KR880701726A - 1-히드록시-3-(n-메틸-n-프로필아미노)-프로판-1,1-디포스폰산 : 이들의 제법 및 이들을 함유하는 약제 - Google Patents

1-히드록시-3-(n-메틸-n-프로필아미노)-프로판-1,1-디포스폰산 : 이들의 제법 및 이들을 함유하는 약제

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KR880701726A
KR880701726A KR1019880700274A KR880700274A KR880701726A KR 880701726 A KR880701726 A KR 880701726A KR 1019880700274 A KR1019880700274 A KR 1019880700274A KR 880700274 A KR880700274 A KR 880700274A KR 880701726 A KR880701726 A KR 880701726A
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methyl
propylamino
propane
hydroxy
diphosphonic acid
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KR1019880700274A
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English (en)
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KR950008997B1 (ko
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루디갈
보지스 엘마르
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다움 포우퀘트
뵈링거 만하임 게엠베하
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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
    • C07F9/28—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)]
    • 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)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4025—Esters of poly(thio)phosphonic acids
    • C07F9/405—Esters of poly(thio)phosphonic 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)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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)

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Luminescent Compositions (AREA)
  • Vehicle Interior And Exterior Ornaments, Soundproofing, And Insulation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Detergent Compositions (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산 : 이들의 제법 및 이들을 함유하는 약제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 일반식(I)을 가지는 1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산 및 이들의 약리학적으로 수용 가능한 염 :
    상기식에서 R은 수소 또는 C1-C4알킬기를 의미한다.
  2. a) 일반식(II)의 카르복실산을 아인산 또는 인산과 아인산 할라이드 또는 포스포릴 할라이드와의 혼합물과 반응시키고 계속하여 일반식(I)의 디포스폰산으로 비누화시키거나, 또는
    b) 일반식(III)의 염화카르복실산을 일반식(IV)의 트리알킬아인산염과 반응시켜서 일반식(V)의 아실포스폰산염을 생성시키고 그 다음 이것을 (VI)의 디알킬아인산염과 반응시켜 일반식(VII)의 디포스폰산염을 형성시키고 결과는 테트라에스테르를 임의로 디에스테르 또는 일반식(I)의 유리 1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산으로 비누화시키고, 또는 c)일반식(Ⅷ)의 화합물을 메틸화시키고, 결과되는 테트라에스테르를 임의로 디에스테르 또는 일반식(I)의 유리 1-히드록시-3-(N-메틸-N-프로필아미노 )-프로판-1,1-디포스폰산으로 비누화시키고, 이렇게 얻어진 화합물을 임의로 약리학적으로 수용 가능한 이들의 염으로 전환시킴을 특징으로 하는 다음 일반식(I)의 1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산, 이들의 에스테르 및 약리학적으로 수용가능한 이들 염의 제조방법 :
    상기식에서 R은 수소 또는 C1-C4알킬기를 의미하고, R'은 C1-C4알킬기, 바람직하게는 메틸, 에틸 및 이소부틸기이다.
  3. 제1항에의 1-히드록시-3-(N-메틸-N-프로필아미노-프로판-1, 1-디포스폰산 또는 이들의 에스테르 또는 약리학적으로 수용 가능한 이들의 염 및 통상적인 약리학적 담체 및/또는 보조제를 함유하는 약제.
  4. 제1항에의 1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산 또는 이들의 에스테르 또는 약리학적으로 수용 가능한 이들의 염을 약제를 제조하기 위해 사용하는 방법.
