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AU2012199A - Prodrugs of aspartyl protease inhibitors - Google Patents

Prodrugs of aspartyl protease inhibitors

Info

Publication number
AU2012199A
AU2012199A AU20121/99A AU2012199A AU2012199A AU 2012199 A AU2012199 A AU 2012199A AU 20121/99 A AU20121/99 A AU 20121/99A AU 2012199 A AU2012199 A AU 2012199A AU 2012199 A AU2012199 A AU 2012199A
Authority
AU
Australia
Prior art keywords
prodrugs
protease inhibitors
aspartyl protease
aspartyl
inhibitors
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.)
Abandoned
Application number
AU20121/99A
Inventor
Christopher T. Baker
Eric Steven Furfine
Michael R. Hale
Istvan Kaldor
Wieslaw Mieczyslaw Kazmierski
Andrew Spaltenstein
Roger D Tung
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2012199A publication Critical patent/AU2012199A/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/36—One oxygen atom with hydrocarbon radicals, substituted by nitrogen atoms, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU20121/99A 1997-12-24 1998-12-24 Prodrugs of aspartyl protease inhibitors Abandoned AU2012199A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US7030997P 1997-12-24 1997-12-24
US60070309 1997-12-24
PCT/US1998/027510 WO1999033795A1 (en) 1997-12-24 1998-12-24 Prodrugs of aspartyl protease inhibitors

Publications (1)

Publication Number Publication Date
AU2012199A true AU2012199A (en) 1999-07-19

Family

ID=22094523

Family Applications (1)

Application Number Title Priority Date Filing Date
AU20121/99A Abandoned AU2012199A (en) 1997-12-24 1998-12-24 Prodrugs of aspartyl protease inhibitors

Country Status (2)

Country Link
AU (1) AU2012199A (en)
WO (1) WO1999033795A1 (en)

Families Citing this family (46)

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AU777824B2 (en) * 1999-11-24 2004-11-04 Merck Sharp & Dohme Corp. Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors
ES2275866T3 (en) 2001-02-14 2007-06-16 Tibotec Pharmaceuticals Ltd. 2- (AMINOSUSTITUDED) -BENZOTIAZOL-SULFONAMIDES OF SPACIOUS INHIBITING SPIRITS OF THE HIV PROTEASE.
EE05384B1 (en) 2001-04-09 2011-02-15 Tibotec�Pharmaceuticals�Ltd. Broad-spectrum Á2- (Substituted Áamino) Benzoxazole Sulphonamides ÁkuiÁHIVÁProtease Inhibitors, Use, Pharmaceutical Formulations, and Method for Inhibiting Antiretroviral Replication
NZ529250A (en) 2001-05-11 2005-05-27 Tibotec Pharm Ltd Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors
PL216539B1 (en) 2001-12-21 2014-04-30 Tibotec Pharm Ltd Broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors
MY142238A (en) 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
CA2485903C (en) 2002-05-17 2011-08-16 Tibotec Pharmaceuticals Ltd. Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
MXPA05001792A (en) 2002-08-14 2005-04-25 Tibotec Pharm Ltd Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors.
MY149978A (en) * 2003-12-15 2013-11-15 Merck Sharp & Dohme Heterocyclic aspartyl protease inhibitors
ES2305887T3 (en) 2003-12-18 2008-11-01 Janssen Pharmaceutica Nv DERIVATIVES OF PIRIDO AND PYRIMIDOPIRIMIDINAS AS ANTIPROLIFERATIVE AGENTS.
EP1789107B1 (en) 2004-08-30 2009-05-27 Interstitial Therapeutics Medical stent provided with inhibitors of atp synthesis
US7723310B2 (en) 2004-10-18 2010-05-25 Three Rivers Pharmaceuticals, Llc Large dose ribavirin formulations
CN101098698A (en) 2004-12-01 2008-01-02 德福根有限公司 5-carboxamido substitued thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family
NI200700147A (en) 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv QUINAZOLINE DERIVATIVES KINE INHIBITORS TARGETING MULTIP
WO2006063848A1 (en) 2004-12-17 2006-06-22 Devgen N.V. Nematicidal compositions
AR053845A1 (en) 2005-04-15 2007-05-23 Tibotec Pharm Ltd 5-TIAZOLILMETIL [(1S, 2R) -3 - [[(2-AMINO-6-BENZOXAZOLIL) SULFONIL)] (2-METHYLPROPIL) AMINO] -2-HYDROXY-1- (PHENYLMETIL) PROPIL] CARBAMATE AS A PHARMACY IMPROVER METABOLIZED BY THE CYCROCHROME P450
WO2006138265A2 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
EP1940856B1 (en) 2005-10-21 2014-10-08 Universiteit Antwerpen Novel urokinase inhibitors
AR058238A1 (en) 2005-11-28 2008-01-23 Tibotec Pharm Ltd COMPOUNDS AND DERIVATIVES OF AMINOPHENYL SULFONAMIDE REPLACED AS HIV PROTEASE INHIBITORS
AR057182A1 (en) 2005-11-28 2007-11-21 Tibotec Pharm Ltd AMINOPHENYL SULFONAMIDE COMPOUNDS REPLACED AS HIV PROTEASE INHIBITORS
US8492377B2 (en) 2006-07-13 2013-07-23 Janssen Pharmaceutica Nv MTKI quinazoline derivatives
BRPI0716554A2 (en) 2006-09-08 2013-09-24 Bayer Schering Pharma Ag compound methods for 18f labeled agents
WO2009016132A1 (en) 2007-07-27 2009-02-05 Janssen Pharmaceutica Nv Pyrrolopyrimidines
EP2053033A1 (en) 2007-10-26 2009-04-29 Bayer Schering Pharma AG Compounds for use in imaging, diagnosing and/or treatment of diseases of the central nervous system or of tumors
EP2100900A1 (en) 2008-03-07 2009-09-16 Universitätsspital Basel Bombesin analog peptide antagonist conjugates
JP5480824B2 (en) 2008-03-10 2014-04-23 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 4-Aryl-2-anilino-pyrimidines as PLK kinase inhibitors
EP2116236A1 (en) 2008-04-21 2009-11-11 Université de Mons-Hainaut Bisbenzamidine derivatives for use as antioxidant
EP2501431B1 (en) 2009-11-19 2020-01-08 Wellinq Medical B.V. Narrow profile composition-releasing expandable medical balloon catheter
WO2011141515A1 (en) 2010-05-14 2011-11-17 Bayer Pharma Aktiengesellschaft Diagnostic agents for amyloid beta imaging
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
GB201019043D0 (en) 2010-11-10 2010-12-22 Protea Biopharma N V Use of 2',5'-oligoadenylate derivative compounds
EP2700396A3 (en) 2012-06-20 2015-04-29 Sylphar Nv Strip for the delivery of oral care compositions
WO2014059034A2 (en) 2012-10-09 2014-04-17 President And Fellows Of Harvard College Nad biosynthesis and precursors for the treatment and prevention of cancer and proliferation
WO2016003450A1 (en) 2014-07-01 2016-01-07 The Regents Of The University Of California Pkc-epsilon inhibitors
WO2016083490A1 (en) 2014-11-27 2016-06-02 Remynd Nv Compounds for the treatment of amyloid-associated diseases
EP3288637B1 (en) 2015-04-28 2022-09-14 NewSouth Innovations Pty Limited Targeting nad+ to treat chemotherapy and radiotherapy induced cognitive impairment, neuropathies and inactivity
EA201992397A1 (en) 2017-05-11 2020-03-16 Реминд Н.В. COMPOUNDS FOR THE TREATMENT OF EPILEPSY, NEURODEGENERATIVE DISORDERS AND OTHER CNS DISORDERS
JP2023514443A (en) 2020-02-24 2023-04-05 カトリーケ、ユニベルシテート、ルーベン Pyrrolopyridine and imidazopyridine antiviral compounds
EP4267579A1 (en) 2020-12-22 2023-11-01 Luxembourg Institute of Health (LIH) Conolidine analogues as selective ackr3 modulators for the treatment of cancer and cardiovascular diseases
US20240002351A1 (en) 2021-03-04 2024-01-04 Universiteit Antwerpen Quinazolin-4-one and thieno[2,3-d]pyrimidin-4-one inhibitors of erbb4 (her4) for use in the treatment of cancer
EP4347541A2 (en) 2021-05-31 2024-04-10 Telix Pharmaceuticals (Innovations) Pty Ltd Improved prostate-specific membrane antigen targeting radiopharmaceuticals and uses thereof
WO2023021132A1 (en) 2021-08-18 2023-02-23 Katholieke Universiteit Leuven 6-substituted- and 6,7-disubstituted-7-deazapurine ribonucleoside analogues
WO2023046900A1 (en) 2021-09-23 2023-03-30 Katholieke Universiteit Leuven Ribonucleoside analogues against -sars-cov-2
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HUP9901024A2 (en) * 1996-01-26 1999-09-28 Vertex Pharmaceuticals Incorporated Oxo derivatives of saturated azoles, pharmaceutical compositions containing them and their use

Also Published As

Publication number Publication date
WO1999033795A1 (en) 1999-07-08

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Legal Events

Date Code Title Description
MK6 Application lapsed section 142(2)(f)/reg. 8.3(3) - pct applic. not entering national phase