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：US20090239854A1

公开(公告)日：2009-09-24

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 ,  Elena F. SHEVTSOVA ,  Vladimir V. GRIGORIEV ,  Nadezhda Sergeevna Beznosko

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 ,  Nadezhda Sergeevna Beznosko

IPC: A61K31/541 ,  C07D471/04 ,  A61K31/437 ,  A61K31/519 ,  C07D471/14 ,  A61P25/18

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：US20070293500A1

公开(公告)日：2007-12-20

申请号：US11765409

申请日：2007-06-19

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: A61K31/519 ,  A61P43/00 ,  C07D475/00 ,  C07D487/04

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

Abstract: Quinazoline derivatives and their pharmaceutically acceptable salts are inhibitors of TGFβ activity and are used to treat conditions characterized by enhanced TGFβ activity.

Abstract translation: 喹唑啉衍生物及其药学上可接受的盐是TGFbeta活性的抑制剂，用于治疗以增强的TGFbeta活性为特征的病症。

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.