  5. 제1항의 1-히드록시-3-(N-메틸-N-프로필아미노)-프로판-1, 1-디포스폰산 또는 약리학적으로 수용가능한 이들의 염을 칼슘대사 질환의 치료를 위해 사용하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880700274A 1986-07-11 1987-07-09 1-히드록시-3-(n-메틸-n-프로필아미노)-프로판-1,1-디포스폰산; 이들의 제법 및 이들을 함유하는 약제 KR950008997B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DEP3623397.8 1986-07-11
DE19863623397 DE3623397A1 (de) 1986-07-11 1986-07-11 Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
DEP3622397.8 1986-07-11
PCT/EP1987/000368 WO1988000590A1 (en) 1986-07-11 1987-07-09 Diphosphonium acid derivates and medicines containing the same

Publications (2)

Publication Number Publication Date
KR880701726A true KR880701726A (ko) 1988-11-04
KR950008997B1 KR950008997B1 (ko) 1995-08-10

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ID=6304949

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1019880700274A KR950008997B1 (ko) 1986-07-11 1987-07-09 1-히드록시-3-(n-메틸-n-프로필아미노)-프로판-1,1-디포스폰산; 이들의 제법 및 이들을 함유하는 약제
KR1019870007485A KR960010418B1 (ko) 1986-07-11 1987-07-10 디포스폰산 유도체 및 이들을 함유하는 제약 조성물

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Application Number Title Priority Date Filing Date
KR1019870007485A KR960010418B1 (ko) 1986-07-11 1987-07-10 디포스폰산 유도체 및 이들을 함유하는 제약 조성물

Country Status (27)

Country Link
US (2) US4942157A (ko)
EP (2) EP0252505B1 (ko)
JP (2) JP2563954B2 (ko)
KR (2) KR950008997B1 (ko)
AT (2) ATE80633T1 (ko)
AU (2) AU598279B2 (ko)
BG (1) BG60839B2 (ko)
CA (2) CA1296739C (ko)
CS (1) CS265242B2 (ko)
DD (1) DD263992A5 (ko)
DE (4) DE3623397A1 (ko)
DK (2) DK168629B1 (ko)
ES (2) ES2036190T3 (ko)
FI (2) FI87221C (ko)
GE (1) GEP20084347B (ko)
GR (2) GR3000616T3 (ko)
HK (1) HK87093A (ko)
HU (2) HU201950B (ko)
IE (2) IE60219B1 (ko)
IL (2) IL83148A (ko)
LU (1) LU88844I2 (ko)
MX (1) MX9203375A (ko)
NL (1) NL960032I2 (ko)
NZ (2) NZ221027A (ko)
PT (1) PT85301B (ko)
WO (1) WO1988000590A1 (ko)
ZA (1) ZA874877B (ko)

Families Citing this family (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6458772B1 (en) * 1909-10-07 2002-10-01 Medivir Ab Prodrugs
DE3623397A1 (de) * 1986-07-11 1988-01-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
EP0317505A1 (de) * 1987-11-13 1989-05-24 Ciba-Geigy Ag Neue Azacycloalkylalkandiphosphonsäuren
ES2054868T3 (es) * 1987-12-11 1994-08-16 Ciba Geigy Ag Acidos aralifatilaminoalcanodifosfonicos.
US5190930A (en) * 1987-12-11 1993-03-02 Ciba-Geigy Corporation Araliphatylaminoalkanediphosphonic acids
US5110807A (en) * 1988-12-01 1992-05-05 Ciba-Geigy Corporation Araliphatylaminoalkanediphosphonic acids
JPH07629B2 (ja) * 1988-01-20 1995-01-11 山之内製薬株式会社 （シクロアルキルアミノ）メチレンビス（フォスフォン酸）および該化合物を有効成分とする医薬
US4933472A (en) * 1988-04-08 1990-06-12 Yamanouchi Pharmaceutical Co., Ltd. Substituted aminomethylenebis(phosphonic acid) derivatives
DE3822650A1 (de) * 1988-07-05 1990-02-01 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
ATE136870T1 (de) * 1988-11-01 1996-05-15 Arch Dev Corp Verfahren zur abtrennung von metallischen ionen mit phosphonsäuren als complexbildner
GB8825589D0 (en) * 1988-11-02 1988-12-07 Albright & Wilson Purification
TW198039B (ko) * 1988-11-28 1993-01-11 Ciba Geigy Ag
US5154843A (en) * 1989-02-08 1992-10-13 The Lubrizol Corporation Hydroxyalkane phosphonic acids and derivatives thereof and lubricants containing the same
PH26923A (en) * 1989-03-08 1992-12-03 Ciba Geigy N-substituted amino alkanediphosphonic acids
US4987767A (en) * 1989-06-09 1991-01-29 Research Corporation Technologies, Inc. Exposive detection screening system
MX21453A (es) * 1989-07-07 1994-01-31 Ciba Geigy Ag Preparaciones farmaceuticas que se administran en forma topica.
