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：US08431575B2

公开(公告)日：2013-04-30

申请号：US13028036

申请日：2011-02-15

申请人： Devi R Gohimukkula ,  David Robert Jones ,  Ghassan Qabaja ,  Jeff J Zhu ,  Jeremy T Cooper ,  William K Banner ,  Kurt Sundermann ,  Muralidhar Bondlela ,  Mohan Rao ,  Pingzhen Wang ,  Suparna Gupta ,  Anitha Hari ,  Raju B Gowda ,  Robert C Andrews

发明人： Devi R Gohimukkula ,  David Robert Jones ,  Ghassan Qabaja ,  Jeff J Zhu ,  Jeremy T Cooper ,  William K Banner ,  Kurt Sundermann ,  Muralidhar Bondlela ,  Mohan Rao ,  Pingzhen Wang ,  Suparna Gupta ,  Anitha Hari ,  Raju B Gowda ,  Robert C Andrews

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

CPC分类号： C07D401/12 ,  A61K31/497 ,  C07D237/14 ,  C07D237/24 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D453/02 ,  C07D471/04

摘要： The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

摘要翻译： 本发明提供式（I）的苯基 - 杂芳基衍生物及其药学上可接受的盐。这些化合物可用于治疗RAGE介导的疾病如阿尔茨海默氏病。 本发明还涉及制备式（I）的化合物及其药学上可接受的盐，包含这些化合物的药物组合物的方法，以及这些化合物和/或药物组合物在治疗RAGE介导的疾病中的用途。

公开(公告)号：US08404731B2

公开(公告)日：2013-03-26

申请号：US12685178

申请日：2010-01-11

申请人： Adnan M. M. Mjalli ,  Dharma R. Polisetti ,  Govindan Subramanian ,  James C. Quada ,  Ravindra R. Yarragunta ,  Robert C. Andrews ,  Rongyuan Xie

发明人： Adnan M. M. Mjalli ,  Dharma R. Polisetti ,  Govindan Subramanian ,  James C. Quada ,  Ravindra R. Yarragunta ,  Robert C. Andrews ,  Rongyuan Xie

IPC分类号： A61K31/4178 ,  C07D233/64

CPC分类号： C07D417/14 ,  C07D417/10

摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.

摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。

公开(公告)号：US08377983B2

公开(公告)日：2013-02-19

申请号：US12703604

申请日：2010-02-10

申请人： Adnan M. M. Mjalli ,  Brian S. Grella ,  Govindan Subramanian ,  Murty N. Arimilli ,  Ramesh Gopalaswamy ,  Robert C. Andrews ,  Stephen Davis ,  Xiaochuan Guo ,  Jeff Zhu

发明人： Adnan M. M. Mjalli ,  Brian S. Grella ,  Govindan Subramanian ,  Murty N. Arimilli ,  Ramesh Gopalaswamy ,  Robert C. Andrews ,  Stephen Davis ,  Xiaochuan Guo ,  Jeff Zhu

IPC分类号： A01N43/38 ,  A01N43/52 ,  A61K31/405 ,  A61K31/497 ,  A61K31/535 ,  A61K31/415 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04

摘要： The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.

摘要翻译： 本发明涉及治疗癌症的化合物和方法。 本发明提供抑制极光激酶的化合物，包含抑制极光激酶的化合物的药物组合物，以及使用本发明化合物或包含本发明化合物的药物组合物治疗癌症的方法。

公开(公告)号：US20120196906A1

公开(公告)日：2012-08-02

申请号：US13412747

申请日：2012-03-06

申请人： Adnan M.M. Mjalli ,  Dharma R. Polisetti ,  Govindan Subramanian ,  James C. Quada ,  Ravindra R. Yarragunta ,  Robert C. Andrews ,  Rongyuan Xie

发明人： Adnan M.M. Mjalli ,  Dharma R. Polisetti ,  Govindan Subramanian ,  James C. Quada ,  Ravindra R. Yarragunta ,  Robert C. Andrews ,  Rongyuan Xie

IPC分类号： A61K31/433 ,  A61P3/10 ,  A61P31/18 ,  A61P37/08 ,  A61P25/28 ,  A61P17/06 ,  A61P31/00 ,  A61P3/04 ,  A61P35/00 ,  C07D417/10 ,  A61P29/00

CPC分类号： C07D417/14 ,  C07D417/10

摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.

摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。

公开(公告)号：US07776919B2

公开(公告)日：2010-08-17

申请号：US12019045

申请日：2008-01-24

申请人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Christopher L. Wysong

发明人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Christopher L. Wysong

IPC分类号： A01N37/18 ,  C07C237/00 ,  C07C233/00 ,  C07C235/00

CPC分类号： C07D231/12 ,  C07C235/38 ,  C07C237/20 ,  C07C271/22 ,  C07C2601/08 ,  C07C2603/18 ,  C07D207/16 ,  C07D211/34 ,  C07D217/26 ,  C07D233/56 ,  C07D249/08 ,  C07D309/04

摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

摘要翻译： 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，淀粉样蛋白和 两性霉素，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

公开(公告)号：US07737285B2

公开(公告)日：2010-06-15

申请号：US11800085

申请日：2007-05-03

申请人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Anitha Hari ,  Kwasi A. Avor ,  Ghassan Qabaja ,  Xiao-Chuan Guo ,  Suparna Gupta ,  David R. Jones ,  Xin Chen

发明人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Anitha Hari ,  Kwasi A. Avor ,  Ghassan Qabaja ,  Xiao-Chuan Guo ,  Suparna Gupta ,  David R. Jones ,  Xin Chen

IPC分类号： C07D233/61 ,  A01N43/50

CPC分类号： C07D233/64 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D235/18 ,  C07D235/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02

摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

摘要翻译： 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，淀粉样蛋白和 两性霉素，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

公开(公告)号：US07714013B2

公开(公告)日：2010-05-11

申请号：US11511163

申请日：2006-08-28

申请人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Anitha Hari ,  Kwasi A. Avor ,  Ghassan Qabaja ,  Xiao-Chuan Guo ,  Suparna Gupta ,  David R. Jones ,  Xin Chen

发明人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Ramesh Gopalaswamy ,  Anitha Hari ,  Kwasi A. Avor ,  Ghassan Qabaja ,  Xiao-Chuan Guo ,  Suparna Gupta ,  David R. Jones ,  Xin Chen

IPC分类号： A61K31/4164 ,  A61K31/4178 ,  C07D233/64 ,  C07D403/02

CPC分类号： C07D233/64 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D235/18 ,  C07D235/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02

摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

公开(公告)号：US20100113331A1

公开(公告)日：2010-05-06

申请号：US12685178

申请日：2010-01-11

申请人： ADNAN M. M. MJALLI ,  DHARMA R. POLISETTI ,  GOVINDAN SUBRAMANIAN ,  JAMES C. QUADA ,  RAVINDRA R. YARRAGUNTA ,  ROBERT C. ANDREWS ,  RONGYUAN XIE

发明人： ADNAN M. M. MJALLI ,  DHARMA R. POLISETTI ,  GOVINDAN SUBRAMANIAN ,  JAMES C. QUADA ,  RAVINDRA R. YARRAGUNTA ,  ROBERT C. ANDREWS ,  RONGYUAN XIE

IPC分类号： A61K31/433 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/715 ,  A61K38/28 ,  A61P3/00 ,  A61P3/10 ,  A61P37/00 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D417/14 ,  C07D417/10

摘要： The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.

摘要翻译： 本发明提供式（I-IV）的咪唑衍生物，其制备方法，包含式（I-IV）化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物抑制蛋白酪氨酸磷酸酶1B，因此可用于对由PTPase活性介导的疾病的治疗，治疗，控制或辅助治疗。 这些疾病包括I型糖尿病和II型糖尿病。

公开(公告)号：US07459472B2

公开(公告)日：2008-12-02

申请号：US10913216

申请日：2004-08-06

申请人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Murty N. Arimilli ,  Mohan Rao ,  Mustafa Guzel ,  Muralidhar Bondlela ,  Xiao-Chuan Guo ,  Guoxiang Huang

发明人： Adnan M. M. Mjalli ,  Robert C. Andrews ,  Murty N. Arimilli ,  Mohan Rao ,  Mustafa Guzel ,  Muralidhar Bondlela ,  Xiao-Chuan Guo ,  Guoxiang Huang

IPC分类号： A61K31/41 ,  C07D271/06

CPC分类号： C07D295/155 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07C2601/08

摘要： This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. Compounds of Formula (I) may be useful for treating viral infections including orthopox viruses, either alone or in combination with other therapeutic agents.

摘要翻译： 本发明提供了本文所述的式（I）的芳基和杂芳基化合物及其制备方法。 还提供了用式（I）的化合物制备的药物组合物和制备这些组合物的方法。 式（I）的化合物可用于单独或与其它治疗剂组合治疗包括正痘病毒的病毒感染。