公开(公告)号：US09434747B2

公开(公告)日：2016-09-06

申请号：US14000197

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/54 ,  C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22 ,  C07D471/08 ,  C07D487/08

CPC classification number: C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/08 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22

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：US20140303144A1

公开(公告)日：2014-10-09

申请号：US14000184

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D513/16 ,  C07D498/16 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D487/04 ,  C07D471/14

CPC classification number: C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/08 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22

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 α2B. 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。 所述化合物还可以结合并拮抗肾上腺素能受体α2B。 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：US08569287B2

公开(公告)日：2013-10-29

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 ,  C07D401/06

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：US20100022580A1

公开(公告)日：2010-01-28

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: A61K31/437 ,  C07D471/04 ,  A61P25/28

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

Abstract: This disclosure relates to 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: 本公开涉及可用于调节个体中组胺受体的新型三环化合物。 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：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：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：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。