MX21452A (es) * 1989-07-07 1994-01-31 Ciba Geigy Ag Preparaciones farmaceuticas que se administran en forma topica.
US5139786A (en) * 1989-07-07 1992-08-18 Ciba-Geigy Corporation Topical formulations
US5324519A (en) * 1989-07-24 1994-06-28 Atrix Laboratories, Inc. Biodegradable polymer composition
US5487897A (en) 1989-07-24 1996-01-30 Atrix Laboratories, Inc. Biodegradable implant precursor
DE69023844T2 (de) * 1989-09-06 1996-06-20 Merck & Co Inc Acyloxymethylester der Bisphonsäuren als Knochenresorptions-Inhibitoren.
US5356887A (en) * 1990-01-31 1994-10-18 Merck & Co., Inc. Pharmaceutical compositions containing insoluble calcium salts of amino-hydroxybutylidene bisphoshonic acids
FI89364C (fi) * 1990-12-20 1993-09-27 Leiras Oy Foerfarande foer framstaellning av nya, farmakologiskt anvaendbara metylenbisfosfonsyraderivat
IT1244698B (it) * 1991-02-01 1994-08-08 Gentili Ist Spa Acidi aril-o arilalchil-acil ammino-alchil-idrossidifosfonici, procedimento per la loro preparazione e loro uso in terapia osteo-articolare e dei tessuti connettori in generale
JPH06508365A (ja) * 1991-06-19 1994-09-22 ジ・アップジョン・カンパニー 抗炎症剤としてのりん酸ジアルキル（ジアルコキシホスフィニル）メチル類
IT1247034B (it) * 1991-06-26 1994-12-12 Gentili Ist Spa Acidi dimetilamino-idrossi alchil difosfonici e loro sali, loro procedimento produttivo e composizioni farmaceutiche che li comprendono
ES2096061T3 (es) * 1991-08-27 1997-03-01 Ciba Geigy Ag Acidos aminometanodifosfonicos n-substituidos.
EP0541037A3 (en) * 1991-11-06 1997-02-26 Takeda Chemical Industries Ltd Squalene synthetase inhibitory composition and use thereof
DE4228552A1 (de) * 1992-08-27 1994-03-03 Boehringer Mannheim Gmbh Diphosphonsäuren und deren Salze enthaltende Arzneimittel
EP0600834A1 (en) * 1992-11-30 1994-06-08 Ciba-Geigy Ag Use of methanebisphosphonic acid derivatives for the manufacture of a medicament for fracture healing
AU670337B2 (en) 1992-11-30 1996-07-11 Novartis Ag Use of certain methanebisphosphonic acid derivatives in fracture healing
US6406714B1 (en) 1992-12-02 2002-06-18 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids
ATE176476T1 (de) * 1992-12-02 1999-02-15 Hoechst Ag Guanidinalkyl-1, 1-bisphosphonsäurederivate, verfahren zu ihrer herstellung und ihre verwendung
US5358941A (en) * 1992-12-02 1994-10-25 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids with lactose
US6399592B1 (en) 1992-12-23 2002-06-04 Merck & Co., Inc. Bishphosphonate/estrogen synergistic therapy for treating and preventing bone loss
EP0675723A4 (en) * 1992-12-23 1998-08-05 Merck & Co Inc BIPHOSPHONATE / ESTROGEN THERAPY FOR TREATING AND PREVENTING BONE LOSS.
