ES2191475T3 - Conjugados de prostaglandina para el tratamiento o prevencion de enfermedades oseas. - Google Patents

Conjugados de prostaglandina para el tratamiento o prevencion de enfermedades oseas.

Info

Publication number
ES2191475T3
ES2191475T3 ES99955618T ES99955618T ES2191475T3 ES 2191475 T3 ES2191475 T3 ES 2191475T3 ES 99955618 T ES99955618 T ES 99955618T ES 99955618 T ES99955618 T ES 99955618T ES 2191475 T3 ES2191475 T3 ES 2191475T3
Authority
ES
Spain
Prior art keywords
conjugates
diseases
oseas
prostaglandine
prevention
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES99955618T
Other languages
English (en)
Inventor
Laurent Gil
Yongxin Han
Rejean Ruel
Robert N Young
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Frosst Canada and Co
Original Assignee
Merck Frosst Canada and Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Frosst Canada and Co filed Critical Merck Frosst Canada and Co
Application granted granted Critical
Publication of ES2191475T3 publication Critical patent/ES2191475T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839Polyphosphonic acids
    • C07F9/3869Polyphosphonic acids containing carboxylic acid or carboxylic acid derivative substituents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839Polyphosphonic acids
    • C07F9/3865Polyphosphonic acids containing sulfur substituents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Un compuesto A seleccionado del grupo constituido por: **(Fórmula)** y mezclas del mismo y las sales farmacéuticamente aceptables del mismo, en los cuales: A es un radical de ciclopentano dioxigenado seleccionado del grupo constituido por: **(Fórmula)** X se selecciona del grupo constituido por: **(Fórmula)** Y se selecciona del grupo constituido por: **(Fórmula)** Ri se selecciona del grupo constituido por H, alquilo Ci-Cio, y Si(CH3)2tBu; R2 se selecciona del grupo constituido por H y alquilo C1-C10; R3 se selecciona del grupo constituido por H, tetrahidropirano, y Si(CH3)2tBu; R4 y R5 se seleccionan independientemente del grupo constituido por H, alquilo C1-C10, fenilo, bencilo, alcoxi C1-C10, y CF3, y n es un número entero entre 0 y 5.
ES99955618T 1998-11-20 1999-11-18 Conjugados de prostaglandina para el tratamiento o prevencion de enfermedades oseas. Expired - Lifetime ES2191475T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10930798P 1998-11-20 1998-11-20

Publications (1)

Publication Number Publication Date
ES2191475T3 true ES2191475T3 (es) 2003-09-01

Family

ID=22326974

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99955618T Expired - Lifetime ES2191475T3 (es) 1998-11-20 1999-11-18 Conjugados de prostaglandina para el tratamiento o prevencion de enfermedades oseas.

Country Status (9)

Country Link
US (1) US6121253A (es)
EP (1) EP1131327B1 (es)
JP (1) JP2002530411A (es)
AT (1) ATE232874T1 (es)
AU (1) AU762396B2 (es)
CA (1) CA2351679A1 (es)
DE (1) DE69905488T2 (es)
ES (1) ES2191475T3 (es)
WO (1) WO2000031084A1 (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7598246B2 (en) * 1998-04-02 2009-10-06 Mbc Pharma, Inc. Bisphosphonate conjugates and methods of making and using the same
US6896871B2 (en) 1998-04-02 2005-05-24 Mbc Research, Inc. Biphosphonate conjugates and methods of making and using the same
US8586781B2 (en) 1998-04-02 2013-11-19 Mbc Pharma, Inc. Bone targeted therapeutics and methods of making and using the same
KR100593393B1 (ko) 1999-01-20 2006-06-28 다카라 바이오 가부시키가이샤 치료제
NZ513825A (en) 1999-03-05 2001-09-28 Procter & Gamble C 16 unsaturated FP-selective prostaglandins analogs
AU776375B2 (en) * 1999-08-04 2004-09-09 Duke University Novel 2-decarboxy-2-phosphinico prostaglandin F analogs
US20010041743A1 (en) * 2000-01-12 2001-11-15 Steven Offenbacher Use of cyclopentenone derivatives for bone and periodontal regeneration
US20020037914A1 (en) 2000-03-31 2002-03-28 Delong Mitchell Anthony Compositions and methods for treating hair loss using C16-C20 aromatic tetrahydro prostaglandins
US20020013294A1 (en) 2000-03-31 2002-01-31 Delong Mitchell Anthony Cosmetic and pharmaceutical compositions and methods using 2-decarboxy-2-phosphinico derivatives
US20020172693A1 (en) 2000-03-31 2002-11-21 Delong Michell Anthony Compositions and methods for treating hair loss using non-naturally occurring prostaglandins
US6476006B2 (en) * 2000-06-23 2002-11-05 Teva Pharmaceutical Industries, Ltd. Composition and dosage form for delayed gastric release of alendronate and/or other bis-phosphonates
WO2002083150A1 (en) * 2001-04-10 2002-10-24 Mbc Research, Inc. Bisphosphonate conjugates and methods of making and using the same
US7288535B2 (en) * 2002-05-02 2007-10-30 Osteoscreen, Inc. Methods and compositions for stimulating bone growth using nitric oxide releasing bisphosphonate conjugates
WO2005080367A1 (en) 2004-02-12 2005-09-01 Pharmagene Laboratories Limited Ep2 receptor agonists
JP2009505973A (ja) 2005-08-09 2009-02-12 アステランド ユーケイ リミテッド Ep2受容体アゴニスト
WO2007092338A2 (en) * 2006-02-06 2007-08-16 Cypress Bioscience, Inc. Compositions comprising a bisphosphonate and an antifolate
EP2155769B1 (en) 2007-05-04 2012-06-27 Katholieke Universiteit Leuven KU Leuven Research & Development Tissue degeneration protection
US8063240B2 (en) 2007-11-14 2011-11-22 Cayman Chemical Company, Incorporated Prostaglandin E1 and E2 analogs for the treatment of various medical conditions
US8623918B2 (en) 2008-10-29 2014-01-07 Novaer Holdings, Inc. Amino acid salts of prostaglandins
US8722739B2 (en) 2008-10-29 2014-05-13 Novaer Holdings, Inc. Amino acid salts of prostaglandins
CA2738045C (en) 2010-05-28 2019-02-19 Simon Fraser University Conjugate compounds, methods of making same, and uses thereof
AU2012290089B2 (en) 2011-08-01 2016-09-29 Mbc Pharma, Inc. Vitamin B6 derivatives of nucleotides, acyclonucleotides and acyclonucleoside phosphonates
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
US11793452B2 (en) 2019-10-03 2023-10-24 Johnson & Johnson Consumer Inc. Method of visualizing and quantifying remineralization

