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：US20130225558A1

公开(公告)日：2013-08-29

申请号：US13579911

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: C07D471/14 ,  C07D487/14 ,  C07D471/20 ,  C07D498/14 ,  C07D513/14

CPC classification number: C07D471/14 ,  C07D471/16 ,  C07D471/20 ,  C07D471/22 ,  C07D487/14 ,  C07D498/14 ,  C07D498/16 ,  C07D498/22 ,  C07D513/14

Abstract: This disclosure is directed to fused tetracyclic 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: 本公开涉及稠合的四环吡啶并[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：US20130172320A1

公开(公告)日：2013-07-04

申请号：US13579912

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 ,  C07D471/18 ,  C07D471/14 ,  C07D471/22

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

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：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：US20130172366A1

公开(公告)日：2013-07-04

申请号：US13540472

申请日：2012-07-02

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: 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：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：US07119199B2

公开(公告)日：2006-10-10

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/91 ,  C07D471/04

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

Abstract translation: 本发明涉及一种制备下式的吡啶并吡啶酮的方法，其中X是N或CH，R是芳基，杂芳基或烷基，所述方法包括使下式的酸衍生物：其中X是N 或CH; Y是一个适当的离开组; Z是卤素，OR 1，NHR 1或SR 1; 并且R 1是低级烷基; 并且脒衍生物是其中R是芳基，杂芳基或烷基。

公开(公告)号：US20050176957A1

公开(公告)日：2005-08-11

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/90 ,  C07D239/91 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a process for making 2-substituted pyridopyrimidones. In particular, 2-substituted pyridopyrimidones are made through the single step reaction of suitable acid derivatives with desired derivatives of amidines.

Abstract translation: 本发明涉及制备2-取代的吡啶并嘧啶酮的方法。 特别地，2-取代的吡啶并嘧啶酮通过合适的酸衍生物与所需的脒衍生物的单步反应制备。