JP2005500290A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005500290A5 JP2005500290A5 JP2003503645A JP2003503645A JP2005500290A5 JP 2005500290 A5 JP2005500290 A5 JP 2005500290A5 JP 2003503645 A JP2003503645 A JP 2003503645A JP 2003503645 A JP2003503645 A JP 2003503645A JP 2005500290 A5 JP2005500290 A5 JP 2005500290A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- hydroxy
- oxy
- androst
- difluoro
- 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
- 150000001875 compounds Chemical class 0.000 claims 23
- 239000002253 acid Substances 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 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 2-methyl-1,3-dioxolan-2-ylcarbonyl Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 2
- 239000000048 adrenergic agonist Substances 0.000 claims 2
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 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
- FLOJNXXFMHCMMR-UHFFFAOYSA-N 1,3-dithiolanyl Chemical group [CH]1SCCS1 FLOJNXXFMHCMMR-UHFFFAOYSA-N 0.000 claims 1
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 230000002152 alkylating effect Effects 0.000 claims 1
- 230000029936 alkylation Effects 0.000 claims 1
- 238000005804 alkylation reaction Methods 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000005997 bromomethyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 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 class F[C]Cl KYKAJFCTULSVSH-UHFFFAOYSA-N 0.000 claims 1
- 125000004218 chloromethyl group Chemical group [H]C([H])(Cl)* 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 239000008249 pharmaceutical aerosol Substances 0.000 claims 1
- 239000003380 propellant Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000002053 thietanyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0114338A GB0114338D0 (en) | 2001-06-12 | 2001-06-12 | Novel compounds |
| GB0202636A GB0202636D0 (en) | 2002-02-05 | 2002-02-05 | Novel compounds |
| PCT/GB2002/002686 WO2002100879A1 (en) | 2001-06-12 | 2002-06-11 | Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005500290A JP2005500290A (ja) | 2005-01-06 |
| JP2005500290A5 true JP2005500290A5 (enExample) | 2006-01-05 |
Family
ID=26246181
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003503645A Pending JP2005500290A (ja) | 2001-06-12 | 2002-06-11 | 抗炎症性の、１７β−カルボチオアートアンドロスタン誘導体である１７α複素環エステル |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20040248867A1 (enExample) |
| EP (1) | EP1395604B1 (enExample) |
| JP (1) | JP2005500290A (enExample) |
| AR (1) | AR034475A1 (enExample) |
| AT (1) | ATE399174T1 (enExample) |
| DE (1) | DE60227254D1 (enExample) |
| ES (1) | ES2307751T3 (enExample) |
| WO (1) | WO2002100879A1 (enExample) |
Families Citing this family (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2417826A1 (en) | 2000-08-05 | 2002-02-14 | Glaxo Group Limited | 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents |
| US6787532B2 (en) | 2000-08-05 | 2004-09-07 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivatives |
| 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 |
| 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 |
| PL366937A1 (en) | 2001-04-30 | 2005-02-07 | Glaxo Group Limited | Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha |
| GB0127160D0 (en) * | 2001-11-12 | 2002-01-02 | Glaxo Group Ltd | Novel compounds |
| WO2003042229A1 (en) * | 2001-11-12 | 2003-05-22 | Glaxo Group Limited | Non-aromatic heterocyclic esters of furan-2-one-esters of 17.beta.-carboxyl or 17.beta.-carbothio glucocorticoids |
| GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
| TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic 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 |
| EP1924553A1 (en) | 2005-08-08 | 2008-05-28 | Argenta Discovery Limited | Bicyclo[2.2.]hept-7-ylamine derivatives and their uses |
| GB0516313D0 (en) | 2005-08-08 | 2005-09-14 | Argenta Discovery Ltd | Azole derivatives and their uses |
| CA2625664C (en) | 2005-10-21 | 2016-01-05 | Novartis Ag | Human antibodies against il13 and therapeutic uses |
| GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| GB0601951D0 (en) | 2006-01-31 | 2006-03-15 | Novartis Ag | Organic compounds |
| EA200801997A1 (ru) | 2006-04-20 | 2009-04-28 | Глаксо Груп Лимитед | Новые соединения |
| PE20080361A1 (es) | 2006-04-21 | 2008-06-03 | Novartis Ag | Compuestos derivados de purina como activadores del receptor de adenosina a2a |
| GB0611587D0 (en) | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
| AU2007302263A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as P13K lipid kinase inhibitors |
| EP2279777A2 (en) | 2007-01-10 | 2011-02-02 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| EA200901082A1 (ru) | 2007-02-09 | 2010-02-26 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
| PE20081889A1 (es) | 2007-03-23 | 2009-03-05 | Smithkline Beecham Corp | Indol carboxamidas como inhibidores de ikk2 |
| AU2008248598B2 (en) | 2007-05-07 | 2011-11-17 | Novartis Ag | Organic compounds |
| CN101939054B (zh) | 2007-12-10 | 2014-10-29 | 诺华股份有限公司 | 有机化合物 |
| JP5584138B2 (ja) | 2008-01-11 | 2014-09-03 | ノバルティス アーゲー | キナーゼ阻害剤としてのピリミジン類 |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| WO2010068311A1 (en) | 2008-05-23 | 2010-06-17 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein inhibitor |
| WO2009147187A1 (en) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases |
| ES2535736T3 (es) | 2008-06-10 | 2015-05-14 | Novartis Ag | Derivados de pirazina como bloqueadores de los canales de sodio epitelial |
| US8236786B2 (en) | 2008-08-07 | 2012-08-07 | Pulmagen Therapeutics (Inflammation) Limited | Respiratory disease treatment |
| PL2379507T3 (pl) | 2008-12-30 | 2014-03-31 | Pulmagen Therapeutics Inflammation Ltd | Związki sulfonamidu do leczenia zaburzeń układu oddechowego |
| SI2391366T1 (sl) | 2009-01-29 | 2013-01-31 | Novartis Ag | Substituirani benzimidazoli za zdravljenje astrocitomov |
| ES2542551T3 (es) | 2009-03-09 | 2015-08-06 | Glaxo Group Limited | 4-Oxadiazol-2-il-indazoles como inhibidores de PI3 cinasas |
| WO2010102968A1 (en) | 2009-03-10 | 2010-09-16 | Glaxo Group Limited | Indole derivatives as ikk2 inhibitors |
| WO2010106016A1 (en) | 2009-03-17 | 2010-09-23 | Glaxo Group Limited | Pyrimidine derivatives used as itk inhibitors |
| US20120035247A1 (en) | 2009-03-19 | 2012-02-09 | Merck Sharp & Dohme Corp. | RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 6 (STAT6) Gene Expression Using Short Interfering Nucleic Acid (siNA) |
