NO323951B1 - Sulfonamider som er inhibitorer av aspartylprotease, sammensetninger inneholdende disse og deres anvendelse - Google Patents

Sulfonamider som er inhibitorer av aspartylprotease, sammensetninger inneholdende disse og deres anvendelse Download PDF

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Publication number
NO323951B1
NO323951B1 NO20016034A NO20016034A NO323951B1 NO 323951 B1 NO323951 B1 NO 323951B1 NO 20016034 A NO20016034 A NO 20016034A NO 20016034 A NO20016034 A NO 20016034A NO 323951 B1 NO323951 B1 NO 323951B1
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NO
Norway
Prior art keywords
amino
mmol
optionally substituted
isobutyl
benzyl
Prior art date
Application number
NO20016034A
Other languages
English (en)
Norwegian (no)
Other versions
NO20016034D0 (no
NO20016034L (no
Inventor
Andrew Spaltenstein
Roger D Tung
Michael Robin Hale
Eric Steven Furfine
Istvan Kaldor
Stephen Price
Robin David Wilkes
Wayne Carl Schairer
Vicente Samano
John Franklin Miller
Michael Stephen Brieger
Ashley Nicholas Jarvis
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of NO20016034D0 publication Critical patent/NO20016034D0/no
Publication of NO20016034L publication Critical patent/NO20016034L/no
Publication of NO323951B1 publication Critical patent/NO323951B1/no

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
NO20016034A 1999-06-11 2001-12-10 Sulfonamider som er inhibitorer av aspartylprotease, sammensetninger inneholdende disse og deres anvendelse NO323951B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13907099P 1999-06-11 1999-06-11
US19021100P 2000-03-17 2000-03-17
PCT/US2000/015781 WO2000076961A1 (en) 1999-06-11 2000-06-08 Inhibitors of aspartyl protease

Publications (3)

Publication Number Publication Date
NO20016034D0 NO20016034D0 (no) 2001-12-10
NO20016034L NO20016034L (no) 2002-01-18
NO323951B1 true NO323951B1 (no) 2007-07-23

Family

ID=26836833

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20016034A NO323951B1 (no) 1999-06-11 2001-12-10 Sulfonamider som er inhibitorer av aspartylprotease, sammensetninger inneholdende disse og deres anvendelse

Country Status (31)

Country Link
EP (2) EP1194404B1 (tr)
JP (2) JP4503896B2 (tr)
KR (1) KR100762188B1 (tr)
CN (2) CN100516034C (tr)
AR (1) AR031520A1 (tr)
AT (2) ATE534622T1 (tr)
AU (1) AU779994B2 (tr)
BR (1) BR0011745A (tr)
CA (1) CA2380858C (tr)
CO (1) CO5160337A1 (tr)
CY (1) CY1112632T1 (tr)
CZ (1) CZ303052B6 (tr)
DE (1) DE60027722T2 (tr)
DK (2) DK1686113T3 (tr)
ES (2) ES2375823T3 (tr)
HK (1) HK1046899B (tr)
HU (1) HUP0300385A3 (tr)
IL (3) IL146918A0 (tr)
MX (1) MXPA01012808A (tr)
MY (1) MY137777A (tr)
NO (1) NO323951B1 (tr)
NZ (1) NZ516003A (tr)
PE (1) PE20010230A1 (tr)
PL (1) PL210227B1 (tr)
PT (2) PT1686113E (tr)
SI (1) SI1194404T1 (tr)
TN (1) TNSN00129A1 (tr)
TR (3) TR200202528T2 (tr)
TW (3) TWI299000B (tr)
WO (1) WO2000076961A1 (tr)
ZA (1) ZA200110177B (tr)

