[go: up one dir, main page]

PE20120894A1 - Derivados de isoxazolidina - Google Patents

Derivados de isoxazolidina

Info

Publication number
PE20120894A1
PE20120894A1 PE2012000303A PE2012000303A PE20120894A1 PE 20120894 A1 PE20120894 A1 PE 20120894A1 PE 2012000303 A PE2012000303 A PE 2012000303A PE 2012000303 A PE2012000303 A PE 2012000303A PE 20120894 A1 PE20120894 A1 PE 20120894A1
Authority
PE
Peru
Prior art keywords
hydroxy
halogen
isoxazolidine
compounds
fenantren
Prior art date
Application number
PE2012000303A
Other languages
English (en)
Inventor
Elisabetta Armani
Elonora Ghidini
Ilaria Peretto
Andrea Virdis
Original Assignee
Chiesi Farma Spa
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41666572&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20120894(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiesi Farma Spa filed Critical Chiesi Farma Spa
Publication of PE20120894A1 publication Critical patent/PE20120894A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036Nitrogen-containing hetero ring
    • C07J71/0057Nitrogen and oxygen
    • C07J71/0068Nitrogen and oxygen at position 16(17)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44Glucocorticosteroids; 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE ISOXAZOLIDINA DE FORMULA (I) DONDE R1 ES (CH2)n-Z-(CH2)n'-R4, EN DONDE n Y n' SON CADA UNO DE 0 A 2; Z ES UNA UNION SIMPLE, S, O, CO, ENTRE OTROS; R4 ES H, HALOGENO, OH, CN, ARILALQUILO(C1-C6), ENTRE OTROS; R2 ES H, ALQUILO(C2-C6), (CH2)mR5, ENTRE OTROS, EN DONDE R5 ES HETEROARILO OPCIONALMENTE SUSTITUIDO CON OXO, OH, HALOGENO, CN, ENTRE OTROS; m ES DE 0 A 6; X E Y SON CADA UNO H O HALOGENO. SON COMPUESTOS PREFERIDOS: (4aR,4bS,5S,6aS,6bR,9aS,10aS,10bS)-8-FURAN-3-ILMETIL-5-HIDROXI-6b-(2-HIDROXI-ACETIL)-4a,6a-DIMETIL-4a,4b,5,6,6a,6b,8,9,9a,10,10a,10b,11,12-TETRADECAHIDRO-7-OXA-8-AZA-PENTALENO[2,1-a]FENANTREN-2-ONA; (4aS,4bR,5S,6aS,6bR,9aS,10aS,10bS,12S)-4b,12-DIFLUORO-8-FURAN-2-ILMETIL-5-HIDROXI-6b-(2-HIDROXI-ACETIL)-4a,6a-DIMETIL-4a,4b,5,6,6a,6b,8,9,9a,10,10a,10b,11,12-TETRADECAHIDRO-7-OXA-8-AZA-PENTALENO[2,1-a]FENANTREN-2-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON GLUCOCORTICOIDES SIENDO UTILES EN EL TRATAMIENTO DE ASMA, BRONQUITIS CRONICA, ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA
PE2012000303A 2009-09-11 2010-09-01 Derivados de isoxazolidina PE20120894A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09011665 2009-09-11

Publications (1)

Publication Number Publication Date
PE20120894A1 true PE20120894A1 (es) 2012-08-13

Family

ID=41666572

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000303A PE20120894A1 (es) 2009-09-11 2010-09-01 Derivados de isoxazolidina

Country Status (27)