TW401276B (en) * 1993-10-07 2000-08-11 Zeneca Ltd Novel compounds and a method of controlling growth of plants
US5728650A (en) * 1993-10-07 1998-03-17 Zeneca Limited Herbicidal aza bisphosphonic acids and compositions containing the same
US5591730A (en) * 1993-10-12 1997-01-07 The Regents Of The University Of California Inhibition of urinary calculi growth
US5681873A (en) * 1993-10-14 1997-10-28 Atrix Laboratories, Inc. Biodegradable polymeric composition
US20010007863A1 (en) * 1998-06-18 2001-07-12 Merck & Co., Inc. Wet granulation formulation for bisphosphonic acids
US5780455A (en) * 1994-08-24 1998-07-14 Merck & Co., Inc. Intravenous alendronate formulations
WO1996039107A1 (en) 1995-06-06 1996-12-12 Merck & Co., Inc. Bisphosphonate cement composition to prevent aseptic loosening of orthopedic implant devices
EP0753523A1 (en) * 1995-07-10 1997-01-15 Gador S.A. Amino-substituted bisphosphonic acids
ATE290871T1 (de) * 1995-09-29 2005-04-15 Novartis Pharma Gmbh Verfahren zur behandlung navikularer krankheiten bei pferden
GB9607945D0 (en) * 1996-04-17 1996-06-19 Univ Nottingham Bisphosponates as Anti-inflammatory agents
DE19615812A1 (de) * 1996-04-20 1997-10-23 Boehringer Mannheim Gmbh Pharmazeutische Zubereitung enthaltend Diphosphonsäuren zur oralen Applikation
KR100192215B1 (ko) * 1996-09-03 1999-06-15 강재헌 3-아미노-1-히드록시프로판-1,1-디포스폰산의 제조방법
DE19719680A1 (de) 1997-05-09 1998-11-19 Boehringer Mannheim Gmbh Verwendung von Diphosphonsäuren zur präventiven Behandlung von Spätfolgen bei Harnblasenerweiterung oder Harnblasenersatz
US20010031244A1 (en) * 1997-06-13 2001-10-18 Chiesi Farmaceutici S.P.A. Pharmaceutical aerosol composition
US6432932B1 (en) 1997-07-22 2002-08-13 Merck & Co., Inc. Method for inhibiting bone resorption
US5994329A (en) 1997-07-22 1999-11-30 Merck & Co., Inc. Method for inhibiting bone resorption
US6255359B1 (en) 1997-12-23 2001-07-03 Board Of Regents Of The University Of Texas System Permeable compositions and methods for their preparation
US6187329B1 (en) 1997-12-23 2001-02-13 Board Of Regents Of The University Of Texas System Variable permeability bone implants, methods for their preparation and use
CN1061661C (zh) * 1997-12-24 2001-02-07 国家医药管理局上海医药工业研究院 (环庚基胺基)亚甲基二膦酸二钠一水合物制备方法
US20020128301A1 (en) * 1998-02-13 2002-09-12 Medivir AB Non-nucleoside reverse transcriptase inhibitors
US6733767B2 (en) 1998-03-19 2004-05-11 Merck & Co., Inc. Liquid polymeric compositions for controlled release of bioactive substances
US7128927B1 (en) 1998-04-14 2006-10-31 Qlt Usa, Inc. Emulsions for in-situ delivery systems
EP0998932A1 (de) 1998-10-09 2000-05-10 Boehringer Mannheim Gmbh Feste pharmazeutische Darreichungsform enthaltend Diphosphonsäure oder deren Salze und Verfahren zu ihrer Herstellung
EP0998933A1 (de) 1998-10-09 2000-05-10 Boehringer Mannheim Gmbh Verfahren zur Herstellung von bisphosphonathaltigen pharmazeutischen Zusammensetzungen zur oralen Applikation
BR9915927A (pt) 1998-12-04 2001-08-21 Roche Diagnostics Gmbh Uso de ácido ibandrÈnico ou seus sais ou ésteres fisiologicamente compatìveis
BR0010808A (pt) * 1999-05-21 2002-08-27 Novartis Ag Composições farmacêuticas e usos
AR024462A1 (es) 1999-07-01 2002-10-02 Merck & Co Inc Tabletas farmaceuticas
US8226598B2 (en) * 1999-09-24 2012-07-24 Tolmar Therapeutics, Inc. Coupling syringe system and methods for obtaining a mixed composition
AR021347A1 (es) 1999-10-20 2002-07-17 Cipla Ltd Una composicion farmaceutica que contiene acido(s) bisfosfoncio o sal(es) del mismo y un proceso de preparacion de la misma
