CN110382033B - 用于设计高效力糖皮质激素的结构与机制 - Google Patents

用于设计高效力糖皮质激素的结构与机制 Download PDF

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CN110382033B
CN110382033B CN201780076320.7A CN201780076320A CN110382033B CN 110382033 B CN110382033 B CN 110382033B CN 201780076320 A CN201780076320 A CN 201780076320A CN 110382033 B CN110382033 B CN 110382033B
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alkyl
compound
dex
heteroaryl
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CN110382033A (zh
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徐华强
何元政
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Van Andel Research Institute
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Van Andel Research Institute
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    • 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
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • 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
    • 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201780076320.7A 2016-10-14 2017-10-13 用于设计高效力糖皮质激素的结构与机制 Active CN110382033B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662408314P 2016-10-14 2016-10-14
US62/408,314 2016-10-14
PCT/US2017/056447 WO2018071736A1 (en) 2016-10-14 2017-10-13 Structures and mechanism for the design of highly potent glucocorticoids

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CN110382033A CN110382033A (zh) 2019-10-25
CN110382033B true CN110382033B (zh) 2022-04-15

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US (1) US10954265B2 (cg-RX-API-DMAC7.html)
EP (1) EP3525870B1 (cg-RX-API-DMAC7.html)
JP (2) JP7146750B2 (cg-RX-API-DMAC7.html)
KR (1) KR102497070B1 (cg-RX-API-DMAC7.html)
CN (1) CN110382033B (cg-RX-API-DMAC7.html)
ES (1) ES2945983T3 (cg-RX-API-DMAC7.html)
MA (1) MA46539A (cg-RX-API-DMAC7.html)
PH (1) PH12019500801A1 (cg-RX-API-DMAC7.html)
RU (1) RU2019111101A (cg-RX-API-DMAC7.html)
SG (1) SG11201903209TA (cg-RX-API-DMAC7.html)
WO (1) WO2018071736A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201902595B (cg-RX-API-DMAC7.html)

Families Citing this family (2)

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Publication number Priority date Publication date Assignee Title
WO2025119398A1 (zh) * 2023-12-08 2025-06-12 浙江柏拉阿图医药科技有限公司 高效力糖皮质激素多晶型及其制备方法和用途
CN120365344A (zh) * 2024-01-24 2025-07-25 浙江柏拉阿图医药科技有限公司 一种高效力糖皮质激素化合物及其制备和用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1901863A (zh) * 2003-11-13 2007-01-24 康宾纳特克斯公司 治疗炎性疾病的方法和药物
CN101300265A (zh) * 2005-09-02 2008-11-05 尼科克斯公司 糖皮质激素硝酰氧基衍生物
CN101883778A (zh) * 2007-10-04 2010-11-10 阿斯利康(瑞典)有限公司 具有糖皮质激素活性的甾类[3，2-c]吡唑化合物
CN101945885A (zh) * 2007-12-20 2011-01-12 阿斯利康(瑞典)有限公司 用作糖皮质激素受体激动剂的甾类衍生物
CN102459306A (zh) * 2009-04-03 2012-05-16 阿斯利康(瑞典)有限公司 具有糖皮质激素活性的甾族[3，2-c]吡唑化合物的新酰胺衍生物
CN105744937A (zh) * 2013-09-25 2016-07-06 范安德尔研究所 高效糖皮质激素

Family Cites Families (12)

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DK66202C (da) 1945-03-03 1948-01-12 Danske Securitas As Kodekontakt til elektriske Alarmanlæg.
DK71662C (da) 1946-09-05 1950-11-06 Ingenioer Frank Broadbent Tørrecentrifuge.
US4049813A (en) 1976-07-15 1977-09-20 Sandoz, Inc. Substituted isoxazolo pyridinones
US5837698A (en) * 1996-05-02 1998-11-17 G. D. Searle & Co. Steroid nitrite and nitrate ester derivatives useful as anti-inflammatory drugs
CA2451057A1 (en) 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Novel isoxazolopyridone derivatives and use thereof
GB0119911D0 (en) 2001-08-15 2001-10-10 Novartis Ag Organic Compounds
CN1813768A (zh) * 2005-11-18 2006-08-09 成都力思特制药股份有限公司 治疗呼吸系统疾病的药用组合物及其在制药中的应用
CA2749585A1 (en) 2009-01-13 2010-07-22 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids
UY32520A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides
UY32523A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
WO2010147947A2 (en) 2009-06-16 2010-12-23 Schering Corporation NOVEL [3,2-c] HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS, COMPOSITIONS AND USES THEREOF
TWI695831B (zh) * 2014-09-13 2020-06-11 香港商南北兄弟藥業投資有限公司 Ｃｒｔｈ２拮抗劑化合物及其用途

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1901863A (zh) * 2003-11-13 2007-01-24 康宾纳特克斯公司 治疗炎性疾病的方法和药物
CN101300265A (zh) * 2005-09-02 2008-11-05 尼科克斯公司 糖皮质激素硝酰氧基衍生物
CN101883778A (zh) * 2007-10-04 2010-11-10 阿斯利康(瑞典)有限公司 具有糖皮质激素活性的甾类[3，2-c]吡唑化合物
CN101945885A (zh) * 2007-12-20 2011-01-12 阿斯利康(瑞典)有限公司 用作糖皮质激素受体激动剂的甾类衍生物
CN102459306A (zh) * 2009-04-03 2012-05-16 阿斯利康(瑞典)有限公司 具有糖皮质激素活性的甾族[3，2-c]吡唑化合物的新酰胺衍生物
CN105744937A (zh) * 2013-09-25 2016-07-06 范安德尔研究所 高效糖皮质激素

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EP3525870A1 (en) 2019-08-21
KR102497070B1 (ko) 2023-02-06
SG11201903209TA (en) 2019-05-30
US10954265B2 (en) 2021-03-23
EP3525870A4 (en) 2020-04-29
US20190263853A1 (en) 2019-08-29
JP2022132464A (ja) 2022-09-08
JP2019532071A (ja) 2019-11-07
MA46539A (fr) 2019-08-21
CN110382033A (zh) 2019-10-25
WO2018071736A1 (en) 2018-04-19
WO2018071736A9 (en) 2019-05-23
RU2019111101A3 (cg-RX-API-DMAC7.html) 2020-11-27
PH12019500801A1 (en) 2019-11-11
EP3525870B1 (en) 2023-05-10
KR20190068577A (ko) 2019-06-18
ZA201902595B (en) 2021-04-28
JP7146750B2 (ja) 2022-10-04
RU2019111101A (ru) 2020-11-16
ES2945983T3 (es) 2023-07-11

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