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1. 发明申请

WO2014188266A1 OPIOID KETAL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：洋芋酮化合物及其用途
公开(公告)号：WO2014188266A1
公开(公告)日：2014-11-27
申请号：PCT/IB2014/000876
申请日：2014-05-23
申请人： RHODES TECHNOLOGIES , KUPPER, Robert, J. , GLOWAKY, Raymond, C.
发明人： KUPPER, Robert, J. , GLOWAKY, Raymond, C.
IPC分类号： C07D489/09 , A61K31/485 , C07D491/20
CPC分类号： C07D489/08 , A61K9/0053 , A61K31/485 , A61K45/06 , C07D489/02 , C07D489/09 , C07D491/20
摘要： This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R 1 is H or CH 3 , R 2 is H or OH, n is 0, 1, 2 or 3, R 3 and R 4 are independently H or optionally substituted C 1 -C 4 alkyl, or when n is 0, then R 3 and R 4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C 1 -C 4 alkyl.The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.
摘要翻译：本发明涉及式（I），式（II）或式（III）的阿片样酮缩酮化合物或其药学上可接受的盐，其中R1是H或CH3，R2是H或OH，n是0,1或 2或3中，R 3和R 4独立地为H或任选取代的C 1 -C 4烷基，或者当n为0时，则R 3和R 4以及与它们相连的碳原子一起形成六元或七元环，或被C 1 -C 4烷基二取代。本发明还涉及式（IV）或（V）的羟考酮缩酮化合物：或其药学上可接受的盐。本发明还涉及这些化合物用于治疗，预防或改善疼痛的用途。

2. 发明申请

WO2006133941A2 CANNABINOID ACTIVE PHARMACEUTICAL INGREDIENT FOR IMPROVED DOSAGE FORMS 审中-公开
标题翻译： CANNABINOID活性药物成分用于改善剂型
公开(公告)号：WO2006133941A2
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005761
申请日：2006-06-14
申请人： EURO-CELTIQUE S.A. , KUPPER, Robert, J.
发明人： KUPPER, Robert, J.
IPC分类号： A61K31/352 , A61P29/02 , A61P1/08
CPC分类号： A61K31/353 , A61K31/352
摘要： Pharmaceutical compositions comprising the cannabinoid active pharmaceutical ingredient, crystalline trans-(±)-Δ 9 -tetrahydrocannabinol, and formulations thereof are disclosed. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of crystalline trans-(±)-Δ 9 -tetrahydrocannabinol. In specific embodiments, the crystalline trans-(±)-Δ 9 -tetrahydrocannabinol administered according to the methods for treating or preventing a condition such as pain can have a purity of at least about 98% based on the total weight of cannabinoids.
摘要翻译：公开了包含大麻素活性药物成分，结晶反式（±）-β9-四氢大麻酚和其制剂的药物组合物。本发明还涉及用于治疗或预防诸如疼痛的病症的方法，包括向有需要的患者施用有效量的结晶反式（±）-β9-四氢大麻酚。在具体实施方案中，根据用于治疗或预防诸如疼痛的病症的方法施用的结晶反式 - （±）-Δ9-四氢大麻酚可以具有至少约98％的纯度，基于大麻素的总重量。

3. 发明申请

WO2006094672A1 METHOD OF REDUCING ALPHA, BETA UNSATURATED KETONES IN OPIOID COMPOSITIONS 审中-公开
标题翻译：降低阿片样物质的方法，在阿片组合物中的不饱和度的酮
公开(公告)号：WO2006094672A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/001798
申请日：2006-02-27
申请人： EURO-CELTIQUE S.A. , KUPPER, Robert, J.
发明人： KUPPER, Robert, J.
IPC分类号： C07D487/08
CPC分类号： C07D487/08
摘要： The present invention is directed to a process for reducing the level of α, β- unsaturated ketone in an opioid analgesic composition by hydrogentation with diimide or a diimide progenitor.
摘要翻译：本发明涉及一种通过用二酰亚胺或二酰亚胺祖细胞进行水解来降低阿片类镇痛组合物中β-不饱和酮的含量的方法。

