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公开(公告)号：EP1934203A2
公开(公告)日：2008-06-25
申请号：EP06802156.7
申请日：2006-08-23
发明人： MCCORMICK, Kevin, D. , BOYCE, Christopher, W. , SHIH, Neng-Yang , ASLANIAN, Robert, G. , MANGIARACINA, Pietro , DE LERA RUIZ, Manuel , YU, Younong , BIJU, Purakkattle, J. , HUANG, Chia-Yu , LIANG, Bo , LIU, Ruiyan , LIU, Rong-Qiang , GUISE-ZAWACKI, Lisa
IPC分类号： C07D403/06 , C07D413/06 , C07D417/06 , A61K31/435 , A61K31/41 , A61P29/00
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as a2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the a2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
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公开(公告)号：EP1694659B8
公开(公告)日：2008-10-08
申请号：EP04814266.5
申请日：2004-12-16
发明人： BIJU, Purakkattle, J. , TAVERAS, Arthur, G. , YU, Younong , ZHENG, Junying , CHAO, Jianhua , AKI, Cynthia, J. , FINE, Jay , LUNDELL, Daniel , PRIESTLEY, Tony , REGGIANI, Angelo , MERRITT, J., Robert , BALDWIN, John, J.
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , A61K31/433 , A61K31/4436
CPC分类号： C07D285/10 , C07D285/06 , C07D417/12 , C07D417/14
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3.发明授权THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS 有权THIADIAZOLDIOXIDE和THIADIAZOLOXIDE AS趋化因子受体CC和配体
公开(公告)号：EP1551818B1
公开(公告)日：2009-02-04
申请号：EP03781311.0
申请日：2003-10-07
发明人： TAVERAS, Arthur, G. , CHAO, Jianhua , BIJU, Purakkattle, J. , YU, Younong , FINE, Jay, S. , HIPKIN, William , AKI, Cynthia, J. , MERRITT, J., Robert , LI, Ge , BALDWIN, John, J. , LAI, Gaifa , WU, Minglang , HECKER, Evan, A.
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , A61K31/433 , A61K31/4436
CPC分类号： C07D285/10 , C07D417/02 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
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4.发明公开C-21 THIOETHERS AS GLUCOCORTICOID RECEPTOR AGONISTS 审中-公开C-21-THIOETHER ALS GLUCOCORTICOIDREZEPTORAGONISTEN
公开(公告)号：EP2235035A2
公开(公告)日：2010-10-06
申请号：EP08866275.4
申请日：2008-12-18
发明人： ANTHES, John, C. , MCCORMICK, Kevin, D. , HEY, John, A. , ASLANIAN, Robert, G. , BIJU, Purakkattle, J. , BERLIN, Michael, Y. , SOLOMON, Daniel, M.
CPC分类号： C07J43/003 , C07J31/006 , C07J71/0031
摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R
1 , R
2 , R
3 , R
4 , and R
5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.-
公开(公告)号：EP1694659B1
公开(公告)日：2008-08-27
申请号：EP04814266.5
申请日：2004-12-16
发明人： BIJU, Purakkattle, J. , TAVERAS, Arthur, G. , YU, Younong , ZHENG, Junying , CHAO, Jianhua , AKI, Cynthia, J. , FINE, Jay , LUNDELL, Daniel , PRIESTLEY, Tony , REGGIANI, Angelo , MERRITT, J., Robert , BALDWIN, John, J.
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , A61K31/433 , A61K31/4436
CPC分类号： C07D285/10 , C07D285/06 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).
