DK1686113T3 - Inhibitorer af aspartylprotease - Google Patents

Inhibitorer af aspartylprotease

Info

Publication number
DK1686113T3
DK1686113T3 DK06009072.7T DK06009072T DK1686113T3 DK 1686113 T3 DK1686113 T3 DK 1686113T3 DK 06009072 T DK06009072 T DK 06009072T DK 1686113 T3 DK1686113 T3 DK 1686113T3
Authority
DK
Denmark
Prior art keywords
inhibitors
aspartyl protease
aspartyl
protease
Prior art date
Application number
DK06009072.7T
Other languages
English (en)
Inventor
Michael Robin Hale
Roger Tung
Stephen Price
Robin David Wilkes
Wayne Carl Schairer
Ashley Nicholas Jarvis
Andrew Spaltenstein
Eric Steven Furfine
Vicente Samano
Istvan Kaldor
John Franklin Miller
Michael Stephen Brieger
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
Application granted granted Critical
Publication of DK1686113T3 publication Critical patent/DK1686113T3/da

Links

Classifications

    • 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
DK06009072.7T 1999-06-11 2000-06-08 Inhibitorer af aspartylprotease DK1686113T3 (da)

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
EP00941279A EP1194404B1 (en) 1999-06-11 2000-06-08 Inhibitors of aspartyl protease

Publications (1)

Publication Number Publication Date
DK1686113T3 true DK1686113T3 (da) 2012-02-20

Family

ID=26836833

Family Applications (2)

Application Number Title Priority Date Filing Date
DK00941279T DK1194404T3 (da) 1999-06-11 2000-06-08 Aspartylproteaseinhibitorer
DK06009072.7T DK1686113T3 (da) 1999-06-11 2000-06-08 Inhibitorer af aspartylprotease

Family Applications Before (1)

Application Number Title Priority Date Filing Date
DK00941279T DK1194404T3 (da) 1999-06-11 2000-06-08 Aspartylproteaseinhibitorer

Country Status (31)

Country Link
EP (2) EP1194404B1 (da)
JP (2) JP4503896B2 (da)
KR (1) KR100762188B1 (da)
CN (2) CN101245058A (da)
AR (1) AR031520A1 (da)
AT (2) ATE534622T1 (da)
AU (1) AU779994B2 (da)
BR (1) BR0011745A (da)
CA (1) CA2380858C (da)
CO (1) CO5160337A1 (da)
CY (1) CY1112632T1 (da)
CZ (1) CZ303052B6 (da)
DE (1) DE60027722T2 (da)
DK (2) DK1194404T3 (da)
ES (2) ES2375823T3 (da)
HK (1) HK1046899B (da)
HU (1) HUP0300385A3 (da)
IL (3) IL146918A0 (da)
MX (1) MXPA01012808A (da)
MY (1) MY137777A (da)
NO (1) NO323951B1 (da)
NZ (1) NZ516003A (da)
PE (1) PE20010230A1 (da)
PL (1) PL210227B1 (da)
PT (2) PT1686113E (da)
SI (1) SI1194404T1 (da)
TN (1) TNSN00129A1 (da)
TR (3) TR200200407T2 (da)
TW (3) TW593248B (da)
WO (1) WO2000076961A1 (da)
ZA (1) ZA200110177B (da)

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AU767728B2 (en) * 1998-06-19 2003-11-20 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
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
DK1370543T3 (da) 2001-02-14 2007-02-19 Tibotec Pharm Ltd Bredspektrede 2-(substitueret amino) benzothiazol- sulfonamid-HIV-proteaseinhibitorer
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
DE60315023T2 (de) * 2002-04-26 2008-04-03 Gilead Sciences, Inc., Foster City Anreicherung in der zelle an phosphonat analoga von hiv protease inhibitor verbindungen und die verbindungen selbst
US6632816B1 (en) * 2002-12-23 2003-10-14 Pharmacor Inc. Aromatic derivatives as HIV aspartyl protease inhibitors
US20060148865A1 (en) * 2003-06-27 2006-07-06 Martin Michael T Preparation of chemical compounds
NZ575575A (en) 2003-08-18 2010-04-30 Lundbeck & Co As H Succinate and malonate salt of trans-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and the use as a medicament
CN101671307B (zh) * 2003-12-15 2014-05-14 默沙东公司 杂环天冬氨酰蛋白酶抑制剂
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
US20080194554A1 (en) * 2005-03-11 2008-08-14 Mclean Ed W Hiv Protease Inhibitors
EP1971615B1 (en) 2005-11-30 2014-01-01 TaiMed Biologics, Inc. Lysme-based prodrugs of aspartyl protease inhibitors and processes for their preparation
JP2009544708A (ja) * 2006-07-24 2009-12-17 ギリアード サイエンシーズ， インコーポレイテッド ビスフラニルプロテアーゼ阻害剤
BRPI0718706B8 (pt) 2006-11-09 2021-05-25 Janssen R & D Ireland métodos para a preparação de hexa-hidrofuro[2,3- b]furan-3-ol
EP2491785A1 (en) * 2006-11-21 2012-08-29 Purdue Research Foundation Method and compositions for treating HIV infections
ATE498606T1 (de) 2007-04-27 2011-03-15 Tibotec Pharm Ltd Herstellungsverfahren für n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)- - nitrobenzolsulfonylamidderivate
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
DK2480220T3 (da) * 2009-09-22 2015-02-23 Janssen R & D Ireland Behandling og forebyggelse af HIV-infektion
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
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections

