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1. 发明申请

US20100284913A1 Methods and compositions for studying, imaging, and treating pain 有权
标题翻译：用于研究，成像和治疗疼痛的方法和组合物
公开(公告)号：US20100284913A1
公开(公告)日：2010-11-11
申请号：US12800053
申请日：2010-05-07
申请人： Justin Du Bois , John Mulcahy , Brian Andresen , David C. Yeomans , Sandip Biswal
发明人： Justin Du Bois , John Mulcahy , Brian Andresen , David C. Yeomans , Sandip Biswal
IPC分类号： A61K51/04 , C07D487/14 , C07K16/00 , C07K14/00 , C07H21/04 , A61K31/519 , A61K47/48 , A61K38/02 , A61P1/00 , A61P13/00 , A61P25/00 , A61P25/08 , A61P29/00 , A61K49/16 , A61K49/14 , A61K49/12 , A61K49/10 , A61K38/43 , A61P17/00 , A61K31/58 , C12N9/96
CPC分类号： C07D487/16 , A61K8/4953 , A61K49/0002 , A61K49/0004 , A61K49/0032 , A61K49/0052 , A61K51/0459 , A61Q19/02 , A61Q19/08 , C07D487/14
摘要： Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a saxitoxin analogue compound, or a pharmaceutically acceptable salt, isomer, tautomer or prodrug thereof, whereby pain in said subject is alleviated.
摘要翻译：提供了类似萨克西汀类似物，组合物，药物组合物，合成硫氧还蛋白类似物的方法，成像方法，治疗方法，包括治疗疼痛的方法。沙眼毒素（STX），戈毒毒素（GTX）和泽西酮毒素，和变体STX化合物结合钠通道，并有效减少或阻断钠离子通过这些通道的流动。这种通道阻滞影响神经和肌肉的作用，并且可以有效地减少或阻止疼痛感觉，放松肌肉，减少肌肉痉挛和减少皱纹。与钠通道的STX类似物结合也可用于定位，成像或标记钠通道，因此可用于研究钠通道和钠通道障碍，以及用于诊断和治疗患有钠通道障碍的患者。在实施方案中，变体STX化合物包括与施用于受试者时相比于STX相比具有增加的血清半衰期的结合物。在实施方案中，本公开提供了一种减轻需要治疗的受试者的疼痛的方法，所述方法包括向受试者施用有效量的沙克西毒素类似物化合物或其药学上可接受的盐，异构体，互变异构体或前药，由此所述受试者的疼痛缓解。

2. 发明申请

US20180230178A1 CYCLIC DI-NUCLEOTIDE COMPOUNDS AS STING AGONISTS 审中-公开
公开(公告)号：US20180230178A1
公开(公告)日：2018-08-16
申请号：US15752144
申请日：2016-08-11
申请人： Michael D. ALTMAN , Brian ANDRESEN , Wonsuk CHANG , Matthew Lloyd CHILDERS , Jared N. CUMMING , Andrew Marc HAIDLE , Timothy J. HENDERSON , James P. JEWELL , Min LU , Alan B. NORTHRUP , Ryan D. OTTE , Tony SIU , Benjamin Wesley TROTTER , Quang T TRUONG , Merck Sharp & Dohme Corp.
发明人： Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
IPC分类号： C07H21/04 , C07H21/02 , C07H19/23 , C07H19/20 , A61P35/00
摘要： A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

