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51. 发明授权

US5889006A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5889006A
公开(公告)日：1999-03-30
申请号：US700628
申请日：1996-08-08
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02 , C07D403/02 , C07D403/14
CPC分类号： C07D405/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物）其中R，R 1，R 2，R 3，R 4，R 21，R 27 R28，X，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱性拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

52. 发明授权

US5846966A Combinations of hydroxy-substituted azetidinone compounds and HMG CoA Reductase Inhibitors 失效
标题翻译：羟基取代的氮杂环丁酮化合物与HMG CoA还原酶抑制剂的组合
公开(公告)号：US5846966A
公开(公告)日：1998-12-08
申请号：US953825
申请日：1997-10-14
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08
CPC分类号： A61K45/06 , A61K31/21 , A61K31/35 , A61K31/395 , A61K31/40 , A61K9/2018 , A61K9/4858 , Y10S514/824
摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl; Ar.sup.3 is aryl or R.sup.5 -substituted aryl; X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--; R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 and R.sup.3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1-5; R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ; R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them, and a process for preparing them.
摘要翻译：式（I）的羟基取代的氮杂环丁酮降胆固醇剂或其药学上可接受的盐，其中：Ar 1和Ar 2是芳基或R 4取代的芳基; Ar 3是芳基或者R 5取代的芳基; X，Y和Z是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R1和R3是H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个是1，m，n，p，q和r的和是1-6; 并且当p为0且r为1时，m，q和n的和为1-5; R4选自低级烷基，R5，-CF3，-CN，-NO2和卤素; R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR6，-O（CO）NR6R7，-NR6R7，-NR6（CO）R7，-NR6（ CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 R 9，-COOR 6，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O）0-2R 9，-O（CH 2）1-10 -COOR 6，-O 1-10CONR6R7， - （低级亚烷基）COOR6和-CH = CH-COOR6; R6，R7和R8是H，低级烷基，芳基或芳基取代的低级烷基; R9是低级烷基，芳基或芳基取代的低级烷基; 以及通过单独或与胆固醇生物合成抑制剂组合使用所述化合物，含有它们的药物组合物及其制备方法来降低血清胆固醇的方法。

53. 发明授权

US5744467A Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
标题翻译：可用作降胆固醇药的硫取代的氮杂环丁酮化合物
公开(公告)号：US5744467A
公开(公告)日：1998-04-28
申请号：US813585
申请日：1997-01-08
申请人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
发明人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.
摘要翻译：公开了具有式“IMAGE”I的硫取代的氮杂环丁酮降胆固醇药或其药学上可接受的盐，以及含有它们的药物组合物，以及通过单独或与胆固醇生物合成组合施用所述化合物来降低血清胆固醇的方法抑制剂。

54. 发明授权

US5624920A Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
公开(公告)号：US5624920A
公开(公告)日：1997-04-29
申请号：US342197
申请日：1994-11-18
申请人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
发明人： Brian A. McKittrick , Sundeep Dugar , Duane A. Burnett
IPC分类号： C07D205/08 , C07D401/12 , C07D409/12 , A61K31/395
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl or R.sup.10 -substituted aryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sup.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

55. 发明授权

US09187448B2 Flavonoid compounds 有权
标题翻译：黄酮类化合物
公开(公告)号：US09187448B2
公开(公告)日：2015-11-17
申请号：US14237167
申请日：2012-08-06
申请人： Cyrus K. Becker , George F. Schreiner , Sundeep Dugar , Dinesh Mahajan
发明人： Cyrus K. Becker , George F. Schreiner , Sundeep Dugar , Dinesh Mahajan
IPC分类号： C07D311/62 , C07D405/10 , A61K31/353 , A61K31/496
CPC分类号： C07D311/62 , A61K31/353 , A61K31/496 , C07D405/10
摘要： The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.
摘要翻译：本发明涉及用于治疗与线粒体功能相关的病症的化合物，组合物和方法。在各个方面，本发明包括施用一种或多种有效刺激细胞中线粒体功能的表儿茶素衍生物。本文所述的化合物，组合物和方法提供了在永久性缺血或缺血/再灌注事件或心脏重建后延迟，减弱或预防的方法中减少心脏梗塞面积的大小，并可有助于预防线粒体生物发生受损，从而预防在各种疾病和病症中受损的线粒体生物发生的后果，以及可能已经发生的线粒体消耗的主动治疗。

56. 发明申请

US20140256741A1 FLAVONOID COMPOUNDS 有权
标题翻译： FLAVONOID化合物
公开(公告)号：US20140256741A1
公开(公告)日：2014-09-11
申请号：US14237167
申请日：2012-08-06
申请人： Cyrus K. Becker , George F. Schreiner , Sundeep Dugar , Dinesh Mahajan
发明人： Cyrus K. Becker , George F. Schreiner , Sundeep Dugar , Dinesh Mahajan
IPC分类号： C07D311/62
CPC分类号： C07D311/62 , A61K31/353 , A61K31/496 , C07D405/10
摘要： The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.
摘要翻译：本发明涉及用于治疗与线粒体功能相关的病症的化合物，组合物和方法。在各个方面，本发明包括施用一种或多种有效刺激细胞中线粒体功能的表儿茶素衍生物。本文所述的化合物，组合物和方法提供在永久缺血或缺血/再灌注事件或心脏延迟，减弱或预防不良心脏重塑后的心脏中降低梗死面积，并可有助于预防线粒体生物发生受损，从而预防在各种疾病和病症中受损的线粒体生物发生的后果，以及提供可能已经发生的线粒体消耗的主动治疗。

