CN107849072B - 酰胺连接的ep4激动剂-二膦酸盐化合物及其用途 - Google Patents

酰胺连接的ep4激动剂-二膦酸盐化合物及其用途 Download PDF

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CN107849072B
CN107849072B CN201680038591.9A CN201680038591A CN107849072B CN 107849072 B CN107849072 B CN 107849072B CN 201680038591 A CN201680038591 A CN 201680038591A CN 107849072 B CN107849072 B CN 107849072B
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compound
bone
compounds
conjugated
acid
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CN107849072A (zh
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马里恩·戴维南
罗本特·N·扬
陈刚
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Simon Fraser University
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    • 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
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • 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
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/3873—Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201680038591.9A 2015-06-12 2016-06-13 酰胺连接的ep4激动剂-二膦酸盐化合物及其用途 Active CN107849072B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562175118P 2015-06-12 2015-06-12
US62/175,118 2015-06-12
PCT/IB2016/053482 WO2016199111A1 (en) 2015-06-12 2016-06-13 Amide-linked ep4 agonist-bisphosphonate compounds and uses thereof

Publications (2)

Publication Number Publication Date
CN107849072A CN107849072A (zh) 2018-03-27
CN107849072B true CN107849072B (zh) 2020-12-15

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US (2) US10400000B2 (enExample)
EP (1) EP3307747A4 (enExample)
JP (1) JP7174982B2 (enExample)
CN (1) CN107849072B (enExample)
WO (1) WO2016199111A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9650414B1 (en) 2014-05-30 2017-05-16 Simon Fraser University Dual-action EP4 agonist—bisphosphonate conjugates and uses thereof
CN107849072B (zh) 2015-06-12 2020-12-15 西蒙弗雷泽大学 酰胺连接的ep4激动剂-二膦酸盐化合物及其用途
US20250295725A1 (en) * 2022-01-14 2025-09-25 Purdue Research Foundation Bone targeted treatment in osteogenesis imperfecta
GB202211232D0 (en) 2022-08-02 2022-09-14 Heptares Therapeutics Ltd Prostaglandin EP4 receptor agonist compounds
WO2026013441A1 (en) * 2024-07-10 2026-01-15 Mesentech Inc. Bisphosphonate-ep4 agonists for selective delivery to damaged muscle

Citations (1)

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US5510517A (en) 1993-08-25 1996-04-23 Merck & Co., Inc. Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
TW257765B (enExample) 1993-08-25 1995-09-21 Merck & Co Inc
JPH10265454A (ja) 1997-01-27 1998-10-06 Ono Pharmaceut Co Ltd ３，７−ジチアプロスタン酸誘導体、それらの製造方法およびそれらを有効成分として含有する薬剤
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ATE327751T1 (de) 2000-01-31 2006-06-15 Pfizer Prod Inc Verwendung von aktivatoren des prostaglandinrezeptores 4 zur behandlung von akuter oder chronischer niereninsuffizienz
WO2001072268A1 (en) 2000-03-31 2001-10-04 Toray Industries, Inc. Hair growth or hair formation controlling agents
AU2001290250A1 (en) 2000-09-21 2002-04-02 Ono Pharmaceutical Co. Ltd. Ep4 receptor agonists containing 8-azaprostaglandin derivatives as the active ingredient
EA200300379A1 (ru) 2000-11-27 2003-08-28 Пфайзер Продактс Инк. Селективные агонисты рецептора ep4 в лечении остеопороза
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Publication number Publication date
JP2018519277A (ja) 2018-07-19
WO2016199111A1 (en) 2016-12-15
EP3307747A1 (en) 2018-04-18
US11312737B2 (en) 2022-04-26
US20190345179A1 (en) 2019-11-14
US10400000B2 (en) 2019-09-03
EP3307747A4 (en) 2019-02-27
US20180170951A1 (en) 2018-06-21
CN107849072A (zh) 2018-03-27
CA2988523A1 (en) 2016-12-15
JP7174982B2 (ja) 2022-11-18
NZ738016A (en) 2024-10-25

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