专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 发明授权

US07671054B1 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：US07671054B1
公开(公告)日：2010-03-02
申请号：US11974941
申请日：2007-10-15
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。

5. 发明授权

US07576084B2 Reverse-turn mimetics and method relating thereto 有权
公开(公告)号：US07576084B2
公开(公告)日：2009-08-18
申请号：US10826972
申请日：2004-04-16
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 , 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.

6. 发明授权

US07511039B2 β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins 失效
标题翻译： β-折叠模拟物及其作为生物活性肽或蛋白质抑制剂的用途
公开(公告)号：US07511039B2
公开(公告)日：2009-03-31
申请号：US11448412
申请日：2006-06-07
申请人： Michael Kahn , Cyprian O. Ogbu , Masakatsu Eguchi , Hwa-Ok Kim , Patrick D. Boatman, Jr.
发明人： Michael Kahn , Cyprian O. Ogbu , Masakatsu Eguchi , Hwa-Ok Kim , Patrick D. Boatman, Jr.
IPC分类号： A01N43/58
CPC分类号： C07K7/06 , A61K31/4035 , A61K31/4152 , A61K31/437 , A61K31/5025 , C07D471/04 , C07D487/04 , C07D513/04 , C07K1/047 , C07K5/0202 , C07K5/021 , C07K5/06139 , C07K5/06191 , C07K5/0821 , C07K5/1024
摘要： There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the β-sheet mimetic is a thrombin inhibitor.
摘要翻译：公开了与赋予或稳定肽，蛋白质或分子的β-折叠结构相关的β-折叠模拟物和方法。一方面，公开了通常用作蛋白酶抑制剂的β-片剂模拟物，更具体地，作为丝氨酸蛋白酶抑制剂如凝血酶，弹性蛋白酶和因子X抑制剂。在一个实施方案中，β-折叠模拟物是凝血酶抑制剂。

7. 发明授权

US07232822B2 Reverse-turn mimetics and method relating thereto 有权
公开(公告)号：US07232822B2
公开(公告)日：2007-06-19
申请号：US10803179
申请日：2004-03-17
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.

8. 发明授权

US5338725A Anti-aggregatory agents for platelets 失效
公开(公告)号：US5338725A
公开(公告)日：1994-08-16
申请号：US906525
申请日：1992-06-30
申请人： Iwao Ojima , Masakatsu Eguchi , Young-Im Oh , Barry S. Coller
发明人： Iwao Ojima , Masakatsu Eguchi , Young-Im Oh , Barry S. Coller
IPC分类号： A61K38/00 , C07K7/02 , C07K14/75 , A61K37/02 , C07K7/06 , C07K7/08
CPC分类号： C07K14/75 , C07K7/02 , A61K38/00
摘要： The present invention provides synthetic antiaggregatory agents for preventing inhibition of fibrinogen-platelet binding. These anti-aggregatory agents have the general formulas (1)-(5).H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --Cx (1)[Ri--C(O)--R--G--D--(AA.sub.j).sub.j --].sub.n --CX (2)Cy--[--AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.i --].sub.n --Z (3)H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --CZ--[--(AA.sub.k).sub.k --R--G--D--(AA.sub.l).sub.l --].sub.m --Z (4)[R.sub.1 --C(O)--R--G--D--(AA.sub.i).sub.i --].sub.n --CZ[--(AA.sub.j).sub.j ]--R--G--D--(AA.sub.k).sub.k --].sub.m --Z (5)in which: R=Arg; G=Gly; D=Asp; AA.sub.i, AA.sub.j, AA.sub.k and AA.sub.l = alpha-, beta- and omega-amino acid residues; (AA.sub.i).sub.i (AA.sub.j).sub.j =peptide chains having the same or different amino acid residues; (AA.sub.k).sub.k =peptide chains having the same or different amino acid residues; (AA.sub.l).sub.l =peptide chains having the same or different amino acid residues; i and j =integers 0-20; m =an integer 1-10; n=an integer 2-10; Cx =a conjugator bearing at least two amine residues in a molecule having 1-30 carbon atoms, i.e, diamines, triamines, tetramines, and polyamines, which can have other functional groups in the molecule; Cy =a conjugator bearing at least two carboxyl residues in a molecule having 1-30 carbon atoms, i.e., aliphatic, aromatic, heteroaromatic, cycloalkyl dicarboxylic acid, tricarboxylic acid, and polycarboxylic acid residues, which can have other functional groups in the molecule; Cz .sup.= a conjugator bearing at least one amine residue and one carboxyl residue in an aromatic or a cycloalkyl skeleton, having 1-30 carbon atoms, i.e., aromatic, heteroaromatic and cycloalkyl amino carboxylic acid, diamino carboxylic acid, diamino dicarboxylic acid, and ployamino polycarboxylic acid residues; R.sub.1 =an alkyl, aromatic, heteroaromatic, or cycloalkyl group having 1-30 carbons, which can have other functional groups in the molecule; and Z=carboxyl, amide, N-substituted amide, hydrazide, N-substituted hydrazide, or ester group.

9. 发明授权

US5134238A Chiral copper amine complexes 失效
标题翻译：手性铜胺配合物
公开(公告)号：US5134238A
公开(公告)日：1992-07-28
申请号：US730001
申请日：1991-07-15
申请人： Bryant E. Rossiter , Masakatsu Eguchi
发明人： Bryant E. Rossiter , Masakatsu Eguchi
IPC分类号： C07C45/69 , C07F1/08 , C07F7/18
CPC分类号： C07C45/69 , C07F1/08 , C07F7/1856 , C07F7/188
摘要： Disclosed herein is a class of chiral copper-amine complexes of the formula R(L*) CuLi in which L* is selected from: ##STR1## In this formula, R is a transferable ligand, which can be alkyl, aryl or aralkyl. M is a metal ion such as Li, Na, K, Cs, Rb, Be, Mg and other metal ions from the first two columns of the periodic table. R.sub.1 is straight chain alkyl, R.sub.2 is aryl or substituted aryl and R.sub.3 and R.sub.4 form a heterocyclic ring or a substituted heterocyclic ring with 4 to 8 members including oxygen and sulfur.Such complexes react with .alpha.,.beta.-unsaturated ketones, aldehydes, esters and other carbonyl containing compounds such that R is transferred to the 3 position enantioselectively as shown below. ##STR2## Such complexes react with .alpha.,.beta.-unsaturated ketones in the presence of trialkysilyl halides to give silyl enol ether in which R is substituted in the 3 position as shown below. ##STR3##
摘要翻译：本文公开了一类式R（L *）CuLi的手性铜胺配合物，其中L *选自：其中R是可转移的配体，其可以是烷基，芳基或芳烷基。 M是周期表前两列的金属离子，如Li，Na，K，Cs，Rb，Be，Mg等金属离子。 R1是直链烷基，R2是芳基或取代的芳基，R3和R4形成杂环或具有4至8个成员的取代杂环，包括氧和硫。这种络合物与α，β-不饱和酮，醛，酯和其它含羰基化合物反应，使得R如下所示以对映异构选择性转移到3位。此类络合物在三烷基硅烷基卤存在下与α，β-不饱和酮反应，得到甲硅烷基烯醇醚，其中R 3在3位被取代，如下所示。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式