AR076036A1 - Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides - Google Patents

Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides

Info

Publication number
AR076036A1
AR076036A1 ARP100101086A ARP100101086A AR076036A1 AR 076036 A1 AR076036 A1 AR 076036A1 AR P100101086 A ARP100101086 A AR P100101086A AR P100101086 A ARP100101086 A AR P100101086A AR 076036 A1 AR076036 A1 AR 076036A1
Authority
AR
Argentina
Prior art keywords
indazol
naphtho
hydroxy
carbonyl
tetradecahydrocyclopenta
Prior art date
Application number
ARP100101086A
Other languages
English (en)
Inventor
Hakan Bladh
Balint Gabos
Peter Hansen
Frank Burkamp
Original Assignee
Astrazeneca Ab
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
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR076036A1 publication Critical patent/AR076036A1/es

Links

Classifications

    • 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)

Landscapes

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

Abstract

Composiciones farmacéuticas que los contienen y su uso en terapia. Reivindicacion 1: Un compuesto caracterizado porque se elige entre el grupo que consiste en: metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-1-{[(2-hidroxietil)sulfanil]carbonil}-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (R)/(S) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (R)/(S) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2S)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aR,10bS,11S,12aS)-7-(4-fluorofenil)-11-hidroxi-1-{[(2-hidroxietil)sulfanil]ccarbonil}-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[cianometiloxi]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[cianometiloxi}carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, furan-2-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, furan-2-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3a5,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil}carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, y metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, o una de sus sales farmacéuticamente aceptables.
ARP100101086A 2009-04-03 2010-03-31 Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides AR076036A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16632509P 2009-04-03 2009-04-03

Publications (1)

Publication Number Publication Date
AR076036A1 true AR076036A1 (es) 2011-05-11

Family

ID=42826695

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101086A AR076036A1 (es) 2009-04-03 2010-03-31 Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides

Country Status (28)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20100087147A (ko) * 2007-10-04 2010-08-03 아스트라제네카 아베 글루코코르티코이드 활성을 갖는 스테로이드성 [3,2-ｃ]피라졸 화합물
JP2011507836A (ja) * 2007-12-20 2011-03-10 アストラゼネカ・アクチエボラーグ グルココルチコステロイド受容体アゴニストとして作用するステロイド誘導体
UY32523A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
UY32521A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Combinación para emplear en el tratamiento de enfermedades respiratorias
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
JP7146750B2 (ja) 2016-10-14 2022-10-04 ヴァン アンデル リサーチ インスティテュート 非常に強力な糖質コルチコイドの構造およびデザインのための機構