US6677320B2 (en) 2000-01-20 2004-01-13 Hoffmann-La Roches Inc. Parenteral bisphosphonate composition with improved local tolerance
US6562974B2 (en) 2000-02-01 2003-05-13 The Procter & Gamble Company Process for making geminal bisphosphonates
US6410520B2 (en) 2000-02-01 2002-06-25 The Procter & Gamble Company Selective crystallization of 3-pyridyl-1-hydroxyethylidene-1, 1-bisphosphonic acid sodium as the hemipentahydrate or monohydrate
SE0000382D0 (sv) 2000-02-07 2000-02-07 Astrazeneca Ab New process
EP1284754B1 (en) 2000-05-05 2006-01-04 F. Hoffmann-La Roche Ag Gel-like pharmaceutical composition for subcutaneous administration comprising bisphosphonic acids or their salts
TWI315982B (en) * 2001-07-19 2009-10-21 Novartis Ag Combinations comprising epothilones and pharmaceutical uses thereof
SK2532004A3 (en) * 2001-12-21 2004-11-03 Procter & Gamble Method for the treatment of bone disorders
US20050070504A1 (en) * 2001-12-21 2005-03-31 The Procter & Gamble Co. Risedronate compositions and their methods of use
AU2002364051A1 (en) * 2002-01-24 2003-09-02 Children's Medical Center Corporation Anti-cancer combination and use thereof
CA2480814A1 (en) * 2002-04-05 2003-10-23 Merck & Co., Inc. Method for inhibiting bone resorption with an alendronate and vitamin d formulation
KR20120065435A (ko) 2002-05-10 2012-06-20 에프. 호프만-라 로슈 아게 골다공증 치료 및 예방용 비스포스폰산
CA2485443C (en) * 2002-05-17 2010-04-06 Teva Pharmaceutical Industries Ltd Use of aromatic hydrocarbons and silicone fluids for making bisphosphonic acids
EP1513523A1 (en) * 2002-06-06 2005-03-16 Merck Frosst Canada & Co. 1,5-disubstituted imidazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of eye and bone diseases
CA2495917A1 (en) * 2002-08-28 2004-03-11 Merck Frosst Canada & Co. Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
US20040138180A1 (en) * 2002-10-03 2004-07-15 Barr Laboratories, Inc. Bisphosphonate composition and process for the preparation thereof
US20040097468A1 (en) * 2002-11-20 2004-05-20 Wimalawansa Sunil J. Method of treating osteoporosis and other bone disorders with upfront loading of bisphosphonates, and kits for such treatment
SG174628A1 (en) 2002-12-20 2011-10-28 Hoffmann La Roche High dose ibandronate formulation
PT1583768E (pt) * 2003-01-17 2008-09-11 Teva Pharma Processo de redução do teor de ferro em risedronato de sódio
PT1656386E (pt) * 2003-08-21 2010-03-05 Sun Pharmaceuticals Ind Ltd Processo para a preparação de compostos de ácido bifosfónico
AU2004266740B2 (en) 2003-08-21 2010-08-26 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
NZ545804A (en) * 2003-09-19 2009-09-25 Wisconsin Alumni Res Found Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-or-vitamin D derivatives and a bisphosphonate
CA2551230A1 (en) 2003-12-23 2005-07-14 Lyogen Limited A process for the preparation of alkyl- and aryl-diphosphonic acids and salts thereof
WO2005090370A1 (en) * 2004-02-05 2005-09-29 The Regents Of The University Of California Pharmacologically active agents containing esterified phosphonates and methods for use thereof
US20050261250A1 (en) * 2004-05-19 2005-11-24 Merck & Co., Inc., Compositions and methods for inhibiting bone resorption
SI1753395T1 (sl) 2004-05-24 2011-01-31 Warner Chilcott Co Llc Enterične trdne formulacije oralnih odmerkov bifosfonata, ki vsebuje kelirno sredstvo
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
MX2007000087A (es) * 2004-06-23 2007-11-06 Teva Pharma Acido ibandronico solido y cristalino.
