CA2710149A1 - C20-c21 substituted glucocorticoid receptor agonists - Google Patents

C20-c21 substituted glucocorticoid receptor agonists Download PDF

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Publication number
CA2710149A1
CA2710149A1 CA2710149A CA2710149A CA2710149A1 CA 2710149 A1 CA2710149 A1 CA 2710149A1 CA 2710149 A CA2710149 A CA 2710149A CA 2710149 A CA2710149 A CA 2710149A CA 2710149 A1 CA2710149 A1 CA 2710149A1
Authority
CA
Canada
Prior art keywords
aryl
alkyl
heteroaryl
formula
haloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2710149A
Other languages
English (en)
French (fr)
Inventor
John C. Anthes
Kevin D. Mccormick
John A. Hey
Robert G. Aslanian
Purakkattle J. Biju
Michael Y. Berlin
Daniel M. Solomon
Hongwu Wang
Yeon-Hee Lim
Yoon Joo Lee
Rema Danielle Bitar
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2710149A1 publication Critical patent/CA2710149A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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)
CA2710149A 2007-12-21 2008-12-18 C20-c21 substituted glucocorticoid receptor agonists Abandoned CA2710149A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1613507P 2007-12-21 2007-12-21
US61/016,135 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
CA2710149A1 true CA2710149A1 (en) 2009-07-09

Family

ID=40532554

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2710149A Abandoned CA2710149A1 (en) 2007-12-21 2008-12-18 C20-c21 substituted glucocorticoid receptor agonists

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)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009085880A2 (en) * 2007-12-21 2009-07-09 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
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
AU2017359043B2 (en) 2016-11-08 2022-06-16 Regeneron Pharmaceuticals, Inc. Steroids and protein-conjugates 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
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
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US4188385A (en) * 1978-04-05 1980-02-12 Syntex (U.S.A.) Inc. Thioetianic acid derivatives
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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
SI1305329T2 (sl) * 2000-08-05 2015-07-31 Glaxo Group Limited S-fluorometil ester 6alfa,9alfa-difluoro-17alfa-(2-furanilkarboksil)oksi-11beta-hidroksi- 16alfa-metil-3-okso-androst-1,4-dien-17-karbotiojske kisline kot protivnetno sredstvo
NZ526216A (en) * 2000-11-03 2005-02-25 Univ Manchester Selective glucocorticoid receptor agonists
BRPI0611567A2 (pt) * 2005-06-14 2016-11-16 Gilead Sciences Inc composto e/ou sais farmaceuticamente aceitáveis dos mesmos, processo para síntese dos compostos, e formulação aerossol, e, uso de pelo menos uma pró-droga mútua de fenilfosfato
WO2009085880A2 (en) * 2007-12-21 2009-07-09 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

Also Published As

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
JP2011507878A (ja) 2011-03-10
EP2245042A1 (en) 2010-11-03
MX2010007023A (es) 2010-09-30

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20141218