AR037976A1 - Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento. - Google Patents

Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento.

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Publication number
AR037976A1
AR037976A1 ARP020105066A ARP020105066A AR037976A1 AR 037976 A1 AR037976 A1 AR 037976A1 AR P020105066 A ARP020105066 A AR P020105066A AR P020105066 A ARP020105066 A AR P020105066A AR 037976 A1 AR037976 A1 AR 037976A1
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Argentina
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alkyl
het1
het2
cycloalkyl
aryl
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ARP020105066A
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Tibotec Pharm Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • 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
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Reivindicación 1: Sulfonamidas que contienen fenilo sustituido con grupos heterocíclicos que tiene la fórmula (1) su N-óxido, sal, forma estereoisomérica, mezcla racémica, pro-fármaco, éster o metabolito, en los que: R1 y R8 son, cada uno, de manera independiente, hidrógeno, alquilo C1-6, alquenilo C2-6, arilalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, arilo, Het1, Het1 alquilo C1-6, Het2, Het2 alquilo C1-6; R1 también puede ser un radical de la fórmula (2) donde: R9, R10a y R10b son, cada uno, de manera independiente, hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4) aminocarbonilo, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 o alquilo C1-4 sustituido, de manera opcional, con arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4) aminocarbonilo, aminosulfonilo, alquil C1-4 S(O)t, hidroxi, ciano, halógeno o amino, mono- o disustituido de manera opcional donde los sustituyentes se seleccionan de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; donde R9, R10a y los átomos de carbono a los cuales están unidos también pueden formar un radical cicloalquilo C3-7; R11a es hidrógeno, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo, aminocarbonilo, mono- o disustituido de manera opcional, aminoalquil C1-4 carboniloxi mono- o di sustituido de manera opcional, alquiloxicarbonilo C1-4, ariloxicarbonilo, Het1 oxicarbonilo, Het2 oxicarbonilo, ariloxicarbonilalquilo C1-4, arilalquil C1-4 oxicarbonilo, alquilcarbonilo C1-4, cicloalquilcarbonilo C3-7, cicloalquil C3-7 alquiloxicarbonilo C1-4, cicloalquilcarboniloxi C3-7, carboxilalquil C1-4 carboniloxi, alquilcarboniloxi C1-4, arilalquilcarboniloxi C1-4, arilcarboniloxi, ariloxicarbonilox, Het1 carbonilo, Het1 carboniloxi, Het1 alquiloxicarbonilo C1-4, Het2 carboniloxi, Het2 alquilcarboniloxi C1-4, Het2 alquiloxicarboniloxi C1-4 o alquilo C1-4 sustituido de manera opcional con arilo, ariloxi, Het2 o hidroxi; donde los sustituyentes en los grupos amino se seleccionan cada uno, de manera independiente, de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; R11b es hidrógeno, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, arilo, Het1, Het2 o alquilo C1-4 sustituido, de manera opcional, con halógeno, hidroxi, alquilo C1-4S(=O)t, arilo, cicloalquilo C3-7, Het1, Het2, amino, mono- o disustituido, de manera opcional, donde los sustituyentes se seleccionan de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; donde R11b puede estar unido al resto de la molécula por medio de un grupo sulfonilo, R2 es hidrógeno o alquilo C1-6; L es -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-alcanodiilo C1-6-C(=O), -NR8-alcanodiilo C1-6-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 donde el grupo C(=O) o el grupo S(=O)2 está unido a la porción NR2; R3 es alquilo C1-6, arilo, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, o arilalquilo C1-4; R4 es hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo mono- o disustituido de manera opcional, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 o alquilo C1-6, donde el cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 y alquilo C1-6 pueden estar sustituidos, de manera opcional, con un sustituyente seleccionado de arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo mono- o disustituido de manera opcional, aminosulfonilo mono- o disustituido de manera opcional, alquil C1-4 S(=O)t, hidroxi, ciano, amino mono- o disustituido de manera opcional y halógeno, y donde los sustituyentes opcionales en la función amino se seleccionan, de manera independiente de alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; t es 0, 1 o 2; cada t seleccionada de manera independiente es 0, 1 o 2; H arilo es un heterociclo monocíclico, bicíclico o tricíclico aromático que tiene de 3 a 14 miembros en el anillo que contiene en el anillo uno o más heteroátomos seleccionados de nitrógeno, oxígeno y azufre y que, pueden, de manera opcional, estar sustituidos en (1) uno o más átomos de carbono por alquilo C1-6, halógeno, hidroxi, amino mono- o disustituido de manera opcional, nitro, ciano, haloalquilo C1-6, carboxilo, cicloalquilo C3-7, aminocarbonilo mono- o disustituido de manera opcional, metiltio, metilsulfonilo, arilo, -(R7a)n-M-R7b, Het1 y Het2; donde los sustituyentes opcionales en cualquier función amino se seleccionan de manera independiente de R5 y -A-R6; y en (2) un átomo de nitrógeno si está presente, por hidroxi o -A-R6; A es alcanodiilo C1-6, -C(=O)-, -C(=S)-, -S(=O)2-, alcanodiilo C1-6 -C(=O)-, alcanodiilo C1-6 -C(=S)- o alcanodiilo C1-6 -S(=O)2; donde para aquellos grupos que contienen una porción alcanodiilo C1-6, la porción alcanodiilo C1-6 está unida al grupo amino; R5 es hidroxi, alquilo C1-6, Het1 alquilo C1-6, aminoalquilo C1-6 donde el grupo amino puede estar mono- o disustituido de manera opcional con alquilo C1-4; R6 es hidrógeno, alquiloxi C1-6, Het1, Het1 oxi, Het2 oxi, arilo, ariloxi o amino; y, en el caso en que -A- sea diferente de alcanodiilo C1-6, entonces, R6 también puede ser alquilo C1-6, Het1 alquilo C1-4, Het1 oxialquilo C1-4, Het2 alquilo C1-4, Het2 oxialquilo C1-4, arilalquilo C1-4, ariloxialquilo C1-4 o aminoalquilo C1-4; donde cada uno de os grupos amino en la definición de R6 pueden estar sustituidos, de manera opcional, con uno o más sustituyentes seleccionados de alquilo C1-4, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1, Het2, arilalquilo C1-4, Het1 alquilo C1-4 o Het2 alquilo C1-4; R7a es alcanodiilo C1-8 sustituido, de manera opcional, por uno o más sustituyentes seleccionados de halógeno, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1 o Het2; R7b es alquilo C1-8, sustituido, de manera opcional, con uno o más sustituyentes seleccionados de halógeno, alquilcarbonilo C1-4, alquiloxicarbonilo C1-4, arilo, arilcarbonilo, ariloxicarbonilo, Het1 o Het2; M se define como -C(=O)-, -O-C(=O)-, -C(=O)-O-, -CH2CHOH-, -CHOH-CH2-, -NR8-C(=O)-, -(C=O)-NR8-, -S(=O)2-, -O-, -S-, -O-S(=O)2-, -S(=O)2-O-, -NR8-S(=O)2 o -S(=O)2-R8-; n es 0 o 1. Fabricación de medicamentos como inhibidores de la proteasa del HIV de amplio espectro, los procesos de preparación, así como también las composiciones farmacéuticas que las comprenden, con otro agente antirretroviral.
ARP020105066A 2001-12-21 2002-12-20 Sulfonamidas que contienen fenilo sustituido con grupos heterociclicos, una composicion farmaceutica, un producto combinado con un agente antirretroviral y el uso de las mismas para la fabricacion de un medicamento. AR037976A1 (es)

