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1.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：EP2125749A2
公开(公告)日：2009-12-02
申请号：EP08714238.6
申请日：2008-02-11
发明人： DE LERA RUIZ, Manuel , MCCORMICK, Kevin, D. , BOYCE, Christopher, W. , ASLANIAN, Robert, G. , YU, Younong , MANGIARACINA, Pietro , ZHENG, Junying , BERLIN, Michael, Y. , CIESLA, Stephanie, L. , HUANG, Chia-yu , LIANG, Bo
IPC分类号： C07D233/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , A61K31/4035 , A61P31/10 , A61P29/00 , A61P9/00 , A61P25/22
CPC分类号： C07D403/14 , C07D233/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
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3.发明公开PHENOXYPIPERIDINES AND ANALOGS THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS 审中-公开Phenoxypiperidines及其类似物AS组胺H3拮抗剂
公开(公告)号：EP1976848A2
公开(公告)日：2008-10-08
申请号：EP06839411.3
申请日：2006-12-19
申请人： Schering Corporation
发明人： MUTAHI, Mwangi, W. , ASLANIAN, Robert, G. , BERLIN, Michael, Y. , BOYCE, Christopher, W. , DE LERA RUIZ, Manuel , MCCORMICK, Kevin, D. , SOLOMON, Daniel, M. , VACCARO, Henry, A. , ZHENG, Junying , PURAKKATTLE, Biju, J. , YU, Younong , ZHOU, Wei , ZHU, Xiaohong
IPC分类号： C07D401/10 , C07D203/12 , C07D403/14 , C07D471/04 , A61K31/4545 , A61P11/00
CPC分类号： C07D471/04 , C07D213/38 , C07D213/73 , C07D277/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D473/00
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, -C(O)-, -C(N-OR5)-, -C(N-OR5)-CH(R6)-, -CH(R6)-C(N-OR5)-, -O-, -OCH2-, -CH2O- or -S(O)0-2-; Y is -O-, -(CH2)2-, -C(=O)-, -C(=NOR7)- or -SO0-2-; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
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4.发明公开
公开(公告)号：EP1965862A2
公开(公告)日：2008-09-10
申请号：EP06847740.5
申请日：2006-12-18
申请人： Schering Corporation
发明人： VAN HEEK, Margaret , HWA, Joyce, J. , GRAZIANO, Michael, P. , LACHOWICZ, Jean, E. , KOWALSKI, Timothy, J. , VELTRI, Enrico, P. , MCCORMICK, Kevin, D. , BERLIN, Michael, Y. , ASLANIAN, Robert, G.
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61K31/4745 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising therapeutic combinations comprising: one or more H3 antagonists/inverse agonists; one or more appetite suppressants selected from the group consisting of CBi antagonists/inverse agonists, sibutramine, phentermine and topiramate; and option one or more HMG-CoA reductase inhibitors. The invention also relates to medicaments and kits comprising the pharmaceutical compositions of the present invention, and methods of treating obesity, obesity related disorders and diabetes using the pharmaceutical compositions of the present invention.
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公开(公告)号：EP1902046A1
公开(公告)日：2008-03-26
申请号：EP06773528.2
申请日：2006-06-19
申请人： Schering Corporation
发明人： ASLANIAN, Robert, G. , BERLIN, Michael, Y. , BOYCE, Christopher, W. , CHAO, Jianhua , DE LERA RUIZ, Manuel , MANGIARACINA, Pietro , MCCORMICK, Kevin, D. , MUTAHI, Mwangi, W. , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , SOLOMON, Daniel, M. , TOM, Wing, C. , VACCARO, Henry, A. , ZHENG, Junying , ZHU, Xiaohong
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61P3/04 , A61P29/00 , A61P37/00 , C07D409/14 , C07D471/04
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- or -SO1-2-; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, -C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
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6.发明授权(1-4-PIPERIDINYL)BENZIMIDAZOLE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 有权1-（4-哌啶基）苯并咪唑AS组胺H3拮抗剂
公开(公告)号：EP1499316B1
公开(公告)日：2008-03-19
申请号：EP03719766.2
申请日：2003-04-16
申请人： Schering Corporation
发明人： ZENG, Qingbei , ASLANIAN, Robert, G. , BERLIN, Michael, Y. , BOYCE, Christopher, W. , CAO, Jianhua , KOZLOWSKI, Joseph, A. , MANGIARACINA, Pietro , MC CORMICK, Kevin, D. , MUTAHI, Mwangi, W. , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , SOLOMON, Daniel, M. , TOM, Wing, C.
