AR039008A1 - Derivados azabiciclicos, azatriciclicos y azaespirociclicos de aminociclohexano antagonistas de los receptores nmda, 5-ht3, y nicotinico neuronal - Google Patents

Derivados azabiciclicos, azatriciclicos y azaespirociclicos de aminociclohexano antagonistas de los receptores nmda, 5-ht3, y nicotinico neuronal

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Publication number
AR039008A1
AR039008A1 ARP030100948A ARP030100948A AR039008A1 AR 039008 A1 AR039008 A1 AR 039008A1 AR P030100948 A ARP030100948 A AR P030100948A AR P030100948 A ARP030100948 A AR P030100948A AR 039008 A1 AR039008 A1 AR 039008A1
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Argentina
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branched chain
straight
hydrogen
formula
ring
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ARP030100948A
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English (en)
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Merz Pharma Gmbh & Co Kgaa
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Publication of AR039008A1 publication Critical patent/AR039008A1/es

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Abstract

Derivados azabicíclicos, azatricíclicos y azaespirocíclicos de aminociclohexanos que son sistémicamente activos como antagonistas de los receptores NMDA. 5HT3, y nicotínico, composiciones farmacéuticas que los comprenden, método de preparación de las mismas, y método para tratar trastornos del SNC que incluyen perturbaciones de la transmisión glutamatérgica, serotoninérgica, y nicotínica, tratar trastornos inmunomodulatorios, y antimalaria, antitripanosoma, anti-virus Borna, anti-HSV y actividad anti-virus de Hepatitis C. Reivindicación 1: un compuesto caracterizado porque se selecciona entre aquellos de fórmula (1) donde: R se selecciona entre el grupo que consiste en hidrógeno, alquilo (C1-6) de cadena lineal o ramificada, alquenilo (C2-6) de cadena lineal o ramificada, alquinilo (C2-6) de cadena lineal o ramificada, arilo, arilo sustituido, y arilalquilo; R1 se selecciona entre el grupo que consiste en alquilo (C1-6) de cadena lineal o ramificada, alquenilo (C2-6) de cadena lineal o ramificada, alquinilo (C2-6) de cadena lineal o ramificada, arilo, arilo sustituido, y arilalquilo; R2 hasta R5 se selecciona independientemente entre los grupos que consisten en hidrógeno, alquilo (C1-6) de cadena lineal o ramificada, alquenilo (C2-6) de cadena lineal o ramificada, alquinilo (C2-6) de cadena lineal o ramificada, arilo, arilo sustituido, y arilalquilo; Z es CH2; n = 0 ó 1; Y = CH; y siempre y cuando por lo menos uno de R2 y R3 no sea hidrógeno y por lo menos uno de R4 y R5 no sea hidrógeno; o aquellos compuestos donde R y R1 se combinan para formar un puente alquileno o alquenileno C3-5 de U-V-W-X, que da la estructura que se puede representar por la fórmula (2), donde X = CH2; m = 0, 1, 2; o aquellos compuestos donde R y R1 se combinan para formar un puente alquileno o alquenileno C3-5 de fórmula U-V-W-X, y los miembros N e Y del anillo no se conectan para formar un puente, que da la estructura básica que se puede representar por la fórmula (3) donde el miembro N del anillo es saturado y el miembro Y del anillo es saturado o se puede combinar con R5 para formar una unión carbono-hidrógeno con el carbono del anillo al cual está unido; sus isómeros ópticos y las sales de adición de ácido o base de los mismos que son aceptables para uso farmacéutico
ARP030100948A 2002-03-21 2003-03-18 Derivados azabiciclicos, azatriciclicos y azaespirociclicos de aminociclohexano antagonistas de los receptores nmda, 5-ht3, y nicotinico neuronal AR039008A1 (es)

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AR039008A1 true AR039008A1 (es) 2005-02-02

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US (4) US7022729B2 (es)
EP (1) EP1485086A1 (es)
JP (1) JP4262606B2 (es)
KR (1) KR100741257B1 (es)
CN (1) CN1638762A (es)
AR (1) AR039008A1 (es)
AU (1) AU2003216855B2 (es)
CA (1) CA2474637A1 (es)
CO (1) CO5611104A2 (es)
EA (1) EA007098B1 (es)
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UA (1) UA77778C2 (es)
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EP1765287A2 (en) 2004-06-17 2007-03-28 Merz Pharma GmbH & Co. KGaA Immediate release formulations of memantine oral dosage forms
US20060205822A1 (en) * 2004-12-22 2006-09-14 Forest Laboratories, Inc. 1-Aminocyclohexane derivatives for the treatment of multiple sclerosis, emotional lability and pseudobulbar affect
EP2111858A1 (en) 2008-04-25 2009-10-28 EPFL Ecole Polytechnique Fédérale de Lausanne Novel treatment for alzheimer's disease
US20090275597A1 (en) * 2008-05-02 2009-11-05 Forest Laboratories Holdings Limited Methods of treating cns disorders
CN102918021B (zh) * 2010-05-27 2015-02-11 塔加西普特公司 烟碱受体非竞争性拮抗剂
BR112014010719A2 (pt) * 2011-11-03 2017-05-02 Targacept Inc moduladores não competitivos de receptor nicotínico
US9173878B2 (en) 2012-01-25 2015-11-03 Tohoku University Brain function improving agent
EA029052B1 (ru) 2013-03-14 2018-02-28 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с
AP2017009733A0 (en) 2014-09-12 2017-02-28 Boehringer Ingelheim Int Spirocyclic inhibitors of cathepsin c

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US7022729B2 (en) 2006-04-04
CN1638762A (zh) 2005-07-13
KR20040091005A (ko) 2004-10-27
CO5611104A2 (es) 2006-02-28
UA77778C2 (en) 2007-01-15
GEP20063954B (en) 2006-10-25
CA2474637A1 (en) 2003-10-02
IL164041A0 (en) 2005-12-18
AU2003216855A1 (en) 2003-10-08
US20060019982A1 (en) 2006-01-26
EP1485086A1 (en) 2004-12-15
EA200401230A1 (ru) 2005-02-24
JP2005525385A (ja) 2005-08-25
WO2003080046A1 (en) 2003-10-02
EA007098B1 (ru) 2006-06-30
ZA200406940B (en) 2005-09-22
MXPA04007755A (es) 2004-10-15
AU2003216855B2 (en) 2005-08-18
NO20044481L (no) 2004-10-20
JP4262606B2 (ja) 2009-05-13
US20070185151A1 (en) 2007-08-09
US20060019983A1 (en) 2006-01-26
KR100741257B1 (ko) 2007-07-19
TW200306189A (en) 2003-11-16
PL372701A1 (en) 2005-07-25
US7238703B2 (en) 2007-07-03

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