JP2012522766A - グルココルチコイド活性を有するステロイド性［３，２−ｃ］ピラゾール化合物の新規アミド誘導体 - Google Patents
グルココルチコイド活性を有するステロイド性［３，２−ｃ］ピラゾール化合物の新規アミド誘導体 Download PDFInfo
- Publication number
- JP2012522766A JP2012522766A JP2012503371A JP2012503371A JP2012522766A JP 2012522766 A JP2012522766 A JP 2012522766A JP 2012503371 A JP2012503371 A JP 2012503371A JP 2012503371 A JP2012503371 A JP 2012503371A JP 2012522766 A JP2012522766 A JP 2012522766A
- Authority
- JP
- Japan
- Prior art keywords
- carbonyl
- phenyl
- naphtho
- sulfanyl
- hydroxy
- 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
- RQOWDAOTCPGSPT-UHFFFAOYSA-N CC(C)(C)OC(NNc1cc(C(NCCOC)=O)ccc1)=O Chemical compound CC(C)(C)OC(NNc1cc(C(NCCOC)=O)ccc1)=O RQOWDAOTCPGSPT-UHFFFAOYSA-N 0.000 description 1
- NVUGBLWYIPGFGA-HCDCZEEPSA-N CCC(O[C@](CC1)([C@@](C)(CC2O)C1[C@H](CC1)C2[C@@](C)(C2)C1=CC(Nc1cc(C(NCCSC)=O)ccc1)=C2C=N)C(SCF)=O)=O Chemical compound CCC(O[C@](CC1)([C@@](C)(CC2O)C1[C@H](CC1)C2[C@@](C)(C2)C1=CC(Nc1cc(C(NCCSC)=O)ccc1)=C2C=N)C(SCF)=O)=O NVUGBLWYIPGFGA-HCDCZEEPSA-N 0.000 description 1
- WZMBNULUHXQOCX-UHFFFAOYSA-N COCCNC(c1cccc(NN)c1)=O Chemical compound COCCNC(c1cccc(NN)c1)=O WZMBNULUHXQOCX-UHFFFAOYSA-N 0.000 description 1
- SYGZIEPAVKOJGN-YZWMQTLBSA-N C[C@](C[C@@H]1O)(C(CC2)[C@H](CC3)C1[C@@](C)(C1)C3=CC(Nc3cc(C(NCCSC)=O)ccc3)=C1C=N)[C@]2(C(O)=O)O Chemical compound C[C@](C[C@@H]1O)(C(CC2)[C@H](CC3)C1[C@@](C)(C1)C3=CC(Nc3cc(C(NCCSC)=O)ccc3)=C1C=N)[C@]2(C(O)=O)O SYGZIEPAVKOJGN-YZWMQTLBSA-N 0.000 description 1
- HHZIRQNLEYLRCP-YZWMQTLBSA-N C[C@](C[C@@H]1O)(C(CC2)[C@H](CC3)C1[C@@](C)(C1)C3=CC(Nc3cc(C(NCCSC)=O)ccc3)=C1C=N)[C@]2(C(S)=O)O Chemical compound C[C@](C[C@@H]1O)(C(CC2)[C@H](CC3)C1[C@@](C)(C1)C3=CC(Nc3cc(C(NCCSC)=O)ccc3)=C1C=N)[C@]2(C(S)=O)O HHZIRQNLEYLRCP-YZWMQTLBSA-N 0.000 description 1
- HINCUIRVVIWHLK-PWOGEFBASA-N C[C@](C[C@@H]1O)([C@@H](CC2)[C@H](CCC([C@]3(C)C4)=Cc5c4cn[n]5-c4cc(C(N(CCC5)[C@H]5C(N)=O)=O)ccc4)[C@]13F)[C@]2(C(SCF)=O)OC(COC)=O Chemical compound C[C@](C[C@@H]1O)([C@@H](CC2)[C@H](CCC([C@]3(C)C4)=Cc5c4cn[n]5-c4cc(C(N(CCC5)[C@H]5C(N)=O)=O)ccc4)[C@]13F)[C@]2(C(SCF)=O)OC(COC)=O HINCUIRVVIWHLK-PWOGEFBASA-N 0.000 description 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0036—Nitrogen-containing hetero ring
- C07J71/0042—Nitrogen only
- C07J71/0047—Nitrogen only at position 2(3)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16632409P | 2009-04-03 | 2009-04-03 | |
| US61/166,324 | 2009-04-03 | ||
| PCT/SE2010/050354 WO2010114471A1 (en) | 2009-04-03 | 2010-03-31 | Novel amide derivatives of steroidal[3,2-c]pyrazole compounds with glucocorticoid activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012522766A true JP2012522766A (ja) | 2012-09-27 |
| JP2012522766A5 JP2012522766A5 (enExample) | 2013-05-02 |
Family
ID=42826696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012503371A Pending JP2012522766A (ja) | 2009-04-03 | 2010-03-31 | グルココルチコイド活性を有するステロイド性［３，２−ｃ］ピラゾール化合物の新規アミド誘導体 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US20100256104A1 (enExample) |
| EP (1) | EP2414375A4 (enExample) |
| JP (1) | JP2012522766A (enExample) |
| KR (1) | KR20120034608A (enExample) |
| CN (1) | CN102459306A (enExample) |
| AR (1) | AR076176A1 (enExample) |
| AU (1) | AU2010231954B2 (enExample) |
| CA (1) | CA2757423A1 (enExample) |
| CL (1) | CL2011002461A1 (enExample) |
