PE20091525A1 - Agonista del receptor glucocorticoide c-20-c21 sustituido - Google Patents
Agonista del receptor glucocorticoide c-20-c21 sustituidoInfo
- Publication number
- PE20091525A1 PE20091525A1 PE2008002140A PE2008002140A PE20091525A1 PE 20091525 A1 PE20091525 A1 PE 20091525A1 PE 2008002140 A PE2008002140 A PE 2008002140A PE 2008002140 A PE2008002140 A PE 2008002140A PE 20091525 A1 PE20091525 A1 PE 20091525A1
- Authority
- PE
- Peru
- Prior art keywords
- glucocorticoid receptor
- halogen
- alkyl
- replaced
- receptor agonist
- Prior art date
Links
- 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 title 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 102000003676 Glucocorticoid Receptors Human genes 0.000 abstract 1
- 108090000079 Glucocorticoid Receptors Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000003431 steroids Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/10—Expectorants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
REFIERE A DERIVADOS DE ESTEROIDES C-21 DE FORMULA (I), DONDE L ES UN RESTO DIVALENTE SELECCIONADO DE (A), (B) Y (C), DONDE G ES N O CH Y n ES UN ENTERO DE 0 A 2, CON LA CONDICION QUE CUANDO n ES 0, G SEA CH; O EN FORMA ALTERNATIVA L ES -CH2-, S-CH2-C(O)-NH-, -CH2O-, ENTRE OTROS; R1 ES ALQUILO, ARILO, ARILALQUILO, ENTRE OTROS; R2 ES -OR8; R3 ES H, HIDROXI Y ALQUILO; R4 ES H Y HALOGENO; R5 ES H, HALOGENO Y ALQUILO; z (LA LINEA PUNTEADA), REPRESENTA UN ENLACE SIMPLE O DOBLE, CON LA CONDICION QUE CUANDO z ES UN ENLACE SIMPLE, ENTONCES R6 ES H; R6 ES H Y HALOGENO; R8 ES H, ALQUILO, HALOALQUILO, ENTRE OTROS. SE REFIERE TAMBIEN A UN METODO DE PREPARACION PARA UNA COMPOSICION QUE LO CONTIENE. DICHO COMPUESTO ES AGONISTA DEL RECEPTOR GLUCOCORTICOIDE, SIENDO DE UTILIDAD PARA EL TRATAMIENTO DE TRASTORNOS ALGERGICOS E INFLAMATORIOS TAL COMO TAL COMO ASMA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1613507P | 2007-12-21 | 2007-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091525A1 true PE20091525A1 (es) | 2009-09-25 |
Family
ID=40532554
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008002140A PE20091525A1 (es) | 2007-12-21 | 2008-12-18 | Agonista del receptor glucocorticoide c-20-c21 sustituido |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8524697B2 (es) |
| EP (1) | EP2245042A1 (es) |
| JP (1) | JP2011507878A (es) |
| CN (1) | CN101970452A (es) |
| AR (1) | AR069804A1 (es) |
| CA (1) | CA2710149A1 (es) |
| CL (1) | CL2008003803A1 (es) |
| MX (1) | MX2010007023A (es) |
| PE (1) | PE20091525A1 (es) |
| TW (1) | TW200944540A (es) |
| WO (1) | WO2009085879A2 (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011507879A (ja) * | 2007-12-21 | 2011-03-10 | シェーリング コーポレイション | グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル |
| RU2420270C2 (ru) * | 2009-07-20 | 2011-06-10 | Государственное образовательное учреждение высшего профессионального образования "Северо-Осетинская государственная медицинская академия" Федерального агентства по здравоохранению и социальному развитию | Способ лечения рецидивирующего обструктивного бронхита у детей |
