KR100258283B1 - 신규한 중간체를 사용하여, 말단 아미노-1-하이드록시-알킬리덴-1,1-비스포스폰산을 제조하는 방법 - Google Patents

신규한 중간체를 사용하여, 말단 아미노-1-하이드록시-알킬리덴-1,1-비스포스폰산을 제조하는 방법 Download PDF

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KR100258283B1
KR100258283B1 KR1019960700883A KR19960700883A KR100258283B1 KR 100258283 B1 KR100258283 B1 KR 100258283B1 KR 1019960700883 A KR1019960700883 A KR 1019960700883A KR 19960700883 A KR19960700883 A KR 19960700883A KR 100258283 B1 KR100258283 B1 KR 100258283B1
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compound
formula
acid
msa
alkyl
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KR1019960700883A
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Korean (ko)
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KR960703932A (ko
Inventor
알. 다우어 리차드
디미쉘 리사
푸트란 마우리시오
알. 키에치코브스키 게라드
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폴락 돈나 엘.
머크 앤드 컴퍼니 인코포레이티드
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Priority claimed from US08/286,151 external-priority patent/US5510517A/en
Application filed by 폴락 돈나 엘., 머크 앤드 컴퍼니 인코포레이티드 filed Critical 폴락 돈나 엘.
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    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • 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
    • C07F9/3873Polyphosphonic 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)
    • 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)]
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • 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
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1019960700883A 1993-08-25 1994-08-24 신규한 중간체를 사용하여, 말단 아미노-1-하이드록시-알킬리덴-1,1-비스포스폰산을 제조하는 방법 Expired - Lifetime KR100258283B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US11175193A 1993-08-25 1993-08-25
US08/111,751 1993-08-25
US8/111751 1993-08-25
US08/286,151 US5510517A (en) 1993-08-25 1994-08-04 Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
US08/286,151 1994-08-04
US8/286151 1994-08-04
PCT/US1994/009620 WO1995006052A1 (en) 1993-08-25 1994-08-24 Process for producing n-amino-1-hydroxy-alkyl-idene-1,1-bisphosphonic acids

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1019997012458A Division KR100261202B1 (ko) 1993-08-25 1994-08-24 신규한 중간체를 사용하여, 말단아미노-1-하이드록시-알킬리덴-1,1-비스포스폰산을제조하는 방법

Publications (2)

Publication Number Publication Date
KR960703932A KR960703932A (ko) 1996-08-31
KR100258283B1 true KR100258283B1 (ko) 2000-07-01

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ID=27381052

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KR1019960700883A Expired - Lifetime KR100258283B1 (ko) 1993-08-25 1994-08-24 신규한 중간체를 사용하여, 말단 아미노-1-하이드록시-알킬리덴-1,1-비스포스폰산을 제조하는 방법

Country Status (5)

Country Link
US (1) US5648491A (OSRAM)
KR (1) KR100258283B1 (OSRAM)
TW (1) TW257765B (OSRAM)
UA (1) UA54368C2 (OSRAM)
YU (1) YU49227B (OSRAM)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030078211A1 (en) * 1998-06-24 2003-04-24 Merck & Co., Inc. Compositions and methods for inhibiting bone resorption
AU757104B2 (en) 1998-06-24 2003-01-30 Merck & Co., Inc. Compositions and methods for inhibiting bone resorption
US6331533B1 (en) 1998-11-16 2001-12-18 Merck & Co., Inc. Method for inhibiting dental resorptive lesions
ES2153794B1 (es) 1999-08-06 2001-10-16 Medichem Sa Procedimiento para la obtencion del acido 4-amino-1-hidroxibutiliden-1,1-bisfosfonico y de su sal monosodica trihidratada.
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
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
IL165227A0 (en) * 2002-05-17 2005-12-18 Tva Pharmaceutical Ind Ltd Cus of certain diluents for making bisphosphonic acids
CA2487977A1 (en) * 2002-06-06 2003-12-18 Merck Frosst Canada & Co./Merck Frosst Canada & Cie 1,5-disubstituted imidazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of eye and bone diseases
JP4485117B2 (ja) * 2002-06-27 2010-06-16 日東電工株式会社 保護剥離用フィルム
WO2004019938A1 (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
US20040206932A1 (en) * 2002-12-30 2004-10-21 Abuelyaman Ahmed S. Compositions including polymerizable bisphosphonic acids and methods
EP1653913B1 (en) * 2003-08-12 2012-05-23 3M Innovative Properties Company Self-etching dental compositions and methods
WO2005019161A1 (en) 2003-08-21 2005-03-03 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
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
CN101018534B (zh) 2004-07-08 2012-07-04 3M创新有限公司 牙科的方法,组合物,和包括酸敏感染料的试剂盒
WO2006020760A1 (en) 2004-08-11 2006-02-23 3M Innovative Properties Company Self-adhesive compositions including a plurality of acidic compounds
DK1855674T3 (da) 2005-03-02 2014-10-20 Merck Sharp & Dohme Sammensætning til hæmning af cathepsin k
WO2006134603A1 (en) * 2005-06-13 2006-12-21 Jubilant Organosys Limited Process for producing bisphosphonic acids and forms thereof
JP5354858B2 (ja) * 2006-05-09 2013-11-27 株式会社Adeka スルホンアミド化合物の金属塩を含有するポリエステル樹脂組成物
MX2008014248A (es) 2006-05-11 2009-02-23 Ind Swift Lab Ltd Proceso para la preparacion de sales y acido risedronico puros.
CN101557791B (zh) * 2006-12-13 2013-05-22 3M创新有限公司 使用具有酸性组分和可光漂白染料的牙科用组合物的方法
DK2222636T3 (da) * 2007-12-21 2013-06-03 Ligand Pharm Inc Selektive androgenreceptormodulatorer (SARMS) og anvendelser deraf
JP5748759B2 (ja) 2009-10-02 2015-07-15 ストレイトマーク・ホールディング・アーゲー アミノヒドロキシジホスホン酸の製造方法
CA2738045C (en) 2010-05-28 2019-02-19 Simon Fraser University Conjugate compounds, methods of making same, and uses thereof
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015051479A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
AU2014332250B2 (en) 2013-10-08 2018-07-19 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015120580A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
US9650414B1 (en) 2014-05-30 2017-05-16 Simon Fraser University Dual-action EP4 agonist—bisphosphonate conjugates and uses thereof
CA2950390C (en) 2014-05-30 2020-09-22 Pfizer Inc. Carbonitrile derivatives as selective androgen receptor modulators
JP7174982B2 (ja) 2015-06-12 2022-11-18 サイモン フレイザー ユニヴァーシティー アミド連結ep4アゴニスト-ビスホスホネート化合物およびその使用
WO2020019108A1 (en) 2018-07-23 2020-01-30 Guangzhou Othrotx Co., Ltd. Bisphosphonate drug conjugates
US12319651B2 (en) 2019-04-19 2025-06-03 Ligand Pharmaceuticals Incorporated Crystalline forms and methods of producing crystalline forms of a compound
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3016289A1 (de) * 1980-04-28 1981-10-29 Henkel KGaA, 4000 Düsseldorf Verfahren zur herstellung von omega -amino-1-hydroxyalkyliden-1,1-bis-phosphonsaeuren
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

Also Published As

Publication number Publication date
US5648491A (en) 1997-07-15
YU51694A (sh) 1997-09-30
TW257765B (OSRAM) 1995-09-21
KR960703932A (ko) 1996-08-31
YU49227B (sh) 2004-11-25
UA54368C2 (uk) 2003-03-17

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