| CO (1) | CO6501167A2 (enExample) |
| CR (1) | CR20110518A (enExample) |
| CU (1) | CU20110186A7 (enExample) |
| DO (1) | DOP2011000305A (enExample) |
| EA (1) | EA201190234A1 (enExample) |
| EC (1) | ECSP11011368A (enExample) |
| IL (1) | IL215342A0 (enExample) |
| MX (1) | MX2011010263A (enExample) |
| NI (1) | NI201100177A (enExample) |
| PE (1) | PE20120544A1 (enExample) |
| SG (1) | SG174506A1 (enExample) |
| TW (1) | TW201040196A (enExample) |
| UY (1) | UY32525A (enExample) |
| WO (1) | WO2010114471A1 (enExample) |
| ZA (1) | ZA201108050B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016531852A (ja) * | 2013-09-25 | 2016-10-13 | ヴァン アンデル リサーチ インスティテュート | 非常に強力なグルココルチコイド |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008306593C1 (en) * | 2007-10-04 | 2012-10-04 | Astrazeneca Ab | Steroidal [3, 2-C] pyrazole compounds, with glucocorticoid activity |
| CA2707618A1 (en) * | 2007-12-20 | 2009-07-02 | Astrazeneca Ab | Steroid derivatives acting as glucocorticosteroid receptor agonists |
| 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 |
| PE20140868A1 (es) | 2011-06-24 | 2014-07-18 | Amgen Inc | Antagonistas trpm8 y su uso en tratamientos |
| CA2839703A1 (en) | 2011-06-24 | 2012-12-27 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| JP7146750B2 (ja) * | 2016-10-14 | 2022-10-04 | ヴァン アンデル リサーチ インスティテュート | 非常に強力な糖質コルチコイドの構造およびデザインのための機構 |
| WO2024159212A1 (en) * | 2023-01-27 | 2024-08-02 | University Of South Florida | Compositions and methods of treating respiratory syncytial virus |
| CN117024499A (zh) * | 2023-07-17 | 2023-11-10 | 陕西汉江药业集团股份有限公司 | 在2位引入亚甲基羟基的甾体化合物制备方法 |
| WO2025119398A1 (zh) * | 2023-12-08 | 2025-06-12 | 浙江柏拉阿图医药科技有限公司 | 高效力糖皮质激素多晶型及其制备方法和用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004528354A (ja) * | 2001-04-30 | 2004-09-16 | グラクソ グループ リミテッド | 抗炎症性の、１７α位に環状エステル基を有するアンドロスタンの１７β−カルボチオ酸エステル誘導体 |
| WO2006108572A2 (en) * | 2005-04-08 | 2006-10-19 | Glaxo Group Limited | Novel crystalline pharmaceutical product |
| JP2010540612A (ja) * | 2007-10-04 | 2010-12-24 | アストラゼネカ・アクチエボラーグ | グルココルチコイド活性を有するステロイド［３，２−ｃ］ピラゾール化合物 |
Family Cites Families (10)
| 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 |
| DE2727367A1 (de) * | 1977-06-14 | 1979-01-04 | Schering Ag | Neue kortikoide |
| 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 |
| UY32520A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| UY32521A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Combinación para emplear en el tratamiento de enfermedades respiratorias |
-
2010
- 2010-03-26 UY UY0001032525A patent/UY32525A/es not_active Application Discontinuation
- 2010-03-30 US US12/749,903 patent/US20100256104A1/en not_active Abandoned
- 2010-03-31 WO PCT/SE2010/050354 patent/WO2010114471A1/en not_active Ceased
- 2010-03-31 EP EP10759125A patent/EP2414375A4/en not_active Withdrawn
- 2010-03-31 MX MX2011010263A patent/MX2011010263A/es not_active Application Discontinuation
- 2010-03-31 CN CN2010800248242A patent/CN102459306A/zh active Pending
- 2010-03-31 PE PE2011001757A patent/PE20120544A1/es not_active Application Discontinuation
- 2010-03-31 AU AU2010231954A patent/AU2010231954B2/en not_active Ceased
- 2010-03-31 SG SG2011068327A patent/SG174506A1/en unknown
- 2010-03-31 EA EA201190234A patent/EA201190234A1/ru unknown
- 2010-03-31 KR KR1020117026112A patent/KR20120034608A/ko not_active Withdrawn
- 2010-03-31 CA CA2757423A patent/CA2757423A1/en not_active Abandoned
- 2010-03-31 AR ARP100101088A patent/AR076176A1/es unknown
- 2010-03-31 JP JP2012503371A patent/JP2012522766A/ja active Pending
- 2010-04-02 TW TW099110330A patent/TW201040196A/zh unknown
-
2011
- 2011-09-22 IL IL215342A patent/IL215342A0/en unknown
- 2011-09-30 CO CO11129266A patent/CO6501167A2/es not_active Application Discontinuation
- 2011-10-03 DO DO2011000305A patent/DOP2011000305A/es unknown
- 2011-10-03 CL CL2011002461A patent/CL2011002461A1/es unknown
- 2011-10-03 CR CR20110518A patent/CR20110518A/es unknown
- 2011-10-03 NI NI201100177A patent/NI201100177A/es unknown
- 2011-10-03 CU CU20110186A patent/CU20110186A7/es unknown
- 2011-10-03 EC EC2011011368A patent/ECSP11011368A/es unknown
- 2011-11-02 ZA ZA2011/08050A patent/ZA201108050B/en unknown
-
2013
- 2013-04-17 US US13/864,644 patent/US20130237507A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004528354A (ja) * | 2001-04-30 | 2004-09-16 | グラクソ グループ リミテッド | 抗炎症性の、１７α位に環状エステル基を有するアンドロスタンの１７β−カルボチオ酸エステル誘導体 |
| WO2006108572A2 (en) * | 2005-04-08 | 2006-10-19 | Glaxo Group Limited | Novel crystalline pharmaceutical product |
| JP2010540612A (ja) * | 2007-10-04 | 2010-12-24 | アストラゼネカ・アクチエボラーグ | グルココルチコイド活性を有するステロイド［３，２−ｃ］ピラゾール化合物 |
Non-Patent Citations (6)
| Title |
|---|
| ADVANCED DRUG DELIVERY REVIEWS, vol. 14, JPN5010013358, 1994, pages 293 - 299, ISSN: 0002854023 * |
| BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, JPN5010013357, 2006, pages 3454 - 3458, ISSN: 0002854021 * |
| CHEMICAL AND PHARMACEUTICAL BULLETIN, vol. 34, no. 4, JPN6014029127, 1986, pages 1613 - 1618, ISSN: 0002854018 * |
| JOURNAL OF MEDICINAL CHEMISTRY, vol. 18, no. 2, JPN6014029128, 1975, pages 168 - 172, ISSN: 0002854019 * |
| JOURNAL OF MEDICINAL CHEMISTRY, vol. 45, JPN5010013355, 2002, pages 5397 - 5405, ISSN: 0002854020 * |
| JOURNAL OF MEDICINAL CHEMISTRY, vol. 7, JPN5010013352, 1964, pages 352 - 355, ISSN: 0002854022 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016531852A (ja) * | 2013-09-25 | 2016-10-13 | ヴァン アンデル リサーチ インスティテュート | 非常に強力なグルココルチコイド |
Also Published As
| Publication number | Publication date |
|---|---|
| SG174506A1 (en) | 2011-10-28 |
| KR20120034608A (ko) | 2012-04-12 |
| IL215342A0 (en) | 2011-12-29 |
| TW201040196A (en) | 2010-11-16 |
| CA2757423A1 (en) | 2010-10-07 |
| ECSP11011368A (es) | 2011-11-30 |
| US20100256104A1 (en) | 2010-10-07 |
| MX2011010263A (es) | 2011-10-11 |
| CN102459306A (zh) | 2012-05-16 |
| WO2010114471A1 (en) | 2010-10-07 |
| CO6501167A2 (es) | 2012-08-15 |
| AR076176A1 (es) | 2011-05-26 |
| EA201190234A1 (ru) | 2012-04-30 |
| ZA201108050B (en) | 2014-04-30 |
| CL2011002461A1 (es) | 2012-04-09 |
| NI201100177A (es) | 2012-06-14 |
| CR20110518A (es) | 2011-11-07 |
| US20130237507A1 (en) | 2013-09-12 |
| DOP2011000305A (es) | 2012-05-31 |
| AU2010231954A1 (en) | 2011-10-27 |
| EP2414375A1 (en) | 2012-02-08 |
| EP2414375A4 (en) | 2012-09-19 |
| CU20110186A7 (es) | 2012-02-15 |
| PE20120544A1 (es) | 2012-06-03 |
| UY32525A (es) | 2010-10-29 |
| AU2010231954B2 (en) | 2012-11-15 |
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