AR079199A1 - Composiciones farmaceuticas que comprenden ligandos de receptores sigma - Google Patents

Composiciones farmaceuticas que comprenden ligandos de receptores sigma

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Publication number
AR079199A1
AR079199A1 ARP100104369A ARP100104369A AR079199A1 AR 079199 A1 AR079199 A1 AR 079199A1 AR P100104369 A ARP100104369 A AR P100104369A AR P100104369 A ARP100104369 A AR P100104369A AR 079199 A1 AR079199 A1 AR 079199A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
nr8r9
group
heterocyclyl
Prior art date
Application number
ARP100104369A
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English (en)
Inventor
Sune Nuria Cubel
Ranzani Luis Soler
Pierandrea Esposito
Pujals Gemma Casadevall
Original Assignee
Esteve Labor Dr
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Publication date
Application filed by Esteve Labor Dr filed Critical Esteve Labor Dr
Publication of AR079199A1 publication Critical patent/AR079199A1/es

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
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Abstract

Reivindicacion 1: Composicion farmacéutica que comprende (i) un compuesto de formula (1) como principio activo farmacéutico en la que R1 se selecciona del grupo que consiste en hidrogeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo no aromático sustituido o no sustituido, heterociclilo aromático sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR8, -C(O)OR8, -C(O)NR8R9, -CH=NR8, -CN, -OR8, -OC(O)R8, -S(O)t-R8, -NR8R9, -NR8C(O)R9, -NO2, -N=CR8R9 y halogeno; R2 se selecciona del grupo que consiste en hidrogeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR8, -C(O)OR8,-C(O)NR8R9, -CH=NR8, -CN, -OR8, -OC(O)R9, -S(O)t-R8, -NR8R9, -NR8C(O)R9, -NO2, -N=CR8R9 y halogeno; R3 y R4 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR8, -C(O)OR8, -C(O)NR8R9, -CH=NR8, -CN, -OR8, -OC(O)R8, -S(O)t-R8, -NR8R9, -NR8C (O)R9, -NO2, -N=CR8R9 y halogeno, o juntos forman, con el grupo fenilo al que están unidos, un grupo arilo sustituido o no sustituido condensado o un grupo heterociclilo sustituido o no sustituido condensado; R5 y R6 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -COR8, -C(O)OR8, -C(O)NR8R9, -CH=NR8, -CN, OR8, -OC(O)R8, -S(O)t-R8, -NR8R9, -NR8C(O)R9, -NO2, -N=CR8R9 y halogeno; o juntos forman, con el átomo de nitrogeno al que están unidos, un grupo heterociclilo sustituido o no sustituido; n es 1, 2, 3, 4, 5, 6, 7 u 8; t es 1,2 o 3; R8 y R9 se selecciona cada uno independientemente del grupo que consiste en hidrogeno, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, arilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, alcoxilo sustituido o no sustituido, ariloxilo sustituido o no sustituido y halogeno; o un solvato, un profármaco, un isomero o una sal farmacéuticamente aceptable del mismo; y (ii) al menos un excipiente farmacéuticamente aceptable, en la que el principio activo farmacéutico está presente en una cantidad de al menos el 80% del peso seco total de la composicion. Reivindicacion 11: Composicion farmacéutica segun cualquier reivindicacion anterior, en la que el principio activo farmacéutico (i) es 4-{2-[5-metil-1-(naftalen-2-il)-1H-pirazol-3-iloxi]etil}morfolina o una sal farmacéuticamente aceptable preferiblemente la sal clorhidrato, o un solvato o un profármaco del mismo.
ARP100104369A 2009-11-25 2010-11-25 Composiciones farmaceuticas que comprenden ligandos de receptores sigma AR079199A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09382261A EP2335688A1 (en) 2009-11-25 2009-11-25 Pharmaceutical compositions comprising sigma receptor ligands

Publications (1)

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AR079199A1 true AR079199A1 (es) 2012-01-04

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US (1) US9241927B2 (es)
EP (2) EP2335688A1 (es)
JP (1) JP5827236B2 (es)
KR (1) KR101794579B1 (es)
CN (2) CN102711736A (es)
AR (1) AR079199A1 (es)
AU (1) AU2010323097B2 (es)
BR (1) BR112012012457A2 (es)
CA (1) CA2781726C (es)
CO (1) CO6501134A2 (es)
CY (1) CY1119357T1 (es)
DK (1) DK2503994T3 (es)
EC (1) ECSP12011958A (es)
ES (1) ES2641637T3 (es)
HR (1) HRP20171448T1 (es)
HU (1) HUE036377T2 (es)
IL (1) IL219996A (es)
LT (1) LT2503994T (es)
MA (1) MA33836B1 (es)
ME (1) ME02876B (es)
MX (1) MX351570B (es)
NZ (1) NZ600231A (es)
PL (2) PL2503993T3 (es)
PT (1) PT2503994T (es)
RS (1) RS56382B1 (es)
RU (1) RU2549882C2 (es)
SG (1) SG10201407504YA (es)
SI (1) SI2503994T1 (es)
TN (1) TN2012000246A1 (es)
TW (1) TWI526207B (es)
UA (2) UA109421C2 (es)
WO (1) WO2011064296A1 (es)
ZA (1) ZA201203774B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
RS55099B1 (sr) * 2009-11-25 2016-12-30 Esteve Labor Dr Hirohloridna so 4-[2-[[5-metil-1-(2-naftalenil)-1h-pirazol-3-il]oksi]etil]morfolina
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2426111A1 (en) * 2010-08-09 2012-03-07 Laboratorios Del. Dr. Esteve, S.A. 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
HUE051406T2 (hu) 2012-11-14 2021-03-01 Grace W R & Co Biológiailag aktív anyagot és rendezetlen szervetlen oxidot tartalmazó kompozíciók
EP2792352A1 (en) 2013-04-16 2014-10-22 Laboratorios Del. Dr. Esteve, S.A. Alpha-2 adrenoreceptor and sigma receptor ligand combinations
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