公开(公告)号：US09199985B2

公开(公告)日：2015-12-01

申请号：US14000171

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: A61K31/40 ,  A61K31/44 ,  A61K31/55 ,  C07D471/04 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C07D471/14 ,  C07D471/18 ,  C07D487/04 ,  C07D487/14 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18

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 adrenergic receptor α2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders 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。 该化合物可以结合并且是肾上腺素能受体α2B拮抗剂。 化合物还可以结合并拮抗肾上腺素能受体α1B-该化合物可用于治疗，例如（i）降低血压和/或（ii）促进肾血流量和/或（iii）降低或抑制钠再吸收 。 所述化合物也可用于治疗对血压降低或预期响应的疾病或病症。 特别描述了化合物治疗心血管和肾脏疾病的用途。

公开(公告)号：US08907097B2

公开(公告)日：2014-12-09

申请号：US12610217

申请日：2009-10-30

Applicant: David T. Hung ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： David T. Hung ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: C07D401/00 ,  A61K31/445 ,  C07D401/14 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D401/14

Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. 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: 本公开涉及具有刚性部分的吡啶并[4,3-b]吲哚。 一个实施方案中的化合物是具有不饱和烃部分的吡啶并[4,3-b]吲哚。 另一个实施方案中的化合物是具有环烷基，环烯基或杂环基部分的吡啶并[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：US20130217675A1

公开(公告)日：2013-08-22

申请号：US13579904

申请日：2011-02-18

Applicant: Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

IPC: C07D471/04 ,  C07D487/14 ,  C07D471/22 ,  C07D487/04 ,  C07D471/14 ,  C07D471/18

CPC classification number: A61K31/55 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14

Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. 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.

公开(公告)号：US20130053367A1

公开(公告)日：2013-02-28

申请号：US13400032

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

IPC: A61K31/437 ,  A61K31/439 ,  A61K31/506 ,  A61K31/4375 ,  A61P3/00 ,  A61K31/519 ,  A61K31/4985 ,  A61P3/08 ,  A61P5/50 ,  A61P3/10 ,  A61K31/55 ,  A61K31/497

CPC classification number: C07D487/04 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  C07D451/00 ,  C07D455/03 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

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 α2A. 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 α2B 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α2A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; 或者化合物不是肾上腺素能受体α2B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：US08030318B2

公开(公告)日：2011-10-04

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

CPC classification number: C07D471/04 ,  A61K31/495

Abstract: 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的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：US20100216814A1

公开(公告)日：2010-08-26

申请号：US12610217

申请日：2009-10-30

Applicant: David T. HUNG ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： David T. HUNG ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  C07D401/14 ,  A61K31/506 ,  A61P25/00

CPC classification number: C07D471/04 ,  C07D401/14

Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. 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: 本公开涉及具有刚性部分的吡啶并[4,3-b]吲哚。 一个实施方案中的化合物是具有不饱和烃部分的吡啶并[4,3-b]吲哚。 另一个实施方案中的化合物是具有环烷基，环烯基或杂环基部分的吡啶并[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：US07488744B2

公开(公告)日：2009-02-10

申请号：US11752255

申请日：2007-05-22

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

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  John J. Perumattam ,  Richard 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：US07304048B2

公开(公告)日：2007-12-04

申请号：US10156996

申请日：2002-05-28

Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

IPC: A61K31/55 ,  C07D223/02 ,  C07D243/08

CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds containing an aromatic system coupled through a 7-membered heterocycle to an indole-type system.

Abstract translation: 本发明涉及使用含有通过7-元杂环偶联到吲哚型系统的芳族体系的化合物来抑制p38-α激酶的方法。

公开(公告)号：US20070161649A1

公开(公告)日：2007-07-12

申请号：US11689418

申请日：2007-03-21

Applicant: Babu Mavunkel ,  Sarvajit Chakravarty ,  John Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

Inventor： Babu Mavunkel ,  Sarvajit Chakravarty ,  John Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

IPC: A61K31/496 ,  A61K31/454 ,  C07D403/02

CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24 Å.

Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物抑制p38-α激酶的方法，其中表示单键或双键; 一个Z 2是CA或CR 8 A，另一个是CR 1，CR 1，2， 其中每个R 1，R 6和R 8独立为氢，NR 6，N 6， 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; 1和k中的每一个是0-2的整数，其中1和k之和为0-3; Ar是被0-5个非直链取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。

公开(公告)号：US20070066632A1

公开(公告)日：2007-03-22

申请号：US11391726

申请日：2006-03-27

Applicant: Barry Hart ,  Sarvajit Chakravarty ,  Jonathan Axon ,  Alison Murphy ,  Glenn McEnroe

Inventor： Barry Hart ,  Sarvajit Chakravarty ,  Jonathan Axon ,  Alison Murphy ,  Glenn McEnroe

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D471/04

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 excessive TGFβ activity and certain viral disorders.

Abstract translation: 在嘧啶环的C-4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过量TGFbeta活性和某些病毒性疾病相关的病症。