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB933868A (en) 1958-12-08 1963-08-14 American Cyanamid Co Process for fluorinating steroids
US3129218A (en) 1961-11-01 1964-04-14 Merck & Co Inc 2-alkoxymethylene steroids of the androstane and pregnane series
US3072639A (en) 1962-03-05 1963-01-08 Merck & Co Inc 16-oxygenated-4-pregneno-[3, 2-c] pyrazoles and process of preparing them
US3129281A (en) * 1962-09-25 1964-04-14 George W Hardin Electric fence insulator and post
US3364203A (en) 1965-09-09 1968-01-16 Syntex Corp 6, 7-methylene and 6, 7-halomethylene pyrazole pregnanes and processes for their preparation
US3471477A (en) 1967-10-18 1969-10-07 Syntex Corp 6-gem-difluoro (3,2-c) and (2,3-d) pyrazole steroids
DE2727367A1 (de) 1977-06-14 1979-01-04 Schering Ag Neue kortikoide
DE2735110A1 (de) 1977-08-04 1979-02-15 Hoechst Ag Corticoid-17-alkylcarbonate und verfahren zu ihrer herstellung
DE2817988A1 (de) 1978-04-25 1979-11-08 Hoechst Ag Corticoid 17-alkylcarbonate und verfahren zu deren herstellung
JPS6067495A (ja) 1983-09-22 1985-04-17 Ota Seiyaku Kk ピラゾール誘導体
SE8306370D0 (sv) 1983-11-18 1983-11-18 Draco Ab Novel androstane-17beta-carboxylic acid esters, a process and intermediates for their preparation, compositions and method for the treatment of inflammatory conditions
WO1994025478A1 (en) 1993-04-29 1994-11-10 Instytut Farmaceutyczny 16α,17α-ACETAL GLUCOCORTICOSTEROIDAL DERIVATIVES
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
PL194689B1 (pl) 1996-02-13 2007-06-29 Astrazeneca Uk Ltd Pochodne chinazoliny, ich kompozycje farmaceutyczne oraz ich zastosowania
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
NZ522074A (en) 2000-05-31 2004-06-25 Astrazeneca Ab Indole derivatives with vascular damaging activity
MXPA02012905A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como agentes de dano vascular..
IL153325A0 (en) 2000-07-07 2003-07-06 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors
GB0110411D0 (en) 2001-04-27 2001-06-20 Astrazeneca Ab Chemical process
US7291608B2 (en) * 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
ITMI20022606A1 (it) 2002-12-09 2004-06-10 Farmabios Spa Processo di sintesi di steroidi polialogenati.
WO2005028495A1 (en) 2003-09-24 2005-03-31 Glaxo Group Limited Anti-inflammatory glucocorticoids
WO2005063777A1 (en) 2003-12-23 2005-07-14 Corus Pharma Benzylphosphate and substituted benzylphosphate prodrugs for the treatment of pulmonary inflammation
GB0507165D0 (en) 2005-04-08 2005-05-18 Glaxo Group Ltd Novel crystalline pharmaceutical product
WO2007054974A2 (en) 2005-09-28 2007-05-18 Arch Pharmalab Limited A green chemistry process for the preparation of pregnadiene esters
KR20100087147A (ko) * 2007-10-04 2010-08-03 아스트라제네카 아베 글루코코르티코이드 활성을 갖는 스테로이드성 [3,2-ｃ]피라졸 화합물
JP2011507836A (ja) 2007-12-20 2011-03-10 アストラゼネカ・アクチエボラーグ グルココルチコステロイド受容体アゴニストとして作用するステロイド誘導体
US20110262368A1 (en) 2007-12-21 2011-10-27 Schering Corporation C21 thioethers as glucocorticoid receptor agonists
WO2009108118A1 (en) 2008-02-27 2009-09-03 Astrazeneca Ab 16 alpha, 17 alpa-acetal glucocorticosteroidal derivatives and their use
UY32521A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Combinación para emplear en el tratamiento de enfermedades respiratorias
UY32525A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
UY32523A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides

Also Published As

Publication number Publication date
EP2414377B1 (en) 2016-01-06
NI201100176A (es) 2012-06-14
JP5739868B2 (ja) 2015-06-24
UA105920C2 (uk) 2014-07-10
ZA201108049B (en) 2014-08-27
TW201040197A (en) 2010-11-16
UY32520A (es) 2010-10-29
WO2010114476A1 (en) 2010-10-07
IL214982A0 (en) 2011-11-30
BRPI1013380A2 (pt) 2016-03-29
JP2012522768A (ja) 2012-09-27
KR20120002984A (ko) 2012-01-09
CO6420349A2 (es) 2012-04-16
CN102459305A (zh) 2012-05-16
US20100256103A1 (en) 2010-10-07
EP2414377A1 (en) 2012-02-08
SG174249A1 (en) 2011-10-28
ECSP11011369A (es) 2011-11-30
EA021342B1 (ru) 2015-05-29
EP2414377A4 (en) 2012-09-19
KR101599574B1 (ko) 2016-03-04
CL2011002463A1 (es) 2012-04-09
CN102459305B (zh) 2015-03-25
ES2568665T3 (es) 2016-05-03
AU2010233020B2 (en) 2012-11-15
US8338587B2 (en) 2012-12-25
CR20110519A (es) 2011-11-07
PE20120644A1 (es) 2012-06-24
MX2011010208A (es) 2011-10-14
AU2010233020A1 (en) 2011-10-20
EA201190236A1 (ru) 2012-04-30
CA2757424A1 (en) 2010-10-07
TWI472533B (zh) 2015-02-11
CU20110185A7 (es) 2012-02-15
DOP2011000304A (es) 2011-10-31
HN2011002578A (es) 2014-09-29

