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公开(公告)号：US09624152B2
公开(公告)日：2017-04-18
申请号：US14674028
申请日：2015-03-31
IPC分类号： A61K31/20 , C07C31/27 , C07C61/12 , C07C47/34 , C07C309/25 , C07F9/24 , C07D261/12 , C07C59/105 , C07C33/26 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07F9/11 , C07C309/24 , C07F9/12 , C07D495/04 , C07C255/00 , C07D257/04 , C07D261/08 , C07D305/12 , C07D307/33 , C07C59/01 , C07D309/30 , A61K31/194 , A61K31/23 , A61K31/191 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/44
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
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公开(公告)号：US20160289190A1
公开(公告)日：2016-10-06
申请号：US15175824
申请日：2016-06-07
申请人： AMGEN INC.
发明人： Matthew BIO , Sebastien CAILLE , Brian COCHRAN , Yuanqing FANG , Brian M. FOX , Brian S. LUCAS , Lawrence R. McGEE , Filisaty VOUNATSOS , Sean H. WIEDEMANN , Sarah WORTMAN
IPC分类号： C07D211/76
CPC分类号： A61K31/451 , C07B2200/13 , C07C309/04 , C07C309/25 , C07C309/35 , C07C313/02 , C07D211/76 , C07D211/94 , C07D491/048 , C07D498/04
摘要： The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
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公开(公告)号：US20160287570A1
公开(公告)日：2016-10-06
申请号：US15175798
申请日：2016-06-07
申请人： AMGEN INC.
发明人： Matthew BIO , Sebastien CAILLE , Brian COCHRAN , Yuanqing FANG , Filisaty VOUNATSOS , Sarah WORTMAN
IPC分类号： A61K31/451
CPC分类号： A61K31/451 , C07B2200/13 , C07C309/04 , C07C309/25 , C07C309/35 , C07C313/02 , C07D211/76 , C07D211/94 , C07D491/048 , C07D498/04
摘要： The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
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4.发明授权Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses 有权用于胆固醇管理和相关用途的环烷基 - 羟基化合物和组合物公开(公告)号：US09006290B2
公开(公告)日：2015-04-14
申请号：US14138919
申请日：2013-12-23
IPC分类号： A61K31/194 , C07C59/245 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/24 , C07F9/44
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病 视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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公开(公告)号：US08937082B2
公开(公告)日：2015-01-20
申请号：US13806069
申请日：2011-06-21
申请人： Maytal Piran , Jacob Rendell
发明人： Maytal Piran , Jacob Rendell
IPC分类号： C07D401/14 , A61K31/506 , A61K31/4178
CPC分类号： C07D401/14 , A61K31/4178 , A61K31/506 , C07B2200/13 , C07C53/126 , C07C55/07 , C07C55/08 , C07C55/12 , C07C55/14 , C07C55/22 , C07C57/15 , C07C59/48 , C07C62/02 , C07C229/24 , C07C309/25 , C07C309/30
摘要： Nilotinib salts and crystalline forms thereof have been prepared and characterized.
摘要翻译： 尼罗替尼盐及其结晶形式已被制备和表征。
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6.发明申请CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 有权环烷基羟基化合物及其组合物用于胆固醇管理及相关用途公开(公告)号：US20140235723A1
公开(公告)日：2014-08-21
申请号：US14138919
申请日：2013-12-23
IPC分类号： C07C62/02
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病 视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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公开(公告)号：US08617791B2
公开(公告)日：2013-12-31
申请号：US13614561
申请日：2012-09-13
申请人： Sen Liu , Pushkara R. Varanasi
发明人： Sen Liu , Pushkara R. Varanasi
IPC分类号： G03F7/028 , G03F7/26 , C07C309/06 , C07C309/26
CPC分类号： G03F7/004 , C07C309/25 , C07C309/26 , C07D209/04 , C07D261/20 , C07D277/62 , C07D307/82 , G03F7/0045 , G03F7/028 , G03F7/029 , G03F7/0382 , G03F7/0392 , Y10S430/121 , Y10S430/122 , Y10S430/123 , Y10S430/126
摘要： The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
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公开(公告)号：US20130158059A1
公开(公告)日：2013-06-20
申请号：US13806069
申请日：2011-06-21
申请人： Maytal Piran , Jacob Rendell
发明人： Maytal Piran , Jacob Rendell
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , A61K31/4178 , A61K31/506 , C07B2200/13 , C07C53/126 , C07C55/07 , C07C55/08 , C07C55/12 , C07C55/14 , C07C55/22 , C07C57/15 , C07C59/48 , C07C62/02 , C07C229/24 , C07C309/25 , C07C309/30
摘要： Nilotinib salts and crystalline forms thereof have been prepared and characterized.
摘要翻译： 尼罗替尼盐及其结晶形式已被制备和表征。
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公开(公告)号：US20130017490A1
公开(公告)日：2013-01-17
申请号：US13617623
申请日：2012-09-14
申请人： Sen Liu , Pushkara R. Varanasi
发明人： Sen Liu , Pushkara R. Varanasi
IPC分类号： C07D333/62 , G03F7/20 , C07D277/76 , G03F7/027
CPC分类号： G03F7/004 , C07C309/25 , C07C309/26 , C07D209/04 , C07D261/20 , C07D277/62 , C07D307/82 , G03F7/0045 , G03F7/028 , G03F7/029 , G03F7/0382 , G03F7/0392 , Y10S430/121 , Y10S430/122 , Y10S430/123 , Y10S430/126
摘要： The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
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10.发明授权Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses 有权用于胆固醇管理和相关用途的环烷基 - 羟基化合物和组合物公开(公告)号：US08309604B2
公开(公告)日：2012-11-13
申请号：US13414855
申请日：2012-03-08
IPC分类号： A61K31/194 , A61K31/225
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病 视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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