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
NO20016034L (no
NO20016034D0 (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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic 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
    • A61K31/352—Heterocyclic 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 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic 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
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides 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
    • C07C311/18—Sulfonamides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, 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
    • C07C311/38—Sulfonamides, 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
    • C07C311/39—Sulfonamides, 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic 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
    • C07D317/46—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Enzymes And Modification Thereof (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 (el)
JP (2) JP4503896B2 (el)
KR (1) KR100762188B1 (el)
CN (2) CN100516034C (el)
AR (1) AR031520A1 (el)
AT (2) ATE534622T1 (el)
AU (1) AU779994B2 (el)
BR (1) BR0011745A (el)
CA (1) CA2380858C (el)
CO (1) CO5160337A1 (el)
CY (1) CY1112632T1 (el)
CZ (1) CZ303052B6 (el)
DE (1) DE60027722T2 (el)
DK (2) DK1686113T3 (el)
ES (2) ES2375823T3 (el)
HK (1) HK1046899B (el)
HU (1) HUP0300385A3 (el)
IL (3) IL146918A0 (el)
MX (1) MXPA01012808A (el)
MY (1) MY137777A (el)
NO (1) NO323951B1 (el)
NZ (1) NZ516003A (el)
PE (1) PE20010230A1 (el)
PL (1) PL210227B1 (el)
PT (2) PT1686113E (el)
SI (1) SI1194404T1 (el)
TN (1) TNSN00129A1 (el)
TR (3) TR200200407T2 (el)
TW (3) TW593248B (el)
WO (1) WO2000076961A1 (el)
ZA (1) ZA200110177B (el)

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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
ATE343567T1 (de) 2001-02-14 2006-11-15 Tibotec Pharm Ltd Breitspektrum 2-(substituierte-amino)- benzothiazol-sulfonamide hiv protease inhibitoren
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
AU2003231766A1 (en) * 2002-04-26 2003-11-10 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
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
US7767683B2 (en) 2003-08-18 2010-08-03 H. Lundbeck A/S Hydrogen succinate salts of trans-4-((1R, 3S)-6-chloro-3-phenylindan-1-YL)-1,2,2-trimethylpiperazine and the use as a medicament
CN102627609B (zh) * 2003-12-15 2016-05-04 默沙东公司 杂环天冬氨酰蛋白酶抑制剂
CN1953964A (zh) 2004-03-11 2007-04-25 塞阔伊亚药品公司 抗耐药性反转录病毒蛋白酶抑制剂
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
JP2008533017A (ja) * 2005-03-11 2008-08-21 スミスクライン ビーチャム コーポレーション Ｈｉｖプロテアーゼ阻害薬
US8227450B2 (en) 2005-11-30 2012-07-24 Ambrilia Biopharma Inc. Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation
EP2069356A1 (en) * 2006-07-24 2009-06-17 Gilead Sciences, Inc. Bisfuranyl protease inhibitors
PL2089371T3 (pl) 2006-11-09 2011-06-30 Janssen Sciences Ireland Uc Sposoby wytwarzania heksahydrofuro[2,3-b]furan-3-olu
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PT2152667E (pt) 2007-04-27 2011-04-06 Tibotec Pharm Ltd Processos para a preparação de derivados de n-isobutil-n- (2-hidroxi-3-amino-4-fenilbutil)-p-nitrobenzenosulfonilamida
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
JPWO2016039403A1 (ja) * 2014-09-11 2017-06-29 塩野義製薬株式会社 持続性ｈｉｖプロテアーゼ阻害剤
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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

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

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