公开(公告)号：US08551718B2

公开(公告)日：2013-10-08

申请号：US13519556

申请日：2010-03-31

申请人： Ishtiyaque Ahmad ,  Reddy Venkat Mekala ,  Reddy Muddukrishna Chillakur ,  Ramkumar Subramaniam ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Ramakrishna Nirogi ,  Venkateswarlu Jasti

发明人： Ishtiyaque Ahmad ,  Reddy Venkat Mekala ,  Reddy Muddukrishna Chillakur ,  Ramkumar Subramaniam ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Ramakrishna Nirogi ,  Venkateswarlu Jasti

IPC分类号： G01N33/567 ,  C12Q1/66

CPC分类号： G01N33/566 ,  G01N2333/726

摘要： The present invention provides novel functional assay for 5-HT2A, histamine H1 or adrenergic alpha 1b receptors, by measuring intracellular cyclic adenosine monophosphate (cAMP) levels utilizing reporter gene driven cell based assay. The novel assay provides both binding affinity as well as mode of action of compounds in a single set. The novel assay of the invention is useful in identification of compounds acting through 5-HT2A, histamine H1 or adrenergic alpha 1b receptors. Furthermore, the assay offers utility in categorizing compounds in to agonist, partial agonist, inverse agonist and antagonist classes. The novel assay can be scaled up to any high throughput format.

摘要翻译： 本发明通过使用基于报告基因驱动细胞的测定法测量细胞内环腺苷酸（cAMP）水平来提供5-HT2A，组胺H1或肾上腺素α1b受体的新功能测定。 该新型测定提供化合物在单一组中的结合亲和力以及作用模式。 本发明的新型测定法可用于鉴定通过5-HT2A，组胺H1或肾上腺素α1b受体起作用的化合物。 此外，该测定提供了将化合物分为激动剂，部分激动剂，反向激动剂和拮抗剂类别的效用。 该新型检测可以扩大到任何高通量格式。

公开(公告)号：US08404720B2

公开(公告)日：2013-03-26

申请号：US13063436

申请日：2009-03-03

申请人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Pradeep Jayarajan ,  Gopinadh Bhyrapuneni ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Pradeep Jayarajan ,  Gopinadh Bhyrapuneni ,  Venkateswarlu Jasti

IPC分类号： A61K31/4468 ,  C07D211/58

CPC分类号： C07D295/30 ,  C07D333/62

摘要： The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.

摘要翻译： 本发明涉及式（I）的新型芳基磺酰胺胺，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，本文所述的其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。

公开(公告)号：US20130072518A1

公开(公告)日：2013-03-21

申请号：US13499998

申请日：2009-12-31

申请人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Srinivas Veeramalla ,  Srinivasa Rao Ravella ,  Ishtiyague Ahmad ,  Pradeep Jayarajan ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampti ,  Gopinadh Bhyrapuneni ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Srinivas Veeramalla ,  Srinivasa Rao Ravella ,  Ishtiyague Ahmad ,  Pradeep Jayarajan ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampti ,  Gopinadh Bhyrapuneni ,  Venkateswarlu Jasti

IPC分类号： C07D401/12

CPC分类号： C07D401/12

摘要： The present invention relates to novel bicyclic compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment and prevention of various disorders that are related to α4β2 nicotinic receptors.

摘要翻译： 本发明涉及式（I）的新型双环化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物。 本发明还涉及制备上述新化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物的方法。 这些化合物可用于治疗和预防与α4和bgr2烟碱受体相关的各种疾病。

公开(公告)号：US20120277216A1

公开(公告)日：2012-11-01

申请号：US13393539

申请日：2009-12-29

申请人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Ishtiyaque Ahmad ,  Pradeep Jayarajan ,  Nagaraj Vishwottam Kandikere ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Gopinadh Bhyrapuneni ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Ishtiyaque Ahmad ,  Pradeep Jayarajan ,  Nagaraj Vishwottam Kandikere ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Gopinadh Bhyrapuneni ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Venkateswarlu Jasti

IPC分类号： A61K31/4709 ,  C07D471/08 ,  C07D401/14 ,  A61P25/00 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/28 ,  C07D401/12 ,  C07D413/12

CPC分类号： C07D401/12 ,  C07D471/10 ,  C07D471/12

摘要： The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them.The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.

