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公开(公告)号：US08569330B1
公开(公告)日：2013-10-29
申请号：US13338329
申请日：2011-12-28
IPC分类号： A61K31/485 , A61K31/44
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
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2.发明授权Opioid salts and formulations exhibiting anti-abuse and anti-dose dumping properties 有权具有抗滥用和抗剂量倾倒性能的阿片类盐和制剂公开(公告)号：US08569329B1
公开(公告)日：2013-10-29
申请号：US13211718
申请日：2011-08-17
IPC分类号： A61K31/485 , A61K31/44
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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公开(公告)号：US09421266B2
公开(公告)日：2016-08-23
申请号：US13723370
申请日：2012-12-21
IPC分类号： A61K31/137 , A61K47/22 , A61K47/26 , A61K9/00 , A61K9/20
CPC分类号： A61K47/22 , A61K9/0095 , A61K9/2013 , A61K31/137 , A61K47/26
摘要： Drug substances comprising a amine containing pharmaceutically active compound, and at least one of an alditol acetal and an aromatic organic acid as an addition salt or an additive.
摘要翻译： 包含含胺药物活性化合物的药物物质和作为加成盐或添加剂的糖醇缩醛和芳族有机酸中的至少一种。
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公开(公告)号：US20140178480A1
公开(公告)日：2014-06-26
申请号：US13723370
申请日：2012-12-21
CPC分类号： A61K47/22 , A61K9/0095 , A61K9/2013 , A61K31/137 , A61K47/26
摘要： Drug substances comprising a amine containing pharmaceutically active compound, and at least one of an alditol acetal and an aromatic organic acid as an addition salt or an additive.
摘要翻译： 包含含胺药物活性化合物的药物物质和作为加成盐或添加剂的糖醇缩醛和芳族有机酸中的至少一种。
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5.发明授权Opioid salts and formulations exhibiting anti-abuse and anti-dumping properties 有权具有抗滥用和反倾销特性的阿片类盐和制剂公开(公告)号：US08476291B1
公开(公告)日：2013-07-02
申请号：US13332548
申请日：2011-12-21
IPC分类号： A61K31/44
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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公开(公告)号：US08338444B1
公开(公告)日：2012-12-25
申请号：US13338459
申请日：2011-12-28
IPC分类号： A61K31/44 , C07D489/00
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
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7.发明授权Opioid salts and formulations exhibiting abuse deterrent and anti-dose dumping properties 有权具有滥用威慑和抗剂量倾倒性质的阿片类盐和制剂公开(公告)号：US08329720B1
公开(公告)日：2012-12-11
申请号：US13008411
申请日：2011-01-18
IPC分类号： A61K31/44 , C07D489/00
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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8.发明授权Opioid salts and formulations exhibiting anti-abuse and anti-dose dumping properties 有权具有抗滥用和抗剂量倾倒性能的阿片类盐和制剂公开(公告)号：US08211905B1
公开(公告)日：2012-07-03
申请号：US12423641
申请日：2009-04-14
IPC分类号： A61K31/44 , C07D489/00
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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9.发明授权Opioid salts and formulations exhibiting anti-abuse and anti-dose dumping properties 有权具有抗滥用和抗剂量倾倒性能的阿片类盐和制剂公开(公告)号：US08921386B1
公开(公告)日：2014-12-30
申请号：US13484964
申请日：2012-05-31
IPC分类号： A61K31/44 , C07D489/00
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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10.发明授权Opioid salts and formulations exhibiting anti-abuse and anti-dumping properties 有权具有抗滥用和反倾销特性的阿片类盐和制剂公开(公告)号：US08748416B1
公开(公告)日：2014-06-10
申请号：US13331298
申请日：2011-12-20
CPC分类号： C07D489/04 , A61K31/485
摘要： A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
摘要翻译： 具有阿片样物质的药学上可接受的有机酸加成盐的药物，其中所述有机酸选自结构A：其中R 1 -R 4独立地选自H，烷基或取代的1-6个碳原子的烷基，相邻基团可以一起 形成环状烷基，环状烷基 - 芳基或环状芳基部分; R5选自H或碱土金属阳离子; R6和R7独立地选自H，烷基的1-6个碳原子，碱土金属阳离子和6至12个碳的芳基，其数量足以完成X的价键，其中X选自氮，氧 或硫磺; 并且其中所述药物具有选自无定形和结晶的形态。
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