公开(公告)号：US20130225558A1

公开(公告)日：2013-08-29

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 ,  C07D487/14 ,  C07D471/20 ,  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：US20130172320A1

公开(公告)日：2013-07-04

申请号：US13579912

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 ,  C07D471/18 ,  C07D471/14 ,  C07D471/22

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

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：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.

公开(公告)号：US09434747B2

公开(公告)日：2016-09-06

申请号：US14000197

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: A61K31/00 ,  A61K31/55 ,  A61K31/54 ,  C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22 ,  C07D471/08 ,  C07D487/08

CPC classification number: C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/08 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22

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：US20140303144A1

公开(公告)日：2014-10-09

申请号：US14000184

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D513/16 ,  C07D498/16 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D487/04 ,  C07D471/14

CPC classification number: C07D513/16 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  C07D451/00 ,  C07D471/04 ,  C07D471/08 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22 ,  C07D487/04 ,  C07D487/08 ,  C07D487/16 ,  C07D498/16 ,  C07D498/22

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 α2B. 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。 所述化合物还可以结合并拮抗肾上腺素能受体α2B。 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：US07119199B2

公开(公告)日：2006-10-10

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/91 ,  C07D471/04

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.

Abstract translation: 本发明涉及一种制备下式的吡啶并吡啶酮的方法，其中X是N或CH，R是芳基，杂芳基或烷基，所述方法包括使下式的酸衍生物：其中X是N 或CH; Y是一个适当的离开组; Z是卤素，OR 1，NHR 1或SR 1; 并且R 1是低级烷基; 并且脒衍生物是其中R是芳基，杂芳基或烷基。

公开(公告)号：US20050176957A1

公开(公告)日：2005-08-11

申请号：US11029139

申请日：2004-12-31

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Richland Tester ,  Aurelia Conte

IPC: C07D239/90 ,  C07D239/91 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D239/91 ,  C07D471/04

Abstract: The present invention is directed to a process for making 2-substituted pyridopyrimidones. In particular, 2-substituted pyridopyrimidones are made through the single step reaction of suitable acid derivatives with desired derivatives of amidines.

Abstract translation: 本发明涉及制备2-取代的吡啶并嘧啶酮的方法。 特别地，2-取代的吡啶并嘧啶酮通过合适的酸衍生物与所需的脒衍生物的单步反应制备。

公开(公告)号：US20050096333A1

公开(公告)日：2005-05-05

申请号：US10957183

申请日：2004-09-30

Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

IPC: A61K20060101 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  C07D471/04 ,  C07D475/10 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D475/10 ,  C07D487/04

Abstract: Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ═O, ═N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.

Abstract translation: 喹唑啉衍生物具有下式：或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8各自为N或CH，其中一个或多个 两个Z 5，Z 6，Z 7和Z 8是N，并且其中两个相邻的Z位置不能是 N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1个基团可以连接形成5-6个成员的脂肪族杂环; 其中R 2独立地是R 1，R 2，R 2卤素，OR-卤素，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12 - 烯基，C