公开(公告)号：US20060281763A1

公开(公告)日：2006-12-14

申请号：US11390980

申请日：2006-03-27

Applicant: Jonathan Axon ,  Sarvajit Chakravarty ,  Barry Hart ,  Glenn McEnroe ,  Alison Murphy ,  Karen Pontius ,  Peijue Sheng ,  Xiaojing Wang ,  Shanthi Yellapregada

Inventor： Jonathan Axon ,  Sarvajit Chakravarty ,  Barry Hart ,  Glenn McEnroe ,  Alison Murphy ,  Karen Pontius ,  Peijue Sheng ,  Xiaojing Wang ,  Shanthi Yellapregada

IPC: C07D403/14 ,  C07D403/02 ,  A61K31/506

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D495/04

Abstract: Certain appropriately substituted forms of pyrimidine having a pyridylamine group at C-4 of the pyrimidine and an amide group on the pyridine ring are useful in the treatment of conditions associated with excessive TGFβ activity.

Abstract translation: 在嘧啶的C-4处具有吡啶基胺基的嘧啶的某些适当取代的形式和吡啶环上的酰胺基可用于治疗与过量TGFbeta活性相关的病症。

公开(公告)号：US20050220784A1

公开(公告)日：2005-10-06

申请号：US11136242

申请日：2005-05-23

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K39/395 ,  A61P1/16 ,  A61P1/18 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

Abstract translation: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。

公开(公告)号：US09255094B2

公开(公告)日：2016-02-09

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 ,  C07D417/04 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Provided are new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Also provided are pyrido[4,3-b]indoles, 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: 提供了可用于调节个体中组胺受体的新的杂环化合物。 还提供了吡啶并[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：US09040519B2

公开(公告)日：2015-05-26

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 ,  C07D471/18 ,  C07D471/16 ,  C07D471/22 ,  C07D498/16 ,  C07D498/22 ,  C07D471/20 ,  C07D487/14 ,  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：US20140206711A1

公开(公告)日：2014-07-24

申请号：US14000179

申请日：2012-02-17

Applicant: Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

IPC: C07D471/04

CPC classification number: A61K31/437 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

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. The compounds may bind to and antagonize receptor α2B, α1B or α2A. 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, or 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. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.

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。 该化合物可以结合并拮抗受体α2B，α1B或α2A。 这些化合物可用于治疗，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，或调节血糖水平，增加胰岛素分泌和 治疗或预期对胰岛素生产增加有反应的疾病或病症。 所述化合物也可用于治疗预期对血压降低有反应的疾病或病症。 具体描述了使用该化合物治疗心血管，肾脏疾病或2型糖尿病。

公开(公告)号：US20140155384A1

公开(公告)日：2014-06-05

申请号：US14000176

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/55 ,  A61K31/439 ,  C07D471/14 ,  A61K31/4985 ,  A61K31/519 ,  C07D487/14 ,  A61K45/06 ,  C07D471/18

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 antagonists of the adrenergic receptor a2A. 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 α2β 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a2A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; 或该化合物不是肾上腺素能受体α2和bgr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：US08741919B2

公开(公告)日：2014-06-03

申请号：US13318124

申请日：2010-04-29

Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

IPC: A61K31/04 ,  C07D215/38

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：US20130210803A1

公开(公告)日：2013-08-15

申请号：US13579900

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 ,  C07D513/00 ,  C07D471/18 ,  C07D498/14

CPC classification number: C07D471/14 ,  C07D471/16 ,  C07D471/18 ,  C07D471/22 ,  C07D498/14 ,  C07D498/16 ,  C07D513/00 ,  C07D513/16

Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles 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: 本公开涉及稠合的四环吡啶并[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：US20130079372A1

公开(公告)日：2013-03-28

申请号：US13685013

申请日：2012-11-26

Applicant: Sarvajit Chakravarty ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Rajendra Parasmal Jain

IPC: A61K31/445 ,  C07D211/06 ,  C07D207/04 ,  A61K31/40 ,  C07C255/50 ,  A61K31/277

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.

公开(公告)号：US08338447B2

公开(公告)日：2012-12-25

申请号：US12410407

申请日：2009-03-24

Applicant: David T. Hung ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

Inventor： David T. Hung ,  Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra P. Jain ,  Sundeep Dugar

IPC: C07D471/14 ,  C07D471/22 ,  A61K31/437 ,  A61K31/438 ,  A61P25/28

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds of formula (I) 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。 描述了式（I）化合物，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/或神经元病症 。