| US20120029054A1 (en) | 2009-03-19 | 2012-02-02 | Merck Sharp & Dohme Corp. | RNA Interference Mediated Inhibition of GATA Binding Protein 3 (GATA3) Gene Expression Using Short Intefering Nucleic Acid (siNA) |
| JP2012520683A (ja) | 2009-03-19 | 2012-09-10 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸（ｓｉＮＡ）を用いた結合組織増殖因子（ＣＴＧＦ）遺伝子発現のＲＮＡ干渉媒介性阻害 |
| CN102439151A (zh) | 2009-03-19 | 2012-05-02 | 默沙东公司 | 使用短干扰核酸（siNA）的RNA干扰介导的BTB和CNC同系物1，碱性亮氨酸拉链转录因子1（Bach1）基因表达的抑制 |
| EP2411018A2 (en) | 2009-03-27 | 2012-02-01 | Merck Sharp&Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF THE NERVE GROWTH FACTOR BETA CHAIN (NGFß) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (SINA) |
| JP2012521763A (ja) | 2009-03-27 | 2012-09-20 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸（ｓｉＮＡ）を用いたシグナル伝達性転写因子１（ＳＴＡＴ１）遺伝子発現のＲＮＡ干渉媒介性阻害 |
| US20120004282A1 (en) | 2009-03-27 | 2012-01-05 | Merck Sharp & Dohme Corp, | RNA Interference Mediated Inhibition of the Intercellular Adhesion Molecule 1 (ICAM-1) Gene Expression Using Short Interfering Nucleic Acid (siNA) |
| US20120022143A1 (en) | 2009-03-27 | 2012-01-26 | Merck Sharp & Dohme Corp | RNA Interference Mediated Inhibition of the Thymic Stromal Lymphopoietin (TSLP) Gene Expression Using Short Interfering Nucliec Acid (siNA) |
| US20120010272A1 (en) | 2009-03-27 | 2012-01-12 | Merck Sharp & Dohme Corp. | RNA Interference Mediated Inhibition of Apoptosis Signal-Regulating Kinase 1 (ASK1) Gene Expression Using Short Interfering Nucleic Acid (siNA) |
| WO2010122088A1 (en) | 2009-04-24 | 2010-10-28 | Glaxo Group Limited | Pyrazole and triazole carboxamides as crac channel inhibitors |
| AR076373A1 (es) | 2009-04-24 | 2011-06-08 | Glaxo Group Ltd | N-pirazolil carboxamidas como inhibidores de canales de calcio |
| AU2010243613B2 (en) | 2009-04-30 | 2015-05-07 | Glaxo Group Limited | Oxazole substituted indazoles as PI3-kinase inhibitors |
| WO2010150014A1 (en) | 2009-06-24 | 2010-12-29 | Pulmagen Therapeutics (Inflammation) Limited | 5r- 5 -deuterated glitazones for respiratory disease treatment |
| US8389526B2 (en) | 2009-08-07 | 2013-03-05 | Novartis Ag | 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives |
| KR20120089643A (ko) | 2009-08-12 | 2012-08-13 | 노파르티스 아게 | 헤테로시클릭 히드라존 화합물, 및 암 및 염증을 치료하기 위한 그의 용도 |
| US9085560B2 (en) | 2009-08-17 | 2015-07-21 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| JP5775871B2 (ja) | 2009-08-20 | 2015-09-09 | ノバルティス アーゲー | ヘテロ環式オキシム化合物 |
| MX2012004792A (es) | 2009-10-22 | 2013-02-01 | Vertex Pharma | Composiciones para el tratamiento de fibrosis quistica y otras enfermedades cronicas. |
| JP2013512879A (ja) | 2009-12-03 | 2013-04-18 | グラクソ グループ リミテッド | Ｐｉ３キナーゼの阻害剤としてのベンズピラゾール誘導体 |
| US20120238559A1 (en) | 2009-12-03 | 2012-09-20 | Glaxo Group Limited | Novel compounds |
| JP2013512880A (ja) | 2009-12-03 | 2013-04-18 | グラクソ グループ リミテッド | Ｐｉ３−キナーゼ阻害剤としてのインダゾール誘導体 |
| WO2011098746A1 (en) | 2010-02-09 | 2011-08-18 | Pulmagen Therapeutics (Inflammation) Limited | Crystalline acid addition salts of ( 5r) -enanti0mer of pioglitazone |
| GB201002224D0 (en) | 2010-02-10 | 2010-03-31 | Argenta Therapeutics Ltd | Respiratory disease treatment |
| GB201002243D0 (en) | 2010-02-10 | 2010-03-31 | Argenta Therapeutics Ltd | Respiratory disease treatment |