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ATE285396T1 (de) * 1998-06-19 2005-01-15 Vertex Pharma Sulfonamide als aspartyl-protease-inhibitoren
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
EE05385B1 (et) * 2001-02-14 2011-02-15 Tibotec�Pharmaceuticals�Ltd. LaiaspektrilisedÁ2-(asendatudÁamino)bensotiasoolsulfoonamiididÁkuiÁHIVÁproteaasiÁinhibiitorid,ÁnendeÁvalmistamismeetodÁjaÁkasutamineÁningÁfarmatseutilineÁkompositsioon
US7285566B2 (en) * 2002-01-07 2007-10-23 Erickson John W Resistance-repellent retroviral protease inhibitors
MY142238A (en) * 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
US20070010489A1 (en) * 2002-04-26 2007-01-11 Arimilli Murty N Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds
US6632816B1 (en) * 2002-12-23 2003-10-14 Pharmacor Inc. Aromatic derivatives as HIV aspartyl protease inhibitors
JP2007521277A (ja) * 2003-06-27 2007-08-02 スミスクライン ビーチャム コーポレーション 化合物の製造
MXPA06001938A (es) 2003-08-18 2006-05-17 Lundbeck & Co As H Trans-1-(6-cloro-3-fenilindan-1-il)-3,3-dimetilpiperazina.
SI1699455T1 (sl) * 2003-12-15 2013-10-30 Merck Sharp & Dohme Corp. Heterocikliäśni aspartil proteazni inhibitorji
AU2005222435B2 (en) 2004-03-11 2012-03-15 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
TWI383975B (zh) 2004-03-31 2013-02-01 Tibotec Pharm Ltd 製備(3R,3aS,6aR)六氫-呋喃并〔2,3-b〕呋喃-3-醇之方法
US7388008B2 (en) 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
TWI376373B (en) 2005-02-16 2012-11-11 Lundbeck & Co As H Crystalline base of a pharmaceutical compound
TWI453198B (zh) 2005-02-16 2014-09-21 Lundbeck & Co As H 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s)-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Hiv protease inhibitors
AU2006319716B2 (en) 2005-11-30 2012-02-02 Taimed Biologics, Inc. Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation
US20090312318A1 (en) * 2006-07-24 2009-12-17 Desai Manoj C Therapeutic compounds and methods
DE602007012365D1 (de) 2006-11-09 2011-03-17 Little Island Co Cork Verfahren zur herstellung von hexahydrofuroä2,3-büfuran-3-ol
US9808527B2 (en) * 2006-11-21 2017-11-07 Purdue Research Foundation Methods and compositions for treating HIV infections
BRPI0810609A2 (pt) 2007-04-27 2014-10-21 Tibotec Pharm Ltd Métodos para a preparação de derivados de n-isobutil-n-(2-hidróxi-a-amino-4-fenilbutil)-p-nitrobe nzenossulfonilamida
GB2452952A (en) * 2007-09-20 2009-03-25 Npil Pharmaceuticals N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
MX2012003424A (es) 2009-09-22 2012-05-08 Tibotec Pharm Ltd Tratamiento y prevencion de infeccion por el virus de inmunodeficiencia humana.
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
CN103193570B (zh) * 2013-04-09 2014-01-22 湖北来凤腾升香料化工有限公司 一种羟基高选择性保护方法
EP3192794A4 (en) * 2014-09-11 2018-06-27 Shionogi & Co., Ltd. Sustained hiv protease inhibitor
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CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
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ATE183499T1 (de) * 1992-10-30 1999-09-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfamins uren verwendbar als inhibitoren retroviraler proteasen
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GB9712504D0 (en) * 1997-06-17 1997-08-20 Dundee Teaching Hospitals Nhs Thermal imaging method and apparatus
WO1999010374A1 (en) * 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Cyclosporin a conjugates and uses therefor
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion

Also Published As

Publication number Publication date
EP1194404A1 (en) 2002-04-10
ZA200110177B (en) 2003-01-13
BR0011745A (pt) 2002-03-19
MY137777A (en) 2009-03-31
PL210227B1 (pl) 2011-12-30
TW200425891A (en) 2004-12-01
TR200202528T2 (tr) 2003-02-21
HK1046899B (zh) 2007-03-02
AU5600600A (en) 2001-01-02
MXPA01012808A (es) 2002-07-22
DK1686113T3 (da) 2012-02-20
IL202633A0 (en) 2010-06-30
IL146918A0 (en) 2002-08-14
PT1194404E (pt) 2006-08-31
KR20020033642A (ko) 2002-05-07
NZ516003A (en) 2004-02-27
DE60027722T2 (de) 2007-04-26
JP2009046493A (ja) 2009-03-05
AR031520A1 (es) 2003-09-24
ES2375823T3 (es) 2012-03-06
TW593248B (en) 2004-06-21
TWI299000B (en) 2008-07-21
CN101245058A (zh) 2008-08-20
HK1046899A1 (en) 2003-01-30
EP1686113B1 (en) 2011-11-23
NO20016034D0 (no) 2001-12-10
TWI318116B (en) 2009-12-11
ES2263478T3 (es) 2006-12-16
PT1686113E (pt) 2012-02-20
AU779994B2 (en) 2005-02-24
TR200603871T2 (tr) 2007-01-22
TW200804252A (en) 2008-01-16
KR100762188B1 (ko) 2007-10-04
CO5160337A1 (es) 2002-05-30
CZ303052B6 (cs) 2012-03-14
JP2003502309A (ja) 2003-01-21
EP1686113A1 (en) 2006-08-02
IL202633A (en) 2013-02-28
HUP0300385A2 (hu) 2003-07-28
JP4503896B2 (ja) 2010-07-14
ATE325091T1 (de) 2006-06-15
TNSN00129A1 (fr) 2005-11-10
SI1194404T1 (sl) 2006-10-31
HUP0300385A3 (en) 2007-05-29
ATE534622T1 (de) 2011-12-15
CZ20014431A3 (cs) 2002-06-12
CN100516034C (zh) 2009-07-22
NO20016034L (no) 2002-01-18
CY1112632T1 (el) 2016-02-10
CN1361765A (zh) 2002-07-31
TR200200407T2 (tr) 2002-08-21
IL146918A (en) 2010-06-16
EP1194404B1 (en) 2006-05-03
CA2380858A1 (en) 2000-12-21
PE20010230A1 (es) 2001-03-15
DE60027722D1 (en) 2006-06-08
CA2380858C (en) 2011-12-06
WO2000076961A1 (en) 2000-12-21
DK1194404T3 (da) 2006-09-04
PL352830A1 (en) 2003-09-08

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