JP2005500290A5 - - Google Patents
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- 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 (https=) | 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 (https=) |
| EP (1) | EP1395604B1 (https=) |
| JP (1) | JP2005500290A (https=) |
| AR (1) | AR034475A1 (https=) |
| AT (1) | ATE399174T1 (https=) |
| DE (1) | DE60227254D1 (https=) |
| ES (1) | ES2307751T3 (https=) |
| WO (1) | WO2002100879A1 (https=) |
Families Citing this family (113)
| 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 |
| US6787532B2 (en) | 2000-08-05 | 2004-09-07 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivatives |
| SI1775305T1 (sl) | 2000-08-05 | 2015-01-30 | Glaxo Group Limited | S-fluorometil ester 6alfa,9alfa-difluoro-17alfa-((2-furanilkarboksil)oksi)- 11beta-hidroksi-16alfa-metil-3-okso-androst-1,4-dien-17-karbotiojske kisline kot protivnetno sredstvo |
| US6858593B2 (en) | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| GB0019172D0 (en) | 2000-08-05 | 2000-09-27 | Glaxo Group Ltd | Novel 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 |
| KR100831534B1 (ko) | 2001-04-30 | 2008-05-22 | 글락소 그룹 리미티드 | 17.알파 위치에 시클릭 에스테르기를 지닌 항염증성의안드로스탄의 17.베타.-카르보티오에이트 에스테르 유도체 |
| 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 |
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| GB0424284D0 (en) | 2004-11-02 | 2004-12-01 | Novartis Ag | Organic compounds |
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| MX2008013411A (es) | 2006-04-20 | 2008-11-04 | Glaxo Group Ltd | Nuevos compuestos. |
| PT2322525E (pt) | 2006-04-21 | 2013-12-26 | Novartis Ag | Derivados de purina para utilização como agonistas do recetor de adenosina a2a |
| GB0611587D0 (en) | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
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| RS51644B (sr) | 2007-01-10 | 2011-10-31 | Irm Llc. | Jedinjenja i preparati kao inhibitori kanal aktivirajuće proteaze |
| MX2009008493A (es) | 2007-02-09 | 2009-08-20 | Irm Llc | Compuestos y composiciones como inhibidores de la proteasa activadora de canal. |
| PE20081889A1 (es) | 2007-03-23 | 2009-03-05 | Smithkline Beecham Corp | Indol carboxamidas como inhibidores de ikk2 |
| CN101687851B (zh) | 2007-05-07 | 2013-02-27 | 诺瓦提斯公司 | 有机化合物 |
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| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| CA2954862A1 (en) | 2014-07-31 | 2016-02-04 | Novartis Ag | Combination therapy |
| GB201602527D0 (en) | 2016-02-12 | 2016-03-30 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| US20190161480A1 (en) | 2016-08-08 | 2019-05-30 | 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 |
| AU2020290094B2 (en) | 2019-06-10 | 2024-01-18 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF, COPD, and bronchiectasis |
| 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 |
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2002
- 2002-06-11 ES ES02730498T patent/ES2307751T3/es not_active Expired - Lifetime
- 2002-06-11 DE DE60227254T patent/DE60227254D1/de not_active Expired - Fee Related
- 2002-06-11 WO PCT/GB2002/002686 patent/WO2002100879A1/en not_active Ceased
- 2002-06-11 JP JP2003503645A patent/JP2005500290A/ja active Pending
- 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 EP EP02730498A patent/EP1395604B1/en not_active Expired - Lifetime
- 2002-06-12 AR ARP020102212A patent/AR034475A1/es not_active Application Discontinuation
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