公开(公告)号：US06410540B1

公开(公告)日：2002-06-25

申请号：US09385494

申请日：1999-08-27

Applicant: R. Richard Goehring ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  Sarvajit Chakravarty ,  Sundeep Dugar ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

Inventor： R. Richard Goehring ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  Sarvajit Chakravarty ,  Sundeep Dugar ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

IPC: A61K3150

CPC classification number: A61K45/06 ,  A61K31/00 ,  A61K31/426 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/445 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  Y02A50/411

Abstract: The invention is directed to methods to treat conditions mediated by p38-&agr;kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR1, R1 is a noninterfering substituent, each of X1 and X2 is a linker, Ar1 and Ar2 are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar1 and Ar2 is an optionally substituted aryl group, with the proviso that when X2 is CH2 or an isostere thereof, X1 is CO or an isostere thereof, and Ar2 is optionally substituted phenyl, Ar1 is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.

Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物治疗由p38-阿拉蛋白酶介导的病症的方法，其中Z是N或CR1，R1是不干扰取代基，X1和X2分别是 连接基，Ar 1和Ar 2相同或不同，并且表示任选取代的C 1 -C 20烃基残基，其中Ar 1和Ar 2中的至少一个是任选取代的芳基，条件是当X 2是CH 2或其等同体时，X 1是CO 或其等同物，Ar 2是任选取代的苯基，Ar 1不同于任选取代的吲哚基，苯并咪唑基或苯并三唑基取代基，并且其中所述任选取代的苯基不是任选取代的吲哚基，苯并咪唑基或苯并三唑基，Y是非干扰取代基， 其中n是0-4的整数，其中m是0-4的整数，1是0-3的整数。

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：US09079904B2

公开(公告)日：2015-07-14

申请号：US12889323

申请日：2010-09-23

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

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

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.

公开(公告)号：US09006234B2

公开(公告)日：2015-04-14

申请号：US13540472

申请日：2012-07-02

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/54 ,  C07D487/08 ,  C07D471/08 ,  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：US08859561B2

公开(公告)日：2014-10-14

申请号：US12889338

申请日：2010-09-23

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: C07D239/42 ,  A61K31/44 ,  C07D471/18 ,  C07D455/00 ,  C07D471/14 ,  C07D471/04 ,  C07D471/22

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：US20130137705A1

公开(公告)日：2013-05-30

申请号：US13498099

申请日：2010-09-23

Applicant: Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: C07D471/04

CPC classification number: 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.

公开(公告)号：US08338408B2

公开(公告)日：2012-12-25

申请号：US12259234

申请日：2008-10-27

Applicant: David T. Hung ,  Andrew A. Protter ,  Rajendra P. Jain ,  Sundeep Dugar ,  Sarvajit Chakravarty ,  Sergey O. Bachurin ,  Anatoly K. Ustinov ,  Bogdan K. Beznosko ,  Nadezhda Sergeevna Beznosko, legal representative ,  Elena F. Shevtsova ,  Vladimir V. Grigoriev

Inventor： David T. Hung ,  Andrew A. Protter ,  Rajendra P. Jain ,  Sundeep Dugar ,  Sarvajit Chakravarty ,  Sergey O. Bachurin ,  Anatoly K. Ustinov ,  Bogdan K. Beznosko ,  Elena F. Shevtsova ,  Vladimir V. Grigoriev

IPC: A61K31/541 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/4439 ,  A61K31/437 ,  C07D279/12 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  C07D417/10 ,  C07D471/10 ,  C07D471/14

Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: 本公开涉及可用于调节个体中组胺受体的新四环化合物。 一个实施方案中的化合物是四环[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：US20120184580A1

公开(公告)日：2012-07-19

申请号：US13263728

申请日：2010-04-09

Applicant: Sarvajit Chakravarty ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Rajendra Parasmal Jain

IPC: A61K31/4166 ,  A61P35/00 ,  C07D401/10 ,  A61K31/454 ,  C07D233/86 ,  C07D403/10

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：US20120172377A1

公开(公告)日：2012-07-05

申请号：US13318124

申请日：2010-04-29

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/437 ,  A61P25/00 ,  A61P25/28 ,  C07D471/04 ,  A61K31/506

CPC classification number: C07D471/04

Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. 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: 描述了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：US20120136008A1

公开(公告)日：2012-05-31

申请号：US13318123

申请日：2010-04-29

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/437 ,  A61K31/444 ,  A61K31/501 ,  A61P25/28 ,  C07D471/04 ,  A61K31/506

CPC classification number: C07D471/04

Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. 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.