公开(公告)号：US20050004143A1

公开(公告)日：2005-01-06

申请号：US10811428

申请日：2004-03-26

Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

IPC: A61K31/517 ,  A61K31/519 ,  C07D239/94 ,  C07D401/12 ,  C07D487/02 ,  C07D487/04 ,  C07D491/02 ,  C07D491/04 ,  C07D495/04 ,  C07D498/02 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/517 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04

Abstract: Compounds in which a pyrimidine nucleus is bridged at the 5 and 6 position and are further substituted at positions 2 and 4 with substituents comprising aromatic moieties are useful in treating subjects with conditions ameliorated by inhibition of TGFβ activity.

Abstract translation: 其中嘧啶核在5和6位上桥连并且在2和4位被含有芳族部分的取代基进一步取代的化合物可用于治疗受抑制TGFbeta活性改善的病症的受试者。

公开(公告)号：US20140155384A1

公开(公告)日：2014-06-05

申请号：US14000176

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/55 ,  A61K31/439 ,  C07D471/14 ,  A61K31/4985 ,  A61K31/519 ,  C07D487/14 ,  A61K45/06 ,  C07D471/18

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/55 ,  A61K45/06 ,  C07D471/08 ,  C07D471/14 ,  C07D471/18 ,  C07D487/04 ,  C07D487/08 ,  C07D487/14 ,  C07D487/18

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α2B; or the compounds are not antagonists of the adrenergic receptor α2β and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

Abstract translation: 描述了氢化吡啶并[4,3-b]吲哚，吡啶并[3,4-b]吲哚和氮杂环[4,5-b]吲哚。 该化合物可以结合肾上腺素能受体a2A并且是拮抗剂。 该化合物还可以结合并且是肾上腺素能受体α2B的拮抗剂; 或该化合物不是肾上腺素能受体α2和bgr的拮抗剂; 并且化合物与减少或预期降低个体血压的第二药剂一起施用。 该化合物可用于治疗，例如调节血糖水平，增加胰岛素分泌并治疗对胰岛素产生增加或预期是响应的疾病或病症。 特别描述了化合物治疗2型糖尿病的用途。

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：US20080182863A1

公开(公告)日：2008-07-31

申请号：US11909118

申请日：2006-03-27

Applicant: Kenneth Alan Simmen ,  Dominique Louis Nestor Ghislain Surleraux ,  Tse-I Lin ,  Oliver Lenz ,  Pierre Jean-Marie Bernard Raboisson ,  Sarvajit Chakravarty ,  Barry Patrick Hart

Inventor： Kenneth Alan Simmen ,  Dominique Louis Nestor Ghislain Surleraux ,  Tse-I Lin ,  Oliver Lenz ,  Pierre Jean-Marie Bernard Raboisson ,  Sarvajit Chakravarty ,  Barry Patrick Hart

IPC: A61K31/519 ,  C07D471/04 ,  A61P31/14

CPC classification number: C07D471/04 ,  A61K31/495

Abstract: Certain appropriately substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.

Abstract translation: 在嘧啶环的C-4处具有酰胺取代的吡啶基胺基团的某些适当取代的稠合双环嘧啶化合物可用于治疗与HCV相关的病症。

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：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.