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    • 1. 发明申请
    • 3-SUBSTITUTED-2(ARYLALKYL)-1- AZABICYCLOALKANES AND METHODS OF USE THEREOF
    • 3-取代-2(芳基)-1-氮杂环丁烷及其使用方法
    • US20080138287A1
    • 2008-06-12
    • US12026847
    • 2008-02-06
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • A61K49/00C07D221/22
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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.
    • 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。
    • 2. 发明授权
    • 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
    • 3-取代-2(芳基烷基)-1-氮杂双环烷烃及其使用方法
    • US06953855B2
    • 2005-10-11
    • US10372642
    • 2003-02-21
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • A61K51/00C07D453/02C07D453/04C07D471/08C07D487/08
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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.
    • 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。
    • 5. 发明授权
    • 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
    • 3-取代-2(芳基烷基)-1-氮杂双环烷烃及其使用方法
    • US07425561B2
    • 2008-09-16
    • US11458231
    • 2006-07-18
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • A61K31/44C07D415/00C07D413/00C07D253/08
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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.
    • 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
    • 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF
    • 3-取代-2(芳基)-1-亚氨基二醇及其使用方法
    • US20100240696A1
    • 2010-09-23
    • US12793773
    • 2010-06-04
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • Anatoly A. MazurovJozef KlucikLan MiaoAngela S. SeamansTeresa Youngpeter PhillipsJeffrey Daniel SchmittCraig Harrison Miller
    • A61K31/46A61P25/18
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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.
    • 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。
    • 7. 发明申请
    • 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF
    • 3-取代-2(芳基)-1-亚氨基二醇及其使用方法
    • US20110071188A1
    • 2011-03-24
    • US12862388
    • 2010-08-24
    • Anatoly A. MazurovJozef KlucikLan Miao
    • Anatoly A. MazurovJozef KlucikLan Miao
    • A61K31/444C07D453/02A61K31/439A61P25/00
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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 C14 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), partidularly 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.
    • 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,并且烷基通常是C 14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)上表现出活性,分散在α7nAChR亚型上,可用于调节神经传递和涉及神经传递的配体的释放。 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。
    • 9. 发明申请
    • 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF
    • 3-取代-2(芳基)-1-亚氨基二醇及其使用方法
    • US20110071187A1
    • 2011-03-24
    • US12862373
    • 2010-08-24
    • Anatoly A. MazurovJozef KlucikLan Miao
    • Anatoly A. MazurovJozef KlucikLan Miao
    • A61K31/439C07D453/02A61P25/00A61K31/4545
    • C07D471/08A61K51/0455C07D453/02C07D487/08
    • 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.
    • 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。