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81. 发明授权

US07662808B2 Diazabicyclic aryl derivatives as cholinergic receptor modulators 失效
标题翻译：二氮杂双环芳基衍生物作为胆碱能受体调节剂
公开(公告)号：US07662808B2
公开(公告)日：2010-02-16
申请号：US10586836
申请日：2005-02-01
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B Timmermann
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Tino Dyhring Jørgensen , Daniel B Timmermann
IPC分类号： A01N43/00 , A61K31/33 , C07D487/00
CPC分类号： C07D471/08
摘要： This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemicals substances.
摘要翻译：本发明涉及新的二氮杂双环芳基衍生物，其在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

82. 发明申请

US20090186880A1 NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONANE DERIVATIVES AND THEIR MEDICAL USE 审中-公开
公开(公告)号：US20090186880A1
公开(公告)日：2009-07-23
申请号：US12299594
申请日：2007-05-21
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jeppe Kejser Christensen , Tino Dyhring
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jeppe Kejser Christensen , Tino Dyhring
IPC分类号： A61K31/551 , C07D487/08
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

83. 发明申请

US20090118266A1 NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL OXADIAZOLYL DERIVATIVES AND THEIR MEDICAL USE 有权
标题翻译：新的1,4-二氮杂双环[3.2.2]壬基氧杂环丁烷衍生物及其医疗用途
公开(公告)号：US20090118266A1
公开(公告)日：2009-05-07
申请号：US12300060
申请日：2007-05-29
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel
IPC分类号： A61K31/5513 , C07D471/08 , A61P25/28 , A61P25/00 , A61P25/36 , A61P25/34 , A61P25/32 , A61P9/12 , A61P17/06 , A61P17/10 , A61P17/00 , A61P15/12 , A61P15/10 , A61P15/06 , A61P11/06 , A61P1/00 , A61P25/14 , A61P25/24 , A61P25/18 , A61P25/22 , A61P25/06
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors.Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新的1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

84. 发明申请

US20090099153A1 NOVEL 8,10-DIAZA-BICYCLO[4.3.1]DECANE DERIVATIVES AND THEIR MEDICAL USE 失效
标题翻译： 8,10-DIAZA-BICYCLO [4.3.1]丹宁衍生物及其医疗用途
公开(公告)号：US20090099153A1
公开(公告)日：2009-04-16
申请号：US12298290
申请日：2007-05-21
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jeppe Kejser Christensen , Tino Dyhring
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jeppe Kejser Christensen , Tino Dyhring
IPC分类号： A61K31/55 , C07D487/08
CPC分类号： C07D487/08
摘要： This invention relates to novel 8,10-diaza-bicyclo[4.3.1]decane derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新的8,10-二氮杂 - 双环[4.3.1]癸烷衍生物，其在烟碱乙酰胆碱受体中被发现是胆碱能配体。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

85. 发明申请

US20080242668A1 Dimeric Azacyclic Compounds and Their Use 失效
标题翻译：二甲基偶氮化合物及其用途
公开(公告)号：US20080242668A1
公开(公告)日：2008-10-02
申请号：US10586838
申请日：2005-02-01
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Daniel B. Timmermann
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Daniel B. Timmermann
IPC分类号： A61K31/498 , C07D221/02 , A61K31/4375 , A61P9/00 , A61P29/00 , A61P25/00 , C07D403/02
摘要： This invention relates to azacyclic derivatives according of formula (I) and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or. disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the′ termination of abuse of chemical substances. Formula (I) Aza-X′-A′-Y′-L-Y-A″-X″-Aza Aza:Azabicyclic group A′,A″:Aromatic monocyclic and/or polycyclic, carbocyclic and/or heterocyclic group Y′,Y″: Linker or absent (covalent bond) L: Monocyclic or polycyclic, carbocyclic or heterocyclic group or is absent X′,X″: Linker or absent (covalent bond)
摘要翻译：本发明涉及式（I）的氮杂环十二烷基衍生物及其作为药物的用途。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或疾病，疾病或。与“终止化学物质的滥用”引起的与炎症，疼痛和戒断症状有关的神经变性，疾病或病症相关的疾病。式（I）Aza-X'-A'-Y'-LY-A“-X” - 氮杂氮杂：氮杂双环基A'，A“：芳族单环和/或多环，碳环和/或杂环基 Y'，Y“：连接体或不存在（共价键）L：单环或多环，碳环或杂环基团或不存在X'，X”：连接基或不存在（共价键）

86. 发明申请

US20080227772A1 Diazabicyclic Aryl Derivatives as Nicotinic Acetylcholine Receptor Ligands 审中-公开
标题翻译：二氮杂双环衍生物作为烟碱乙酰胆碱受体配体
公开(公告)号：US20080227772A1
公开(公告)日：2008-09-18
申请号：US10586749
申请日：2005-02-01
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Philip K. Ahring , Daniel B. Timmermann
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Ostergaard Nielsen , Tino Dyhring Jorgensen , Philip K. Ahring , Daniel B. Timmermann
IPC分类号： A61K31/551 , C07D243/10 , A61P1/00 , A61P25/02 , A61P29/00 , A61P37/02
CPC分类号： C07D471/08 , C07D487/08
摘要： This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及在尼古丁乙酰胆碱受体中被发现是胆碱能配体的新的二氮杂双环芳基衍生物。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

