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1. 发明授权

US08318738B2 Reverse-turn mimetics and method relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US08318738B2
公开(公告)日：2012-11-27
申请号：US13194428
申请日：2011-07-29
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这种反转模拟结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。本发明还涉及这种化合物用于抑制或治疗由Wnt信号传导途径调节的疾病，例如癌症，特别是结肠直肠癌，与血管成形术，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化综合征相关的再狭窄，阿尔茨海默氏病，过度毛发生长或损失，或溃疡性结肠炎。

2. 发明授权

US08138337B2 Reverse-turn mimetics and method relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US08138337B2
公开(公告)日：2012-03-20
申请号：US12649161
申请日：2009-12-29
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
IPC分类号： C07D487/04 , A61K31/53 , A61P19/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/53
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
摘要翻译：公开了模拟生物活性肽和蛋白质的逆转转区域的二级结构及其前药的构象约束化合物。这种反转模拟结构和前药在广泛的领域中具有实用性，包括用作诊断和治疗剂。还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。本发明还涉及这些化合物和前药用于抑制或治疗由Wnt信号传导途径调节的疾病如癌症，特别是结肠直肠癌，与血管成形术相关的再狭窄，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化综合征，阿尔茨海默氏病，过度头发生长或损失，或溃疡性结肠炎。

3. 发明授权

US07932384B2 Reverse-turn mimetics and method relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US07932384B2
公开(公告)日：2011-04-26
申请号：US12510107
申请日：2009-07-27
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
IPC分类号： C07D487/04 , A61K31/53 , A61P19/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/337 , A61K31/4745 , A61K31/513 , A61K31/53 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这种反转模拟结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。本发明还涉及这种化合物用于抑制或治疗由Wnt信号传导途径调节的疾病，例如癌症，特别是结肠直肠癌，与血管成形术，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化综合征相关的再狭窄，阿尔茨海默氏病，过度毛发生长或损失，或溃疡性结肠炎。

4. 发明申请

US20100228027A1 NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF (2) 有权
标题翻译：反向混合物的新型化合物及其用途（2）
公开(公告)号：US20100228027A1
公开(公告)日：2010-09-09
申请号：US12682881
申请日：2008-10-15
申请人： Jae Uk Chung , Kyung-Yun Jung , Sang-Hwi Lee , Myoung-Joo Kang
发明人： Jae Uk Chung , Kyung-Yun Jung , Sang-Hwi Lee , Myoung-Joo Kang
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/53
摘要： Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic frame-work are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to the use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.
摘要翻译：公开了具有新颖性并且模拟生物活性肽和蛋白质的反转转区的二级结构并具有双环框架功能的构象约束化合物及其前药。这种反转模拟结构和前药在广泛的领域中具有实用性，包括用作诊断和治疗剂。本发明还涉及这些化合物在制备用于治疗或预防包括急性骨髓性白血病的癌症的药物中的用途。

5. 发明申请

US20100222303A1 REVERSE-TURN MIMETICS AND METHOD RELATING THERETO 有权
公开(公告)号：US20100222303A1
公开(公告)日：2010-09-02
申请号：US12649161
申请日：2009-12-29
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen , Soo Jin Lee
IPC分类号： A61K31/675 , C07D487/04 , A61K31/53 , A61K31/4985 , C07D413/14 , A61K31/5377 , C07D265/36 , A61K31/538 , A61P19/02
CPC分类号： C07D487/04 , A61K31/53
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

6. 发明申请

US20100120758A1 REVERSE-TURN MIMETICS AND METHOD RELATING THERETO 有权
公开(公告)号：US20100120758A1
公开(公告)日：2010-05-13
申请号：US12553858
申请日：2009-09-03
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
IPC分类号： A61K31/53 , C07D487/04 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

7. 发明授权

US08940739B2 Compound of a reverse-turn mimetic and a production method and use therefor 有权
标题翻译：反转模拟物和生产方法的复合物及其用途
公开(公告)号：US08940739B2
公开(公告)日：2015-01-27
申请号：US13878990
申请日：2011-10-14
申请人： Jae-Uk Chung , Mi-Jung Kim , Yong-Sil Lee , Sang-Ho Ma , Young-Seok Cho , Sang-Hak Lee , Young-Jun Na , Myoung-Joo Kang , Woul-Seong Park
发明人： Jae-Uk Chung , Mi-Jung Kim , Yong-Sil Lee , Sang-Ho Ma , Young-Seok Cho , Sang-Hak Lee , Young-Jun Na , Myoung-Joo Kang , Woul-Seong Park
IPC分类号： A01N43/64 , A61K31/53 , C07D487/12
CPC分类号： C07D487/04 , C07D519/00
摘要： This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia.
摘要翻译：本发明涉及具有吡嗪并三嗪酮作为基本框架的逆转模拟物的新型化合物及其制备方法及其用于治疗诸如癌症，特别是急性骨髓性白血病的疾病的用途。

8. 发明授权

US08729262B2 Reverse-turn mimetics and method relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US08729262B2
公开(公告)日：2014-05-20
申请号：US13172315
申请日：2011-06-29
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4985 , Y02A50/467
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这种反转模拟结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。本发明还涉及这种化合物用于抑制或治疗由Wnt信号传导途径调节的疾病，例如癌症，特别是结肠直肠癌，与血管成形术，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化综合征相关的再狭窄，阿尔茨海默氏病，过度毛发生长或损失，或溃疡性结肠炎。

9. 发明授权

US08106049B2 Reverse-turn mimetics and method relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US08106049B2
公开(公告)日：2012-01-31
申请号：US12553858
申请日：2009-09-03
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility as diagnostic and therapeutic agents for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. In one embodiment, these reverse-term mimetics have a general structure of formula (VI): wherein Ra, Rb, Rc, X1, X2 and X3 are defined as provided herein.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这种反转模拟结构具有用作抑制或治疗由Wnt信号传导途径调节的疾病，如癌症，特别是结肠直肠癌，与血管成形术，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病相关的再狭窄的诊断和治疗剂的效用，结节性硬化综合征，阿尔茨海默氏病，过度毛发生长或丧失或溃疡性结肠炎。在一个实施方案中，这些反相模拟物具有式（VI）的通式结构：其中R a，R b，R c，X 1，X 2和X 3如本文所提供。

10. 发明申请

US20110294797A1 REVERSE-TURN MIMETICS AND METHOD RELATING THERETO 有权
标题翻译：反向转换和相关的方法
公开(公告)号：US20110294797A1
公开(公告)日：2011-12-01
申请号：US13194428
申请日：2011-07-29
申请人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
发明人： Sung Hwan Moon , Jae Uk Chung , Sung Chan Lee , Masakatsu Eguchi , Michael Kahn , Kwang Won Jeong , Cu Nguyen
IPC分类号： A61K31/538 , A61K31/53 , A61P17/14 , A61P35/00 , A61P19/02 , A61P25/28 , C07D487/04 , A61K31/5377
CPC分类号： C07D487/04
摘要： Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
摘要翻译：公开了模拟生物活性肽和蛋白质的反转转区的二级结构的构象约束化合物。这种反转模拟结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。还公开了含有本发明的反转模拟结构的文库以及筛选该文库以鉴定生物活性成员的方法。本发明还涉及这种化合物用于抑制或治疗由Wnt信号传导途径调节的疾病，例如癌症，特别是结肠直肠癌，与血管成形术，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化综合征相关的再狭窄，阿尔茨海默氏病，过度毛发生长或损失，或溃疡性结肠炎。

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