AR070040A1 - Tioeteres c-21 como agonistas del receptor de glucocorticoides - Google Patents
Tioeteres c-21 como agonistas del receptor de glucocorticoidesInfo
- Publication number
- AR070040A1 AR070040A1 ARP080105526A ARP080105526A AR070040A1 AR 070040 A1 AR070040 A1 AR 070040A1 AR P080105526 A ARP080105526 A AR P080105526A AR P080105526 A ARP080105526 A AR P080105526A AR 070040 A1 AR070040 A1 AR 070040A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- halogen
- membered
- membered heteroaryl
- Prior art date
Links
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 title 1
- 150000003568 thioethers Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000003862 glucocorticoid Substances 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 230000009885 systemic effect Effects 0.000 abstract 1
- 229940037128 systemic glucocorticoids Drugs 0.000 abstract 1
- 238000011282 treatment Methods 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/34—Gestagens
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/0026—Oxygen-containing hetero ring cyclic ketals
- C07J71/0031—Oxygen-containing hetero ring cyclic ketals at positions 16, 17
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Otolaryngology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (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)
Abstract
Se proveen composiciones farmacéuticas y métodos para el tratamiento y profilaxis de un amplio rango de enfermedades y afecciones inmunes, autoinmunes, e inflamatorias. Los compuestos poseen actividad farmacologica util y actividad sistémica inesperadamente baja. Así, estos compuestos representan una alternativa segura a aquellos glucocorticoides que tienen perfiles de efectos colaterales escasos. Reivindicacion 1: Un compuesto que tiene la estructura general mostrada en la formula (1), o una sal aceptable para uso farmacéutico, solvato, éster, prodroga o isomero del mismo donde L, R1, R2, R3, R4, y R5 se seleccionan en forma independiente entre sí y donde L es -CH2S-; R1 se selecciona de arilo, arilalquil-, cicloalquilo, heterocicloalquenilo de 5 miembros, heterocicloalquenil- de 5 miembros benzofusionado, heteroarilo de 5 miembros, heteroaril- de 5 miembros benzofusionado, heterocicloalquenilo de 6 miembros y heteroarilo de 6 miembros, donde cada grupo R1 no está sustituido o está opcionalmente sustituido con 1 a 5 sustituyentes seleccionados en forma independiente de alquilo, halogeno, alcoxi, -N(R7)2, y -CO2R7; R2 es -OR8; R3 se selecciona de hidrogeno, hidroxi, alquilo inferior recto o ramificado, o R2 y R3 tomados en conjunto pueden formar un resto de formula 2; donde X e Y se seleccionan en forma independiente de hidrogeno, alquilo y fenilo, con la condicion de que cuando uno de X o Y es fenilo, el otro es hidrogeno; z (la línea punteada junto a z) es un enlace simple o doble; R4 se selecciona de H y halogeno, con la condicion de que cuando R4 es halogeno, z es un enlace simple; R5 se selecciona de H y alquilo; cada R7 se selecciona en forma independiente de hidrogeno, alquilo, haloalquilo, arilo y heteroarilo; R8 se selecciona de hidrogeno, alquilo, y -C(O)R9; y R9 se selecciona de alquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1614407P | 2007-12-21 | 2007-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070040A1 true AR070040A1 (es) | 2010-03-10 |
Family
ID=40513892
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105526A AR070040A1 (es) | 2007-12-21 | 2008-12-18 | Tioeteres c-21 como agonistas del receptor de glucocorticoides |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20110262368A1 (es) |
| EP (1) | EP2235035A2 (es) |
| JP (1) | JP2011507879A (es) |
| CN (1) | CN102099368A (es) |
| AR (1) | AR070040A1 (es) |
| CA (1) | CA2710240A1 (es) |
| CL (1) | CL2008003802A1 (es) |
| MX (1) | MX2010007024A (es) |
| PE (1) | PE20091215A1 (es) |
| TW (1) | TW200940070A (es) |
