JP2005509642A5 - - Google Patents
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- Publication number
- JP2005509642A5 JP2005509642A5 JP2003538181A JP2003538181A JP2005509642A5 JP 2005509642 A5 JP2005509642 A5 JP 2005509642A5 JP 2003538181 A JP2003538181 A JP 2003538181A JP 2003538181 A JP2003538181 A JP 2003538181A JP 2005509642 A5 JP2005509642 A5 JP 2005509642A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- solvate
- physiologically acceptable
- acceptable salt
- 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 38
- 150000003839 salts Chemical class 0.000 claims 16
- 239000012453 solvate Substances 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 239000011737 fluorine Substances 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- -1 heteroaryl compound Chemical class 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- GBTODAKMABNGIJ-VWLOTQADSA-N 3-[4-[6-[[(2r)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]ethyl]amino]hexoxy]butyl]benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC(CCCCOCCCCCCNC[C@H](O)C=2C=C(CO)C(O)=CC=2)=C1 GBTODAKMABNGIJ-VWLOTQADSA-N 0.000 claims 1
- 108060003345 Adrenergic Receptor Proteins 0.000 claims 1
- 102000017910 Adrenergic receptor Human genes 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 239000000048 adrenergic agonist Substances 0.000 claims 1
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- KYKAJFCTULSVSH-UHFFFAOYSA-N chloro(fluoro)methane Chemical compound F[C]Cl KYKAJFCTULSVSH-UHFFFAOYSA-N 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- NBVXSUQYWXRMNV-UHFFFAOYSA-N fluoromethane Chemical compound FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 150000002596 lactones Chemical group 0.000 claims 1
- 244000144972 livestock Species 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 239000008249 pharmaceutical aerosol Substances 0.000 claims 1
- 239000003380 propellant Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 0 N*(CCCO1)C1=O Chemical compound N*(CCCO1)C1=O 0.000 description 1
- VIHAEDVKXSOUAT-UHFFFAOYSA-N O=C1OCC=C1 Chemical compound O=C1OCC=C1 VIHAEDVKXSOUAT-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0125259.2A GB0125259D0 (en) | 2001-10-20 | 2001-10-20 | Novel compounds |
| PCT/EP2002/011634 WO2003035668A2 (en) | 2001-10-20 | 2002-10-17 | Novel anti-inflammatory androstane derivatives -17-carboxy-lactone substituted steroids with an aryl-carboxylic ester in position 17.alpha |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005509642A JP2005509642A (ja) | 2005-04-14 |
| JP2005509642A5 true JP2005509642A5 (enExample) | 2006-01-05 |
| JP4495456B2 JP4495456B2 (ja) | 2010-07-07 |
Family
ID=9924247
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003538181A Expired - Lifetime JP4495456B2 (ja) | 2001-10-20 | 2002-10-17 | 新規の抗炎症性アンドロスタン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7405206B2 (enExample) |
| EP (1) | EP1444248B1 (enExample) |
| JP (1) | JP4495456B2 (enExample) |
| AT (1) | ATE393771T1 (enExample) |
| AU (1) | AU2002350561A1 (enExample) |
| DE (1) | DE60226334T2 (enExample) |
| ES (1) | ES2304457T3 (enExample) |
| GB (1) | GB0125259D0 (enExample) |
| WO (1) | WO2003035668A2 (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6858596B2 (en) | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivative |
| GB0019172D0 (en) | 2000-08-05 | 2000-09-27 | Glaxo Group Ltd | Novel compounds |
| US6858593B2 (en) | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6777399B2 (en) | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| EP1305329B2 (en) | 2000-08-05 | 2015-03-18 | Glaxo Group Limited | 6.alpha.,9.alpha.-difluoro-17.alpha.-(2-furanylcarboxyl)oxy-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent |
| UA77656C2 (en) | 2001-04-07 | 2007-01-15 | Glaxo Group Ltd | S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent |
| EP2039700A2 (en) | 2001-04-30 | 2009-03-25 | Glaxo Group Limited | Novel anti-inflammatory androstane derivatives |
| GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
| TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
| GB0316290D0 (en) * | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
| GB0401334D0 (en) | 2004-01-21 | 2004-02-25 | Novartis Ag | Organic compounds |
