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1. 发明授权

US09187485B2 Methods and compositions for the treatment of cancer and related hyperproliferative disorders 有权
标题翻译：用于治疗癌症和相关过度增生性疾病的方法和组合物
公开(公告)号：US09187485B2
公开(公告)日：2015-11-17
申请号：US14052074
申请日：2013-10-11
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
IPC分类号： C07D213/06 , C07D277/24 , C07D417/04 , C07D487/04 , C07D417/14 , A61K31/4439 , A61K31/454 , A61K31/496 , C07D213/76 , C07D235/14 , C07D417/12 , C07D277/22 , C07D213/16 , A61K31/427 , A61K31/428 , C07D471/04 , C07D277/66 , A61K31/437
CPC分类号： A61K31/5025 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , C07D213/06 , C07D213/16 , C07D213/76 , C07D235/14 , C07D277/22 , C07D277/24 , C07D277/66 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.
摘要翻译：本发明涉及通过给予治疗有效量的具有一般三分体结构A-B-C的化合物治疗与细胞增殖相关的疾病的方法。三方结构A，B和C是相同或不相同的结构，例如但不限于具有或不具有取代的杂环，苯基或苄基环结构，并在此详细描述。该方法可以使用具体的化合物，例如具有哌啶基，吡咯啉基或吡啶基A环，噻唑B环和可以独立地进一步取代的苯基C环。

2. 发明授权

US08927578B2 Compositions and methods for the treatment of metabolic disorders 有权
标题翻译：用于治疗代谢紊乱的组合物和方法
公开(公告)号：US08927578B2
公开(公告)日：2015-01-06
申请号：US13484702
申请日：2012-05-31
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
IPC分类号： A61K31/4439 , A61K31/425 , A61K31/426 , A61K31/4709 , C07D277/22 , C07D277/24 , C07D417/04 , C07D417/14 , C07D277/10
CPC分类号： A61K31/4439 , A61K31/426 , A61K31/4709 , C07D277/10 , C07D277/22 , C07D277/24 , C07D417/04 , C07D417/14
摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
摘要翻译：本发明涉及使用脂肪抑制素A和/或其衍生物和/或类似物治疗和/或预防一种或多种代谢紊乱。在其它方面，用于治疗和/或预防一种或多种代谢紊乱的化合物利用A-B-C三方结构，其中A，B和C是相同或不相同的结构，并在本文中进行详细描述。在具体方面，例如，代谢障碍包括肥胖或糖尿病。

3. 发明申请

US20130005768A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS 有权
公开(公告)号：US20130005768A1
公开(公告)日：2013-01-03
申请号：US13484685
申请日：2012-05-31
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
IPC分类号： A61K31/4439 , C07D277/24 , A61K31/4709 , A61P3/00 , C07D417/14 , C07D417/04 , A61K31/426
CPC分类号： A61K31/4439 , A61K31/426 , A61K31/4709 , C07D277/10 , C07D277/22 , C07D277/24 , C07D417/04 , C07D417/14
摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

4. 发明申请

US20090131475A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS 有权
标题翻译：用于治疗代谢性疾病的组合物和方法
公开(公告)号：US20090131475A1
公开(公告)日：2009-05-21
申请号：US12024530
申请日：2008-02-01
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
IPC分类号： A61K31/4709 , C07D417/04 , A61K31/4439 , A61P3/10 , A61K31/426 , C07D277/24 , A61K31/4436 , C07D409/10 , C07D417/14
CPC分类号： A61K31/4439 , A61K31/426 , A61K31/4709 , C07D277/10 , C07D277/22 , C07D277/24 , C07D417/04 , C07D417/14
摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B—C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
摘要翻译：本发明涉及使用脂肪抑制素A和/或其衍生物和/或类似物治疗和/或预防一种或多种代谢紊乱。在其它方面，用于治疗和/或预防一种或多种代谢紊乱的化合物利用A-B-C三方结构，其中A，B和C是相同或不相同的结构，并在本文中进行详细描述。在具体方面，例如，代谢障碍包括肥胖或糖尿病。

