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41. 发明专利

AU2003245753A1 N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 未知
公开(公告)号：AU2003245753A1
公开(公告)日：2004-01-23
申请号：AU2003245753
申请日：2003-06-27
申请人： TARGACEPT INC
发明人： BHATTI BALWINDER S , MILLER CRAIG H , SCHMITT JEFFREY D
IPC分类号： 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 , C07D487/10 , C07D487/20 , A61K31/40 , A61K31/435
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).

42. 发明专利

NO332760B1 未知
公开(公告)号：NO332760B1
公开(公告)日：2013-01-07
申请号：NO20110014
申请日：2011-01-06
申请人： TARGACEPT INC
发明人： MILLER CRAIG H , MAZUROV ANATOLY A , KLUCIK JOZEF , SEAMANS ANGELA S , PHILLIPS TERESA YOUNGPETER , SCHMITT JEFFREY DANIEL , MIAO LAN
IPC分类号： C07D453/02 , A61K51/00 , C07D453/00 , 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.

43. 发明专利

AU2007317433B2 Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes 未知
公开(公告)号：AU2007317433B2
公开(公告)日：2012-05-10
申请号：AU2007317433
申请日：2007-11-01
申请人： TARGACEPT INC
发明人： AKIREDDY SRINIVISA RAO , MAZUROV ANATOLY , MURTHY V SRINIVASA , WHITAKER REGINA C , HAMMOND PHILIP S , MIAO LAN , XIAO YUN-DE , MILLER CRAIG H , BREINING SCOTT R , MELVIN MATT S
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00 , C07D487/04
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).

44. 发明专利

NZ587847A Nicotinic acetylcholine receptorsub-type selective amides of diazabicycloalkanes 未知
公开(公告)号：NZ587847A
公开(公告)日：2011-09-30
申请号：NZ58784707
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
IPC分类号： C07D487/04 , A61K31/407 , A61P25/00 , C07D471/08
摘要： Disclosed is a 3,7-diazabicyclo[3.3.0]octane of Formula I wherein n is 0 or 1; and Cy is a heteroaryl group selected from the group consisting of 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 1,3,4-thiadiazol-2-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl and 4-pyridinyl. Also disclosed is the use of said octane in the treatment of age-associated memory impairment, mild cognitive impairment, pre-senile dementia, early onset Alzheimer's disease, senile dementia, dementia of the Alzheimer's type, Lewy body dementia, vascular dementia, Alzheimer's disease, stroke, AIDS dementia complex, attention deficit disorder, attention deficit hyperactivity disorder, dyslexia, schizophrenia, schizophreniform disorder and schizoaffective disorder.

45. 发明专利

CA2491506C N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 未知
公开(公告)号：CA2491506C
公开(公告)日：2011-04-26
申请号：CA2491506
申请日：2003-06-27
申请人： TARGACEPT INC
发明人： BHATTI BALWINDER S , MILLER CRAIG H , SCHMITT JEFFREY D
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 , C07D453/02 , C07D471/10 , C07D471/20 , C07D487/20
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryldiazaspirocyclic compounds, bridged analogs 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 choligernic 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 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).

46. 发明专利

AU2008258188B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 未知
公开(公告)号：AU2008258188B2
公开(公告)日：2011-02-24
申请号：AU2008258188
申请日：2008-12-17
申请人： TARGACEPT INC
发明人： DULL GARY MAURICE , MILLER CRAIG H , CAPET MARC , GENEVOIS-BORELLA ARIELLE , SCHMITT JEFFREY DANIEL , CHEVE MICHEL
IPC分类号： C07D401/06 , C07D403/06 , C07D405/14
摘要： The vinylazacycloalkane compound 3-(2-pyrrolidin-3-ylvinyl)-5-(tetrahydropyran-4-yloxy)pyridine is disclosed. The compound is a ligand of nAChRs. The compound and its pharmaceutically acceptable salt can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of the type of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioural disorders and inflammatory disorders within the gastrointestinal system. The compound can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

47. 发明专利

SI1678172T1 AzabicikliŽŤne spojine za lajĹˇanje boleŽŤine in zdravljenje motenj centralnega ĹľivŽŤnega sistema 未知
公开(公告)号：SI1678172T1
公开(公告)日：2010-04-30
申请号：SI200431352
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 , A61K31/46 , A61K31/506 , C07D221/22 , C07D401/04

49. 发明专利

MX2009004801A AMIDAS DE DIAZABICICLOALCANOS SELECTIVAS DE SUBTIPO DE RECEPTOR NICOTINICO DE ACETILCOLINA. 未知
公开(公告)号：MX2009004801A
公开(公告)日：2009-07-31
申请号：MX2009004801
申请日：2007-11-01
申请人： TARGACEPT INC
发明人： MIAO LAN , MILLER CRAIG H , MAZUROV ANATOLY , XIAO YUN-DE , HAMMOND PHILIP S , AKIREDDY SRINIVISA RAO , WHITAKER REGINA C , MURTHY V SRINIVASA , BREINING SCOTT R , MELVIN MATT S
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00 , C07D487/04
摘要： Se describen compuestos, composiciones farmacéuticas que incluyen los compuestos, y métodos de preparación y uso de los mismos; los compuestos son compuestos de amida que se pueden preparar a partir de ciertos ácidos heteroarilcarboxílicos y ciertos diazabicicloalcanos; los compuestos presentan selectividad para, y unión con alta afinidad a, receptores nicotínicos neuronales del subtipo a4ß2 en el sistema nervioso central (SNC); los compuestos y composiciones se pueden usar para tratar y/o prevenir una amplia variedad de condiciones o trastornos, particularmente trastornos del SNC; los compuestos pueden: (i) alterar el número de receptores colinérgicos nicotínicos del cerebro del paciente, (ii) presentan efectos neuroprotectores, y (iii) cuando se utilizan en cantidades efectivas, no dan por resultado efectos colaterales adversos apreciables (v.gr., efectos colaterales tales como incrementos significativos en presión sanguínea y ritmo cardiaco, efectos negativos significativos sobre el tracto gastrointestinal, y efectos significativos sobre músculo esquelético).

50. 发明专利

NO20091251L 未知
公开(公告)号：NO20091251L
公开(公告)日：2009-05-28
申请号：NO20091251
申请日：2009-03-26
申请人： TARGACEPT INC
发明人： MILLER CRAIG H , MAZUROV ANATOLY A , MIAO LAN , XIAO YUN-DE , HAMMOND PHILIP S , AKIREDDY SRINIVISA RAO , MURTHY V SRINIVISA , WHITAKER REGINA C , BREINING SCOTT R , MELVIN MATT S
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00 , C07D487/04
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 heteroraryl 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, particularly 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). Formula I: wherein n has the value of 0 or 1, and Cy is a heteroaryl group chosen from the group of 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 1,3,4-thiadiazol-2-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl and 4-pyridinyl.

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