JP2011507836A5 - - Google Patents
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- Publication number
- JP2011507836A5 JP2011507836A5 JP2010539381A JP2010539381A JP2011507836A5 JP 2011507836 A5 JP2011507836 A5 JP 2011507836A5 JP 2010539381 A JP2010539381 A JP 2010539381A JP 2010539381 A JP2010539381 A JP 2010539381A JP 2011507836 A5 JP2011507836 A5 JP 2011507836A5
- Authority
- JP
- Japan
- Prior art keywords
- dioxolo
- naphtho
- cyclopenta
- hydroxy
- dodecahydro
- 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 19
- -1 1,3-dioxolanyl group Chemical group 0.000 claims 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000006699 (C1-C3) hydroxyalkyl group Chemical group 0.000 claims 3
- IQPXEDXRDNPCEY-UHFFFAOYSA-N C1=CC2=CC3=NN=CC3=CC2=C2C1=C1C=CC=C1C=C2 Chemical compound C1=CC2=CC3=NN=CC3=CC2=C2C1=C1C=CC=C1C=C2 IQPXEDXRDNPCEY-UHFFFAOYSA-N 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 102000009410 Chemokine receptor Human genes 0.000 claims 1
- 108050000299 Chemokine receptor Proteins 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000000048 adrenergic agonist Substances 0.000 claims 1
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 1
- 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229910052731 fluorine Chemical group 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 239000003862 glucocorticoid Substances 0.000 claims 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 claims 1
- WRSXUNSJGJUKHE-UHFFFAOYSA-N indazole Chemical compound C1=CC=C[C]2C=NN=C21 WRSXUNSJGJUKHE-UHFFFAOYSA-N 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 229940037128 systemic glucocorticoids Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1540407P | 2007-12-20 | 2007-12-20 | |
| PCT/SE2008/051489 WO2009082342A1 (en) | 2007-12-20 | 2008-12-18 | Steroid derivatives acting as glucocorticosteroid receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011507836A JP2011507836A (ja) | 2011-03-10 |
| JP2011507836A5 true JP2011507836A5 (enExample) | 2012-01-26 |
Family
ID=40801455
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010539381A Pending JP2011507836A (ja) | 2007-12-20 | 2008-12-18 | グルココルチコステロイド受容体アゴニストとして作用するステロイド誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20110160167A1 (enExample) |
| EP (1) | EP2235037A1 (enExample) |
| JP (1) | JP2011507836A (enExample) |
| KR (1) | KR20100102121A (enExample) |
| CN (1) | CN101945885A (enExample) |
| AU (1) | AU2008341590A1 (enExample) |
| BR (1) | BRPI0821139A2 (enExample) |
| CA (1) | CA2707618A1 (enExample) |
| RU (1) | RU2010124799A (enExample) |
| WO (1) | WO2009082342A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2207788A1 (en) | 2007-10-04 | 2010-07-21 | AstraZeneca AB | Steroidal [3, 2-c]pyrazole compounds, with glucocorticoid activity |
| UY32520A (es) | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| EP3407916B1 (en) | 2016-01-29 | 2023-12-20 | Merck Sharp & Dohme LLC | Phosphonate linkers and their use to facilitate cellular retention of compounds |
| WO2018071736A1 (en) * | 2016-10-14 | 2018-04-19 | Van Andel Research Institute | Structures and mechanism for the design of highly potent glucocorticoids |
| CN110105420A (zh) * | 2019-06-04 | 2019-08-09 | 博诺康源(北京)药业科技有限公司 | 一种布地奈德杂质ep-zg的合成方法 |
| WO2025231369A1 (en) * | 2024-05-03 | 2025-11-06 | Emory University | Veragranine analogs, pharmaceutical compositions, and uses in managing pain or inflammatory conditions |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3129218A (en) * | 1961-11-01 | 1964-04-14 | Merck & Co Inc | 2-alkoxymethylene steroids of the androstane and pregnane series |
| US3072639A (en) * | 1962-03-05 | 1963-01-08 | Merck & Co Inc | 16-oxygenated-4-pregneno-[3, 2-c] pyrazoles and process of preparing them |
| US3364203A (en) * | 1965-09-09 | 1968-01-16 | Syntex Corp | 6, 7-methylene and 6, 7-halomethylene pyrazole pregnanes and processes for their preparation |
| US3471477A (en) * | 1967-10-18 | 1969-10-07 | Syntex Corp | 6-gem-difluoro (3,2-c) and (2,3-d) pyrazole steroids |
| DE2735110A1 (de) * | 1977-08-04 | 1979-02-15 | Hoechst Ag | Corticoid-17-alkylcarbonate und verfahren zu ihrer herstellung |
| DE2817988A1 (de) * | 1978-04-25 | 1979-11-08 | Hoechst Ag | Corticoid 17-alkylcarbonate und verfahren zu deren herstellung |
| SE8306370D0 (sv) * | 1983-11-18 | 1983-11-18 | Draco Ab | Novel androstane-17beta-carboxylic acid esters, a process and intermediates for their preparation, compositions and method for the treatment of inflammatory conditions |
| DE3540537A1 (de) * | 1985-11-15 | 1987-05-21 | Klaus Kurt Koelzer | Verstaerkungsmaterial |
| WO2005063777A1 (en) * | 2003-12-23 | 2005-07-14 | Corus Pharma | Benzylphosphate and substituted benzylphosphate prodrugs for the treatment of pulmonary inflammation |
| EP2207788A1 (en) * | 2007-10-04 | 2010-07-21 | AstraZeneca AB | Steroidal [3, 2-c]pyrazole compounds, with glucocorticoid activity |
| UY32521A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Combinación para emplear en el tratamiento de enfermedades respiratorias |
| UY32523A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| UY32520A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| UY32525A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
-
2008
- 2008-12-18 CA CA2707618A patent/CA2707618A1/en not_active Abandoned
- 2008-12-18 CN CN2008801268528A patent/CN101945885A/zh active Pending
- 2008-12-18 RU RU2010124799/04A patent/RU2010124799A/ru unknown
- 2008-12-18 KR KR1020107013463A patent/KR20100102121A/ko not_active Withdrawn
- 2008-12-18 US US12/809,131 patent/US20110160167A1/en not_active Abandoned
- 2008-12-18 WO PCT/SE2008/051489 patent/WO2009082342A1/en not_active Ceased
- 2008-12-18 BR BRPI0821139-6A patent/BRPI0821139A2/pt not_active IP Right Cessation
- 2008-12-18 EP EP08863416A patent/EP2235037A1/en not_active Withdrawn
- 2008-12-18 AU AU2008341590A patent/AU2008341590A1/en not_active Abandoned
- 2008-12-18 JP JP2010539381A patent/JP2011507836A/ja active Pending
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