WO2003016266A1 - Composes $g(b)-cetoamides et leur utilisation medicinale - Google Patents

Composes $g(b)-cetoamides et leur utilisation medicinale Download PDF

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Publication number
WO2003016266A1
WO2003016266A1 PCT/JP2002/008211 JP0208211W WO03016266A1 WO 2003016266 A1 WO2003016266 A1 WO 2003016266A1 JP 0208211 W JP0208211 W JP 0208211W WO 03016266 A1 WO03016266 A1 WO 03016266A1
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
hiv agents
hiv
inhibitory activity
integrase
Prior art date
Application number
PCT/JP2002/008211
Other languages
English (en)
Japanese (ja)
Inventor
Susumu Katoh
Susumu Miyazaki
Noriyuki Habuka
Original Assignee
Japan Tobacco Inc.
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 Japan Tobacco Inc. filed Critical Japan Tobacco Inc.
Publication of WO2003016266A1 publication Critical patent/WO2003016266A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/80—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms having carbon atoms of carboxamide groups and keto groups bound to the same carbon atom, e.g. acetoacetamides
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/68—One oxygen atom attached in position 4

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

L'invention concerne des composés β-cétoamides représentés par la formule générale (I), dans laquelle chaque symbole est tel que défini dans la description. L'invention porte également sur des agents anti-VIH contenant lesdits composés et sur des sels desdits composés, acceptables au plan pharmaceutique. Compte tenu de leur activité inhibitrice de l'intégrase du VIH, les composés de l'invention sont utiles en tant qu'agents anti-VIH à utiliser dans des produits curatifs ou préventifs pour le SIDA. D'autres agents anti-VIH efficaces peuvent être obtenus par la combinaison desdits composés à d'autres agents anti-VIH, tels que l'inhibiteur de la protéase ou un inhibiteur de la transcriptase inverse. De par leur activité inhibitrice particulièrement élevée sur l'intégrase, lesdits composés peuvent être utilisés en tant que médicaments sûrs avec peu d'effets secondaires sur le corps humain.
PCT/JP2002/008211 2001-08-16 2002-08-12 Composes $g(b)-cetoamides et leur utilisation medicinale WO2003016266A1 (fr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP2001247346 2001-08-16
JP2001-247346 2001-08-16
JP2001372066 2001-12-05
JP2001-372066 2001-12-05
JP2002-151232 2002-05-24
JP2002151232 2002-05-24

Publications (1)

Publication Number Publication Date
WO2003016266A1 true WO2003016266A1 (fr) 2003-02-27

Family

ID=27347336

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/008211 WO2003016266A1 (fr) 2001-08-16 2002-08-12 Composes $g(b)-cetoamides et leur utilisation medicinale

Country Status (2)

Country Link
PE (1) PE20030434A1 (fr)
WO (1) WO2003016266A1 (fr)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006520759A (ja) * 2003-03-21 2006-09-14 ハー・ルンドベック・アクチエゼルスカベット 置換されたｐ−ジアミノベンゼン誘導体
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
US7211572B2 (en) 2003-08-13 2007-05-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
US7820818B2 (en) 2002-08-30 2010-10-26 Novartis Ag Heteroaryl nitrile derivatives
US8609717B2 (en) 2010-08-18 2013-12-17 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as WNT/β-catenin signaling pathway activators
US9533976B2 (en) 2013-02-22 2017-01-03 Samumed, Llc γ-diketones as WNT/β-catenin signaling pathway activators
US9795550B2 (en) 2014-08-20 2017-10-24 Samumed, Llc Gamma-diketones for treatment and prevention of aging skin and wrinkles
EP2344456B1 (fr) * 2008-08-29 2018-07-25 Japan Tobacco Inc. Nouveau bloquant du canal potassique