| WO2011110575A1 (en) | 2010-03-11 | 2011-09-15 | Glaxo Group Limited | Derivatives of 2-[2-(benzo- or pyrido-) thiazolylamino]-6-aminopyridine, useful in the treatment of respiratoric, allergic or inflammatory diseases |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| GB201007203D0 (en) | 2010-04-29 | 2010-06-16 | Glaxo Group Ltd | Novel compounds |
| EP2613781B1 (en) | 2010-09-08 | 2016-08-24 | GlaxoSmithKline Intellectual Property Development Limited | Indazole derivatives for use in the treatment of influenza virus infection |
| PL2614058T3 (pl) | 2010-09-08 | 2015-12-31 | Glaxosmithkline Ip Dev Ltd | Polimorfy i sole n-[5-[4-(5-{[(2r,6s)-2,6-dimetylo-4-morfolinylo]-metylo}-1,3-oksazol-2-ilo)-1h-indazol-6-ilo]-2-(metyloksy)-3-pirydynylo]metanosulfonamidu |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| WO2012035055A1 (en) | 2010-09-17 | 2012-03-22 | Glaxo Group Limited | Novel compounds |
| EP2630127A1 (en) | 2010-10-21 | 2013-08-28 | Glaxo Group Limited | Pyrazole compounds acting against allergic, inflammatory and immune disorders |
| JP5795643B2 (ja) | 2010-10-21 | 2015-10-14 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ | アレルギー性状態、免疫性状態及び炎症性状態に作用するピラゾール化合物 |
| GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
| EP2673277A1 (en) | 2011-02-10 | 2013-12-18 | Novartis AG | [1, 2, 4]triazolo [4, 3 -b]pyridazine compounds as inhibitors of the c-met tyrosine kinase |
| JP5808826B2 (ja) | 2011-02-23 | 2015-11-10 | インテリカイン， エルエルシー | 複素環化合物およびその使用 |
| CA2828219A1 (en) | 2011-02-25 | 2012-08-30 | Irm Llc | Pyrazolo [1,5-a] pyridines as trk inhibitors |
| WO2012123312A1 (en) | 2011-03-11 | 2012-09-20 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| GB201104153D0 (en) | 2011-03-11 | 2011-04-27 | Glaxo Group Ltd | Novel compounds |
| US8883819B2 (en) | 2011-09-01 | 2014-11-11 | Irm Llc | Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension |
| US9062045B2 (en) | 2011-09-15 | 2015-06-23 | Novartis Ag | Triazolopyridine compounds |
| ES2558457T3 (es) | 2011-09-16 | 2016-02-04 | Novartis Ag | Compuestos heterocíclicos para el tratamiento de fibrosis quística |
| WO2013038378A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
| EP2755652B1 (en) | 2011-09-16 | 2021-06-02 | Novartis AG | N-substituted heterocyclyl carboxamides |
| 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 |
| US20130209543A1 (en) | 2011-11-23 | 2013-08-15 | Intellikine Llc | Enhanced treatment regimens using mtor inhibitors |
| US8809340B2 (en) | 2012-03-19 | 2014-08-19 | Novartis Ag | Crystalline form |
| ES2894830T3 (es) | 2012-04-03 | 2022-02-16 | Novartis Ag | Productos combinados con inhibidores de tirosina·cinasa 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 |
| US10155001B2 (en) | 2013-06-14 | 2018-12-18 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | RAC1 inhibitors for inducing bronchodilation |
| AU2014336251A1 (en) | 2013-10-17 | 2016-04-14 | Glaxosmithkline Intellectual Property Development Limited | PI3K inhibitor for treatment of respiratory disease |
| CN105658218A (zh) | 2013-10-17 | 2016-06-08 | 葛兰素史克知识产权开发有限公司 | 用于治疗呼吸疾病的pi3k抑制剂 |
| WO2015084804A1 (en) | 2013-12-03 | 2015-06-11 | Novartis Ag | Combination of mdm2 inhibitor and braf inhibitor and their use |
| KR20160145780A (ko) | 2014-04-24 | 2016-12-20 | 노파르티스 아게 | 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피리딘 유도체 |
