AR088663A1 - Derivados de [1,2,3]triazolo[4,5-d]pirimidina agonistas de receptores canabinoides - Google Patents

Derivados de [1,2,3]triazolo[4,5-d]pirimidina agonistas de receptores canabinoides

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Publication number
AR088663A1
AR088663A1 ARP120104159A ARP120104159A AR088663A1 AR 088663 A1 AR088663 A1 AR 088663A1 AR P120104159 A ARP120104159 A AR P120104159A AR P120104159 A ARP120104159 A AR P120104159A AR 088663 A1 AR088663 A1 AR 088663A1
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AR
Argentina
Prior art keywords
alkyl
heterocyclyl
cycloalkylalkyl
oxa
haloalkyl
Prior art date
Application number
ARP120104159A
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English (en)
Inventor
Nettekoven Matthias
Rogers-Evans Mark
Bissantz Caterina
Grether Uwe
Kimbara Atsushi
Adam Jean
Michel-Roever Stephan
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Hoffmann La Roche
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Publication of AR088663A1 publication Critical patent/AR088663A1/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1) en la que: A es alquilo, hidroxialquilo, -CH₂C(O)-, -C(O)-, -SO₂- o está ausente; R¹ es hidrógeno, alquilo, haloalquilo, hidroxilo, alcoxi, haloalcoxi, fenilo, halofenilo, alcoxifenilo, haloalquilfenilo, haloalcoxifenilo, (halo)(haloalquil)fenilo, cianofenilo, hidroxialcoxifenilo, alquilsulfonilfenilo, alquilsulfonilaminofenilo, ciano, cicloalquilo, cicloalquilalcoxi, amino, (alquilsulfonil)(alquil)[1,2,4]tri-azolilo, (halo)(dialquilamino)piridinilo, (alquil)(oxi)piridinilo, nitro-benzo[1,2,5]oxadiazolilaminopiridinilo, heterociclilo, alquilheterociclilo, hidroxiheterociclilo, alquilheterociclilo, heteroarilo, haloheteroarilo, alquilheteroarilo, cicloalquilheteroarilo o haloalquilheteroarilo, dicho heterociclilo es un anillo carbocíclico de tres a ocho miembros que contiene por lo menos un átomo de nitrógeno o de oxígeno, y dicho heteroarilo es piridinilo, pirazolilo, oxadiazolilo, furazanilo, tetrazolilo o triazolilo; R² es halógeno, -NR³R⁴ o -OR⁵; uno de R³ y R⁴ es hidrógeno o alquilo y el otro es alquilo o cicloalquilo; o R³ y R⁴ junto con el átomo de nitrógeno al que están unidos forman un heterociclilo o heterociclilo sustituido, dicho heterociclilo es morfolinilo, piperidinilo, piperazinilo, pirrolidinilo, 2-oxa-6-azaespiro[3.3]heptilo, azetidinilo, tiazolidinilo, tiomorfolinilo, dioxotiomorfolinilo, oxazepanilo, 2-oxa-6-azaespiro[3.4]octilo, 6-oxa-1-azaespiro[3.3]heptilo, 2-oxa-5-azaespiro[3.4]-octilo, isoxazolidinilo, aziridinilo, dioxoisotiazolidinilo o oxopirrolidinilo y dicho heterociclilo sustituido es un heterociclilo sustituido de una a cuatro veces por sustituyentes elegidos con independencia entre alquilo, halógeno, hidroxilo, alcoxi, hidroxialquilo, carboxilo, alcoxialquilo, ciano, alquilamino, dialquilamino, alquilcarbonilamino, alquilcarbonil(alquilamino), fenilo, alcoxicarbonilo, aminoalquilo, alquilpirazolilo y alquilisoxazolilo; R⁵ es alquilo, cicloalquilo, cicloalquilalquilo, haloalquilo u oxetanilo; o una sal o un éster farmacéuticamente aceptable del mismo; con la condición de que se excluyan la 3-[(2-clorofenil)-metil]-5-(1,1-dimetiletil)-7-(4-morfolinil)-3H-1,2,3-tri-azolo[4,5-d]pirimidina y la N-ciclopropil-5-(1,1-dimetil-etil)-3-(fenilmetil)-3H-1,2,3-triazolo[4,5-d]pirimidina-7-amina.
ARP120104159A 2011-11-08 2012-11-06 Derivados de [1,2,3]triazolo[4,5-d]pirimidina agonistas de receptores canabinoides AR088663A1 (es)

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EP11188333 2011-11-08

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AR088663A1 true AR088663A1 (es) 2014-06-25

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US (2) US8741906B2 (es)
EP (1) EP2776442B1 (es)
JP (1) JP6138141B2 (es)
KR (1) KR102032337B1 (es)
CN (1) CN103930426B (es)
AR (1) AR088663A1 (es)
AU (1) AU2012334173B2 (es)
BR (1) BR112014011055B1 (es)
CA (1) CA2850458C (es)
CL (1) CL2014001174A1 (es)
CO (1) CO6920295A2 (es)
CY (1) CY1117147T1 (es)
DK (1) DK2776442T3 (es)
EA (1) EA023581B1 (es)
ES (1) ES2553704T3 (es)
HK (1) HK1194732A1 (es)
HR (1) HRP20160052T1 (es)
HU (1) HUE025543T2 (es)
IL (1) IL231949A (es)
MX (1) MX342309B (es)
MY (1) MY170878A (es)
PE (1) PE20141588A1 (es)
PL (1) PL2776442T3 (es)
PT (1) PT2776442E (es)
RS (1) RS54436B1 (es)
SG (1) SG11201402197UA (es)
SI (1) SI2776442T1 (es)
TW (2) TWI639600B (es)
UA (1) UA111640C2 (es)
WO (1) WO2013068306A1 (es)
ZA (1) ZA201402905B (es)

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MX2022012260A (es) 2020-03-31 2022-11-30 Nuevolution As Compuestos activos frente a receptores nucleares.
MX2022012259A (es) 2020-03-31 2022-12-08 Nuevolution As Compuestos activos frente a receptores nucleares.
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