CN101970452A - C20-c21取代的糖皮质激素受体激动剂 - Google Patents

C20-c21取代的糖皮质激素受体激动剂 Download PDF

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Publication number
CN101970452A
CN101970452A CN2008801273812A CN200880127381A CN101970452A CN 101970452 A CN101970452 A CN 101970452A CN 2008801273812 A CN2008801273812 A CN 2008801273812A CN 200880127381 A CN200880127381 A CN 200880127381A CN 101970452 A CN101970452 A CN 101970452A
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CN
China
Prior art keywords
heteroaryl
fused
alkyl
aryl
formula
Prior art date
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Pending
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CN2008801273812A
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English (en)
Chinese (zh)
Inventor
J·C·安瑟斯
K·D·麦科尔米克
J·A·黑
R·G·阿斯拉尼安
P·J·比于
M·Y·伯林
D·M·索罗蒙
王鸿武
林勇希
李勇俊
雷马·丹妮尔·比塔尔
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of CN101970452A publication Critical patent/CN101970452A/zh
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

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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)
  • 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)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (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)
CN2008801273812A 2007-12-21 2008-12-18 C20-c21取代的糖皮质激素受体激动剂 Pending CN101970452A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1613507P 2007-12-21 2007-12-21
US61/016135 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
CN101970452A true CN101970452A (zh) 2011-02-09

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN2008801273812A Pending CN101970452A (zh) 2007-12-21 2008-12-18 C20-c21取代的糖皮质激素受体激动剂

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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN110291097A (zh) * 2016-11-08 2019-09-27 里珍纳龙药品有限公司 类固醇类化合物及其蛋白质-偶联物
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
CN114702543A (zh) * 2022-04-19 2022-07-05 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
CN115430392A (zh) * 2022-08-31 2022-12-06 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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TW200940070A (en) * 2007-12-21 2009-10-01 Schering Corp C-21 thioethers as glucocorticoid receptor agonists
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
CA2773594C (en) * 2009-09-11 2018-09-25 Chiesi Farmaceutici S.P.A. Isoxazolidine derivatives
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
CN105073119A (zh) * 2013-01-23 2015-11-18 司菲埃拉制药私人有限公司 用于线粒体生物发生和与线粒体功能障碍或耗竭相关的疾病的新颖11β-羟基类固醇化合物
GB201320091D0 (en) * 2013-11-14 2014-01-01 Univ Manchester Selective glucocorticoid receptor ligands
WO2016013030A2 (en) 2014-07-23 2016-01-28 Sphaera Pharma Pvt. Ltd. Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
SG10202001787QA (en) 2016-06-02 2020-04-29 Abbvie Inc Glucocorticoid receptor agonist and immunoconjugates thereof
TW201825456A (zh) * 2016-11-24 2018-07-16 日商帝人製藥股份有限公司 硫醚化合物的製造方法
JP7364471B2 (ja) 2017-05-18 2023-10-18 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 シクロデキストリンタンパク質薬物コンジュゲート
IL316355A (en) 2017-07-24 2024-12-01 Regeneron Pharma Anti-CD8 antibodies and their uses
AU2018365946B2 (en) 2017-11-07 2025-08-28 Regeneron Pharmaceuticals, Inc. Hydrophilic linkers for antibody drug conjugates
MX2020005465A (es) * 2017-12-01 2020-09-07 Abbvie Inc Conjugados anticuerpo anti-cd40-farmaco.
JP6813712B2 (ja) 2017-12-01 2021-01-13 アッヴィ・インコーポレイテッド グルココルチコイド受容体作動薬及びそのイムノコンジュゲート
EP3737420A2 (en) 2018-01-08 2020-11-18 Regeneron Pharmaceuticals, Inc. Steroids and antibody-conjugates thereof
CN118955710A (zh) 2018-05-09 2024-11-15 里珍纳龙药品有限公司 抗msr1抗体及其使用方法
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
AR125084A1 (es) 2021-03-23 2023-06-07 Lilly Co Eli Agonistas del receptor de glucocorticoides novedosos
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
AR125079A1 (es) 2021-03-23 2023-06-07 Lilly Co Eli Agonistas de receptores de glucocorticoides sustituidos con carboxi

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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
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
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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
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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
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AU7576001A (en) * 2000-08-05 2002-02-18 Glaxo Group Ltd 6.alpha., 9.alpha.-difluoro-17.alpha.-`(2-furanylcarboxyl) oxy]-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent
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TW200940070A (en) * 2007-12-21 2009-10-01 Schering Corp C-21 thioethers as glucocorticoid receptor agonists
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

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN110291097A (zh) * 2016-11-08 2019-09-27 里珍纳龙药品有限公司 类固醇类化合物及其蛋白质-偶联物
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
CN114702543A (zh) * 2022-04-19 2022-07-05 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
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
CN115430392A (zh) * 2022-08-31 2022-12-06 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
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

Also Published As

Publication number Publication date
MX2010007023A (es) 2010-09-30
PE20091525A1 (es) 2009-09-25
AR069804A1 (es) 2010-02-17
US8524697B2 (en) 2013-09-03
JP2011507878A (ja) 2011-03-10
TW200944540A (en) 2009-11-01
US20110182828A1 (en) 2011-07-28
EP2245042A1 (en) 2010-11-03
CL2008003803A1 (es) 2010-02-19
WO2009085879A2 (en) 2009-07-09
CA2710149A1 (en) 2009-07-09

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