AR058094A1 - Inhibidores nnrt basados en fenil-acetamida - Google Patents

Inhibidores nnrt basados en fenil-acetamida

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Publication number
AR058094A1
AR058094A1 ARP060104513A ARP060104513A AR058094A1 AR 058094 A1 AR058094 A1 AR 058094A1 AR P060104513 A ARP060104513 A AR P060104513A AR P060104513 A ARP060104513 A AR P060104513A AR 058094 A1 AR058094 A1 AR 058094A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
group
independently
haloalkyl
Prior art date
Application number
ARP060104513A
Other languages
English (en)
Inventor
Tania Silva
Taraneh Mirzadegan
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37606927&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR058094(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR058094A1 publication Critical patent/AR058094A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/29—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • 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
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/56—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • 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
    • C07C311/23—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/24—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • 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
    • C07C311/31—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 atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/35—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 atoms of the sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/52—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente proporciona compuestos utiles para el tratamiento de una infeccion del VIH, para prevenir una infeccion del VIH, o para tratar el SIDA o el ARC. Los compuestos de la presente son de la formula (1), en la que e R1 a R4 y Ar tienen los significados definidos anteriormente. Se describen también en la presente, métodos de tratamiento de una infeccion del VIH con compuestos definidos en esta solicitud y composiciones farmacéuticas que contienen dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) en la que: R1 es halogeno, alquilo C1-6, alcoxi C1-6, nitro o amino; R2 es H o F; R3 es fenilo sustituido de 1 a 3 veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, halogeno, ciano y nitro; R4 es H, alquilo C1-6 o halogeno; Ar es un anillo fenilo sustituido de la formula (2) con la condicion de que R7a y R7c no sean ambos H o que si R7c es H, entonces R7a es halogeno, haloalquilo C1-6, alcoxi C1-6, ciano o alquilo C1-6; en la que R7a se elige entre el grupo formado por H, alquilo C1-6, haloalquilo C1-3, cicloalquilo C3-7, alcoxi C1-6, haloalcoxi C1-6, halogeno y ciano; R7c se elige entre el grupo formado por halogeno, -S(O)2N-R8R9, -X2CH2(CH2)pS(O)2NR8R9; -X4(CH2)vCOOR10, -X4(CH2)vCN, -OR13, -CO2R11, -CN, -CONR8aR9a y X4(CH2)vCONR8aR9a; R7b con independencia de su aparicion se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, amino-alquilsulfonilo C1-6, SO2NR11aR11b, haloalcoxi C1-6, haloalquiltio C1-6, halogeno, hidroxi, amino, alquilamino C1-6, di(alquil C1-6)amino, aminoacilo, acilo, CONR8R9, nitro, ciano y heteroalcoxi C1-6; R8 y R9 (i) tomados independientemente, uno de R8 y R9 es H o alquilo C1-6 y el otro de R8 y R9 se elige entre el grupo formado por H, alquilo C1-6, -C(=O)R12, -(CH2)2N[(CH2)2]2X3 o -(CH2)2NR11aR11b; o (ii) R8 y R9 tomados juntos son (CH2)2-X3-(CH2)2 o -(CH2)o- opcionalmente sustituidos por 1 o 2 sustituyentes elegidos entre el grupo formado por halogeno, hidroxilo y NR11aR11b; R8a y R9a (i) tomados independientemente, uno de R8 y R9 es H o alquilo C1-6 y el otro de R8 y R9 se elige entre el grupo formado por H, hidroxialquilo C1-6, -(CH2)vN[(CH2)2]2X3 y -(CH2)vNR11aR11b o, (ii) R8a y R9a junto con el N al que están unidos son pirrolidina, piperidina; dicha pirrolidina o dicha piperidina están opcionalmente sustituidas por un hidroxilo o (iii) R8a y R9a tomados juntos son (CH2)2-X3-(CH2)2; R10 es alquilo C1-6; R11 es H o alquilo C1-6; R11a y R11b con independencia entre sí son R11; R12 es alquilo C1-10, -(CH2)sNHR11aR11b, -(CH2)sOR11, -CH2-CH(OH)CH3, - CH2N[(CH2)2]2O, -(CH2)2CO2R11, fenilo o piridinilo opcionalmente sustituidos; R13 es H o alquilo C1-6; X2 es -O- o un enlace; X3 es -O-, -S(O)n- o NR11; X4 es O-o -S(O)n-; m y n con independencia entre sí son numeros enteros de 0 a 2; o es un numero entero de 4 a 6; p es un numero entero de 0 a 6; s es un numero entero de 1 a 2; v es un numero entero de 1 a 6; y los hidratos, solvatos y las sales farmacéuticamente aceptables de los mismos.
ARP060104513A 2005-10-19 2006-10-17 Inhibidores nnrt basados en fenil-acetamida AR058094A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US72844305P 2005-10-19 2005-10-19

Publications (1)

Publication Number Publication Date
AR058094A1 true AR058094A1 (es) 2008-01-23

Family

ID=37606927

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060104513A AR058094A1 (es) 2005-10-19 2006-10-17 Inhibidores nnrt basados en fenil-acetamida

Country Status (12)

Country Link
US (1) US7388111B2 (es)
EP (1) EP1940781A1 (es)
JP (1) JP2009515826A (es)
KR (1) KR20080056220A (es)
CN (1) CN101291905A (es)
AR (1) AR058094A1 (es)
AU (1) AU2006303368B2 (es)
BR (1) BRPI0617720A2 (es)
CA (1) CA2625047A1 (es)
IL (1) IL190442A0 (es)
TW (1) TW200804244A (es)
WO (1) WO2007045573A1 (es)

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