AR089011A1 - 2h-indazoles como antagonistas del receptor ep₂ - Google Patents

2h-indazoles como antagonistas del receptor ep₂

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Publication number
AR089011A1
AR089011A1 ARP120104465A ARP120104465A AR089011A1 AR 089011 A1 AR089011 A1 AR 089011A1 AR P120104465 A ARP120104465 A AR P120104465A AR P120104465 A ARP120104465 A AR P120104465A AR 089011 A1 AR089011 A1 AR 089011A1
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AR
Argentina
Prior art keywords
alkyl
residue
cycloalkyl
membered
heterocyclyl
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Pending
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ARP120104465A
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English (en)
Inventor
Dra Rotgeri Andrea
Dr Bruer Nico
Dr Ter Laak Antonius
Dr Buchmann Bernd
Dr Lindenthal Bernhard
Dra Rhn Ulrike
Dra Mengel Anne
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Bayer Intellectual Property GmbH
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Bayer Intellectual Property GmbH
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Application filed by Bayer Intellectual Property GmbH filed Critical Bayer Intellectual Property GmbH
Publication of AR089011A1 publication Critical patent/AR089011A1/es
Pending legal-status Critical Current

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    • A61K31/415—1,2-Diazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

La presente se refiere a 2H-indazoles de la fórmula general (1), métodos para su preparación y su uso para la producción de agentes farmacéuticos para el tratamiento de enfermedades e indicaciones que están ligadas con el receptor de EP₂, enfermedades relativas a la biología reproductiva femenina (menorragia, dismenorrea, endometriosis, procesos neurodegenerativos, etc.). Reivindicación 1: Compuestos de la fórmula general (1) en donde R¹: significa H, alquilo C₁₋₂ o alquil C₁₋₂-oxi; R²: es H o metilo; siempre que uno de los dos residuos R¹ o R² sea H; X: es -(CH₂)ₗ-, -(CH₂)ₖ-O-, -CH₂-S-, CH₂-S(O)₂-, -CH(CH₃)-, -CH(CH₃)-O- o -C(CH₃)₂-O-; k: es 1 ó 2; I: es 0, 1 ó 2; R⁴: H, alquilo C₁₋₄, cicloalquilo C₃₋₄ o CH₂-cicloalquilo C₃₋₄; y el caso de que X: -CH₂- o -CH(CH₃)- R⁴: significa adicionalmente un residuo de heterociclilo de 4 - 6 miembros; el caso de que X: -(CH₂)ₗ- o -CH(CH₃)- R⁴: significa adicionalmente CN; o X junto con R⁴ forman un residuo de heterociclilo de 4 - 6 miembros por medio de una ligación de carbono de anillo; m: es 1 ó 2; n: es 1 ó 2; Ar: es un residuo de arilo de 6 - 10 miembros o residuo de hetarilo de 5 - 10 miembros, R³: es halógeno, CN, SF₅, alquilo C₁₋₄, cicloalquilo C₃₋₆, heterociclilo C₄₋₆, O-alquilo C₁₋₄, O-cicloalquilo C₃₋₆, O-heterociclilo C₄₋₆, S-alquilo C₁₋₄, S(O)₂-alquilo C₁₋₄, Ar, O-Ar, C(CH₃)₂-CN o C(CH₃)₂-OH; y Ar: un residuo de arilo de 6 miembros o residuo de heteroarilo de 5 - 6 miembros opcionalmente mono- o disustituido; en donde los sustituyentes están seleccionados de F, Cl, CN, alquilo C₁₋₄, O-alquilo C₁₋₄, C₍CH₃)₂-CN, C(CH₃)₂-OH y C(O)NH₂; y sus isómeros, diastereómeros, enantiómeros y sales o clatratos de ciclodextrina.
ARP120104465A 2011-11-28 2012-11-28 2h-indazoles como antagonistas del receptor ep₂ Pending AR089011A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102011087170 2011-11-28
DE102012206715 2012-04-24

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AR089011A1 true AR089011A1 (es) 2014-07-23

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US (1) US9062041B2 (es)
EP (1) EP2785707B1 (es)
JP (1) JP6192654B2 (es)
KR (1) KR20140103984A (es)
CN (1) CN104144922B (es)
AR (1) AR089011A1 (es)
AU (1) AU2012344015A1 (es)
BR (1) BR112014012459A2 (es)
CA (1) CA2856769A1 (es)
CL (1) CL2014001392A1 (es)
CO (1) CO6970595A2 (es)
CR (1) CR20140257A (es)
DO (1) DOP2014000114A (es)
EA (1) EA201400623A1 (es)
EC (1) ECSP14002542A (es)
ES (1) ES2665510T3 (es)
HK (1) HK1203938A1 (es)
IL (1) IL232503A (es)
IN (1) IN2014CN03854A (es)
MX (1) MX2014006433A (es)
PE (1) PE20141579A1 (es)
PH (1) PH12014501195A1 (es)
SG (1) SG11201402269RA (es)
TW (1) TW201326154A (es)
WO (1) WO2013079425A1 (es)

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EP2755944B1 (en) 2011-09-16 2017-06-14 Sanofi Biarylderivatives,their preparation and their therapeutic application
TW201326154A (zh) 2011-11-28 2013-07-01 拜耳知識產權公司 作為ｅｐ２受體拮抗劑之新穎２ｈ－吲唑
WO2014187744A1 (de) * 2013-05-23 2014-11-27 Bayer Pharma Aktiengesellschaft Pharmazeutische zusammensetzung und deren verwendung sowie anwendungsregime dieser pharmazeutischen zusammensetzung zur bedarfsweisen („on-demand") kontrazeption
WO2014187793A1 (de) * 2013-05-23 2014-11-27 Bayer Pharma Aktiengesellschaft Verwendung einer pharmazeutischen zusammensetzung zur notfallkontrazeption
EP3151820A4 (en) 2014-06-06 2017-11-22 Flexus Biosciences, Inc. Immunoregulatory agents
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
EA201790806A1 (ru) 2014-11-05 2017-11-30 Флексус Байосайенсиз, Инк. Иммунорегулирующие средства
AR102537A1 (es) 2014-11-05 2017-03-08 Flexus Biosciences Inc Agentes inmunomoduladores
JP2022506850A (ja) 2018-11-08 2022-01-17 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド 化学化合物
WO2022138792A1 (ja) * 2020-12-24 2022-06-30 小野薬品工業株式会社 Ｅｐ２拮抗活性を有する化合物の塩、溶媒和物および結晶

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