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1. 发明授权

US06294525B1 Reverse-turn mimetics and methods relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US06294525B1
公开(公告)日：2001-09-25
申请号：US09388854
申请日：1999-09-01
申请人： Marcin Stasiak , Michael Kahn
发明人： Marcin Stasiak , Michael Kahn
IPC分类号： A61K2133
CPC分类号： C07D487/04 , A61K38/00 , C07K5/06139 , C40B40/00 , G01N2333/70546
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反向转转区域的二级结构的构象约束化合物：其中A，R1，R2，R2a，R3，R3a和R4如本文所定义。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作药物组合物作为抗炎剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

2. 发明授权

US07598253B2 Reverse-turn mimetics and methods relating thereto 有权
公开(公告)号：US07598253B2
公开(公告)日：2009-10-06
申请号：US10360549
申请日：2003-02-07
申请人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
发明人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
IPC分类号： A61K31/519 , A61K31/495 , A61K31/33
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K31/551 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/06139 , C40B40/00 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

3. 发明授权

US06184223B2 Reverse-turn mimetics and methods relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US06184223B2
公开(公告)日：2001-02-06
申请号：US09344221
申请日：1999-06-25
申请人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
发明人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K31/551 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/06139 , C40B40/00 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.
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。这种逆转模拟物可用于治疗细胞粘附指示疾病，例如多发性硬化，动脉粥样硬化，哮喘和炎症性肠病。

4. 发明授权

US06413963B2 Reverse-turn mimetics and methods relating thereto 有权
公开(公告)号：US06413963B2
公开(公告)日：2002-07-02
申请号：US09742682
申请日：2000-12-19
申请人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
发明人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K31/551 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/06139 , C40B40/00 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

5. 发明授权

US06548500B2 Reverse-turn mimetics and methods relating thereto 有权
公开(公告)号：US06548500B2
公开(公告)日：2003-04-15
申请号：US09742680
申请日：2000-12-19
申请人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
发明人： Michael Kahn , Masakatsu Eguchi , Hwa-Ok Kim , Marcin Stasiak
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61K31/551 , A61K38/00 , C07K5/0202 , C07K5/0205 , C07K5/06139 , C40B40/00 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

6. 发明授权

US06440955B1 Reverse-turn mimetics and methods relating thereto 有权
标题翻译：反转模拟物及其相关方法
公开(公告)号：US06440955B1
公开(公告)日：2002-08-27
申请号：US09946789
申请日：2001-09-04
申请人： Marcin Stasiak , Michael Kahn
发明人： Marcin Stasiak , Michael Kahn
IPC分类号： A61K3133
CPC分类号： C07D487/04 , A61K38/00 , C07K5/06139 , C40B40/00 , G01N2333/70546
摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
摘要翻译：公开了具有以下结构的模拟具有生物活性肽和蛋白质的反向转转区域的二级结构的构象约束化合物：其中A，R1，R2，R2a，R3，R3a和R4如本文所定义。这些化合物可用于广泛的领域，包括用作诊断和治疗剂。特别地，本发明的化合物可用作药物组合物作为抗炎剂。还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。

7. 发明授权

US09371330B2 Substituted pyrazino[1,2-a]pyrimidines useful as CBP/catenin antagonists for enhancing asymmetric division of somatic stem cells 有权
标题翻译：可用作CBP /连环蛋白拮抗剂的取代的吡嗪并[1,2-a]嘧啶，用于增强体细胞干细胞的不对称分裂
公开(公告)号：US09371330B2
公开(公告)日：2016-06-21
申请号：US14350342
申请日：2012-05-15
申请人： Michael Kahn , Jia-Ling Teo , Michael McMillan , Yi Zhao , Yongfeng Wu
发明人： Michael Kahn , Jia-Ling Teo , Michael McMillan , Yi Zhao , Yongfeng Wu
IPC分类号： A61K31/4985 , C07D241/38 , C07D487/04
CPC分类号： C07D487/04
摘要： Provided are: composition and methods for: treating aging or an age-related condition, symptom or disease; stimulating hair growth, regrowth or pigmentation (or preventing hair loss); for increasing adenosine receptor expression in dermal cells (in combination with hair growth); for treating a condition or disease of the skin or at least one symptom thereof, including cosmetic treatment (e.g., wrinkles, hyperpigmentation, redness, rosacea, dryness, cracking, loss of firmness, loss of elasticity, thinning, and loss of vibrancy). The methods comprise administering a sufficient amount of the disclosed CBP/catenin (e.g., CBP/(β-catenin) antagonist compositions, and particularly wherein administration is in an amount and manner sufficient to provide for increasing the number of asymmetric renewing divisions relative to, or at the expense of symmetric divisions in relevant somatic stem cell population. In particular aspects, the CBP/catenin (e.g., CBP/(β-catenin) antagonist comprises an alkyl and/or fatty acid ester derivative of formula (I) as disclosed herein
摘要翻译：提供：用于治疗老化或年龄相关病症，症状或疾病的组合物和方法; 刺激头发生长，再生长或色素沉着（或防止脱发）; 用于增加真皮细胞中的腺苷受体表达（与头发生长结合）; 用于治疗皮肤或其至少一种症状的病症或疾病，包括美容治疗（例如皱纹，色素沉着过度，发红，红斑痤疮，干燥，开裂，硬度丧失，弹性丧失，变薄和活力丧失）。所述方法包括施用足量的所公开的CBP /连环蛋白（例如CBP /（＆bgr-连翘蛋白）拮抗剂组合物），特别是其中给药的量和方式足以提供增加不对称更新分隔数相对于在特定方面，CBP /连环蛋白（例如，CBP /（＆bgr-连环蛋白）拮抗剂）包含式（I）的烷基和/或脂肪酸酯衍生物，或者以相关体细胞干细胞群体的对称分裂为代价。如本文所公开的

8. 发明申请

US20120059010A1 ALPHA-HELIX MIMETICS AND METHODS RELATING TO THE TREATMENT OF FIBROSIS 有权
标题翻译： ALPHA-HELIX纤维化和治疗纤维化的方法
公开(公告)号：US20120059010A1
公开(公告)日：2012-03-08
申请号：US13073176
申请日：2011-03-28
申请人： Michael Kahn , Masakatsu Eguchi
发明人： Michael Kahn , Masakatsu Eguchi
IPC分类号： A61K31/53 , C07D487/04 , A61P13/12 , A61P25/28 , A61P1/16 , A61P7/04 , A61P15/00 , A61P17/00 , A61K31/498 , A61P11/00
CPC分类号： C07K7/56
摘要： The invention provides α-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.
摘要翻译：本发明提供α-螺旋模拟结构和与其相关的化学文献。包含该化合物的化合物，药物组合物和使用该化合物的本发明的方法涉及治疗包括纤维化在内的疾病，例如肺纤维化。

9. 发明授权

US08101751B2 Reverse-turn mimetics and method relating thereto 有权
公开(公告)号：US08101751B2
公开(公告)日：2012-01-24
申请号：US12541388
申请日：2009-08-14
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 , 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.

10. 发明申请

US20100081655A1 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：US20100081655A1
公开(公告)日：2010-04-01
申请号：US12541388
申请日：2009-08-14
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 , A61K31/538 , A61K31/5377
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。

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