摘要翻译： 公开了式（IA）的新化合物及其药学上可接受的盐和溶剂化物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的例子包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病例如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化症，类风湿性关节炎，骨关节炎，中风和局部缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎症性疼痛和神经性疼痛）使用式（IA）的化合物。
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6.发明公开
公开(公告)号：EP1697354A1
公开(公告)日：2006-09-06
申请号：EP04814856.3
申请日：2004-12-20
发明人： TAVERAS, Arthur, G. , ZHENG, Junying , BIJU, Purakkattle, J. , YU, Younong , CHAO, Jianhua , FINE, Jay , LUNDELL, Daniel , PRIESTLEY, Tony , REGGIANI, Angelo , MERRITT, J., Robert , BALDWIN, John, J. , LAI, Gaifa , WU, Minglang
IPC分类号： C07D417/12 , C07D275/02 , C07D417/14 , A61K31/427 , A61P35/00 , A61P29/00
CPC分类号： C07D275/03 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
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7.发明公开NOVEL [3,2-c]HETEROARYL STEROIDS AS GLUCOCORTICOID RECEPTOR AGONISTS, COMPOSITIONS AND USES THEREOF 审中-公开NEW并[3,2-C] HETEROARYLSTEROIDE ALS糖皮质激素受体，组合物和使用
公开(公告)号：EP2443134A2
公开(公告)日：2012-04-25
申请号：EP10727310.4
申请日：2010-06-15
申请人： Schering Corporation
发明人： BIJU, Purakkattle, J. , BERLIN, Michael, Y. , LIM, Yeon-Hee , BITAR, Rema, D. , MCCORMICK, Kevin, D. , ASLANIAN, Robert, G. , LEE, Yoon Joo , ZHENG, Junying , HUANG, Ying , WON, Walter
CPC分类号： C07J71/0047 , C07J71/0063
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: Formula (I) wherein L, R
1 , R
2 , R
3 , R
4 , R
5 , and R
6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas (H-A), (II-A1 ), (II-A2), (II-A2.1 ), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (Vl), as described herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.-
公开(公告)号：EP2245042A1
公开(公告)日：2010-11-03
申请号：EP08868864.3
申请日：2008-12-18
申请人： Schering Corporation
发明人： ANTHES, John, C. , MCCORMICK, Kevin, D. , HEY, John, A. , ASLANIAN, Robert, G. , BIJU, Purakkattle, J. , BERLIN, Michael, Y. , SOLOMON, Daniel, M. , WANG, Hongwu , LIM, Yeon-hee , LEE, Yoon Joo , BITAR, Rema Danielle
CPC分类号： C07J43/003
摘要： The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having general structure (I); wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and Vl, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
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9.发明授权3,4-dihydro-2H-benzo[1,4]oxazine and 3,4-dihydro-2H-benzo[1,4]thiazine COMPOUNDS AS ALPHA2C ADRENORECEPTOR AGONISTS 有权3,4-二氢-2H-苯并[1,4]恶嗪和3,4-二氢-2H-苯并[1,4]噻嗪化合物作为alpha2C阻断剂
公开(公告)号：EP1934203B1
公开(公告)日：2010-08-18
申请号：EP06802156.7
申请日：2006-08-23
发明人： MCCORMICK, Kevin, D. , BOYCE, Christopher, W. , SHIH, Neng-Yang , ASLANIAN, Robert, G. , MANGIARACINA, Pietro , DE LERA RUIZ, Manuel , YU, Younong , BIJU, Purakkattle, J. , HUANG, Chia-Yu , LIANG, Bo , LIU, Ruiyan , LIU, Rong-Qiang , GUISE-ZAWACKI, Lisa
IPC分类号： C07D403/06 , C07D413/06 , C07D417/06 , A61K31/435 , A61K31/41 , A61P29/00
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as a2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the a2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
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公开(公告)号：EP1694659A1
公开(公告)日：2006-08-30
申请号：EP04814266.5
申请日：2004-12-16
发明人： BIJU, Purakkattle, J. , TAVERAS, Arthur, G. , YU, Younong , ZHENG, Junying , CHAO, Jianhua , AKI, Cynthia, J. , FINE, Jay , LUNDELL, Daniel , PRIESTLEY, Tony , REGGIANI, Angelo , MERRITT, J., Robert , BALDWIN, John, J.
IPC分类号： C07D285/10 , C07D417/12 , C07D417/14 , A61K31/433 , A61K31/4436
CPC分类号： C07D285/10 , C07D285/06 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).
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