AR083543A1 - Diamidas de amino-pirrolidin-azetidinas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar dolores inflamatorios - Google Patents

Diamidas de amino-pirrolidin-azetidinas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar dolores inflamatorios

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Publication number
AR083543A1
AR083543A1 ARP110103928A ARP110103928A AR083543A1 AR 083543 A1 AR083543 A1 AR 083543A1 AR P110103928 A ARP110103928 A AR P110103928A AR P110103928 A ARP110103928 A AR P110103928A AR 083543 A1 AR083543 A1 AR 083543A1
Authority
AR
Argentina
Prior art keywords
group
phenyl
substituted
fluoro
alkyl
Prior art date
Application number
ARP110103928A
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English (en)
Original Assignee
Janssen Pharmaceutica Nv
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Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR083543A1 publication Critical patent/AR083543A1/es

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    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Reivindicación 1: Un compuesto de fórmula (1) en donde Y es un heteroarilo o arilo C6-10 seleccionado del grupo que consiste en tiazolilo, tienilo, isotiazolilo, pirrolilo, benzofuranilo y benzotienilo; en donde Y es no sustituido o se sustituye con uno o más sustituyentes seleccionados independientemente del grupo que consiste en fluoro, cloro, alquilo C1-4, alcoxi C1-4, ciano y trifluorometilo; Z es i) arilo C6-10; ii) 9H-fluorenilo; iii) fenil(Ra)-fenilo, en donde el anillo de fenilo en el fenil(Ra) es no sustituido o se sustituye con un sustituyente seleccionado del grupo que consiste en trifluorometilo, cloro, alquilo C1-4, y fluoro; Ra es CH(F), CF2, o CH(OH); iv) un heterociclilo fusionado en benzo, seleccionado del grupo que consiste en 1,2,3,4-tetrahidroisoquinolinilo, isoindolinilo, indolinilo e indazolinilo; en donde el heterociclilo fusionado en benzo es no sustituido o se sustituye con un sustituyente que es fenilo o bromo, en donde el fenilo es no sustituido o se sustituye con un sustituyente seleccionado del grupo que consiste en bromo, cloro, fluoro, yodo, alquilo C1-4, alquenilo C2-4, alcoxi C1-4, trifluorometilo y trifluorometoxi; o v) un heteroarilo seleccionado del grupo que consiste en tiazolilo, benzotienilo, benzofuranilo, benzotiazolilo, quinazolinilo, indolilo e indazolilo; en donde el arilo C6-10 y el heteroarilo de Z no son sustituidos o se sustituyen con uno o dos sustituyentes, cada uno de los cuales se seleccionan del grupo que consiste en bromo, cloro, fluoro, yodo, alquilo C1-4, alquenilo C2-4, alcoxi C1-4, trifluorometilo, trifluorometoxi, y Rb; siempre que no más de un sustituyente sea Rb; y Rb se selecciona del grupo que consiste en 2,2-difluoroetilo; fenilmetilo; cicloalquilo C3-6; N-metil-N-fenilaminocarbonil-metilo tienilo; piridinilo; pirimidinilo; y fenilo; en donde la porción fenilo de fenilmetilo, y el tienilo, piridinilo, pirimidinilo, y fenilo de Rb no son sustituidos o se sustituyen con uno o dos sustituyentes, cada uno de los cuales se seleccionan independientemente del grupo que consiste en trifluorometilo, trifluorometoxi, alquilo C1-4, cloro y fluoro; R1 es hidrógeno, fluoro, hidroxi o metoxi; R2 es hidrógeno, alquilo C1-6, hidroxi, formilo, o acetilo; y enantiómeros, diastereómeros, solvatos y sales farmacéuticamente aceptables de estos.
ARP110103928A 2010-10-22 2011-10-24 Diamidas de amino-pirrolidin-azetidinas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar dolores inflamatorios AR083543A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40598410P 2010-10-22 2010-10-22

Publications (1)

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AR083543A1 true AR083543A1 (es) 2013-03-06

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ARP110103928A AR083543A1 (es) 2010-10-22 2011-10-24 Diamidas de amino-pirrolidin-azetidinas, composiciones farmaceuticas que las contienen y uso de las mismas para tratar dolores inflamatorios

Country Status (13)

Country Link
US (2) US8575363B2 (es)
EP (1) EP2630139A1 (es)
JP (1) JP2013540160A (es)
KR (1) KR20130140020A (es)
CN (1) CN103261189B (es)
AR (1) AR083543A1 (es)
AU (1) AU2011316975A1 (es)
BR (1) BR112013009828A2 (es)
CA (1) CA2815353A1 (es)
IL (1) IL225815A0 (es)
RU (1) RU2013123274A (es)
TW (1) TW201305137A (es)
WO (1) WO2012054721A1 (es)

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Publication number Publication date
TW201305137A (zh) 2013-02-01
IL225815A0 (en) 2013-06-27
RU2013123274A (ru) 2014-11-27
CN103261189A (zh) 2013-08-21
JP2013540160A (ja) 2013-10-31
BR112013009828A2 (pt) 2016-07-26
WO2012054721A8 (en) 2013-05-16
CA2815353A1 (en) 2012-04-26
KR20130140020A (ko) 2013-12-23
US20120101081A1 (en) 2012-04-26
CN103261189B (zh) 2015-01-28
US20130196970A1 (en) 2013-08-01
US8575363B2 (en) 2013-11-05
EP2630139A1 (en) 2013-08-28
AU2011316975A1 (en) 2013-05-23
WO2012054721A1 (en) 2012-04-26
US8748417B2 (en) 2014-06-10

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