公开(公告)号：US20070293500A1

公开(公告)日：2007-12-20

申请号：US11765409

申请日：2007-06-19

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: A61K31/519 ,  A61P43/00 ,  C07D475/00 ,  C07D487/04

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

Abstract: Quinazoline derivatives and their pharmaceutically acceptable salts are inhibitors of TGFβ activity and are used to treat conditions characterized by enhanced TGFβ activity.

Abstract translation: 喹唑啉衍生物及其药学上可接受的盐是TGFbeta活性的抑制剂，用于治疗以增强的TGFbeta活性为特征的病症。

公开(公告)号：US07220763B2

公开(公告)日：2007-05-22

申请号：US10654840

申请日：2003-09-03

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  John J. Perumattam ,  Richland W. Tester

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  Qing Lu ,  Gregory R. Luedtke ,  Babu J. Mavunkel ,  John J. Perumattam ,  Richland W. Tester

IPC: A01N43/64 ,  A61K31/41 ,  C07D209/04

CPC classification number: C07D401/06 ,  C07D209/18 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D409/12 ,  C07D409/14

Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.

Abstract translation: 本发明涉及使用包含通过哌啶或哌嗪核连接的苯基或噻吩基的化合物至吲哚残基来抑制p38-α激酶的方法，其中吲哚残基在作为氨基或取代的氨基的环氮上强制取代基 。

公开(公告)号：US20050288299A1

公开(公告)日：2005-12-29

申请号：US11107027

申请日：2005-04-15

Applicant: Babu Mavunkel ,  John Perumattam ,  Qing Lu ,  Sundeep Dugar ,  Bindu Goyal ,  Dan Wang ,  Sarvajit Chakravarty ,  Gregory Luedtke ,  Imad Nashashibi ,  Richland Tester ,  Xuefei Tan

Inventor： Babu Mavunkel ,  John Perumattam ,  Qing Lu ,  Sundeep Dugar ,  Bindu Goyal ,  Dan Wang ,  Sarvajit Chakravarty ,  Gregory Luedtke ,  Imad Nashashibi ,  Richland Tester ,  Xuefei Tan

IPC: A61K31/496 ,  A61K31/56 ,  A61K39/395 ,  A61K45/06 ,  C07D471/04 ,  A61K31/454 ,  C07D487/02 ,  C07D43/02

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/56 ,  A61K39/395 ,  A61K45/06 ,  Y02A50/412 ,  A61K2300/00

Abstract: The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety.

Abstract translation: 本发明涉及使用氮杂吲哚化合物抑制p38激酶，优选p38-α的方法，其中所述氮杂吲哚通过哌啶或哌嗪型连接体偶联至另一个环状部分。

公开(公告)号：US20050171123A1

公开(公告)日：2005-08-04

申请号：US11053121

申请日：2005-02-07

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 ,  A61K31/535 ,  A61K31/525

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.

公开(公告)号：US06903096B2

公开(公告)日：2005-06-07

申请号：US09972582

申请日：2001-10-05

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: 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.

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：US09023869B2

公开(公告)日：2015-05-05

申请号：US13685013

申请日：2012-11-26

Applicant: Sarvajit Chakravarty ,  Rajendra Parasmal Jain

Inventor： Sarvajit Chakravarty ,  Rajendra Parasmal Jain

IPC: C07C211/02 ,  C07D207/04 ,  A61K31/445 ,  C07C237/30 ,  C07D213/75 ,  C07D213/81 ,  C07D295/135 ,  A61K31/277 ,  A61K31/40 ,  C07C255/50 ,  C07D211/06

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.

Abstract translation: 取代的苯基氨基甲酰基烷基氨基芳烃; 取代的苯基硫代氨基甲酰基烷基氨基芳烃; 取代的苯基氨基甲酰基烷基氨基杂芳烃; 取代的苯基硫代氨基甲酰基烷基氨基杂芳烃; N-取代芳基，N'取代芳基脲化合物; N-取代的芳基，N'取代的杂芳基脲化合物; 提供N-取代的芳基，N'取代的芳基硫脲化合物和N-取代的芳基，N'-取代的杂芳基硫脲化合物，并且可以用作雄激素受体调节剂。 该化合物可以特别用于治疗前列腺癌，包括抗阉割抗性前列腺癌和/或激素敏感性前列腺癌。

公开(公告)号：US20140296209A1

公开(公告)日：2014-10-02

申请号：US14000171

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty

IPC: C07D471/04 ,  C07D487/14 ,  C07D487/18 ,  C07D471/14 ,  C07D487/08 ,  C07D471/08

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 adrenergic receptor α2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α1B—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。 化合物还可以结合并拮抗肾上腺素能受体α1B-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：US08815843B2

公开(公告)日：2014-08-26

申请号：US13400032

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

IPC: A61K31/519 ,  A61P3/08 ,  A61P5/50

CPC classification number: C07D487/04 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  C07D451/00 ,  C07D455/03 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

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：US08791132B2

公开(公告)日：2014-07-29

申请号：US13400031

申请日：2012-02-17

Applicant: Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

Inventor： Andrew Asher Protter ,  Sarvajit Chakravarty ,  Rajendra Parasmal Jain ,  Michael John Green

IPC: A61K31/04

CPC classification number: C07D487/04 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  C07D451/00 ,  C07D455/03 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22

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 α1B. 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。 所述化合物还可结合并拮抗肾上腺素能受体α1B。 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。