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：US20110237570A1

公开(公告)日：2011-09-29

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： A61K31/55 ,  C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61P25/28 ,  A61P25/00 ,  A61P7/04

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-淀粉样蛋白前体蛋白切割酶（BACE），其可以是 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：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：US08598353B2

公开(公告)日：2013-12-03

申请号：US12950718

申请日：2010-11-19

申请人： Adnan M. M. Mjalli ,  David R. Jones ,  Devi Reddy Gohimukkula ,  Guoxiang Huang ,  Jeff J. Zhu ,  Mohan Rao ,  Robert C. Andrews ,  Tan Ren

发明人： Adnan M. M. Mjalli ,  David R. Jones ,  Devi Reddy Gohimukkula ,  Guoxiang Huang ,  Jeff J. Zhu ,  Mohan Rao ,  Robert C. Andrews ,  Tan Ren

IPC分类号： C07D401/12 ,  A61K31/4725

CPC分类号： C07D401/14 ,  A61K31/4725 ,  C07D235/30 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention 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 prevention or treatment of such diseases in which BACE is involved.

摘要翻译： 本发明涉及抑制β-位淀粉样蛋白前体蛋白切割酶（BACE）的苯并唑化合物，其可用于治疗或预防BACE所涉及的疾病如阿尔茨海默氏病。 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预防或治疗涉及BACE的疾病中的用途。

公开(公告)号：US20110160198A1

公开(公告)日：2011-06-30

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： A61K31/4741 ,  C07D491/056 ,  C07D498/04 ,  A61K31/497 ,  A61K31/5383 ,  A61K31/5377 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10 ,  A61P9/12

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.

摘要翻译： 本发明涉及调节人GLP-1受体并且可用于治疗人GLP-1受体调节有益的疾病，病症或病症的取代的偶氮蒽衍生物或其药学上可接受的盐， 例如2型糖尿病。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人GLP-1受体调节有益的疾病，病症或病症中的用途 。