WO1992010504A3 - Acides phosphoniques derives utiles comme agents antiinflammatoires - Google Patents

Acides phosphoniques derives utiles comme agents antiinflammatoires Download PDF

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Publication number
WO1992010504A3
WO1992010504A3 PCT/US1991/008817 US9108817W WO9210504A3 WO 1992010504 A3 WO1992010504 A3 WO 1992010504A3 US 9108817 W US9108817 W US 9108817W WO 9210504 A3 WO9210504 A3 WO 9210504A3
Authority
WO
WIPO (PCT)
Prior art keywords
bisphosphonic acid
methylene
bis
tetramethyl ester
acid tetramethyl
Prior art date
Application number
PCT/US1991/008817
Other languages
English (en)
Other versions
WO1992010504A2 (fr
Inventor
Roy Allen Johnson
Herman Walden Smith
Original Assignee
Upjohn Co
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 Upjohn Co filed Critical Upjohn Co
Priority to DE69108739T priority Critical patent/DE69108739T2/de
Priority to JP4501562A priority patent/JPH06503329A/ja
Priority to EP92901352A priority patent/EP0561948B1/fr
Publication of WO1992010504A2 publication Critical patent/WO1992010504A2/fr
Publication of WO1992010504A3 publication Critical patent/WO1992010504A3/fr

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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
    • C07F9/547—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
    • C07F9/650994—Six-membered rings having the nitrogen atoms in the positions 1 and 4 condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • C07F9/6564—Heterocyclic 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
    • C07F9/6571—Heterocyclic 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
    • C07F9/657163—Heterocyclic 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
    • C07F9/657181—Heterocyclic 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

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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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

De nouveaux acides, esters, et sels d'acides biphosphoniques de phényle, naphthyle, quinoxalinyle, de biphényle, et des nouvelles 1,2-oxaphosphépines sont décrits. Ces composés sont utiles comme agents anti-inflammatoires et anti-arthritiques. L'invention concerne également des composés connus des classes de bisphosphonates de phényle, naphthyle, quinoxalinyle, et biphényle, qui sont également utiles comme agents anti-inflammatoires et anti-arthritiques. Dans les composés représentatifs de cette invention sont compris l'ester de tétraméthyle d'acide [1,2-phénylediyl]-bis(méthylène)bisphosphonique, l'ester de tétraméthyle d'acide [2,3-quinoxalinediyl]bis(méthylène)bisphosphonique, l'ester de tétraméthyle d'acide [[3-(propyl)-4-(méthoxy)-1,8-naphthalènediyl]bis(méthylène)]bisphosphonique, l'ester de tétraéthyle d'acide [2,6-naphthalènediylbis(méthylène)bisphosphonique, et l'ester de tétraméthyle d'acide [2,2'-biphénylènebis(méthyl)]bisphosphonique. Des oxaphosphépines représentatives de l'invention comprennent le 3,4-dihydro-3-méthoxy-7-(phénylméthoxy)-1H-naphth[1,8de][1,2]oxaphosphépine-3-oxyde préféré.
PCT/US1991/008817 1990-12-07 1991-12-03 Acides phosphoniques derives utiles comme agents antiinflammatoires WO1992010504A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
DE69108739T DE69108739T2 (de) 1990-12-07 1991-12-03 Phosphonsäurederivate als entzündungshemmende mittel.
JP4501562A JPH06503329A (ja) 1990-12-07 1991-12-03 抗炎症剤として有用なホスホン酸誘導体
EP92901352A EP0561948B1 (fr) 1990-12-07 1991-12-03 Acides phosphoniques derives utiles comme agents antiinflammatoires

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US924,119 1978-07-13
US62411990A 1990-12-07 1990-12-07

Publications (2)

Publication Number Publication Date
WO1992010504A2 WO1992010504A2 (fr) 1992-06-25
WO1992010504A3 true WO1992010504A3 (fr) 1992-09-17

Family

ID=24500731

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1991/008817 WO1992010504A2 (fr) 1990-12-07 1991-12-03 Acides phosphoniques derives utiles comme agents antiinflammatoires

Country Status (8)

