WO1998045276A3 - 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors - Google Patents

4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors Download PDF

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Publication number
WO1998045276A3
WO1998045276A3 PCT/US1998/006733 US9806733W WO9845276A3 WO 1998045276 A3 WO1998045276 A3 WO 1998045276A3 US 9806733 W US9806733 W US 9806733W WO 9845276 A3 WO9845276 A3 WO 9845276A3
Authority
WO
WIPO (PCT)
Prior art keywords
disubstituted
dihydro
reverse transcriptase
hiv reverse
transcriptase inhibitors
Prior art date
Application number
PCT/US1998/006733
Other languages
French (fr)
Other versions
WO1998045276A2 (en
Inventor
Jeffrey W Corbett
Soo Sung Ko
Original Assignee
Du Pont Pharm 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
Priority to EEP199900452A priority Critical patent/EE9900452A/en
Priority to AU67960/98A priority patent/AU734928B2/en
Priority to JP54297198A priority patent/JP2002504095A/en
Priority to BR9808513-1A priority patent/BR9808513A/en
Priority to EP98913401A priority patent/EP0973753A2/en
Priority to EA199900907A priority patent/EA001991B1/en
Priority to IL13218898A priority patent/IL132188A0/en
Priority to HU0001446A priority patent/HUP0001446A3/en
Application filed by Du Pont Pharm Co filed Critical Du Pont Pharm Co
Priority to NZ500592A priority patent/NZ500592A/en
Priority to CA002284996A priority patent/CA2284996A1/en
Priority to SK1378-99A priority patent/SK137899A3/en
Publication of WO1998045276A2 publication Critical patent/WO1998045276A2/en
Publication of WO1998045276A3 publication Critical patent/WO1998045276A3/en
Priority to NO19994904A priority patent/NO314936B1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms

Abstract

The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolines of formula (I), or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
PCT/US1998/006733 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors WO1998045276A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
IL13218898A IL132188A0 (en) 1997-04-09 1998-04-07 4,4- Disubstituted-3,4-dihydro-2 (H)-quinazolineones useful as hiv reverse transcriptase inhibitors
JP54297198A JP2002504095A (en) 1997-04-09 1998-04-07 4,4-Disubstituted-3,4-dihydro-2 (1H) -quinazolinones useful as HIV reverse transcriptase inhibitors
BR9808513-1A BR9808513A (en) 1997-04-09 1998-04-07 Compound, pharmaceutical composition, method for treating HIV infections and pharmaceutical kit.
EP98913401A EP0973753A2 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors
EA199900907A EA001991B1 (en) 1997-04-09 1998-04-07 4,4-disubstituted -3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitots
EEP199900452A EE9900452A (en) 1997-04-09 1998-04-07 4,4-Disubstituted-3,4-Dihydro-2 (1H) -quinazolinones useful as HIV reverse transcriptase inhibitors
HU0001446A HUP0001446A3 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinone derivatives as hiv reverse transcriptase inhibitors, their use and pharmaceutical compositions containing them
AU67960/98A AU734928B2 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
NZ500592A NZ500592A (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
CA002284996A CA2284996A1 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors
SK1378-99A SK137899A3 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors
NO19994904A NO314936B1 (en) 1997-04-09 1999-10-08 4,4-Disubstituted-3,4-dihydro-2 (1H) -quinazolinones, pharmaceutical compositions, preparations and pharmaceutical kits for the treatment of HIV infection, as well as the use of certain quinazolinones for the preparation of a pharmaceutical preparation

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US83854097A 1997-04-09 1997-04-09
US7132298P 1998-01-14 1998-01-14
US08/838,540 1998-01-14
US60/071,322 1998-01-14

Publications (2)

Publication Number Publication Date
WO1998045276A2 WO1998045276A2 (en) 1998-10-15
WO1998045276A3 true WO1998045276A3 (en) 1999-01-14

