FI104901B - Nya metylenbisfosfonsyraderivat - Google Patents

Nya metylenbisfosfonsyraderivat Download PDF

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Publication number
FI104901B
FI104901B FI974001A FI974001A FI104901B FI 104901 B FI104901 B FI 104901B FI 974001 A FI974001 A FI 974001A FI 974001 A FI974001 A FI 974001A FI 104901 B FI104901 B FI 104901B
Authority
FI
Finland
Prior art keywords
dichloromethylene
ppm
acid
bisphosphonate
salt
Prior art date
Application number
FI974001A
Other languages
English (en)
Finnish (fi)
Other versions
FI974001A (sv
FI974001A0 (fi
Inventor
Heikki Nupponen
Esko Kalervo Pohjala
Leena Lauren
Ritva Hannuniemi
Jouko Juhani Vepsaelaeinen
Jouni Pekka Kaehkoenen
Tomi Lauri Jaervinen
Marko Juhani Ahlmark
Original Assignee
Leiras Oy
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
Application filed by Leiras Oy filed Critical Leiras Oy
Publication of FI974001A0 publication Critical patent/FI974001A0/fi
Priority to FI974001A priority Critical patent/FI104901B/sv
Priority to PCT/FI1998/000814 priority patent/WO1999020634A1/en
Priority to RU2000112534/04A priority patent/RU2205833C2/ru
Priority to JP2000516975A priority patent/JP2001520232A/ja
Priority to TR2000/01055T priority patent/TR200001055T2/xx
Priority to BR9813102-8A priority patent/BR9813102A/pt
Priority to CNB988103710A priority patent/CN1147497C/zh
Priority to EP98949022A priority patent/EP1032578A1/en
Priority to AU95437/98A priority patent/AU740355B2/en
Priority to IL13563998A priority patent/IL135639A0/xx
Priority to HU0004386A priority patent/HUP0004386A3/hu
Priority to EEP200000239A priority patent/EE04061B1/xx
Priority to KR1020007004256A priority patent/KR20010031269A/ko
Priority to PL98340055A priority patent/PL340055A1/xx
Priority to NZ504390A priority patent/NZ504390A/en
Priority to US09/529,826 priority patent/US6326363B1/en
Priority to CA002306080A priority patent/CA2306080A1/en
Publication of FI974001A publication Critical patent/FI974001A/sv
Priority to NO20002006A priority patent/NO20002006L/no
Application granted granted Critical
Publication of FI104901B publication Critical patent/FI104901B/sv
Priority to BG104452A priority patent/BG104452A/xx

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Classifications

    • 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
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/409—Compounds containing the structure P(=X)-X-acyl, P(=X) -X-heteroatom, P(=X)-X-CN (X = O, S, Se)
    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/409—Compounds containing the structure P(=X)-X-acyl, P(=X) -X-heteroatom, P(=X)-X-CN (X = O, S, Se)
    • C07F9/4093—Compounds containing the structure P(=X)-X-C(=X)- (X = O, S, Se)

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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)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Rheumatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (4)