5. 发明申请

US20140045854A1 Methods and Compositions for the Treatment of Cancer and Related Hyperproliferative Disorders 有权
标题翻译：用于治疗癌症和相关的过度增生性疾病的方法和组合物
公开(公告)号：US20140045854A1
公开(公告)日：2014-02-13
申请号：US14052074
申请日：2013-10-11
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Al-Elheiga , Mizuki Watanabe
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Al-Elheiga , Mizuki Watanabe
IPC分类号： C07D487/04 , C07D213/06 , C07D277/24 , C07D417/04 , C07D417/14
CPC分类号： A61K31/5025 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , C07D213/06 , C07D213/16 , C07D213/76 , C07D235/14 , C07D277/22 , C07D277/24 , C07D277/66 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.
摘要翻译：本发明涉及通过给予治疗有效量的具有一般三分体结构A-B-C的化合物治疗与细胞增殖相关的疾病的方法。三方结构A，B和C是相同或不相同的结构，例如但不限于具有或不具有取代的杂环，苯基或苄基环结构，并在此详细描述。该方法可以使用具体的化合物，例如具有哌啶基，吡咯啉基或吡啶基A环，噻唑B环和可以独立地进一步取代的苯基C环。

6. 发明申请

US20130012538A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
公开(公告)号：US20130012538A1
公开(公告)日：2013-01-10
申请号：US13484702
申请日：2012-05-31
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Qian Mao , Shinji Kamisuki , Akira Kugimiya
IPC分类号： A61K31/4439 , A61K31/4709 , A61P3/06 , A61P3/00 , A61P9/12 , A61P35/00 , A61P9/00 , A61K31/425 , A61P3/10
CPC分类号： A61K31/4439 , A61K31/426 , A61K31/4709 , C07D277/10 , C07D277/22 , C07D277/24 , C07D417/04 , C07D417/14
摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

7. 发明授权

US06548738B2 ACC2-knockout mice and uses thereof 失效
标题翻译： ACC2敲除小鼠及其用途
公开(公告)号：US06548738B2
公开(公告)日：2003-04-15
申请号：US09749109
申请日：2000-12-26
申请人： Salih J. Wakil , Martin M. Matzuk , Lutfi Abu-Elheiga
发明人： Salih J. Wakil , Martin M. Matzuk , Lutfi Abu-Elheiga
IPC分类号： A01K67027
CPC分类号： G01N33/5061 , A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/0362 , C12N9/93 , C12N15/8509 , G01N33/5008 , G01N33/502 , G01N33/5067 , G01N33/5088
摘要： The present invention discloses transgenic mice with inactivating mutations in the endogenous gene for the acetyl-CoA carboxylase-2 isoform of acetyl-CoA carboxylase. Inactivation of acetyl-CoA carboxylase-2 results in mice exhibiting a phenotype of reduced malonyl-CoA levels in skeletal muscle and heart, unrestricted fat oxidation, and reduced fat accumulation in the liver and fat storage cells. As a result, the mice consume more food but accumulate less fat and remain leaner than wild type mice fed the same diet. These results demonstrate that inhibition of ACC2 acetyl-CoA carboxylase could be used to regulate fat oxidation and accumulation for purposes of weight control. The transgenic mice of the instant invention provide a useful animal model to identify such inhibitors and for studying the mechanisms of fat metabolism and weight control.
摘要翻译：本发明公开了乙酰辅酶A羧化酶的乙酰辅酶A羧化酶-2同种型的内源基因中具有失活突变的转基因小鼠。乙酰辅酶A羧化酶-2的失活导致在骨骼肌和心脏中表现出降低的丙二酰辅酶A水平的表型的小鼠，不受限制的脂肪氧化以及在肝脏和脂肪储存细胞中减少的脂肪蓄积。结果，小鼠消耗更多的食物，但是积累较少的脂肪，并且保持比通过相同饮食的野生型小鼠更瘦。这些结果表明，ACC2乙酰辅酶A羧化酶的抑制可用于调节脂肪氧化和积累，用于体重控制。本发明的转基因小鼠提供了一种有用的动物模型来鉴定这些抑制剂并用于研究脂肪代谢和体重控制的机制。

