CO4900065A1 - NON-ULCEROGENIC ANALGESIC / ANTI-INFLAMMATORY DERIVATIVE OF CLONIXINE - Google Patents

NON-ULCEROGENIC ANALGESIC / ANTI-INFLAMMATORY DERIVATIVE OF CLONIXINE

Info

Publication number
CO4900065A1
CO4900065A1 CO97046964A CO97046964A CO4900065A1 CO 4900065 A1 CO4900065 A1 CO 4900065A1 CO 97046964 A CO97046964 A CO 97046964A CO 97046964 A CO97046964 A CO 97046964A CO 4900065 A1 CO4900065 A1 CO 4900065A1
Authority
CO
Colombia
Prior art keywords
clonixate
analgesic
clonixine
ulcerogenic
inflammatory
Prior art date
Application number
CO97046964A
Other languages
Spanish (es)
Inventor
Gustavo Enrique Aldoma
Susana Elida Piatti
Original Assignee
Handforth Invest Ltd
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 Handforth Invest Ltd filed Critical Handforth Invest Ltd
Publication of CO4900065A1 publication Critical patent/CO4900065A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • 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]

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

El derivado de clonixina de fórmula (I), o clonixato de4-Nitroxibutilo, es un nuevo producto analgésico-antiinflamatorio no esteroideo, que tiene un equilibrio extraordinariamente bueno entre una alta actividad analgésica/antiinflamatoria y bajos efectos adversos ulcerogenicos, principalmente como una consecuencia de una sorprendentemente alta actividad inflamatoria (dos veces la del ácido clonixico).El compuesto (I) se prepara haciendo reaccionar el clonixato de 4-clorobutilo con nitrato de plata en acetonitrilo. El clonixato de 4-clorobutilo se prepara por reacción de un clonixato alcalino con 1-bromo-4-clorubutano en acetonitrilo. El clonixato de 4-nitroxibutilo (I) es especialmente útil como principio activo para el tratamiento del dolor y/o inflamación en mamíferos.The clonixine derivative of formula (I), or 4-Nitroxybutyl clonixate, is a new non-steroidal analgesic-anti-inflammatory product, which has an extraordinarily good balance between high analgesic / anti-inflammatory activity and low ulcerogenic adverse effects, mainly as a consequence of surprisingly high inflammatory activity (twice that of clonic acid). Compound (I) is prepared by reacting 4-chlorobutyl clonixate with silver nitrate in acetonitrile. The 4-chlorobutyl clonixate is prepared by reacting an alkaline clonixate with 1-bromo-4-chlorubutane in acetonitrile. 4-Nitroxybutyl (I) clonixate is especially useful as an active ingredient for the treatment of pain and / or inflammation in mammals.

CO97046964A 1996-08-16 1997-08-15 NON-ULCEROGENIC ANALGESIC / ANTI-INFLAMMATORY DERIVATIVE OF CLONIXINE CO4900065A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP1996/003610 WO1998007701A1 (en) 1996-08-16 1996-08-16 Non-ulcerogenic analgesic/anti-inflammatory clonixin derivative

Publications (1)

Publication Number Publication Date
CO4900065A1 true CO4900065A1 (en) 2000-03-27

Family

ID=8166287

Family Applications (1)

Application Number Title Priority Date Filing Date
CO97046964A CO4900065A1 (en) 1996-08-16 1997-08-15 NON-ULCEROGENIC ANALGESIC / ANTI-INFLAMMATORY DERIVATIVE OF CLONIXINE

Country Status (9)

Country Link
JP (1) JP2000516235A (en)
AU (1) AU714258B2 (en)
BR (1) BR9612730A (en)
CA (1) CA2262788A1 (en)
CO (1) CO4900065A1 (en)
PE (1) PE99398A1 (en)
TW (1) TW337521B (en)
UY (1) UY24666A1 (en)
WO (1) WO1998007701A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20030042935A (en) * 2001-11-26 2003-06-02 알앤피코리아 주식회사 Clonixin lysinate formulation
ITMI20021861A1 (en) * 2002-08-29 2004-02-29 Nicox Sa NITROXIALKYL ESTER SYNTHESIS PROCESS OF CARBOXYLIC ACIDS, INTERMEDIATES THAT CAN BE USED IN THAT PROCEDURE AND THEIR PREPARATION.

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4273777A (en) * 1979-06-04 1981-06-16 Laboratorios Bago S.A. Methods of treating mammals suffering from inflammation and pain
IT1256345B (en) * 1992-08-20 1995-12-01 NITRIC ESTERS OF PHENYLACETIC 2- (2,6-DI-HALO-PHENYLAMIN) DERIVATIVES AND PROCEDURE FOR THEIR PREPARATION

Also Published As

Publication number Publication date
JP2000516235A (en) 2000-12-05
PE99398A1 (en) 1999-01-25
TW337521B (en) 1998-08-01
BR9612730A (en) 1999-08-24
WO1998007701A1 (en) 1998-02-26
UY24666A1 (en) 1998-02-03
AU714258B2 (en) 1999-12-23
AU6924996A (en) 1998-03-06
CA2262788A1 (en) 1998-02-26

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