CN1022630C - (环烷基胺基)亚甲基双(膦酸)化合物的制备方法 - Google Patents

(环烷基胺基)亚甲基双(膦酸)化合物的制备方法 Download PDF

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Publication number
CN1022630C
CN1022630C CN89101539A CN89101539A CN1022630C CN 1022630 C CN1022630 C CN 1022630C CN 89101539 A CN89101539 A CN 89101539A CN 89101539 A CN89101539 A CN 89101539A CN 1022630 C CN1022630 C CN 1022630C
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CN
China
Prior art keywords
compound
preparation example
lower alkyl
phosphonic acid
bone
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Expired - Lifetime
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CN89101539A
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English (en)
Chinese (zh)
Other versions
CN1035829A (zh
Inventor
矶村八州男
竹内诚
坂本修一
阿部哲士
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Yamanouchi Pharmaceutical Co Ltd
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Yamanouchi Pharmaceutical Co Ltd
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Publication of CN1035829A publication Critical patent/CN1035829A/zh
Priority to CN92114203A priority Critical patent/CN1046853C/zh
Application granted granted Critical
Publication of CN1022630C publication Critical patent/CN1022630C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • 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)
    • 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
    • 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
    • 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)

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN89101539A 1988-01-20 1989-01-20 (环烷基胺基)亚甲基双(膦酸)化合物的制备方法 Expired - Lifetime CN1022630C (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN92114203A CN1046853C (zh) 1988-01-20 1992-12-11 制备药用组合物的方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP1165688 1988-01-20
JP11656/1988 1988-01-20

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN92114203A Division CN1046853C (zh) 1988-01-20 1992-12-11 制备药用组合物的方法

Publications (2)

Publication Number Publication Date
CN1035829A CN1035829A (zh) 1989-09-27
CN1022630C true CN1022630C (zh) 1993-11-03

Family

ID=11784011

Family Applications (1)

Application Number Title Priority Date Filing Date
CN89101539A Expired - Lifetime CN1022630C (zh) 1988-01-20 1989-01-20 (环烷基胺基)亚甲基双(膦酸)化合物的制备方法

Country Status (14)

Country Link
US (2) US4970335A (2)
EP (1) EP0325482B1 (2)
KR (1) KR970005179B1 (2)
CN (1) CN1022630C (2)
AT (1) ATE74361T1 (2)
AU (1) AU615711B2 (2)
CA (1) CA1339805C (2)
DE (1) DE68901097D1 (2)
DK (1) DK174744B1 (2)
ES (1) ES2032105T3 (2)
GR (1) GR3004461T3 (2)
HU (1) HU202243B (2)
IE (1) IE60477B1 (2)
PH (1) PH26819A (2)

