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1.发明申请Sigma Ligands For the Prevention or Treatment of Pain Induced by Chemotherapy 审中-公开Sigma配体用于预防或治疗化疗引起的疼痛公开(公告)号：US20160220575A1
公开(公告)日：2016-08-04
申请号：US15093589
申请日：2016-04-07
申请人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
发明人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
IPC分类号： A61K31/5377
CPC分类号： A61K31/5377 , A61K31/337 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.
摘要翻译： 本发明涉及使用式（I）的Sigma配体来预防或治疗由化学治疗剂诱导的疼痛，特别是由紫杉烷类，长春花生物碱或含铂化疗药引起的疼痛。
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公开(公告)号：US20160199380A1
公开(公告)日：2016-07-14
申请号：US15073460
申请日：2016-03-17
申请人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
发明人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
IPC分类号： A61K31/5377 , A61K31/337 , A61K33/24 , A61K45/06
CPC分类号： A61K31/5377 , A61K31/337 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.
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3.发明申请SIGMA LIGANDS FOR THE PREVENTION OR TREATMENT OF PAIN INDUCED BY CHEMOTHERAPY 审中-公开用于预防或治疗由化疗引起的疼痛的SIGMA配偶公开(公告)号：US20120141606A1
公开(公告)日：2012-06-07
申请号：US13389733
申请日：2010-08-12
申请人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
发明人： José Manuel Baeyens-Cabrera , Helmut Heinrich Buschmann , José Miguel Vela Hernández , Daniel Zamanillo-Castanedo , Francisco-Rafael Nieto-López
IPC分类号： A61K31/4152 , A61K31/4155 , A61K31/454 , A61K31/4178 , A61P35/00 , A61K31/496 , A61K31/541 , A61K33/24 , A61K31/475 , A61K31/69 , A61K31/5377 , A61K31/4545
CPC分类号： A61K31/5377 , A61K31/337 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.
摘要翻译： 本发明涉及使用式（I）的Sigma配体来预防或治疗由化学治疗剂诱导的疼痛，特别是由紫杉烷类，长春花生物碱或含铂化疗药引起的疼痛。
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4.发明申请1-ARYL-3-AMINOALKOXY PYRAZOLES AS SIGMA LIGANDS ENHANCING ANALGESIC EFFECT OF OPIOIDS AND ATTENUATING THE DEPENDENCY THEREOF 有权1-ARYL-3-AMINOALKOXY PYRAZOLES作为SIGMA配体，增强了光合作用的有效作用并使其丧失依赖性公开(公告)号：US20110112095A1
公开(公告)日：2011-05-12
申请号：US12988951
申请日：2009-04-24
IPC分类号： A61K31/5377 , A61K31/485 , A61P25/36
CPC分类号： C07D231/22 , A61K31/4152 , A61K31/4155 , A61K31/485 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , A61K2300/00
摘要： The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.
摘要翻译： 本发明涉及一组式（I）的σ受体配体用于增强阿片样物质和阿片剂的镇痛作用，同时降低它们引起的依赖性。
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5.发明授权1-aryl-3-aminoalkoxy pyrazoles as sigma ligands enhancing analgesic effect of opioids and attenuating the dependency thereof 有权1-芳基-3-氨基烷氧基吡唑作为西格玛配体增强阿片样物质的镇痛作用并减弱其依赖性公开(公告)号：US08877753B2
公开(公告)日：2014-11-04
申请号：US12988951
申请日：2009-04-24
IPC分类号： A61K31/4152 , A61K31/4155 , A61K31/485 , A61K31/5377 , A61P25/36 , C07D231/22 , C07D401/12 , C07D403/12 , C07D471/04 , A61K45/06
CPC分类号： C07D231/22 , A61K31/4152 , A61K31/4155 , A61K31/485 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , A61K2300/00
摘要： The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.
摘要翻译： 本发明涉及一组式（I）的σ受体配体用于增强阿片样物质和阿片剂的镇痛作用，同时降低它们引起的依赖性。
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公开(公告)号：US20110257134A1
公开(公告)日：2011-10-20
申请号：US13124027
申请日：2009-10-16
申请人： Helmut Heinrich Buschmann , Lluis Sola Carandell , Jordi Benet Buchholz , Jordi Carles Ceron Bertran , Carlos Ramon Plata Salaman , Nicolas Tesson
发明人： Helmut Heinrich Buschmann , Lluis Sola Carandell , Jordi Benet Buchholz , Jordi Carles Ceron Bertran , Carlos Ramon Plata Salaman , Nicolas Tesson
IPC分类号： A61K31/135 , A61P25/04 , A61P29/00 , A61K31/192 , A61K31/63
CPC分类号： A61K31/635 , A61K9/16 , A61K31/135 , A61K31/137 , A61K31/192 , A61K45/06 , C07B2200/13 , C07C59/64 , C07C217/74 , C07C2601/14 , C07D231/12 , A61K2300/00
摘要： The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same, their uses in pharmaceutical formulations, and for the treatment of various disorders, including pain.