ATE495747T1 (de) * 2004-08-23 2011-02-15 Teva Pharma Kristalline form des ibandronat-natriums und herstellungsverfahren dafür
WO2006039721A2 (en) * 2004-10-08 2006-04-13 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases
US8012949B2 (en) * 2004-10-08 2011-09-06 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods with enhanced potency for multiple targets including FPPS, GGPPS, and DPPS
US7214818B2 (en) * 2004-10-29 2007-05-08 Hoffmann-La Roche Inc. Method for synthesizing bisphosphonate
US20080069901A1 (en) * 2004-12-10 2008-03-20 Tmrc Co. , Ltd. Therapeutic Agent for Metastatic Cancer and Cancer Metastasis Inhibitor
EP1848727B1 (en) * 2005-02-01 2015-06-17 F.Hoffmann-La Roche Ag Ibandronate polymorph b
AU2006210009B2 (en) * 2005-02-01 2009-08-13 F. Hoffmann-La Roche Ag Ibandronate polymorph A
DK1855674T3 (da) 2005-03-02 2014-10-20 Merck Sharp & Dohme Sammensætning til hæmning af cathepsin k
CN101198316A (zh) * 2005-03-17 2008-06-11 伊兰制药国际有限公司 纳米微粒双膦酸盐组合物
JP2008538354A (ja) * 2005-04-08 2008-10-23 キメリクス，インコーポレイテッド ウイルス感染症およびその他の内科疾患を治療するための化合物、組成物および方法
JP2008535862A (ja) 2005-04-08 2008-09-04 キメリクス，インコーポレイテッド ポックスウイルス感染の治療のための化合物、組成物および方法
WO2007013097A1 (en) * 2005-07-25 2007-02-01 Natco Pharma Limited Improved process for the preparation of ibandronate sodium
US8362086B2 (en) 2005-08-19 2013-01-29 Merial Limited Long acting injectable formulations
US20070049557A1 (en) * 2005-08-24 2007-03-01 Hashim Ahmed Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers
WO2007074475A2 (en) * 2005-12-27 2007-07-05 Natco Pharma Limited Novel polymorphic forms of ibandronate
US20070191315A1 (en) * 2006-02-16 2007-08-16 Bengt Bergstrom Method for administering ibandronate
AU2007226964B2 (en) * 2006-03-17 2012-03-22 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods
AU2007298508B2 (en) 2006-06-23 2012-02-09 Cipla Ltd. Process for the synthesis of ibandronate sodium
CN101506147B (zh) * 2006-09-07 2012-03-21 霍夫曼-拉罗奇有限公司 用于制备snac（n-（8-[2-羟基苯甲酰基]-氨基）辛酸钠）的方法
EP1966227A1 (en) * 2006-11-16 2008-09-10 Teva Pharmaceutical Industries Ltd. Crystalline forms of ibandronate sodium
US20080139514A1 (en) * 2006-11-29 2008-06-12 Subhash Pandurang Gore Diphosphonic acid pharmaceutical compositions
CA2570949A1 (en) * 2006-12-12 2008-06-12 Apotex Pharmachem Inc. Ibandronate sodium propylene glycol solvate and processes for the preparation thereof
CA2671728C (en) * 2006-12-20 2015-05-26 Genpharm Ulc Pharmaceutical composition comprising a hot-melt granulated lubricant
JP2010513328A (ja) 2006-12-20 2010-04-30 ミラン ファーマシューティカルズ ユーエルシー ビタミンｄおよびビスホスホン酸を含有する組成物
US20100144679A1 (en) * 2007-03-21 2010-06-10 Duke University Medication kits and formulations for preventing, treating or reducing secondary fractures after previous fracture
PL2144919T3 (pl) * 2007-04-11 2016-05-31 Hoffmann La Roche Wieloetapowa synteza ibandronianu
CN101679466A (zh) * 2007-04-12 2010-03-24 伊利诺伊大学评议会 对包括fpps、ggpps和dpps在内的多靶点效力提高的二膦酸盐化合物及方法
WO2008131160A1 (en) 2007-04-19 2008-10-30 Dr. Reddy's Laboratories Ltd. Ibandronate sodium polymorphs
US20090042839A1 (en) * 2007-08-09 2009-02-12 Sharon Avhar-Maydan Crystalline forms of ibandronate sodium
US8366706B2 (en) 2007-08-15 2013-02-05 Cardiodex, Ltd. Systems and methods for puncture closure
US20090075944A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched ibandronate