IPC分类号： A61K31/4545 , C07D471/04 , C07D401/14 , A61K31/4184 , A61P37/08
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substitutd aryl or heteroaryl; M1 and M2 are C(R3) or N; Q is -N(R8)-, -S- or -O-; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I. Also disclosed are methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.
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7.发明公开
公开(公告)号：EP2350067A2
公开(公告)日：2011-08-03
申请号：EP09740590.6
申请日：2009-10-14
申请人： Schering Corporation
发明人： PALANI, Anandan , BERLIN, Michael, Y. , ASLANIAN, Robert, G. , VACCARO, Henry, M. , CHAN, Tin-Yau , XIAO, Dong , DEGRADO, Sylvia , RAO, Ashwin, U. , CHEN, Xiao , LEE, Yoon, Joo , SOFOLARIDES, Michael, J. , SHAO, Ning , HUANG, Ying, R. , LIU, Zhidan , WANG, Li Yuan , PU, Haiyan
IPC分类号： C07D417/04 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D285/135 , C07D271/113 , C07D491/107 , A61K31/4355 , A61K31/437 , A61K31/4439 , A61K31/444 , A61P3/10
CPC分类号： C07D285/135 , C07D271/113 , C07D417/04 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/107
摘要： The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
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公开(公告)号：EP2350048A2
公开(公告)日：2011-08-03
申请号：EP09744830.2
申请日：2009-10-14
申请人： Schering Corporation
发明人： PALANI, Anandan , XIAO, Dong , ASLANIAN, Robert, G. , BERLIN, Michael, Y. , RAO, Ashwin, U. , CHEN, Xiao , LEE, Yoon, Joo , DEGRADO, Sylvia , SHAO, Ning , HUANG, Ying, R. , LIU, Zhidan
IPC分类号： C07D401/12 , A61K31/4427 , A61P7/12
CPC分类号： C07D401/06 , C07D213/643 , C07D213/81 , C07D401/12 , C07D417/04
摘要： The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
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公开(公告)号：EP1902046B1
公开(公告)日：2009-12-02
申请号：EP06773528.2
申请日：2006-06-19
申请人： Schering Corporation
发明人： ASLANIAN, Robert, G. , BERLIN, Michael, Y. , BOYCE, Christopher, W. , CHAO, Jianhua , DE LERA RUIZ, Manuel , MANGIARACINA, Pietro , MCCORMICK, Kevin, D. , MUTAHI, Mwangi, W. , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , SOLOMON, Daniel, M. , TOM, Wing, C. , VACCARO, Henry, A. , ZHENG, Junying , ZHU, Xiaohong
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61P3/04 , A61P29/00 , A61P37/00 , C07D409/14 , C07D471/04
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- or -SO1-2-; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, -C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
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公开(公告)号：EP1326858A2
公开(公告)日：2003-07-16
申请号：EP01983968.7
申请日：2001-10-15
申请人： Schering Corporation
发明人： ASLANIAN, Robert, G. , SHIH, Neng-Yang , TING, Pauline, C. , BERLIN, Michael, Y. , ROSENBLUM, Stuart, B. , MC CORMICK, Kevin, D. , TOM, Wing, C. , BOYCE, Christopher, W. , MANGIARACINA, Pietro , MUTAHI, Mwangi, Wa , PIWINSKI, John, J.
IPC分类号： C07D401/14 , C07D413/14 , C07D401/12 , C07D409/14 , C07D498/04 , C07D417/14
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula: (I) Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I) in combination with a H1 receptor antagonist.
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