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1. 发明申请

WO2008091588A1 INTRANASAL, BUCCAL, AND SUBLINGUAL ADMINISTRATION OF METANICOTINE ANALOGS 审中-公开
标题翻译：金属蛋白酶类似物的内分泌，细胞和亚型管理
公开(公告)号：WO2008091588A1
公开(公告)日：2008-07-31
申请号：PCT/US2008/000802
申请日：2008-01-22
申请人： TARGACEPT, INC. , LETCHWORTH, Sharon, Rae , BENCHERIF, Merouane , DULL, Gary, Maurice , MOORE, David , JAMES, John, W.
发明人： LETCHWORTH, Sharon, Rae , BENCHERIF, Merouane , DULL, Gary, Maurice , MOORE, David , JAMES, John, W.
IPC分类号： A61K9/00 , A61K31/44
CPC分类号： A61K9/006 , A61K9/0056 , A61K31/44
摘要： The present invention generally relates to pharmaceutical compositions for the intranasal, buccal, or sublingual administration of metanicotine analogs.
摘要翻译：本发明一般涉及间苯二胺类似物的鼻内，口腔或舌下施用的药物组合物。

2. 发明申请

WO0071520A2 PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE 审中-公开
标题翻译：药物组合物和使用方法
公开(公告)号：WO0071520A2
公开(公告)日：2000-11-30
申请号：PCT/US0011256
申请日：2000-04-27
申请人： TARGACEPT INC , DULL GARY MAURICE , REICH ERIN E , WAGNER JARED MILLER , BHATTI BALWINDER SINGH , CONSILVIO MICHAEL B
发明人： DULL GARY MAURICE , REICH ERIN E , WAGNER JARED MILLER , BHATTI BALWINDER SINGH , CONSILVIO MICHAEL B
IPC分类号： A61K31/13 , A61K31/136 , A61K31/138 , A61K31/44 , A61K31/4406 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P43/00 , C07C205/37 , C07C217/16 , C07C217/20 , C07C217/52 , C07C217/56 , C07C217/84 , C07C323/25 , C07D213/65 , C07D213/69 , C07D213/70 , C07D213/71 , C07D317/64 , C07C205/06 , C07C211/46 , C07C211/48
CPC分类号： C07D213/70 , C07C205/37 , C07C217/16 , C07C217/20 , C07D213/65 , C07D317/64
摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines and arylthioalkylamines, including pyridyloxylalkylamines, phenoxyalkylamines, pyridylthiolalkylamines and phenylthioalkylamines.
摘要翻译：通过向有需要的患者施用芳氧基烷基胺和芳硫基烷基胺，包括吡啶氧基烷基胺，苯氧基烷基胺，吡啶硫醇烷基胺和苯硫基烷基胺来治疗易患或患有病症和障碍的患者，例如中枢神经系统疾病。

3. 发明申请

WO2011146009A8 NEW PROCESS FOR THE PREPARATION OF ARYL SUBSTITUTED OLEFINIC AMINES 审中-公开
标题翻译：制备芳基取代的烯醇胺的新工艺
公开(公告)号：WO2011146009A8
公开(公告)日：2012-01-19
申请号：PCT/SE2011050630
申请日：2011-05-19
申请人： ASTRAZENECA AB , TARGACEPT INC , DULL GARY MAURICE , GENUS JOHN , RATILAINEN TOMMI , RYBERG PER OLOF , HELLSTROEM JANNA , WAHLSTROEM NIKLAS , WAENNMAN THOMAS
发明人： DULL GARY MAURICE , GENUS JOHN , RATILAINEN TOMMI , RYBERG PER OLOF , HELLSTROEM JANNA , WAHLSTROEM NIKLAS , WAENNMAN THOMAS
IPC分类号： C07C29/40 , C07C211/21 , C07C231/14 , C07D213/65
CPC分类号： C07D213/65 , C07C29/36 , C07C211/21 , C07C269/04 , C07C33/03 , C07C271/12
摘要： An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N- methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.
摘要翻译：用于制备芳基取代的烯属胺如（2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）基] -4-戊烯-2-胺和（2S） - （4E）-N-甲基-5- [3-（5-甲氧基吡啶）基] -4-戊烯-2-胺和用于所述方法的新中间体。

4. 发明申请

WO2010065449A1 (R) -3- (E) -2- (PYRR0LIDIN-3-YL) VINYL) -5- (TETRAHYDR0PYRAN-4-YL0XY) PYRIDINE, ITS SALTS, ITS SYNTHESIS AND ITS USE AS LIGAND FOR NICOTINIC ACETYLCHOLINERGIC RECEPTORS 审中-公开
标题翻译：（R）-3-（E）-2-（PYRR0LIDIN-3-YL）VINYL）-5-（四氢吡喃-4-基）吡啶，其盐，其合成及其用作NICOTINIC乙酰胆碱受体的配体
公开(公告)号：WO2010065449A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/066092
申请日：2009-11-30
申请人： TARGACEPT, INC. , AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , CUTHBERTSON, Timothy, J. , DULL, Gary, Maurice , GATTO, Gregory, J. , GENUS, John , HAMMOND, Philip, S. , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , OTTEN, Pieter, Albert , YOHANNES, Daniel , FEDOROV, Nikolai
发明人： AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , CUTHBERTSON, Timothy, J. , DULL, Gary, Maurice , GATTO, Gregory, J. , GENUS, John , HAMMOND, Philip, S. , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , OTTEN, Pieter, Albert , YOHANNES, Daniel , FEDOROV, Nikolai
IPC分类号： C07D405/14 , A61P25/00 , A61K31/4439
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention relates to (R) -3- ( (E) -2- (pyrrolidin-3-yl) vinyl) -5- (tetrahydropyran-4-yloxy) pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions. The present invention relates also the use of this compound in the manufacture of a medicament for the treatment of CNS related disorders.
摘要翻译：本发明涉及（R）-3 - （（E）-2-（吡咯烷-3-基）乙烯基）-5-（四氢吡喃-4-基氧基）吡啶及其盐形式，这些化合物的大规模生产具有足够的纯度和质量用于药物组合物。本发明还涉及该化合物在制备用于治疗CNS相关疾病的药物中的用途。

5. 发明申请

WO2009091561A1 PREPARATION AND ENANTIOMERIC SEPARATION OF 7-(3-PYRIDINYL)-1,7-DIAZASPIRO[4.4] NONANE AND NOVEL SALT FORMS OF THE RACEMATE AND ENANTIOMERS 审中-公开
标题翻译： 7-（3-吡啶基）-1,7-二氮杂萘的制备和分离方法[4.4]非特异性和新型盐酸盐形式
公开(公告)号：WO2009091561A1
公开(公告)日：2009-07-23
申请号：PCT/US2009/000242
申请日：2009-01-15
申请人： TARGACEPT, INC. , BEAVER, Jessica , BREINING, Scott , DULL, Gary, Maurice , GATTO, Gergory, J. , GENUS, John , MATHEW, Jacob , MUNOZ, Julio, A. , PFEIFFER, Inigo , TOLER, Steve , WAMSLEY, James , XIE, Jianxun
发明人： BEAVER, Jessica , BREINING, Scott , DULL, Gary, Maurice , GATTO, Gergory, J. , GENUS, John , MATHEW, Jacob , MUNOZ, Julio, A. , PFEIFFER, Inigo , TOLER, Steve , WAMSLEY, James , XIE, Jianxun
IPC分类号： A01N43/42 , A61K31/44 , C07D491/10
CPC分类号： C07D487/10
摘要： A novel scalable synthesis for the preparation of 7-(3- pyridinyI)- 1,7- diazaspiro[4.4)nonane has been developed, and7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane salts have been formed with succinic acid and oxalic acid. Additionally, 7-(3-pyridinyl)-1,7- diazaspiro[4.4]nonane has been separated into its stereoisomers via resolution with L and D di-p-toluoyltartaric acids, giving (R)- and (S)-7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane of high enantiomeric purity. Numerous solid salts of the resulting (R)- and (S)-7-(3-pyridinyl)-1,7- diazaspiro[4.4}nonane have been prepared. Methods for the preparation of the racemic and enantiomeric salts, pharmaceutical compositions comprising such salts, and uses thereof are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
摘要翻译：已经开发了用于制备7-（3-吡啶基）-1,7-二氮杂螺[4.4]壬烷的新的可伸缩合成物，已经形成了7-（3-吡啶基）-1,7-二氮杂螺[4.4]壬烷盐用琥珀酸和草酸。另外，7-（3-吡啶基）-1,7-二氮杂螺[4.4]壬烷已经通过用L和D二对甲苯甲酰基酒石酸分解来分离成其立体异构体，得到（R） - 和（S）-7- （3-吡啶基）-1,7-二氮杂螺[4.4]壬烷，具有高对映体纯度。制备了所得（R） - 和（S）-7-（3-吡啶基）-1,7-二氮杂螺[4.4]壬烷的许多固体盐。公开了制备外消旋和对映异构体盐的方法，包含这些盐的药物组合物及其用途。盐可以施用于易患或患有诸如中枢神经系统障碍的病症和障碍的患者，以治疗和/或预防这些疾病。