| WO (1) | WO2009085880A2 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20091525A1 (es) * | 2007-12-21 | 2009-09-25 | Schering Corp | Agonista del receptor glucocorticoide c-20-c21 sustituido |
| UY32520A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| CN103694306B (zh) * | 2014-01-07 | 2016-03-23 | 成都医路康医学技术服务有限公司 | 一种布地奈德s异构体制备r异构体的方法 |
| PE20190622A1 (es) | 2016-06-02 | 2019-04-26 | Abbvie Inc | Agonista del receptor de glucocorticoides e inmunoconjugados del mismo |
| AU2017359043B2 (en) | 2016-11-08 | 2022-06-16 | Regeneron Pharmaceuticals, Inc. | Steroids and protein-conjugates thereof |
| WO2018213077A1 (en) | 2017-05-18 | 2018-11-22 | Regeneron Pharmaceuticals, Inc. | Cyclodextrin protein drug conjugates |
| UA126595C2 (uk) | 2017-12-01 | 2022-11-02 | Еббві Інк. | Кон'югат антитіло-лікарський засіб |
| MX2020011546A (es) | 2018-05-09 | 2021-01-29 | Regeneron Pharma | Anticuerpos anti-msr1 y metodos de uso de los mismos. |
| EP3868368A1 (en) * | 2020-02-21 | 2021-08-25 | Dompe' Farmaceutici S.P.A. | Cxcl8 (interleukin-8) activity inhibitor and corticosteroid combination and pharmaceutical composition and use thereof |
| WO2024125639A1 (zh) * | 2022-12-16 | 2024-06-20 | 津药生物科技（天津）有限公司 | 新型糖皮质激素、其制备方法及用途 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2231374B1 (es) * | 1973-05-30 | 1976-10-22 | Jouveinal Sa | |
| FR2510582B1 (fr) * | 1981-07-30 | 1986-05-30 | Sipsy | Steroides esterifies en la position 17 et thio-esterifies en la position 21, leur procede de preparation et leur application comme medicament |
| FR2551069B1 (fr) * | 1983-08-26 | 1986-07-25 | Jouveinal Sa | 17-oxo-21-thioesters d'hydrocortisone, leur preparation et leurs applications comme medicament |
| US5223493A (en) * | 1984-12-28 | 1993-06-29 | Alcon Laboratories, Inc. | Anti-inflammatory compounds for ophthalmic use |
| US4861765A (en) * | 1985-06-26 | 1989-08-29 | Jouveinal | 21-alkyl-, cycloalkyl- or aryl-substituted thio steroids and pharmaceutical compositions containing them |
| US5420120A (en) * | 1993-12-17 | 1995-05-30 | Alcon Laboratories, Inc. | Anti-inflammatory glucocorticoid compounds for topical ophthalmic use |
| US6013244A (en) * | 1995-12-29 | 2000-01-11 | Glaxo Wellcome Inc. | 21-(2-oxo-tetrahydrofuran)-thio pregnane derivatives, a process for their production and pharmaceutical compositions containing them |
| CA2612364A1 (en) * | 2005-06-14 | 2006-12-28 | Corus Pharma, Inc. | Substituted phenylphosphates as mutual prodrugs of steroids and .beta.-agonists the treatment of pulmonary inflammation and bronchoconstriction |
| PE20091525A1 (es) * | 2007-12-21 | 2009-09-25 | Schering Corp | Agonista del receptor glucocorticoide c-20-c21 sustituido |
-
2008
- 2008-12-18 AR ARP080105526A patent/AR070040A1/es not_active Application Discontinuation
- 2008-12-18 CA CA2710240A patent/CA2710240A1/en not_active Abandoned
- 2008-12-18 EP EP08866275A patent/EP2235035A2/en not_active Withdrawn
- 2008-12-18 MX MX2010007024A patent/MX2010007024A/es not_active Application Discontinuation
- 2008-12-18 TW TW097149503A patent/TW200940070A/zh unknown
- 2008-12-18 US US12/736,064 patent/US20110262368A1/en not_active Abandoned
- 2008-12-18 PE PE2008002135A patent/PE20091215A1/es not_active Application Discontinuation
- 2008-12-18 CL CL2008003802A patent/CL2008003802A1/es unknown
- 2008-12-18 JP JP2010539763A patent/JP2011507879A/ja active Pending
- 2008-12-18 WO PCT/US2008/087301 patent/WO2009085880A2/en active Application Filing
- 2008-12-18 CN CN2008801273009A patent/CN102099368A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| MX2010007024A (es) | 2010-09-30 |
| US20110262368A1 (en) | 2011-10-27 |
| CL2008003802A1 (es) | 2010-02-19 |
| WO2009085880A2 (en) | 2009-07-09 |
| TW200940070A (en) | 2009-10-01 |
| CA2710240A1 (en) | 2009-07-09 |
| WO2009085880A8 (en) | 2011-01-27 |
| JP2011507879A (ja) | 2011-03-10 |
| PE20091215A1 (es) | 2009-08-14 |
| WO2009085880A3 (en) | 2009-09-17 |
| CN102099368A (zh) | 2011-06-15 |
| EP2235035A2 (en) | 2010-10-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |