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)
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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
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Classifications

    • 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
JP11656/1988 1988-01-20
JP1165688 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 (https=)
EP (1) EP0325482B1 (https=)
KR (1) KR970005179B1 (https=)
CN (1) CN1022630C (https=)
AT (1) ATE74361T1 (https=)
AU (1) AU615711B2 (https=)
CA (1) CA1339805C (https=)
DE (1) DE68901097D1 (https=)
DK (1) DK174744B1 (https=)
ES (1) ES2032105T3 (https=)
GR (1) GR3004461T3 (https=)
HU (1) HU202243B (https=)
IE (1) IE60477B1 (https=)
PH (1) PH26819A (https=)

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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
IE914417A1 (en) * 1990-12-19 1992-07-01 Takeda Chemical Industries Ltd Bisphosphonic acid derivatives, their production and use
US5350743A (en) * 1991-02-07 1994-09-27 Kaken Pharmaceutical Co., Ltd. Bisphosphonic acid derivatives, as bone resorption inhibitors
CA2102303A1 (en) * 1991-06-19 1992-12-20 Roy Allen Johnson Dialkyl (dialkoxyphosphinyl) methyl phosphates as anti-inflammatory agents
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
WO1996039107A1 (en) 1995-06-06 1996-12-12 Merck & Co., Inc. Bisphosphonate cement composition to prevent aseptic loosening of orthopedic implant devices
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
US6682718B1 (en) * 1999-11-25 2004-01-27 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
RU2294203C2 (ru) * 2001-12-21 2007-02-27 Дзе Проктер Энд Гэмбл Компани Способ лечения костных нарушений
US20050070504A1 (en) * 2001-12-21 2005-03-31 The Procter & Gamble Co. Risedronate compositions and their methods of use
CA2472578A1 (en) * 2002-01-24 2003-07-31 Yissum Research Development Company Of The Hebrew University Of Jerusalem Anti-cancer combination and use thereof
RU2387451C2 (ru) 2002-05-10 2010-04-27 Ф.Хоффманн-Ля Рош Аг Бисфосфоновые кислоты, предназначенные для лечения и профилактики остеопороза
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
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
HRP20041013B1 (hr) 2002-12-20 2013-10-25 F. Hoffmann - La Roche Ag Formulacija visoke doze ibandronata
CN1839114A (zh) 2003-08-21 2006-09-27 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
WO2005027921A1 (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
NZ551118A (en) 2004-05-24 2010-09-30 Warner Chilcott Co Llc Enteric solid oral dosage form of bisphosphonate containing a chelating agent
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
BRPI0606280A2 (pt) * 2005-03-17 2009-06-09 Elan Pharma Int Ltd composições de bisfosfonato nanoparticulado
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
EP2222636B1 (en) 2007-12-21 2013-04-10 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
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
US8791162B2 (en) 2011-02-14 2014-07-29 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
GB201200868D0 (en) 2012-01-19 2012-02-29 Depuy Int Ltd Bone filler composition
WO2015051479A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
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
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
ES2864079T3 (es) 2014-05-30 2021-10-13 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos
WO2020214834A1 (en) 2019-04-19 2020-10-22 Ligand Pharmaceuticals Inc. 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 (6)

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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
DE2037586C3 (de) * 1970-07-29 1980-05-22 Henkel Kgaa, 4000 Duesseldorf Gipsmassen
DE2104476C2 (de) * 1971-02-01 1983-12-01 Henkel KGaA, 4000 Düsseldorf Verfahren zur Verhinderung von Ausfällungen in Wasser oder wäßrigen Lösungen
DE3540150A1 (de) * 1985-11-13 1987-05-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
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
US5041428A (en) 1991-08-20
CN1035829A (zh) 1989-09-27
EP0325482A1 (en) 1989-07-26
DE68901097D1 (de) 1992-05-07
IE60477B1 (en) 1994-07-13
DK24389D0 (da) 1989-01-20
ATE74361T1 (de) 1992-04-15
AU615711B2 (en) 1991-10-10
KR970005179B1 (ko) 1997-04-14
GR3004461T3 (https=) 1993-03-31
EP0325482B1 (en) 1992-04-01
US4970335A (en) 1990-11-13
AU2867089A (en) 1989-07-20
KR890011601A (ko) 1989-08-21
DK174744B1 (da) 2003-10-13
PH26819A (en) 1992-11-05
CA1339805C (en) 1998-04-07
ES2032105T3 (es) 1993-01-01
DK24389A (da) 1989-07-21
HUT50841A (en) 1990-03-28
IE890183L (en) 1989-07-20
HU202243B (en) 1991-02-28

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