CA2710149A1 - C20-c21 substituted glucocorticoid receptor agonists - Google Patents

C20-c21 substituted glucocorticoid receptor agonists Download PDF

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Publication number
CA2710149A1
CA2710149A1 CA2710149A CA2710149A CA2710149A1 CA 2710149 A1 CA2710149 A1 CA 2710149A1 CA 2710149 A CA2710149 A CA 2710149A CA 2710149 A CA2710149 A CA 2710149A CA 2710149 A1 CA2710149 A1 CA 2710149A1
Authority
CA
Canada
Prior art keywords
aryl
alkyl
heteroaryl
formula
haloalkyl
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
CA2710149A
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
Hongwu Wang
Yeon-Hee Lim
Yoon Joo Lee
Rema Danielle Bitar
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 and 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 CA2710149A1 publication Critical patent/CA2710149A1/en
Abandoned legal-status Critical Current

Links

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
    • 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
    • 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
    • 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
    • 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
    • A61P5/38—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)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2710149A 2007-12-21 2008-12-18 C20-c21 substituted glucocorticoid receptor agonists Abandoned CA2710149A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1613507P 2007-12-21 2007-12-21
US61/016,135 2007-12-21
PCT/US2008/087300 WO2009085879A2 (en) 2007-12-21 2008-12-18 C20-c21 substituted glucocorticoid receptor agonists

Publications (1)

Publication Number Publication Date
CA2710149A1 true CA2710149A1 (en) 2009-07-09

Family

ID=40532554

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2710149A Abandoned CA2710149A1 (en) 2007-12-21 2008-12-18 C20-c21 substituted glucocorticoid receptor agonists

Country Status (11)

Country Link
US (1) US8524697B2 (enExample)
EP (1) EP2245042A1 (enExample)
JP (1) JP2011507878A (enExample)
CN (1) CN101970452A (enExample)
AR (1) AR069804A1 (enExample)
CA (1) CA2710149A1 (enExample)
CL (1) CL2008003803A1 (enExample)
MX (1) MX2010007023A (enExample)
PE (1) PE20091525A1 (enExample)
TW (1) TW200944540A (enExample)
WO (1) WO2009085879A2 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2008003802A1 (es) * 2007-12-21 2010-02-19 Schering Corp Compuestos derivados de tioeteres c-21, agonistas del receptor de glucocorticoide; composicion farmaceutica; y uso para el tratamiento o profilaxis de una enfermedad o afeccion inmune, autoinmune o inflamatoria, tales como artritis reumatoide y esclerosis multiple.
RU2420270C2 (ru) * 2009-07-20 2011-06-10 Государственное образовательное учреждение высшего профессионального образования "Северо-Осетинская государственная медицинская академия" Федерального агентства по здравоохранению и социальному развитию Способ лечения рецидивирующего обструктивного бронхита у детей
EP2993178A1 (en) * 2009-09-11 2016-03-09 CHIESI FARMACEUTICI S.p.A. Glucocorticoid condensed in position 16,17 with an isoxazolidine group
CN103087137A (zh) * 2011-11-07 2013-05-08 天津金耀集团有限公司 一种21位为硫代烃基的糖皮质激素
UA111867C2 (uk) * 2011-11-11 2016-06-24 Аллерган, Інк. ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ І СПОСІБ ЗАСТОСУВАННЯ ПОХІДНИХ 4-ПРЕГНЕН-11β-17-21-ТРІОЛ-3,20-ДІОНУ
US20150376225A1 (en) * 2013-01-23 2015-12-31 Sphaera Pharma Pvtd. Ltd. Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion
GB201320091D0 (en) * 2013-11-14 2014-01-01 Univ Manchester Selective glucocorticoid receptor ligands
US10618933B2 (en) 2014-07-23 2020-04-14 Epirium Bio Inc. Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
PE20190622A1 (es) 2016-06-02 2019-04-26 Abbvie Inc Agonista del receptor de glucocorticoides e inmunoconjugados del mismo
KR20250114431A (ko) * 2016-11-08 2025-07-29 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
WO2018097149A1 (ja) * 2016-11-24 2018-05-31 帝人ファーマ株式会社 スルフィド化合物の製造方法
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
MY197688A (en) 2017-07-24 2023-07-05 Regeneron Pharma Anti-cd8 antibodies and uses thereof
IL313068A (en) 2017-11-07 2024-07-01 Regeneron Pharma Hydrophilic linkers for antibody drug conjugates
MA49796A (fr) 2017-12-01 2020-06-03 Abbvie Inc Agoniste du récepteur des glucocorticoïdes et immunoconjugués de celui-ci
CN111465399A (zh) * 2017-12-01 2020-07-28 艾伯维公司 抗cd40抗体药物结合物
IL275757B2 (en) 2018-01-08 2025-08-01 Regeneron Pharma Steroids and antibody-conjugates thereof
MX2020011546A (es) 2018-05-09 2021-01-29 Regeneron Pharma Anticuerpos anti-msr1 y metodos de uso de los mismos.
CN112851743A (zh) * 2019-11-27 2021-05-28 重庆华邦胜凯制药有限公司 一种氧化杂质的制备方法
CN112876531A (zh) * 2019-11-29 2021-06-01 重庆华邦胜凯制药有限公司 一种合成地奈德杂质的方法
TWI899455B (zh) 2021-03-23 2025-10-01 美商美國禮來大藥廠 糖皮質素受體激動劑
AR125084A1 (es) 2021-03-23 2023-06-07 Lilly Co Eli Agonistas del receptor de glucocorticoides novedosos
AR125079A1 (es) 2021-03-23 2023-06-07 Lilly Co Eli Agonistas de receptores de glucocorticoides sustituidos con carboxi
CN114702543B (zh) * 2022-04-19 2023-08-22 中国药科大学 Clascoterone衍生物或其可药用的盐及其制备方法和用途
CN115430392B (zh) * 2022-08-31 2024-04-16 江苏诺盟化工有限公司 一种苯偶酰的制备方法及专用文丘里喷射器