57. 发明申请

US20140031421A1 NOVEL PROCESS FOR SYNTHESIS OF POLYPHENOLS 有权
标题翻译：用于合成聚苯乙烯的新方法
公开(公告)号：US20140031421A1
公开(公告)日：2014-01-30
申请号：US13981279
申请日：2012-01-24
申请人： Sundeep Dugar , Dinesh Mahajan , Pantelis Peter Giannousis , Vijay Singh , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Pantelis Peter Giannousis , Vijay Singh , Kamal Kishore Kapoor
IPC分类号： C07D311/74
CPC分类号： C07D311/74 , C07D311/30
摘要： The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
摘要翻译：本发明提供用于制备外消旋和/或光学纯的表儿茶素，表没食子儿茶素和相关多酚本身或其各种官能化衍生物的合成方法。本公开的主要目的是提供一种新的有用的合成方法以获得异构纯和/或外消旋形式的多酚。

58. 发明授权

US07291613B2 Inhibitors of p38 kinase 有权
标题翻译： p38激酶抑制剂
公开(公告)号：US07291613B2
公开(公告)日：2007-11-06
申请号：US10992968
申请日：2004-11-18
申请人： Sundeep Dugar , John Perumattam , Gregory Luedtke , Xuefei Tan , Qing Lu
发明人： Sundeep Dugar , John Perumattam , Gregory Luedtke , Xuefei Tan , Qing Lu
IPC分类号： C07D401/06 , C07D401/14 , A61K31/454
CPC分类号： C07D401/06 , C07D209/42 , C07D401/14 , C07D403/06 , C07D403/12 , C07D417/14
摘要： The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system.
摘要翻译：本发明涉及使用包含与稠环系统偶合的饱和杂环的化合物来抑制p38-α激酶的方法。

59. 发明申请

US20050065344A1 Reagents for N-amination 审中-公开
标题翻译： N-胺化试剂
公开(公告)号：US20050065344A1
公开(公告)日：2005-03-24
申请号：US10618573
申请日：2003-07-11
申请人： Babu Mavunkel , John Perumattam , Richland Tester , Sundeep Dugar
发明人： Babu Mavunkel , John Perumattam , Richland Tester , Sundeep Dugar
IPC分类号： C07C239/20 , C07D215/12
CPC分类号： C07C239/20
摘要： Improved reagents and methods of amination are provided. The reagents are phenyl hydroxylamines containing one nitro and at least one CF3 substituent on the phenyl moiety.
摘要翻译：提供改进的试剂和胺化方法。试剂是苯基部分上含有一个硝基和至少一个CF 3取代基的苯基羟胺。

60. 发明授权

US06329395B1 Neuropeptide Y5 receptor antagonists 失效
标题翻译：神经肽Y5受体拮抗剂
公开(公告)号：US06329395B1
公开(公告)日：2001-12-11
申请号：US09326575
申请日：1999-06-07
申请人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
发明人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
IPC分类号： A61K31445
CPC分类号： C07D213/40 , C07C233/15 , C07C233/25 , C07C233/29 , C07C275/28 , C07C275/32 , C07C275/34 , C07C275/38 , C07C311/05 , C07C323/41 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/58 , C07D213/38 , C07D213/74 , C07D295/135 , C07D295/15 , C07D295/215 , C07D317/72
摘要： Compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; X is —O—, —S—, —SO—, —SO2—, —CH(OR8)—, —C(O)—, —C(R23)2—, optionally substituted alkenyl, alkynyl or; R1 is optionally substituted aryl, heteroaryl, substituted amino, alkyl-OC(O)R8, aryloxyalkyl, wherein m is 1-4, or wherein d and e are 0-2; R2, R3, R4 and R5 are H, alkyl, optionally substituted cycloalkyl, halogen, —OR8, —N(R8)2, —CO2R8 or CF3; R6 and R7 are H, alkyl, alkenyl, hydroxyalkyl, aminoalkyl, alkoxy-alkyl, cycloalkyl or cycloalkylalkyl, or R6 and R7, form a 3-7-membered carbocyclic ring, or a 4-7-membered heterocyclic ring; R8 is H, alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R9 is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R11 is H, alkyl or cycloalkyl; and R23 is R8 or halogen; are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using said novel compounds in the treatment of eating disorders and diabetes.
摘要翻译：式I的化合物或其药学上可接受的盐，其中a和b为0-2，条件是总和为0-3; X是-O - ， - S - ， - SO - ， - SO 2 - ， - CH（OR 8 ） - ， - C（O） - ， - C（R 23）2 - ，任选取代的烯基，炔基或R 1是任选取代的芳基，杂芳基，取代的氨基，烷基-C（O）R 8，芳氧基烷基，其中m是1 -4或其中d和e为0-2; R 2，R 3，R 4和R 5为H，烷基，任选取代的环烷基，卤素，-OR 8，-N（R 8）2，-CO 2 R 8或CF 3; R 6和R 7为 H，烷基，烯基，羟基烷基，氨基烷基，烷氧基 - 烷基，环烷基或环烷基烷基，或R6和R7形成3-7元碳环或4-7元杂环; R8是H，烷基，环烷基，任选取代的芳基或杂芳基; R 9为烷基，环烷基，任选取代的芳基或杂芳基; R 11为H，烷基或环烷基; R 23为R 8或卤素; 以及其他新型化合物; 还要求的是使用所述新型化合物治疗进食障碍和糖尿病的药物组合物和方法。

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