AR085817A1 - Derivados de isoxazolidina - Google Patents
Derivados de isoxazolidinaInfo
- Publication number
- AR085817A1 AR085817A1 ARP120100843A ARP120100843A AR085817A1 AR 085817 A1 AR085817 A1 AR 085817A1 AR P120100843 A ARP120100843 A AR P120100843A AR P120100843 A ARP120100843 A AR P120100843A AR 085817 A1 AR085817 A1 AR 085817A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- branched
- linear
- cycloalkyl
- Prior art date
Links
- 150000002546 isoxazolidines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000005947 C1-C6 alkylsulfonyloxy group Chemical group 0.000 abstract 1
- 125000005138 alkoxysulfonyl group Chemical group 0.000 abstract 1
- 125000005157 alkyl carboxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 230000003266 anti-allergic effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 239000003862 glucocorticoid Substances 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 230000001225 therapeutic effect Effects 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
- C07J71/0057—Nitrogen and oxygen
- C07J71/0068—Nitrogen and oxygen at position 16(17)
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P11/06—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
- A61P11/08—Bronchodilators
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Compuestos anti-inflamatorios y anti-alérgicos de la serie de los glucocorticosteroides, métodos para preparar dichos compuestos, composiciones farmacéuticas que comprenden a los mismos y combinaciones y usos terapéuticos de los mismos.Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1) donde R1 es -(CH2)n-Z-(CH2)n’-R3 donde n y n’ son en forma independiente entre sí 0, 1 ó 2; Z es una unión simple o se selecciona entre -S-, -O- y -OC(R4R5)-; R3 se selecciona entre el grupo que consiste en: H, halógeno, CN, OH, CONH2, alquilo C1-6, alquenilo C2-4, haloalquilo C1-6, alquinilo C2-4 y alquil C1-6sulfonilo y alquil C1-6carbonilo; NR4R5, donde R4 y R5 se seleccionan en forma independiente entre el grupo que consiste en alquilo C1-6 y alcoxi C1-6; cicloalquilo C3-8, heterocicloalquilo C3-8, arilo y heteroarilo, cada uno de los cuales está opcionalmente sustituido con uno o más átomos de halógeno o grupos oxo o grupos CN; y R2 se selecciona entre el grupo que consiste en: alquilo C1-8 lineal o ramificado, alcoxi C1-6, haloalquilo C1-6, opcionalmente sustituido con uno o más grupos CN o átomos de halógeno; -(CH2)mR6, donde R6 se selecciona entre el grupo que consiste en cicloalquilo C3-8, heterocicloalquilo C3-8, arilo, arilalquilo C1-6, ariloxi, ariltio y heteroarilo, cada uno de los cuales opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en oxo, OH, halógeno, CN, NH2, CONH2, NO2, NHC(O)H, alquilo C1-6 lineal o ramificado, haloalquilo C1-6 lineal o ramificado, alcoxi C1-6 lineal o ramificado, haloalcoxi C1-6 lineal o ramificado, hidroxialcoxi C1-6, haloalcoxi C1-6, alcoxi C1-6carbonilo, alquil C1-6carboxilo, alquil C1-6sulfonilo y alquil C1-6sulfanilo, alquil C1-6oxisulfonilo, haloalquil C1-6sulfoniloxi, aminosulfonilo, cicloalquilo C3-8, heterocicloalquilo C3-6 y heteroarilo, donde m es 0 o un entero entre 1 y 3 y X e Y son en forma independiente H o halógeno; y sales farmacéuticamente aceptables del mismo; con la condición de que cuando R1 es un grupo -CH2OH y R2 es alquilo C1-6 o cicloalquilo C3-8, luego X e Y son átomos de flúor; o sales farmacéuticamente aceptables del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11158230 | 2011-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR085817A1 true AR085817A1 (es) | 2013-10-30 |
Family
ID=44351355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100843A AR085817A1 (es) | 2011-03-15 | 2012-03-14 | Derivados de isoxazolidina |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US20120234316A1 (es) |
| EP (2) | EP2686332A2 (es) |
| JP (1) | JP6053700B2 (es) |
| KR (1) | KR101956937B1 (es) |
| CN (1) | CN103391945B (es) |
| AR (1) | AR085817A1 (es) |
| AU (1) | AU2012228334B2 (es) |
| BR (1) | BR112013023539B1 (es) |
| CA (1) | CA2850081C (es) |
| CL (1) | CL2013002629A1 (es) |
| EA (1) | EA028904B1 (es) |
| GE (1) | GEP201606566B (es) |
| IL (1) | IL228382A (es) |
| MX (1) | MX345400B (es) |
| MY (1) | MY194140A (es) |
| PE (1) | PE20140890A1 (es) |
| PH (1) | PH12013501813A1 (es) |
| SG (1) | SG193262A1 (es) |
| TN (1) | TN2013000313A1 (es) |
| TW (1) | TWI658047B (es) |
| UA (1) | UA113508C2 (es) |
| WO (1) | WO2012123482A2 (es) |