WO2009042179A1 (en) * 2007-09-24 2009-04-02 Teva Pharmaceutical Industries Ltd. Crystalline forms of ibandronic acid and processeses for the preparation thereof
EP2128166A1 (en) 2008-05-20 2009-12-02 Chemo Ibérica, S.A. Polymorphic forms of Ibandronate sodium and processes for preparation thereof
WO2009061336A1 (en) * 2007-11-05 2009-05-14 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of ibandronate disodium
EP2234608A2 (en) 2007-12-11 2010-10-06 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties
WO2009082437A2 (en) 2007-12-21 2009-07-02 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (sarms) and uses thereof
WO2009093258A2 (en) * 2008-01-24 2009-07-30 Fleming Laboratories Limited A new and improved process for the preparation of ibandronate sodium monohydrate
EP3085377A1 (en) * 2008-01-25 2016-10-26 Chimerix, Inc. Methods of treating viral infections
WO2010035664A1 (ja) * 2008-09-24 2010-04-01 田辺三菱製薬株式会社 ビスホスホン酸誘導体の製法
EP2180003A1 (en) 2008-10-21 2010-04-28 Zentiva, k.s. Preparation of ibandronate trisodium
EP2210596A1 (en) 2009-01-22 2010-07-28 Laboratorios Liconsa, S.A. Pharmaceutical composition of ibandronate sodium salt or a hydrate thereof
GB0906068D0 (en) 2009-04-07 2009-05-20 King S College London Bisphosphonate Compounds for chelating radionuclides
US20120100206A1 (en) 2009-06-11 2012-04-26 Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. Targeted liposomes comprising n-containing bisphosphonates and uses thereof
US8614200B2 (en) 2009-07-21 2013-12-24 Chimerix, Inc. Compounds, compositions and methods for treating ocular conditions
BR112012002551A2 (pt) 2009-08-03 2017-06-13 Chimerix Inc composição e métodos de tratamento de infecções virais e tumores induzidos por vírus
WO2011016738A1 (en) 2009-08-05 2011-02-10 Zaklady Farmaceutyczne Polpharma Sa A process for the synthesis of 1-hydroxy-3-(n-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate
HUE025737T2 (en) 2009-09-01 2016-05-30 Univ Duke Bisphosphonate compositions and methods for treating heart failure
FR2954320B1 (fr) 2009-12-17 2012-06-15 Cll Pharma Composition pharmaceutique orale suprabiodisponible contenant un acide biphosphonique ou un de ses sels
PT2534150T (pt) 2010-02-12 2017-05-02 Chimerix Inc Métodos para tratar uma infecção viral
US9278135B2 (en) 2010-04-26 2016-03-08 Chimerix Inc. Methods of treating retroviral infections and related dosage regimes
WO2012007021A1 (en) 2010-07-14 2012-01-19 Pharmathen S.A. Process for the preparation of 3-(n-methyl-n-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid salt or derivatives thereof
TR201100151A2 (tr) 2011-01-06 2012-07-23 Bi̇lgi̇ç Mahmut İbandronate formülasyonu.
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
LT2731591T (lt) 2011-07-13 2020-12-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Liposomos, kuriose kartu inkapsuliuotas bisfosfonatas ir amfipatinis agentas
CA2856030A1 (en) 2011-11-16 2013-05-23 Duke University Bisphosphonate compositions and methods for treating and/or reducing cardiac dysfunction
US8748097B1 (en) 2011-12-02 2014-06-10 President And Fellows Of Harvard College Identification of agents for treating calcium disorders and uses thereof
TR201200588A2 (tr) 2012-01-18 2012-07-23 Koçak Farma İlaç Ve Ki̇mya Sanayi̇ Anoni̇m Şi̇rketi̇ Sodyum ibandronat monohidrat polimorflarini ve polimorflu karışımlarını hazırlamak için prosesler.
GB201200868D0 (en) 2012-01-19 2012-02-29 Depuy Int Ltd Bone filler composition
CN103396332A (zh) * 2013-08-19 2013-11-20 四川协力制药有限公司 3—[（n—甲基—n—戊基）氨基]丙酸盐酸盐的制备方法
CA2923272A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015051479A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015120580A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
PL407922A1 (pl) 2014-04-16 2015-10-26 Wrocławskie Centrum Badań Eit + Spółka Z Ograniczoną Odpowiedzialnością Nowe bisfosfoniany i ich zastosowanie
KR20160147007A (ko) 2014-05-30 2016-12-21 화이자 인코포레이티드 선택적인 안드로겐 수용체 조절제로서의 카보니트릴 유도체
CN111225672B (zh) 2017-10-16 2023-09-29 清华大学 甲羟戊酸通路抑制剂及其药物组合物
KR20200085441A (ko) 2019-01-07 2020-07-15 엠에프씨 주식회사 이반드로네이트의 신규한 결정형 및 이의 제조방법
KR20220115062A (ko) 2021-02-09 2022-08-17 (주)오스티오뉴로젠 크로몬 구조의 화합물을 포함하는 골다공증의 예방 및 치료용 약학적 조성물
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH9776A (en) * 1967-12-11 1976-03-17 M Francis Compositions for inhibiting anomalous deposition and mobilization of calcium phosphate in animal tissue and method of use
US3733270A (en) * 1971-03-08 1973-05-15 Monsanto Co Methods of scale inhibition
DE2405254C2 (de) * 1974-02-04 1982-05-27 Henkel KGaA, 4000 Düsseldorf Verwendung von 3-Amino-1-Hydroxypropan-1, 1-diphosphonsäure oder ihrer wasserlöslichen Salze bei der Beeinflußung von Calciumstoffwechselstörungen im menschlichen oder tierischen Körper
US4134969A (en) * 1974-02-04 1979-01-16 Henkel Kommanditgesellschaft Auf Aktien (Henkel Kgaa) Method of treatment of calcium disorders using aminoalkane-diphosphonic acids
DE2534391C2 (de) * 1975-08-01 1983-01-13 Henkel KGaA, 4000 Düsseldorf 1-Hydroxy-3-aminoalkan-1,1-diphosphonsäuren
SU739076A1 (ru) * 1976-05-19 1980-06-05 Институт Химической Кинетики И Горения Со Ан Ссср Способ получени -аминоэтилидендифосфоновых кислот
DE2702631A1 (de) * 1977-01-22 1978-07-27 Henkel Kgaa Verfahren zur herstellung von 1-hydroxy-3-amino-propan-1,1-diphosphonsaeuren
DE2943498C2 (de) * 1979-10-27 1983-01-27 Henkel KGaA, 4000 Düsseldorf Verfahren zur Herstellung von 3-Amino-1-hydroxypropan-1,1-diphosphonsäure
SU1002300A1 (ru) * 1981-10-29 1983-03-07 Ордена Ленина институт элементоорганических соединений им.А.Н.Несмеянова Способ получени @ -аминозамещенных- @ -оксипропилидендифосфоновых кислот
DE3365492D1 (en) * 1982-01-27 1986-10-02 Schering Ag Diphosphonic acid derivatives and pharmaceutical preparations containing them
IT1201087B (it) * 1982-04-15 1989-01-27 Gentili Ist Spa Bifosfonati farmacologicamente attivi,procedimento per la loro preparazione e relative composizioni farmaceutiche
ATE26071T1 (de) * 1982-06-10 1987-04-15 Mallinckrodt Inc Roentgen-sichtbarmachungsmittel.
DE3434667A1 (de) * 1984-09-21 1986-04-03 Henkel KGaA, 4000 Düsseldorf 4-dimethylamino-1-hydroxybutan-1,1-diphosphonsaeure, deren wasserloesliche salze, verfahren zu ihrer herstellung sowie ihre verwendung
DE3540150A1 (de) * 1985-11-13 1987-05-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
DE3623397A1 (de) * 1986-07-11 1988-01-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel

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