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公开(公告)号：US07964608B2
公开(公告)日：2011-06-21
申请号：US12532861
申请日：2009-01-23
IPC分类号： A01N43/54 , A61K31/505 , C07D239/70 , C07D471/00
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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2.发明授权Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US08853226B2
公开(公告)日：2014-10-07
申请号：US13040382
申请日：2011-03-04
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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3.发明申请Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US20120172381A1
公开(公告)日：2012-07-05
申请号：US13410628
申请日：2012-03-02
IPC分类号： A61K31/519 , A61P11/06
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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4.发明授权Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US08329715B2
公开(公告)日：2012-12-11
申请号：US13410628
申请日：2012-03-02
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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5.发明申请Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors 有权三环化合物作为TNF-α合成的调节剂和PDE4抑制剂公开(公告)号：US20110160234A1
公开(公告)日：2011-06-30
申请号：US13040382
申请日：2011-03-04
IPC分类号： A61K31/519 , A61P11/00 , A61P11/06 , A61P19/02
CPC分类号： A61K31/519 , C07D471/04 , Y02A50/411
摘要： The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。
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![SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS](/abs-image/US/2012/04/26/US20120101093A1/abs.jpg.150x150.jpg)
6.发明申请SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS 审中-公开取代的咪唑并[1,2-A]吡啶衍生物，药物组合物和使用作为β-分泌酶抑制剂的方法公开(公告)号：US20120101093A1
公开(公告)日：2012-04-26
申请号：US13214762
申请日：2011-08-22
申请人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Robert Carl Andrews , Rongyuan Xie , Tan Ren
发明人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Robert Carl Andrews , Rongyuan Xie , Tan Ren
IPC分类号： A61K31/437 , A61K31/496 , A61K31/444 , A61K31/506 , A61P25/28 , A61K31/4545 , C07D471/04 , A61K31/5377
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention is directed to substituted imidazo[1,2-a]pyridine derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及取代的咪唑并[1,2-a]吡啶衍生物，其药学上可接受的盐，以及这些化合物或盐的互变异构体，其可抑制β-淀粉样蛋白前体蛋白切割酶（BACE），并且可以是 可用于治疗涉及BACE的疾病，例如阿尔茨海默病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及BACE的疾病中的用途。
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![Substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutical compositions, and methods of use as β-secretase inhibitors](/abs-image/US/2013/05/28/US08450354B2/abs.jpg.150x150.jpg)
7.发明授权Substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutical compositions, and methods of use as β-secretase inhibitors 失效取代的咪唑并[1,2-b]哒嗪衍生物，药物组合物和用作β-分泌酶抑制剂的方法公开(公告)号：US08450354B2
公开(公告)日：2013-05-28
申请号：US13052544
申请日：2011-03-21
申请人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Mohan Rao , Raju Bore Gowda , Robert Carl Andrews , Rongyuan Xie , Soumya P. Sahoo , Tan Ren , William Kenneth Banner
发明人： Adnan M. M. Mjalli , Anitha Hari , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Mohan Rao , Raju Bore Gowda , Robert Carl Andrews , Rongyuan Xie , Soumya P. Sahoo , Tan Ren , William Kenneth Banner
IPC分类号： A01N43/50 , A61K31/415 , C07D403/02
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit β-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.
摘要翻译： 本发明提供了取代的咪唑并[1,2-b]哒嗪衍生物，其药学上可接受的盐和任何前述的互变异构体，其中这些化合物抑制β-位淀粉样蛋白前体蛋白切割酶（BACE），其可能是有用的 用于治疗BACE所涉及的疾病，如阿尔茨海默病。 本发明还提供包含任何这些化合物的药物组合物以及这些化合物和组合物中任何一种用于治疗BACE所涉及的疾病，病症或病症的用途。
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公开(公告)号：US07727983B2
公开(公告)日：2010-06-01
申请号：US12399504
申请日：2009-03-06
申请人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
发明人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
IPC分类号： C07D498/02 , A61K31/5365
CPC分类号： C07D498/04 , C07D498/14
摘要： The present invention provides oxadiazoanthracene derivatives of the formula (I), wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, pharmaceutical compositions comprising oxadiazoanthracene derivatives, use of the oxadiazoanthracene derivatives for the preparation of pharmaceutical compositions, methods of use thereof for the treatment and/or prevention of disorders and diseases, such as diabetes, and intermediates useful for the preparation of oxadiazoanthracene derivatives of Formula (I).
摘要翻译： 本发明提供式（I）的恶二唑并蒽衍生物，其中A，B，C，R，R 1，R 2，R 3，R 4和R 5如本文所述，包含恶二唑并蒽衍生物的药物组合物，使用恶二唑衍生物用于制备 的药物组合物，其用于治疗和/或预防疾病和疾病的方法，例如糖尿病，以及可用于制备式（I）的恶二唑衍生物的中间体。
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公开(公告)号：US07906507B2
公开(公告)日：2011-03-15
申请号：US12849225
申请日：2010-08-03
申请人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
发明人： Adnan M. M. Mjalli , Dharma Rao Polisetti , Thomas Scott Yokum , Kalpathy Santhosh , Mustafa Guzel , Christopher Behme , Stephen Thomas Davis
IPC分类号： C07D498/02 , A61K31/5365
CPC分类号： C07D498/04 , C07D498/14
摘要： The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, and wherein said methods of use include uses for the treatment and/or prevention of disorders and diseases, such as diabetes.
摘要翻译： 本发明提供使用式（I）的恶二唑衍生物及其药学上可接受的盐的方法，其中A，B，C，R，R 1，R 2，R 3，R 4和R 5如本文所述，并且其中所述方法 包括用于治疗和/或预防疾病和疾病如糖尿病的用途。
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10.发明授权Substituted isoquinoline derivatives, pharmaceutical compositions, and methods of use as beta-secretase inhibitors 失效取代的异喹啉衍生物，药物组合物和用作β-分泌酶抑制剂的方法公开(公告)号：US08350039B2
公开(公告)日：2013-01-08
申请号：US13214434
申请日：2011-08-22
申请人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
发明人： Adnan M. M. Mjalli , Bapu Gaddam , Devi Reddy Gohimukkula , Dharma Rao Polisetti , Hassan El Abdellaoui , Mohan Rao , Pingzhen Wang , Robert Carl Andrews , Rongyuan Xie , Tan Ren
IPC分类号： C07D217/26 , A61K31/472 , A61K31/4725 , A61P25/28
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.
摘要翻译： 本发明涉及取代的异喹啉衍生物，其药学上可接受的盐，以及此类化合物或盐的互变异构体，其可抑制β-淀粉样蛋白前体蛋白切割酶（BACE），并可用于治疗疾病，其中 BACE参与，如阿尔茨海默病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及BACE的疾病中的用途。
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