摘要翻译： 本发明涉及选自NSAIDs的曲马多和共晶体形成剂的共晶体，其制备方法，其在药物制剂中的用途以及用于治疗各种疾病，包括疼痛的共晶体。
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7.发明申请SALTS OF TRAMADOL AND IBUPROFEN AND THEIR CRYSTAL FORM IN THE TREATMENT OF PAIN 审中-公开TRAMADOL和IBUPROFEN及其在治疗疼痛中的晶体形态的研究公开(公告)号：US20110178174A1
公开(公告)日：2011-07-21
申请号：US13056250
申请日：2009-07-30
申请人： Helmut Heinrich Buschmann , Lluis Sola Caranedell l.n. , Jordi Benet Buchholz , Jordi Carles Ceron Bertran
发明人： Helmut Heinrich Buschmann , Lluis Sola Caranedell l.n. , Jordi Benet Buchholz , Jordi Carles Ceron Bertran
IPC分类号： A61K31/205 , C07C57/30 , A61P29/00
CPC分类号： C07C57/30 , A61K31/135 , A61K31/192 , C07B2200/07 , C07B2200/13 , C07C51/487 , C07C217/74 , C07C2601/14 , A61K2300/00
摘要： The present invention relates to salts and compositions of tramadol and ibuprofen, their crystal form, processes for preparation of the same and their uses for the treatment of pain.
摘要翻译： 本发明涉及曲马多和布洛芬的盐和组合物，它们的晶体形式，其制备方法及其用于治疗疼痛的用途。
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8.发明申请Crystalline Modifications of 6-Dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol 审中-公开6-二甲基氨基甲基-1-（3-甲氧基苯基） - 环己烷-1,3-二醇的结晶改性公开(公告)号：US20110060053A1
公开(公告)日：2011-03-10
申请号：US12880614
申请日：2010-09-13
IPC分类号： A61K31/135 , C07C217/74 , A61P29/00
CPC分类号： C07C217/74 , C07B2200/13
摘要： Crystalline modifications of (1R,3R,6R)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol, (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol and mixtures thereof, pharmaceutical compositions and medicaments comprising these modifications, the use of these modifications as well as to a process for the enrichment of (1R,3R,6R)- or (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol.
摘要翻译： （1R，3R，6R）-6-二甲基氨基甲基-1-（3-甲氧基苯基） - 环己烷-1,3-二醇，（1S，3S，6S）-6-二甲基氨基甲基-1-（3-甲氧基苯基） - 环己烷-1,3-二醇及其混合物，包含这些修饰的药物组合物和药物，这些修饰的用途以及富集（1R，3R，6R） - 或（1S，3S，6S ）-6-二甲基氨基甲基-1-（3-甲氧基苯基） - 环己烷-1,3-二醇。
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9.发明申请SALTS OF TRAMADOL AND NAPROXEN AND THEIR CRYSTAL FORMS IN THE TREATMENT OF PAIN 有权TRAMADOL和NAPROXEN的盐及其在治疗疼痛中的晶体形态公开(公告)号：US20100227927A1
公开(公告)日：2010-09-09
申请号：US12672416
申请日：2008-07-31
申请人： Helmut Heinrich Buschmann , Antoni Torrens-Jover , Josep Mas-Prio , Jordi Benet-Buchholz , Lluis Sola-Carandell , Jordi Carles Ceron-Bertran
发明人： Helmut Heinrich Buschmann , Antoni Torrens-Jover , Josep Mas-Prio , Jordi Benet-Buchholz , Lluis Sola-Carandell , Jordi Carles Ceron-Bertran
IPC分类号： A61K31/195 , C07C59/13 , C07C51/00 , A61P25/00
CPC分类号： C07C217/74 , C07B2200/07 , C07B2200/13 , C07C59/64 , C07C2601/14
摘要： The present invention concerns salts of Tramadol and Naproxen and their crystalline forms, and compositions thereof, for the treatment of pain, as well as their process for preparation.
摘要翻译： 本发明涉及曲马多和萘普生的盐及其结晶形式及其组合物，用于治疗疼痛及其制备方法。
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公开(公告)号：US20100197939A1
公开(公告)日：2010-08-05
申请号：US12669517
申请日：2008-07-17
申请人： Rosa M. Ortuno , Sandra Izquierdo , Helmut Heinrich Buschmann , Antoni Torrens Jover , Monica Garcia Lopez
发明人： Rosa M. Ortuno , Sandra Izquierdo , Helmut Heinrich Buschmann , Antoni Torrens Jover , Monica Garcia Lopez
IPC分类号： C07D405/04 , C07C227/32 , C07D207/26 , C07D207/27 , C07C271/22
CPC分类号： C07D317/20 , C07C227/22 , C07C227/32 , C07D207/267 , C07D207/27 , C07D207/273 , C07D491/056 , C07C229/08
摘要： The invention provides a new enantioselective process for the preparation of (S)-pregabalin, or a pharmaceutical acceptable addition acid salt comprising: acid hydrolysis of the dioxolan ring of a chiral compound of general formula (I) to obtain compound of general formula (II); oxidation of compound (II) to obtain a compound of general formula (III) and transforming compound (III) into compound of general formula (IV); subjecting compound (IV) to basic hydrolysis to obtain a compound of general formula (V) which is reduced to obtain enantiomerically pure S-pregabalin. The invention also provides new chiral intermediates involved in the process.
摘要翻译： 本发明提供了用于制备（S） - 普瑞巴林或一种药学上可接受的加成酸盐的新的对映选择性方法，包括：通式（I）的手性化合物的二氧戊环的酸水解，得到通式（II）的化合物 ）; 化合物（II）的氧化，得到通式（III）的化合物和将化合物（III）转化为通式（IV）的化合物; 使化合物（Ⅳ）进行碱性水解，得到通式（Ⅴ）的化合物，将其还原，得到对映体纯的S-普瑞巴林。 本发明还提供了涉及该方法的新的手性中间体。
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