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1. 发明申请

WO2001090109A1 HETEROARYLDIAZABICYCLOALKANES AS NICOTINIC CHOLINERGIC RECEPTOR LIGANDS 审中-公开
标题翻译：作为非甾体类胆碱受体配体的异氟烷基胆碱
公开(公告)号：WO2001090109A1
公开(公告)日：2001-11-29
申请号：PCT/US2001/016941
申请日：2001-05-24
申请人： TARGACEPT, INC. , MILLER, Craig, Harrison , DULL, Gary, Maurice , MIAO, Lan , LYNM, Dwo , SCHMITT, Jeffrey, Daniel , CLARK, Thomas, Jeffrey
发明人： MILLER, Craig, Harrison , DULL, Gary, Maurice , MIAO, Lan , LYNM, Dwo , SCHMITT, Jeffrey, Daniel , CLARK, Thomas, Jeffrey
IPC分类号： C07D487/08
CPC分类号： C07D487/08
摘要： The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include: (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(3,4-dimethoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.
摘要翻译：本发明涉及二氮杂双环化合物，优选涉及N-芳基二氮杂双环化合物。特别令人感兴趣的是2-吡啶基二氮杂双环化合物，例如（1S，4S）-2-（5-（3-甲氧基苯氧基）-3-吡啶基）-2,5-二氮杂双环[2.2.1]庚烷。本发明的其它示例性化合物包括：（1S，4S）-2-（5-（4-甲氧基苯氧基）-3-吡啶基）-2,5-二氮杂双环[2.2.1]庚烷，（1S，4S）-2 （5-（3,4-二甲氧基苯氧基）-3-吡啶基）-2,5-二氮杂双环[2.2.1]庚烷，（1S，4S）-2-（5-（4-氟苯氧基）-3-吡啶基） -2,5-二氮杂双环[2.2.1]庚烷和（1S，4S）-2-（5-苯甲酰基-3-吡啶基）-2,5-二氮杂双环[2.2.1]庚烷。本发明还涉及本发明化合物的前药衍生物。

2. 发明申请

WO2004076449A2 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 3-取代-2（芳基）-1-氮杂环十二烷及其使用方法
公开(公告)号：WO2004076449A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/005044
申请日：2004-02-20
申请人： TARGACEPT, INC. , MAZUROV, Anatoly, A. , KLUCIK, Jozef , MIAO, Lan , SEAMANS, Angela, S. , PHILLIPS, Teresa, Youngpeter , SCHMITT, Jeffrey, Daniel , MILLER, Craig, Harrison
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
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.
摘要翻译：本发明涉及3-取代-2-（芳基烷基）-1-氮杂双环烷烃，制备该化合物的方法和使用该化合物的治疗方法。氮杂双环烷烃通常是氮杂二环庚烷，氮杂二环辛烷或氮杂二环壬烷。芳基烷基部分中的芳基是5或6元环杂芳族，优选3-吡啶基和5-嘧啶基部分，并且烷基典型地为C 1-4烷基。 1-氮杂双环烷烃3-位上的取代基是含羰基的部分，如酰胺，氨基甲酸酯，脲，硫代酰胺，硫代氨基甲酸酯，硫脲或类似的官能团。这些化合物对烟碱型乙酰胆碱受体（nAChRs），特别是a7 nAChR亚型表现出活性，并且可用于调节神经传递和参与神经传递的配体的释放。还公开了预防或治疗以正常神经传递改变为特征的包括中枢神经系统（CNS）障碍的病症和障碍的方法。还公开了用于治疗炎症，自身免疫病症，疼痛和过量新血管形成的方法，例如与肿瘤生长有关的方法。

