen Warren Kaldor | Anti-viral compounds |
| US6083986A (en) | 1996-07-26 | 2000-07-04 | Icagen, Inc. | Potassium channel inhibitors |
| TW467902B (en) | 1996-07-31 | 2001-12-11 | Bristol Myers Squibb Co | Diphenyl heterocycles as potassium channel modulators |
| US6194458B1 (en) * | 1998-10-30 | 2001-02-27 | Merck & Co., Inc. | Benzamide potassium channel inhibitors |
-
1999
- 1999-10-21 US US09/422,143 patent/US6632836B1/en not_active Expired - Fee Related
- 1999-10-26 AT AT99955159T patent/ATE423557T1/de not_active IP Right Cessation
- 1999-10-26 CA CA002348742A patent/CA2348742C/en not_active Expired - Fee Related
- 1999-10-26 AU AU11331/00A patent/AU764477B2/en not_active Ceased
- 1999-10-26 WO PCT/US1999/024949 patent/WO2000025770A1/en not_active Ceased
- 1999-10-26 JP JP2000579211A patent/JP4504570B2/ja not_active Expired - Fee Related
- 1999-10-26 DE DE69940480T patent/DE69940480D1/de not_active Expired - Lifetime
- 1999-10-26 EP EP99955159A patent/EP1143965B1/en not_active Expired - Lifetime
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