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1. 发明申请

WO2005089764A9 CARBOLINE DERIVATIVES USEFUL IN THE INHIBITION OF ANGIOGENESIS 审中-公开
标题翻译：卡波醇衍生物有助于抑制血管生成
公开(公告)号：WO2005089764A9
公开(公告)日：2007-09-13
申请号：PCT/US2005008481
申请日：2005-03-15
申请人： PTC THERAPEUTICS INC , MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS , HWANG SEONGWOO
发明人： MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS , HWANG SEONGWOO
IPC分类号： A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/506 , A61K31/5355 , A61K31/541 , A61K31/551 , A61K31/724 , C07D471/04
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/5355 , A61K31/541 , A61K31/551 , C07D471/04
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2006058088A2 CARBAZOLE, CARBOLINE, AND INDOLE DERIVATIVES USEFUL IN THE INHIBITION OF VEGF PRODUCTION 审中-公开
标题翻译：卡泊唑，碳水化合物和含有抑制VEGF生成的吲哚衍生物
公开(公告)号：WO2006058088A2
公开(公告)日：2006-06-01
申请号：PCT/US2005042484
申请日：2005-11-23
申请人： PTC THERAPEUTICS INC , CAO LIANGXIAN , CHOI SOONGYU , MOON YOUNG-CHOON , TAMILARASU NADARAJAN , QI HONGYAN , LENNOX WILLIAM JOSEPH , HWANG SEONGWOO
发明人： CAO LIANGXIAN , CHOI SOONGYU , MOON YOUNG-CHOON , TAMILARASU NADARAJAN , QI HONGYAN , LENNOX WILLIAM JOSEPH , HWANG SEONGWOO
IPC分类号： C07D209/88 , C07D209/94 , C07D317/66 , C07D495/04
CPC分类号： A61K31/403 , A61K31/343 , A61K31/4035 , A61K31/407 , A61K31/4162 , A61K31/4184 , A61K31/4188 , A61K31/424 , A61K31/4245 , A61K31/506 , A61K31/5377 , C07D209/08 , C07D209/90 , C07D471/04
摘要： 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 and compositions useful in the inhibition of BEGF production, and/or 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.
摘要翻译：根据本发明，已经鉴定了抑制VEGF转录后表达的化合物，并提供了它们的用途。在本发明的一个方面，提供了可用于抑制BEGF产生和/或抑制血管发生和/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和组合物。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。

3. 发明申请

WO2005089752A3 TETRA-CYCLIC CARBOLINE DERIVATIVES FOR INHIBITING ANGIOGENESIS 审中-公开
标题翻译：抑制血管生成的四环碳氢化合物衍生物
公开(公告)号：WO2005089752A3
公开(公告)日：2005-12-15
申请号：PCT/US2005008452
申请日：2005-03-15
申请人： PTC THERAPEUTICS INC , MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS
发明人： MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS
IPC分类号： A61K31/4166 , A61P3/04 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/00 , A61P29/00 , A61P35/00
CPC分类号： A61K31/4166 , C07D221/18 , C07D235/02 , C07D239/26 , C07D241/04 , C07D265/30 , C07D307/78 , C07D317/48
摘要： In accordance with the present invention,tetracyclic caboline derivatives that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, these 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.
摘要翻译：根据本发明，已经鉴定了抑制VEGF转录后表达的四环caboline衍生物，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生成，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这些化合物。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。