3. 发明申请

WO2009018505A1 (2S,3R)-N-(2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL)BENZOFURAN-2-CARBOXAMIDE, NOVEL SALT FORMS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：（2S，3R）-N-（2 - （（3-吡啶基）甲基）-1-氮杂双环[2.2.2] OCT-3-YL）苯并呋喃-2-羧酰胺，新型盐形式及其使用方法
公开(公告)号：WO2009018505A1
公开(公告)日：2009-02-05
申请号：PCT/US2008/071872
申请日：2008-08-01
申请人： TARGACEPT, INC. , BENCHERIF, Merouane , BENSON, Lisa , DULL, Gary Maurice , FEDOROV, Nikolai , GATTO, Gregory J. , GENUS, John , JORDAN, Kristen G. , MATHEW, Jacob , MAZUROV, Anatoly A. , MIAO, Lan , MUNOZ, Julio A. , PFEIFFER, Inigo , PFEIFFER, Sondra , PHILLIPS, Teresa Y.
发明人： BENCHERIF, Merouane , BENSON, Lisa , DULL, Gary Maurice , FEDOROV, Nikolai , GATTO, Gregory J. , GENUS, John , JORDAN, Kristen G. , MATHEW, Jacob , MAZUROV, Anatoly A. , MIAO, Lan , MUNOZ, Julio A. , PFEIFFER, Inigo , PFEIFFER, Sondra , PHILLIPS, Teresa Y.
IPC分类号： A61K31/4545 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00
CPC分类号： C07D453/02 , A61K31/439
摘要： The present invention relates to (2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.
摘要翻译：本发明涉及（2S，3R）-N-（2 - （（3-吡啶基）甲基）-1-氮杂双环[2.2.2]辛-3-基）苯并呋喃-2-甲酰胺，其新的盐形式，其制备方法，新型中间体和用于治疗各种病症和障碍的方法，包括与中枢神经系统和自主神经系统的功能障碍相关的方法。

4. 发明申请

WO2012094437A2 NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS 审中-公开
标题翻译：烟碱受体非竞争性拮抗剂
公开(公告)号：WO2012094437A2
公开(公告)日：2012-07-12
申请号：PCT/US2012/020246
申请日：2012-01-05
申请人： TARGACEPT, INC. , AKIREDDY, Srinivasa Rao , BREINING, Scott R. , MELVIN, Matt S. , MURTHY, Srinivasa V. , MAZUROV, Anatoly A. , BHATTI, Balwinder Singh , STRACHAN, Jon-Paul , HEEMSTRA, Ronald Joseph , SHOWALTER, Todd , XIAO, Yunde , HAMMOND, Philip S. , MIAO, Lan , KOMBO, David , YOHANNES, Daniel , SPEAKE, Jason
发明人： AKIREDDY, Srinivasa Rao , BREINING, Scott R. , MELVIN, Matt S. , MURTHY, Srinivasa V. , MAZUROV, Anatoly A. , BHATTI, Balwinder Singh , STRACHAN, Jon-Paul , HEEMSTRA, Ronald Joseph , SHOWALTER, Todd , XIAO, Yunde , HAMMOND, Philip S. , MIAO, Lan , KOMBO, David , YOHANNES, Daniel , SPEAKE, Jason
IPC分类号： C07C211/35 , A61K31/13 , A61P9/12
CPC分类号： C07D493/08 , C07C211/38 , C07C2602/40 , C07C2602/42 , C07C2602/44
摘要： The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.
摘要翻译：本发明涉及作为非竞争性拮抗剂调节烟碱受体的化合物，它们的合成方法，它们的使用方法和它们的药物组合物。

5. 发明申请

WO2010028011A1 AMIDES OF DIAZABICYCLONONANES AND USES THEREOF 审中-公开
标题翻译：双酚A的化合物及其用途
公开(公告)号：WO2010028011A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/055687
申请日：2009-09-02
申请人： TARGACEPT, INC. , AKIREDDY, Srinivisa Rao , MAZUROV, Anatoly , YOHANNES, Daniel , MIAO, Lan , SPEAKE, Jason Daniel
发明人： AKIREDDY, Srinivisa Rao , MAZUROV, Anatoly , YOHANNES, Daniel , MIAO, Lan , SPEAKE, Jason Daniel
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体活性的下式（I）化合物，制备这些化合物的方法，含有这些化合物的药物组合物，以及使用这些化合物治疗各种各样的病症和疾病，包括与中枢神经系统（CNS）功能障碍有关的疾病。

