AR061943A1 - Inhibidores no nucleosidos de la transcriptasa inversa - Google Patents

Inhibidores no nucleosidos de la transcriptasa inversa

Info

Publication number
AR061943A1
AR061943A1 ARP070103236A ARP070103236A AR061943A1 AR 061943 A1 AR061943 A1 AR 061943A1 AR P070103236 A ARP070103236 A AR P070103236A AR P070103236 A ARP070103236 A AR P070103236A AR 061943 A1 AR061943 A1 AR 061943A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
azetidine
pyrrolidine
piperidine
Prior art date
Application number
ARP070103236A
Other languages
English (en)
Inventor
Zachary Kevin Sweeney
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR061943A1 publication Critical patent/AR061943A1/es

Links

Classifications

    • 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
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • 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
    • C07C311/30—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
    • 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
    • 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
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/51—Y being a hydrogen or a carbon atom
    • 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members

Landscapes

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

Abstract

Reivindicacion 1: Un compuesto de la formula (1) en la que: R1 es fluor o hidrogeno; R2 es hidrogeno, cloro, bromo, alquilo C1-3, cicloalquilo C3-5 o alcoxi C1-3; X1 es O o S; X2 es cloro, bromo, ciano, alcoxi C1-3, cicloalquilo C3-5 o haloalquilo C1-3, R3 se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-3, alcoxi C1-6, haloalcoxi C1-6, cicloalquilo C3-5, halogeno y ciano; R4 es SONHR5aR6a, COX4, -CsCC(Me)2R8, o de los restos de formulas (2) o (3); X4 es OH o NR5bR6b; R5a y R6a (i) tomados con independencia, uno de R5a y R6a es hidrogeno o alquilo C1-6 y el otro R5a y R6a se elige entre el grupo formado por hidrogeno, alquilo C1-6 y -C(=O)R7; o (ii) tomados junto con el átomo de nitrogeno al que están unidos forman un anillo de azetidina, pirrolidina, piperidina o azepina, dicho anillo de azetidina, pirrolidina, piperidina o azepina está opcionalmente sustituido por hidroxi, amino, (alquil C1-3-amina o dialquil C1-3-amina; o (iii) tomados juntos son (CH2)2-X3- (CH2)2; R5b y R6b (i) se elige con independencia entre el grupo formado por hidrogeno, alquilo C1-6, hidroxialquilo C1-6, carboxi-alquilo C1-6, (CH2)rNR5cR6c en el que r es un numero de 2 a 6, y SO2-alquilo C1-6, (ii) tomados junto con el átomo de nitrogeno al que están unidos forman un anillo de azetidina, pirrolidina, piperidina o azepina, dicho anillo de azetidina, pirrolidina, piperidina o azepina está opcionalmente sustituido por hidroxi, amino, alquil C1-3-amina o dialquil C1-3-amina; o, (iii) tomados juntos son (CH2)2X3(CH2)2; R5cy R6c (i) se eligen con independencia entre el grupo formado por hidrogeno y alquilo C1-6, (ii) junto con el átomo de nitrogeno al que están unidos forman un anillo de azetidina, pirrolidina, piperidina o azepina, dicho anillo de azetidina, pirrolidina, piperidina o azepina está opcionalmente sustituido por hidroxi, amino, alquil C1-3-amina o dialquil C1-3-amina, o (iii) tomados juntos son (CH2)2X3(CH2)2; R5d y R6d son con independencia de su aparicion hidrogeno, alquilo C1-6, hidroxialquilo C1-6 o carboxi-alquilo C1-6; X3 es O, S(O)p o NR10; R7 es hidrogeno o alquilo C1-6; R8 es OH, NR5dR6d, CO2H, CONR5dR5d o C(=O)NR9aC(=NR9b)NR9cR9d; R9a, R9b, R9c y R9d son (i) con independencia hidrogeno o alquilo C1-6 o (ii) R9a y R9b son con independencia hidrogeno o alquilo C1-6 y R9b y R9c juntos son alquileno C2-4; R10 es hidrogeno, alquilo C1-6 o acilo C1-6; p es un numero de 0 a 2; y sus sales farmacéuticamente aceptables.
ARP070103236A 2006-07-21 2007-07-20 Inhibidores no nucleosidos de la transcriptasa inversa AR061943A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US83248206P 2006-07-21 2006-07-21

Publications (1)

