AR076176A1 - Derivados de amida de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides - Google Patents
Derivados de amida de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroidesInfo
- Publication number
- AR076176A1 AR076176A1 ARP100101088A ARP100101088A AR076176A1 AR 076176 A1 AR076176 A1 AR 076176A1 AR P100101088 A ARP100101088 A AR P100101088A AR P100101088 A ARP100101088 A AR P100101088A AR 076176 A1 AR076176 A1 AR 076176A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- hydroxyl
- group
- halogen
- Prior art date
Links
- 230000001270 agonistic effect Effects 0.000 title 1
- 150000003431 steroids Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 6
- 229920006395 saturated elastomer Polymers 0.000 abstract 6
- -1 cyano, hydroxyl Chemical group 0.000 abstract 5
- 150000002367 halogens Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract 4
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000005102 carbonylalkoxy group Chemical group 0.000 abstract 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 abstract 1
- 125000005518 carboxamido group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 229910052731 fluorine Chemical group 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 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 (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16632409P | 2009-04-03 | 2009-04-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076176A1 true AR076176A1 (es) | 2011-05-26 |
Family
ID=42826696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101088A AR076176A1 (es) | 2009-04-03 | 2010-03-31 | Derivados de amida de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides |
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) |
Families Citing this family (12)
| 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 |
| WO2015048316A1 (en) * | 2013-09-25 | 2015-04-02 | Van Andel Research Institute | Highly potent glucocorticoids |
| 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 |
Family Cites Families (13)
| 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 |
| ES2314052T3 (es) * | 2001-04-30 | 2009-03-16 | Glaxo Group Limited | Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa. |
| GB0507165D0 (en) * | 2005-04-08 | 2005-05-18 | Glaxo Group Ltd | Novel crystalline pharmaceutical product |
| AU2008306593C1 (en) * | 2007-10-04 | 2012-10-04 | 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 |
| 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
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 |
| EA201190234A1 (ru) | 2012-04-30 |
| ZA201108050B (en) | 2014-04-30 |
| JP2012522766A (ja) | 2012-09-27 |
| 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |