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1. 发明授权

US08859609B2 Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes 有权
标题翻译：烟碱乙酰胆碱受体亚型二氮杂双环烷烃选择性酰胺
公开(公告)号：US08859609B2
公开(公告)日：2014-10-14
申请号：US13342635
申请日：2012-01-03
申请人： Anatoly Mazurov , Lan Miao , Yunde Xiao
发明人： Anatoly Mazurov , Lan Miao , Yunde Xiao
IPC分类号： A61K31/40 , C07D471/08 , 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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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).
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。这些化合物是可以由某些杂芳基羧酸和某些二氮杂双环烷烃制备的酰胺化合物。该化合物对中枢神经系统（CNS）中α4和bgr2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。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不良副作用因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。

2. 发明授权

US08268860B2 Sub-type selective amides of diazabicycloalkanes 失效
标题翻译：二氮杂双环烷烃的亚型选择性酰胺
公开(公告)号：US08268860B2
公开(公告)日：2012-09-18
申请号：US12723790
申请日：2010-03-15
申请人： Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
发明人： Anatoly A. Mazurov , Lan Miao , Yun-De Xiao , Philip S. Hammond , Craig H. Miller , Srinivisa Rao Akireddy , V. Srinivasa Murthy , Regina C. Whitaker , Scott R. Breining , Matt S. Melvin
IPC分类号： A61K43/42 , A01N31/44
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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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).
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。这些化合物是可以由某些杂芳基羧酸和某些二氮杂双环烷烃制备的酰胺化合物。该化合物对中枢神经系统（CNS）中α4和bgr2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。化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示神经保护作用，和（iii）当以有效量使用时，不会产生明显的副作用（例如副作用因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。

3. 发明授权

US08143272B2 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof 有权
公开(公告)号：US08143272B2
公开(公告)日：2012-03-27
申请号：US12636269
申请日：2009-12-11
申请人： Anatoly A. Mazurov , Lan Miao
发明人： Anatoly A. Mazurov , Lan Miao
IPC分类号： A01N43/90 , A61K31/519
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 compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 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.

4. 发明申请

US20080242693A1 Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders 审中-公开
标题翻译：减轻疼痛和治疗中枢性神经系统疾病的药物组合物和方法
公开(公告)号：US20080242693A1
公开(公告)日：2008-10-02
申请号：US12123530
申请日：2008-05-20
申请人： Scott R. Breining , Balwinder S. Bhatti , Gregory D. Hawkins , Lan Miao , Anatoly Mazurov , Craig H. Miller
发明人： Scott R. Breining , Balwinder S. Bhatti , Gregory D. Hawkins , Lan Miao , Anatoly Mazurov , Craig H. Miller
IPC分类号： A61K31/439 , A61P25/30
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.
摘要翻译：特征在于正常神经递质释放（如多巴胺释放（如帕金森综合征，帕金森氏病，图雷特氏综合征，注意缺陷障碍或精神分裂症））改变的中枢神经系统疾病易患或患有疾病的患者是通过施用如本文所述的式1或2的化合物进行治疗。式1和式2化合物也可用于治疗疼痛，治疗药物成瘾，尼古丁成瘾和/或肥胖症。该化合物可作为单独的立体异构体，外消旋混合物，非对映异构体等存在。

5. 发明申请

US20080138287A1 3-SUBSTITUTED-2(ARYLALKYL)-1- AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
标题翻译： 3-取代-2（芳基）-1-氮杂环丁烷及其使用方法
公开(公告)号：US20080138287A1
公开(公告)日：2008-06-12
申请号：US12026847
申请日：2008-02-06
申请人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
发明人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
IPC分类号： A61K49/00 , C07D221/22
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 α7 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，制备化合物的方法和使用该化合物的处理方法。氮杂双环烷烃通常是氮杂双环庚烷，氮杂双环辛烷或氮杂双环壬烷。芳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，并且烷基通常是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，例如酰胺，氨基甲酸酯，脲，硫代酰胺，硫代氨基甲酸酯，硫脲或类似官能团。该化合物在烟碱乙酰胆碱受体（nAChRs），特别是α7nAChR亚型中表现出活性，并且可用于调节神经传递和涉及神经传递的配体释放。还公开了预防或治疗包括中枢神经系统（CNS）病症在内的病症和障碍的方法，其特征在于正常神经传递的改变。还公开了用于治疗炎症，自身免疫疾病，疼痛和过量新生血管形成（例如与肿瘤生长相关的）的方法。

