公开(公告)号：US20120202763A1

公开(公告)日：2012-08-09

申请号：US13321257

申请日：2010-05-27

Applicant: Neil Almstead ,  Tamil Arasu ,  Soongyu Choi ,  Liangxian Cao ,  Jeffrey Allen Campbelll ,  Donald Corson ,  Thomas W. Davis ,  Jason D. Graci ,  Zhengxian Gu ,  Peter Seong Woo Hwang ,  William Lennox ,  Harry H. Miao ,  Langdon Miller ,  Young-Choon Moon ,  Hongyan Qi ,  Christopher Trotta ,  Marla L. Weetall

Inventor： Neil Almstead ,  Tamil Arasu ,  Soongyu Choi ,  Liangxian Cao ,  Jeffrey Allen Campbelll ,  Donald Corson ,  Thomas W. Davis ,  Jason D. Graci ,  Zhengxian Gu ,  Peter Seong Woo Hwang ,  William Lennox ,  Harry H. Miao ,  Langdon Miller ,  Young-Choon Moon ,  Hongyan Qi ,  Christopher Trotta ,  Marla L. Weetall

IPC: A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/541 ,  A61K31/53 ,  A61K31/497 ,  A61P35/00 ,  A61P31/12 ,  A61P19/02 ,  A61P37/00 ,  A61P3/04 ,  A61P17/06 ,  A61P9/10 ,  A61P27/02 ,  A61P27/06 ,  A61P27/14 ,  A61P3/02 ,  A61P29/00 ,  A61P11/00 ,  A61P13/12 ,  A61P9/12 ,  A61P17/02 ,  A61P1/04 ,  A61P31/22 ,  A61P33/02 ,  A61P17/12 ,  A61P9/00 ,  A61P7/06 ,  A61P19/04 ,  A61P31/04 ,  A61P27/10 ,  A61P31/14 ,  A61P31/16 ,  A61P31/20 ,  A61P31/18 ,  C12N5/09 ,  C12N5/071 ,  C07H19/056 ,  A61K31/7056 ,  C07F7/10 ,  A61K31/695 ,  A61P17/10 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4745 ,  A61K45/06 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/393 ,  Y02A50/401 ,  Y02A50/463 ,  Y02A50/465

Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.

Abstract translation: 描述了选择性抑制人血管内皮生长因子（VEGF）的病理生成的化合物和包含这些化合物的组合物。 描述了抑制病毒复制或产生病毒RNA或DNA或病毒蛋白的化合物和包含这些化合物的组合物。 还描述了使用这些化合物还原VEGF的方法以及用于治疗涉及施用这些化合物的癌症和非肿瘤性病症的方法。 进一步描述的是使用这种用于治疗涉及施用这些化合物的病毒感染的化合物和方法来抑制病毒复制或产生病毒RNA或DNA或病毒蛋白质的方法。 化合物可以作为单一药物治疗或与一种或多种另外的治疗组合施用于需要这种治疗的人。

公开(公告)号：US20110130397A1

公开(公告)日：2011-06-02

申请号：US12441932

申请日：2007-09-21

Applicant: Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

Inventor： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

IPC: A61K31/428 ,  C07D417/04 ,  C07D417/14 ,  A61K31/433 ,  A61K31/427 ,  A61K31/4439 ,  C07D413/14 ,  A61K31/423 ,  C07D473/30 ,  A61K31/52 ,  C07D405/14 ,  A61K31/506 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61P31/04 ,  A01N43/90 ,  A01N43/84 ,  A01N43/824 ,  A01N43/78

CPC classification number: C07D417/04 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D487/04

Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

Abstract translation: 本文提供调节细菌肽基tRNA水解酶的活性的化合物，包括组合物和包含该化合物的剂型。 本文还提供了用于预防或抑制细菌增殖的方法以及使用这些化合物和组合物预防，治疗和/或控制细菌感染的方法。