8. 发明申请

US20180071289A1 METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER AND RELATED HYPERPROLIFERATIVE DISORDERS 审中-公开
公开(公告)号：US20180071289A1
公开(公告)日：2018-03-15
申请号：US15658211
申请日：2017-07-24
申请人： Motonari UESUGI , Salih J. WAKIL , Lutfi ABU-ELHEIGA , Mizuki WATANABE
发明人： Motonari UESUGI , Salih J. WAKIL , Lutfi ABU-ELHEIGA , Mizuki WATANABE
IPC分类号： A61K31/5025 , C07D213/06 , A61K31/426 , C07D417/14 , C07D417/04 , C07D487/04 , C07D277/24 , A61K31/4709 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/496 , C07D213/76 , C07D235/14 , C07D417/12 , C07D277/22 , C07D213/16 , A61K31/437 , A61K31/427 , A61K31/428 , C07D471/04 , C07D277/66
CPC分类号： A61K31/5025 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , C07D213/06 , C07D213/16 , C07D213/76 , C07D235/14 , C07D277/22 , C07D277/24 , C07D277/66 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.

9. 发明授权

US09233941B2 Methods and compositions for the treatment of body weight related disorders 有权
标题翻译：用于治疗体重相关疾病的方法和组合物
公开(公告)号：US09233941B2
公开(公告)日：2016-01-12
申请号：US14270130
申请日：2014-05-05
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
IPC分类号： A61K31/427 , A61K31/4436 , A61K31/4439 , C07D277/66 , C07D417/04 , A61K45/06 , A61K31/428 , C07D471/04 , A61K31/437 , C07D417/12 , C07D417/14 , A61K31/4709 , A61K31/454 , C07D401/14 , C07D401/04 , A61K31/496 , A23L1/30 , A23K1/16 , C07D213/76 , C07D235/14 , C07D487/04 , C07D277/22 , C07D277/24 , C07D213/06 , C07D213/16 , A61K31/4418 , A61K31/495 , A61K31/5025
CPC分类号： A61K31/427 , A23K20/137 , A23L33/10 , A61K31/428 , A61K31/437 , A61K31/4418 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/5025 , A61K45/06 , C07D213/06 , C07D213/16 , C07D213/76 , C07D235/14 , C07D277/22 , C07D277/24 , C07D277/66 , C07D401/04 , C07D401/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.
摘要翻译：本发明涉及通过给予治疗有效量的具有一般三分体结构A-B-C的化合物来减少有需要的动物体重的方法。三方结构A，B和C是相同或不相同的结构，例如但不限于具有或不具有取代的杂环，苯基或苄基环结构，并在此详细描述。该方法可以使用具体的化合物，例如具有哌啶基，吡咯啉基或吡啶基A环，噻唑B环和可以独立地进一步取代的苯基C环。还提供了通过施用治疗有效量的所述化合物来增加产热而不减少体重减轻中的瘦体重的方法。

10. 发明授权

US09212179B2 Compositions and methods for the treatment of metabolic disorders 有权
标题翻译：用于治疗代谢紊乱的组合物和方法
公开(公告)号：US09212179B2
公开(公告)日：2015-12-15
申请号：US14310339
申请日：2014-06-20
申请人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
发明人： Motonari Uesugi , Salih J. Wakil , Lutfi Abu-Elheiga , Mizuki Watanabe
IPC分类号： C07D417/04 , C07D277/24 , C07D417/14 , C07D277/10 , C07D277/22
CPC分类号： C07D417/04 , C07D277/10 , C07D277/22 , C07D277/24 , C07D417/14
摘要： The present invention relates to the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. Also provided are methods for the treatment and/or prevention of one or more metabolic disorders, for example, obesity or diabetes, utilizing fatostatin A and/or a derivative and/or analog thereof and/or the A-B-C tripartite compounds.
摘要翻译：本发明涉及用于治疗和/或预防一种或多种代谢紊乱的化合物利用ABC三方结构，其中A，B和C是相同或不相同的结构，例如但不限于杂环，具有或不具有取代的苯基或苄基环结构，并在此详细描述。还提供了使用脂肪抑制素A和/或其衍生物和/或类似物和/或A-B-C三分体化合物治疗和/或预防一种或多种代谢紊乱（例如肥胖症或糖尿病）的方法。

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