PE20010230A1 - Sulfonamidas como inhibidores de aspartil proteasa - Google Patents

Sulfonamidas como inhibidores de aspartil proteasa

Info

Publication number
PE20010230A1
PE20010230A1 PE2000000573A PE0005732000A PE20010230A1 PE 20010230 A1 PE20010230 A1 PE 20010230A1 PE 2000000573 A PE2000000573 A PE 2000000573A PE 0005732000 A PE0005732000 A PE 0005732000A PE 20010230 A1 PE20010230 A1 PE 20010230A1
Authority
PE
Peru
Prior art keywords
alkyl
aspartile
heterocycle
cycloalkyl
aryl
Prior art date
Application number
PE2000000573A
Other languages
English (en)
Inventor
Andrew Spaltenstein
Istvan Kaldor
Vicente Samano
Roger Tung
Robin David Wilkes
Ashley Nicholas Jarvis
John Franklin Miller
Michael Stephen Brieger
Eric Steven Furfine
Wayne Carl Schairer
Stephen Price
Michael Robin Hale
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 PE20010230A1 publication Critical patent/PE20010230A1/es

Links

Classifications

    • 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

Abstract

SE REFIERE A UN COMPUESTO SULFONAMIDA DE FORMULA I, DONDE: A ES H, Ht, R1-Ht, R1-ALQUILO C1-C6; R1 ES -C(O)-, S(O)2, -C(O)-C(O)-, -O-C(O)-, O-S(O)2, ENTRE OTROS; Ht ES CICLOALQUILO C3-C7, CICLOALQUENILO C5-C7, ARILO C6-C14, HETEROCICLO C5-C7 QUE CONTIENE N, N(R2), O, S, S(O)n, DICHO ARILO O HETEROCICLO ESTA FUSIONADO A Q; R2 ES H, ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO CON UN ANILLO CARBOXICLICO DE 3 A 7 MIEMBROS, HETEROCICLO DE 5-7 MIEMBROS OPCIONALMENTE SUSTITUIDO CON 1-4 -X`-Y', O-ARILALQUILO, ENTRE OTROS; X' ES O, S, NH, NHCO, NHCOO, ENTRE OTROS; Y' ES ALQUILO C1-C15, ALQUENILO C2-C15; G ES H, R7, ALQUILO C1-C4; CUANDO G ES ALQUILO C1-C4, G Y R7 ESTAN UNIDOS Y FORMAN UN ANILLO HETEROCICLO; D ES ALQUILO C1-C6 SUSTITUIDO CON Q OPCIONALMENTE SUSTITUIDO CON CICLOALQUILO C3-C6, ENTRE OTROS; E ES Ht, O-Ht, ALQUILO C1-C6, ENTRE OTROS; R7 ES GRUPO a, b; M ES Na, Mg, ENTRE OTROS; M' ES H, ALQUILO C1-C12, ALQUENILO C2-C12, ENTRE OTROS; x ES 0-1; y ES P, S; X ES O, S; Z ES O, S, N(R2)2. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS (1O,2ß,3O)-9-[2,3-BIS(HIDROXIMETIL)CICLOBUTIL]GUANINA, NUCLEOSIDOS ACICLICOS, ACICLOVIR, LAMIVUDINA, RIBAVIRINA, INTERFERON, ENTRE OTROS. EL COMPUESTO I INHIBE A LA ASPARTIL PROTEASA HIVY PUEDE SER UTIL PARA EL TRATAMIENTO DEL SIDA, LINFADENOPATIA PROGRESIVA GENERALIZADA, SARCOMA DE KAPOSI
PE2000000573A 1999-06-11 2000-06-08 Sulfonamidas como inhibidores de aspartil proteasa PE20010230A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13907099P 1999-06-11 1999-06-11
US19021100P 2000-03-17 2000-03-17

Publications (1)

Publication Number Publication Date
PE20010230A1 true PE20010230A1 (es) 2001-03-15

Family

ID=26836833

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000573A PE20010230A1 (es) 1999-06-11 2000-06-08 Sulfonamidas como inhibidores de aspartil proteasa

Country Status (31)

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

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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
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Also Published As

Publication number Publication date
CZ20014431A3 (cs) 2002-06-12
DK1686113T3 (da) 2012-02-20
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
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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