Family

ID=26752095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/006733 WO1998045276A2 (en) 1997-04-09 1998-04-07 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinones useful as hiv reverse transcriptase inhibitors

Country Status (19)

Country Link
EP (1) EP0973753A2 (en)
JP (1) JP2002504095A (en)
KR (1) KR20010006146A (en)
CN (1) CN1252063A (en)
AR (1) AR012340A1 (en)
AU (1) AU734928B2 (en)
BR (1) BR9808513A (en)
CA (1) CA2284996A1 (en)
EA (1) EA001991B1 (en)
EE (1) EE9900452A (en)
HR (1) HRP980143A2 (en)
HU (1) HUP0001446A3 (en)
IL (1) IL132188A0 (en)
NO (1) NO314936B1 (en)
NZ (1) NZ500592A (en)
PL (1) PL336305A1 (en)
SK (1) SK137899A3 (en)
TW (1) TW587078B (en)
WO (1) WO1998045276A2 (en)

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8690796B2 (en) 2002-04-19 2014-04-08 Sanofi-Aventis Deutschland Gmbh Method and apparatus for penetrating tissue
US8845549B2 (en) 2002-04-19 2014-09-30 Sanofi-Aventis Deutschland Gmbh Method for penetrating tissue
US8845550B2 (en) 2001-06-12 2014-09-30 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US8905945B2 (en) 2002-04-19 2014-12-09 Dominique M. Freeman Method and apparatus for penetrating tissue
US8945910B2 (en) 2003-09-29 2015-02-03 Sanofi-Aventis Deutschland Gmbh Method and apparatus for an improved sample capture device
US8965476B2 (en) 2010-04-16 2015-02-24 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US9144401B2 (en) 2003-06-11 2015-09-29 Sanofi-Aventis Deutschland Gmbh Low pain penetrating member
US9226699B2 (en) 2002-04-19 2016-01-05 Sanofi-Aventis Deutschland Gmbh Body fluid sampling module with a continuous compression tissue interface surface
US9314194B2 (en) 2002-04-19 2016-04-19 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US9351680B2 (en) 2003-10-14 2016-05-31 Sanofi-Aventis Deutschland Gmbh Method and apparatus for a variable user interface
US9375169B2 (en) 2009-01-30 2016-06-28 Sanofi-Aventis Deutschland Gmbh Cam drive for managing disposable penetrating member actions with a single motor and motor and control system
US9386944B2 (en) 2008-04-11 2016-07-12 Sanofi-Aventis Deutschland Gmbh Method and apparatus for analyte detecting device
US9775553B2 (en) 2004-06-03 2017-10-03 Sanofi-Aventis Deutschland Gmbh Method and apparatus for a fluid sampling device