摘要翻译： 本发明涉及新的式（I）的1,2-二氢-2-氧代喹啉化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂化物，水合物，代谢物，N-氧化物，药学上可接受的盐和组合物 包含它们 本发明还涉及制备上述新化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物的方法。 本发明的化合物可用于治疗/预防由5-HT4受体活性介导的各种疾病。

公开(公告)号：US09079894B2

公开(公告)日：2015-07-14

申请号：US13982486

申请日：2012-01-05

申请人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Suresh Yarlagadda ,  Srinivasa Rao Ravella ,  Anil Karbhari Shinde ,  Ramasastri Kambhampati ,  Praveen Kumar Roayapalley ,  Pradeep Jayarajan ,  Gopinadh Bhyrapuneni ,  Sriramachandra Murthy Patnala ,  Jyothsna Ravula ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Suresh Yarlagadda ,  Srinivasa Rao Ravella ,  Anil Karbhari Shinde ,  Ramasastri Kambhampati ,  Praveen Kumar Roayapalley ,  Pradeep Jayarajan ,  Gopinadh Bhyrapuneni ,  Sriramachandra Murthy Patnala ,  Jyothsna Ravula ,  Venkateswarlu Jasti

IPC分类号： A61K31/445 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07D211/22 ,  C07D211/32 ,  C07D413/14 ,  C07D413/06

CPC分类号： A61K31/454 ,  A61K31/4245 ,  C07D413/06 ,  C07D413/14

摘要： The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.

摘要翻译： 本发明涉及式（I）的新化合物及其药学上可接受的盐和组合物。 本发明还涉及制备上述新化合物及其药学上可接受的盐的方法。 式（I）化合物可用于治疗与5-HT4受体相关的各种疾病。

公开(公告)号：US09018231B2

公开(公告)日：2015-04-28

申请号：US13520136

申请日：2010-03-24

申请人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Rajesh Kumar Badange ,  Veena Reballi ,  Anil Kashinath Chindhe ,  Rambabu Namala ,  Mohamad Sadik Abdulhamid Mulla ,  Ishtiyaque Ahmad ,  Renny Abraham ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Rajesh Kumar Badange ,  Veena Reballi ,  Anil Kashinath Chindhe ,  Rambabu Namala ,  Mohamad Sadik Abdulhamid Mulla ,  Ishtiyaque Ahmad ,  Renny Abraham ,  Venkateswarlu Jasti

IPC分类号： C07D401/12 ,  A61K31/4468 ,  A61P25/18 ,  A61P25/28 ,  C07D211/58 ,  C07D401/14 ,  A61K31/4709 ,  A61K31/4725

CPC分类号： C07D211/58 ,  A61K31/4468 ,  A61K31/4709 ,  A61K31/4725 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them.These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.

摘要翻译： 本发明涉及作为式（I）的5-HT6受体配体的新型砜化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物 。 本发明还涉及制备上述新化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物的方法。 这些化合物可用于治疗/预防与5-HT 6受体功能相关的各种疾病。

公开(公告)号：US20140148440A1

公开(公告)日：2014-05-29

申请号：US13818152

申请日：2010-11-15

申请人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Ramasastri Kambhampati ,  Rambabu Namala ,  Adi Reddy Dwarampudi ,  Laxman Kota ,  Murlimohan Gampa ,  Padmavathi Kodru ,  Taraka Naga Vinaykumar Tiriveedhi ,  Vishwottam Nagaraj Kandikere ,  Nageshwara Rao Muddana ,  Ramanatha Shrikantha Saralaya ,  Pradeep Jayarajan ,  Dhanalakshmi Shanmuganathan ,  Ishtiyaque Ahmad ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Ramasastri Kambhampati ,  Rambabu Namala ,  Adi Reddy Dwarampudi ,  Laxman Kota ,  Murlimohan Gampa ,  Padmavathi Kodru ,  Taraka Naga Vinaykumar Tiriveedhi ,  Vishwottam Nagaraj Kandikere ,  Nageshwara Rao Muddana ,  Ramanatha Shrikantha Saralaya ,  Pradeep Jayarajan ,  Dhanalakshmi Shanmuganathan ,  Ishtiyaque Ahmad ,  Venkateswarlu Jasti

IPC分类号： C07D513/04 ,  C07D417/12

CPC分类号： C07D513/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

摘要： The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.

摘要翻译： 本发明涉及式（I）的杂环基化合物及其药学上可接受的盐和组合物。 本发明还涉及制备上述新化合物及其药学上可接受的盐的方法。 式（I）化合物可用于治疗与组胺H3受体相关的各种疾病，例如认知障碍，睡眠障碍，肥胖症和疼痛。

公开(公告)号：US20130005709A1

公开(公告)日：2013-01-03

申请号：US13520136

申请日：2010-03-24

申请人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Rajesh Kumar Badange ,  Veena Reballi ,  Anil Kashinath Chindhe ,  Rambabu Namala ,  Mohamad Sadik Abdulhamid Mulla ,  Ishtiyaque Ahmad ,  Renny Abraham ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Anil Karbhari Shinde ,  Rama Sastri Kambhampati ,  Rajesh Kumar Badange ,  Veena Reballi ,  Anil Kashinath Chindhe ,  Rambabu Namala ,  Mohamad Sadik Abdulhamid Mulla ,  Ishtiyaque Ahmad ,  Renny Abraham ,  Venkateswarlu Jasti

