JP2011507879A - 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 - Google Patents

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 Download PDF

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Publication number
JP2011507879A
JP2011507879A JP2010539763A JP2010539763A JP2011507879A JP 2011507879 A JP2011507879 A JP 2011507879A JP 2010539763 A JP2010539763 A JP 2010539763A JP 2010539763 A JP2010539763 A JP 2010539763A JP 2011507879 A JP2011507879 A JP 2011507879A
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compound
alkyl
hydrogen
formula
compound according
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JP2010539763A
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Japanese (ja)
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JP2011507879A5 (enExample
Inventor
ジョン シー． アンテス，
ケビン ディー． マッコーミック，
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，
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of JP2011507879A publication Critical patent/JP2011507879A/ja
Publication of JP2011507879A5 publication Critical patent/JP2011507879A5/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
    • 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

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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)
  • 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)
JP2010539763A 2007-12-21 2008-12-18 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 Pending JP2011507879A (ja)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
JP2011507879A true JP2011507879A (ja) 2011-03-10
JP2011507879A5 JP2011507879A5 (enExample) 2012-02-02

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JP2010539763A Pending JP2011507879A (ja) 2007-12-21 2008-12-18 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

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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011507878A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
SG11201810678WA (en) 2016-06-02 2018-12-28 Abbvie Inc Glucocorticoid receptor agonist and immunoconjugates thereof
JP7330101B2 (ja) * 2016-11-08 2023-08-21 レゲネロン ファーマシューティカルス，インコーポレーテッド ステロイド及びそのタンパク質コンジュゲート
MX2019013690A (es) 2017-05-18 2020-01-27 Regeneron Pharma Conjugados de farmaco-proteina con ciclodextrina.
IL313068A (en) 2017-11-07 2024-07-01 Regeneron Pharma Hydrophilic linkers for antibody drug conjugates
US10772970B2 (en) 2017-12-01 2020-09-15 Abbvie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
JP7366028B2 (ja) 2018-01-08 2023-10-20 レゲネロン ファーマシューティカルス，インコーポレーテッド ステロイド及びその抗体コンジュゲート
JP7590871B2 (ja) 2018-05-09 2024-11-27 レゲネロン ファーマシューティカルス，インコーポレーテッド 抗ｍｓｒ１抗体及びその使用方法
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
CN120344545A (zh) * 2022-12-16 2025-07-18 津药生物科技（天津）有限公司 新型糖皮质激素、其制备方法及用途

Citations (6)

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Publication number Priority date Publication date Assignee Title
JPS5030863A (enExample) * 1973-05-30 1975-03-27
JPS6289694A (ja) * 1985-06-26 1987-04-24 Taisho Pharmaceut Co Ltd ２１−置換チオステロイド化合物
US5420120A (en) * 1993-12-17 1995-05-30 Alcon Laboratories, Inc. Anti-inflammatory glucocorticoid compounds for topical ophthalmic use
JPH11501676A (ja) * 1995-12-29 1999-02-09 グラクソ、グループ、リミテッド ２１―（２―オキソテトラヒドロフラン）チオプレグナン誘導体、それらの製造方法、およびそれらを含有した医薬組成物
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
JP2011507878A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト

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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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5030863A (enExample) * 1973-05-30 1975-03-27
JPS6289694A (ja) * 1985-06-26 1987-04-24 Taisho Pharmaceut Co Ltd ２１−置換チオステロイド化合物
US5420120A (en) * 1993-12-17 1995-05-30 Alcon Laboratories, Inc. Anti-inflammatory glucocorticoid compounds for topical ophthalmic use
JPH11501676A (ja) * 1995-12-29 1999-02-09 グラクソ、グループ、リミテッド ２１―（２―オキソテトラヒドロフラン）チオプレグナン誘導体、それらの製造方法、およびそれらを含有した医薬組成物
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
JP2011507878A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト

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JPN6013038017; Ｂｉｏｃｈｅｍｉｓｔｒｙ １８（２２）, 1979, ４９１５-４９２２ *
JPN6013038019; Ｓｔｅｒｏｉｄｓ １８（４）, 1971, ４２１-４３２ *
JPN6013038022; Ｂｉｏｃｈｅｍｉｃａｌ　Ｐｈａｒｍａｃｏｌｏｇｙ １２, 1963, １０８１-１０９０ *
JPN6013038024; Ｊｏｕｒｎａｌ　ｏｆ　ｔｈｅ　Ｃｈｅｍｉｃａｌ　Ｓｏｃｉｅｔｙ ２６, 1961, ５０５２-５０５４ *
JPN6013038026; Ｊｏｕｒｎａｌ　ｏｆ　Ｍｅｄｉｃｉｎａｌ　Ｃｈｅｍｉｓｔｒｙ １２（５）, 1969, ８１０-８１８ *
JPN6013038029; Ｃｈｅｍｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ ３７（７）, 1989, １７９５-１８０１ *
JPN6013038031; Ｃｈｅｍｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ ３７（１２）, 1989, ３２８６-３２９３ *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011507878A (ja) * 2007-12-21 2011-03-10 シェーリング コーポレイション Ｃ２０−ｃ２１置換グルココルチコイド受容体アゴニスト

Also Published As

Publication number Publication date
EP2235035A2 (en) 2010-10-06
WO2009085880A2 (en) 2009-07-09
MX2010007024A (es) 2010-09-30
CA2710240A1 (en) 2009-07-09
US20110262368A1 (en) 2011-10-27
CN102099368A (zh) 2011-06-15
CL2008003802A1 (es) 2010-02-19
AR070040A1 (es) 2010-03-10
WO2009085880A8 (en) 2011-01-27
TW200940070A (en) 2009-10-01
PE20091215A1 (es) 2009-08-14
WO2009085880A3 (en) 2009-09-17

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