| PE20120894A1 (es) * | 2009-09-11 | 2012-08-13 | Chiesi Farma Spa | Derivados de isoxazolidina |
| CN103087137A (zh) * | 2011-11-07 | 2013-05-08 | 天津金耀集团有限公司 | 一种21位为硫代烃基的糖皮质激素 |
| UA111867C2 (uk) | 2011-11-11 | 2016-06-24 | Аллерган, Інк. | ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ І СПОСІБ ЗАСТОСУВАННЯ ПОХІДНИХ 4-ПРЕГНЕН-11β-17-21-ТРІОЛ-3,20-ДІОНУ |
| WO2014115167A2 (en) * | 2013-01-23 | 2014-07-31 | Sphaera Pharma Pvt. Ltd. | Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion |
| GB201320091D0 (en) * | 2013-11-14 | 2014-01-01 | Univ Manchester | Selective glucocorticoid receptor ligands |
| CN106714770B (zh) | 2014-07-23 | 2024-04-19 | 斯法尔制药私人有限公司 | 羟基类固醇化合物、其中间体、制备方法、组合物及其用途 |
| SG10202001787QA (en) | 2016-06-02 | 2020-04-29 | Abbvie Inc | Glucocorticoid receptor agonist and immunoconjugates thereof |
| ES3046537T3 (en) * | 2016-11-08 | 2025-12-02 | Regeneron Pharma | Steroids and protein-conjugates thereof |
| TW201825456A (zh) * | 2016-11-24 | 2018-07-16 | 日商帝人製藥股份有限公司 | 硫醚化合物的製造方法 |
| IL270594B2 (en) | 2017-05-18 | 2024-06-01 | Regeneron Pharma | Cyclodextrin protein drug conjugates |
| MX2020000916A (es) | 2017-07-24 | 2020-09-10 | Regeneron Pharma | Anticuerpos anti-cd8 y usos de estos. |
| SG11202004151YA (en) | 2017-11-07 | 2020-06-29 | Regeneron Pharma | Hydrophilic linkers for antibody drug conjugates |
| WO2019106608A1 (en) * | 2017-12-01 | 2019-06-06 | Abbvie Inc. | Anti-cd40 antibody drug conjugates |
| PE20201286A1 (es) | 2017-12-01 | 2020-11-24 | Abbvie Inc | Agonista del receptor de glucocorticoides e inmunoconjugados de este |
| IL319417A (en) | 2018-01-08 | 2025-05-01 | Regeneron Pharma | Steroids and their anti-inflammatory properties |
| CN112533951A (zh) | 2018-05-09 | 2021-03-19 | 里珍纳龙药品有限公司 | 抗msr1抗体及其使用方法 |
| CN112851743A (zh) * | 2019-11-27 | 2021-05-28 | 重庆华邦胜凯制药有限公司 | 一种氧化杂质的制备方法 |
| CN112876531A (zh) * | 2019-11-29 | 2021-06-01 | 重庆华邦胜凯制药有限公司 | 一种合成地奈德杂质的方法 |
| AR125079A1 (es) | 2021-03-23 | 2023-06-07 | Lilly Co Eli | Agonistas de receptores de glucocorticoides sustituidos con carboxi |
| TW202304464A (zh) | 2021-03-23 | 2023-02-01 | 美商美國禮來大藥廠 | 新穎糖皮質素受體激動劑 |
| TWI899455B (zh) | 2021-03-23 | 2025-10-01 | 美商美國禮來大藥廠 | 糖皮質素受體激動劑 |
| CN114702543B (zh) * | 2022-04-19 | 2023-08-22 | 中国药科大学 | Clascoterone衍生物或其可药用的盐及其制备方法和用途 |
| CN115430392B (zh) * | 2022-08-31 | 2024-04-16 | 江苏诺盟化工有限公司 | 一种苯偶酰的制备方法及专用文丘里喷射器 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1119082A (en) | 1914-03-16 | 1914-12-01 | George A Inman | Protector-plate. |
| US3020275A (en) * | 1960-06-07 | 1962-02-06 | American Cyanamid Co | 21-nitrogen substituted steroids of the pregnane series and methods of preparing the same |
| GB1119082A (en) * | 1966-07-11 | 1968-07-10 | Lepetit Spa | New steroids |
