RU2010124799A - Производные стероидов, действующие в качестве агонистов глюкокортикостероидных рецепторов - Google Patents
Производные стероидов, действующие в качестве агонистов глюкокортикостероидных рецепторов Download PDFInfo
- Publication number
- RU2010124799A RU2010124799A RU2010124799/04A RU2010124799A RU2010124799A RU 2010124799 A RU2010124799 A RU 2010124799A RU 2010124799/04 A RU2010124799/04 A RU 2010124799/04A RU 2010124799 A RU2010124799 A RU 2010124799A RU 2010124799 A RU2010124799 A RU 2010124799A
- Authority
- RU
- Russia
- Prior art keywords
- naphtho
- hydroxy
- dioxolo
- dodecahydro
- indazole
- Prior art date
Links
- 239000003862 glucocorticoid Substances 0.000 title claims 2
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000003431 steroids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 17
- -1 1,3-dioxolanyl group Chemical group 0.000 claims abstract 15
- 150000003839 salts Chemical class 0.000 claims abstract 10
- 125000005843 halogen group Chemical group 0.000 claims abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 8
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 8
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 6
- 125000006699 (C1-C3) hydroxyalkyl group Chemical group 0.000 claims abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 5
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 5
- 239000001301 oxygen Substances 0.000 claims abstract 5
- 125000001424 substituent group Chemical group 0.000 claims abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 4
- 239000001257 hydrogen Substances 0.000 claims abstract 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 3
- 125000005842 heteroatom Chemical group 0.000 claims abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 2
- 229910052731 fluorine Chemical group 0.000 claims abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 claims abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 2
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 2
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 2
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 7
- LMKPHJYTFHAGHK-UHFFFAOYSA-N cyclodrine Chemical compound C1CCCC1(O)C(C(=O)OCCN(CC)CC)C1=CC=CC=C1 LMKPHJYTFHAGHK-UHFFFAOYSA-N 0.000 claims 5
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims 2
- 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
- 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 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- XKTYXVDYIKIYJP-UHFFFAOYSA-N 3h-dioxole Chemical compound C1OOC=C1 XKTYXVDYIKIYJP-UHFFFAOYSA-N 0.000 claims 1
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 claims 1
- AXZYVPCYGTXTTK-UHFFFAOYSA-N 8h-naphtho[1,2-f]indazole Chemical compound C1=CC=C2C3=CC4=CNN=C4C=C3C=CC2=C1 AXZYVPCYGTXTTK-UHFFFAOYSA-N 0.000 claims 1
- 229940124225 Adrenoreceptor agonist Drugs 0.000 claims 1
- 102000009410 Chemokine receptor Human genes 0.000 claims 1
- 108050000299 Chemokine receptor Proteins 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
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 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
- 239000003814 drug Substances 0.000 claims 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 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
- 229940075993 receptor modulator Drugs 0.000 claims 1
- 230000003637 steroidlike Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1540407P | 2007-12-20 | 2007-12-20 | |
| US61/015,404 | 2007-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2010124799A true RU2010124799A (ru) | 2012-01-27 |
Family
ID=40801455
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2010124799/04A RU2010124799A (ru) | 2007-12-20 | 2008-12-18 | Производные стероидов, действующие в качестве агонистов глюкокортикостероидных рецепторов |
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
Also Published As
| Publication number | Publication date |
|---|---|
| JP2011507836A (ja) | 2011-03-10 |
| US20110160167A1 (en) | 2011-06-30 |
| EP2235037A1 (en) | 2010-10-06 |
| CA2707618A1 (en) | 2009-07-02 |
| CN101945885A (zh) | 2011-01-12 |
| KR20100102121A (ko) | 2010-09-20 |
| AU2008341590A1 (en) | 2009-07-02 |
| WO2009082342A1 (en) | 2009-07-02 |
| BRPI0821139A2 (pt) | 2015-06-16 |
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