公开(公告)号：US5744467A

公开(公告)日：1998-04-28

申请号：US813585

申请日：1997-01-08

Applicant: Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

Inventor： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

IPC: A61K31/395 ,  A61K31/397 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61P3/06 ,  A61P9/10 ,  C07D205/08 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D401/12 ,  C07D205/08 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5624920A

公开(公告)日：1997-04-29

申请号：US342197

申请日：1994-11-18

Applicant: Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

Inventor： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

IPC: C07D205/08 ,  C07D401/12 ,  C07D409/12 ,  A61K31/395

CPC classification number: C07D401/12 ,  C07D205/08 ,  C07D409/12

Abstract: 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.

公开(公告)号：US09187448B2

公开(公告)日：2015-11-17

申请号：US14237167

申请日：2012-08-06

Applicant: Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

Inventor： Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

IPC: C07D311/62 ,  C07D405/10 ,  A61K31/353 ,  A61K31/496

CPC classification number: C07D311/62 ,  A61K31/353 ,  A61K31/496 ,  C07D405/10

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20140256741A1

公开(公告)日：2014-09-11

申请号：US14237167

申请日：2012-08-06

Applicant: Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

Inventor： Cyrus K. Becker ,  George F. Schreiner ,  Sundeep Dugar ,  Dinesh Mahajan

IPC: C07D311/62

CPC classification number: C07D311/62 ,  A61K31/353 ,  A61K31/496 ,  C07D405/10

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20140031421A1

公开(公告)日：2014-01-30

申请号：US13981279

申请日：2012-01-24

Applicant: Sundeep Dugar ,  Dinesh Mahajan ,  Pantelis Peter Giannousis ,  Vijay Singh ,  Kamal Kishore Kapoor

Inventor： Sundeep Dugar ,  Dinesh Mahajan ,  Pantelis Peter Giannousis ,  Vijay Singh ,  Kamal Kishore Kapoor

IPC: C07D311/74

CPC classification number: C07D311/74 ,  C07D311/30

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07291613B2

公开(公告)日：2007-11-06

申请号：US10992968

申请日：2004-11-18

Applicant: Sundeep Dugar ,  John Perumattam ,  Gregory Luedtke ,  Xuefei Tan ,  Qing Lu

Inventor： Sundeep Dugar ,  John Perumattam ,  Gregory Luedtke ,  Xuefei Tan ,  Qing Lu

IPC: C07D401/06 ,  C07D401/14 ,  A61K31/454

CPC classification number: C07D401/06 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system.

Abstract translation: 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。

公开(公告)号：US07119199B2

公开(公告)日：2006-10-10

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/91 ,  C07D471/04

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

Abstract translation: 本发明涉及一种制备下式的吡啶并吡啶酮的方法，其中X是N或CH，R是芳基，杂芳基或烷基，所述方法包括使下式的酸衍生物：其中X是N 或CH; Y是一个适当的离开组; Z是卤素，OR 1，NHR 1或SR 1; 并且R 1是低级烷基; 并且脒衍生物是其中R是芳基，杂芳基或烷基。

公开(公告)号：US20050176957A1

公开(公告)日：2005-08-11

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/90 ,  C07D239/91 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a process for making 2-substituted pyridopyrimidones. In particular, 2-substituted pyridopyrimidones are made through the single step reaction of suitable acid derivatives with desired derivatives of amidines.

Abstract translation: 本发明涉及制备2-取代的吡啶并嘧啶酮的方法。 特别地，2-取代的吡啶并嘧啶酮通过合适的酸衍生物与所需的脒衍生物的单步反应制备。

公开(公告)号：US20050096333A1

公开(公告)日：2005-05-05

申请号：US10957183

申请日：2004-09-30

Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

IPC: A61K20060101 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  C07D471/04 ,  C07D475/10 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D475/10 ,  C07D487/04

Abstract: Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ═O, ═N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.

Abstract translation: 喹唑啉衍生物具有下式：或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8各自为N或CH，其中一个或多个 两个Z 5，Z 6，Z 7和Z 8是N，并且其中两个相邻的Z位置不能是 N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1个基团可以连接形成5-6个成员的脂肪族杂环; 其中R 2独立地是R 1，R 2，R 2卤素，OR-卤素，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12 - 烯基，C

公开(公告)号：US20050065344A1

公开(公告)日：2005-03-24

申请号：US10618573

申请日：2003-07-11

Applicant: Babu Mavunkel ,  John Perumattam ,  Richland Tester ,  Sundeep Dugar

Inventor： Babu Mavunkel ,  John Perumattam ,  Richland Tester ,  Sundeep Dugar

IPC: C07C239/20 ,  C07D215/12

CPC classification number: C07C239/20

Abstract: 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.

Abstract translation: 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。