| DE1300940B (de) * | 1966-10-13 | 1969-08-14 | Hoechst Ag | Verfahren zur Herstellung von Tetrahydropyranylaethern von Steroiden |
| US4188385A (en) * | 1978-04-05 | 1980-02-12 | Syntex (U.S.A.) Inc. | Thioetianic acid derivatives |
| US4861765A (en) | 1985-06-26 | 1989-08-29 | Jouveinal | 21-alkyl-, cycloalkyl- or aryl-substituted thio steroids and pharmaceutical compositions containing them |
| ZA866097B (en) * | 1985-09-12 | 1988-03-30 | Upjohn Co | 20-and 21-amino steroids |
| JP2659279B2 (ja) * | 1993-05-17 | 1997-09-30 | アルコン ラボラトリーズ，インコーポレイテッド | 眼科用抗炎症化合物 |
| US5420120A (en) | 1993-12-17 | 1995-05-30 | Alcon Laboratories, Inc. | Anti-inflammatory glucocorticoid compounds for topical ophthalmic use |
| ATE416184T1 (de) * | 2000-08-05 | 2008-12-15 | Glaxo Group Ltd | 17.beta.-carbothioat 17.alpha.- arylkarbonyloxyloxy androstanderivate als anti- phlogistische medikamente |
| NZ526216A (en) * | 2000-11-03 | 2005-02-25 | Univ Manchester | Selective glucocorticoid receptor agonists |
| WO2006138212A1 (en) * | 2005-06-14 | 2006-12-28 | Gilead Sciences, Inc. | SUBSTITUTED PHENYLPHOSPHATES AS MUTUAL PRODRUGS OF STEROIDS AND β -AGONISTS FOR THE TREATMENT OF PULMONARY INFLAMMATION AND BRONCHOCONSTRICTION |
| JP2011507879A (ja) * | 2007-12-21 | 2011-03-10 | シェーリング コーポレイション | グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル |
| US8916136B2 (en) * | 2010-04-23 | 2014-12-23 | Indian Institute Of Technology Bombay | Glucose biosensor system coupled with an anti-inflammatory module and methods for using the same |
-
2008
- 2008-12-18 PE PE2008002140A patent/PE20091525A1/es not_active Application Discontinuation
- 2008-12-18 TW TW097149406A patent/TW200944540A/zh unknown
- 2008-12-18 CL CL2008003803A patent/CL2008003803A1/es unknown
- 2008-12-18 CN CN2008801273812A patent/CN101970452A/zh active Pending
- 2008-12-18 CA CA2710149A patent/CA2710149A1/en not_active Abandoned
- 2008-12-18 EP EP08868864A patent/EP2245042A1/en not_active Withdrawn
- 2008-12-18 AR ARP080105525A patent/AR069804A1/es not_active Application Discontinuation
- 2008-12-18 JP JP2010539762A patent/JP2011507878A/ja active Pending
- 2008-12-18 MX MX2010007023A patent/MX2010007023A/es not_active Application Discontinuation
- 2008-12-18 US US12/736,063 patent/US8524697B2/en not_active Expired - Fee Related
- 2008-12-18 WO PCT/US2008/087300 patent/WO2009085879A2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| TW200944540A (en) | 2009-11-01 |
| WO2009085879A2 (en) | 2009-07-09 |
| CA2710149A1 (en) | 2009-07-09 |
| US8524697B2 (en) | 2013-09-03 |
| JP2011507878A (ja) | 2011-03-10 |
| CN101970452A (zh) | 2011-02-09 |
| EP2245042A1 (en) | 2010-11-03 |
| MX2010007023A (es) | 2010-09-30 |
| CL2008003803A1 (es) | 2010-02-19 |
| AR069804A1 (es) | 2010-02-17 |
| US20110182828A1 (en) | 2011-07-28 |
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Legal Events
| Date | Code | Title | Description |
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| FC | Refusal |