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WO2003016266A1 - β-KETOAMIDE COMPOUNDS AND MEDICINAL USE THEREOF - Google Patents

β-KETOAMIDE COMPOUNDS AND MEDICINAL USE THEREOF 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
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.)
Ceased
Application number
PCT/JP2002/008211
Other languages
French (fr)
Japanese (ja)
Inventor
Susumu Katoh
Susumu Miyazaki
Noriyuki Habuka
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.)
Japan Tobacco Inc
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/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

β-Ketoamide compounds represented by the following general formula [I]: [I] wherein each symbol is as defined in the description; pharmaceutically acceptable salts thereof and anti-HIV agents containing these compounds. Because of having an HIV integrase inhibitory activity, the above compounds are useful as anti-HIV agents to be used in remedies or preventives for AIDS. Further efficacious anti-HIV agents can be obtained by combining the compounds with other anti-HIV agents such as a protease inhibitor or a reverse transcriptase inhibitor. Because of showing a specifically high inhibitory activity on integrase, these compounds are usable as safe drugs with little side effects on the human body.
PCT/JP2002/008211 2001-08-16 2002-08-12 β-KETOAMIDE COMPOUNDS AND MEDICINAL USE THEREOF Ceased WO2003016266A1 (en)

Applications Claiming Priority (6)

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

Publications (1)

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

Family

ID=27347336

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/008211 Ceased WO2003016266A1 (en) 2001-08-16 2002-08-12 β-KETOAMIDE COMPOUNDS AND MEDICINAL USE THEREOF

Country Status (2)

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

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006520759A (en) * 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 Substituted p-diaminobenzene derivatives
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 (en) * 2008-08-29 2018-07-25 Japan Tobacco Inc. Novel potassium channel blocker

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07267903A (en) * 1994-03-31 1995-10-17 Nagase & Co Ltd Fluorine-containing compound having anti-hiv activity
WO1999062520A1 (en) * 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
WO2001096283A2 (en) * 2000-06-16 2001-12-20 Bristol-Myers Squibb Company Hiv integrase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07267903A (en) * 1994-03-31 1995-10-17 Nagase & Co Ltd Fluorine-containing compound having anti-hiv activity
WO1999062520A1 (en) * 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
WO2001096283A2 (en) * 2000-06-16 2001-12-20 Bristol-Myers Squibb Company Hiv integrase inhibitors

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 (en) * 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 Substituted p-diaminobenzene derivatives
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 (en) 2003-08-13 2009-04-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP2344456B1 (en) * 2008-08-29 2018-07-25 Japan Tobacco Inc. Novel potassium channel blocker
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 (en) 2003-07-03

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