AR097794A1 - Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b - Google Patents
Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2bInfo
- Publication number
- AR097794A1 AR097794A1 ARP140103584A ARP140103584A AR097794A1 AR 097794 A1 AR097794 A1 AR 097794A1 AR P140103584 A ARP140103584 A AR P140103584A AR P140103584 A ARP140103584 A AR P140103584A AR 097794 A1 AR097794 A1 AR 097794A1
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- AR
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- Prior art keywords
- alkyl
- group
- alkylene
- optionally substituted
- substituents
- Prior art date
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- 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
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- 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
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- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
Se describen compuestos que modulan selectivamente de forma negativa los receptores de NMDA que contienen una subunidad NR1/NR2B, composiciones farmacéuticas que comprenden los compuestos y métodos para tratar una enfermedad usando los compuestos. Estos compuestos pueden utilizarse como terapia para mejorar la transmisión sináptica cerebral. Reivindicación 1: Un compuesto de la fórmula (1) o sal, profármaco, solvato, hidrato, tautómero o estereoisómero farmacéuticamente aceptable de este, donde: L¹ es alquilo C₂₋₄ lineal o ramificado opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, D, OR¹⁰, NH₂, NHR¹⁰ y N(R¹⁰)(R¹⁰), con la condición de que no más de un oxígeno o nitrógeno se una a ningún carbono, o L¹ se selecciona del grupo que consiste en -CO-alquilenil C₁₋₂-, -S(O)₂-, -S(O)₂NH-, -C(O)NH-, -C(O)NR¹⁰-, -alquilenil C₁₋₃-C(O)-alquilenil C₁₋₃-, y un enlace, donde el alquilenil C₁₋₂ o alquilenil C₁₋₃ se sustituye opcionalmente con alquilo C₁₋₄; cada R¹⁰ Y R¹⁰ se selecciona independientemente del grupo que consiste en H; O-alquil C₁₋₅; alquilo C₁₋₆ opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, O-alquil C₁₋₅, -OP(O)(OH)₂, OP(O)O₂⁻²M₂, -OC(O)alquilo, -OC(O)O-alquilo, arilo y heteroarilo; y cicloalquilo opcionalmente sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste en OH y O-alquil C₁₋₅; con la condición de que no más de un oxígeno se una a ningún carbono de R¹⁰ y R¹⁰; M es un catión metálico monovalente; o R¹⁰ y R¹⁰, junto con el nitrógeno al cual están unidos, pueden formar un heterociclo; R¹ es arilo o heteroarilo, los cuales se sustituyen opcionalmente con uno o más sustituyentes que se seleccionan del grupo que consiste en OH, CN, halógeno, -O-R¹⁰, -OP(O)(OH)₂, OP(O)O₂⁻²M₂, -SH, -S-R¹⁰, alquilo C₁₋₅, alquilo ramificado, -haloalquil C₁₋₆, NH₂, NHR¹⁰, -hidroxialquil C₁₋₆, N(R¹⁰)(NR¹⁰), -NHS(O)₂R¹⁰, -O-alquilarilo, -O-(CH₂)ₙ-C(O)-arilo y NHCOR¹⁰; M es un catión metálico monovalente, o R¹ es cicloalquilo; X se selecciona del grupo que consiste en H, halógeno, OH, O-alquil C₁₋₆, O-alquilo ramificado, alquilo C₁₋₅ lineal y alquilo C₁₋₅ ramificado; Y e Y son independientemente H, F o metilo; L² es -(CH₂)ₙ- o -(CHR¹¹)ₙ-, o un enlace; cada R¹¹ se selecciona independientemente del grupo que consiste en H, -alquilenil C₁₋₅-, -C(O)-alquilenil C₁₋₅- y -alquilenil-CO-alquilenil-; R² es cicloalquil C₃₋₈; heterociclil C₃₋₈, fenilo, naftilo, heteroarilo o heteroarilo bicíclico, cada uno de los cuales se sustituye opcionalmente con uno o más sustituyentes que se seleccionan del grupo que consiste en halógeno, OH, alquil C₁₋₆, OR¹⁰, CN, NH₂, NHR¹⁰, N(R¹⁰)(R¹⁰), SH, SR¹⁰, SOR¹⁰, SO₂R¹⁰, SO₂NHR¹⁰, SO₂N(R¹⁰)(R¹⁰), CONH₂, CONR¹⁰ y CON(R¹⁰)(R¹⁰); y n es 1, 2 ó 3.