6. 发明申请

WO0182978A3 IMAGING OF NICOTINIC ACETYLCHOLINE RECEPTOR SUBTYPES 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体亚型的成像
公开(公告)号：WO0182978A3
公开(公告)日：2002-08-01
申请号：PCT/US0113950
申请日：2001-05-01
申请人： TARGACEPT INC , BENCHERIF MEROUANE , MILLER CRAIG HARRISON , DULL GARY MAURICE , BHATTI BALWINDER SINGH , CALDWELL WILLIAM SCOTT
发明人： BENCHERIF MEROUANE , MILLER CRAIG HARRISON , DULL GARY MAURICE , BHATTI BALWINDER SINGH , CALDWELL WILLIAM SCOTT
IPC分类号： A61K51/04
CPC分类号： A61K51/0455 , A61K51/0459
摘要： Compounds useful as probes for determining the relative number and/or function of specific receptor subtypes. Of particular interest are nicotinic agonists and antagonists (e.g., metanicotine-type compounds and azaadamantane-type compounds) that are selective to certain nicotinic receptor subtypes. Those compounds are labeled with a radioactive isotopic moiety such as C, F, Br, I or I. Central nervous system disorders are diagnosed by administering to a patient a detectably labeled compound, and detecting the binding of that compound to selected nicotinic receptor subtypes (e.g., alpha 7 and/or alpha 4 beta 2 receptor subtypes). The compounds that have been administered are detected using methods such as position emission topography (PET) and single-photon emission computed tomography (SPECT). The present invention is useful in the diagnosis of a wide variety of CNS diseases and disorders, including Alzheimer's disease, Parkinson's disease and schizophrenia.
摘要翻译：用作确定特异性受体亚型的相对数量和/或功能的探针的化合物。特别感兴趣的是对某些烟碱型受体亚型具有选择性的烟碱激动剂和拮抗剂（例如间断烟碱型化合物和氮杂金刚烷型化合物）。这些化合物用放射性同位素部分标记，例如11 C，18 F，76 Br，123 I或125 I。通过向患者施用可检测标记的化合物，并检测该化合物与选定的烟碱受体亚型（例如α7和/或α4β2受体亚型）的结合来诊断中枢神经系统疾病。使用诸如位置发射形貌（PET）和单光子发射计算机断层摄影（SPECT）的方法检测已经施用的化合物。本发明可用于诊断各种CNS疾病和疾病，包括阿尔茨海默氏病，帕金森病和精神分裂症。

7. 发明申请

WO2009018367A3 SALT FORMS OF (2S)-(4E)-N-METHYL-5-[3-(5-METHOXYPYRIDIN)YL]-4-PENTEN-2-AMINE 审中-公开
标题翻译：（2S） - （4E）-N-甲基-5- [3-（5-甲氧基吡啶）基] -4-苯基-2-胺的盐形式
公开(公告)号：WO2009018367A3
公开(公告)日：2010-05-27
申请号：PCT/US2008071631
申请日：2008-07-30
申请人： TARGACEPT INC , DULL GARY MAURICE , MUNOZ JULIO A , GENUS JOHN , BHATTI BALWINDER SINGH , YOUNG JENNIFER A , BENCHERIF MEROUANE , JAMES JOHN W , WILLIAMS MICHAEL G , JORDAN KRISTEN , LIPPIELLO PATRICK M , FORDHAM-MEIER BETH
发明人： DULL GARY MAURICE , MUNOZ JULIO A , GENUS JOHN , BHATTI BALWINDER SINGH , YOUNG JENNIFER A , BENCHERIF MEROUANE , JAMES JOHN W , WILLIAMS MICHAEL G , JORDAN KRISTEN , LIPPIELLO PATRICK M , FORDHAM-MEIER BETH
IPC分类号： C07D213/62 , A61K31/44 , A61P25/28
CPC分类号： C07D213/62
摘要： Salts of (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine, methods for their preparation, pharmaceutical compositions comprising said salts, and their use are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat or prevent such disorders.
摘要翻译：（2S） - （4E）-N-甲基-5- [3-（5-甲氧基吡啶）基] -4-戊烯-2-胺的盐，其制备方法，包含所述盐的药物组合物及其用途披露。盐可以施用于易患或患有诸如中枢神经系统疾病的病症和障碍的患者，以治疗或预防这些疾病。