公开(公告)号：US07767689B2

公开(公告)日：2010-08-03

申请号：US11107783

申请日：2005-04-18

Applicant: Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Joseph Lennox ,  Donald Thomas Corson ,  Seongwoo Hwang ,  Thomas Davis

Inventor： Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Joseph Lennox ,  Donald Thomas Corson ,  Seongwoo Hwang ,  Thomas Davis

IPC: A61K31/437 ,  C07D487/04

CPC classification number: A61K31/337 ,  A61K31/4353 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5513 ,  G01N2333/475 ,  G01N2333/515 ,  A61K2300/00

Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.

Abstract translation: 根据本发明，已经鉴定了抑制VEGF转录后表达的化合物，并提供了它们的使用方法。 在本发明的一个方面，提供了可用于抑制VEGF产生，治疗实体瘤癌症和降低血浆和/或肿瘤VEGF水平的化合物。 在本发明的另一方面，提供了使用本发明化合物抑制VEGF产生，治疗癌症以及降低血浆和/或肿瘤VEGF水平的方法。

公开(公告)号：US20100125065A1

公开(公告)日：2010-05-20

申请号：US12506485

申请日：2009-07-21

Applicant: Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Joseph Lennox ,  Donald Thomas Corson ,  Seongwoo Hwang

Inventor： Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Joseph Lennox ,  Donald Thomas Corson ,  Seongwoo Hwang

IPC: A61K31/551 ,  C07D401/14 ,  A61K31/497 ,  C07D471/02 ,  A61K31/437 ,  A61K31/506 ,  C07D413/14 ,  A61K31/5377 ,  C07D243/08 ,  C07D417/14 ,  A61K31/541 ,  A61P9/00

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/551 ,  C07D471/04

Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.

Abstract translation: 根据本发明，已经鉴定了抑制VEGF转录后表达的化合物，并提供了它们的使用方法。 在本发明的一个方面，提供了可用于抑制VEGF产生，抑制血管发生和/或治疗癌症，糖尿病性视网膜病变或渗出性黄斑变性的化合物。 在本发明的另一方面，提供了使用本发明化合物抑制VEGF产生，抑制血管发生和/或治疗癌症，糖尿病性视网膜病变或渗出性黄斑变性的方法。

公开(公告)号：US07714004B2

公开(公告)日：2010-05-11

申请号：US10537630

申请日：2003-12-19

Applicant: Louis-David Cantin ,  Soongyu Choi ,  Roger B. Clark ,  Martin F. Hentemann ,  Xin Ma ,  Joachim Rudolph ,  Sidney X. Liang ,  Christiana Akuche ,  Rico C. Lavoie ,  Libing Chen ,  Dyuti Majumdar ,  Philip L. Wickens

Inventor： Louis-David Cantin ,  Soongyu Choi ,  Roger B. Clark ,  Martin F. Hentemann ,  Xin Ma ,  Joachim Rudolph ,  Sidney X. Liang ,  Christiana Akuche ,  Rico C. Lavoie ,  Libing Chen ,  Dyuti Majumdar ,  Philip L. Wickens

IPC: A61K31/426 ,  C07D277/20

CPC classification number: C07D213/30 ,  C07C59/72 ,  C07C59/90 ,  C07C69/734 ,  C07C211/48 ,  C07C217/24 ,  C07C255/54 ,  C07C327/48 ,  C07C333/04 ,  C07C2602/08 ,  C07D209/08 ,  C07D213/63 ,  C07D213/83 ,  C07D213/84 ,  C07D215/20 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/52 ,  C07D249/06 ,  C07D249/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/56 ,  C07D277/24 ,  C07D277/34 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D285/08 ,  C07D307/42 ,  C07D307/79 ,  C07D333/16 ,  C07D405/04 ,  C07D417/04 ,  C07D513/04

Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

公开(公告)号：US20100069380A1

公开(公告)日：2010-03-18

申请号：US12441929

申请日：2007-09-21

Applicant: Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

Inventor： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

IPC: C07D491/052 ,  A61K31/5377 ,  A61K31/4741 ,  C07D491/22 ,  C07D491/16 ,  A61P31/04 ,  A61K31/4743 ,  A61K31/506 ,  C07D491/147 ,  C07D491/153 ,  A61K31/4375

CPC classification number: C07D417/04 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D487/04

Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

Abstract translation: 本文提供调节细菌肽基tRNA水解酶的活性的化合物，包括组合物和包含该化合物的剂型。 本文还提供了筛选和鉴定调节细菌肽基tRNA水解酶活性的化合物的方法。 特别地，本文提供了用于鉴定抑制或降低细菌肽基tRNA水解酶的活性的化合物的测定法。 本文提供的方法提供了一种用于高通量筛选化合物文库的简单敏感测定，以鉴定可用于预防，治疗和管理细菌感染或其一种或多种症状的药物引线。 本文还提供了用于预防或抑制细菌增殖的方法以及使用这些化合物和组合物预防，治疗和/或控制细菌感染的方法。

公开(公告)号：US07071207B2

公开(公告)日：2006-07-04

申请号：US10487976

申请日：2002-09-24

Applicant: Roger A. Smith ,  Stephen J. O'Connor ,  Wai C. Wong ,  Soongyu Choi ,  Harold C. Kluender ,  Jianmei Fan ,  Zhonghua Zhang ,  Rico C. Lavoie ,  Brent L. Podlogar

Inventor： Roger A. Smith ,  Stephen J. O'Connor ,  Wai C. Wong ,  Soongyu Choi ,  Harold C. Kluender ,  Jianmei Fan ,  Zhonghua Zhang ,  Rico C. Lavoie ,  Brent L. Podlogar

IPC: A61K31/40 ,  A61K31/395 ,  A61K31/437 ,  C07D471/04 ,  C07D471/14

CPC classification number: C07D471/04

Abstract: This invention relates to 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

Abstract translation: 本发明涉及已被发现抑制食欲并引起体重减轻的1,5,6,7-四氢吡咯并[3,2-c]吡啶衍生物。 本发明还提供了合成化合物的方法，包含该化合物的药物组合物，以及使用这些组合物诱导体重减轻和治疗肥胖症和肥胖相关疾病的方法。

公开(公告)号：US20050282849A1

公开(公告)日：2005-12-22

申请号：US11107783

申请日：2005-04-18

Applicant: Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Lennox ,  Donald Corson ,  Seongwoo Hwang ,  Thomas Davis

Inventor： Young-Choon Moon ,  Liangxian Cao ,  Nadarajan Tamilarasu ,  Hongyan Qi ,  Soongyu Choi ,  William Lennox ,  Donald Corson ,  Seongwoo Hwang ,  Thomas Davis

IPC: A61K31/4745 ,  A61K31/724

CPC classification number: A61K31/337 ,  A61K31/4353 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5513 ,  G01N2333/475 ,  G01N2333/515 ,  A61K2300/00

Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.

Abstract translation: 根据本发明，已经鉴定了抑制VEGF转录后表达的化合物，并提供了它们的使用方法。 在本发明的一个方面，提供了可用于抑制VEGF产生，治疗实体瘤癌症和降低血浆和/或肿瘤VEGF水平的化合物。 在本发明的另一方面，提供了使用本发明化合物抑制VEGF产生，治疗癌症以及降低血浆和/或肿瘤VEGF水平的方法。

公开(公告)号：US06784167B2

公开(公告)日：2004-08-31

申请号：US09967430

申请日：2001-09-28

Applicant: Jill E. Wood ,  Jeremy L. Baryza ,  Catherine R. Brennan ,  Soongyu Choi ,  James H. Cook ,  Brian R. Dixon ,  Paul P. Ehrlich ,  David E. Gunn ,  Ian McAlexander ,  Peiying Liu ,  Derek B. Lowe ,  Anikó M. Redman ,  William J. Scott ,  Yamin Wang

