JP2011507878A - Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト - Google Patents

Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト Download PDF

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Publication number
JP2011507878A
JP2011507878A JP2010539762A JP2010539762A JP2011507878A JP 2011507878 A JP2011507878 A JP 2011507878A JP 2010539762 A JP2010539762 A JP 2010539762A JP 2010539762 A JP2010539762 A JP 2010539762A JP 2011507878 A JP2011507878 A JP 2011507878A
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Japan
Prior art keywords
heteroaryl
fused
alkyl
aryl
formula
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Pending
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JP2010539762A
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English (en)
Japanese (ja)
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JP2011507878A5 (enExample
Inventor
ジョン シー． アンテス，
ケビン ディー． マッコルミック，
ジョン エー． ヘイ，
ロバート ジー． アスラニアン，
プラッカットル ジェイ． ビジュ，
マイケル ワイ． ベルリン，
ダニエル エム． ソロモン，
ホンウ ワン，
ヨン−ヒー リム，
ユーン チョー リー，
レマ ダニエル ビター，
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Merck Sharp and Dohme LLC
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Schering Corp
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Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of JP2011507878A publication Critical patent/JP2011507878A/ja
Publication of JP2011507878A5 publication Critical patent/JP2011507878A5/ja
Pending legal-status Critical Current

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    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (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)
JP2010539762A 2007-12-21 2008-12-18 Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト Pending JP2011507878A (ja)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
JP2011507878A true JP2011507878A (ja) 2011-03-10
JP2011507878A5 JP2011507878A5 (enExample) 2013-01-24

Family

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Family Applications (1)

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JP2010539762A Pending JP2011507878A (ja) 2007-12-21 2008-12-18 Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト

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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011507879A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル
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
KR20240025695A (ko) * 2016-11-08 2024-02-27 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체

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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
JP2013504524A (ja) * 2009-09-11 2013-02-07 シエシー ファルマセウティチィ ソシエタ ペル アチオニ イソオキサゾリジン誘導体
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
UA116622C2 (uk) * 2011-11-11 2018-04-25 Аллерган, Інк. Похідні 4-прегенен-11ss-17-21-тріол-3,20-діону для лікування хвороб очей
JP2016505038A (ja) * 2013-01-23 2016-02-18 スファエラ ファーマ プライベート リミテッド ミトコンドリア生合成ならびにミトコンドリア機能不全または欠乏に関連する疾患において使用するための１１β−ヒドロキシステロイドの新規の化合物
GB201320091D0 (en) * 2013-11-14 2014-01-01 Univ Manchester Selective glucocorticoid receptor ligands
CN106714770B (zh) 2014-07-23 2024-04-19 斯法尔制药私人有限公司 羟基类固醇化合物、其中间体、制备方法、组合物及其用途
ES2877548T3 (es) 2016-06-02 2021-11-17 Abbvie Inc Agonista del receptor de glucocorticoides e inmunoconjugados del mismo
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
KR102880156B1 (ko) 2017-07-24 2025-11-05 리제너론 파마슈티칼스 인코포레이티드 항cd8 항체 및 이의 용도
CA3080857A1 (en) 2017-11-07 2019-05-16 Regeneron Pharmaceuticals, Inc. Hydrophilic linkers for antibody drug conjugates
AU2018374634A1 (en) 2017-12-01 2020-05-28 Abbvie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
RU2020117156A (ru) * 2017-12-01 2022-01-04 Эббви Инк. Конъюгаты анти-cd40 антитела и лекарственного средства
EA202091672A1 (ru) 2018-01-08 2021-02-01 Регенерон Фармасьютикалз, Инк. Стероиды и их антитело-конъюгаты
WO2019217591A1 (en) 2018-05-09 2019-11-14 Regeneron Pharmaceuticals, Inc. Anti-msr1 antibodies and methods of use thereof
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
AR125084A1 (es) 2021-03-23 2023-06-07 Lilly Co Eli Agonistas del receptor de glucocorticoides novedosos
PE20240889A1 (es) 2021-03-23 2024-04-24 Lilly Co Eli Agonistas del receptor de glucocorticoides
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