4. 发明申请

WO2006133941A3 CANNABINOID ACTIVE PHARMACEUTICAL INGREDIENT FOR IMPROVED DOSAGE FORMS 审中-公开
标题翻译： CANNABINOID活性药物成分用于改善剂量形式
公开(公告)号：WO2006133941A3
公开(公告)日：2007-03-15
申请号：PCT/EP2006005761
申请日：2006-06-14
申请人： EURO CELTIQUE SA , KUPPER ROBERT J
发明人： KUPPER ROBERT J
IPC分类号： A61K31/352 , A61P1/08 , A61P29/02
CPC分类号： A61K31/353 , A61K31/352
摘要： Pharmaceutical compositions comprising the cannabinoid active pharmaceutical ingredient, crystalline trans-(±)-? 9 -tetrahydrocannabinol, and formulations thereof are disclosed. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of crystalline trans-(±)-? 9 -tetrahydrocannabinol. In specific embodiments, the crystalline trans-(±)-? 9 -tetrahydrocannabinol administered according to the methods for treating or preventing a condition such as pain can have a purity of at least about 98% based on the total weight of cannabinoids.
摘要翻译：公开了包含大麻素活性药物成分，结晶反式（±）-β9-四氢大麻酚，及其制剂的药物组合物。本发明还涉及用于治疗或预防诸如疼痛的病症的方法，包括向有需要的患者施用有效量的结晶反式 - （±）-β9-四氢大麻酚。在具体实施方案中，根据用于治疗或预防诸如疼痛的病症的方法施用的结晶反式（±）-β9-四氢大麻酚可以具有至少约98％的纯度，基于大麻素的总重量。

5. 发明申请

WO2005113487A3 POLYUREA COMPOSITIONS AND COMPOUNDS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：聚氨酯组合物及其制备方法
公开(公告)号：WO2005113487A3
公开(公告)日：2006-06-01
申请号：PCT/US2005017018
申请日：2005-05-16
申请人： SAWYER KENNETH I , KUPPER ROBERT J
发明人： SAWYER KENNETH I , KUPPER ROBERT J
IPC分类号： C08G18/50 , C07C205/37 , C07C205/57 , C07C205/59 , C07C217/84 , C07C229/60 , C07C233/78 , C07C237/30 , C07C251/24 , C07C251/54 , C08G18/10 , C08G18/32 , C08G18/64 , C08G18/79 , C08K5/29 , C08K5/32 , C08K5/353 , C08L75/02
CPC分类号： C07C205/37 , C07C205/57 , C07C217/84 , C07C237/30 , C07C251/54 , C08G18/10 , C08G18/3256 , C08G18/5027 , C08G18/6423 , C08G18/797 , C08K5/29 , C08K5/32 , C08K5/353 , C08G18/307 , C08G18/3821 , C08L75/02
摘要： The invention is directed to novel compounds that are used in the formation of polyurea compositions, including one-part and two-part polyurea compositions. The invention is also directed to polyureas formed from such compounds, cross-linked polyureas, and UV-stabilized polyureas.
摘要翻译：本发明涉及用于形成聚脲组合物的新型化合物，包括一部分和两部分聚脲组合物。本发明还涉及由这些化合物形成的聚脲，交联的聚脲和UV稳定的聚脲。

6. 发明申请

WO03070191A3 TAMPER-RESISTANT TRANSDERMAL OPIOID DELIVERY DEVICES 审中-公开
标题翻译：防篡改传感器输送装置
公开(公告)号：WO03070191A3
公开(公告)日：2004-09-10
申请号：PCT/US0304999
申请日：2003-02-19
申请人： EURO CELTIQUE SA , SHEVCHUK IHOR , CASSIDY JAMES P , REIDENBERG BRUCE , SHARP DALE E , KUPPER ROBERT J
发明人： SHEVCHUK IHOR , CASSIDY JAMES P , REIDENBERG BRUCE , SHARP DALE E , KUPPER ROBERT J
IPC分类号： A61K9/70 , A61K31/485 , A61K45/06 , A61P25/04 , A61P25/36 , C07D489/08 , A61K31/4468 , A61K31/55 , C07D221/26 , C07D221/28
CPC分类号： A61K9/7084 , A61K31/485 , A61K45/06 , C07D489/08 , A61K2300/00
摘要： This invention relates to a tamper-resistant transdermal-delivery device comprising an opioid, or a pharmaceutically acceptable salt thereof, and an acyl opiod antagonist, or a pharmaceutically acceptable salt thereof. The transdermal-delivery device allows an analgesically effective amount of the opioid, or a pharmaceutically acceptable salt thereof, to be transdermally administered to a patient. The invention further relates to methods for treating or preventing pain in a patient comprising contacting the skin of a patient in need thereof with the transdermal-delivery device of the invention for an amount of time sufficient to treat or prevent pain. The invention further relates to acyl opioid antagonists.
摘要翻译：本发明涉及包含阿片样物质或其药学上可接受的盐和酰基阿片剂拮抗剂或其药学上可接受的盐的抗篡改透皮递送装置。透皮递送装置允许将止痛有效量的阿片样物质或其药学上可接受的盐透皮给药给患者。本发明还涉及用于治疗或预防患者疼痛的方法，包括将有需要的患者的皮肤与本发明的透皮递送装置接触足以治疗或预防疼痛的时间量。本发明还涉及酰基阿片样物质拮抗剂。