Applications Claiming Priority (1)
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US201361883050P | 2013-09-26 | 2013-09-26 |
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AR097794A1 true AR097794A1 (es) | 2016-04-13 |
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ARP140103584A AR097794A1 (es) | 2013-09-26 | 2014-09-26 | Moduladores octahidro-ciclopenta[c]pirrol negativos de nr2b |
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JP (1) | JP6546596B2 (es) |
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AR (1) | AR097794A1 (es) |
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TW (1) | TW201605791A (es) |
UY (1) | UY35750A (es) |
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EP3461827B1 (en) | 2013-09-26 | 2022-02-23 | Cadent Therapeutics, Inc. | Selective octahydro-cyclopenta[c]pyrrole negative modulators of nr2b |
JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
DK3331886T3 (da) | 2015-08-05 | 2020-08-24 | Indivior Uk Ltd | Dopamin-d3-receptorantagonister med en bicyclo-del |
WO2018232158A1 (en) * | 2017-06-15 | 2018-12-20 | Belite Bio, Inc. | Methods of treating metabolic diseases with fused bicyclic pyrroles |
WO2020142662A1 (en) | 2019-01-03 | 2020-07-09 | Avive Solutions, Inc. | Defibrillator communications architecture |
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2014
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- 2014-09-26 EP EP14849302.6A patent/EP3036221B1/en active Active
- 2014-09-26 ES ES14849302T patent/ES2707739T3/es active Active
- 2014-09-26 AR ARP140103584A patent/AR097794A1/es unknown
- 2014-09-26 CN CN201480058773.3A patent/CN105916843B/zh active Active
- 2014-09-26 WO PCT/US2014/057800 patent/WO2015048507A1/en active Application Filing
- 2014-09-26 TW TW103133682A patent/TW201605791A/zh unknown
- 2014-09-26 US US14/498,462 patent/US9540324B2/en active Active
- 2014-09-26 UY UY0001035750A patent/UY35750A/es not_active Application Discontinuation
- 2014-09-26 ES ES18202051T patent/ES2910848T3/es active Active
- 2014-09-26 JP JP2016545243A patent/JP6546596B2/ja active Active
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2016
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EP3461827A1 (en) | 2019-04-03 |
JP6546596B2 (ja) | 2019-07-17 |
ES2910848T3 (es) | 2022-05-13 |
US9540324B2 (en) | 2017-01-10 |
US11116749B2 (en) | 2021-09-14 |
ES2707739T3 (es) | 2019-04-04 |
EP3036221A1 (en) | 2016-06-29 |
EP3461827B1 (en) | 2022-02-23 |
CN105916843A (zh) | 2016-08-31 |
UY35750A (es) | 2015-04-30 |
US20170071906A1 (en) | 2017-03-16 |
CN105916843B (zh) | 2019-09-20 |
US10052306B2 (en) | 2018-08-21 |
JP2016536348A (ja) | 2016-11-24 |
EP3036221A4 (en) | 2017-01-25 |
TW201605791A (zh) | 2016-02-16 |
US20230012073A1 (en) | 2023-01-12 |
EP3036221B1 (en) | 2018-11-07 |
WO2015048507A1 (en) | 2015-04-02 |
US20180325868A1 (en) | 2018-11-15 |
US20150225342A1 (en) | 2015-08-13 |
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