ES2039259T3 - Procedimiento para la obtencion de acidos azacicloalquil alcandifosfonicos aromaticamente substituidos. - Google Patents

Procedimiento para la obtencion de acidos azacicloalquil alcandifosfonicos aromaticamente substituidos.

Info

Publication number
ES2039259T3
ES2039259T3 ES198787810666T ES87810666T ES2039259T3 ES 2039259 T3 ES2039259 T3 ES 2039259T3 ES 198787810666 T ES198787810666 T ES 198787810666T ES 87810666 T ES87810666 T ES 87810666T ES 2039259 T3 ES2039259 T3 ES 2039259T3
Authority
ES
Spain
Prior art keywords
formula
acids
azacicloalkyl
alcandiphosphonic
procedure
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
ES198787810666T
Other languages
English (en)
Inventor
Knut A. Dr. Jaeggi
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.)
Novartis AG
Original Assignee
Ciba Geigy AG
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 Ciba Geigy AG filed Critical Ciba Geigy AG
Application granted granted Critical
Publication of ES2039259T3 publication Critical patent/ES2039259T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • 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)]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/5532—Seven-(or more) membered rings
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/650952—Six-membered rings having the nitrogen atoms in the positions 1 and 4
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Anti-Oxidant Or Stabilizer Compositions (AREA)
  • Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
  • Polymerization Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

LOS ACIDOS AZACICLO-ALQUILALCANODIFOSFORICOS DE FORMULA (I), EN LA QUE R REPRESENTA UN RESTO AZACICLOALIFATICO UNIDO AL GRUPO ALK A TRAVES DE UN ATOMO DE NITROGENO, Y PRESENTANDO OPCINALMENTE UN ATOMO DE NITROGENO ADICIONAL, Y ALK REPRESENTA UN RESTO ALIFATICO DIVALENTE, Y LAS SALES DE ESTOS, PUEDEN EMPLEARSE PARA EL TRATAMIENTO DE LAS ENFERMEDADES PROVOCADAS POR ALTERACIONES DEL METABOLISMO DEL CALCIO. SE OBTIENEN, POR EJEMPLO, HACIENDO REACCIONAR UN COMPUESTO DE FORMULA (IV), EN EL QUE X3 ES CARBOXI, CARBAMILO O CIANO, CON ACIDO FOSFOROSO Y TRICLORURO DE FOSFORO, Y, EN UN PRODUCTO INTERMEDIO DE FORMULA (V) O UNA SAL DEL MISMO, OBTENIDO POR TRATAMIENTO HIDROLITICO A PARTIR DE COMPUESTOS DE FORMULA (IV), DONDE X3 ES CIANO O CARBAMILO, SE SUSTITUYE EL GRUPO AMINO POR UN GRUPO HIDROXILO MEDIANTE TRATAMIENTO CON ACIDO NITROSO.
ES198787810666T 1986-11-21 1987-11-16 Procedimiento para la obtencion de acidos azacicloalquil alcandifosfonicos aromaticamente substituidos. Expired - Lifetime ES2039259T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH466486 1986-11-21

Publications (1)

Publication Number Publication Date
ES2039259T3 true ES2039259T3 (es) 1993-09-16

Family

ID=4280315

Family Applications (1)

Application Number Title Priority Date Filing Date
ES198787810666T Expired - Lifetime ES2039259T3 (es) 1986-11-21 1987-11-16 Procedimiento para la obtencion de acidos azacicloalquil alcandifosfonicos aromaticamente substituidos.

Country Status (20)