| WO2015162461A1 (en) | 2014-04-24 | 2015-10-29 | Novartis Ag | Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
| 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 |
| CN107072976A (zh) | 2014-05-12 | 2017-08-18 | 葛兰素史克知识产权第二有限公司 | 用于治疗传染性疾病的包含Danirixin的药物组合物 |
| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| KR20170036037A (ko) | 2014-07-31 | 2017-03-31 | 노파르티스 아게 | 조합 요법 |
| GB201602527D0 (en) | 2016-02-12 | 2016-03-30 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| EP3497100A1 (en) | 2016-08-08 | 2019-06-19 | GlaxoSmithKline Intellectual Property Development Limited | Chemical compounds |
| GB201706102D0 (en) | 2017-04-18 | 2017-05-31 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| GB201712081D0 (en) | 2017-07-27 | 2017-09-13 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| KR20220019015A (ko) | 2019-06-10 | 2022-02-15 | 노파르티스 아게 | Cf, copd, 및 기관지확장증 치료를 위한 피리딘 및 피라진 유도체 |
| AU2020338971B2 (en) | 2019-08-28 | 2023-11-23 | Novartis Ag | Substituted 1,3-phenyl heteroaryl derivatives and their use in the treatment of disease |
| 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 |
| WO2021191875A1 (en) | 2020-03-26 | 2021-09-30 | Glaxosmithkline Intellectual Property Development Limited | Cathepsin inhibitors for preventing or treating viral infections |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2837464A (en) * | 1955-01-11 | 1958-06-03 | Schering Corp | Process for production of dienes by corynebacteria |
| US3067197A (en) * | 1961-04-26 | 1962-12-04 | Pfizer & Co C | 11-oxygenated 6alpha-fluoro-16-methylene-delta-pregnenes and derivatives |
| GB1047518A (en) * | 1963-06-11 | 1966-11-02 | Glaxo Lab Ltd | 17ª-monoesters of 11,17,21-trihydroxy steroid compounds |
| GB1158492A (en) * | 1966-02-09 | 1969-07-16 | Boots Pure Drug Co Ltd | Improvements in Acylated Steroids |
| US3639434A (en) * | 1967-02-02 | 1972-02-01 | Boots Pure Drug Co Ltd | 17-acyloxysteroids and their manufacture |
| GB1227992A (enExample) * | 1968-01-23 | 1971-04-15 | Koninklijke Gist Spiritus | |
| IT1034011B (it) * | 1969-06-26 | 1979-09-10 | Vister Vismara Terapeutici S P | Processo per la prapratzione di 17 monoesteri di 17 a 21 diossisteroidi per idrolisi die corpispondenti 17 21 ortoesteri ciclici a ph control lato |
| US3828080A (en) * | 1972-01-20 | 1974-08-06 | Glaxo Lab Ltd | Androstane-17beta-carboxylic acids and processes for the preparation thereof |
| US4263289A (en) * | 1978-04-05 | 1981-04-21 | Syntex (U.S.A.) Inc. | Thio etianic acid derivatives |
| US4188385A (en) * | 1978-04-05 | 1980-02-12 | Syntex (U.S.A.) Inc. | Thioetianic acid derivatives |
| ZA81976B (en) * | 1980-02-15 | 1982-07-28 | Glaxo Group Ltd | Androstane carbothioates |
| US4996335A (en) * | 1980-07-10 | 1991-02-26 | Nicholas S. Bodor | Soft steroids having anti-inflammatory activity |
| ATE8790T1 (de) * | 1981-02-02 | 1984-08-15 | Schering Corporation | Aromatische heterocyclische steroidester, verfahren zu ihrer herstellung und pharmazeutische zusammensetzungen, die sie enthalten. |
| US4994439A (en) * | 1989-01-19 | 1991-02-19 | California Biotechnology Inc. | Transmembrane formulations for drug administration |
| US5202316A (en) * | 1989-03-22 | 1993-04-13 | Roussel Uclaf | N,N,N',N'-6-(1-piperazinyl)-2,5-pyridinediamines |
