公开(公告)号：US20130331421A1

公开(公告)日：2013-12-12

申请号：US13925507

申请日：2013-06-24

Applicant: Rajendra Parasmal Jain ,  Jacqueline A. Gibbons

Inventor： Rajendra Parasmal Jain ,  Jacqueline A. Gibbons

IPC: C07D233/86 ,  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.

Abstract translation: 提供了包含特定的二芳基乙内酰脲和二芳基硫代乙内酰脲化合物的组合物，例如药物组合物，或其盐或溶剂合物。 还描述了分离和纯化形式的化合物，单位剂型，基本上纯的化合物的组合物和包含该化合物的试剂盒也是如此。 其化合物及其药物组合物可用于预防和/或治疗各种病症，包括前列腺癌，帕金森病，阿尔茨海默病等。

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：US20120035231A1

公开(公告)日：2012-02-09

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 ,  A61P25/16 ,  A61P35/00 ,  A61P25/28 ,  C07D233/72 ,  C07D233/86

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.

Abstract translation: 提供了包含特定的二芳基乙内酰脲和二芳基硫代乙内酰脲化合物的组合物，例如药物组合物，或其盐或溶剂合物。 还描述了分离和纯化形式的化合物，单位剂型，基本上纯的化合物的组合物和包含该化合物的试剂盒也是如此。 其化合物及其药物组合物可用于预防和/或治疗各种病症，包括前列腺癌，帕金森病，阿尔茨海默病等。

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：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。

公开(公告)号：US20130217675A1

公开(公告)日：2013-08-22

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

公开(公告)号：US20130190507A1

公开(公告)日：2013-07-25

申请号：US13785504

申请日：2013-03-05

Applicant: Rajendra Parasmal JAIN ,  Remy ANGELAUD ,  Andrew Thompson ,  Carol LAMBERSON ,  Scott GREENFIELD

Inventor： Rajendra Parasmal JAIN ,  Remy ANGELAUD ,  Andrew Thompson ,  Carol LAMBERSON ,  Scott GREENFIELD

IPC: C07D233/86 ,  C07D235/02

CPC classification number: C07D233/86 ,  C07C231/12 ,  C07C237/30 ,  C07D235/02

Abstract: Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.

Abstract translation: 提供了二芳基硫代乙内酰脲和二芳基乙内酰脲化合物的合成方法。 含有该药物的药物在治疗前列腺癌方面特别有用，包​​括抗阉割前列腺癌和/或激素敏感性前列腺癌。

公开(公告)号：US20130053367A1

公开(公告)日：2013-02-28

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: A61K31/437 ,  A61K31/439 ,  A61K31/506 ,  A61K31/4375 ,  A61P3/00 ,  A61K31/519 ,  A61K31/4985 ,  A61P3/08 ,  A61P5/50 ,  A61P3/10 ,  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 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：US20100216814A1

公开(公告)日：2010-08-26

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: A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  C07D401/14 ,  A61K31/506 ,  A61P25/00

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。