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07267903A (ja) * 1994-03-31 1995-10-17 Nagase & Co Ltd 抗ｈｉｖ活性を有するフッ素含有化合物
WO1999062520A1 (fr) * 1998-06-03 1999-12-09 Merck & Co., Inc. Inhibiteurs de vih integrase
WO2001096283A2 (fr) * 2000-06-16 2001-12-20 Bristol-Myers Squibb Company Inhibiteurs d'integrase du vih

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07267903A (ja) * 1994-03-31 1995-10-17 Nagase & Co Ltd 抗ｈｉｖ活性を有するフッ素含有化合物
WO1999062520A1 (fr) * 1998-06-03 1999-12-09 Merck & Co., Inc. Inhibiteurs de vih integrase
WO2001096283A2 (fr) * 2000-06-16 2001-12-20 Bristol-Myers Squibb Company Inhibiteurs d'integrase du vih

Cited By (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
US7820818B2 (en) 2002-08-30 2010-10-26 Novartis Ag Heteroaryl nitrile derivatives
JP2006520759A (ja) * 2003-03-21 2006-09-14 ハー・ルンドベック・アクチエゼルスカベット 置換されたｐ−ジアミノベンゼン誘導体
US7906537B2 (en) 2003-03-21 2011-03-15 H. Lundbeck A/S Substituted p-diaminobenzene derivatives
US7211572B2 (en) 2003-08-13 2007-05-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP2042502A1 (fr) 2003-08-13 2009-04-01 Japan Tobacco Inc. Composé cyclique fondu contenant de l'azote et son utilisation en tant qu'inhibiteur de l'intégrase du VIH
EP2344456B1 (fr) * 2008-08-29 2018-07-25 Japan Tobacco Inc. Nouveau bloquant du canal potassique
US8609717B2 (en) 2010-08-18 2013-12-17 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as WNT/β-catenin signaling pathway activators
US8921413B2 (en) 2010-08-18 2014-12-30 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as WNT/ β-catenin signaling pathway activators
US9303010B2 (en) 2010-08-18 2016-04-05 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as Wnt/β-catenin signaling pathway activators
US9493437B2 (en) 2010-08-18 2016-11-15 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as Wnt/ β-catenin signaling pathway activators
US8629176B1 (en) 2010-08-18 2014-01-14 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as WNT/ β-catenin signaling pathway activators
US10314832B2 (en) 2010-08-18 2019-06-11 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as Wnt/β-catenin signaling pathway activators
US9884053B2 (en) 2010-08-18 2018-02-06 Samumed, Llc β- and γ-diketones and γ-hydroxyketones as WNT/β-catenin signaling pathway activators
US9533976B2 (en) 2013-02-22 2017-01-03 Samumed, Llc γ-diketones as WNT/β-catenin signaling pathway activators
US9951053B2 (en) 2013-02-22 2018-04-24 Samumed, Llc γ-diketones as Wnt/β-catenin signaling pathway activators
US10457672B2 (en) 2013-02-22 2019-10-29 Samumed, Llc γ-diketones as Wnt/β-catenin signaling pathway activators
US11034682B2 (en) 2013-02-22 2021-06-15 Samumed, Llc Gamma-diketones as wnt/β-catenin signaling pathway activators
US11673885B2 (en) 2013-02-22 2023-06-13 Biosplice Therapeutics, Inc. γ-diketones as Wnt/β-catenin signaling pathway activators
US9795550B2 (en) 2014-08-20 2017-10-24 Samumed, Llc Gamma-diketones for treatment and prevention of aging skin and wrinkles
US10434052B2 (en) 2014-08-20 2019-10-08 Samumed, Llc Gamma-diketones for treatment and prevention of aging skin and wrinkles
US11077046B2 (en) 2014-08-20 2021-08-03 Biosplice Therapeutics, Inc. Gamma-diketones for treatment and prevention of aging skin and wrinkles
US11839679B2 (en) 2014-08-20 2023-12-12 Biosplice Therapeutics, Inc. Gamma-diketones for treatment and prevention of aging skin and wrinkles

Also Published As

Publication number Publication date
PE20030434A1 (es) 2003-07-03

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