7. 发明申请

WO2003070191A1 TAMPER-RESISTANT TRANSDERMAL OPIOID DELIVERY DEVICES 审中-公开
标题翻译：防篡改透明阿片类物质递送装置
公开(公告)号：WO2003070191A1
公开(公告)日：2003-08-28
申请号：PCT/US2003/004999
申请日：2003-02-19
申请人： EURO-CELTIQUE, S.A. , SHEVCHUK, Ihor , CASSIDY, James, P. , REIDENBERG, Bruce , SHARP, Dale, E. , KUPPER, Robert, J.
发明人： SHEVCHUK, Ihor , CASSIDY, James, P. , REIDENBERG, Bruce , SHARP, Dale, E. , KUPPER, Robert, J.
IPC分类号： A61K
摘要： This invention relates to a tamper-resistant transdermal-delivery device comprising an opioid, or a pharmaceutically acceptable salt thereof, and an acyl opiod antagonist, or a pharmaceutically acceptable salt thereof. The transdermal-delivery device allows an analgesically effective amount of the opioid, or a pharmaceutically acceptable salt thereof, to be transdermally administered to a patient. The invention further relates to methods for treating or preventing pain in a patient comprising contacting the skin of a patient in need thereof with the transdermal-delivery device of the invention for an amount of time sufficient to treat or prevent pain. The invention further relates to acyl opioid antagonists.
摘要翻译：本发明涉及包含阿片样物质或其药学上可接受的盐和酰基阿片类拮抗剂或其药学上可接受的盐的抗篡改透皮递送装置。透皮递送装置允许镇痛有效量的阿片样物质或其药学上可接受的盐透皮施用于患者。本发明进一步涉及治疗或预防患者疼痛的方法，其包括使有需要的患者的皮肤与本发明的透皮递送装置接触足以治疗或预防疼痛的时间量。本发明进一步涉及酰基阿片样物质拮抗剂。

8. 发明申请

WO2003029186A1 SYNTHESIS OF (±)-2-((DIMETHYLAMINO)METHYL)-1-(ARYL)CYCLOHEXANOLS 审中-公开
标题翻译：（+/-） - 2 - （（二甲基氨基）甲基）-1-（芳基）环己醇的合成
公开(公告)号：WO2003029186A1
公开(公告)日：2003-04-10
申请号：PCT/US2002/031384
申请日：2002-10-02
申请人： EURO-CELTIQUE, S.A. , KUPPER, Robert, J. , STUMPF, Andreas
发明人： KUPPER, Robert, J. , STUMPF, Andreas
IPC分类号： C07C225/12
CPC分类号： C07C213/02 , C07C213/00 , C07C225/12 , C07C2601/14 , C07F15/025 , C07C217/74
摘要： Compositions comprising (±)-2-((dimethylamino)methyl)cyclohexanone, a transition-metal salt, and an organic solvent and methods ofpreparing (±)-cis-2-((dimethylamino)methyl)-l-(aryl)cyclohexanols, in particular (±)-cis-2-((dimethylamino)methyl)-1-(3-methoxyphenyl)cyclohexanol, are disclosed herein. In one embodiment, the (±)-2-((dimethylamino)methyl)cyclohexanone and transition-metal salt are in the form of a (±)-2-((dimethylamino)methyl)cyclohexanone:transition-metal salt complex. In another embodimemt, aryl is 3-methoxyphenyl.
摘要翻译：包含（+/-） - 2 - （（二甲基氨基）甲基）环己酮，过渡金属盐和有机溶剂的组合物和制备（+/-） - 顺式-2 - （（二甲基氨基）甲基）-1- （芳基）环己醇，特别是（+/-） - 顺式-2 - （（二甲基氨基）甲基）-1-（3-甲氧基苯基）环己醇。在一个实施方案中，（+/-） - 2 - （（二甲基氨基）甲基）环己酮和过渡金属盐为（+/-） - 2 - （（二甲基氨基）甲基）环己酮：过渡金属盐复合物。在另一个实施方案中，芳基是3-甲氧基苯基。