6. 发明申请

WO2008112734A1 HETEROCYCLIC-CARBONYL-DIAZABICYCLOALKANES AS MODULATORS OF THE NEURONAL NICOTINIC ACETYLCHOLINE ALPHA 4 BETA 2, SUBTYPE RECEPTOR FOR THE TREATMENT OF CNS RELATED DISORDERS 审中-公开
标题翻译：作为神经细胞性乙酰胆碱酯酶4β2的调节剂的杂环碳二亚氨基二醇，用于治疗CNS相关疾病的亚型受体
公开(公告)号：WO2008112734A1
公开(公告)日：2008-09-18
申请号：PCT/US2008/056607
申请日：2008-03-12
申请人： TARGACEPT, INC. , HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , MIAO, Lan , XIAO, Yun-De , BHATTI, Balwinder , STRACHAN, Jon-Paul , MURTHY, V. Srinivasa , KOMBO, David, C. , AKIREDDY, Srinivasa Rao
发明人： HAMMOND, Philip, S. , MAZUROV, Anatoly, A. , MIAO, Lan , XIAO, Yun-De , BHATTI, Balwinder , STRACHAN, Jon-Paul , MURTHY, V. Srinivasa , KOMBO, David, C. , AKIREDDY, Srinivasa Rao
IPC分类号： C07D471/02 , C07D487/02 , A61K31/407 , A61K31/4353 , A61K31/437 , A61P25/00 , A61P25/28 , A61P25/18
CPC分类号： C07D487/04 , C07D471/04 , C07D471/08
摘要： A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1 ]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryi group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α402 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 are believed to: (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, namely 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.
摘要翻译：式1的化合物：A-C（O）-Cy，其中A是具有7,8或9个环原子的二氮杂双环核心，并且选自以下：2,6-二氮杂双环[3.2.0]庚烷; 3,6-二氮杂双环[3.ZO]庚烷; 2,7-二氮杂双环[4.2.0]辛烷; 3,7-二氮杂双环[4.2.0]辛烷; 3,8-二氮杂双环[4.2.0]辛烷; 2,7-二氮杂双环[3.3.0]辛烷; 2,7- diazbicyclo [4.3.0]壬烷; 2,8- diazbicyclo [4.3.0]壬烷; 3,7-二氮杂双环[4.3.0]壬烷; 3,8-二氮杂双环[4.3.0]壬烷; 3,9-二氮杂双环[4.3.0]壬烷; 2,6-二氮杂双环[3.2.1]辛烷; 3,6-二氮杂双环[3.2.1]辛烷; 其中所述二氮杂双环通过两个环氮原子中的任一个连接到所描绘的羰基上，使得羰基与环氮形成酰胺键; Cy是一个杂种组; 该化合物对中枢神经系统（CNS）中a402亚型的神经元烟碱受体表现出选择性并且以高亲和力结合。化合物和组合物可用于治疗和/或预防多种病症或病症，特别是CNS疾病。这些化合物被认为是：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用影响如血压和心率显着升高，对胃肠道的显着负面影响，以及对骨骼肌的显着影响。

