CN103118682A - 合成tlr7激动剂的磷脂缀合物的用途 - Google Patents

合成tlr7激动剂的磷脂缀合物的用途 Download PDF

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Publication number
CN103118682A
CN103118682A CN2011800330222A CN201180033022A CN103118682A CN 103118682 A CN103118682 A CN 103118682A CN 2011800330222 A CN2011800330222 A CN 2011800330222A CN 201180033022 A CN201180033022 A CN 201180033022A CN 103118682 A CN103118682 A CN 103118682A
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alkyl
compound
aryl
replacement
phospholipid
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D·A·卡森
H·B·科塔姆
林公子
M·陈
C·C·N·吴
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University of California San Diego UCSD
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/39Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544Phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/54Medicinal preparations containing antigens or antibodies characterised by the route of administration
    • A61K2039/541Mucosal route
    • A61K2039/543Mucosal route intranasal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/555Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511Organic adjuvants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/555Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511Organic adjuvants
    • A61K2039/55555Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Molecular Biology (AREA)
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  • Engineering & Computer Science (AREA)
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  • Communicable Diseases (AREA)
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  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN2011800330222A 2010-04-30 2011-04-29 合成tlr7激动剂的磷脂缀合物的用途 Pending CN103118682A (zh)

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US34357310P 2010-04-30 2010-04-30
US61/343,573 2010-04-30
PCT/US2011/000757 WO2011139348A2 (en) 2010-04-30 2011-04-29 Uses of phospholipid conjugates of synthetic tlr7 agonists

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US (1) US20130202629A1 (enExample)
EP (1) EP2563366A4 (enExample)
JP (1) JP2013525431A (enExample)
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WO (1) WO2011139348A2 (enExample)

Cited By (5)

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CN108348618A (zh) * 2015-09-29 2018-07-31 大日本住友制药株式会社 腺嘌呤缀合物化合物及其作为疫苗佐剂的用途
CN110678183A (zh) * 2017-04-28 2020-01-10 诺华股份有限公司 包含toll样受体激动剂的抗体缀合物以及组合疗法
CN112867725A (zh) * 2018-07-06 2021-05-28 坎塞拉有限公司 7-氨基-5-硫代-噻唑并[4,5-d]嘧啶的磷酸酯和膦酸酯衍生物及其在治疗与cx3cr1和/或cx3cl1的水平升高相关联的病况中的用途
WO2024199063A1 (zh) * 2023-03-30 2024-10-03 浙江养生堂天然药物研究所有限公司 含磷或含硫的大环化合物及其用途
WO2024250985A1 (zh) * 2023-06-07 2024-12-12 上海维申医药有限公司 Toll样受体激动剂杂环类衍生物及其制备和应用

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EP2700638A1 (en) 2006-05-31 2014-02-26 The Regents Of the University of California Purine analogs
HUE025555T2 (en) 2007-02-07 2016-02-29 Univ California Conjugates and applications of synthetic tlr agonists
WO2010088924A1 (en) 2009-02-06 2010-08-12 Telormedix Sa Pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof suitable for local administration
EP2396328A2 (en) * 2009-02-11 2011-12-21 The Regents of The University of California Toll-like receptor modulators and treatment of diseases
EP2674170B1 (en) 2012-06-15 2014-11-19 Invivogen Novel compositions of TLR7 and/or TLR8 agonists conjugated to lipids
WO2014052828A1 (en) 2012-09-27 2014-04-03 The Regents Of The University Of California Compositions and methods for modulating tlr4
US9295732B2 (en) 2013-02-22 2016-03-29 Invivogen Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
WO2015023858A2 (en) * 2013-08-16 2015-02-19 The Regents Of The University Of California Uses of phospholipid conjugates of synthetic tlr7 agonists
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WO2017046112A1 (en) 2015-09-17 2017-03-23 F. Hoffmann-La Roche Ag Sulfinylphenyl or sulfonimidoylphenyl benzazepines
CN108290845B (zh) 2015-10-07 2021-08-03 大日本住友制药株式会社 嘧啶化合物
JP6918838B2 (ja) 2016-05-23 2021-08-11 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 第三級アミド基を有するベンズアゼピンジカルボキサミド化合物
JP7022702B2 (ja) 2016-05-23 2022-02-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 第二級アミド基を有するベンズアゼピンジカルボキサミド化合物
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US20200087625A1 (en) * 2017-03-30 2020-03-19 Dennis A. Carson Methods for isolating, expanding and administering cancer specific cd8+ t cells
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US10472361B2 (en) 2017-08-16 2019-11-12 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor
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WO2021136488A1 (zh) 2020-01-02 2021-07-08 江苏恒瑞医药股份有限公司 一种吡啶并嘧啶类衍生物的结晶形式及其制备方法
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JP2023512208A (ja) 2020-01-27 2023-03-24 ブリストル-マイヤーズ スクイブ カンパニー トール様受容体7(TLR7)アゴニストとしての1H-ピラゾロ[4,3-d]ピリミジン化合物
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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108348618A (zh) * 2015-09-29 2018-07-31 大日本住友制药株式会社 腺嘌呤缀合物化合物及其作为疫苗佐剂的用途
CN108348618B (zh) * 2015-09-29 2021-06-15 大日本住友制药株式会社 腺嘌呤缀合物化合物及其作为疫苗佐剂的用途
CN110678183A (zh) * 2017-04-28 2020-01-10 诺华股份有限公司 包含toll样受体激动剂的抗体缀合物以及组合疗法
CN112867725A (zh) * 2018-07-06 2021-05-28 坎塞拉有限公司 7-氨基-5-硫代-噻唑并[4,5-d]嘧啶的磷酸酯和膦酸酯衍生物及其在治疗与cx3cr1和/或cx3cl1的水平升高相关联的病况中的用途
US12060380B2 (en) 2018-07-06 2024-08-13 Kancera Ab Phosphate and phosphonate derivatives of 7-amino-5-thio-thiazolo[4,5-d]pyrimidines and their use in treating conditions associated with elevated levels of CX3CR1 and/or CX3CL1
WO2024199063A1 (zh) * 2023-03-30 2024-10-03 浙江养生堂天然药物研究所有限公司 含磷或含硫的大环化合物及其用途
WO2024250985A1 (zh) * 2023-06-07 2024-12-12 上海维申医药有限公司 Toll样受体激动剂杂环类衍生物及其制备和应用

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US20130202629A1 (en) 2013-08-08
WO2011139348A2 (en) 2011-11-10
EP2563366A4 (en) 2013-11-20
WO2011139348A9 (en) 2011-12-22
WO2011139348A3 (en) 2012-03-15
JP2013525431A (ja) 2013-06-20
EP2563366A2 (en) 2013-03-06

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Application publication date: 20130522