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KR (1) KR100942743B1 (es)
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AR (1) AR037976A1 (es)
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Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100364531C (zh) * 2002-12-18 2008-01-30 西托维亚公司 3,5－二取代－[1,2,4]－二唑及类似物和其用途
US20080234288A1 (en) * 2003-09-30 2008-09-25 Kenneth Alan Simmen Hcv Inhibiting Sulfonamides
EP2422781A1 (en) * 2004-05-07 2012-02-29 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
AU2006217922B2 (en) 2005-02-25 2012-04-05 Janssen Sciences Ireland Uc Protease inhibitor precursor synthesis
WO2008004100A2 (en) 2006-07-05 2008-01-10 Pfizer Products Inc. Therapeutic compounds
US20120316161A1 (en) 2009-12-23 2012-12-13 Katholieke Universiteit Leuven Novel antiviral compounds
US8563597B2 (en) * 2010-09-02 2013-10-22 Purdue Research Foundation Fused tricyclic ether carbamates and their use
CA2817896A1 (en) 2010-11-15 2012-05-24 Viiv Healthcare Uk Limited Inhibitors of hiv replication
EP2640705A2 (en) 2010-11-15 2013-09-25 Katholieke Universiteit Leuven Novel antiviral compounds
EP3192794A4 (en) * 2014-09-11 2018-06-27 Shionogi & Co., Ltd. Sustained hiv protease inhibitor

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
PH30929A (en) 1992-09-03 1997-12-23 Janssen Pharmaceutica Nv Beads having a core coated with an antifungal and a polymer.
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
DE69415326T2 (de) 1993-08-24 1999-06-02 G.D. Searle & Co., Chicago, Ill. Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
IL111080A (en) 1993-10-01 1999-08-17 Astra Ab Method for treating a finely divided powder medicament
JP4014220B2 (ja) 1995-01-20 2007-11-28 ジー．ディー．サール アンド カンパニー ビス−スルホンアミドヒドロキシエチルアミノ レトロ ウイルスプロテアーゼインヒビター
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
US5705500A (en) 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
RU2174519C2 (ru) 1995-03-10 2001-10-10 Джи. Ди. Сирл Энд Ко. Гидроксиэтиламино сульфонамиды гетероциклокарбонил аминокислоты, ингибирующие ретровирусную протеазу
JPH09124630A (ja) * 1995-10-26 1997-05-13 Kissei Pharmaceut Co Ltd カルバミン酸テトラヒドロフリルエステル誘導体の製造方法
WO1997018205A1 (en) 1995-11-15 1997-05-22 G.D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
CN1165291C (zh) 1996-05-20 2004-09-08 詹森药业有限公司 具有改进的生物利用度的抗真菌组合物
HU224217B1 (hu) 1997-03-26 2005-06-28 Janssen Pharmaceutica N.V. Gombaellenes hatóanyaggal és polimerrel bevont magrészt tartalmazó pelletek
AU2010299A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
BR9814484A (pt) 1997-12-24 2000-10-10 Vertex Pharma "pró-drogas de inibidores de aspartil protease"
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
DK1086076T3 (da) * 1998-06-19 2005-03-29 Vertex Pharma Sulfonamidinhibitorer af aspartylprotease
WO1999067417A2 (en) 1998-06-23 1999-12-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Fitness assay and associated methods
WO1999067254A2 (en) 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof

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CA2470964A1 (en) 2003-07-03
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HUP0500164A2 (hu) 2005-05-30
BR0215260A (pt) 2004-12-07
CN100448444C (zh) 2009-01-07
ZA200405784B (en) 2005-11-30
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