公开(公告)号：US5543496A

公开(公告)日：1996-08-06

申请号：US279763

申请日：1994-07-25

Applicant: Donald J. Kyle ,  Sarvajit Chakravarty

Inventor： Donald J. Kyle ,  Sarvajit Chakravarty

IPC: A61K38/00 ,  C07K7/18 ,  A61K38/12 ,  C07K7/52

CPC classification number: C07K7/18 ,  A61K38/00 ,  Y10S930/27

Abstract: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

Abstract translation: 基于修饰的缓激肽序列的环化合物是有效的缓激肽受体拮抗剂。 在位置2和5或6处进行氨基酸取代，以通过氨基酸侧链的共价键来促进肽的环化。 所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

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：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：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：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

公开(公告)号：US06277989B1

公开(公告)日：2001-08-21

申请号：US09525034

申请日：2000-03-14

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

IPC: C07D23942

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

Abstract: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; 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R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。