CA2710240A1 - C-21 thioethers as glucocorticoid receptor agonists - Google Patents

C-21 thioethers as glucocorticoid receptor agonists Download PDF

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Publication number
CA2710240A1
CA2710240A1 CA2710240A CA2710240A CA2710240A1 CA 2710240 A1 CA2710240 A1 CA 2710240A1 CA 2710240 A CA2710240 A CA 2710240A CA 2710240 A CA2710240 A CA 2710240A CA 2710240 A1 CA2710240 A1 CA 2710240A1
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CA
Canada
Prior art keywords
compound
compound according
alkyl
hydrogen
formula
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2710240A
Other languages
English (en)
French (fr)
Inventor
John C. Anthes
Kevin D. Mccormick
John A. Hey
Robert G. Aslanian
Purakkattle J. Biju
Michael Y. Berlin
Daniel M. Solomon
Yoon Joo Lee
Rema Danielle Bitar
Yeon-Hee Lim
Hongwu Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme LLC
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2710240A1 publication Critical patent/CA2710240A1/en
Abandoned legal-status Critical Current

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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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
CA2710240A 2007-12-21 2008-12-18 C-21 thioethers as glucocorticoid receptor agonists Abandoned CA2710240A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1614407P 2007-12-21 2007-12-21
US61/016,144 2007-12-21
PCT/US2008/087301 WO2009085880A2 (en) 2007-12-21 2008-12-18 C-21 thioethers as glucocorticoid receptor agonists

Publications (1)

Publication Number Publication Date
CA2710240A1 true CA2710240A1 (en) 2009-07-09

Family

ID=40513892

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2710240A Abandoned CA2710240A1 (en) 2007-12-21 2008-12-18 C-21 thioethers as glucocorticoid receptor agonists

Country Status (11)

Country Link
US (1) US20110262368A1 (enExample)
EP (1) EP2235035A2 (enExample)
JP (1) JP2011507879A (enExample)
CN (1) CN102099368A (enExample)
AR (1) AR070040A1 (enExample)
CA (1) CA2710240A1 (enExample)
CL (1) CL2008003802A1 (enExample)
MX (1) MX2010007024A (enExample)
PE (1) PE20091215A1 (enExample)
TW (1) TW200940070A (enExample)
WO (1) WO2009085880A2 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101970452A (zh) * 2007-12-21 2011-02-09 先灵公司 C20-c21取代的糖皮质激素受体激动剂
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
RS62040B1 (sr) 2016-06-02 2021-07-30 Abbvie Inc Agonist receptora glukokortikoida i njegovi imunokonjugati
CA3042428A1 (en) * 2016-11-08 2018-05-17 Regeneron Pharmaceuticals, Inc. Steroids and protein-conjugates thereof
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
CA3247730A1 (en) 2017-11-07 2025-10-30 Regeneron Pharmaceuticals, Inc. Hydrophilic linkers for antibody drug conjugates
EP3658192B1 (en) 2017-12-01 2021-04-28 AbbVie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
MA50259A1 (fr) 2018-01-08 2021-07-29 Regeneron Pharma Stéroïdes et leurs conjugués-anticorps
WO2019217591A1 (en) 2018-05-09 2019-11-14 Regeneron Pharmaceuticals, Inc. Anti-msr1 antibodies and methods of use thereof
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
EP4635969A4 (en) * 2022-12-16 2026-06-10 Tianjin Pharmaceutical Biotechnology Co Ltd NEW GLUCOCORTICOID, ITS PREPARATION PROCESS AND ITS USE

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2231374B1 (enExample) * 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
WO1997024367A1 (en) * 1995-12-29 1997-07-10 Glaxo Group Limited 21-(2-oxo-tetrahydrofuran)-thio pregnane derivatives, a process for their production and pharmaceutical compositions containing them
AU2006259604A1 (en) * 2005-06-14 2006-12-28 Gilead Sciences, Inc. Substituted phenylphosphates as mutual prodrugs of steroids and beta -agonists for the treatment of pulmonary inflammation and bronchoconstriction
CN101970452A (zh) * 2007-12-21 2011-02-09 先灵公司 C20-c21取代的糖皮质激素受体激动剂

Also Published As

Publication number Publication date
JP2011507879A (ja) 2011-03-10
MX2010007024A (es) 2010-09-30
WO2009085880A3 (en) 2009-09-17
WO2009085880A2 (en) 2009-07-09
WO2009085880A8 (en) 2011-01-27
TW200940070A (en) 2009-10-01
CN102099368A (zh) 2011-06-15
AR070040A1 (es) 2010-03-10
PE20091215A1 (es) 2009-08-14
EP2235035A2 (en) 2010-10-06
CL2008003802A1 (es) 2010-02-19
US20110262368A1 (en) 2011-10-27

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FZDE Discontinued

Effective date: 20141218