Publication Number Publication Date
AR061943A1 true AR061943A1 (es) 2008-10-01

Family

ID=38521766

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103236A AR061943A1 (es) 2006-07-21 2007-07-20 Inhibidores no nucleosidos de la transcriptasa inversa

Country Status (16)

Country Link
US (1) US20080020981A1 (es)
EP (1) EP2046731A1 (es)
JP (1) JP2009544645A (es)
KR (1) KR20090031584A (es)
CN (1) CN101484418A (es)
AR (1) AR061943A1 (es)
AU (1) AU2007276180A1 (es)
BR (1) BRPI0714509A2 (es)
CA (1) CA2657723A1 (es)
CL (1) CL2007002105A1 (es)
IL (1) IL196144A0 (es)
MX (1) MX2009000574A (es)
PE (1) PE20080558A1 (es)
TW (1) TW200812942A (es)
WO (1) WO2008009613A1 (es)
ZA (1) ZA200900071B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0617720A2 (pt) * 2005-10-19 2011-08-02 Hoffmann La Roche compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém
CN101784529A (zh) * 2007-06-22 2010-07-21 弗·哈夫曼-拉罗切有限公司 作为非核苷逆转录酶抑制剂的脲和氨基甲酸酯衍生物
CN102229547A (zh) * 2011-04-20 2011-11-02 复旦大学 一种萘苯醚类苯磺酰胺衍生物及其制备方法和用途
CN102206177A (zh) * 2011-04-20 2011-10-05 复旦大学 1-萘基苯甲酮衍生物及其制备方法和用途
ES2895773T3 (es) * 2016-05-12 2022-02-22 Res Triangle Inst Fenetilaminas vinílogas como liberadores de neurotransmisores

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003095463A1 (en) * 2002-05-07 2003-11-20 Akzo Nobel N.V. Neopentylglycol bis (diarylphosphate) esters
TW200423930A (en) * 2003-02-18 2004-11-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitors
BRPI0408704A (pt) * 2003-03-24 2006-03-07 Hoffmann La Roche benzil-piridazinonas como inibidores de transcriptase reversa
TW200505441A (en) * 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
US7220772B2 (en) * 2003-09-05 2007-05-22 Pfizer, Inc. Pyrazole derivatives
WO2005090317A1 (en) * 2004-03-23 2005-09-29 F.Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
US7625949B2 (en) * 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
MX2007000788A (es) * 2004-07-27 2007-03-23 Hoffmann La Roche Compuestos de benciltriazolona como inhibidores no nucleosidos de transcriptasa inversa.
CA2577144C (en) * 2004-09-30 2011-06-21 Boehringer Ingelheim International Gmbh Alkynyl compounds as non-nucleoside reverse transcriptase inhibitors
JP2008525419A (ja) * 2004-12-22 2008-07-17 ファイザー・リミテッド Ｈｉｖ−１逆転写酵素の非ヌクレオシド阻害剤
CN101180280A (zh) * 2005-03-24 2008-05-14 弗·哈夫曼-拉罗切有限公司 作为杂环逆转录酶抑制剂的1,2,4-三唑-5-酮化合物
AR057455A1 (es) * 2005-07-22 2007-12-05 Merck & Co Inc Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
ES2317584T3 (es) * 2005-09-30 2009-04-16 F. Hoffmann-La Roche Ag Inhibidores de nnrt.
BRPI0617720A2 (pt) * 2005-10-19 2011-08-02 Hoffmann La Roche compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém
EP1940782B1 (en) * 2005-10-19 2009-03-11 F.Hoffmann-La Roche Ag N-phenyl phenylacetamide non-nucleoside reverse transcriptase inhibitors

Also Published As

Publication number Publication date
BRPI0714509A2 (pt) 2014-04-08
CA2657723A1 (en) 2008-01-24
WO2008009613A1 (en) 2008-01-24
CN101484418A (zh) 2009-07-15
KR20090031584A (ko) 2009-03-26
EP2046731A1 (en) 2009-04-15
TW200812942A (en) 2008-03-16
PE20080558A1 (es) 2008-05-16
JP2009544645A (ja) 2009-12-17
AU2007276180A1 (en) 2008-01-24
CL2007002105A1 (es) 2008-02-22
MX2009000574A (es) 2009-01-27
US20080020981A1 (en) 2008-01-24
ZA200900071B (en) 2010-01-27
IL196144A0 (en) 2009-09-22

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