Country Link
US (1) US4871720A (es)
EP (1) EP0272208B1 (es)
JP (1) JPS63150292A (es)
KR (1) KR880006254A (es)
AT (1) ATE64397T1 (es)
AU (1) AU605202B2 (es)
DD (1) DD265901A5 (es)
DE (1) DE3770787D1 (es)
DK (1) DK168630B1 (es)
ES (1) ES2039259T3 (es)
FI (1) FI86186C (es)
GR (1) GR3002561T3 (es)
HU (1) HU198730B (es)
IE (1) IE60147B1 (es)
IL (1) IL84493A (es)
NO (1) NO170939C (es)
NZ (1) NZ222609A (es)
PH (1) PH25049A (es)
PT (1) PT86165B (es)
ZA (1) ZA878628B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3640938A1 (de) * 1986-11-29 1988-06-01 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindung enthaltende arzneimittel
EP0317505A1 (de) * 1987-11-13 1989-05-24 Ciba-Geigy Ag Neue Azacycloalkylalkandiphosphonsäuren
US4883877A (en) * 1987-11-13 1989-11-28 Ciba-Geigy Corporation Azabicycloheptanes and process for their preparation
US5110807A (en) * 1988-12-01 1992-05-05 Ciba-Geigy Corporation Araliphatylaminoalkanediphosphonic acids
US5190930A (en) * 1987-12-11 1993-03-02 Ciba-Geigy Corporation Araliphatylaminoalkanediphosphonic acids
GB8808138D0 (en) * 1988-04-07 1988-05-11 Leo Pharm Prod Ltd Chemical compounds
US4990503A (en) * 1988-08-12 1991-02-05 Yamanouchi Pharmaceutical Co., Ltd. Heterocyclic bisphosphonic acid derivatives
JPH0699457B2 (ja) * 1988-08-12 1994-12-07 山之内製薬株式会社 ヘテロ環ビスフォスフォン酸誘導体およびその医薬
DE3843481A1 (de) * 1988-12-23 1990-06-28 Boehringer Ingelheim Kg Substituierte 3-azabicyclo/3.1.1/heptane, ihre herstellung und ihre verwendung
PH26923A (en) * 1989-03-08 1992-12-03 Ciba Geigy N-substituted amino alkanediphosphonic acids
MX21452A (es) * 1989-07-07 1994-01-31 Ciba Geigy Ag Preparaciones farmaceuticas que se administran en forma topica.
US5139786A (en) * 1989-07-07 1992-08-18 Ciba-Geigy Corporation Topical formulations
WO1991010646A1 (en) * 1990-01-12 1991-07-25 Rhone-Poulenc Rorer International (Holdings) Inc. 1-azetidyl and 1-hexamethylenimine alkyl or aryl bisphosphonic acids and their use as pharmacological agents
US5204334A (en) * 1990-10-18 1993-04-20 Ciba-Geigy Corporation Benzoheterocyclylalkylaminoalkanediphosphonic acids, compositions thereof, and use thereof in the treatment of calcium metabolism disorders
EP0521622B1 (en) * 1991-07-03 1997-08-13 PHARMACIA & UPJOHN COMPANY Pyrazolopyrimidine and pyrimidinyl bisphosphonic esters as anti-inflammatories
US5270365A (en) * 1991-12-17 1993-12-14 Merck & Co., Inc. Prevention and treatment of periodontal disease with alendronate
JPH05345791A (ja) * 1992-03-18 1993-12-27 Hoechst Japan Ltd 環状アミノメチレンビスホスホン酸誘導体
US5283057A (en) * 1992-04-24 1994-02-01 The Procter & Gamble Company Risedronate in oral compositions
US5475029A (en) * 1993-07-08 1995-12-12 The Board Of Trustees Of The Leland Stanford Junior University Farnesyl compounds as cholesterol lowering agents
US5880111A (en) * 1995-06-07 1999-03-09 Farcasiu; Dan Therapeutic derivations of diphosphonates
US7700626B2 (en) * 2004-06-04 2010-04-20 Adolor Corporation Compositions containing opioid antagonists
US8012949B2 (en) * 2004-10-08 2011-09-06 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods with enhanced potency for multiple targets including FPPS, GGPPS, and DPPS
US7687482B2 (en) * 2006-03-17 2010-03-30 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods
EP1802641B8 (en) * 2004-10-08 2012-03-07 The Board Of Trustees Of The University Of Illinois Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5598194A (en) * 1979-01-22 1980-07-25 Nissan Chem Ind Ltd Pyrrolidinomethylene-diphosphonic acid derivative and herbicide comprising it as active constituent
SU1002300A1 (ru) * 1981-10-29 1983-03-07 Ордена Ленина институт элементоорганических соединений им.А.Н.Несмеянова Способ получени @ -аминозамещенных- @ -оксипропилидендифосфоновых кислот
DE3232997A1 (de) * 1982-09-04 1984-03-08 Henkel KGaA, 4000 Düsseldorf Diphosphonsaeuren
DE3428524A1 (de) * 1984-08-02 1986-02-13 Boehringer Mannheim Gmbh, 6800 Mannheim Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
IL77243A (en) * 1984-12-21 1996-11-14 Procter & Gamble Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds
DE3512536A1 (de) * 1985-04-06 1986-10-16 Boehringer Mannheim Gmbh, 6800 Mannheim Neue diphosphonsaeure-derivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
US4761406A (en) * 1985-06-06 1988-08-02 The Procter & Gamble Company Regimen for treating osteoporosis
DE3540150A1 (de) * 1985-11-13 1987-05-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel

Also Published As

Publication number Publication date
DD265901A5 (de) 1989-03-15
HUT46332A (en) 1988-10-28
IL84493A0 (en) 1988-04-29
AU8145187A (en) 1988-05-26
FI875094A7 (fi) 1988-05-22
EP0272208A1 (de) 1988-06-22
NO170939C (no) 1992-12-30
NO170939B (no) 1992-09-21
FI86186B (fi) 1992-04-15
PT86165A (en) 1987-12-01
NO874860L (no) 1988-05-24
AU605202B2 (en) 1991-01-10
NO874860D0 (no) 1987-11-20
DK609687A (da) 1988-05-22
ATE64397T1 (de) 1991-06-15
FI875094A0 (fi) 1987-11-18
DE3770787D1 (en) 1991-07-18
IL84493A (en) 1993-01-14
US4871720A (en) 1989-10-03
IE60147B1 (en) 1994-06-01
NZ222609A (en) 1990-09-26
JPS63150292A (ja) 1988-06-22
PH25049A (en) 1991-01-28
DK609687D0 (da) 1987-11-20
HU198730B (en) 1989-11-28
GR3002561T3 (en) 1993-01-25
DK168630B1 (da) 1994-05-09
ZA878628B (en) 1988-05-23
EP0272208B1 (de) 1991-06-12
KR880006254A (ko) 1988-07-22
IE873146L (en) 1988-05-21
FI86186C (fi) 1992-07-27
PT86165B (pt) 1990-11-20

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