| GB0411056D0 (en) | 2004-05-18 | 2004-06-23 | Novartis Ag | Organic compounds |
| GT200500281A (es) | 2004-10-22 | 2006-04-24 | Novartis Ag | Compuestos organicos. |
| GB0424284D0 (en) | 2004-11-02 | 2004-12-01 | Novartis Ag | Organic compounds |
| GB0426164D0 (en) | 2004-11-29 | 2004-12-29 | Novartis Ag | Organic compounds |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| BRPI0614290A2 (pt) | 2005-08-08 | 2011-03-22 | Argenta Discovery Ltd | derivados de biciclo [ 2.2.1 ] hept-7-ilamina e seus usos |
| GB0516313D0 (en) | 2005-08-08 | 2005-09-14 | Argenta Discovery Ltd | Azole derivatives and their uses |
| KR20130020850A (ko) | 2005-10-21 | 2013-02-28 | 노파르티스 아게 | Ｉｌ-13에 대항한 인간 항체 및 치료적 용도 |
| GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| TWI374147B (en) * | 2006-01-27 | 2012-10-11 | Sun Pharma Advance Res Company Ltd | Novel 11β-hydroxyandrosta-4-ene-3-ones |
| GB0601951D0 (en) | 2006-01-31 | 2006-03-15 | Novartis Ag | Organic compounds |
| SI2013211T1 (sl) | 2006-04-21 | 2012-07-31 | Novartis Ag | Purinski derivati za uporabo kot agonisti receptorja adenozina A A |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| MX2009007476A (es) | 2007-01-10 | 2009-07-22 | Irm Llc | Compuestos y composiciones como inhibidores de proteasa activadora de canal. |
| CA2685546A1 (en) | 2007-05-07 | 2008-11-13 | Novartis Ag | Organic compounds |
| EP2231280B1 (en) | 2007-12-10 | 2016-08-10 | Novartis AG | Amiloride-like Pyrazine-carboxamides as ENaC blockers |
| ES2535736T3 (es) | 2008-06-10 | 2015-05-14 | Novartis Ag | Derivados de pirazina como bloqueadores de los canales de sodio epitelial |
| DK2379507T3 (da) | 2008-12-30 | 2014-01-27 | Pulmagen Therapeutics Inflammation Ltd | Sulfonamidforbindelser til behandling af åndedrætsforstyrrelser |
| HRP20121006T1 (hr) | 2009-01-29 | 2013-01-31 | Novartis Ag | Supstituirani benzimidazoli za lijeäśenje astrocitoma |
| JP2012530140A (ja) | 2009-06-16 | 2012-11-29 | メルク・シャープ・アンド・ドーム・コーポレーション | グルココルチコイド受容体アゴニストとしての新規［３，２−ｃ］ヘテロアリールステロイド、組成物およびこの使用 |
| US8389526B2 (en) | 2009-08-07 | 2013-03-05 | Novartis Ag | 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives |
| BR112012003262A8 (pt) | 2009-08-12 | 2016-05-17 | Novartis Ag | compostos de hidrazona heterocíclica e seus usos para tratar câncer e inflamação |
| ES2709108T3 (es) | 2009-08-17 | 2019-04-15 | Intellikine Llc | Compuestos heterocíclicos y usos de los mismos |
| EA201200318A1 (ru) | 2009-08-20 | 2012-09-28 | Новартис Аг | Гетероциклические оксимы |
| MX2012004792A (es) | 2009-10-22 | 2013-02-01 | Vertex Pharma | Composiciones para el tratamiento de fibrosis quistica y otras enfermedades cronicas. |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| US8637516B2 (en) | 2010-09-09 | 2014-01-28 | Irm Llc | Compounds and compositions as TRK inhibitors |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| JP2014505088A (ja) | 2011-02-10 | 2014-02-27 | ノバルティス アーゲー | Ｃ−ＭＥＴチロシンキナーゼ阻害剤としての［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン化合物 |
| EP2678016B1 (en) | 2011-02-23 | 2016-08-10 | Intellikine, LLC | Heterocyclic compounds and uses thereof |
| EA201391230A1 (ru) | 2011-02-25 | 2014-01-30 | АйАрЭм ЭлЭлСи | Соединения и композиции в качестве ингибиторов trk |
| US8883819B2 (en) | 2011-09-01 | 2014-11-11 | Irm Llc | Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension |
| WO2013038362A1 (en) | 2011-09-15 | 2013-03-21 | Novartis Ag | 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase |
| WO2013038373A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
| WO2013038381A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine/pyrazine amide derivatives |
| WO2013038390A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | N-substituted heterocyclyl carboxamides |
| CN103946221B (zh) | 2011-09-16 | 2016-08-03 | 诺华股份有限公司 | 用于治疗囊性纤维化的杂环化合物 |
| WO2013038378A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
| WO2013078440A2 (en) | 2011-11-23 | 2013-05-30 | Intellikine, Llc | Enhanced treatment regimens using mtor inhibitors |
| US8809340B2 (en) | 2012-03-19 | 2014-08-19 | Novartis Ag | Crystalline form |
| MX371119B (es) | 2012-04-03 | 2020-01-17 | Novartis Ag | Productos de combinacion con los inhibidores de cinasa de tirosina y su uso. |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| WO2014151147A1 (en) | 2013-03-15 | 2014-09-25 | Intellikine, Llc | Combination of kinase inhibitors and uses thereof |
