EA201190236A1 - Новые производные стероидных соединений [3,2-c]пиразолов с глюкокортикоидной активностью - Google Patents

Новые производные стероидных соединений [3,2-c]пиразолов с глюкокортикоидной активностью

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Publication number
EA201190236A1
EA201190236A1 EA201190236A EA201190236A EA201190236A1 EA 201190236 A1 EA201190236 A1 EA 201190236A1 EA 201190236 A EA201190236 A EA 201190236A EA 201190236 A EA201190236 A EA 201190236A EA 201190236 A1 EA201190236 A1 EA 201190236A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrazols
new derivatives
steroid compounds
glucocorticoid activity
compounds
Prior art date
Application number
EA201190236A
Other languages
English (en)
Other versions
EA021342B1 (ru
Inventor
Хокан Бладх
Франк Буркамп
Балинт Габос
Петер Роберт Хансен
Original Assignee
Астразенека Аб
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.)
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Publication date
Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of EA201190236A1 publication Critical patent/EA201190236A1/ru
Publication of EA021342B1 publication Critical patent/EA021342B1/ru

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    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)

Abstract

Согласно настоящему изобретению предложены указанные соединения формулы (I), фармацевтические композиции, содержащие их, и их применение в терапии.
EA201190236A 2009-04-03 2010-04-01 Стероидное производное с глюкокортикоидной активностью EA021342B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16632509P 2009-04-03 2009-04-03
PCT/SE2010/050367 WO2010114476A1 (en) 2009-04-03 2010-04-01 Novel derivatives of steroidal[3,2-c]pyrazole compounds with glucocorticoid activity

Publications (2)

Publication Number Publication Date
EA201190236A1 true EA201190236A1 (ru) 2012-04-30
EA021342B1 EA021342B1 (ru) 2015-05-29

Family

ID=42826695

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190236A EA021342B1 (ru) 2009-04-03 2010-04-01 Стероидное производное с глюкокортикоидной активностью

Country Status (28)

Country Link
US (1) US8338587B2 (ru)
EP (1) EP2414377B1 (ru)
JP (1) JP5739868B2 (ru)
KR (1) KR101599574B1 (ru)
CN (1) CN102459305B (ru)
AR (1) AR076036A1 (ru)
AU (1) AU2010233020B2 (ru)
BR (1) BRPI1013380A2 (ru)
CA (1) CA2757424A1 (ru)
CL (1) CL2011002463A1 (ru)
CO (1) CO6420349A2 (ru)
CR (1) CR20110519A (ru)
CU (1) CU20110185A7 (ru)
DO (1) DOP2011000304A (ru)
EA (1) EA021342B1 (ru)
EC (1) ECSP11011369A (ru)
ES (1) ES2568665T3 (ru)
HN (1) HN2011002578A (ru)
IL (1) IL214982A0 (ru)
MX (1) MX2011010208A (ru)
NI (1) NI201100176A (ru)
PE (1) PE20120644A1 (ru)
SG (1) SG174249A1 (ru)
TW (1) TWI472533B (ru)
UA (1) UA105920C2 (ru)
UY (1) UY32520A (ru)
WO (1) WO2010114476A1 (ru)
ZA (1) ZA201108049B (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
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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
UY32521A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Combinación para emplear en el tratamiento de enfermedades respiratorias
UY32523A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
UY32525A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
GB201016912D0 (en) 2010-10-07 2010-11-24 Astrazeneca Ab Novel combination
CN104402964B (zh) * 2014-12-10 2016-06-15 南京大学 闭花木酮的o-(咪唑基)乙基衍生物、制备方法及其用途
CN104744556B (zh) * 2015-04-15 2016-06-29 马修尧 闭花木酮的o-(1h-四氮唑基)乙基衍生物、制备方法及其用途
US10954265B2 (en) 2016-10-14 2021-03-23 Van Andel Research Institute Structures and mechanism for the design of highly potent glucocorticoids

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Also Published As

Publication number Publication date
SG174249A1 (en) 2011-10-28
KR20120002984A (ko) 2012-01-09
KR101599574B1 (ko) 2016-03-04
CA2757424A1 (en) 2010-10-07
HN2011002578A (es) 2014-09-29
ES2568665T3 (es) 2016-05-03
AU2010233020B2 (en) 2012-11-15
EA021342B1 (ru) 2015-05-29
ZA201108049B (en) 2014-08-27
PE20120644A1 (es) 2012-06-24
WO2010114476A1 (en) 2010-10-07
JP5739868B2 (ja) 2015-06-24
CN102459305A (zh) 2012-05-16
MX2011010208A (es) 2011-10-14
TWI472533B (zh) 2015-02-11
NI201100176A (es) 2012-06-14
AR076036A1 (es) 2011-05-11
ECSP11011369A (es) 2011-11-30
EP2414377A1 (en) 2012-02-08
CL2011002463A1 (es) 2012-04-09
CO6420349A2 (es) 2012-04-16
UA105920C2 (ru) 2014-07-10
IL214982A0 (en) 2011-11-30
CR20110519A (es) 2011-11-07
US8338587B2 (en) 2012-12-25
UY32520A (es) 2010-10-29
JP2012522768A (ja) 2012-09-27
EP2414377A4 (en) 2012-09-19
TW201040197A (en) 2010-11-16
CN102459305B (zh) 2015-03-25
US20100256103A1 (en) 2010-10-07
AU2010233020A1 (en) 2011-10-20
CU20110185A7 (es) 2012-02-15
DOP2011000304A (es) 2011-10-31
EP2414377B1 (en) 2016-01-06
BRPI1013380A2 (pt) 2016-03-29

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