6. 发明申请

US20070197579A1 Heteroaryl-Substituted Diazatricycloalkanes and Methods of Use Thereof 失效
标题翻译：杂芳基取代的二氮杂环烷烃及其使用方法
公开(公告)号：US20070197579A1
公开(公告)日：2007-08-23
申请号：US11465914
申请日：2006-08-21
申请人： Anatoly Mazurov , Lan Miao , Jozef Klucik
发明人： Anatoly Mazurov , Lan Miao , Jozef Klucik
IPC分类号： A61K31/4745 , C07D471/14
CPC分类号： C07D471/18 , C07D471/14
摘要： The present invention relates to amide and urea derivatives of heteroaryl-substituted diazatricycloalkanes, 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 substitutent 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：本发明涉及杂芳基取代的二氮三环环烷烃的酰胺和脲衍生物，包括该化合物的药物组合物，制备该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α7nAChR亚型介导的病症来调节α7nAChR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。取代基杂芳基是直接连接到二氮杂环烷烃上的5-或6-元环杂芳族化合物，例如3-吡啶基和5-嘧啶基部分。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，特别是α7nAChR亚型的活性，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。

7. 发明授权

US06953855B2 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof 有权
标题翻译： 3-取代-2（芳基烷基）-1-氮杂双环烷烃及其使用方法
公开(公告)号：US06953855B2
公开(公告)日：2005-10-11
申请号：US10372642
申请日：2003-02-21
申请人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
发明人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
IPC分类号： A61K51/00 , C07D453/02 , C07D453/04 , C07D471/08 , C07D487/08
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 α7 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，制备化合物的方法和使用该化合物的处理方法。氮杂双环烷烃通常是氮杂双环庚烷，氮杂双环辛烷或氮杂双环壬烷。芳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，并且烷基通常是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，例如酰胺，氨基甲酸酯，脲，硫代酰胺，硫代氨基甲酸酯，硫脲或类似官能团。该化合物在烟碱乙酰胆碱受体（nAChRs），特别是α7nAChR亚型中表现出活性，并且可用于调节神经传递和涉及神经传递的配体释放。还公开了预防或治疗包括中枢神经系统（CNS）病症在内的病症和障碍的方法，其特征在于正常神经传递的改变。还公开了用于治疗炎症，自身免疫疾病，疼痛和过量新生血管形成（例如与肿瘤生长相关的）的方法。

8. 发明授权

US06852721B2 Pharmaceutical compositions and methods for use 有权
标题翻译：药物组合物和使用方法
公开(公告)号：US06852721B2
公开(公告)日：2005-02-08
申请号：US09864905
申请日：2001-05-24
申请人： Craig Harrison Miller , Gary Maurice Dull , Lan Miao , Dwo Lynm , Jeffrey Daniel Schmitt , Thomas Jeffrey Clark
发明人： Craig Harrison Miller , Gary Maurice Dull , Lan Miao , Dwo Lynm , Jeffrey Daniel Schmitt , Thomas Jeffrey Clark
IPC分类号： A61K31/407 , A61K31/439 , A61P25/00 , A61P25/26 , A61P43/00 , C07D471/08 , C07D487/08 , A61K31/40 , C07D209/00
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-pyridinyl 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-thienyl)-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-噻吩基）-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）（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。

9. 发明授权

US08124619B2 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof 有权
公开(公告)号：US08124619B2
公开(公告)日：2012-02-28
申请号：US12862388
申请日：2010-08-24
申请人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao
发明人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao
IPC分类号： A01N43/90 , A61K31/44 , C07D453/02
CPC分类号： C07D471/08 , A61K51/0455 , C07D453/02 , C07D487/08
摘要： The present invention relates to pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the α7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.

10. 发明授权

US08084462B2 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof 有权
标题翻译： 3-取代-2（芳基烷基）-1-氮杂双环烷烃及其使用方法
公开(公告)号：US08084462B2
公开(公告)日：2011-12-27
申请号：US12793773
申请日：2010-06-04
申请人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
发明人： Anatoly A. Mazurov , Jozef Klucik , Lan Miao , Angela S. Seamans , Teresa Youngpeter Phillips , Jeffrey Daniel Schmitt , Craig Harrison Miller
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/08 , A61K51/0455 , C07D453/02 , C07D487/08
摘要： The present invention relates to the pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the α7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
摘要翻译：本发明涉及包含能够影响烟碱乙酰胆碱能受体（nAChR）的化合物的药物组合物，例如作为特定烟碱型受体亚型（特别是α7nAChR亚型）的调节剂。本发明还涉及用于治疗各种各样的病症和疾病的方法，特别是与中枢神经系统和自主神经系统的功能障碍有关的方法。

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