| ZA (2) | ZA201306881B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103814043A (zh) | 2011-08-01 | 2014-05-21 | 奇斯药制品公司 | 在16，17位与吡咯烷环稠合的抗炎类固醇 |
| US9155747B2 (en) * | 2012-09-13 | 2015-10-13 | Chiesi Farmaceutici S.P.A. | Isoxazolidine derivatives |
| EP2902382A1 (en) * | 2014-01-30 | 2015-08-05 | Fundació Institut de Recerca Biomèdica IRB (Barcelona) | Primary hydroxylamines and uses thereof |
| SI3662910T1 (sl) * | 2014-03-31 | 2025-05-30 | The Scripps Research Institute | Farmakofor za induciranje TRAIL |
| CN113332439A (zh) | 2014-09-03 | 2021-09-03 | 理森制药股份公司 | 包含双重PI3Kδ-γ激酶抑制剂和皮质类固醇的治疗方法及组合物 |
| CN104262440B (zh) * | 2014-09-10 | 2016-08-17 | 江西赣亮医药原料有限公司 | 一种16ɑ-羟基泼尼松龙的制备方法 |
| CN117050128A (zh) * | 2023-08-15 | 2023-11-14 | 黄冈人福药业有限责任公司 | 一种11β-羟基-孕甾-1,4,16-三烯-3,20-二酮-21-醋酸酯的制备方法和设备 |
| CN118638008B (zh) * | 2024-08-14 | 2024-12-17 | 淄博飞源化工有限公司 | 甲基丙烯酸三氟乙酯及其合成方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL31997A (en) * | 1968-05-03 | 1974-03-14 | Lepetit Spa | Process for the preparation of pregnano(17alpha,16alpha-d)oxazolines and 16alpha,21-dihydroxy-17alpha-aminopregnanes |
| US4018774A (en) | 1976-02-13 | 1977-04-19 | E. R. Squibb & Sons, Inc. | Steroidal [16α,17-d]isoxazolidines |
| AR224124A1 (es) * | 1978-04-05 | 1981-10-30 | Syntex Inc | Procedimiento para preparar 4-halo-pregna-1,4-dieno-3,20-dionas |
| WO2005028495A1 (en) * | 2003-09-24 | 2005-03-31 | Glaxo Group Limited | Anti-inflammatory glucocorticoids |
| GB0415747D0 (en) * | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| JP2008526776A (ja) | 2005-01-03 | 2008-07-24 | ミリアド ジェネティクス， インコーポレイテッド | 脳癌の治療の方法 |
| EA201070535A1 (ru) * | 2007-11-30 | 2010-12-30 | Пфайзер Лимитед | Новые агонисты глюкокортикоидных рецепторов |
| WO2009108118A1 (en) * | 2008-02-27 | 2009-09-03 | Astrazeneca Ab | 16 alpha, 17 alpa-acetal glucocorticosteroidal derivatives and their use |
| CN101926805A (zh) * | 2009-06-24 | 2010-12-29 | 天津金耀集团有限公司 | 一种含有16,17异恶唑烷类甾体化合物的药物组合物 |
| PE20120894A1 (es) * | 2009-09-11 | 2012-08-13 | Chiesi Farma Spa | Derivados de isoxazolidina |
| TW201139369A (en) * | 2010-02-05 | 2011-11-16 | Chiesi Farma Spa | Pyrrolidine derivatives |
| KR20140039161A (ko) | 2011-03-15 | 2014-04-01 | 키에시 파르마슈티시 엣스. 피. 에이. | 이소옥사졸리딘 유도체 |
| CN103814043A (zh) | 2011-08-01 | 2014-05-21 | 奇斯药制品公司 | 在16，17位与吡咯烷环稠合的抗炎类固醇 |
| US9155747B2 (en) | 2012-09-13 | 2015-10-13 | Chiesi Farmaceutici S.P.A. | Isoxazolidine derivatives |
-
2012
- 2012-03-14 EP EP12711601.0A patent/EP2686332A2/en not_active Withdrawn
- 2012-03-14 JP JP2013558416A patent/JP6053700B2/ja not_active Expired - Fee Related
- 2012-03-14 EA EA201391173A patent/EA028904B1/ru not_active IP Right Cessation
- 2012-03-14 EP EP13197855.3A patent/EP2716648B1/en active Active
- 2012-03-14 CN CN201280008928.3A patent/CN103391945B/zh not_active Expired - Fee Related
- 2012-03-14 BR BR112013023539-0A patent/BR112013023539B1/pt not_active IP Right Cessation
- 2012-03-14 TW TW101108588A patent/TWI658047B/zh not_active IP Right Cessation
- 2012-03-14 UA UAA201310933A patent/UA113508C2/uk unknown
- 2012-03-14 KR KR1020137022976A patent/KR101956937B1/ko not_active Expired - Fee Related
- 2012-03-14 PE PE2013002015A patent/PE20140890A1/es active IP Right Grant
- 2012-03-14 AU AU2012228334A patent/AU2012228334B2/en not_active Ceased
- 2012-03-14 MX MX2013010354A patent/MX345400B/es active IP Right Grant
- 2012-03-14 PH PH1/2013/501813A patent/PH12013501813A1/en unknown
- 2012-03-14 CA CA2850081A patent/CA2850081C/en active Active
- 2012-03-14 SG SG2013065974A patent/SG193262A1/en unknown
- 2012-03-14 WO PCT/EP2012/054439 patent/WO2012123482A2/en not_active Ceased
- 2012-03-14 AR ARP120100843A patent/AR085817A1/es active IP Right Grant
- 2012-03-14 GE GEAP201213223A patent/GEP201606566B/en unknown
- 2012-03-14 MY MYPI2013002925A patent/MY194140A/en unknown
- 2012-03-15 US US13/421,150 patent/US20120234316A1/en not_active Abandoned
-
2013
- 2013-07-24 TN TNP2013000313A patent/TN2013000313A1/fr unknown
- 2013-09-12 ZA ZA2013/06881A patent/ZA201306881B/en unknown
- 2013-09-12 CL CL2013002629A patent/CL2013002629A1/es unknown
- 2013-09-12 IL IL228382A patent/IL228382A/en active IP Right Grant
-
2014
- 2014-07-31 ZA ZA2014/05681A patent/ZA201405681B/en unknown
- 2014-11-10 US US14/537,184 patent/US9845337B2/en not_active Expired - Fee Related
-
2017
- 2017-11-08 US US15/807,066 patent/US10280193B2/en active Active
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |