DE69406936D1 - Verfahren zur herstellung von amino-1-hydroxy-alkyliden-1,1-bisphosphonsäuren - Google Patents

Verfahren zur herstellung von amino-1-hydroxy-alkyliden-1,1-bisphosphonsäuren

Info

Publication number
DE69406936D1
DE69406936D1 DE69406936T DE69406936T DE69406936D1 DE 69406936 D1 DE69406936 D1 DE 69406936D1 DE 69406936 T DE69406936 T DE 69406936T DE 69406936 T DE69406936 T DE 69406936T DE 69406936 D1 DE69406936 D1 DE 69406936D1
Authority
DE
Germany
Prior art keywords
alkyliden
hydroxy
bisphosphonic acids
producing amino
producing
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
DE69406936T
Other languages
English (en)
Other versions
DE69406936T2 (de
Inventor
Richard Dauer
Lisa Dimichele
Mauricio Futran
Gerard Kieczykowski
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 Sharp and Dohme LLC
Original Assignee
Merck and Co Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27381051&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE69406936(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of DE69406936D1 publication Critical patent/DE69406936D1/de
Publication of DE69406936T2 publication Critical patent/DE69406936T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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
    • C07F9/547Heterocyclic 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
    • C07F9/547Heterocyclic 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

Landscapes

  • 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
DE69406936T 1993-08-25 1994-08-24 Verfahren zur herstellung von amino-1-hydroxy-alkyliden-1,1-bisphosphonsäuren Expired - Lifetime DE69406936T2 (de)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US11175193A 1993-08-25 1993-08-25
US23964094A 1994-05-09 1994-05-09
US08/286,151 US5510517A (en) 1993-08-25 1994-08-04 Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
PCT/US1994/009620 WO1995006052A1 (en) 1993-08-25 1994-08-24 Process for producing n-amino-1-hydroxy-alkyl-idene-1,1-bisphosphonic acids

Publications (2)

Publication Number Publication Date
DE69406936D1 true DE69406936D1 (de) 1998-01-02
DE69406936T2 DE69406936T2 (de) 1998-06-04

Family

ID=27381051

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69406936T Expired - Lifetime DE69406936T2 (de) 1993-08-25 1994-08-24 Verfahren zur herstellung von amino-1-hydroxy-alkyliden-1,1-bisphosphonsäuren

Country Status (25)

Country Link
US (1) US5510517A (de)
EP (1) EP0715631B1 (de)
JP (1) JP3675818B2 (de)
KR (1) KR100261202B1 (de)
CN (2) CN1067079C (de)
AT (1) ATE160352T1 (de)
AU (2) AU692468B2 (de)
BR (1) BR9407563A (de)
CA (1) CA2169561C (de)
CY (1) CY2086B1 (de)
CZ (1) CZ290185B6 (de)
DE (1) DE69406936T2 (de)
DK (1) DK0715631T3 (de)
ES (1) ES2109731T3 (de)
FI (1) FI115526B (de)
GR (1) GR3025450T3 (de)
HK (1) HK1008883A1 (de)
HR (1) HRP940479B1 (de)
HU (1) HU217362B (de)
LV (1) LV12189B (de)
NZ (1) NZ273458A (de)
RO (1) RO115524B1 (de)
RU (1) RU2154647C2 (de)
SI (1) SI0715631T1 (de)
WO (1) WO1995006052A1 (de)

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US5449819A (en) * 1994-06-06 1995-09-12 Merck & Co., Inc. Process for removing waste pox, alendronate and its by products
US5589691A (en) * 1994-06-06 1996-12-31 Merck & Co., Inc. Process for recovery and recycle of methanesulfonic acid and phosphorous acid
AU723357B2 (en) * 1996-10-04 2000-08-24 Merck & Co., Inc. Liquid alendronate formulations
CA2197267C (en) * 1997-02-11 2000-02-08 Yong Tao Process for the production of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
GB9800452D0 (en) * 1998-01-10 1998-03-04 Albright & Wilson Preparation of phosphonic acid derivatives
US6432931B1 (en) 1998-06-24 2002-08-13 Merck & Co., Inc. Compositions and methods for inhibiting bone resorption
US20030078211A1 (en) * 1998-06-24 2003-04-24 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.
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
ITMI20020908A1 (it) * 2002-04-29 2003-10-29 Chemi Spa Processo di preparazione di sodio alendronato
KR20120065435A (ko) * 2002-05-10 2012-06-20 에프. 호프만-라 로슈 아게 골다공증 치료 및 예방용 비스포스폰산
ATE461205T1 (de) * 2002-05-17 2010-04-15 Teva Pharma Verwendung von bestimmten lösungsmitteln zur herstellung von bisphosphonsäuren
JP2005534653A (ja) * 2002-06-06 2005-11-17 メルク フロスト カナダ アンド カンパニー 眼及び骨疾患の治療に於いてep4受容体作動薬として使用するための1,5−二置換イミダゾリジン−2−オン誘導体
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
EP1545517A1 (de) * 2002-08-28 2005-06-29 Merck Frosst Canada & Co. Oxazolidin-2-on und thiazolidin-2-on-derivate zur verwendung als ep4-rezeptor-agonisten bei der behandlung von glaukom
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
WO2005018581A2 (en) * 2003-08-12 2005-03-03 3M Innovative Properties Company Self-etching dental compositions and methods
EP1673336B1 (de) 2003-08-21 2014-06-04 Merck Canada Inc. Cathepsincysteinproteasehemmer
CA2539359A1 (en) * 2003-09-19 2005-03-31 Pfizer Products Inc. Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and a bisphosphonate
US20050181043A1 (en) * 2004-02-12 2005-08-18 Indranil Nandi Alendronate salt tablet compositions
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
CA2573020A1 (en) * 2004-07-08 2006-02-09 3M Innovative Properties Company Dental methods, compositions, and kits including acid-sensitive dyes
EP1784155B1 (de) * 2004-08-11 2011-09-28 3M Innovative Properties Company Selbstklebende zusammensetzungen mit einer vielzahl von sauren verbindungen
EP1855674B1 (de) 2005-03-02 2014-07-16 Merck Sharp & Dohme Corp. Zusammensetzung zur hemmung von cathepsin k
CA2606879A1 (en) * 2005-05-06 2007-03-01 Medichem, S.A. Process of making geminal bisphosphonic acids and pharmaceutically acceptable salts and/or hydrates thereof
US8003820B2 (en) 2005-10-20 2011-08-23 Dr. Reddy's Laboratories Limited Process for preparing bisphosphonic acids
AR058168A1 (es) * 2005-11-07 2008-01-23 Merck & Co Inc Sintesis del alendronato de sodio trihidratado
WO2007083240A2 (en) 2006-01-20 2007-07-26 Aurobindo Pharma Limited An improved process for the preparation of bisphosphonic acids
WO2007096896A1 (en) * 2006-02-20 2007-08-30 Alembic Limited An improved process for the preparation of biphosphonic derivatives
EP2101716A2 (de) 2006-12-13 2009-09-23 3M Innovative Properties Company Verfahren zur verwendung einer dentalen zusammensetzung mit saurer komponente und lichtbleichbarem farbstoff
WO2008157050A1 (en) * 2007-06-19 2008-12-24 Albemarle Corporation Processes for manufacturing bisphosphonic acids
EP2489656A1 (de) 2007-12-21 2012-08-22 Ligand Pharmaceuticals Inc. Selektive Androgenrezeptormodulatoren (SARMS) und ihre Verwendung
US8026388B2 (en) * 2008-07-11 2011-09-27 Synthon Bv Process for making 1-hydroxyalkylidene-1,1-biphosphonic acids
US20100130746A1 (en) * 2008-11-26 2010-05-27 Martin Kas Process for Making Zoledronic Acid
EP2192126B1 (de) 2008-11-26 2013-03-27 Synthon B.V. Verfahren zur Herstellung von Zoledronsäure
EA201270328A1 (ru) 2009-08-28 2012-09-28 Синтон Б. В. Способ получения 1-гидроксиалкилиден-1,1-дифосфоновых кислот
EP2493905B1 (de) 2009-10-26 2016-11-30 Warner Chilcott Company, LLC Bisphosphonatverbindungen zur behandlung von gestörtem knochenmetabolismus
CA2738045C (en) 2010-05-28 2019-02-19 Simon Fraser University Conjugate compounds, methods of making same, and uses thereof
BR112013010476B1 (pt) 2010-12-06 2021-07-06 Effrx Pharmaceuticals Sa formulações efervescentes estáveis de bisfosfonato com características de solubilização rápida
EP2675440B1 (de) 2011-02-14 2020-03-25 Merck Sharp & Dohme Corp. Cathepsin-cysteinproteasehemmer
FI20115315A0 (fi) * 2011-04-01 2011-04-01 Itae Suomen Yliopisto Menetelmä metallien keräämiseksi
CN105593230B (zh) 2013-10-08 2018-07-06 默沙东公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
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
KR20160147007A (ko) 2014-05-30 2016-12-21 화이자 인코포레이티드 선택적인 안드로겐 수용체 조절제로서의 카보니트릴 유도체
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
EP3827010A4 (de) 2018-07-23 2022-03-16 Brise Pharmaceuticals Co., Ltd. Bisphosphonat-wirkstoff-konjugate
CN109456363A (zh) * 2018-11-01 2019-03-12 南京海纳医药科技股份有限公司 一种米诺膦酸工艺杂质的制备方法
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

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DD216465A1 (de) * 1983-07-01 1984-12-12 Agrochemie Piesteritz 4602 Wit Verfahren zur herstellung substituierter alkanphosphonsaeuren
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
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Also Published As

Publication number Publication date
GR3025450T3 (en) 1998-02-27
AU692468B2 (en) 1998-06-11
ATE160352T1 (de) 1997-12-15
LV12189A (lv) 1998-12-20
HU217362B (hu) 2000-01-28
DE69406936T2 (de) 1998-06-04
HUT75261A (en) 1997-05-28
HRP940479A2 (en) 1997-02-28
CZ290185B6 (cs) 2002-06-12
RO115524B1 (ro) 2000-03-30
RU2154647C2 (ru) 2000-08-20
HRP940479B1 (en) 2000-10-31
WO1995006052A1 (en) 1995-03-02
CZ54296A3 (en) 1996-10-16
AU7993798A (en) 1998-10-15
ES2109731T3 (es) 1998-01-16
AU7674394A (en) 1995-03-21
CA2169561A1 (en) 1995-03-02
SI0715631T1 (en) 1998-02-28
CN1211392C (zh) 2005-07-20
CN1308082A (zh) 2001-08-15
EP0715631A1 (de) 1996-06-12
HU9600429D0 (en) 1996-04-29
HK1008883A1 (en) 1999-05-21
LV12189B (en) 1999-02-20
CN1067079C (zh) 2001-06-13
AU714996B2 (en) 2000-01-13
CY2086B1 (en) 2002-04-05
CA2169561C (en) 2007-02-20
NZ273458A (en) 1998-04-27
KR100261202B1 (ko) 2000-07-01
DK0715631T3 (da) 1997-12-22
US5510517A (en) 1996-04-23
CN1134703A (zh) 1996-10-30
BR9407563A (pt) 1996-12-31
EP0715631B1 (de) 1997-11-19
FI115526B (fi) 2005-05-31
JPH09501935A (ja) 1997-02-25
JP3675818B2 (ja) 2005-07-27
FI960851A0 (fi) 1996-02-23
FI960851A (fi) 1996-02-23

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