Country Link
US (1) US8637662B2 (es)
EP (2) EP2993178A1 (es)
JP (1) JP2013504524A (es)
KR (1) KR101451486B1 (es)
CN (2) CN102482318B (es)
AR (2) AR078164A1 (es)
AU (1) AU2010294598B2 (es)
BR (1) BR112012005503B1 (es)
CA (1) CA2773594C (es)
CL (1) CL2012000450A1 (es)
CO (1) CO6511204A2 (es)
EA (1) EA025191B1 (es)
GE (1) GEP20146135B (es)
IL (1) IL218539A (es)
JO (1) JO3760B1 (es)
MA (1) MA33561B1 (es)
ME (1) ME01331B (es)
MX (1) MX2012002967A (es)
MY (1) MY164842A (es)
NZ (1) NZ598662A (es)
PE (1) PE20120894A1 (es)
SG (2) SG10201608490VA (es)
TN (1) TN2012000077A1 (es)
TW (1) TWI494318B (es)
UA (1) UA108858C2 (es)
WO (1) WO2011029547A2 (es)
ZA (1) ZA201201705B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP2686332A2 (en) * 2011-03-15 2014-01-22 Chiesi Farmaceutici S.p.A. Isoxazolidine 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
SI3231444T1 (sl) 2014-05-12 2020-04-30 Verona Pharma Plc Novo zdravljenje
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
CN109206471B (zh) * 2017-06-30 2022-07-12 天津药业研究院股份有限公司 一种哈西奈德的制备方法
CN109575096B (zh) * 2019-01-20 2021-01-01 湖南科瑞生物制药股份有限公司 一种制备16a-羟基泼尼松龙产品的新方法
CN112142820A (zh) * 2019-06-29 2020-12-29 天津药业研究院股份有限公司 曲安奈德的合成方法
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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1131213B (de) * 1958-06-13 1962-06-14 Syntex Sa Verfahren zur Herstellung neuer Pregnanverbindungen
US3048581A (en) * 1960-04-25 1962-08-07 Olin Mathieson Acetals and ketals of 16, 17-dihydroxy steroids
BR6678983D0 (pt) * 1965-05-04 1973-09-18 Merck & Co Inc Processo para preparar 21-fosfato esteroides
SE307576B (es) * 1966-01-27 1969-01-13 Bofors Ab
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
GB1302572A (es) * 1969-05-05 1973-01-10
US3996359A (en) * 1972-05-19 1976-12-07 Ab Bofors Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith
SE378110B (es) * 1972-05-19 1975-08-18 Bofors Ab
US4018774A (en) * 1976-02-13 1977-04-19 E. R. Squibb & Sons, Inc. Steroidal [16α,17-d]isoxazolidines
DE3133631A1 (de) * 1981-08-21 1983-03-03 Schering Ag, 1000 Berlin Und 4619 Bergkamen Neue kortikoide ihre herstellung und verwendung
US5200518A (en) * 1991-02-21 1993-04-06 Kangweon National University Anti-inflammatory carboxycyclic acetal pregnane derivatives
JP2749778B2 (ja) * 1994-09-05 1998-05-13 日清食品株式会社 トリアムシノロン誘導体
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
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
PE20091525A1 (es) * 2007-12-21 2009-09-25 Schering Corp Agonista del receptor glucocorticoide c-20-c21 sustituido
WO2009108118A1 (en) * 2008-02-27 2009-09-03 Astrazeneca Ab 16 alpha, 17 alpa-acetal glucocorticosteroidal derivatives and their use
PE20120894A1 (es) * 2009-09-11 2012-08-13 Chiesi Farma Spa Derivados de isoxazolidina

