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。

公开(公告)号：US20050171123A1

公开(公告)日：2005-08-04

申请号：US11053121

申请日：2005-02-07

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K39/395 ,  A61P1/16 ,  A61P1/18 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/02 ,  A61K31/535 ,  A61K31/525

CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

公开(公告)号：US06903096B2

公开(公告)日：2005-06-07

申请号：US09972582

申请日：2001-10-05

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K39/395 ,  A61P1/16 ,  A61P1/18 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

公开(公告)号：US5631365A

公开(公告)日：1997-05-20

申请号：US257593

申请日：1994-06-09

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: A process for preparing compounds of the formula ##STR1## wherein R and R.sup.2 are independently --OH, --O(lower alkyl) or --0-benzyl and the remaining variables are as defined in the specification, comprising(a) treating with a strong base in an anhydrous organic solvent a lactone of the formula ##STR2## respectively, wherein Ar.sup.10 is Ar.sup.1 or a suitably protected hydroxy- or amino-substituted aryl, and R' and R.sup.2' are R and R.sup.2 as defined above or are suitably protected hydroxy groups;(b) reacting a product of step (a) with an imine of the formula ##STR3## wherein Ar.sup.20 and Ar.sup.30 are Ar.sup.2 or Ar.sup.3 or suitably protected hydroxy- or amino-substituted aryl;c) quenching the reaction with an acid; andd) removing protecting groups as necssary.

Abstract translation: 制备式IMA化合物的方法其中R和R 2独立地是-OH，-O（低级烷基）或-O-苄基，其余的变量如说明书中所定义，包括（a） 在无水有机溶剂中具有分子式为“IMAGE”的内酯的强碱，其中Ar10为Ar1或适当保护的羟基或氨基取代的芳基，R'和R2'为如上所定义的R和R 2，或者为 适当保护的羟基; （b）使步骤（a）的产物与下式的亚胺反应：其中Ar 20和Ar 30是Ar 2或Ar 3或适当保护的羟基或氨基取代的芳基; c）用酸淬灭反应; 和d）去除保护基团。

公开(公告)号：US5627176A

公开(公告)日：1997-05-06

申请号：US403081

申请日：1995-03-13

Applicant: Michael P. Kirkup ,  Sundeep Dugar

Inventor： Michael P. Kirkup ,  Sundeep Dugar

IPC: A61K31/395 ,  A61K31/397 ,  A61P3/06 ,  A61P9/10 ,  C07B53/00 ,  C07C227/32 ,  C07C229/34 ,  C07C311/06 ,  C07C311/19 ,  C07C311/37 ,  C07C319/20 ,  C07C323/62 ,  C07D205/08 ,  C07D403/04 ,  C07D403/06

CPC classification number: C07C227/32 ,  C07C229/34 ,  C07D205/08 ,  C07C2101/14

Abstract: Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is R.sup.3 -substituted aryl;Ar.sup.2 is R.sup.4 -substituted aryl;Ar.sup.3 is R.sup.5 -substituted aryl;Y and Z are independently --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;A is --O--, --S--, --S(O)-- or --S(O).sub.2 --;R.sup.1 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.2 is hydrogen, lower alkyl or aryl; or R.sup.1 and R.sub.2 together are .dbd.O;q is 1, 2 or 3; p is 0, 1,2, 3 or 4;R.sup.5 is 1-3 substitutes independently selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.9, --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 -lower alkyl, --NR.sup.6 SO.sub.2 -aryl, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 -alkyl, S(O).sub.0-2 -aryl, --O(CH.sub.2).sub.1-10 -COOR.sup.6, --O(CH.sub.2).sub.0-10 CONR.sup.6 R.sup.7, o-halogeno, m-halogeno, o-lower alkyl, m-lower alkyl, -(lower alkylene)-COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.3 and R.sup.4 are 1-3 substituents independently selected from R.sup.5, hydrogen, p-lower alkyl, aryl, --NO.sub.2, CF.sub.3 and p-halogeno;R.sup.6, R.sup.7 and R.sup.8 are hydrogen, lower alkyl, aryl or aryl-substituted lower alkyl; andR.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, pharmaceutical compositions containing them, the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis, novel intermediates and methods for preparing said intermediates.