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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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KR100336699B1 (ko) * 1992-08-25 2002-05-13 윌리암스 로저 에이 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
EP0666843B1 (en) * 1992-10-30 1999-08-18 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors
DE69415326T2 (de) * 1993-08-24 1999-06-02 Searle & Co Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
DE69637380T2 (de) * 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028465A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5705500A (en) * 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
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WO1999010373A1 (en) * 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Non-immunosuppressive cyclosporins and their use in the prevention and treatment of hiv infection
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
CZ20014431A3 (cs) 2002-06-12
KR100762188B1 (ko) 2007-10-04
JP4503896B2 (ja) 2010-07-14
PL210227B1 (pl) 2011-12-30
PL352830A1 (en) 2003-09-08
JP2003502309A (ja) 2003-01-21
CO5160337A1 (es) 2002-05-30
NO20016034D0 (no) 2001-12-10
BR0011745A (pt) 2002-03-19
CN101245058A (zh) 2008-08-20
AU779994B2 (en) 2005-02-24
PT1194404E (pt) 2006-08-31
EP1194404B1 (en) 2006-05-03
EP1194404A1 (en) 2002-04-10
TW200425891A (en) 2004-12-01
IL146918A0 (en) 2002-08-14
DE60027722D1 (en) 2006-06-08
AU5600600A (en) 2001-01-02
CA2380858A1 (en) 2000-12-21
NO20016034L (no) 2002-01-18
TR200200407T2 (tr) 2002-08-21
EP1686113A1 (en) 2006-08-02
MXPA01012808A (es) 2002-07-22
HUP0300385A2 (hu) 2003-07-28
NO323951B1 (no) 2007-07-23
TNSN00129A1 (fr) 2005-11-10
ES2263478T3 (es) 2006-12-16
MY137777A (en) 2009-03-31
ZA200110177B (en) 2003-01-13
IL202633A (en) 2013-02-28
SI1194404T1 (sl) 2006-10-31
DE60027722T2 (de) 2007-04-26
WO2000076961A1 (en) 2000-12-21
CZ303052B6 (cs) 2012-03-14
ATE325091T1 (de) 2006-06-15
IL146918A (en) 2010-06-16
TWI299000B (en) 2008-07-21
PT1686113E (pt) 2012-02-20
AR031520A1 (es) 2003-09-24
TR200603871T2 (tr) 2007-01-22
IL202633A0 (en) 2010-06-30
TR200202528T2 (tr) 2003-02-21
HK1046899B (zh) 2007-03-02
ATE534622T1 (de) 2011-12-15
TWI318116B (en) 2009-12-11
HUP0300385A3 (en) 2007-05-29
TW593248B (en) 2004-06-21
PE20010230A1 (es) 2001-03-15
CN100516034C (zh) 2009-07-22
CA2380858C (en) 2011-12-06
TW200804252A (en) 2008-01-16
CN1361765A (zh) 2002-07-31
HK1046899A1 (en) 2003-01-30
DK1194404T3 (da) 2006-09-04
JP2009046493A (ja) 2009-03-05
KR20020033642A (ko) 2002-05-07
NZ516003A (en) 2004-02-27
ES2375823T3 (es) 2012-03-06
EP1686113B1 (en) 2011-11-23
CY1112632T1 (el) 2016-02-10

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