Inventor： Jill E. Wood ,  Jeremy L. Baryza ,  Catherine R. Brennan ,  Soongyu Choi ,  James H. Cook ,  Brian R. Dixon ,  Paul P. Ehrlich ,  David E. Gunn ,  Ian McAlexander ,  Peiying Liu ,  Derek B. Lowe ,  Anikó M. Redman ,  William J. Scott ,  Yamin Wang

IPC: A61K3140

CPC classification number: C07D207/26 ,  C07D207/325 ,  C07D403/06 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D417/06

Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl. Pharmaceutically acceptable salts and N-oxides of these materials are also included. Also claimed are pharmaceutical compositions containing these materials and methods of using them.

Abstract translation: 具有被标记为A的苯基的基团的结构式-17-β-羟基类固醇脱氢酶II抑制剂和基团-C（R 4）（R 6）Y取代为彼此顺式; W表示O或S; R 1表示-H或任选取代的 - （C 1 -C 4）烷基; n表示0或1-3的整数; 并且R 2代表环A上的任何取代基.R 4通常表示-H，但可以是在环A的邻位终止的键.Y表示氟，-OR 5或 - （C 1 -C 4）烷基，任选取代的 - 苯基，任选取代的（C 1 -C 4）烷基 - 苯基或任选取代的 - （C 1 -C 4） 酰基。 R 6表示说明书和权利要求中定义的各种基团中的任何一种，包括杂芳基，芳基烷基，杂芳基烷基，芳基烯基，杂芳基烯基，炔基，芳基炔基，杂芳基炔基，芳基和吲哚基。 也包括这些材料的药学上可接受的盐和N-氧化物。 还要求保护的是含有这些材料的药物组合物和使用它们的方法。

公开(公告)号：US20140088079A1

公开(公告)日：2014-03-27

申请号：US14122836

申请日：2012-06-01

Applicant: Soongyu Choi ,  Kwang Seop Song ,  Suk Ho Lee ,  Min Ju Kim ,  Hee Jeong Seo ,  Eun-Jung Park ,  Younggyu Kong ,  So Ok Park ,  Hyunku Kang ,  Myung Eun Jung ,  Kinam Lee ,  Hyun Jung Kim ,  Jun Sung Lee ,  Min Woo Lee ,  Mi-Soon KIM ,  Dong Ho Hong ,  Misuk Kang

Inventor： Soongyu Choi ,  Kwang Seop Song ,  Suk Ho Lee ,  Min Ju Kim ,  Hee Jeong Seo ,  Eun-Jung Park ,  Younggyu Kong ,  So Ok Park ,  Hyunku Kang ,  Myung Eun Jung ,  Kinam Lee ,  Hyun Jung Kim ,  Jun Sung Lee ,  Min Woo Lee ,  Mi-Soon KIM ,  Dong Ho Hong ,  Misuk Kang

IPC: C07D309/10 ,  C07D405/10 ,  C07D413/04 ,  C07D409/10 ,  C07D413/10 ,  C07D405/14 ,  C07D407/04 ,  C07D407/10

CPC classification number: C07D309/10 ,  C07D405/10 ,  C07D405/14 ,  C07D407/04 ,  C07D407/10 ,  C07D407/14 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D411/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.

Abstract translation: 本发明涉及具有对存在于肠和肾中的钠依赖性葡萄糖协同转运蛋白2（SGLT2）具有抑制活性的二苯基甲烷部分的化合物和包含其作为活性成分的药物组合物，其可用于预防 或治疗代谢紊乱，特别是糖尿病。 本发明还提供了一种制备该化合物的方法，以及通过使用该化合物来预防或治疗代谢紊乱，特别是糖尿病的方法。