公开(公告)号：US6043255A

公开(公告)日：2000-03-28

申请号：US266079

申请日：1999-03-10

Applicant: 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

Inventor： 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: 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

CPC classification number: 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

Abstract: 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.

Abstract translation: 根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（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，R 28，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氏病的毒蕈碱拮抗剂。 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。

公开(公告)号：US5767115A

公开(公告)日：1998-06-16

申请号：US617751

申请日：1996-03-18

Applicant: Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

Inventor： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

IPC: A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61P3/06 ,  A61P7/00 ,  A61P9/10 ,  C07D205/08

CPC classification number: C07D205/08 ,  Y02P20/55

Abstract: 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 O 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.sub.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 Ic 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.

Abstract translation: 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中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O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，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）OR9，-NR6（CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O） -2R9，-O（CH2）1-10-COOR6，-O（CH2）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Ic 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含有它们的药物组合物来施用所述化合物来降低血清胆固醇的方法; 和一个准备它们的过程。

公开(公告)号：US5238935A

公开(公告)日：1993-08-24

申请号：US839522

申请日：1992-02-20

Applicant: Sundeep Dugar ,  Timothy Kogan

Inventor： Sundeep Dugar ,  Timothy Kogan

IPC: C07D217/06 ,  C07D217/14 ,  C07D217/18 ,  C07D217/20

CPC classification number: C07D217/18 ,  C07D217/06 ,  C07D217/14 ,  C07D217/20

Abstract: N-acyltetrahydroisoquinolines including novel compounds of the formula ##STR1## wherein R.sup.1 is a C10-C25 alkyl chain; a substituted C10-C25 alkyl chain; an interrupted C10-C25 alkyl chain; a substituted interrupted C10-C25 alkyl chain; diphenylamino; di-(R.sup.2 -substituted phenyl)amino; di-(heteroaryl)amino; di-(R.sup.2 -substituted heteroaryl)amino; diphenylmethyl; or di-(R.sup.2 -substituted phenyl)methyl;R.sup.2 is hydroxy, lower alkyl, lower alkoxy, halogeno, amino, lower alkylamino or di-(lower alkyl)amino;R.sup.3, R.sup.4 and R.sup.5 are independently H or --(CH.sub.2).sub.n --Ar;Ar is phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 - substituted heteroaryl;n=0,1 or 2;m=0,1 or 2;or a pharmaceutically acceptable salt thereof, useful in the treatment of atherosclerosis are disclosed.

Abstract translation: N-酰基四氢异喹啉，包括新的式（Ⅰ）化合物，其中R1是C10-C25烷基链; 取代的C 10 -C 25烷基链; 中断的C10-C25烷基链; 取代的中断C10-C25烷基链; 二苯胺 二（R 2取代的苯基）氨基; 二（杂芳基）氨基; 二（R2-取代的杂芳基）氨基; 二苯基甲基; 或二（R 2取代的苯基）甲基; R2是羟基，低级烷基，低级烷氧基，卤代，氨基，低级烷基氨基或二（低级烷基）氨基; R3，R4和R5独立地为H或 - （CH2）n-Ar; Ar是苯基，R 2取代的苯基，杂芳基或R 2取代的杂芳基; n = 0,1或2; m = 0,1或2; 或其药学上可接受的盐，其可用于治疗动脉粥样硬化。

公开(公告)号：US09428482B2

公开(公告)日：2016-08-30

申请号：US13981279

申请日：2012-01-24

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

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

IPC: C07D311/74 ,  C07D311/30

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：US20140121367A1

公开(公告)日：2014-05-01

申请号：US14110373

申请日：2012-04-09

Applicant: Sundeep Dugar ,  Dinesh Mahajan ,  Frank Peter Hollinger

Inventor： Sundeep Dugar ,  Dinesh Mahajan ,  Frank Peter Hollinger

IPC: C07D495/14 ,  C07D471/04 ,  C07D487/22 ,  C07D213/803 ,  C07D491/147 ,  C07D405/12 ,  C07D213/82 ,  C07D487/04

CPC classification number: C07D495/14 ,  C07D213/80 ,  C07D213/803 ,  C07D213/81 ,  C07D213/82 ,  C07D295/20 ,  C07D305/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/22 ,  C07D491/147 ,  C07D491/22

Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.