104901
1. Metylenbisfosfonsyraanhydridderivat med den allmänna formeln I 5 O Y1 u Q1^ ^9—-Y2
10 -Y3 o ^ Y' i vilken formel Y1, Y2, Y3 och Y4 betecknar en grupp OR1,
15 NR2R3, OCOR1, OCNR2R3, O(CO)OR1, 0(S02)R3, 0(S02)0Rl eller OP (O) R2 (OR3) , väri R1, R2 och R3 är oberoende av varandra väte, en rak eller förgrenad, eventuellt substituerad, eventuellt omättad Cj-Cjj alkyl, en eventuellt substituerad, eventuellt omättad C3-C10 alicyklyl, heterocyklyl, 20 aryl, heteroaryl, aralkyl eller silyl SiR3, väri R betecknar en Ci-C, alkyl, fenyl, en substituerad fenyl eller kombinationer av Cj-C, alkyler och/eller fenyler, eller grupperna R2 och R3 bildar tillsammans med en intill belä-gen kväveatom en mättad, delvis mättad eller aromatisk 25 ring med 3-10 medlemmar, väri utöver kväveatomen kan fin-nas en eller tvä heteroatomer ur gruppen N, o och S, fö-rutsatt att ätminstone en av grupperna Y1, Y2, Y3 eller Y' i formeln I är nägon annan än en grupp OR1 eller NR2R3; Q1 och Q2 är oberoende av varandra väte, fluor, klor, brom 30 eller jod, inklusive föreningarnas stereoisomerer, säsom geometriska isomerer och optiskt aktiva isomerer, samt farmakologiskt godtagna salter av dessa föreningar.
2. Metylenbisfosfonsyraanhydridderivat enligt patentkrav 1, kännetecknat därav, att det är 104901 p, p'-diacetyl(diklormetylen)bisfosfonat dinatriumsalt eller fri syra, p, p'-dibutyroyl(diklormetylen)bisfosfonat dinatriumsalt eller fri syra,
5 P,P'-bis(pivaloyl)(diklormetylen)bisfosfonsyrans dinat- riumsalt eller fri syra, P,P'-bis(bensoyl)(diklormetylen)bisfosfonsyrans dinat-riumsalt eller fri syra, P,P'-bis(isobutyroyl)(diklormetylen)bisfosfonsyrans di-10 natriumsalt eller fri syra, P,P'-bis(tetradekanoyl)(diklormetylen)bisfosfonsyrans dinatr iumsalt eller fri syra, P,P'-bis(oktadekanoyl)(diklormetylen)bisfosfonsyrans dinatr iumsalt eller fri syra. 15
3. Förfarande för framstalining av metylenbisfosfonsy-raanhydridderivat enligt patentkrav 1, kännetecknat dä-rav, att 20 a) ett utgängsämne med formeIn II, väri ätminstone en av grupperna X^X4 eller alla är oberoende av varandra OH eller OM, väri M kan vara en metall- eller ammoniumgrupp, och Q1 och Q2 är väte eller halogen, selektivt omsättes med ett önskat syraderivat Z-A, vari A betecknar en grupp 25 OCOR1, OCNR2R\ OfCOJOR1, 0(S02)R!, OfSO^OR1 eller OP (o) R2 (OR3) och Z är halogen eller analog; eller O X1 30 n1 p<—-x2 \ / + Z-A ---> I Q2 ^P—-X3 l|X\ 0 ^x' 35 (II) 104901 b) ett utgängsämne med formeIn II, väri ätminstone en av grupperna X^X1 eller alla är oberoende av varandra halogen eller halogenanalog, omsättes med en vald syra eller valda syror A-OH (Z=OH) eller med dess metallsalt A-OM 5 (Z=OM), väri A och M betecknar detsamma som under punkt a), och till slut avlägsnas extra X-grupper och even-tuellt extra Y-grupper tili exempel genom att hydrolysera med vatten; eller 10 c) för framställning av tri-, di- och monopartiellanhyd-ridderivat I, hydrolyseras de ovan under punkterna a) eller b) erh&llna tetraanhydriderna selektivt.
4. Farmaceutiskt preparat, kännetecknat därav, att det 15 som aktiv ingrediens innehäller ett metylenbisfosfonsy-raanhydridderivat enligt patentkrav 1. • «
FI974001A 1997-10-20 1997-10-20 Nya metylenbisfosfonsyraderivat FI104901B (sv)

Priority Applications (19)

