公开(公告)号：US09023869B2

公开(公告)日：2015-05-05

申请号：US13685013

申请日：2012-11-26

Applicant: Sarvajit Chakravarty ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Rajendra Parasmal Jain

IPC: C07C211/02 ,  C07D207/04 ,  A61K31/445 ,  C07C237/30 ,  C07D213/75 ,  C07D213/81 ,  C07D295/135 ,  A61K31/277 ,  A61K31/40 ,  C07C255/50 ,  C07D211/06

CPC classification number: C07D295/155 ,  A61K31/277 ,  A61K31/40 ,  A61K31/445 ,  C07C237/30 ,  C07C255/50 ,  C07C335/20 ,  C07C2601/02 ,  C07D207/04 ,  C07D211/06 ,  C07D213/75 ,  C07D213/81 ,  C07D295/135

Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.

Abstract translation: 取代的苯基氨基甲酰基烷基氨基芳烃; 取代的苯基硫代氨基甲酰基烷基氨基芳烃; 取代的苯基氨基甲酰基烷基氨基杂芳烃; 取代的苯基硫代氨基甲酰基烷基氨基杂芳烃; N-取代芳基，N'取代芳基脲化合物; N-取代的芳基，N'取代的杂芳基脲化合物; 提供N-取代的芳基，N'取代的芳基硫脲化合物和N-取代的芳基，N'-取代的杂芳基硫脲化合物，并且可以用作雄激素受体调节剂。 该化合物可以特别用于治疗前列腺癌，包括抗阉割抗性前列腺癌和/或激素敏感性前列腺癌。

公开(公告)号：US20140296209A1

公开(公告)日：2014-10-02

申请号：US14000171

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D471/04 ,  C07D487/14 ,  C07D487/18 ,  C07D471/14 ,  C07D487/08 ,  C07D471/08

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：US08815843B2

公开(公告)日：2014-08-26

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: A61K31/519 ,  A61P3/08 ,  A61P5/50

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：US08791132B2

公开(公告)日：2014-07-29

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: A61K31/04

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.

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。 所述化合物还可结合并拮抗肾上腺素能受体α1B。 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：US08710086B2

公开(公告)日：2014-04-29

申请号：US13263728

申请日：2010-04-09

Applicant: Sarvajit Chakravarty ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Rajendra Parasmal Jain

IPC: A61K31/4439 ,  A61K31/4166 ,  C07D403/04 ,  C07D233/72

CPC classification number: C07D233/76 ,  C07D233/86

Abstract: Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer.

Abstract translation: 提供了取代的二芳基乙内酰脲和二芳基硫代乙内酰脲，可以用作雄激素受体调节剂。 这些化合物可以特别用于治疗前列腺癌，包括CRPC和/或激素敏感性前列腺癌。

公开(公告)号：US08546381B2

公开(公告)日：2013-10-01

申请号：US12410425

申请日：2009-03-24

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: A61K31/54

CPC classification number: C07D451/00 ,  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：US20130190293A1

公开(公告)日：2013-07-25

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: C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D471/08 ,  C07D471/14

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：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：US20110237582A1

公开(公告)日：2011-09-29

申请号：US12889323

申请日：2010-09-23

Applicant: Rajendra Parasmal JAIN ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal JAIN ,  Sarvajit Chakravarty

IPC: A61K31/5377 ,  C07D471/18 ,  A61K31/439 ,  A61K31/496 ,  C07D413/14 ,  C07D471/14 ,  A61K31/437 ,  A61P25/18 ,  A61P25/24

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.

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。