IPC分类号： A61K31/454 ,  C07D211/58 ,  A61K31/4468 ,  C07D401/14 ,  A61P25/18 ,  A61K31/4725 ,  A61K31/55 ,  A61P25/28 ,  A61P25/24 ,  C07D401/12 ,  A61K31/4709

CPC分类号： C07D211/58 ,  A61K31/4468 ,  A61K31/4709 ,  A61K31/4725 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them.These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.

摘要翻译： 本发明涉及作为式（I）的5-HT6受体配体的新型砜化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物 。 本发明还涉及制备上述新化合物及其衍生物，前体药物，互变异构体，立体异构体，多晶型物，溶剂合物，水合物，代谢物，N-氧化物，药学上可接受的盐和含有它们的组合物的方法。 这些化合物可用于治疗/预防与5-HT 6受体功能相关的各种疾病。

公开(公告)号：US20120315657A1

公开(公告)日：2012-12-13

申请号：US13519556

申请日：2010-03-31

申请人： Ishtiyaque Ahmad ,  Reddy Venkat Mekala ,  Reddy Muddukrishna Chillakur ,  Ramkumar Subramaniam ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Ramakrishna Nirogi ,  Venkateswarlu Jasti

发明人： Ishtiyaque Ahmad ,  Reddy Venkat Mekala ,  Reddy Muddukrishna Chillakur ,  Ramkumar Subramaniam ,  Jyothsna Ravula ,  Sriramachandra Murthy Patnala ,  Ramakrishna Nirogi ,  Venkateswarlu Jasti

IPC分类号： G01N21/76

CPC分类号： G01N33/566 ,  G01N2333/726

摘要： The present invention provides novel functional assay for 5-HT2A, histamine H1 or adrenergic alpha 1b receptors, by measuring intracellular cyclic adenosine monophosphate (cAMP) levels utilizing reporter gene driven cell based assay. The novel assay provides both binding affinity as well as mode of action of compounds in a single set. The novel assay of the invention is useful in identification of compounds acting through 5-HT2A, histamine H1 or adrenergic alpha 1b receptors. Furthermore, the assay offers utility in categorizing compounds in to agonist, partial agonist, inverse agonist and antagonist classes. The novel assay can be scaled up to any high throughput format.

摘要翻译： 本发明通过使用基于报告基因驱动细胞的测定法测量细胞内环腺苷酸（cAMP）水平来提供5-HT2A，组胺H1或肾上腺素α1b受体的新功能测定。 该新型测定提供化合物在单一组中的结合亲和力以及作用模式。 本发明的新型测定法可用于鉴定通过5-HT2A，组胺H1或肾上腺素α1b受体起作用的化合物。 此外，该测定提供了将化合物分为激动剂，部分激动剂，反向激动剂和拮抗剂类别的效用。 该新型检测可以扩大到任何高通量格式。

公开(公告)号：US08003670B2

公开(公告)日：2011-08-23

申请号：US12598616

申请日：2008-04-15

申请人： Ramakrishna Nirogi ,  Rama Sastri Kambhampati ,  Anil Karbhari Shinde ,  Anand Vijaykumar Daulatabad ,  Adi Reddy Dwarampudi ,  Nagaraj Vishwottam Kandikere ,  Santosh Vishwakarma ,  Venkateswarlu Jasti

发明人： Ramakrishna Nirogi ,  Rama Sastri Kambhampati ,  Anil Karbhari Shinde ,  Anand Vijaykumar Daulatabad ,  Adi Reddy Dwarampudi ,  Nagaraj Vishwottam Kandikere ,  Santosh Vishwakarma ,  Venkateswarlu Jasti

IPC分类号： A61K31/454 ,  A61K31/405 ,  C07D401/12 ,  C07D209/04

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D401/12

摘要： The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.

摘要翻译： 本发明涉及式（I）的新型氨基烷氧基芳基磺酰胺化合物，其衍生物，其立体异构体，其药学上可接受的盐和含有它们的药学上可接受的组合物。 本发明还涉及制备上述新化合物，其衍生物，其立体异构体，其药学上可接受的盐和含有它们的药学上可接受的组合物的方法。 这些化合物可用于治疗与5-HT 6受体功能相关的各种疾病。 具体地说，本发明的化合物也可用于治疗各种CNS病症，血液病症，进食障碍，与疼痛有关的疾病，呼吸系统疾病，泌尿系疾病，心血管疾病和癌症。