Abstract translation: 本发明涉及合成和应用新的手性/非手性取代的甲酰甲酰基试剂以改性药物和/或生物活性物质，以改变未经修饰的原始药剂的所得化合物的物理化学，生物学和/或药代动力学性质。

公开(公告)号：US08338447B2

公开(公告)日：2012-12-25

申请号：US12410407

申请日：2009-03-24

Applicant: David T. Hung ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

Inventor： David T. Hung ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

IPC: C07D471/14 ,  C07D471/22 ,  A61K31/437 ,  A61K31/438 ,  A61P25/28

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds of formula (I) are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract translation: 本公开涉及可用于调节个体中组胺受体的新杂环化合物。 描述了式（I）化合物，以及包含该化合物的药物组合物以及在各种治疗应用中使用该化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症 。

公开(公告)号：US20090270412A1

公开(公告)日：2009-10-29

申请号：US12410407

申请日：2009-03-24

Applicant: David T. HUNG ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

Inventor： David T. HUNG ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

IPC: A61K31/496 ,  A61K31/437 ,  C07D471/14 ,  A61P25/00 ,  C07D471/04 ,  A61K31/4375

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

Abstract translation: 本公开涉及可用于调节个体中组胺受体的新杂环化合物。 描述吡啶并[3,4-b]吲哚，以及包含该化合物的药物组合物以及在各种治疗应用中使用该化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或 神经元紊乱。

公开(公告)号：US07220763B2

公开(公告)日：2007-05-22

申请号：US10654840

申请日：2003-09-03

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  John J. Perumattam ,  Richland W. Tester

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  John J. Perumattam ,  Richland W. Tester

IPC: A01N43/64 ,  A61K31/41 ,  C07D209/04

CPC classification number: C07D401/06 ,  C07D209/18 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D409/12 ,  C07D409/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.

Abstract translation: 本发明涉及使用包含通过哌啶或哌嗪核连接的苯基或噻吩基的化合物至吲哚残基来抑制p38-α激酶的方法，其中吲哚残基在作为氨基或取代的氨基的环氮上强制取代基 。

公开(公告)号：US20060199821A1

公开(公告)日：2006-09-07

申请号：US11196650

申请日：2005-08-03

Applicant: Richard Tester ,  Xuefei Tan ,  Kurt Schinzel ,  Imad Nashashibi ,  Gregory Luedtke ,  Weiling Liang ,  Joon Jung ,  R. Goehring ,  Sundeep Dugar ,  Steven Do

Inventor： Richard Tester ,  Xuefei Tan ,  Kurt Schinzel ,  Imad Nashashibi ,  Gregory Luedtke ,  Weiling Liang ,  Joon Jung ,  R. Goehring ,  Sundeep Dugar ,  Steven Do

IPC: A61K31/5377 ,  A61K31/53 ,  A61K31/513 ,  A61K31/506 ,  C07D413/02 ,  C07D403/02 ,  C07D405/02

CPC classification number: C07D405/12 ,  C07D213/75 ,  C07D239/48 ,  C07D401/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

Abstract: The invention is directed to compounds and methods to inhibit p38 kinase wherein the compounds are a pyrimidine or pyridine coupled to two mandatory substituents.

Abstract translation: 本发明涉及抑制p38激酶的化合物和方法，其中化合物是与两个强制性取代基偶联的嘧啶或吡啶。

公开(公告)号：US20050288299A1

公开(公告)日：2005-12-29

申请号：US11107027

申请日：2005-04-15

Applicant: Babu Mavunkel ,  John Perumattam ,  Qing Lu ,  Sundeep Dugar ,  Bindu Goyal ,  Dan Wang ,  Sarvajit Chakravarty ,  Gregory Luedtke ,  Imad Nashashibi ,  Richland Tester ,  Xuefei Tan

Inventor： Babu Mavunkel ,  John Perumattam ,  Qing Lu ,  Sundeep Dugar ,  Bindu Goyal ,  Dan Wang ,  Sarvajit Chakravarty ,  Gregory Luedtke ,  Imad Nashashibi ,  Richland Tester ,  Xuefei Tan

IPC: A61K31/496 ,  A61K31/56 ,  A61K39/395 ,  A61K45/06 ,  C07D471/04 ,  A61K31/454 ,  C07D487/02 ,  C07D43/02

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/56 ,  A61K39/395 ,  A61K45/06 ,  Y02A50/412 ,  A61K2300/00

Abstract: The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety.

Abstract translation: 本发明涉及使用氮杂吲哚化合物抑制p38激酶，优选p38-α的方法，其中所述氮杂吲哚通过哌啶或哌嗪型连接体偶联至另一个环状部分。