公开(公告)号：US08383644B2

公开(公告)日：2013-02-26

申请号：US12825631

申请日：2010-06-29

申请人： Adnan M. M. Mjalli ,  Christopher Behme ,  Daniel P. Christen ,  Devi Reddy Gohimukkula ,  Dharma Rao Polisetti ,  James Quada ,  Jennifer L. R. Freeman ,  Kalpathy Santhosh ,  Muralidhar Bondlela ,  Mustafa Guzel ,  Ravindra Reddy Yarragunta ,  Robert Carl Andrews ,  Stephen Thomas Davis ,  Thomas Scott Yokum

发明人： Adnan M. M. Mjalli ,  Christopher Behme ,  Daniel P. Christen ,  Devi Reddy Gohimukkula ,  Dharma Rao Polisetti ,  James Quada ,  Jennifer L. R. Freeman ,  Kalpathy Santhosh ,  Muralidhar Bondlela ,  Mustafa Guzel ,  Ravindra Reddy Yarragunta ,  Robert Carl Andrews ,  Stephen Thomas Davis ,  Thomas Scott Yokum

IPC分类号： C07D491/056 ,  A61K31/436

CPC分类号： C07D491/056 ,  C07D319/20 ,  C07D491/06

摘要： The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.

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。

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。

公开(公告)号：US08524708B2

公开(公告)日：2013-09-03

申请号：US12872580

申请日：2010-08-31

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。

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。

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。

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。

公开(公告)号：US20120101125A1

公开(公告)日：2012-04-26

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： A61K31/472 ,  A61K31/4725 ,  A61P25/28 ,  C07D217/26

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。

公开(公告)号：US08063081B2

公开(公告)日：2011-11-22

申请号：US11981997

申请日：2007-10-31

申请人： Dharma Rao Polisetti ,  Janos Tibor Kodra ,  Jesper Lau ,  Paw Bloch ,  Maria Carmen Valcarce Lopez ,  Niels Blume ,  Mustafa Guzel ,  Kalpathy Chidambareswaran Santhosh ,  Adnan M. M. Mjalli ,  Robert Carl Andrews ,  Govindan Subramanian ,  Michael Ankersen ,  Per Vedso ,  Anthony Murray ,  Lone Jeppesen

发明人： Dharma Rao Polisetti ,  Janos Tibor Kodra ,  Jesper Lau ,  Paw Bloch ,  Maria Carmen Valcarce Lopez ,  Niels Blume ,  Mustafa Guzel ,  Kalpathy Chidambareswaran Santhosh ,  Adnan M. M. Mjalli ,  Robert Carl Andrews ,  Govindan Subramanian ,  Michael Ankersen ,  Per Vedso ,  Anthony Murray ,  Lone Jeppesen

IPC分类号： A61K31/425 ,  A61K31/44 ,  C07D277/04 ,  C07D211/72

CPC分类号： C07D277/38 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  A61K31/55 ,  A61K45/06 ,  C07D213/75 ,  C07D277/46 ,  C07D277/48 ,  C07D277/52 ,  C07D277/54 ,  C07D277/56 ,  C07D285/135 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D473/38

摘要： This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.

摘要翻译： 本发明涉及作为葡萄糖激酶活化剂的芳基羰基衍生物，其可用于治疗，治疗，控制或辅助治疗疾病，其中增加葡糖激酶活性是有益的。

公开(公告)号：US20110201604A1

公开(公告)日：2011-08-18

申请号：US13028406

申请日：2011-02-16

申请人： Adnan M. M. Mjalli ,  Dharma Rao Polisetti ,  Jareer Nabeel Kassis ,  Matthew J. Kostura ,  Mustafa Guzel ,  Otis Clinton Attucks ,  Robert Carl Andrews ,  Samuel Victory ,  Suparna Gupta

发明人： Adnan M. M. Mjalli ,  Dharma Rao Polisetti ,  Jareer Nabeel Kassis ,  Matthew J. Kostura ,  Mustafa Guzel ,  Otis Clinton Attucks ,  Robert Carl Andrews ,  Samuel Victory ,  Suparna Gupta

IPC分类号： A61K31/428 ,  C07D417/12 ,  C07D417/14 ,  A61K31/5377 ,  C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/496 ,  A61K31/541 ,  A61K31/506 ,  A61P11/00 ,  A61P1/16 ,  A61P31/12 ,  A61P17/06 ,  A61P17/00 ,  A61P25/28 ,  A61P25/16 ,  A61P9/12 ,  A61P9/00 ,  A61P7/02 ,  A61P29/00 ,  A61P11/06 ,  A61P13/12 ,  A61P27/02 ,  A61P3/10 ,  A61P3/04 ,  A61P35/00

CPC分类号： C07D417/12 ,  A61K31/4168 ,  A61K31/4188 ,  A61K31/428 ,  A61K31/437 ,  C07D235/30 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

摘要翻译： 提供取代的稠合咪唑衍生物，其制备方法，包含取代的稠合咪唑衍生物的药物组合物和用于治疗炎症的方法。 取代的稠合咪唑衍生物可以控制血红素氧合酶的活性或活性和量的量。