7. 发明申请

WO2007024814A1 HETEROARYL-SUBSTiTUTED DIAZATRICYCLOALKANES, METHODS FOR ITS PREPARATION AND USE THEREOF 审中-公开
标题翻译：异丁基二异氰酸酯盐，其制备方法及其用途
公开(公告)号：WO2007024814A1
公开(公告)日：2007-03-01
申请号：PCT/US2006/032685
申请日：2006-08-21
申请人： TARGACEPT, INC. , MAZUROV, Anatoly , MIAO, Lan , KLUCIK, Jozef
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.
摘要翻译：本发明涉及式（I）的杂芳基取代的二氮三环环烷烃的酰胺和脲衍生物，其定义如本说明书所述的药物组合物包括化合物，制备化合物的方法和使用该化合物的治疗方法。更具体地，治疗方法包括通过施用一种或多种化合物来治疗或预防由a7 nAChR亚型介导的病症来调节a7 nAChR亚型的活性。二氮杂环烷烃通常由与吡咯烷环稠合的1-氮杂双环辛烷组成。取代基杂芳基是5-或6-元环杂芳族化合物，例如3-吡啶基和5-嘧啶基部分，其直接连接到二氮杂环烷烃上。吡咯烷部分的仲氮被芳基羰基（酰胺型衍生物）或芳基氨基羰基（N-芳基氨基甲酰基）（脲型衍生物）基团取代。这些化合物在需要在某些nAChR亚型选择性相互作用的治疗应用中是有益的。也就是说，化合物调节某些nAChR亚型的活性，特别是a7 nAChR亚型，并且对毒蕈碱受体没有明显的活性。化合物的放射性标记版本可用于诊断方法。

8. 发明申请

WO2005037832A3 AZABICYCYCLIC COMPOUNDS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
公开(公告)号：WO2005037832A3
公开(公告)日：2005-04-28
申请号：PCT/US2004/034051
申请日：2004-10-15
申请人： TARGACEPT, INC. , BREINING, Scott R. , BHATTI, Balwinder S. , HAWKINS, Gregory D. , MIAO, Lan , MAZUROV, Anatoly , PHILLIPS, Teresa Y. , MILLER, Craig H.
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： 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.

9. 发明申请

WO2013028587A1 1,4-DIAZABICYCLO[3.2.2]NONANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 审中-公开
标题翻译： 1,4-DIAZABICYCLO [3.2.2] NONANES作为神经烯醇类乙酰胆碱受体配体
公开(公告)号：WO2013028587A1
公开(公告)日：2013-02-28
申请号：PCT/US2012/051518
申请日：2012-08-20
申请人： TARGACEPT, INC. , MAZUROV, Anatoly A. , MIAO, Lan , SHOWALTER, Todd
发明人： MAZUROV, Anatoly A. , MIAO, Lan , SHOWALTER, Todd
IPC分类号： C07D498/04 , A61K31/551 , A61P25/00
CPC分类号： C07D519/00 , A61K31/551 , C07D498/04
摘要： The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (CNS).
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法，含有这些化合物的药物组合物的化合物，以及使用这些化合物治疗各种各样的病症和疾病的方法，包括与中枢神经系统（CNS）功能障碍相关的炎性疾病和疾病。

10. 发明申请

WO2010028033A1 AMIDES OF DIAZABICYCLOOCTANES AND USES THEREOF 审中-公开
标题翻译：双酚A的氨基酸及其用途
公开(公告)号：WO2010028033A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/055718
申请日：2009-09-02
申请人： TARGACEPT, INC. , STRACHAN, Jon-Paul , BHATTI, Balwinder Singh , MAZUROV, Anatoly , KLUCIK, Jozef , XIAO, Yun-De , HAMMOND, Philip S. , KOMBO, David , MIAO, Lan , SPEAKE, Jason Daniel , YOHANNES, Daniel
发明人： STRACHAN, Jon-Paul , BHATTI, Balwinder Singh , MAZUROV, Anatoly , KLUCIK, Jozef , XIAO, Yun-De , HAMMOND, Philip S. , KOMBO, David , MIAO, Lan , SPEAKE, Jason Daniel , YOHANNES, Daniel
IPC分类号： C07D471/08 , A61K31/407 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to compounds of the following formulae I and II that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). Formula (I ), Formula (Il)
摘要翻译：本发明涉及结合并调节神经元烟碱乙酰胆碱受体的活性，制备这些化合物的方法，含有这些化合物的药物组合物的下式I和II的化合物，以及使用这些化合物治疗各种各样的病症和疾病，包括与中枢神经系统（CNS）功能障碍有关的疾病。式（I），式（II）

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