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1. 发明授权

US08063068B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US08063068B2
公开(公告)日：2011-11-22
申请号：US12348605
申请日：2009-01-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D401/02 , A61K31/351
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

2. 发明申请

US20110105548A1 N-ARYL DIAZASPIROCYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 审中-公开
标题翻译： N-ARYL DIAZASPIROCYCLIC化合物及其制备和使用方法
公开(公告)号：US20110105548A1
公开(公告)日：2011-05-05
申请号：US12986494
申请日：2011-01-07
申请人： Balwinder S. Bhatti , Craig Harrison Miller , Jeffrey Daniel Schmitt
发明人： Balwinder S. Bhatti , Craig Harrison Miller , Jeffrey Daniel Schmitt
IPC分类号： A61K31/438 , A61P25/00
CPC分类号： C07D487/20 , C07D453/02 , C07D471/10 , C07D471/20 , C07D487/10
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。化合物是N-芳基二氮杂螺环化合物，N-杂芳基二氮杂螺环化合物的桥连类似物，或这些化合物的前药或代谢物。芳基可以是五元或六元杂环（杂芳基）。化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。化合物和组合物也可用于缓解疼痛。化合物可以：（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（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以及对骨骼肌的显着影响）。

3. 发明授权

US07897611B2 Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders 失效
标题翻译：用于缓解疼痛和治疗中枢神经系统疾病的药物组合物和方法
公开(公告)号：US07897611B2
公开(公告)日：2011-03-01
申请号：US12714014
申请日：2010-02-26
申请人： Balwinder Singh Bhatti , Scott R. Breining , Gregory D. Hawkins , Anatoly Mazurov , Lan Miao , Craig Harrison Miller , Teresa Y. Phillips
发明人： Balwinder Singh Bhatti , Scott R. Breining , Gregory D. Hawkins , Anatoly Mazurov , Lan Miao , Craig Harrison Miller , Teresa Y. Phillips
IPC分类号： A61K31/439 , C07D221/22
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。

4. 发明申请

US20100240696A1 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF 有权
标题翻译： 3-取代-2（芳基）-1-亚氨基二醇及其使用方法
公开(公告)号：US20100240696A1
公开(公告)日：2010-09-23
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： A61K31/46 , A61P25/18
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。

5. 发明申请

US20100010042A1 ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 有权
公开(公告)号：US20100010042A1
公开(公告)日：2010-01-14
申请号：US12348605
申请日：2009-01-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： A61K31/454 , A61K31/4545 , C07D401/02 , A61P25/00 , A61P1/00
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

6. 发明授权

US06531606B1 Pharmaceutical compositions incorporating aryl substituted olefinic amine compounds 失效
标题翻译：含有芳基取代烯属胺化合物的药物组合物
公开(公告)号：US06531606B1
公开(公告)日：2003-03-11
申请号：US08804250
申请日：1997-02-21
申请人： Gary Maurice Dull , William Scott Caldwell , Grayland Page Dobson , Craig Harrison Miller
发明人： Gary Maurice Dull , William Scott Caldwell , Grayland Page Dobson , Craig Harrison Miller
IPC分类号： C07D21172
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61
摘要： Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds include (E)-N-methyl-4-[3-(5-benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.
摘要翻译：通过施用有效量的芳基取代的烯烃胺化合物来治疗患有中枢神经系统疾病（例如阿尔茨海默氏病，帕金森氏病，图雷特综合征，注意力缺陷障碍或精神分裂症）的患者。示例性化合物包括（E）-N-甲基-4- [3-（5-苄氧基吡啶）基] -3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-苯氧基吡啶）吡啶-3-基] -3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-异丙氧基吡啶）基] -3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-甲氧基甲基吡啶）基] -3-丁烯-1-胺和（E）-N-甲基-4- [3-（5-苯基吡啶）基] -3-丁烯-1-胺。

7. 发明授权

US06440970B1 Pharmaceutical compositions and methods for use 失效
标题翻译：药物组合物和使用方法
公开(公告)号：US06440970B1
公开(公告)日：2002-08-27
申请号：US09578768
申请日：2000-05-25
申请人： Thomas Jeffrey Clark , Gary Maurice Dull , Dwo Lynm , Lan Miao , Craig Harrison Miller , Jeffrey Daniel Schmitt
发明人： Thomas Jeffrey Clark , Gary Maurice Dull , Dwo Lynm , Lan Miao , Craig Harrison Miller , Jeffrey Daniel Schmitt
IPC分类号： C07D48708
CPC分类号： C07D487/08
摘要： The present invention relates to diazabicyclic compounds, and preferably N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl diazabicyclic compounds, such as (1S,4S)-2-(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-pyrimidinyl)-2,5-diazabicyclo[2.2.1]heptane and (1S,4S)-2-(6-chloro-3-pyridazinyl)-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-（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-嘧啶基）-2,5-二氮杂双环[2.2.1]庚烷和（1S，4S）-2-（6-氯-3-哒嗪基）-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。

8. 发明授权

US08153821B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08153821B2
公开(公告)日：2012-04-10
申请号：US13130954
申请日：2009-11-30
申请人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Timothy J. Cuthbertson , Craig Harrison Miller , Joseph Pike Mitchener, Jr.
发明人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Timothy J. Cuthbertson , Craig Harrison Miller , Joseph Pike Mitchener, Jr.
IPC分类号： C07D207/12 , A61K31/40
CPC分类号： A61K31/4439 , C07D405/14
摘要： The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, 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化合物，其新型盐，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多种的病症和障碍，包括与中枢神经系统（CNS）功能障碍相关的疾病。

9. 发明申请

US20110281895A1 SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-PYRROLIDIN-3YLVINYL)PYRIMIDINE 有权
标题翻译： -5 - （（E）-2-吡咯烷-3-基]乙烯基）吡咯烷酮的合成和新型盐形式
公开(公告)号：US20110281895A1
公开(公告)日：2011-11-17
申请号：US13129898
申请日：2009-11-30
申请人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Timothy J. Cuthbertson , Gary Maurice Dull , Craig Harrison Miller , Joseph Pike Mitchener, JR. , Julio A. Munoz , Pieter Albert Otten
发明人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Timothy J. Cuthbertson , Gary Maurice Dull , Craig Harrison Miller , Joseph Pike Mitchener, JR. , Julio A. Munoz , Pieter Albert Otten
IPC分类号： A61K31/506 , A61P1/10 , A61P1/00 , C07D401/06
CPC分类号： C07D403/06
摘要： The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
摘要翻译：本发明涉及（R）-5 - （（E）-2-吡咯烷-3-基）嘧啶的立体有择合成，新的盐形式，以及这些盐的新型多晶形式。

10. 再颁专利

USRE41439E1 Pharmaceutical compositions and methods for use 失效
标题翻译：药物组合物和使用方法
公开(公告)号：USRE41439E1
公开(公告)日：2010-07-13
申请号：US11702484
申请日：2007-02-05
申请人： Craig Harrison Miller , Gary Maurice Dull , Lan Miao , Dwo Lynm , Jeffrey Daniel Schmitt , Thomas Jeff Clark
发明人： Craig Harrison Miller , Gary Maurice Dull , Lan Miao , Dwo Lynm , Jeffrey Daniel Schmitt , Thomas Jeff Clark
IPC分类号： C07D487/08 , C07D209/00 , A61K31/40 , A61P25/00
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。

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