3. 发明申请

US20050233085A1 Method for preparing a solid phase microextraction device using aerogel 失效
标题翻译：使用气凝胶制备固相微萃取装置的方法
公开(公告)号：US20050233085A1
公开(公告)日：2005-10-20
申请号：US11146562
申请日：2005-06-06
申请人： Fred Miller , Brian Andresen
发明人： Fred Miller , Brian Andresen
IPC分类号： B01D15/00 , B01J20/28 , B01J20/32 , B05D1/12 , B05D3/02 , B05D7/00 , G01N1/40 , G01N30/00
CPC分类号： B01J20/28026 , B01J20/28019 , B01J20/28033 , B01J20/28047 , B01J20/3204 , B01J20/3206 , B01J20/3236 , B01J20/3289 , B01J20/3295 , B01J2220/64 , G01N1/40 , G01N1/405 , G01N2030/009 , Y10T436/255
摘要： A sample collection substrate of aerogel and/or xerogel materials bound to a support structure is used as a solid phase microextraction (SPME) device. The xerogels and aerogels may be organic or inorganic and doped with metals or other compounds to target specific chemical analytes. The support structure is typically formed of a glass fiber or a metal wire (stainless steel or kovar). The devices are made by applying gel solution to the support structures and drying the solution to form aerogel or xerogel. Aerogel particles may be attached to the wet layer before drying to increase sample collection surface area. These devices are robust, stable in fields of high radiation, and highly effective at collecting gas and liquid samples while maintaining superior mechanical and thermal stability during routine use. Aerogel SPME devices are advantageous for use in GC/MS analyses due to their lack of interfering background and tolerance of GC thermal cycling.
摘要翻译：使用与支持结构结合的气凝胶和/或干凝胶材料的样品收集基质作为固相微萃取（SPME）装置。干凝胶和气凝胶可以是有机的或无机的，并掺杂有金属或其他化合物以靶向特定的化学分析物。支撑结构通常由玻璃纤维或金属线（不锈钢或科瓦）形成。通过将凝胶溶液施加到支撑结构并干燥溶液以形成气凝胶或干凝胶来制备装置。在干燥之前，气凝胶颗粒可附着在湿层上以增加样品收集表面积。这些设备在高辐射领域是稳健的，稳定的，并且在采集气体和液体样品时非常有效，同时在常规使用过程中保持优异的机械和热稳定性。由于气凝胶SPME设备缺乏GC热循环的干扰背景和耐受性，气相色谱仪器在GC / MS分析中是有利的。

4. 发明授权

US09174999B2 Methods and compositions for studying, imaging, and treating pain 有权
标题翻译：用于研究，成像和治疗疼痛的方法和组合物
公开(公告)号：US09174999B2
公开(公告)日：2015-11-03
申请号：US12800053
申请日：2010-05-07
申请人： Justin Du Bois , John Mulcahy , Brian Andresen , David C. Yeomans , Sandip Biswal
发明人： Justin Du Bois , John Mulcahy , Brian Andresen , David C. Yeomans , Sandip Biswal
IPC分类号： C07D487/14
CPC分类号： C07D487/16 , A61K8/4953 , A61K49/0002 , A61K49/0004 , A61K49/0032 , A61K49/0052 , A61K51/0459 , A61Q19/02 , A61Q19/08 , C07D487/14
摘要： Saxitoxin analog compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogs, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analog binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a saxitoxin analog compound, or a pharmaceutically acceptable salt, isomer, tautomer or prodrug thereof, whereby pain in said subject is alleviated.
摘要翻译：提供萨克西汀类似物，组合物，药物组合物，合成沙星毒素类似物的方法，成像方法，治疗方法，包括治疗疼痛的方法。沙眼毒素（STX），戈毒毒素（GTX）和泽西酮毒素，和变体STX化合物结合钠通道，并有效减少或阻断钠离子通过这些通道的流动。这种通道阻滞影响神经和肌肉的作用，并且可以有效地减少或阻止疼痛感觉，放松肌肉，减少肌肉痉挛和减少皱纹。与钠通道的STX类似物结合也可用于定位，成像或标记钠通道，因此可用于研究钠通道和钠通道障碍，以及用于诊断和治疗患有钠通道障碍的患者。在实施方案中，变体STX化合物包括与施用于受试者时相比于STX相比具有增加的血清半衰期的结合物。在实施方案中，本公开提供了一种减轻需要治疗的受试者的疼痛的方法，所述方法包括向受试者施用有效量的沙克西毒素类似物化合物或其药学上可接受的盐，异构体，互变异构体或前药，由此所述受试者的疼痛缓解。

5. 发明授权

US10738074B2 Cyclic di-nucleotide compounds as STING agonists 有权
公开(公告)号：US10738074B2
公开(公告)日：2020-08-11
申请号：US15752144
申请日：2016-08-11
申请人： Merck Sharp & Dohme Corp. , Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
发明人： Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
IPC分类号： A01N43/04 , A61K31/70 , C07H21/04 , C07H21/02 , A61K39/39 , C07H19/20 , C07H19/23 , C07H21/00 , A61P35/00 , A61K31/7064 , A61K31/7084 , A61K31/708 , A61K31/706 , A61K31/7076
摘要： A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

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