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1. 发明专利

AT451373T 未知
公开(公告)号：AT451373T
公开(公告)日：2009-12-15
申请号：AT03739358
申请日：2003-06-27
申请人： TARGACEPT INC
发明人： BHATTI BALWINDER , MILLER CRAIG , SCHMITT JEFFREY
IPC分类号： C07D487/10 , A61K31/40 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/506 , A61P1/02 , A61P1/04 , A61P1/16 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P37/06 , A61P43/00 , C07D453/00 , C07D471/10 , C07D487/20
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are bridged analogues of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can (i) alter the number of nicotinic cholinergic receptors in the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

2. 发明专利

AT381563T 未知
公开(公告)号：AT381563T
公开(公告)日：2008-01-15
申请号：AT04713356
申请日：2004-02-20
申请人： TARGACEPT INC
发明人： MAZUROV ANATOLY , KLUCIK JOZEF , MIAO LAN , SEAMANS ANGELA , PHILLIPS TERESA , SCHMITT JEFFREY , MILLER CRAIG
IPC分类号： C07D453/00 , A61K51/00 , C07D453/02 , C07D453/04 , C07D471/08 , C07D487/08
摘要： The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the alpha7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

4. 发明专利

AU2002256401A1 Heteroaryl ofefinic azacyclic and heteroaryl acetylenic azacyclic compounds for the treatment of cns disorders 未知
公开(公告)号：AU2002256401A1
公开(公告)日：2002-11-11
申请号：AU2002256401
申请日：2002-04-29
申请人： TARGACEPT INC
发明人： MILLER CRAIG H , SCHMITT JEFFREY , DULL GARY M , BHATTI BALWINDER S
IPC分类号： A61K31/407 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/5377 , A61P1/04 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/28 , C07D209/02 , C07D213/32 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/02 , C07D453/02 , C07D487/04
摘要： The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.

5. 发明专利

ES2355157T3 COMPUESTOS DIAZASPIROCICLICO N-ARILO Y METODOS DE PREPARACION Y USO DE LAS MISMAS. 未知
公开(公告)号：ES2355157T3
公开(公告)日：2011-03-23
申请号：ES03739358
申请日：2003-06-27
申请人： TARGACEPT INC
发明人： MILLER CRAIG , BHATTI BALWINDER , SCHMITT JEFFREY
IPC分类号： C07D487/10 , A61K31/40 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/506 , A61P1/02 , A61P1/04 , A61P1/16 , A61P19/02 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P37/06 , A61P43/00 , C07D453/00 , C07D471/10 , C07D487/20
摘要： Un compuesto que tiene la siguiente fórmula: **(Ver fórmula)** y sales farmacéuticamente aceptables de la misma,donde Q1 es (CZ2)u, QII es (CZ2)v, QIII es (CZ2)w, y QIV es (CZ2)x u, v, w y x son individualmente 0, 1, 2, 3 o 4, preferible 0, 1, 2 o 3 y son seleccionados de modo que el anillo diazaspirocíclico del compuesto de la Formula 1 contiene 7, 8 o 9 miembros, R es hidrógeno, alquilo inferior, acil, alcoxicarbonil o ariloxicarbonil, Z es, individualmente, seleccionado del grupo consistente de hidrógeno, alquilo inferior y aril; Cy es un anillo heteroaromático de seis miembros de la fórmula: **(Ver fórmula)** donde cada uno de X, X', X'', X'''' y X'''' es individualmente nitrógeno, nitrógeno unido a oxígeno o carbono unido a especies sustituyentes, donde no mas de tres de X, X', X'', X'''' y X'''' son nitrógeno o nitrógeno unido a oxígeno,o Cy es un anillo heteroaromático de cinco miembros de la fórmula: **(Ver fórmula)** donde Y y Y'' son individualmente nitrógeno, nitrógeno unido a un especie sustituyente, oxígeno, sulfuro o carbono unido a una especie sustituyente y Y' y Y''' arte nitrógeno o carbono unido a una especie sustituyente,donde "especies sustituyentes" son, individualmente, seleccionadas del grupo consistente de hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, heterociclil, heterociclil sustituido, cicloalquilo, cilcoalquilo sustituido, aril, aril sustituido, alquiloaril, alquiloaril sustituido, arilalquilo, arilalquilo sustituido, halo, -OR', -NR'R'', -CF3, -CN, -NO2, -C2R', -SR', -N3, -C(= O)NR'R'', -NR'C(=O) R'', -C(=O)OR', -OC(=O)R', -O(CR'R''),C(=O)R', -O(CR'R'')rNR''C(=O)R', -O(CR'R'')rNR''SO2R', -OC(=O)NR'R'', -NR'C(=O)O R'', -SO2R', -SO2NR'R'', y -NR'SO2R'', donde R' y R'' son individualmente hidrógeno, C1-C8 alquilo, cicloalquilo, heterociclil, aril, o arilalquilo, y r es un integro de 1 a 6, o R' y R'' pueden combinarse para formar una funcionalidad cíclica, donde el termino sustituido como se aplica a alquilo, cicloalquilo, alquenil, heterociclil, alquiloaril y arilalquilo se refiere a los sustituyentes descritos anteriormente, comenzando con halo y terminando con NR'SO2R'', y donde las lineas discontinuas indican que las uniones (entre Y y Y' y entre Y' y Y'') pueden ser tanto uniones simples o dobles, con la salvedad de que cuando la unión entre Y y Y' es un unión simple, la unión entre Y' y Y'' debe ser una unión doble y viceversa, donde Y o Y'' es oxígeno o sulfuro, solo uno de Y y Y'' es tanto oxígeno o sulfuro, y al menos uno de Y, Y', Y'' y Y''' deben ser oxígeno, sulfuro, nitrógeno o nitrógeno unido a una especie sustituyente.

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