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002509922A (en) * 1998-03-27 2002-04-02 デュポン ファーマシューティカルズ カンパニー 4,4-Disubstituted-3,4-dihydro-2 (1H) -quinazolinethione derivatives, their preparation, and their use as HIV reverse transcriptase inhibitors
AU6508899A (en) 1998-10-13 2000-05-01 Du Pont Pharmaceuticals Company Selective eradication of virally-infected cells by combined use of a cytotoxic agent and an antiviral agent
HRP990359A2 (en) * 1998-11-19 2000-08-31 Du Pont Pharm Co A process for the preparation of quinazolinones
BR9916750A (en) * 1998-11-19 2001-11-06 Du Pont Pharm Co Reverse transcriptase inhibiting compounds, pharmaceutical compositions, methods of treating infections by human immunodeficiency virus, processes for preparing the compound and its crystalline form
US6175009B1 (en) 1999-11-18 2001-01-16 Dupont Pharmaceuticals Company Process for the preparation of quinazolinones
US6982270B1 (en) 1999-11-23 2006-01-03 Smithkline Beecham Corporation 3,4-dihydro-(1H)quinazolin-2-one compounds as CSBP/p38 kinase inhibitors
US6759410B1 (en) 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
CA2403230A1 (en) * 2000-03-23 2001-09-27 Lilian A. Radesca Asymmetric synthesis of quinazolin-2-ones useful as hiv reverse transcriptase inhibitors
US6555686B2 (en) 2000-03-23 2003-04-29 Bristol-Myers Squibb Pharma Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors
ZA200300255B (en) 2000-07-20 2004-09-28 Bristol Myers Squibb Pharma Co Tricyclic 2-pyridone compounds useful as HIV reverse transcriptase inhibitors.
US6596729B2 (en) 2000-07-20 2003-07-22 Bristol-Myers Squibb Company Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
US8641644B2 (en) 2000-11-21 2014-02-04 Sanofi-Aventis Deutschland Gmbh Blood testing apparatus having a rotatable cartridge with multiple lancing elements and testing means
US9795747B2 (en) 2010-06-02 2017-10-24 Sanofi-Aventis Deutschland Gmbh Methods and apparatus for lancet actuation
US9427532B2 (en) 2001-06-12 2016-08-30 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US7713214B2 (en) 2002-04-19 2010-05-11 Pelikan Technologies, Inc. Method and apparatus for a multi-use body fluid sampling device with optical analyte sensing
US8702624B2 (en) 2006-09-29 2014-04-22 Sanofi-Aventis Deutschland Gmbh Analyte measurement device with a single shot actuator
US8784335B2 (en) 2002-04-19 2014-07-22 Sanofi-Aventis Deutschland Gmbh Body fluid sampling device with a capacitive sensor
US9248267B2 (en) 2002-04-19 2016-02-02 Sanofi-Aventis Deustchland Gmbh Tissue penetration device
WO2004060370A1 (en) * 2002-12-16 2004-07-22 Boehringer Ingelheim Pharmaceuticals, Inc. Treatment of hiv infection through combined administration of tipranavir and capravirine
US8574895B2 (en) 2002-12-30 2013-11-05 Sanofi-Aventis Deutschland Gmbh Method and apparatus using optical techniques to measure analyte levels
US8668656B2 (en) 2003-12-31 2014-03-11 Sanofi-Aventis Deutschland Gmbh Method and apparatus for improving fluidic flow and sample capture
EP1751546A2 (en) 2004-05-20 2007-02-14 Albatros Technologies GmbH & Co. KG Printable hydrogel for biosensors
US9820684B2 (en) 2004-06-03 2017-11-21 Sanofi-Aventis Deutschland Gmbh Method and apparatus for a fluid sampling device
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CN102060786A (en) * 2011-01-20 2011-05-18 天津大学 4-(substituted-1,3-diyne)-4-(trifluoromethyl)-3,4-dihydro substituted quinazoline-2-ketone compound as well as preparation method and application thereof
PL2694101T3 (en) * 2011-04-06 2017-07-31 Université Paris Descartes Pharmaceutical compositions for preventing and/or treating an hiv disease in humans
CN104321325B (en) 2012-05-24 2016-11-16 诺华股份有限公司 Pyrrolopyrrole alkanone compound
WO2014115080A1 (en) 2013-01-22 2014-07-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
EP2948451B1 (en) 2013-01-22 2017-07-12 Novartis AG Substituted purinone compounds
BR112015029491A2 (en) 2013-05-27 2017-07-25 Novartis Ag imidazopyrrolidinone derivatives and their use in the treatment of disease
EA028035B1 (en) 2013-05-28 2017-09-29 Новартис Аг Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
JP2016520118A (en) 2013-05-28 2016-07-11 ノバルティス アーゲー Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of diseases
EA029269B1 (en) 2013-11-21 2018-02-28 Новартис Аг Pyrrolopyrrolone derivatives and their use for treating diseases

