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：US08524755B2

公开(公告)日：2013-09-03

申请号：US13202970

申请日：2010-02-24

Applicant: Rajendra Parasmal Jain ,  Jacqueline A. Gibbons

Inventor： Rajendra Parasmal Jain ,  Jacqueline A. Gibbons

IPC: A61K31/4166 ,  C07D233/72

CPC classification number: C07D233/86 ,  A61K31/4166 ,  C07D233/72 ,  C07D233/74 ,  C07D233/84

Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.

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。

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：US20100099667A1

公开(公告)日：2010-04-22

申请号：US12410425

申请日：2009-03-24

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

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

IPC: A61K31/541 ,  C07D471/08 ,  C07D279/12 ,  C07D413/14 ,  A61K31/439 ,  A61K31/5377 ,  A61P25/18 ,  A61P25/28

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.

Abstract translation: 本公开涉及可用于调节个体中组胺受体的新化合物。 描述了新的化合物，包括新的桥连杂环[4,3-b]吲哚化合物。 还提供药物组合物。 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：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。