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CA1339805C (en) * 1988-01-20 1998-04-07 Yasuo Isomura (cycloalkylamino)methylenebis(phosphonic acid) and medicines containing the same as an active
IE912115A1 (en) * 1990-06-25 1992-01-01 Takeda Chemical Industries Ltd Bisphosphonic acid derivatives, their production and use
US5073339A (en) * 1990-08-23 1991-12-17 W. R. Grace & Co. - Conn Method of inhibiting corrosion and scale formation in aqueous systems
ATE133677T1 (de) * 1990-12-19 1996-02-15 Takeda Chemical Industries Ltd Bisphosphonsäurederivate, ihre produktion und ihre verwendung
AU642336B2 (en) * 1991-02-07 1993-10-14 Kaken Pharmaceutical Co., Ltd. Bisphosphonic acid derivatives, their intermediates and bone resorption inhibitors containing them as active ingredients
DE69224830D1 (en) * 1991-06-19 1998-04-23 Upjohn Co Dialkyl (dialkoxyphosphinyl)methyl phosphate als antientzündungsmittel
EP0522576A3 (en) * 1991-07-12 1993-07-14 Hoechst Aktiengesellschaft Aminoethane-1,1-bisphosphonic acids and aminoethane-1,1-alkylphospinic/phosphonic acids, process of their preparation and their use
EP0541037A3 (en) * 1991-11-06 1997-02-26 Takeda Chemical Industries Ltd Squalene synthetase inhibitory composition and use thereof
US5391743A (en) * 1992-05-29 1995-02-21 Procter & Gamble Pharmaceuticals, Inc. Quaternary nitrogen-containing phosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism and methods of treating and preventing dental calculus and plaque
US5358941A (en) 1992-12-02 1994-10-25 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids with lactose
US6406714B1 (en) 1992-12-02 2002-06-18 Merck & Co., Inc. Dry mix formulation for bisphosphonic acids
US6399592B1 (en) 1992-12-23 2002-06-04 Merck & Co., Inc. Bishphosphonate/estrogen synergistic therapy for treating and preventing bone loss
FR2703590B1 (fr) * 1993-04-05 1995-06-30 Sanofi Elf Utilisation de derives d'acide bisphosphonique pour la preparation de medicaments destines a favoriser la reparation osseuse .
US5854227A (en) * 1994-03-04 1998-12-29 Hartmann; John F. Therapeutic derivatives of diphosphonates
US20010007863A1 (en) * 1998-06-18 2001-07-12 Merck & Co., Inc. Wet granulation formulation for bisphosphonic acids
JPH11511041A (ja) 1995-06-06 1999-09-28 メルク エンド カンパニー インコーポレーテッド 整形外科的埋め込み装置の無菌性動揺を防止するビスホスホネートセメント組成物
US20030096760A1 (en) * 1997-03-10 2003-05-22 Smithklinebeecham Corporation Method of antagonizing the human SRC SH2 domain
IT1303672B1 (it) 1998-07-28 2001-02-23 Nicox Sa Sali nitrati di farmaci attivi nei disordini ossei
AR024462A1 (es) 1999-07-01 2002-10-02 Merck & Co Inc Tabletas farmaceuticas
AU1549001A (en) * 1999-11-25 2001-06-04 Yamanouchi Pharmaceutical Co., Ltd. Remedies for periodontosis
US6677320B2 (en) 2000-01-20 2004-01-13 Hoffmann-La Roches Inc. Parenteral bisphosphonate composition with improved local tolerance
US20050070504A1 (en) * 2001-12-21 2005-03-31 The Procter & Gamble Co. Risedronate compositions and their methods of use
SK2532004A3 (en) * 2001-12-21 2004-11-03 Procter & Gamble Method for the treatment of bone disorders
JP4502641B2 (ja) * 2002-01-24 2010-07-14 ティルタン ファーマ リミテッド 抗癌組み合わせおよびその使用方法
KR20060058151A (ko) * 2002-05-10 2006-05-29 에프. 호프만-라 로슈 아게 골다공증 치료 및 예방용 비스포스폰산
WO2003103664A1 (en) * 2002-06-06 2003-12-18 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
AU2003258433A1 (en) * 2002-08-28 2004-03-19 Merck Frosst Canada Ltd Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
ES2291749T5 (es) 2002-12-20 2011-07-21 F. Hoffmann-La Roche Ag Formulación de altas dosis de ibandronato.
AU2004266740B2 (en) 2003-08-21 2010-08-26 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
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
US20050261250A1 (en) * 2004-05-19 2005-11-24 Merck & Co., Inc., Compositions and methods for inhibiting bone resorption
DK2283825T3 (da) 2004-05-24 2022-06-27 Theramex Hq Uk Ltd Enterisk fast oral doseringsform af en bisfosfonat indeholdende et chelateringsmiddel
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
AU2006302797B2 (en) 2005-03-02 2012-02-02 Merck Canada Inc. Composition for inhibition of 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
JP2011517313A (ja) 2007-12-11 2011-06-02 ビアメト ファーマシューティカルズ，インク． 金属結合部分を標的化部分と組み合わせて使用する金属酵素阻害剤
KR101595238B1 (ko) 2007-12-21 2016-02-18 리간드 파마슈티칼스 인코포레이티드 선택적 안드로겐 수용체 조절제(ｓａｒｍ) 및 이의 용도
US20090181138A1 (en) 2008-01-11 2009-07-16 David Howard Process for producing precooked bacon slices
FR2954320B1 (fr) 2009-12-17 2012-06-15 Cll Pharma Composition pharmaceutique orale suprabiodisponible contenant un acide biphosphonique ou un de ses sels
WO2012112363A1 (en) 2011-02-14 2012-08-23 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
GB201200868D0 (en) 2012-01-19 2012-02-29 Depuy Int Ltd Bone filler composition
WO2015054089A1 (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
SG11201609050UA (en) 2014-05-30 2016-12-29 Pfizer Carbonitrile derivatives as selective androgen receptor modulators
AU2020257397B2 (en) 2019-04-19 2026-02-26 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
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DE1958123C3 (de) * 1969-11-19 1978-09-28 Henkel Kgaa, 4000 Duesseldorf Verfahren zur Herstellung von 1 -Aminoalkan-1,1 -diphosphonsäuren oder deren Salzen
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CA1339805C (en) * 1988-01-20 1998-04-07 Yasuo Isomura (cycloalkylamino)methylenebis(phosphonic acid) and medicines containing the same as an active
JPH01231980A (ja) * 1988-03-10 1989-09-18 Ishikawajima Harima Heavy Ind Co Ltd 管内作業用ピグ

Also Published As

Publication number Publication date
IE890183L (en) 1989-07-20
AU615711B2 (en) 1991-10-10
ES2032105T3 (es) 1993-01-01
IE60477B1 (en) 1994-07-13
DE68901097D1 (de) 1992-05-07
EP0325482A1 (en) 1989-07-26
AU2867089A (en) 1989-07-20
EP0325482B1 (en) 1992-04-01
ATE74361T1 (de) 1992-04-15
CN1035829A (zh) 1989-09-27
DK24389D0 (da) 1989-01-20
DK24389A (da) 1989-07-21
PH26819A (en) 1992-11-05
US4970335A (en) 1990-11-13
KR970005179B1 (ko) 1997-04-14
KR890011601A (ko) 1989-08-21
HU202243B (en) 1991-02-28
GR3004461T3 (2) 1993-03-31
CA1339805C (en) 1998-04-07
US5041428A (en) 1991-08-20
HUT50841A (en) 1990-03-28
DK174744B1 (da) 2003-10-13

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