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1. 发明专利

IL259199D0 Ion channel inhibitory compounds, pharmaceutical formulations and uses 未知
公开(公告)号：IL259199D0
公开(公告)日：2018-07-31
申请号：IL25919918
申请日：2018-05-08
申请人： AFASCI INC , XINMIN XIE , FRANK KAYSER
发明人： XINMIN XIE , FRANK KAYSER
IPC分类号： A61K20060101
摘要： The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and/or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.

2. 发明专利

IL259199A Ion channel inhibitory compounds, pharmaceutical formulations and uses 未知
公开(公告)号：IL259199A
公开(公告)日：2022-03-01
申请号：IL25919918
申请日：2018-05-08
申请人： AFASCI INC , XINMIN XIE , FRANK KAYSER
发明人： XINMIN XIE , FRANK KAYSER
IPC分类号： A61K31/4747 , A61K31/4453 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P29/00 , A61P43/00
摘要： The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and/or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.

3. 发明专利

IL273990D0 Broad spectrum antiviral compositions and methods 未知
公开(公告)号：IL273990D0
公开(公告)日：2020-05-31
申请号：IL27399020
申请日：2020-04-16
申请人： EVRYS BIO LLC , STACY REMISZEWSKI , QUN SUN , LILLIAN W CHIANG , EAIN ANTHONY MURPHY , FRANK KAYSER , SARAH JOCELYN FINK
发明人： STACY REMISZEWSKI , QUN SUN , LILLIAN W CHIANG , EAIN ANTHONY MURPHY , FRANK KAYSER , SARAH JOCELYN FINK
IPC分类号： A61K31/4725 , A61K31/4741 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K45/06 , A61P31/12
摘要： Novel thiazole- and isoquinoline-containing compounds are presented that are useful for treating and/or preventing broad-spectrum viral infections. Methods of treating and/or preventing broad-specturm viral infections are also presented. These compounds have shown inhibition of HCMV, influenza viruses, Zika virus, BK Virus and RSV replication in cell-based assays.

4. 发明授权

US07763624B2 Substituted pyrazolo[3,4-d]pyrimidines as ACK-1 and LCK inhibitors 有权
标题翻译：取代的吡唑并[3,4-d]嘧啶作为ACK-1和LCK抑制剂
公开(公告)号：US07763624B2
公开(公告)日：2010-07-27
申请号：US11506381
申请日：2006-08-18
申请人： John L. Buchanan , William H. Buckner , Mario G. Cardozo , Erin F. DiMauro , Jiasheng Fu , Xiaolin Hao , Xian Yun Jiao , Frank Kayser , David J. Kopecky , Craig E. Masse , Susan A. Tomlinson , Ryan White , Xiaotian Zhu
发明人： John L. Buchanan , William H. Buckner , Mario G. Cardozo , Erin F. DiMauro , Jiasheng Fu , Xiaolin Hao , Xian Yun Jiao , Frank Kayser , David J. Kopecky , Craig E. Masse , Susan A. Tomlinson , Ryan White , Xiaotian Zhu
IPC分类号： C07D487/04 , A61K31/519 , A61K31/496 , A61P35/00 , C07D231/56 , A61K31/416
CPC分类号： C07D403/06 , C07D231/56 , C07D401/14 , C07D405/06 , C07D487/04
摘要： The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.
摘要翻译：本发明涉及式I化合物或立体异构体，互变异构体，溶剂合物，药学上可接受的盐或前药，含有化合物的药物制剂，使用该化合物的治疗方法，例如蛋白质酪氨酸激酶相关诸如免疫学和肿瘤学障碍的疾病以及制备包含该化合物的药物的方法。

5. 发明授权

US07645779B2 Linked biaryl compounds 失效
标题翻译：联结联芳基化合物
公开(公告)号：US07645779B2
公开(公告)日：2010-01-12
申请号：US10939918
申请日：2004-08-20
申请人： Hiroyuki Abe , Jonathan Houze , Hisashi Kawasaki , Frank Kayser , Rajiv Sharma , Samuel Sperry
发明人： Hiroyuki Abe , Jonathan Houze , Hisashi Kawasaki , Frank Kayser , Rajiv Sharma , Samuel Sperry
IPC分类号： A61K31/44 , A61K31/19 , C07D213/02
CPC分类号： C07C317/22 , C07C323/20 , C07C323/21 , C07C2602/10
摘要： Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.
摘要翻译：本文提供了可用于治疗代谢紊乱，炎性疾病和癌症的化合物，组合物和方法。特别地，本发明提供调节参与脂质代谢，炎症和细胞增殖的蛋白质的表达和/或功能的化合物。主题化合物是联芳基化合物。

6. 发明授权

US07358250B2 Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity 失效
标题翻译：吡咯并[2,3-d]嘧啶，其调节ACK1活性
公开(公告)号：US07358250B2
公开(公告)日：2008-04-15
申请号：US11169313
申请日：2005-06-29
申请人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
发明人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
IPC分类号： C07D487/04 , C07D413/10 , A61P35/04 , C07F9/02 , A61K31/519 , A61K31/5355 , A61K31/675
CPC分类号： C07D487/04
摘要： Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.
摘要翻译：描述了调节ACK1和LCK的作用的化合物以及用于治疗ACK1和LCK介导的疾病的相关组合物方法。在一个方面，化合物具有一般结构：其中本文提供取代基的值。