| FR2644788B1 (fr) * | 1989-03-22 | 1995-02-03 | Roussel Uclaf | Nouveaux steroides 3-ceto comportant une chaine en 17 amino-substituee, leur procede de preparation et les intermediaires de ce procede, leur application comme medicaments et les compositions pharmaceutiques les contenant |
| JPH07116215B2 (ja) * | 1989-04-19 | 1995-12-13 | エスエス製薬株式会社 | 新規なステロイド化合物 |
| DE4025342A1 (de) * | 1990-08-10 | 1992-02-13 | Hoechst Ag | In 17-stellung substituierte corticoid-17-alkylcarbonate, verfahren zu deren herstellung und diese enthaltende arzneimittel |
| US6127353A (en) * | 1991-09-06 | 2000-10-03 | Schering Corporation | Mometasone furoate monohydrate, process for making same and pharmaceutical compositions |
| US5658549A (en) * | 1991-12-12 | 1997-08-19 | Glaxo Group Limited | Aerosol formulations containing propellant 134a and fluticasone propionate |
| DE4328819A1 (de) * | 1993-08-27 | 1995-03-02 | Hoechst Ag | Corticosteroid-17-alkylcarbonat-21/0/-Carbonsäure- und Kohlensäureester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel |
| DE4333920A1 (de) * | 1993-10-05 | 1995-04-13 | Hoechst Ag | Corticoid-17,21-dicarbonsäureester sowie Corticosteroid-17-carbonsäureester-21-kohlensäureester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel |
| US5420120A (en) * | 1993-12-17 | 1995-05-30 | Alcon Laboratories, Inc. | Anti-inflammatory glucocorticoid compounds for topical ophthalmic use |
| US5837699A (en) * | 1994-01-27 | 1998-11-17 | Schering Corporation | Use of mometasone furoate for treating upper airway passage diseases |
| GB9419536D0 (en) * | 1994-09-28 | 1994-11-16 | Glaxo Inc | Medicaments |
| US5707984A (en) * | 1995-12-08 | 1998-01-13 | G. D. Searle & Co. | Steroid nitrite/nitrate ester derivatives useful as anti-inflammatory drugs |
| SI0876392T1 (en) * | 1995-12-29 | 2000-12-31 | Glaxo Group Limited | Lactone derivatives of 17.beta.-carboxy, carbothio and amide androstane derivatives |
| US5981517A (en) * | 1996-05-09 | 1999-11-09 | Soft Drugs, Inc. | Androstene derivatives |
| US5972920A (en) * | 1998-02-12 | 1999-10-26 | Dermalogix Partners, Inc. | Formulation containing a carrier, active ingredient, and surfactant for treating skin disorders |
| US6136294C1 (en) * | 1998-09-22 | 2002-09-24 | Aeropharm Technology Inc | Amino acid stabilized medical aerosol formulation |
| US6261539B1 (en) * | 1998-12-10 | 2001-07-17 | Akwete Adjei | Medicinal aerosol formulation |
| US6395300B1 (en) * | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| US20020081266A1 (en) * | 1999-08-20 | 2002-06-27 | Norton Healthcare Ltd. | Spray dried powders for pulmonary or nasal administration |
| GB0015876D0 (en) * | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| US6858596B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivative |
| CA2417826A1 (en) * | 2000-08-05 | 2002-02-14 | Glaxo Group Limited | 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents |
| US6750210B2 (en) * | 2000-08-05 | 2004-06-15 | Smithkline Beecham Corporation | Formulation containing novel anti-inflammatory androstane derivative |
| US6787532B2 (en) * | 2000-08-05 | 2004-09-07 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivatives |
| US6777400B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6759398B2 (en) * | 2000-08-05 | 2004-07-06 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative |
| US6858593B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| CN101518537A (zh) * | 2000-12-22 | 2009-09-02 | 日本新药株式会社 | 炎症性呼吸道疾病的预防/治疗剂 |
| 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 |
| US20030018019A1 (en) * | 2001-06-23 | 2003-01-23 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics |
| JP3691459B2 (ja) * | 2002-06-14 | 2005-09-07 | 久光メディカル株式会社 | 粉末状吸入剤組成物 |
| US7244742B2 (en) * | 2002-08-17 | 2007-07-17 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Pharmaceutical compositions for inhalation containing an anticholinergic, corticosteroid and betamimetic |
-
2002
- 2002-06-11 EP EP02730498A patent/EP1395604B1/en not_active Expired - Lifetime
- 2002-06-11 JP JP2003503645A patent/JP2005500290A/ja active Pending
- 2002-06-11 ES ES02730498T patent/ES2307751T3/es not_active Expired - Lifetime
- 2002-06-11 AT AT02730498T patent/ATE399174T1/de not_active IP Right Cessation
- 2002-06-11 US US10/480,071 patent/US20040248867A1/en not_active Abandoned
- 2002-06-11 WO PCT/GB2002/002686 patent/WO2002100879A1/en not_active Ceased
- 2002-06-11 DE DE60227254T patent/DE60227254D1/de not_active Expired - Fee Related
- 2002-06-12 AR ARP020102212A patent/AR034475A1/es not_active Application Discontinuation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005500290A5 (enExample) | ||
| JP3396888B2 (ja) | 医薬組成物 | |
| RU2005141064A (ru) | Специфическое глюкокортикостероидное соединение, обладающее противовоспалительной активностью | |
| JP2005500290A (ja) | 抗炎症性の、１７β−カルボチオアートアンドロスタン誘導体である１７α複素環エステル | |
| ES2425739T3 (es) | Sorafenib-tosilato para el tratamiento de enfermedades caracterizadas por angiogénesis anormal | |
| KR100827379B1 (ko) | 항염증제로서의 6.알파., 9.알파.-디플루오로-17.알파.-'(2-푸라닐카르복실)옥시-11.베타.-히드록시-16.알파.-메틸-3-옥소-안드로스트-1,4-디엔-17-카르보티오산 ｓ-플루오로메틸 에스테르 | |
| AU767349B2 (en) | Purine derivatives inhibitors of tyrosine protein kinase syk | |
| TWI843372B (zh) | 用於降解突變kras蛋白之化合物及其應用 | |
| EP2456781B1 (de) | 17-hydroxy-17-pentafluorethyl-estra-4,9 (10)-dien-11-acyloxyalkylenphenyl-derivate, verfahren zu ihrer herstellung und ihre verwendung zur behandlung von krankheiten | |
| JP2008519865A6 (ja) | 純粋な臭化ロクロニウム | |
| JP6196302B2 (ja) | ３−置換エストラ−１，３，５（１０），１６−テトラエン誘導体、その調製法、これらを含む医薬製剤および医薬を調製するためのその使用 | |
| ATE346058T1 (de) | Glucocorticoid mimetika, verfahren zu ihrer herstellung, pharmazeutische formulierungen sie enthaltend und verwendungen davon | |
| JP2006506318A (ja) | ハロアセトアミド若しくはアジ化物置換化合物及びその使用方法 | |
| RU2005106846A (ru) | Производные бензотиазола, характеризующиеся агонистической активностью к бета-2-адренорецепторам | |
| JP2004531523A5 (enExample) | ||
| WO1991019713A1 (fr) | Derive de nucleoside de pyrimidine | |
| US6319912B1 (en) | Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides | |
| RU2007108863A (ru) | Производные пиразола для лечения состояний, опосредованных активацией рецептора аденозина а2в или а3 | |
| EP2785707A1 (en) | Novel 2h-indazoles as ep2 receptor antagonists | |
| JP2009508808A (ja) | プロゲステロンレセプターモジュレータの使用 | |
| CN110461837A (zh) | 新型吡咯并吡啶衍生物、其制备方法及用途 | |
| HU177333B (en) | Process for producing gona-4,9-bracket-10-bracket closeddienes | |
| JP6407415B2 (ja) | ３−窒素または硫黄置換エストラ−１，３，５（１０），１６−テトラエンａｋｒ１ｃ３阻害剤 | |
| RU2289582C2 (ru) | Соединение карбапенема | |
| JP2000026494A5 (enExample) |