8. 发明申请

WO2008091592A1 INTRANASAL, BUCCAL, AND SUBLINGUAL ADMINISTRATION OF METANICOTINE ANALOGS 审中-公开
标题翻译：金属蛋白酶类似物的内分泌，阴性和亚型管理
公开(公告)号：WO2008091592A1
公开(公告)日：2008-07-31
申请号：PCT/US2008/000806
申请日：2008-01-22
申请人： TARGACEPT, INC. , LETCHWORTH, Sharon, Rae , BENCHERIF, Merouane , DULL, Gary, Maurice , MOORE, David , JAMES, John
发明人： LETCHWORTH, Sharon, Rae , BENCHERIF, Merouane , DULL, Gary, Maurice , MOORE, David , JAMES, John
IPC分类号： A61K9/00 , A61K31/44
CPC分类号： A61K9/006 , A61K9/0056 , A61K31/44
摘要： The present invention generally relates to pharmaceutical compositions for the intranasal, buccal, or sublingual administration of meta nicotine analogs.
摘要翻译：本发明一般涉及鼻内，口腔或舌下施用次尼古丁类似物的药物组合物。

9. 发明申请

WO2007134034A1 POLYMORPH FORMS OF (2S) - (4E) -N-METHYL-5- (3-ISOPROPOXYPYRIDIN) YL] -4-PENTEN-2-AMINE FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：（2S） - （4E）-N-甲基-5-（3-异丙氧基吡啶）YL] -4-丁烯-2-胺的多聚体形式用于治疗中枢神经系统疾病
公开(公告)号：WO2007134034A1
公开(公告)日：2007-11-22
申请号：PCT/US2007/068446
申请日：2007-05-08
申请人： Targacept, Inc. , DULL, Gary, Maurice , MUNOZ, Julio, A.
发明人： DULL, Gary, Maurice , MUNOZ, Julio, A.
IPC分类号： C07D213/63 , A61K31/44 , A61P25/28
CPC分类号： C07D213/65
摘要： Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4- penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
摘要翻译：（2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）基] -4-戊烯-2-胺对羟基苯甲酸酯的多晶型及其制备方法，含有所述多晶型物（s）和使用。可将多晶型物施用于易患或患有诸如中枢神经系统疾病的病症和病症的患者，以治疗和/或预防这些病症。

10. 发明申请

WO9951216A3 3-PYRIDYLOXYALKYLAMINE OR ARYLOXYALKYLAMINE DERIVATIVES AS CHOLINERGIC AGONISTS 审中-公开
标题翻译： 3-吡啶基甲酰胺或芳基酰胺衍生物作为胆固醇激素
公开(公告)号：WO9951216A3
公开(公告)日：1999-11-18
申请号：PCT/US9904235
申请日：1999-02-26
申请人： REYNOLDS TOBACCO CO R , DULL GARY MAURICE , DOBSON GRAYLAND PAGE , WAGNER JARED MILLER
发明人： DULL GARY MAURICE , DOBSON GRAYLAND PAGE , WAGNER JARED MILLER
IPC分类号： A61K31/138 , A61K31/44 , A61K31/4406 , A61P25/00 , A61P43/00 , C07D213/65
CPC分类号： C07D213/65 , A61K31/138 , A61K31/44 , A61K31/4406
摘要： Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines, such as (3-(3-pyridyloxy)propyl)methylamine and (3-(5-bromo(3-pyridyloxy))propyl)methylamine.
摘要翻译：通过向有需要的患者施用芳氧基烷基胺，包括吡啶氧基烷基胺和苯氧基烷基胺，例如（3-（3-吡啶氧基）丙基）甲胺和（3 - （5-溴（3-吡啶氧基））丙基）甲胺。

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