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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CN2011800330222A
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Chinese (zh)
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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
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University of California, San Diego
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/39—Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
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    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/02—Bacterial antigens
    • A61K39/07—Bacillus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544—Phospholipids
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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
    • C07F9/65616—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/54—Medicinal preparations containing antigens or antibodies characterised by the route of administration
    • A61K2039/541—Mucosal route
    • A61K2039/543—Mucosal route intranasal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/555—Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511—Organic adjuvants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/555—Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511—Organic adjuvants
    • A61K2039/55555—Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Dermatology (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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KR20110117705A (ko) * 2009-02-11 2011-10-27 더 리전트 오브 더 유니버시티 오브 캘리포니아 톨-유사 수용체 조정제 및 질병의 치료
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
EP3033089A2 (en) * 2013-08-16 2016-06-22 The Regents of The University of California Uses of phospholipid conjugates of synthetic tlr7 agonists
ES2804101T3 (es) 2014-04-22 2021-02-03 Hoffmann La Roche Compuestos de 4-amino-imidazoquinolina
HUE042563T2 (hu) 2015-03-06 2019-07-29 Hoffmann La Roche Benzazepin-dikarboxamid vegyületek
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CN115279765B (zh) 2020-01-27 2024-11-12 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物
JP7684316B2 (ja) 2020-01-27 2025-05-27 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
CN115151547A (zh) 2020-01-27 2022-10-04 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物
KR20220132594A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
WO2021154662A1 (en) 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
CN115210235A (zh) 2020-01-27 2022-10-18 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物
JP2023512206A (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
JP7712941B2 (ja) 2020-01-27 2025-07-24 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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EP2563366A4 (en) 2013-11-20
US20130202629A1 (en) 2013-08-08
WO2011139348A2 (en) 2011-11-10
WO2011139348A9 (en) 2011-12-22
WO2011139348A3 (en) 2012-03-15
EP2563366A2 (en) 2013-03-06
JP2013525431A (ja) 2013-06-20

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Application publication date: 20130522