Application Number Priority Date Filing Date Title
FI974001A FI104901B (sv) 1997-10-20 1997-10-20 Nya metylenbisfosfonsyraderivat
HU0004386A HUP0004386A3 (en) 1997-10-20 1998-10-20 Methylenebisphosphonic acid derivatives, process for producing them and medicaments containing the same as active agent
KR1020007004256A KR20010031269A (ko) 1997-10-20 1998-10-20 신규한 메틸렌비스포스폰산 유도체
JP2000516975A JP2001520232A (ja) 1997-10-20 1998-10-20 新規なメチレンビスホスホン酸誘導体
TR2000/01055T TR200001055T2 (tr) 1997-10-20 1998-10-20 Yeni metilenbifosfonik asit türevleri
BR9813102-8A BR9813102A (pt) 1997-10-20 1998-10-20 Derivados de ácido metilenobisfosfÈnico novos
CNB988103710A CN1147497C (zh) 1997-10-20 1998-10-20 亚甲基双膦酸类衍生物
EP98949022A EP1032578A1 (en) 1997-10-20 1998-10-20 Novel methylenebisphosphonic acid derivatives
AU95437/98A AU740355B2 (en) 1997-10-20 1998-10-20 Novel Methylenebisphosphonic Acid Derivatives
IL13563998A IL135639A0 (en) 1997-10-20 1998-10-20 Novel methylenebisphosphonic acid derivatives
PCT/FI1998/000814 WO1999020634A1 (en) 1997-10-20 1998-10-20 Novel methylenebisphosphonic acid derivatives
EEP200000239A EE04061B1 (et) 1997-10-20 1998-10-20 Metüleenbisfosfoonhappe derivaadid
RU2000112534/04A RU2205833C2 (ru) 1997-10-20 1998-10-20 Производные ангидрида метиленбисфосфоновой кислоты, способы их получения, фармацевтическая композиция
PL98340055A PL340055A1 (en) 1997-10-20 1998-10-20 Novel derivatives of methylene biphosphonic acid
NZ504390A NZ504390A (en) 1997-10-20 1998-10-20 Methylenebisphosphonic acid anhydride derivatives and pharmaceuticals thereof
US09/529,826 US6326363B1 (en) 1997-10-20 1998-10-20 Methylenebisphosphonic acid derivatives
CA002306080A CA2306080A1 (en) 1997-10-20 1998-10-20 Novel methylenebisphosphonic acid derivatives
NO20002006A NO20002006L (no) 1997-10-20 2000-04-17 Nye metylenbisfosfonsyrederivater
BG104452A BG104452A (en) 1997-10-20 2000-05-17 New derivatives of the methylenebisphosphonic acid

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI974001 1997-10-20
FI974001A FI104901B (sv) 1997-10-20 1997-10-20 Nya metylenbisfosfonsyraderivat

Publications (3)

Publication Number Publication Date
FI974001A0 FI974001A0 (fi) 1997-10-20
FI974001A FI974001A (sv) 1999-04-21
FI104901B true FI104901B (sv) 2000-04-28

Family

ID=8549759

Family Applications (1)

Application Number Title Priority Date Filing Date
FI974001A FI104901B (sv) 1997-10-20 1997-10-20 Nya metylenbisfosfonsyraderivat

Country Status (19)

Country Link
US (1) US6326363B1 (sv)
EP (1) EP1032578A1 (sv)
JP (1) JP2001520232A (sv)
KR (1) KR20010031269A (sv)
CN (1) CN1147497C (sv)
AU (1) AU740355B2 (sv)
BG (1) BG104452A (sv)
BR (1) BR9813102A (sv)
CA (1) CA2306080A1 (sv)
EE (1) EE04061B1 (sv)
FI (1) FI104901B (sv)
HU (1) HUP0004386A3 (sv)
IL (1) IL135639A0 (sv)
NO (1) NO20002006L (sv)
NZ (1) NZ504390A (sv)
PL (1) PL340055A1 (sv)
RU (1) RU2205833C2 (sv)
TR (1) TR200001055T2 (sv)
WO (1) WO1999020634A1 (sv)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO313180B1 (no) * 2000-07-04 2002-08-26 Anticancer Therapeutic Inv Sa Bensökende alfapartikkel emitterende radiofarmasöytika
US7862552B2 (en) 2005-05-09 2011-01-04 Boston Scientific Scimed, Inc. Medical devices for treating urological and uterine conditions
WO2008024169A1 (en) * 2006-07-21 2008-02-28 Glsynthesis, Inc. Reactive pyrophosphoric and bisphosphonic acid derivatives and methods of their use
CA2747188C (en) 2008-11-20 2017-06-13 Glsynthesis Inc. Antithrombotic diadenosine tetraphosphates and related analogs
CN107011380A (zh) * 2016-01-28 2017-08-04 臧伟 一种二膦酸衍生物及含二膦酸衍生物的组合物治疗骨折的应用

