CN102099368A - 作为糖皮质激素受体激动剂的c-21硫醚 - Google Patents

作为糖皮质激素受体激动剂的c-21硫醚 Download PDF

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Publication number
CN102099368A
CN102099368A CN2008801273009A CN200880127300A CN102099368A CN 102099368 A CN102099368 A CN 102099368A CN 2008801273009 A CN2008801273009 A CN 2008801273009A CN 200880127300 A CN200880127300 A CN 200880127300A CN 102099368 A CN102099368 A CN 102099368A
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CN
China
Prior art keywords
compound according
alkyl
compound
hydrogen
formula
Prior art date
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Pending
Application number
CN2008801273009A
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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
李伦珠
雷马·丹妮尔·比塔尔
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Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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Publication of CN102099368A publication Critical patent/CN102099368A/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
    • 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

Landscapes

  • 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)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
CN2008801273009A 2007-12-21 2008-12-18 作为糖皮质激素受体激动剂的c-21硫醚 Pending CN102099368A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1614407P 2007-12-21 2007-12-21
US61/016144 2007-12-21
PCT/US2008/087301 WO2009085880A2 (en) 2007-12-21 2008-12-18 C-21 thioethers as glucocorticoid receptor agonists

Publications (1)

Publication Number Publication Date
CN102099368A true CN102099368A (zh) 2011-06-15

Family

ID=40513892

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2008801273009A Pending CN102099368A (zh) 2007-12-21 2008-12-18 作为糖皮质激素受体激动剂的c-21硫醚

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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103694306A (zh) * 2014-01-07 2014-04-02 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
WO2024125639A1 (zh) * 2022-12-16 2024-06-20 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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009085879A2 (en) 2007-12-21 2009-07-09 Schering Corporation C20-c21 substituted glucocorticoid receptor agonists
UY32520A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides
MY194619A (en) 2016-06-02 2022-12-07 Abbvie Inc Glucocorticoid receptor agonist and immunoconjugates thereof
MY199937A (en) 2016-11-08 2023-11-29 Regeneron Pharma Steroids and protein-conjugates thereof
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
CN111601619A (zh) 2017-11-07 2020-08-28 里珍纳龙药品有限公司 用于抗体药物偶联物的亲水性连接体
BR112020010694A2 (pt) 2017-12-01 2020-11-10 Abbvie Inc. agonista de receptor de glicocorticoides e imunoconjugados do mesmo
US12070506B2 (en) 2018-01-08 2024-08-27 Regeneron Pharmaceuticals, Inc. Steroids and antibody-conjugates thereof
AU2019265703A1 (en) 2018-05-09 2020-11-19 Regeneron Pharmaceuticals, Inc. Anti-MSR1 antibodies and methods of use thereof
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2231374B1 (enExample) * 1973-05-30 1976-10-22 Jouveinal Sa
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
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
ATE194357T1 (de) * 1995-12-29 2000-07-15 Glaxo Group Ltd 21-(2-oxo-tetrahydrofuran)-thio pregnan derivative, ein verfahren zu ihrer herstellung und pharmazeutische präparate davon
US20100209508A1 (en) * 2005-06-14 2010-08-19 Corus Pharma, Inc. Substituted Phenylphosphates as Mutual Prodrugs of Steroids and ß-Agonists for the Treatment of Title Pulmonary Inflammation and Bronchoconstriction
WO2009085879A2 (en) * 2007-12-21 2009-07-09 Schering Corporation C20-c21 substituted glucocorticoid receptor agonists

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103694306A (zh) * 2014-01-07 2014-04-02 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
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
WO2024125639A1 (zh) * 2022-12-16 2024-06-20 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

Also Published As

Publication number Publication date
WO2009085880A8 (en) 2011-01-27
TW200940070A (en) 2009-10-01
CL2008003802A1 (es) 2010-02-19
JP2011507879A (ja) 2011-03-10
MX2010007024A (es) 2010-09-30
WO2009085880A3 (en) 2009-09-17
WO2009085880A2 (en) 2009-07-09
EP2235035A2 (en) 2010-10-06
CA2710240A1 (en) 2009-07-09
PE20091215A1 (es) 2009-08-14
AR070040A1 (es) 2010-03-10
US20110262368A1 (en) 2011-10-27

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