AR082887A1 - Derivados de piridin-3-il-metil, y composiciones para la inhibicion de nampt - Google Patents
Derivados de piridin-3-il-metil, y composiciones para la inhibicion de namptInfo
- Publication number
- AR082887A1 AR082887A1 ARP110103220A ARP110103220A AR082887A1 AR 082887 A1 AR082887 A1 AR 082887A1 AR P110103220 A ARP110103220 A AR P110103220A AR P110103220 A ARP110103220 A AR P110103220A AR 082887 A1 AR082887 A1 AR 082887A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocycloalkyl
- aryl
- cycloalkyl
- haloalkyl
- Prior art date
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- 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
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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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- 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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Abstract
Reivindicación 1: Compuestos de la fórmula (1) en donde: Ra es 1, 2, 3 ó 4 y pueden seleccionarse del grupo que consiste en hidrógeno, amino, oxo, halo, alcoxi, alquilo, haloalquilo, -N(alquil)2, -NH(CO)O-alquilo, 1H-pirazol, 1H-imidazol, y -C(O)NH2; y en donde dicha piridina puede comprender un N-óxido formado con su miembro N atómico; R1 es -NR3R4 en donde R3 es H, alquilo o -S(O)2alquilo y R4 es alquilo, hidroxialquilo, -S(O)2alquilo, -(CH2)q-cicloalquilo, -(CH2)q-heterocicloalquilo, arilo, arilalquilo-, -(CH2)q-heteroarilo; haloalquilo; cicloalquilo; arilo; heterocicloalquilo; o heteroarilo; en donde cada uno de dicho cicloalquilo, arilo, heterocicloalquilo o heteroarilo no está sustituido o está sustituido con 1, 2, 3, 4 ó 5 sustituyentes que pueden ser iguales o diferentes y se seleccionan en forma independiente del grupo que consiste en: halo, ciano, alquilo, hidroxilo, hidroxialquilo, hidroxialcoxi, haloalquilo, alcoxi, alquilalcoxi, haloalcoxi, arilalquenilo-, ariloxi, benciloxi, oxo, -(CH2)q-NRbRc, -(CH2)q-CONRbRc, -S(O)2-alquilo, -S(O)2NH-alquilo, -S(O)2-heterocicloalquilo, -S(O)2-CF3, -C(O)alquilo, -C(O)arilo, -C(O)alquilenilarilo, -C(O)O-alquilo, -(CH2)q-cicloalquilo, cicloalquilalcoxi-, arilo, arilalquilo-, -(CH2)q-heteroarilo, y -(CH2)q-heterocicloalquilo; en donde cada uno de dicho cicloalquilo, heterocicloalquilo, arilo o heteroarilo puede estar sustituido por uno o más halo, nitro, haloalquilo, haloalcoxi, oxo, ciano, alquilo, haloalquilo, o alcoxi; Rb y Rc se seleccionan en forma independiente del grupo que consiste en H, alquilo, hidroxialquilo, alcoxi, arilo, alcoxialquilo, -S(O)2alquilo y cicloalquilo; o Rb y Rc pueden formar un grupo heterocicloalquilo de 5 o 6 miembros junto con el átomo de nitrógeno al cual están unidos, en donde dicho grupo heterocicloalquilo puede contener uno o más heteroátomo(s) adicional(es) seleccionado(s) de N, S u O; q es 0 ó 1; y sales aceptables desde el punto de vista farmacéutico de los anteriores, con la salvedad de que los compuestos de la fórmula (1) no sean: N-[4-(fenilsulfonil)fenil]-N’-(3-piridinilmetil)urea; N,N-dietil-4-[[[(3-piridinilmetil)amino]carbonil]amino]bencensulfonamida; o 4-[[[(3-piridinilmetil)amino]carbonil]amino]bencensulfonamida.
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US37981910P | 2010-09-03 | 2010-09-03 | |
US37981210P | 2010-09-03 | 2010-09-03 | |
US38603710P | 2010-09-24 | 2010-09-24 | |
US38604410P | 2010-09-24 | 2010-09-24 | |
US201161478995P | 2011-04-26 | 2011-04-26 | |
US201161480423P | 2011-04-29 | 2011-04-29 |
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US (4) | US20130273034A1 (es) |
EP (1) | EP2611777B1 (es) |
JP (2) | JP6038792B2 (es) |
KR (1) | KR20130114653A (es) |
CN (2) | CN103270023B (es) |
AR (1) | AR082887A1 (es) |
AU (1) | AU2011295724B2 (es) |
BR (1) | BR112013004858A8 (es) |
CA (1) | CA2809391A1 (es) |
MX (1) | MX342481B (es) |
RU (2) | RU2016116533A (es) |
TW (1) | TW201217359A (es) |
WO (1) | WO2012031196A1 (es) |
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-
2011
- 2011-09-02 US US13/820,496 patent/US20130273034A1/en not_active Abandoned
- 2011-09-02 RU RU2016116533A patent/RU2016116533A/ru unknown
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- 2011-09-02 MX MX2013002431A patent/MX342481B/es active IP Right Grant
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- 2011-09-02 BR BR112013004858A patent/BR112013004858A8/pt not_active Application Discontinuation
- 2011-09-02 CN CN201180053248.9A patent/CN103270023B/zh not_active Expired - Fee Related
- 2011-09-02 RU RU2013114844A patent/RU2617424C2/ru active IP Right Revival
- 2011-09-02 WO PCT/US2011/050320 patent/WO2012031196A1/en active Application Filing
- 2011-09-02 KR KR1020137008447A patent/KR20130114653A/ko not_active Application Discontinuation
- 2011-09-02 EP EP11758024.1A patent/EP2611777B1/en not_active Not-in-force
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- 2019-05-22 US US16/419,333 patent/US10647695B2/en active Active
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US20180291000A1 (en) | 2018-10-11 |
MX2013002431A (es) | 2013-06-03 |
RU2617424C2 (ru) | 2017-04-25 |
JP2013536868A (ja) | 2013-09-26 |
MX342481B (es) | 2016-09-30 |
RU2016116533A (ru) | 2018-11-30 |
EP2611777A1 (en) | 2013-07-10 |
WO2012031196A9 (en) | 2013-06-13 |
AU2011295724A1 (en) | 2013-05-02 |
EP2611777B1 (en) | 2016-05-11 |
US20190270721A1 (en) | 2019-09-05 |
CN103270023B (zh) | 2016-11-02 |
CN106986856A (zh) | 2017-07-28 |
US10647695B2 (en) | 2020-05-12 |
AU2011295724A8 (en) | 2013-06-20 |
US11279687B2 (en) | 2022-03-22 |
AU2011295724B2 (en) | 2016-05-12 |
RU2016116533A3 (es) | 2018-11-30 |
CA2809391A1 (en) | 2012-03-08 |
US10329275B2 (en) | 2019-06-25 |
BR112013004858A8 (pt) | 2018-01-02 |
CN103270023A (zh) | 2013-08-28 |
JP6038792B2 (ja) | 2016-12-07 |
TW201217359A (en) | 2012-05-01 |
BR112013004858A2 (pt) | 2016-06-07 |
RU2013114844A (ru) | 2014-10-10 |
WO2012031196A1 (en) | 2012-03-08 |
KR20130114653A (ko) | 2013-10-17 |
JP2017019825A (ja) | 2017-01-26 |
US20130273034A1 (en) | 2013-10-17 |
US20200283403A1 (en) | 2020-09-10 |
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