4. 发明申请

WO2006065479A2 SUBSTITUTED PHENOLS AS ACTIVE AGENTS INHIBITING VEGF PRODUCTION 审中-公开
标题翻译：取代苯酚作为抑制血管内皮生长因子产生的活性药物
公开(公告)号：WO2006065479A2
公开(公告)日：2006-06-22
申请号：PCT/US2005042482
申请日：2005-11-23
申请人： PTC THERAPEUTICS INC , CHOI SOONGYU , MOON YOUNG-CHOON , TAMILARASU NADARAJAN
发明人： CHOI SOONGYU , MOON YOUNG-CHOON , TAMILARASU NADARAJAN
IPC分类号： C07D211/22 , A61K31/325 , A61K31/4025 , A61K31/404 , A61K31/444 , A61K31/4523 , A61K31/472 , A61K31/496 , A61P35/00 , C07C271/44 , C07C271/58 , C07C311/08 , C07D209/08 , C07D211/60 , C07D211/66 , C07D215/08 , C07D215/20 , C07D217/06 , C07D217/24 , C07D243/08 , C07D295/20 , C07D401/12 , C07D471/04 , C07D491/10
CPC分类号： A61K31/403 , A61K31/343 , A61K31/4035 , A61K31/407 , A61K31/4162 , A61K31/4184 , A61K31/4188 , A61K31/424 , A61K31/4245 , A61K31/506 , A61K31/5377 , C07D209/08 , C07D209/90 , C07D471/04
摘要： The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
摘要翻译：本发明涉及用于抑制血管生成的方法，化合物和组合物。更具体地说，本发明涉及用于抑制VEGF产生的方法，化合物和组合物。

5. 发明申请

WO2008127275A3 PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF 审中-公开
标题翻译：吡咯烷酮化合物作为细菌蛋白酶抑制剂的抑制剂及其用途
公开(公告)号：WO2008127275A3
公开(公告)日：2009-01-08
申请号：PCT/US2007020462
申请日：2007-09-21
申请人： PTC THERAPEUTICS INC , CHOI SOONGYU , BRANSTROM ARTHUR , GOTHE SCOTT A , LIPMAN RICHARD , TAMILARASU NADARAJAN , WILDE RICHARD G
发明人： CHOI SOONGYU , BRANSTROM ARTHUR , GOTHE SCOTT A , LIPMAN RICHARD , TAMILARASU NADARAJAN , WILDE RICHARD G
IPC分类号： C07D413/14 , A61K31/445 , A61P31/04 , C07D417/04 , C07D417/14 , C07D419/14 , C07D487/04
CPC分类号： C07D417/04 , C07D413/14 , C07D417/14 , C07D419/14 , C07D487/04
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2008127274A3 HETEROCYCLIC INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF 审中-公开
标题翻译：细菌肽类TRNA水解物的杂环抑制剂及其用途
公开(公告)号：WO2008127274A3
公开(公告)日：2009-03-05
申请号：PCT/US2007020461
申请日：2007-09-21
申请人： PTC THERAPEUTICS INC , CHOI SOONGYU , BRANSTROM ARTHUR , GOTHE SCOTT A , LIPMAN RICHARD , TAMILARASU NADARAJAN , WILDE RICHARD G
发明人： CHOI SOONGYU , BRANSTROM ARTHUR , GOTHE SCOTT A , LIPMAN RICHARD , TAMILARASU NADARAJAN , WILDE RICHARD G
IPC分类号： C07D491/052 , A61K31/366 , A61K31/37 , A61K31/4375 , A61K31/4741 , A61K31/4743 , A61P31/00 , C07D471/04 , C07D491/147 , C07D491/153 , C07D491/16 , C07D491/22 , C07D493/04 , C07D513/14
CPC分类号： C07D417/04 , C07D413/14 , C07D417/14 , C07D419/14 , C07D487/04
摘要： 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.
摘要翻译：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用于化合物文库的高通量筛选的简单，灵敏的测定，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。

7. 发明专利

JP2012012398A Carboline derivatives useful in inhibition of angiogenesis 审中-公开
标题翻译：卡波醇衍生物有助于抑制血管生成
公开(公告)号：JP2012012398A
公开(公告)日：2012-01-19
申请号：JP2011162351
申请日：2011-07-25
申请人： Ptc Therapeutics Inc , ピーティーシーセラピューティクス,インコーポレーテッド
发明人： MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS , HWANG SEONGWOO
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/724 , A61P27/02 , A61P35/00 , A61P43/00 , C07D519/00
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/5355 , A61K31/541 , A61K31/551 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and in the treatment of cancer and the like.SOLUTION: What are provided are carboline compounds of formula (I) or pharmaceutically acceptable salts, racemates, or stereoisomers thereof (wherein X is a halogen or the like; A and B are each CH or N, provided that at least either of them is N; and Ris an optionally substituted 6-10C aryl group or the like).
摘要翻译：待解决的问题：提供可用于抑制VEGF产生，抑制血管生成和治疗癌症等的化合物。解决方案：提供式（I）的咔啉化合物或其药学上可接受的盐，外消旋物或立体异构体（其中X是卤素等; A和B各自为CH或N，条件是至少的N为N，R“为任选取代的6-10C芳基等）。版权所有（C）2012，JPO＆INPIT

8. 发明申请

US2009227618A9 Carboline Derivatives Useful in the Inhibition of Angiogenesis 有权
标题翻译：可用于抑制血管生成的Carboline衍生物
公开(公告)号：US2009227618A9
公开(公告)日：2009-09-10
申请号：US7942005
申请日：2005-03-15
申请人： PTC THERAPEUTICS INC
发明人： MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM , CORSON DONALD , HWANG SEONGWOO
IPC分类号： A61K31/4745 , A61K31/437 , A61K31/497 , A61K31/506 , A61K31/5355 , A61K31/541 , A61K31/551 , A61K31/724 , C07D471/04
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/5355 , A61K31/541 , A61K31/551 , C07D471/04
摘要： 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.
摘要翻译：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。