7. 发明授权

US07326812B2 Arylsulfonamidobenzylic compounds 失效
标题翻译：芳基磺酰胺基苄基化合物
公开(公告)号：US07326812B2
公开(公告)日：2008-02-05
申请号：US11333958
申请日：2006-01-17
申请人： Xian Yun Jiao , Frank Kayser , Sharon McKendry , Derek E. Piper , Andrew K. Shiau
发明人： Xian Yun Jiao , Frank Kayser , Sharon McKendry , Derek E. Piper , Andrew K. Shiau
IPC分类号： C07C311/15
CPC分类号： C07D207/33 , C07C311/21 , C07C317/32 , C07C2601/08 , C07C2601/16 , C07D207/333 , C07D207/335 , C07D213/30 , C07D213/42 , C07D231/12 , C07D233/61 , C07D233/64 , C07D235/12 , C07D235/14 , C07D239/26 , C07D257/04 , C07D277/24 , C07D277/28 , C07D333/34 , C07F7/081
摘要： Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.
摘要翻译：提供了芳基磺酰胺苄醇，胺和磺酰胺，其可用于治疗脂质疾病，代谢疾病和细胞增殖性疾病。

8. 发明授权

US07244727B2 Fused bicyclic nitrogen-containing heterocycles 失效
标题翻译：稠合双环含氮杂环
公开(公告)号：US07244727B2
公开(公告)日：2007-07-17
申请号：US10720844
申请日：2003-11-21
申请人： Brian M. Fox , Noboru Furukawa , Xiaolin Hao , Kiyosei Iio , Takashi Inaba , Simon M. Jackson , Frank Kayser , Marc Labelle , Kexue Li , Takuya Matsui , Dustin L. McMinn , Nobuya Ogawa , Steven M. Rubenstein , Shoichi Sagawa , Kazuyuki Sugimoto , Masahiro Suzuki , Masahiro Tanaka , Guosen Ye , Atsuhito Yoshida , Jian Zhang
发明人： Brian M. Fox , Noboru Furukawa , Xiaolin Hao , Kiyosei Iio , Takashi Inaba , Simon M. Jackson , Frank Kayser , Marc Labelle , Kexue Li , Takuya Matsui , Dustin L. McMinn , Nobuya Ogawa , Steven M. Rubenstein , Shoichi Sagawa , Kazuyuki Sugimoto , Masahiro Suzuki , Masahiro Tanaka , Guosen Ye , Atsuhito Yoshida , Jian Zhang
IPC分类号： C07D498/04 , A61K31/542 , A61P3/04 , A61P3/08 , C07D491/04 , C07D495/04 , A61K31/538 , A61K31/519
CPC分类号： C07D491/04
摘要： Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.
摘要翻译：本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。特别地，本发明提供调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

9. 发明申请

US20060046977A1 Furanopyridine derivatives and methods of use 有权
标题翻译：呋喃并吡啶衍生物和使用方法
公开(公告)号：US20060046977A1
公开(公告)日：2006-03-02
申请号：US11184237
申请日：2005-07-18
申请人： Joseph Nunes , Matthew Martin , Ryan White , David McGowan , Jean Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , Xian Jiao
发明人： Joseph Nunes , Matthew Martin , Ryan White , David McGowan , Jean Bemis , Frank Kayser , Jiasheng Fu , Jinqian Liu , Xian Jiao
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4741 , C07F7/02 , C07D491/02 , A61K31/695
CPC分类号： C07D491/04 , C07D491/14
摘要： The present invention relates to furanopyridine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of modulating Lck and ACK-1 enzymes and of treating various related diseases and conditions, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, comprising administering to the mammal a therapeutically effective amount a compound of Formula I, as described above, and methods of manufacturing medicaments comprising the compound of Formula I.
摘要翻译：本发明涉及具有通式I的呋喃并吡啶化合物及其立体异构体，互变异构体，溶剂合物，药用盐和衍生物及其前药。本发明还包括药物组合物，其包含式I化合物，调节Lck和ACK-1酶的方法以及治疗各种相关疾病和病症，包括炎症，T细胞活化抑制，增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗塞，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球肾炎，过敏性疾病，哮喘，干草组织，湿疹，癌症，结肠癌，胸腺瘤，仅举几个例子，在哺乳动物中，包括向哺乳动物施用治疗有效量的如上所述的式I化合物和制备包含以下化合物的药物的方法：一级方程式

10. 发明授权

US06869975B2 Linked biaryl compounds 失效
标题翻译：联结联芳基化合物
公开(公告)号：US06869975B2
公开(公告)日：2005-03-22
申请号：US10244063
申请日：2002-09-13
申请人： Hiroyuki Abe , Jonathan Houze , Hisashi Kawasaki , Frank Kayser , Rajiv Sharma , Samuel Sperry
发明人： Hiroyuki Abe , Jonathan Houze , Hisashi Kawasaki , Frank Kayser , Rajiv Sharma , Samuel Sperry
IPC分类号： C07D215/20 , A61K31/192 , A61K31/216 , A61K31/4184 , A61K31/421 , A61K31/426 , A61K31/4406 , A61K31/47 , A61P1/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/00 , A61P25/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , C07C317/22 , C07C321/30 , C07C323/20 , C07C323/21 , C07D213/65 , C07D215/22 , C07D235/26 , C07D263/40 , C07D277/20 , C07D277/34 , A01N37/10
CPC分类号： C07C317/22 , C07C323/20 , C07C323/21 , C07C2602/10
摘要： Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.
摘要翻译：本文提供了可用于治疗代谢紊乱，炎性疾病和癌症的化合物，组合物和方法。特别地，本发明提供调节参与脂质代谢，炎症和细胞增殖的蛋白质的表达和/或功能的化合物。主题化合物是联芳基化合物。

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