87. 发明授权

US07332507B2 3-substituted quinuclidines and their use 失效
标题翻译： 3-取代的奎宁和它们的用途
公开(公告)号：US07332507B2
公开(公告)日：2008-02-19
申请号：US10512570
申请日：2003-05-27
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Philip K. Ahring , Tino Dyhring Jørgensen
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Philip K. Ahring , Tino Dyhring Jørgensen
IPC分类号： A01N43/90 , A61K31/44 , C07D453/02
CPC分类号： C07D453/02
摘要： This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新的3-取代的奎宁环衍生物，其被发现是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

88. 发明授权

US06680314B2 Azacyclooctane and heptane derivatives, their preparation and use in therapy 失效
标题翻译：氮杂环辛烷和庚烷衍生物，其制备和用于治疗
公开(公告)号：US06680314B2
公开(公告)日：2004-01-20
申请号：US10134498
申请日：2002-04-30
申请人： Dan Peters , Gunnar M. Olsen , Simon F. Nielsen , Elsebet O. Nielsen
发明人： Dan Peters , Gunnar M. Olsen , Simon F. Nielsen , Elsebet O. Nielsen
IPC分类号： A61K3155
CPC分类号： C07D401/04 , C07D223/06 , C07D225/02
摘要： Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group. The compounds, enantiomers, and salts are useful as ligands for nicotinic ACh receptors.
摘要翻译：式（1）或（2）的化合物，其对映异构体，其混合物及其药学上可接受的盐：其中：n为0或1; R是氢，烷基，烯基，炔基，环烷基，环烷基烷基，芳基或芳烷基; 并且R 1为任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基或单环5至或者R是任选被烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN取代的单环5至6元杂芳基，氨基，硝基，芳基或单环5至6元杂芳基，或R为由与苯环稠合的单环5至6元杂芳基组成的双环杂芳基，任选被烷基，环烷基，环烷基烷基烯基炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基或单环5至6元杂芳基。化合物，对映体和盐可用作烟碱型ACh受体的配体。

89. 发明授权

US06420395B1 Azacyclooctane and heptane derivatives, their preparation and use in therapy 失效
标题翻译：氮杂环辛烷和庚烷衍生物，其制备和用于治疗
公开(公告)号：US06420395B1
公开(公告)日：2002-07-16
申请号：US09450636
申请日：1999-11-29
申请人： Dan Peters , Gunnar M. Olsen , Simon F. Nielsen , Elsebet O. Nielsen
发明人： Dan Peters , Gunnar M. Olsen , Simon F. Nielsen , Elsebet O. Nielsen
IPC分类号： A61K3144
CPC分类号： C07D401/04 , C07D223/06 , C07D225/02
摘要： The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3. CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group, or a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring and which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group. The compounds of the invention are useful as nicotinic ACh receptor ligands.
摘要翻译：本发明公开了式（1）或（2）的化合物，其任何对映体或其任何混合物或其药学上可接受的盐; 其中n为0或1; R是氢，烷基，烯基，炔基，环烷基，环烷基，芳基或芳烷基; 并且R 1是可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基的取代基取代一次或多次的芳基，硝基，芳基和单环5至6元杂芳基，可以被选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3。 CN，氨基，硝基，芳基和单环5至6元杂芳基，或由与苯环稠合的单环5至6元杂芳基组成的双环杂芳基，其可以被取代基取代一次或多次选自烷基，环烷基，环烷基烷基烯基，炔基，烷氧基，环烷氧基，硫代烷氧基，硫代环烷氧基，亚甲二氧基，芳氧基，卤素，CF 3，OCF 3，CN，氨基，硝基，芳基和单环5至6元杂芳基。本发明的化合物可用作烟碱ACh受体配体。

90. 发明授权

US08372832B2 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl compounds and their medical use 有权
标题翻译： 1,4-二氮杂双环[3.2.2]壬基恶二唑基化合物及其医疗用途
公开(公告)号：US08372832B2
公开(公告)日：2013-02-12
申请号：US13420071
申请日：2012-03-14
申请人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jens Damsgaard Mikkelsen , Henrik Björk Hansen , John Paul Redrobe , Jeppe Kejser Christensen , Tino Dyhring
发明人： Dan Peters , Gunnar M. Olsen , Elsebet Østergaard Nielsen , Daniel B. Timmermann , Steven Charles Loechel , Jens Damsgaard Mikkelsen , Henrik Björk Hansen , John Paul Redrobe , Jeppe Kejser Christensen , Tino Dyhring
IPC分类号： A61P25/00 , A61K31/551 , C07D471/08
CPC分类号： C07D471/08
摘要： This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters.Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
摘要翻译：本发明涉及新的1,4-二氮杂 - 双环[3.2.2]壬基恶二唑基衍生物及其在制备药物组合物中的用途。发现本发明的化合物是烟碱乙酰胆碱受体的胆碱能配体和单胺受体和转运蛋白的调节剂。由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

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