Also Published As

Publication number Publication date
CN105175479B (zh) 2017-06-09
KR101451486B1 (ko) 2014-10-22
MY164842A (en) 2018-01-30
HK1166085A1 (zh) 2012-10-19
HK1218759A1 (zh) 2017-03-10
CN105175479A (zh) 2015-12-23
AU2010294598A1 (en) 2012-04-05
EP2475676A2 (en) 2012-07-18
NZ598662A (en) 2014-03-28
BR112012005503A2 (pt) 2016-04-19
TW201114776A (en) 2011-05-01
JP2013504524A (ja) 2013-02-07
CL2012000450A1 (es) 2012-08-10
BR112012005503B1 (pt) 2021-10-13
WO2011029547A2 (en) 2011-03-17
UA108858C2 (xx) 2015-06-25
GEP20146135B (en) 2014-08-11
US20110065678A1 (en) 2011-03-17
TN2012000077A1 (en) 2013-09-19
JO3760B1 (ar) 2021-01-31
CA2773594A1 (en) 2011-03-17
CO6511204A2 (es) 2012-08-31
CN102482318B (zh) 2015-11-25
EP2993178A1 (en) 2016-03-09
KR20120055651A (ko) 2012-05-31
WO2011029547A3 (en) 2011-08-18
ME01331B (me) 2013-12-20
EA201290091A1 (ru) 2012-12-28
MA33561B1 (fr) 2012-09-01
AU2010294598B2 (en) 2016-09-01
EP2475676B1 (en) 2020-05-27
IL218539A0 (en) 2012-05-31
WO2011029547A8 (en) 2011-06-16
IL218539A (en) 2015-09-24
ZA201201705B (en) 2013-05-29
TWI494318B (zh) 2015-08-01
US8637662B2 (en) 2014-01-28
MX2012002967A (es) 2012-04-30
AR078164A1 (es) 2011-10-19
CN102482318A (zh) 2012-05-30
AR118123A2 (es) 2021-09-22
EA025191B1 (ru) 2016-11-30
SG179055A1 (en) 2012-04-27
CA2773594C (en) 2018-09-25
SG10201608490VA (en) 2016-11-29

Similar Documents

Publication Publication Date Title
PE20120894A1 (es) Derivados de isoxazolidina
CO2022002729A2 (es) Métodos de tratamiento del cáncer de mama con derivados de tetrahidronaftaleno como degradadores del receptor de estrógenos
AR078622A1 (es) Piperidinas sustituidas que aumentan la actividad de p53 y sus usos
HRP20191443T1 (hr) Antitumorska sjedinjenja
EA201190234A1 (ru) Новые амидные производные стероидных соединений [3,2-c]пиразолов с глюкокортикоидной активностью
AR119018A1 (es) Inhibidores de proteína quinasas dependientes de adn
ECSP099177A (es) Derivados de quinazolinona e isoquinolinona
AR072994A1 (es) Derivados de carbonato de quinuclidina y composicion medicinal de los mismos
PE20040937A1 (es) Derivados de piridazin-3(2h)-ona como inhibidores de fosfodiesterasa-4 (pde 4)
ECSP066911A (es) Polimorfo cristalino de un acetato de bazedoxifeno
JO2787B1 (en) Alternative amide derivatives and methods of use
NZ600430A (en) Spiro-oxindole mdm2 antagonists
CO6321239A2 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
AR070352A1 (es) Derivado de pirrolopirimidina como inhibidor de la enzima pi3k, un procedimiento de elaboracion del compuesto, una composicion farmaceutica y un agente preventivo o terapeutico en base al compuesto.
AR076731A1 (es) Prostamidas donadoras de oxido nitrico, uso de los mismos y composiciones farmaceuticas
EA201201170A1 (ru) Гетариламинонафтиридины
TW200616940A (en) Novel hexafluoroisopropanol substituted ether derivatives
PE20091036A1 (es) Derivado de quinolina como antagonista del receptor p2x7
AR081725A1 (es) Derivados de oxadiazol, proceso de preparacion de los mismos, composicion farmaceutica que los contienen y su uso en el tratamiento del cancer
PE20060379A1 (es) Derivados de 4-cicloalcoxibenzonitrilos como moduladores de androgenos
AR060213A1 (es) Compuesto de piperazinil - piridinil -bencensulfonamida , su uso para fabricar un medicamento proceso para la preparacion del mismo composicion farmaceutica que lo comprende y proceso para prepararla
CO5680443A2 (es) Derivados de bencimidazol, composiciones que los contienen, preparacion de los mismos y usos de los mismos
ECSP066910A (es) Polimorfo cristalino de acetato de bazedoxifeno
EA201190236A1 (ru) Новые производные стероидных соединений [3,2-c]пиразолов с глюкокортикоидной активностью
PE20220376A1 (es) Compuestos triciclicos y su uso

Legal Events

Date Code Title Description
FG Grant, registration