| WO2014198909A1 (en) | 2013-06-14 | 2014-12-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Rac1 inhibitors for inducing bronchodilation |
| TW201605450A (zh) | 2013-12-03 | 2016-02-16 | 諾華公司 | Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途 |
| BR112016024533A8 (pt) | 2014-04-24 | 2021-03-30 | Novartis Ag | derivados de amino pirazina como inibidores de fosfatidilinositol 3-cinase ou sal, seu uso, e composição e combinação farmacêuticas |
| EA201692140A1 (ru) | 2014-04-24 | 2017-04-28 | Новартис Аг | Производные аминопиридина в качестве ингибиторов фосфатидилинозитол 3-киназы |
| CA2945257A1 (en) | 2014-04-24 | 2015-10-29 | Novartis Ag | Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| US10195208B2 (en) | 2014-07-31 | 2019-02-05 | Novartis Ag | Combination therapy |
| JP2022537667A (ja) | 2019-06-10 | 2022-08-29 | ノバルティス アーゲー | Ｃｆ、ｃｏｐｄ、及び気管支拡張症の治療のためのピリジン及びピラジン誘導体 |
| BR112022002569A2 (pt) | 2019-08-28 | 2022-07-19 | Novartis Ag | Derivados de 1,3-fenil heteroarila substituídos e seu uso no tratamento de doenças |
| TW202140550A (zh) | 2020-01-29 | 2021-11-01 | 瑞士商諾華公司 | 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3828080A (en) | 1972-01-20 | 1974-08-06 | Glaxo Lab Ltd | Androstane-17beta-carboxylic acids and processes for the preparation thereof |
| GB1438940A (en) * | 1972-07-19 | 1976-06-09 | Glaxo Lab Ltd | 17beta-haloalkoxycarbonyl-17alpha-oxysteroids |
| ATE8790T1 (de) * | 1981-02-02 | 1984-08-15 | Schering Corporation | Aromatische heterocyclische steroidester, verfahren zu ihrer herstellung und pharmazeutische zusammensetzungen, die sie enthalten. |
| NZ324373A (en) * | 1995-12-29 | 1999-10-28 | Glaxo Group Ltd | Lactone derivatives of 17-beta-carboxy, carbonyl-thio and amide androstane derivatives |
| GB0015876D0 (en) * | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| US6759398B2 (en) * | 2000-08-05 | 2004-07-06 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative |
| GB0019172D0 (en) * | 2000-08-05 | 2000-09-27 | Glaxo Group Ltd | Novel compounds |
| US6777400B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6787532B2 (en) * | 2000-08-05 | 2004-09-07 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivatives |
| US6858593B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6750210B2 (en) * | 2000-08-05 | 2004-06-15 | Smithkline Beecham Corporation | Formulation containing novel anti-inflammatory androstane derivative |
| US6777399B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6858596B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivative |
| EP1305329B2 (en) * | 2000-08-05 | 2015-03-18 | Glaxo Group Limited | 6.alpha.,9.alpha.-difluoro-17.alpha.-(2-furanylcarboxyl)oxy-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent |
| GB0103630D0 (en) * | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
| UA77656C2 (en) * | 2001-04-07 | 2007-01-15 | Glaxo Group Ltd | S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent |
| US20050175545A1 (en) * | 2002-02-04 | 2005-08-11 | Keith Biggadike | Formulation for inhalation comprising a glucocorticoid and a beta 2-adrenoreceptor agonist |
| AU2003244451A1 (en) * | 2002-02-04 | 2003-09-02 | Glaxo Group Limited | Amorphous fluticasone 2-furoate, pharmaceutical compositions thereof and its conversion to the crystalline unsolvated form |
| GB0316290D0 (en) * | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
-
2001
- 2001-10-20 GB GBGB0125259.2A patent/GB0125259D0/en not_active Ceased
-
2002
- 2002-10-17 WO PCT/EP2002/011634 patent/WO2003035668A2/en not_active Ceased
- 2002-10-17 EP EP02785235A patent/EP1444248B1/en not_active Expired - Lifetime
- 2002-10-17 JP JP2003538181A patent/JP4495456B2/ja not_active Expired - Lifetime
- 2002-10-17 AU AU2002350561A patent/AU2002350561A1/en not_active Abandoned
- 2002-10-17 ES ES02785235T patent/ES2304457T3/es not_active Expired - Lifetime
- 2002-10-17 AT AT02785235T patent/ATE393771T1/de not_active IP Right Cessation
- 2002-10-17 DE DE60226334T patent/DE60226334T2/de not_active Expired - Lifetime
- 2002-10-17 US US10/492,813 patent/US7405206B2/en not_active Expired - Lifetime
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