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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
US3598816A (en) * 1966-10-13 1971-08-10 Hoechst Ag Tetrahydropyranylethers of steroids and process for their manufacture
JPS54141758A (en) * 1978-04-05 1979-11-05 Syntex Inc Thioetianic acid derivative
JPS63500868A (ja) * 1985-09-12 1988-03-31 ジ・アップジョン・カンパニ− アミノステロイド
JPH08501804A (ja) * 1993-05-17 1996-02-27 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
WO2002036606A1 (en) * 2000-11-03 2002-05-10 Matrix Therapeutics Limited Selective glucocorticoid receptor agonists
JP2004505990A (ja) * 2000-08-05 2004-02-26 グラクソ　グループ　リミテッド 抗炎症剤としての１７β−カルボチオエート−１７α−アリールカルボニルオキシルオキシアンドロスタン誘導体
JP2008546694A (ja) * 2005-06-14 2008-12-25 コラス・フアーマ・インコーポレイテツド 肺炎及び気管支の治療のためのステロイド及びβ−アゴニストの相互プロドラッグとしての置換されたフェニルホスファート
JP2011507879A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル

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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
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

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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
US3598816A (en) * 1966-10-13 1971-08-10 Hoechst Ag Tetrahydropyranylethers of steroids and process for their manufacture
JPS54141758A (en) * 1978-04-05 1979-11-05 Syntex Inc Thioetianic acid derivative
JPS63500868A (ja) * 1985-09-12 1988-03-31 ジ・アップジョン・カンパニ− アミノステロイド
JPH08501804A (ja) * 1993-05-17 1996-02-27 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
JP2004505990A (ja) * 2000-08-05 2004-02-26 グラクソ　グループ　リミテッド 抗炎症剤としての１７β−カルボチオエート−１７α−アリールカルボニルオキシルオキシアンドロスタン誘導体
WO2002036606A1 (en) * 2000-11-03 2002-05-10 Matrix Therapeutics Limited Selective glucocorticoid receptor agonists
JP2008546694A (ja) * 2005-06-14 2008-12-25 コラス・フアーマ・インコーポレイテツド 肺炎及び気管支の治療のためのステロイド及びβ−アゴニストの相互プロドラッグとしての置換されたフェニルホスファート
JP2011507879A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル

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JPN6013038003; Ｊｏｕｒｎａｌ　ｏｆ　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　ａｎｄ　Ｂｉｏｍｅｄｉｃａｌ　Ａｎａｌｙｓｉｓ １７, 1998, １０２９-１０３６ *
JPN6013038005; Ｂｉｏｃｈｅｍｉｓｔｒｙ １８（２２）, 1979, ４９１５-４９２２ *
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JPN6013038009; Ｃｈｅｍｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ ３７（１２）, 1989, ３２８６-３２９３ *
JPN6013038012; Ｊｏｕｒｎａｌ　ｏｆ　ｔｈｅ　Ｃｈｅｍｉｃａｌ　Ｓｏｃｉｅｔｙ ２６, 1961, ５０５２-５０５４ *
JPN6013038014; Ｊｏｕｒｎａｌ　ｏｆ　Ｓｔｅｒｏｉｄ　Ｂｉｏｃｈｅｍｉｓｔｒｙ ３３（４Ａ）, 1989, ５５７-５６３ *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011507879A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル
KR20240025695A (ko) * 2016-11-08 2024-02-27 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
KR102835535B1 (ko) * 2016-11-08 2025-07-18 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

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Publication number Publication date
TW200944540A (en) 2009-11-01
AR069804A1 (es) 2010-02-17
CL2008003803A1 (es) 2010-02-19
US20110182828A1 (en) 2011-07-28
US8524697B2 (en) 2013-09-03
PE20091525A1 (es) 2009-09-25
WO2009085879A2 (en) 2009-07-09
CN101970452A (zh) 2011-02-09
CA2710149A1 (en) 2009-07-09
EP2245042A1 (en) 2010-11-03
MX2010007023A (es) 2010-09-30

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