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公开(公告)号：US08754223B2
公开(公告)日：2014-06-17
申请号：US13910708
申请日：2013-06-05
IPC分类号： C07D215/38
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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公开(公告)号：US20130289281A1
公开(公告)日：2013-10-31
申请号：US13910708
申请日：2013-06-05
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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公开(公告)号：US20120283289A1
公开(公告)日：2012-11-08
申请号：US13328386
申请日：2011-12-16
IPC分类号： A61K31/4709 , A61P11/06 , A61P11/08 , A61P11/00
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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公开(公告)号：US08476299B2
公开(公告)日：2013-07-02
申请号：US13328386
申请日：2011-12-16
IPC分类号： A61K31/04
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
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公开(公告)号：US08101766B2
公开(公告)日：2012-01-24
申请号：US12369605
申请日：2009-02-11
IPC分类号： C07D215/38
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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公开(公告)号：US20090221638A1
公开(公告)日：2009-09-03
申请号：US12369605
申请日：2009-02-11
IPC分类号： A61K31/4709 , A61P35/00
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5 -yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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公开(公告)号：US07521558B2
公开(公告)日：2009-04-21
申请号：US11204065
申请日：2005-08-15
IPC分类号： C07D453/04 , C07D211/56
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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![CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND](/abs-image/US/2011/07/28/US20110184008A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110184008A1
公开(公告)日：2011-07-28
申请号：US13081162
申请日：2011-04-06
IPC分类号： A61K31/46 , A61P1/00 , A61K31/485 , A61P25/04
CPC分类号： A61K31/46 , A61K31/485 , A61K45/06 , C07D451/02
摘要： The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
摘要翻译： 本发明提供3-内 - （8- {2- [环己基甲基 - （（S）-2,3-二羟基 - 丙酰基）氨基]乙基} -8-氮杂 - 双环[3.2.1]辛烷的结晶硫酸盐 -3-基）苯甲酰胺或其溶剂合物。 本发明还提供包含这种结晶盐形式的药物组合物，使用这种结晶盐形式治疗与阿片样物质受体活性相关的疾病的方法，以及可用于制备此类结晶盐形式的方法。
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公开(公告)号：US07320990B2
公开(公告)日：2008-01-22
申请号：US11057009
申请日：2005-02-11
申请人： Robert Chao , Miroslav Rapta , Pierre-Jean Colson , Junning Lee
发明人： Robert Chao , Miroslav Rapta , Pierre-Jean Colson , Junning Lee
IPC分类号： C07D211/56 , C07D211/72 , A61K31/47
CPC分类号： C07D401/12
摘要： The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of biphenyl-2-ylcarbamic acid 1-{9-[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydro-quinolin-5 -yl)ethylamino]nonyl}piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译： 本发明提供联苯-2-基氨基甲酸1- {9 - [（R）-2-羟基-2-（8-羟基-2-氧代-1,2-二氢 - 二氢 - 喹啉-5-基）乙基氨基]壬基}哌啶-4-基酯或其溶剂合物。 本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。
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10.发明授权公开(公告)号：US08492399B2
公开(公告)日：2013-07-23
申请号：US13652808
申请日：2012-10-16
IPC分类号： A01N43/42
CPC分类号： C07C237/48 , A61K9/0075 , A61K9/2054 , A61K9/4858 , A61K31/197 , A61K31/485 , A61K45/06 , A61K47/02 , A61K47/12 , C07B2200/07 , C07C215/64 , C07C229/28 , C07C229/34 , C07C2601/14 , C07C2602/10 , Y10T436/173845
摘要： The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
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