Similar Documents

Publication Publication Date Title
AR076036A1 (es) Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides
UY31375A1 (es) Derivados sustituidos de (1r, 3as, 3bs, 10ar, 10bs, 11s, 12as)-11-hidroxi-10a, 12a-dimetil-1,2,3,3a,3b, 4,5,7,10,10a,10b, 11,12, 12a tetradecahidrociclopenta [5,6] nafto[1,2-f]indazol-1-il esteres, sus sales farmacéuticamente aceptables, composicione
ECSP13012788A (es) Derivados de biciclo[3,2,1]octilamida y sus usos
GT201700044A (es) Derivados de imidazol pentacíclicos fusionados
CY1115991T1 (el) Φαρμακευτικη ψεκαζομενη συνθεση που περιλαμβανει ενα αναλογο της βιταμινης d προϊον και ενα κορτικοστεροειδες
JO3670B1 (ar) ملح سكسينات من 7-سيكلوبنتيل -2- (5-بيبرازين-1-يل-بيريدين-2-يل أمينو) -7h-بيرولو [2، 3-d] بيريميدين -6-ثنائي ميثيل أميد حمض الكربوكسيل وعمليات تصنيعه
ECSP13012678A (es) Antagonistas de mdm2 de espiro-oxindol
ECSP11011257A (es) Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata
PE20191710A1 (es) Modulador del receptor de androgeno y usos de este
PL2809307T3 (pl) Plaster farmaceutyczny do podawania przezskórnego (1r,4r)-6'-fluoro-N,N-dimetylo-4-fenylo-4',9'-dihydro-3'H-spiro[cykloheksano-1,1'-pirano[3,4-b]indolo]-4-aminy
MX2013001989A (es) Composicion que comprende compuestos tetraciclicos.
AR105592A1 (es) b-AMINOÁCIDOS b-SUSTITUIDOS Y ANÁLOGOS COMO AGENTES QUIMIOTERAPÉUTICOS Y USOS DE LOS MISMOS
MX2013001402A (es) Proceso para preparar tubulisinas.
MX2014004960A (es) Composiciones liposomales combinadas para terapia contra el cancer.
PE20151205A1 (es) Formulaciones que contienen linaclotida para administracion oral
UY33201A (es) Compuestos de pirazol como antagonistas de crth2.
EP3110429A4 (en) Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods
RU2014119713A (ru) Комбинирование лечения рака
MX2021009439A (es) Derivados de imidazo [2,1-f] [1,2,4] triazin-4-amina como agonista de tlr7.
CL2011003046A1 (es) Composicion farmaceutica que comprende 7-(2,5-dihidro-4-imidazo[1,2-a]-piridin-3-il-2,5-dioxo-1h-pirrol-3-il)-9-fluoro-1,2,3,4-tetrahidro-2-(1-piperidinil-carbonil)pirrolo[3,2,1-jk] [1,4]benzodiazepina, una sal o solvato, sbe7-b-cd y opcionalmente un tampon; proceso de preparacion; util para tratar cancer (div. sol. 1848-08).
GT201200304A (es) Composiciones farmacéuticas que comprenden hidromorfona y naloxona
ECSP19026973A (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia
ECSP14013155A (es) 1-piperazino-3-fenil-indanos deuterados para el tratamiento de esquizofrenia
CO7111279A2 (es) Composiciones farmacéuticas orales estables de liberación inmediata que contienen prasugrel
CY1119777T1 (el) Φαρμακευτικη συνθεση περιλαμβανουσα (1r,4r)-6'-φθοpo-n,n-διμεθυλ-4-φαινυλ-4',9'διυδρο-3'h-σπειρο[κυκλοεξανο-1,1'-πυρανο[3,4,β]ινδολ]-4-αμινη και γκαμπαπεντινοειδες

Legal Events

Date Code Title Description
FB Suspension of granting procedure