9. 发明专利

ES2401335T3 Derivados de carbolina útiles en la inhibición de la angiogénesis 未知
公开(公告)号：ES2401335T3
公开(公告)日：2013-04-18
申请号：ES05725560
申请日：2005-03-15
申请人： PTC THERAPEUTICS INC
发明人： MOON YOUNG-CHOON , CAO LIANGXIAN , TAMILARASU NADARAJAN , QI HONGYAN , CHOI SOONGYU , LENNOX WILLIAM JOSEPH , CORSON DONALD THOMAS , HWANG SEONGWOO
IPC分类号： A61K31/497 , A61K31/437 , A61K31/4745 , A61K31/506 , A61K31/5355 , A61K31/541 , A61K31/551 , A61K31/724 , A61P35/00 , C07D471/04
摘要： Un compuesto de Formula (IV), o una sal farmacéuticamente aceptable, racemato o estereoisómero del mismo; en la que, X es hidrógeno; un alquilo C1 a C6, opcionalmente sustituido con uno o más halógenos; un grupo hidroxilo; un halógeno; o un alcoxi C1 a C5, opcionalmente sustituido con un grupo arilo C6 a C10; Ro es un halógeno; un ciano; un nitro; un sulfonilo, en el que el sulfonilo está opcionalmente sustituido con un alquilo C1 a C6 o un heterociclo de 3 a 10 miembros; un grupo amino, en el que el grupo amino está opcionalmente sustituido con un alquilo C1 a C6, -C(O)-Rb, -C(O)O-Rb, un sulfonilo, un alquilsulfonilo, un grupo heterociclo de 3 a 10 miembros opcionalmente sustituido con un -C(O)O-Rn; -C(O)-NH-Rb; un heterociclo de 5 a 6 miembros; un heteroarilo de 5 a 6 miembros; un grupo alquilo C1 a C6, en el que el grupo alquilo está opcionalmente sustituido con al menos un grupo hidroxilo, halógeno, amino, o heterociclo de 3 a 12 miembros seleccionado independientemente, en el que el grupo amino y el grupo heterociclo están opcionalmente sustituidos con al menos un grupo alquilo C1 a C4 seleccionado independientemente, cuyo grupo alquilo C1 a C4 está opcionalmente sustituido con al menos un grupo alcoxi C1 a C4, grupo amino, grupo alquilamino, o grupo heterociclo de 5 a 10 miembros seleccionado independientemente; un grupo -C(O)-Rn; o un grupo -ORa; Ra es hidrógeno; alquileno C2 a C8; un grupo -C(O)O-Rb; un -C(O)-NH-Rb; un alquilo C1 a C8, en el que el grupo alquilo está opcionalmente sustituido con al menos un grupo hidroxilo, halógeno, alcoxi C1 a C4, amino, alquilamino, acetamida, -C(O)-Rb, -C(O)O-Rb, arilo C6 a C10, heterociclo de 3 a 12 miembros, o heteroarilo de 5 a 12 miembros seleccionado independientemente, en el que además el alquilamino está opcionalmente sustituido con un hidroxilo, un alcoxi C1 a C4, o un heteroarilo de 5 a 12 miembros opcionalmente sustituido con un alquilo C1 a C4, en el que además la acetamida está opcionalmente sustituida con un alcoxi C1 a C4, sulfonilo, o alquilsulfonilo, en el que además el grupo heterociclo está opcionalmente sustituido con un alquilo C1 a C4 opcionalmente sustituido con un grupo hidroxilo, -C(O)-Rn, -C(O)O-Rn, o un grupo oxo; Rb es hidroxilo; un amino; un alquilamino, en el que el alquilamino está opcionalmente sustituido con un hidroxilo, un amino, un alquilamino, un alcoxi C1 a C4, un heterociclo de 3 a 12 miembros opcionalmente sustituido con al menos un alquilo C1 a C6, oxo, -C(O)O-Rn, o un heteroarilo de 5 a 12 miembros opcionalmente sustituido con un alquilo C1 a C6, seleccionado independientemente; un alcoxi C1 a C4; un alquenilo C2 a C8; un alquinilo C2 a C8; un arilo C6 a C10, en el que el arilo está opcionalmente sustituido con al menos un halógeno o alcoxi C1 a C4 seleccionado independientemente; un heteroarilo de 5 a 12 miembros; grupo heterociclo de 3 a 12 miembros, en el que el heterociclo está opcionalmente sustituido con al menos un grupo acetamida, -C(O)O-Rn, heterociclo de 5 a 6 miembros, o alquilo C1 a C6 opcionalmente sustituido con a hidroxilo, alcoxi C1 a C4, grupo amino, o alquilamino, seleccionado independientemente; o un alquilo C1 a C8, en el que el alquilo está opcionalmente sustituido con al menos un grupo alcoxi C1 a C4, arilo C6 a C10, amino, o heterociclo de 3 a 12 miembros seleccionado independientemente, en el que los grupos amino y heterociclo están opcionalmente sustituidos con al menos un grupo alquilo C1 a C6, oxo, o -C(O)O-Rn seleccionado independientemente; Rd es fenilo sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, nitro, alquilo C1 a C6, -C(O)O-Re, y -ORe; Re es un hidrógeno; un grupo alquilo C1 a C6, en el que el grupo alquilo está opcionalmente sustituido con al menos un grupo halógeno o alcoxi seleccionado independientemente; o un grupo arilo C6 a C10, en el que el grupo arilo está opcionalmente sustituido con al menos un grupo halógeno o alcoxi seleccionado independientemente; y Rn es un grupo hidroxilo, alcoxi C1 a C4, amino, o alquilo C1 a C6.

10. 发明专利

CA2559545A1 TETRA-CYCLIC CARBOLINE DERIVATIVES FOR INHIBITING ANGIOGENESIS 未知
公开(公告)号：CA2559545A1
公开(公告)日：2005-09-29
申请号：CA2559545
申请日：2005-03-15
申请人： PTC THERAPEUTICS INC
发明人： MOON YOUNG-CHOON , QI HONGYAN , TAMILARASU NADARAJAN , CHOI SOONGYU , CAO LIANGXIAN , CORSON DONALD THOMAS , LENNOX WILLIAM JOSEPH
IPC分类号： A61K31/4166 , A61P3/04 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/00 , A61P29/00 , A61P35/00

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