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4447256A (en) 1977-07-20 1984-05-08 Nissan Chemical Industries, Ltd. N-(Unsubstituted or substituted pyridyl)aminomethylene-diphosphonic acids, herbicidal compositions containing same, their use for herbicides, and process for preparing same
DE2758580A1 (de) 1977-12-29 1979-07-05 Hoechst Ag Verfahren zur herstellung von phosphin- und phosphonsaeure-anhydriden
HU199151B (en) 1987-03-10 1990-01-29 Yamanouchi Pharma Co Ltd Process for producing bis-phosphonic acid derivatives
US4933472A (en) 1988-04-08 1990-06-12 Yamanouchi Pharmaceutical Co., Ltd. Substituted aminomethylenebis(phosphonic acid) derivatives
EP0356866A3 (en) 1988-08-29 1991-03-27 E.R. SQUIBB &amp; SONS, INC. Phosphorus-containing squalene synthetase inhibitors and method
FI83421C (sv) 1989-06-21 1991-07-10 Huhtamaeki Oy Förfarande för framställning av farmakologiskt användbara metylenbisfo sfonsyraderivat
DE69023844T2 (de) 1989-09-06 1996-06-20 Merck & Co Inc Acyloxymethylester der Bisphonsäuren als Knochenresorptions-Inhibitoren.
FI89366C (sv) * 1990-12-20 1993-09-27 Leiras Oy Förfarande för framställning av nya farmakologiskt användbara metylenb isfosfonsyraderivat
FI89364C (sv) 1990-12-20 1993-09-27 Leiras Oy Förfarande för framställning av nya, farmakologiskt användbara metylen bisfosfonsyraderivat
FI89365C (sv) 1990-12-20 1993-09-27 Leiras Oy Förfarande för framställning av nya farmakologiskt användbara metylenb isfosfonsyraderivat
WO1992017488A1 (en) 1991-04-06 1992-10-15 Fisons Plc Atp analogues
TW237386B (sv) 1992-04-15 1995-01-01 Ciba Geigy
DE69406649T2 (de) * 1993-02-10 1998-03-05 Astra Pharmaceuticals Ltd., Kings Langley, Hertfordshire N-alkyl-2-substituierte atp-analoge
US5462932A (en) 1994-05-17 1995-10-31 Merck & Co., Inc. Oral liquid alendronate formulations

Also Published As

Publication number Publication date
KR20010031269A (ko) 2001-04-16
WO1999020634A1 (en) 1999-04-29
NZ504390A (en) 2001-10-26
CA2306080A1 (en) 1999-04-29
HUP0004386A3 (en) 2002-08-28
IL135639A0 (en) 2001-05-20
BR9813102A (pt) 2000-08-22
FI974001A (sv) 1999-04-21
US6326363B1 (en) 2001-12-04
EE04061B1 (et) 2003-06-16
AU740355B2 (en) 2001-11-01
HUP0004386A2 (hu) 2001-04-28
PL340055A1 (en) 2001-01-15
RU2205833C2 (ru) 2003-06-10
BG104452A (en) 2000-12-29
CN1147497C (zh) 2004-04-28
FI974001A0 (fi) 1997-10-20
EP1032578A1 (en) 2000-09-06
NO20002006L (no) 2000-06-15
AU9543798A (en) 1999-05-10
CN1276793A (zh) 2000-12-13
EE200000239A (et) 2001-08-15
TR200001055T2 (tr) 2000-09-21
NO20002006D0 (no) 2000-04-17
JP2001520232A (ja) 2001-10-30

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