Family Cites Families (14)

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US1119082A (en) * 1914-03-16 1914-12-01 George A Inman Protector-plate.
US3020275A (en) * 1960-06-07 1962-02-06 American Cyanamid Co 21-nitrogen substituted steroids of the pregnane series and methods of preparing the same
GB1119082A (en) * 1966-07-11 1968-07-10 Lepetit Spa New steroids
DE1300940B (de) * 1966-10-13 1969-08-14 Hoechst Ag Verfahren zur Herstellung von Tetrahydropyranylaethern von Steroiden
US4188385A (en) * 1978-04-05 1980-02-12 Syntex (U.S.A.) Inc. Thioetianic acid derivatives
US4861765A (en) * 1985-06-26 1989-08-29 Jouveinal 21-alkyl-, cycloalkyl- or aryl-substituted thio steroids and pharmaceutical compositions containing them
ZA866097B (en) * 1985-09-12 1988-03-30 Upjohn Co 20-and 21-amino steroids
JP2659279B2 (ja) * 1993-05-17 1997-09-30 アルコン ラボラトリーズ，インコーポレイテッド 眼科用抗炎症化合物
US5420120A (en) * 1993-12-17 1995-05-30 Alcon Laboratories, Inc. Anti-inflammatory glucocorticoid compounds for topical ophthalmic use
EP2067784A3 (en) * 2000-08-05 2012-08-22 Glaxo Group Limited 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivatives as anti-inflammatory agents
ATE303398T1 (de) * 2000-11-03 2005-09-15 Univ Manchester Selektive glucocorticoid rezeptor agonisten
RU2008100237A (ru) 2005-06-14 2009-07-20 Джилид Сайэнс, Инк. (US) ОБЩИЕ ПРОЛЕКАРСТВЕННЫЕ ФОРМЫ СТЕРОИДОВ И β-АГОНИСТОВ (ВАРИАНТЫ), ВКЛЮЧАЮЩИЙ ИХ АЭРОЗОЛЬНЫЙ СОСТАВ (ВАРИАНТЫ) И СПОСОБ ПРЕДОТВРАЩЕНИЯ И/ИЛИ ЛЕЧЕНИЯ ЛЕГОЧНЫХ ВОСПАЛЕНИЙ И/ИЛИ БРОНХОСТЕНОЗА С ИХ ПОМОЩЬЮ
CL2008003802A1 (es) 2007-12-21 2010-02-19 Schering Corp Compuestos derivados de tioeteres c-21, agonistas del receptor de glucocorticoide; composicion farmaceutica; y uso para el tratamiento o profilaxis de una enfermedad o afeccion inmune, autoinmune o inflamatoria, tales como artritis reumatoide y esclerosis multiple.
US8916136B2 (en) * 2010-04-23 2014-12-23 Indian Institute Of Technology Bombay Glucose biosensor system coupled with an anti-inflammatory module and methods for using the same

Also Published As

Publication number Publication date
US8524697B2 (en) 2013-09-03
JP2011507878A (ja) 2011-03-10
US20110182828A1 (en) 2011-07-28
CL2008003803A1 (es) 2010-02-19
AR069804A1 (es) 2010-02-17
TW200944540A (en) 2009-11-01
CN101970452A (zh) 2011-02-09
EP2245042A1 (en) 2010-11-03
WO2009085879A2 (en) 2009-07-09
MX2010007023A (es) 2010-09-30
PE20091525A1 (es) 2009-09-25

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20141218