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18 条记录 (耗时 0.026 秒)

    NICOTINIC ACETYLCHOLINE RECEPTORSUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES
    7.
    发明授权
    NICOTINIC ACETYLCHOLINE RECEPTORSUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES 有权
    烟碱乙酰胆碱受体亚型选择性DIAZABICYCLOALKANAMIDE

    公开(公告)号：EP2094703B1

    公开(公告)日：2011-05-11

    申请号：EP07863786.5

    申请日：2007-11-01

    申请人： Targacept, Inc.

    发明人： MAZUROV, Anatoly ,  MIAO, Lan ,  XIAO, Yun-de

    IPC分类号： C07D471/08 ,  A61P25/00 ,  A61K31/407 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D471/08

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4ß2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particuarly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse 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).

    3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF
    8.
    发明授权
    3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
    3-取代的-2（芳基烷基）供其使用-1- azabicycloalkanes AND METHODS

    公开(公告)号：EP1594869B9

    公开(公告)日：2009-04-01

    申请号：EP04713356.6

    申请日：2004-02-20

    申请人： Targacept, Inc.

    发明人： MAZUROV, Anatoly, A. ,  KLUCIK, Jozef ,  MIAO, Lan ,  SEAMANS, Angela, S. ,  PHILLIPS, Teresa, Youngpeter ,  SCHMITT, Jeffrey, Daniel ,  MILLER, Craig, Harrison

    IPC分类号： C07D453/00 ,  C07D453/02

    CPC分类号： C07D471/08 ,  A61K51/0455 ,  C07D453/02 ,  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 a7 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.

    HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF
    9.
    发明公开
    HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF 有权
    杂芳基DIAZATRICYCLOALKANE，方法及其及其应用

    公开(公告)号：EP1917265A1

    公开(公告)日：2008-05-07

    申请号：EP06813627.4

    申请日：2006-08-21

    申请人： Targacept, Inc.

    发明人： MAZUROV, Anatoly ,  MIAO, Lan ,  KLUCIK, Jozef

    IPC分类号： C07D471/18 ,  A61K31/439 ,  A61P25/00

    CPC分类号： C07D471/18 ,  C07D471/14

    摘要： The present invention relates to amide and urea derivatives of heteroaryl- substituted diazatricycloalkanes, of the Formula (I) with the definition as set out in the description pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the α7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the α7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N- arylcarbamoyl) (urea type derivative) group. The compounds are beneficial in therapeutic applications requiring a selective interaction at certain nAChR subtypes. That is, the compounds modulate the activity of certain nAChR subtypes, particularly the α7 nAChR subtype, and do not have appreciable activity toward muscarinic receptors. Radiolabeled versions of the compounds can be used in diagnostic methods.

    3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF
    10.
    发明授权
    3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
    3-取代的-2（芳基烷基）供其使用-1- azabicycloalkanes AND METHODS

    公开(公告)号：EP1594869B1

    公开(公告)日：2007-12-19

    申请号：EP04713356.6

    申请日：2004-02-20

    申请人： Targacept, Inc.

    发明人： MAZUROV, Anatoly, A. ,  KLUCIK, Jozef ,  MIAO, Lan ,  SEAMANS, Angela, S. ,  PHILLIPS, Teresa, Youngpeter ,  SCHMITT, Jeffrey, Daniel ,  MILLER, Craig, Harrison

    IPC分类号： C07D453/00 ,  C07D453/02

    CPC分类号： C07D471/08 ,  A61K51/0455 ,  C07D453/02 ,  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 a7 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.