Abstract translation: 取代的式“IMAGE”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是R 3取代的芳基; Ar2是R4-取代的芳基; Ar 3是R 5取代的芳基; Y和Z独立地是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 A是-O - ， - S - ， - S（O） - 或-S（O）2 - ; R1是-OR6，-O（CO）R6，-O（CO）OR9或-O（CO）NR6R7; R2是氢，低级烷基或芳基; 或R 1和R 2一起为= O; q为1,2或3; p为0,1,2,3或4; R5是独立地选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR9，-O（CO）NR6R7，-NR6R7，-NR6（CO） R 7，-NR 6（CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 - 低级烷基，-NR 6 SO 2 - 芳基，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O） 0-2-芳基，-O（CH 2）1-10 -COOR 6，-O（CH 2）0-10 CONR 6 R 7，o-卤代，间 - 卤代，邻 - 低级烷基，间 - 低级烷基， - （低级亚烷基） COOR 6和-CH = CH-COOR 6; R3和R4是1-3个独立地选自R5，氢，对 - 低级烷基，芳基，-NO2，CF3和对 - 卤代的取代基; R6，R7和R8是氢，低级烷基，芳基或芳基取代的低级烷基; 并且R 9为低级烷基，芳基或芳基取代的低级烷基; 以及通过施用所述化合物，含有它们的药物组合物，取代的氮杂环丁酮和用于治疗和预防动脉粥样硬化的胆固醇生物合成抑制剂的组合来降低血清胆固醇的方法，新型中间体和制备所述中间体的方法。

公开(公告)号：US09481670B2

公开(公告)日：2016-11-01

申请号：US13981579

申请日：2012-01-25

Applicant: Sundeep Dugar ,  Dinesh Mahajan ,  Chandraban Rhushikesh Deokar ,  Frank Peter Hollinger ,  Kamal Kishore Kapoor

Inventor： Sundeep Dugar ,  Dinesh Mahajan ,  Chandraban Rhushikesh Deokar ,  Frank Peter Hollinger ,  Kamal Kishore Kapoor

IPC: C07D401/14 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/53 ,  A61P35/00 ,  C07D471/04 ,  C07D491/107 ,  C07D498/08

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D403/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D498/08

Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.

Abstract translation: 本发明涉及式（1）的新型三嗪化合物，其制备方法，含有这些化合物的药物组合物以及这些化合物用于治疗增殖性疾病如肿瘤和癌症的用途，以及与其相关或与之相关的其他病症和病症 PI3激酶，PI3激酶途径，mTOR和/或mTOR途径的调节异常。

公开(公告)号：US08338408B2

公开(公告)日：2012-12-25

申请号：US12259234

申请日：2008-10-27

Applicant: David T. Hung ,  Andrew A. Protter ,  Rajendra P. Jain ,  Sundeep Dugar ,  Sarvajit Chakravarty ,  Sergey O. Bachurin ,  Anatoly K. Ustinov ,  Bogdan K. Beznosko ,  Nadezhda Sergeevna Beznosko, legal representative ,  Elena F. Shevtsova ,  Vladimir V. Grigoriev

Inventor： David T. Hung ,  Andrew A. Protter ,  Rajendra P. Jain ,  Sundeep Dugar ,  Sarvajit Chakravarty ,  Sergey O. Bachurin ,  Anatoly K. Ustinov ,  Bogdan K. Beznosko ,  Elena F. Shevtsova ,  Vladimir V. Grigoriev

IPC: A61K31/541 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/4439 ,  A61K31/437 ,  C07D279/12 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  C07D417/10 ,  C07D471/10 ,  C07D471/14

Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are 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四环化合物。 一个实施方案中的化合物是四环[4,3-b]吲哚。 还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，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：US07393851B2

公开(公告)日：2008-07-01

申请号：US10683656

申请日：2003-10-09

Applicant: Sundeep Dugar

Inventor： Sundeep Dugar

IPC: A61K31/495 ,  C07D471/02

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。