Country Link
US (2) US5298498A (fr)
EP (2) EP0561948B1 (fr)
JP (1) JPH06503329A (fr)
AU (1) AU9097791A (fr)
CA (1) CA2094123A1 (fr)
DE (1) DE69108739T2 (fr)
DK (1) DK0561948T3 (fr)
WO (1) WO1992010504A2 (fr)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2094123A1 (fr) * 1990-12-07 1992-06-08 Pharmacia & Upjohn Company Llc Derives de l'acide phosphonique servant d'agents antiinflammatoires
EP0661978A1 (fr) * 1992-09-23 1995-07-12 PHARMACIA & UPJOHN COMPANY Arylmethylphosphonates et acides phosphoniques utiles en tant qu'agents anti-inflammatoires
JP3951367B2 (ja) * 1996-11-28 2007-08-01 住友化学株式会社 ５価のリン系化合物を有効成分とする熱可塑性樹脂用安定剤、その製造方法およびその用途
GB2326369B (en) * 1997-06-20 2001-06-27 Aea Technology Plc Double lid system
US6096730A (en) * 1997-07-24 2000-08-01 University Of Kentucky Research Foundation Phosphonated agents and their antiangiogenic and antitumorigenic use
US5932563A (en) * 1998-10-23 1999-08-03 Ohio State Research Foundation Methods for treating spinal cord injury
US6627215B1 (en) * 1998-12-30 2003-09-30 Oligos Etc. Inc. Devices for improved wound management
US20020032164A1 (en) * 1998-12-30 2002-03-14 Dale Roderic M. K. Antimicrobial compounds and methods for their use
US7868162B2 (en) * 1998-12-30 2011-01-11 Lakewood-Amedex, Inc. Antimicrobial and antiviral compounds and methods for their use
JP5005127B2 (ja) 1999-05-04 2012-08-22 ストラカン・インターナショナル・リミテッド アンドロゲングリコシド及びそのアンドロゲン作用活性
JP4164718B2 (ja) * 1999-10-06 2008-10-15 ソニー株式会社 ビス（アミノスチリル）ナフタレン化合物及びその合成中間体、これらの製造方法、並びに有機電界発光素子
WO2003009815A2 (fr) 2001-07-25 2003-02-06 Biomarin Pharmaceutical Inc. Compositions et procedes de modulation du transport a travers la barriere hematho-encephalique
EP2671508B1 (fr) 2005-04-28 2020-09-16 Proteus Digital Health, Inc. Système pharma-informatique
BRPI0620268B8 (pt) * 2005-12-22 2021-05-25 Oakwood Laboratories LLC composição eficaz como sistema de fornecimento para liberação controlada, seu uso, seu método de fabricação, e método para proteger um agente biologicamente ativo
CA2663377A1 (fr) 2006-09-18 2008-03-27 Raptor Pharmaceutical Inc. Traitement des troubles hepatiques par l'administration de conjugues de proteine associee au recepteur (rap)
ES2720080T3 (es) 2007-11-14 2019-07-17 Fresenius Kabi Austria Gmbh Procedimiento continúo para la preparación de lactulosa cristalina
AU2010216512B2 (en) 2009-02-20 2016-06-30 2-Bbb Medicines B.V. Glutathione-based drug delivery system
EP2427178B1 (fr) 2009-05-06 2023-01-04 Laboratory Skin Care, Inc. Compositions pour libération dermique comprenant des complexes principe actif-particule de phosphate de calcium et procédés d'utilisation associés
US20120077778A1 (en) 2010-09-29 2012-03-29 Andrea Bourdelais Ladder-Frame Polyether Conjugates

Citations (3)

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Publication number Priority date Publication date Assignee Title
DE1124949B (de) * 1960-03-04 1962-03-08 Basf Ag Verfahren zur Herstellung von Verbindungen der 1,2-Bis-(vinyl)-benzolreihe
EP0085321A2 (fr) * 1982-01-27 1983-08-10 Schering Aktiengesellschaft Dérivés d'acides diphosphoniques et préparations pharmaceutiques les contenant
EP0149802A2 (fr) * 1983-12-21 1985-07-31 Hoechst Aktiengesellschaft 2,3-Bis(arylethényl)-quinoxalines, procédé pour leur préparation et leur usage comme composés photoconducteurs

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JPS5038861A (fr) * 1973-08-11 1975-04-10
JPS53105716A (en) * 1977-02-25 1978-09-14 Daicel Chem Ind Ltd Hose or tube for solvent
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Publication number Priority date Publication date Assignee Title
DE1124949B (de) * 1960-03-04 1962-03-08 Basf Ag Verfahren zur Herstellung von Verbindungen der 1,2-Bis-(vinyl)-benzolreihe
EP0085321A2 (fr) * 1982-01-27 1983-08-10 Schering Aktiengesellschaft Dérivés d'acides diphosphoniques et préparations pharmaceutiques les contenant
EP0149802A2 (fr) * 1983-12-21 1985-07-31 Hoechst Aktiengesellschaft 2,3-Bis(arylethényl)-quinoxalines, procédé pour leur préparation et leur usage comme composés photoconducteurs

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Title
Chemical Abstracts, vol. 68, no. 19, 6 May 1968, (Columbus, Ohio, US), V.S. ABRAMOV et al.: "Effect of some dihalo derivatives on sodium salts of dialkylphosphonic acids and phosphites", see page 8428, abstract no. 87351r, & ZH. OBSHCH. KHIM. 37(10), 2243-7(1967), see the abstract *
Chemical Abstracts, vol. 90, no. 13, 26 March 1979, (Columbus, Ohio, US), L. MAIER et al.: "Organic phosphorus compounds. 70. Preparation and properties of new phosphorus containing chelating agents for calcium and magnesium ions", see page 605, abstract no. 104063x, & PHOSPHORUS SULFUR 1978, 5(1), 45-51, see the abstract *
Journal of the American Chemical Society, vol. 93, no. 3, 10 February 1971, J. MEINWALD et al.: "Photochemical reactions of 1,8-divinylnaphthalene and 1,8-distyrylnaphthalene", pages 725-731, see page 726, compound 13; page 729, column 2, middle *

Also Published As

Publication number Publication date
DE69108739D1 (de) 1995-05-11
DE69108739T2 (de) 1995-09-14
JPH06503329A (ja) 1994-04-14
EP0622373A1 (fr) 1994-11-02
EP0561948A1 (fr) 1993-09-29
AU9097791A (en) 1992-07-08
WO1992010504A2 (fr) 1992-06-25
DK0561948T3 (da) 1995-08-21
CA2094123A1 (fr) 1992-06-08
US5360797A (en) 1994-11-01
EP0561948B1 (fr) 1995-04-05
US5298498A (en) 1994-03-29

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