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Publication number Priority date Publication date Assignee Title
WO1993004047A1 (en) * 1991-08-16 1993-03-04 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
EP0530994A1 (en) * 1991-08-16 1993-03-10 Merck & Co. Inc. Quinazoline derivatives as inhibitors of HIV reverse transcriptase
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DE4320347A1 (en) * 1993-06-19 1994-12-22 Boehringer Mannheim Gmbh Quinazoline derivatives and medicaments containing them
GB2281297A (en) * 1993-08-27 1995-03-01 Merck & Co Inc Quinazoline compounds
WO1995012583A1 (en) * 1993-11-05 1995-05-11 Merck & Co., Inc. New quinazolines as inhibitors of hiv reverse transcriptase
WO1995013273A1 (en) * 1993-11-08 1995-05-18 Merck & Co., Inc. Asymmetric synthesis of (s)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1h)-quinazolinone
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Patent Citations (8)

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EP0530994A1 (en) * 1991-08-16 1993-03-10 Merck & Co. Inc. Quinazoline derivatives as inhibitors of HIV reverse transcriptase
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Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8845550B2 (en) 2001-06-12 2014-09-30 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US9339612B2 (en) 2002-04-19 2016-05-17 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US8845549B2 (en) 2002-04-19 2014-09-30 Sanofi-Aventis Deutschland Gmbh Method for penetrating tissue
US8905945B2 (en) 2002-04-19 2014-12-09 Dominique M. Freeman Method and apparatus for penetrating tissue
US9226699B2 (en) 2002-04-19 2016-01-05 Sanofi-Aventis Deutschland Gmbh Body fluid sampling module with a continuous compression tissue interface surface
US9314194B2 (en) 2002-04-19 2016-04-19 Sanofi-Aventis Deutschland Gmbh Tissue penetration device
US8690796B2 (en) 2002-04-19 2014-04-08 Sanofi-Aventis Deutschland Gmbh Method and apparatus for penetrating tissue
US9144401B2 (en) 2003-06-11 2015-09-29 Sanofi-Aventis Deutschland Gmbh Low pain penetrating member
US8945910B2 (en) 2003-09-29 2015-02-03 Sanofi-Aventis Deutschland Gmbh Method and apparatus for an improved sample capture device
US9351680B2 (en) 2003-10-14 2016-05-31 Sanofi-Aventis Deutschland Gmbh Method and apparatus for a variable user interface
US9775553B2 (en) 2004-06-03 2017-10-03 Sanofi-Aventis Deutschland Gmbh Method and apparatus for a fluid sampling device
US9386944B2 (en) 2008-04-11 2016-07-12 Sanofi-Aventis Deutschland Gmbh Method and apparatus for analyte detecting device
US9375169B2 (en) 2009-01-30 2016-06-28 Sanofi-Aventis Deutschland Gmbh Cam drive for managing disposable penetrating member actions with a single motor and motor and control system
US8965476B2 (en) 2010-04-16 2015-02-24 Sanofi-Aventis Deutschland Gmbh Tissue penetration device

Also Published As

Publication number Publication date
NO994904D0 (en) 1999-10-08
EP0973753A2 (en) 2000-01-26
KR20010006146A (en) 2001-01-26
HUP0001446A3 (en) 2001-11-28
IL132188A0 (en) 2001-03-19
WO1998045276A2 (en) 1998-10-15
HUP0001446A2 (en) 2001-05-28
AR012340A1 (en) 2000-10-18
CA2284996A1 (en) 1998-10-15
AU6796098A (en) 1998-10-30
BR9808513A (en) 2000-05-23
CN1252063A (en) 2000-05-03
JP2002504095A (en) 2002-02-05
NZ500592A (en) 2001-09-28
EA001991B1 (en) 2001-10-22
AU734928B2 (en) 2001-06-28
TW587078B (en) 2004-05-11
SK137899A3 (en) 2000-05-16
HRP980143A2 (en) 1999-02-28
NO994904L (en) 1999-12-01
EA199900907A1 (en) 2000-04-24
PL336305A1 (en) 2000-06-19
NO314936B1 (en) 2003-06-16
EE9900452A (en) 2000-04-17

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