公开(公告)号：EP1678172B1

公开(公告)日：2009-12-09

申请号：EP04795238.7

申请日：2004-10-15

申请人： Targacept, Inc.

发明人： BREINING, Scott R. ,  BHATTI, Balwinder S. ,  HAWKINS, Gregory D. ,  MIAO, Lan ,  MAZUROV, Anatoly ,  PHILLIPS, Teresa Y. ,  MILLER, Craig H.

IPC分类号： C07D471/00

CPC分类号： C07D221/22 ,  C07D401/04

摘要： Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas (1 or 2), as described herein. The compounds of Formulas (1 and 2) are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

公开(公告)号：EP2094703A1

公开(公告)日：2009-09-02

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 ,  HAMMOND, Philip S. ,  MILLER, Craig H. ,  AKIREDDY, Srinivisa Rao ,  MURTHY, V. Srinivasa ,  WHITAKER, Regina C. ,  BREINING, Scott R. ,  MELVIN, Matt S.

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).

公开(公告)号：EP1678172A2

公开(公告)日：2006-07-12

申请号：EP04795238.7

申请日：2004-10-15

申请人： Targacept, Inc.

发明人： BREINING, Scott R. ,  BHATTI, Balwinder S. ,  HAWKINS, Gregory D. ,  MIAO, Lan ,  MAZUROV, Anatoly ,  PHILLIPS, Teresa Y. ,  MILLER, Craig H.

IPC分类号： C07D471/00

CPC分类号： C07D221/22 ,  C07D401/04

摘要： Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas (1 or 2), as described herein. The compounds of Formulas (1 and 2) are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.