公开(公告)号：US20130053366A1

公开(公告)日：2013-02-28

申请号：US13400031

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 ,  A61P3/12 ,  A61K31/519 ,  A61K31/4985 ,  A61P9/12 ,  A61P13/12 ,  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 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.

公开(公告)号：US20110245272A1

公开(公告)日：2011-10-06

申请号：US12889338

申请日：2010-09-23

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/437 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22 ,  A61K31/439 ,  A61K31/506 ,  A61P25/00 ,  A61P25/18

CPC classification number: C07D471/22 ,  C07D453/06 ,  C07D455/00 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-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。 描述了吡啶并[4,3-b]吲哚，以及包含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：US20100152163A1

公开(公告)日：2010-06-17

申请号：US12610152

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: A61K31/55 ,  C07D487/04 ,  A61P25/00

CPC classification number: C07D487/04 ,  A61K31/55 ,  C07D471/04

Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.

Abstract translation: 本公开涉及可用于调节个体中组胺受体的新的氮杂环[4,5-b]吲哚化合物。 描述了新的化合物，包括新的1,2,3,4,5,6-四氮杂吖庚因[4,5-b]吲哚。 还提供药物组合物。

公开(公告)号：US09187471B2

公开(公告)日：2015-11-17

申请号：US13579908

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: A61K31/54 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D487/04 ,  C07D487/14 ,  C07D471/08

CPC classification number: A61K31/55 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/18 ,  C07D487/04 ,  C07D487/14

Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-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: 本公开涉及四环吡啶并[4,3-b]吲哚和吡啶并[3,4-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：US09115137B2

公开(公告)日：2015-08-25

申请号：US12360061

申请日：2009-01-26

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

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

IPC: A61K31/44 ,  C07D487/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04

CPC classification number: C07D487/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04

Abstract: Provided are new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. 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: 提供可用于调节个体中组胺受体的新的三环化合物。 描述了化合物，包括新的2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚化合物。 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：US09079904B2

公开(公告)日：2015-07-14

申请号：US12889323

申请日：2010-09-23

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: C07D471/04 ,  C07D471/08 ,  C07D471/18 ,  C07D471/14

CPC classification number: A61K31/439 ,  A61K31/437 ,  A61K31/5377 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/18

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.

公开(公告)号：US09035056B2

公开(公告)日：2015-05-19

申请号：US14000179

申请日：2012-02-17

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

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

IPC: C07D471/04 ,  A61K31/4745 ,  A61K31/55 ,  A61K45/06

CPC classification number: A61K31/437 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

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. The compounds may bind to and antagonize receptor α2B, α1B or α2A. 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, or 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. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.

Abstract translation: 本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。 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。 该化合物可以结合并拮抗受体α2B，α1B或α2A。 这些化合物可用于治疗，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，或调节血糖水平，增加胰岛素分泌和 治疗或预期对胰岛素生产增加有反应的疾病或病症。 所述化合物也可用于治疗预期对血压降低有反应的疾病或病症。 具体描述了使用该化合物治疗心血管，肾脏疾病或2型糖尿病。

公开(公告)号：US09034865B2

公开(公告)日：2015-05-19

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: C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  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.

Abstract translation: 本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。 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：US09006234B2

公开(公告)日：2015-04-14

申请号：US13540472

申请日：2012-07-02

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/54 ,  C07D487/08 ,  C07D471/08 ,  C07D471/18

CPC classification number: C07D487/08 ,  C07D471/08 ,  C07D471/18

Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. 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：US08859561B2

公开(公告)日：2014-10-14

申请号：US12889338

申请日：2010-09-23

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: C07D239/42 ,  A61K31/44 ,  C07D471/18 ,  C07D455/00 ,  C07D471/14 ,  C07D471/04 ,  C07D471/22

CPC classification number: C07D471/22 ,  C07D453/06 ,  C07D455/00 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-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。 描述了吡啶并[4,3-b]吲哚，以及包含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。