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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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)
  • 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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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

ID=40532554

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 (https=)
EP (1) EP2245042A1 (https=)
JP (1) JP2011507878A (https=)
CN (1) CN101970452A (https=)
AR (1) AR069804A1 (https=)
CA (1) CA2710149A1 (https=)
CL (1) CL2008003803A1 (https=)
MX (1) MX2010007023A (https=)
PE (1) PE20091525A1 (https=)
TW (1) TW200944540A (https=)
WO (1) WO2009085879A2 (https=)

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

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2235035A2 (en) * 2007-12-21 2010-10-06 Schering Corporation 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
WO2011029547A2 (en) * 2009-09-11 2011-03-17 Chiesi Farmaceutici S.P.A. Pregnane derivatives condensed in the 16, 17 position with an n-substituted isoxazolidine ring as anti-inflammatory agents
UA116622C2 (uk) * 2011-11-11 2018-04-25 Аллерган, Інк. Похідні 4-прегенен-11ss-17-21-тріол-3,20-діону для лікування хвороб очей
WO2014115167A2 (en) * 2013-01-23 2014-07-31 Sphaera Pharma Pvt. 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
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
MY194619A (en) 2016-06-02 2022-12-07 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
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
KR102880156B1 (ko) 2017-07-24 2025-11-05 리제너론 파마슈티칼스 인코포레이티드 항cd8 항체 및 이의 용도
MX2020004691A (es) 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
AU2018374634A1 (en) 2017-12-01 2020-05-28 Abbvie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
KR20200095493A (ko) * 2017-12-01 2020-08-10 애브비 인코포레이티드 항-cd40 항체 약물 공액체
CN112004557B (zh) 2018-01-08 2024-07-30 里珍纳龙药品有限公司 类固醇类化合物及其抗体偶联物
CN112533951A (zh) 2018-05-09 2021-03-19 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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2002012266A1 (en) * 2000-08-05 2002-02-14 Glaxo Group Limited 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
US20040102425A1 (en) * 2000-11-03 2004-05-27 Barr Alexander Stephen Selective glucocorticoid receptor agonists
EP1893220A4 (en) * 2005-06-14 2011-06-15 Gilead Sciences Inc SUBSTITUTED PHENYLPHOSPHATES AS MUTUAL PROMO PRODUCTS CONSISTING OF STEROIDS AND BETA-AGONISTS FOR THE TREATMENT OF PULMONARY INFLAMMATION AND BRONCHOCONSTRICTION
EP2235035A2 (en) * 2007-12-21 2010-10-06 Schering Corporation 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
CL2008003803A1 (es) 2010-02-19
JP2011507878A (ja) 2011-03-10
MX2010007023A (es) 2010-09-30
US20110182828A1 (en) 2011-07-28
PE20091525A1 (es) 2009-09-25
WO2009085879A2 (en) 2009-07-09
EP2245042A1 (en) 2010-11-03
US8524697B2 (en) 2013-09-03
CA2710149A1 (en) 2009-07-09
TW200944540A (en) 2009-11-01
AR069804A1 (es) 2010-02-17

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