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3975404A (en) * 1971-05-04 1976-08-17 The Upjohn Company Bicyclic lactone intermediates
US3927197A (en) * 1974-04-19 1975-12-16 Pfizer Tertiary alcohol stabilized E-series prostaglandins
US4018892A (en) * 1975-08-06 1977-04-19 Pfizer Inc. Bone deposition by 16-aryl-13,14-dihydro-PGE2 p-biphenyl esters
US4097601A (en) * 1977-08-26 1978-06-27 Pfizer Inc. Bone deposition by 2-descarboxy-2-(tetrazol-5-yl)-11-dexosy-16-aryl prostaglandins
US4171331A (en) * 1978-06-05 1979-10-16 Miles Laboratories, Inc. 1 And 2-substituted analogues of certain prostaglandins
US4621100A (en) * 1981-09-25 1986-11-04 The Upjohn Company Treatment of osteoporosis with prostaglandins
ATE114473T1 (de) * 1984-04-30 1994-12-15 Procter & Gamble Ausrüstung für die verwendung bei der behandlung von osteoporose.
JPS6191137A (ja) * 1984-10-11 1986-05-09 Kao Corp 外用薬剤組成物
DE3519361A1 (de) * 1985-05-30 1986-12-04 Boehringer Ingelheim International GmbH, 6507 Ingelheim (gamma)-ifn als wirkstoff zur hemmung (verhinderung) von abbauprozessen im knochen
US4761406A (en) * 1985-06-06 1988-08-02 The Procter & Gamble Company Regimen for treating osteoporosis
US5071840A (en) * 1986-12-19 1991-12-10 Norwich Eaton Pharmaceuticals, Inc. Certain heterocyclic substituted diphosphonate compounds pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism
EP0341961A3 (en) * 1988-05-09 1990-06-20 Merck & Co. Inc. Polymalonic acids as boneaffinity agents
JPH0778024B2 (ja) * 1988-10-14 1995-08-23 藤沢薬品工業株式会社 医薬化合物とジホスホン酸誘導体の結合体を含有する医薬用製剤
JPH0759505B2 (ja) * 1988-11-17 1995-06-28 帝人株式会社 シクロペンテノン類を活性成分とする骨形成促進剤
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JPH07507315A (ja) * 1992-05-29 1995-08-10 プロクター、エンド、ギャンブル、ファーマスーティカルズ、インコーポレーテッド カルシウムおよびホスフェート代謝異常治療用含硫ホスホネート化合物
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Also Published As

Publication number Publication date
ATE232874T1 (de) 2003-03-15
EP1131327B1 (en) 2003-02-19
AU1255600A (en) 2000-06-13
DE69905488T2 (de) 2003-12-24
US6121253A (en) 2000-09-19
AU762396B2 (en) 2003-06-26
CA2351679A1 (en) 2000-06-02
WO2000031084A1 (en) 2000-06-02
EP1131327A1 (en) 2001-09-12
JP2002530411A (ja) 2002-09-17
DE69905488D1 (de) 2003-03-27

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