9. 发明申请

WO1998000606A1 PAPER SIZING COMPOSITION AND PROCESS 审中-公开
标题翻译：纸张尺寸组成和工艺
公开(公告)号：WO1998000606A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997003369
申请日：1997-06-26
申请人： BETZDEARBORN INC. , NYGREN, Lovisa, Monica, Maria , PERSSON, Git, Elisabeth , KUPPER, Robert, J.
发明人： BETZDEARBORN INC.
IPC分类号： D21H21/16
CPC分类号： D21H21/16 , D21H17/07 , D21H17/14 , D21H17/16 , D21H17/17 , D21H17/72
摘要： A process for making paper products is described in which sizing is effected by use of a hydrophobic cellulose-reactive sizing agent in combination with a promoter. As promoters water-insoluble bases are used which are formed by the reaction of saturated fatty acids, unsaturated fatty acids, hydroxy substituted fatty acids and/or mixtures thereof and alkanoldimaines and/or aliphatic polymaines. Further a corresponding paper sizing composition is described which comprises a hydrophobic cellulose-reactive sizing agent and such a promoter. The combination of hydrophobic celluulose-reactive sizing agent and promoter provides a synergistic effect so that for achieving the same sizing level a lower amount of hydrophobic cellulose-reactive sizing agent is required. Alternatively at the same concentration of the hydrophobic cellulose-reactive sizing agent a higher sizing level can be achieved.
摘要翻译：描述了制造纸制品的方法，其中通过使用疏水纤维素反应性施胶剂与促进剂组合来进行施胶。作为助溶剂，使用通过饱和脂肪酸，不饱和脂肪酸，羟基取代的脂肪酸和/或其混合物和烷基酰亚胺和/或脂族多聚核苷酸的反应形成的不溶于水的碱。此外，描述了相应的纸张施胶组合物，其包含疏水性纤维素反应性施胶剂和这种促进剂。疏水纤维素糖反应性施胶剂和促进剂的组合提供了协同效应，使得为达到相同的施胶水平，需要较少量的疏水纤维素反应性施胶剂。或者，在相同浓度的疏水性纤维素反应性施胶剂中，可以实现更高的施胶量。

10. 发明申请

WO2005113487A2 POLYUREA COMPOSITIONS AND COMPOUNDS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：聚氨酯组合物及其制备方法
公开(公告)号：WO2005113487A2
公开(公告)日：2005-12-01
申请号：PCT/US2005/017018
申请日：2005-05-16
申请人： SAWYER, Kenneth, I. , KUPPER, Robert J.
发明人： SAWYER, Kenneth, I. , KUPPER, Robert J.
IPC分类号： C07C251/00
CPC分类号： C07C205/37 , C07C205/57 , C07C217/84 , C07C237/30 , C07C251/54 , C08G18/10 , C08G18/3256 , C08G18/5027 , C08G18/6423 , C08G18/797 , C08K5/29 , C08K5/32 , C08K5/353 , C08G18/307 , C08G18/3821 , C08L75/02
摘要： The invention is directed to novel compounds that are used in the formation of polyurea compositions, including one-part and two-part polyurea compositions. The invention is also directed to polyureas formed from such compounds, cross-linked polyureas, and UV-stabilized polyureas.
摘要翻译：本发明涉及用于形成聚脲组合物的新型化合物，包括一份和两份聚脲组合物。本发明还涉及由这种化合物，交联聚脲和UV稳定的聚脲形成的聚脲。

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