CO6410301A2 - 1 aril -3- aminoalcoxi-pirazoles como ligandos sigma para potenciar ell efecto analgesico de los opioides y atenuar la dependencia de ellos - Google Patents

1 aril -3- aminoalcoxi-pirazoles como ligandos sigma para potenciar ell efecto analgesico de los opioides y atenuar la dependencia de ellos

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Publication number
CO6410301A2
CO6410301A2 CO10148511A CO10148511A CO6410301A2 CO 6410301 A2 CO6410301 A2 CO 6410301A2 CO 10148511 A CO10148511 A CO 10148511A CO 10148511 A CO10148511 A CO 10148511A CO 6410301 A2 CO6410301 A2 CO 6410301A2
Authority
CO
Colombia
Prior art keywords
substituted
group
unsubstituted
sigma
independently selected
Prior art date
Application number
CO10148511A
Other languages
English (en)
Inventor
Jose Miguel Vela-Hernandez
Helmut Heinrich
Daniel Zamanillo-Castanedo
Original Assignee
Esteve Labor Dr
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=39768934&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO6410301(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Esteve Labor Dr filed Critical Esteve Labor Dr
Publication of CO6410301A2 publication Critical patent/CO6410301A2/es

Links

Classifications

    • 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
    • C07D231/14—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 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
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Objeto de la invención: Grupo de ligandos sigma de fórmula (I) para la potenciación del efecto analgésico de los opioides y opiáceos, así como la atenuación de la dependencia inducida por los mismos.Características de la invención: Combinación de al menos un ligando sigma, sal, isómero, profármaco o solvato farmacéuticamente aceptable del mismo, y al menos un compuesto opioide u opiáceo, mediante administración simultánea, separada o secuencial de dicha combinación, donde el ligando sigma presenta la fórmula (I) en la que: R1-R9 se seleccionan independientemente del grupo formado por hidrógeno, alquilo, cicloalquilo, alquenilo, arilo o heterociclilo, sustituidos o no sustituidos (R1 solamente heterociclilo no aromático sustituido o no sustituido); o bien R1-R6 se seleccionan independientemente del grupo formado por arilaquilo, o, heterociclilalquilo, sustituidos o no sustituidos-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 halógeno; o bien R3 y R4 forman juntos un sistema de anillos condensados; o bien R5 y R6 forman junto con el átomo de nitrógeno al que están unidos, un grupo heterociclilo sustituido o no sustituido; o bien R8 y R9 se seleccionan independientemente del grupo formado por alcoxi, o ariloxi, sustituidos o no sustituidos, y halógeno; n se selecciona entre 1, 2, 3, 4, 5, 6, 7 y 8; y t es 1, 2 ó 3.
CO10148511A 2008-04-25 2010-11-25 1 aril -3- aminoalcoxi-pirazoles como ligandos sigma para potenciar ell efecto analgesico de los opioides y atenuar la dependencia de ellos CO6410301A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08380122A EP2116539A1 (en) 2008-04-25 2008-04-25 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof

Publications (1)

Publication Number Publication Date
CO6410301A2 true CO6410301A2 (es) 2012-03-30

Family

ID=39768934

Family Applications (1)

Application Number Title Priority Date Filing Date
CO10148511A CO6410301A2 (es) 2008-04-25 2010-11-25 1 aril -3- aminoalcoxi-pirazoles como ligandos sigma para potenciar ell efecto analgesico de los opioides y atenuar la dependencia de ellos

Country Status (28)

Country Link
US (3) US8877753B2 (es)
EP (3) EP2116539A1 (es)
JP (1) JP5753076B2 (es)
KR (1) KR101764817B1 (es)
CN (1) CN102066334B (es)
AU (1) AU2009239968B2 (es)
BR (1) BRPI0910677A2 (es)
CA (1) CA2722345C (es)
CO (1) CO6410301A2 (es)
CY (1) CY1115848T1 (es)
DK (1) DK2276744T3 (es)
EC (1) ECSP10010634A (es)
ES (1) ES2526360T3 (es)
HK (1) HK1155724A1 (es)
HR (1) HRP20141263T1 (es)
IL (1) IL208865B (es)
MA (1) MA32301B1 (es)
MX (1) MX2010011673A (es)
MY (1) MY160800A (es)
NZ (1) NZ588829A (es)
PL (1) PL2276744T3 (es)
PT (1) PT2276744E (es)
RS (1) RS53717B1 (es)
RU (1) RU2519060C2 (es)
SG (1) SG190578A1 (es)
SI (1) SI2276744T1 (es)
UA (1) UA105900C2 (es)
WO (1) WO2009130310A1 (es)

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EP2335688A1 (en) 2009-11-25 2011-06-22 Laboratorios Del. Dr. Esteve, S.A. Pharmaceutical compositions comprising sigma receptor ligands
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
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EP2426112A1 (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 polymorphs and solvates
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
EP2460519A1 (en) * 2010-12-03 2012-06-06 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in bone cancer pain
EP2524694A1 (en) * 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
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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