JP6082692B2 - プロスタグランジンビスホスホネート結合体化合物およびその作製方法ならびにその使用 - Google Patents

プロスタグランジンビスホスホネート結合体化合物およびその作製方法ならびにその使用 Download PDF

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JP6082692B2
JP6082692B2 JP2013511491A JP2013511491A JP6082692B2 JP 6082692 B2 JP6082692 B2 JP 6082692B2 JP 2013511491 A JP2013511491 A JP 2013511491A JP 2013511491 A JP2013511491 A JP 2013511491A JP 6082692 B2 JP6082692 B2 JP 6082692B2
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compound
bone
optionally substituted
pharmaceutically acceptable
carbon atoms
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JP2013531627A5 (enExample
JP2013531627A (ja
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ロバート エヌ． ヤング，
ロバート エヌ． ヤング，
スティーブン アーンズ，
スティーブン アーンズ，
アン モロー，
アン モロー，
モハメッド モンズール モルシェッド，
モハメッド モンズール モルシェッド，
ロメロ ギベ，
ロメロ ギベ，
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サイモン フレイザー ユニバーシティ
サイモン フレイザー ユニバーシティ
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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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • 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
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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)
    • 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
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • 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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2013511491A 2010-05-28 2011-05-30 プロスタグランジンビスホスホネート結合体化合物およびその作製方法ならびにその使用 Active JP6082692B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US34969410P 2010-05-28 2010-05-28
US61/349,694 2010-05-28
CA2,738,045 2011-04-21
CA2738045A CA2738045C (en) 2010-05-28 2011-04-21 Conjugate compounds, methods of making same, and uses thereof
PCT/CA2011/000633 WO2011147034A1 (en) 2010-05-28 2011-05-30 Prostaglandin-bisphosphonate conjugate compounds, methods of making same, and uses thereof

Publications (3)

Publication Number Publication Date
JP2013531627A JP2013531627A (ja) 2013-08-08
JP2013531627A5 JP2013531627A5 (enExample) 2014-07-17
JP6082692B2 true JP6082692B2 (ja) 2017-02-15

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JP2013511491A Active JP6082692B2 (ja) 2010-05-28 2011-05-30 プロスタグランジンビスホスホネート結合体化合物およびその作製方法ならびにその使用

Country Status (5)

Country Link
US (1) US9611284B2 (enExample)
EP (1) EP2576575B1 (enExample)
JP (1) JP6082692B2 (enExample)
CA (1) CA2738045C (enExample)
WO (1) WO2011147034A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2738045C (en) 2010-05-28 2019-02-19 Simon Fraser University Conjugate compounds, methods of making same, and uses thereof
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
EP3454913A4 (en) 2016-03-15 2019-11-27 The Regents of the University of California BONE OBTAINING ANTIBODY CONJUGATE AND METHOD FOR THE PRODUCTION AND USE THEREOF
CN108659083A (zh) * 2017-03-31 2018-10-16 天津药业研究院有限公司 一种依碳氯替泼诺的合成方法
CN108659084A (zh) * 2017-03-31 2018-10-16 天津药业研究院有限公司 一种17β-羧酸氯甲酯类甾体化合物的制备方法
WO2025024714A2 (en) * 2023-07-25 2025-01-30 Bioventures, Llc Bone-targeted canonical notch inhibitor
WO2026013441A1 (en) * 2024-07-10 2026-01-15 Mesentech Inc. Bisphosphonate-ep4 agonists for selective delivery to damaged muscle

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US4320136A (en) * 1980-08-11 1982-03-16 E. I. Du Pont De Nemours And Company 8-Aza-16,16-difluoroprostanoids
US4922007A (en) 1989-06-09 1990-05-01 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
US5019651A (en) 1990-06-20 1991-05-28 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof
US5409911A (en) * 1992-09-11 1995-04-25 Merck & Co., Inc. Prostaglandin analog for treating osteoporosis
TW257765B (enExample) 1993-08-25 1995-09-21 Merck & Co Inc
US5510517A (en) 1993-08-25 1996-04-23 Merck & Co., Inc. Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
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
EP1114816A4 (en) 1998-09-14 2002-09-04 Ono Pharmaceutical Co SUBSTITUTED PHENYL-PROSTAGLANDIN E DERIVATIVES- $ g (V) AND MEDICINAL PRODUCTS CONTAINING THEM AS ACTIVE INGREDIENT
US6121253A (en) * 1998-11-20 2000-09-19 Merck Frosst Canada & Co. Prostaglandin conjugates for treating or preventing bone disease
AP2002002555A0 (en) 1999-12-22 2002-06-30 Pfizer Prod Inc EP4 Receptor selective agonists in the treatment of osteoporosis.
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
WO2003047417A2 (en) 2001-12-03 2003-06-12 Merck & Co., Inc. Ep4 receptor agonist, compositions and methods thereof
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CA2738045C (en) 2010-05-28 2019-02-19 Simon Fraser University Conjugate compounds, methods of making same, and uses thereof

Also Published As

Publication number Publication date
EP2576575B1 (en) 2018-09-05
US9611284B2 (en) 2017-04-04
US20130157984A1 (en) 2013-06-20
JP2013531627A (ja) 2013-08-08
EP2576575A4 (en) 2013-11-06
WO2011147034A1 (en) 2011-12-01
CA2738045A1 (en) 2011-11-28
EP2576575A1 (en) 2013-04-10
WO2011147034A8 (en) 2012-05-18
CA2738045C (en) 2019-02-19

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