公开(公告)号：US20070066632A1

公开(公告)日：2007-03-22

申请号：US11391726

申请日：2006-03-27

Applicant: Barry Hart ,  Sarvajit Chakravarty ,  Jonathan Axon ,  Alison Murphy ,  Glenn McEnroe

Inventor： Barry Hart ,  Sarvajit Chakravarty ,  Jonathan Axon ,  Alison Murphy ,  Glenn McEnroe

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D471/04

Abstract: Certain appropriately substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with excessive TGFβ activity and certain viral disorders.

Abstract translation: 在嘧啶环的C-4具有酰胺取代的吡啶基胺基团的某些适当取代的稠合双环嘧啶化合物可用于治疗与过量TGFbeta活性和某些病毒性疾病相关的病症。

公开(公告)号：US07189726B2

公开(公告)日：2007-03-13

申请号：US10146703

申请日：2002-05-14

Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

IPC: A61K31/495 ,  A61K31/445

CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.

Abstract translation: 本发明涉及使用含有通过哌啶与苯并呋喃部分偶联的芳香残基的化合物来抑制p38-α激酶的方法。

公开(公告)号：US06867209B1

公开(公告)日：2005-03-15

申请号：US09575060

申请日：2000-05-19

Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

IPC: C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04 ,  A61K31/495 ,  C07D241/04

CPC classification number: C07D235/06 ,  C07D209/08 ,  C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; as Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24 Å.

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抑制p38-α激酶的方法，其中表示单键或双键;一个Z 2为CA或CR <8> A，另一个为CR <1> ，CR 1，NR 6或N，其中每个R 1，R 6和R 8独立地是氢或非干扰取代基; A是-Wi-COX j Y，其中Y是COR 2或 其等同基团和R 2是氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3为NR 7 >或O;每个R 3独立地为非干扰取代基; n为0-3; L 1和L 2各自为连接基;每个R 4独立地为非干扰取代基; m为0 -4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; 1和k各自是整数fr om 0-2其中1和k的和为0-3; Ar是被0-5个非干扰取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且连接到L 2的Ar原子与α环的中心之间的距离为4.5-24。

公开(公告)号：US20050004143A1

公开(公告)日：2005-01-06

申请号：US10811428

申请日：2004-03-26

Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Aurelia Conte ,  Jonathan Axon ,  Glenn McEnroe ,  Alison Murphy

IPC: A61K31/517 ,  A61K31/519 ,  C07D239/94 ,  C07D401/12 ,  C07D487/02 ,  C07D487/04 ,  C07D491/02 ,  C07D491/04 ,  C07D495/04 ,  C07D498/02 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/517 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04

Abstract: Compounds in which a pyrimidine nucleus is bridged at the 5 and 6 position and are further substituted at positions 2 and 4 with substituents comprising aromatic moieties are useful in treating subjects with conditions ameliorated by inhibition of TGFβ activity.

Abstract translation: 其中嘧啶核在5和6位上桥连并且在2和4位被含有芳族部分的取代基进一步取代的化合物可用于治疗受抑制TGFbeta活性改善的病症的受试者。

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：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：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 。

公开(公告)号：US20090270412A1

公开(公告)日：2009-10-29

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: A61K31/496 ,  A61K31/437 ,  C07D471/14 ,  A61P25/00 ,  C07D471/04 ,  A61K31/4375

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. 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。