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61.发明公开USE OF N-SUBSTITUTED-1,5-DIDEOXY-1,5-IMINO-D-GLUCITOL COMPOUNDS FOR TREATING HEPATITIS VIRUS INFECTIONS 审中-公开N-取代-1,5-二脱氧-1,5-亚氨基-D- GLUCITOLVERBINDUNGEN的肝炎病毒感染的治疗中使用
公开(公告)号：EP1261339A1
公开(公告)日：2002-12-04
申请号：EP01909153.7
申请日：2001-02-13
IPC分类号： A61K31/445 , A61P31/14
CPC分类号： A61K31/445 , A61K45/06 , A61K2300/00
摘要： Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds alone or in combination with nucleoside antiviral agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immuno stimulating agents.
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公开(公告)号：EP1239856A1
公开(公告)日：2002-09-18
申请号：EP00990268.5
申请日：2000-12-20
IPC分类号： A61K31/415 , A61K9/20 , A61P19/02 , A61K31/42
CPC分类号： A61K45/06 , A61K9/1623 , A61K9/1635 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/209 , A61K9/5026 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/135 , A61K31/137 , A61K31/341 , A61K31/415 , A61K31/42 , A61K31/44
摘要： There is provided an orally deliverable pharmaceutical composition comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility such as celecoxib and a release-extending polymer. The composition is useful in treatment of cyclooxygenase-2 mediated conditions and disorders by once-a-day administration.
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63.发明公开TREATMENT OF CYCLOOXYGENASE-2 MEDIATED DISORDERS USING CONJUGATED FATTY ACID COMPOUNDS 审中-公开治疗中使用CONJUGIERTEN脂肪化合物环氧合酶-2相关的病症
公开(公告)号：EP1231913A2
公开(公告)日：2002-08-21
申请号：EP00951029.8
申请日：2000-06-07
发明人： ABBAS, Zaheer , KOBOLDT, Carol
IPC分类号： A61K31/201 , A61P3/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P25/28 , A61P27/00 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00
CPC分类号： A61K31/661 , A61K31/201 , A61K31/205 , A61K31/231 , A61K31/28 , A61K31/295 , A61K31/30 , A61K31/315 , A61K38/44 , A61K45/06 , C12Y113/11 , A61K2300/00
摘要： This invention is directed to a process for the prevention or treatment of inflammation or other cyclooxygenase-2 mediated disorders. This process comprises administering a conjugated fatty acid to an organism in an amount effective to prevent or treat the cyclooxygenase-2 mediated disorder by inhibiting cyclooxygenase -2. In one embodiment, the process comprises administering a fatty acid compound having formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, hydrocarbyl, or substituted hydrocarbyl; m is from 6 to 11; and the sum of n and m is from 13 to 16. In another embodiment, the process comprises administering a fatty acid compound having formula (VI) or a pharmaceutically acceptable salt thereof, wherein R6 is hydrogen, hydrocarbyl, or substituted hydrocarbyl; R7 is -OH, -SO¿3?H, -SH, -NH2, -PO3H2, or halogen; v is from 7 to 11; and the sum of v and w is from 11 to 15. This invention is also directed to a process for preparing a fatty acid compound. The process comprises combining a ylide with an aldehyde.
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64.发明授权CRYSTALLINE SOLID FORM OF (2S-5Z)-2-AMINO-7-(ETHANIMIDOYLAMINO)-2-METHYLHEPT-5-ENOIC ACID 有权作者（2S-5Z）-2-氨基-7-（ETHANIMIDOYLAMINO）-2-甲基庚-5-烯羧酸结晶固体形式
公开(公告)号：EP1534668B1
公开(公告)日：2012-05-02
申请号：EP03793292.8
申请日：2003-08-22
发明人： HALLINAN, Ann, E.
IPC分类号： C07C257/14 , A61K31/155 , A61P29/00
CPC分类号： C07C257/14
摘要： (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as 'S'. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.
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65.发明授权S-[2-[(1-IMINOETHYL)AMINO]ETHYL]-2-METHYL-L-CYSTEINE MALEATE HYDROCHLORIDE CRYSTALLINE SALT 有权S- [2 - [（I-IMINOETHYL）氨基]乙基] -2-甲基-L-胞嘧啶 - 马来酸 - 羟基氯化钠晶体沉淀
公开(公告)号：EP1603872B1
公开(公告)日：2011-05-18
申请号：EP04717188.9
申请日：2004-03-04
IPC分类号： C07C323/59 , A61K31/198 , A61P29/00 , C07C319/28
CPC分类号： C07C323/59 , C07B2200/07 , C07B2200/13 , C07C319/28
摘要： A novel mixed salt of S-[2-[(1-Iminoethyl)amino]ethyl] -2-methyl-L-cysteine is disclosed. The novel mixed salt, S-[2-[(1 Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, may be produced to form crystals that may be arranged as generally orderly packed agglomerates, which are particularly useful in making pharmaceutical compositions. Such pharmaceutical compositions are also described, as well as methods to make crystalline S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine maleate hydrochloride, and methods of treating conditions characterized by an overexpression on nitric oxide from the inducible isoform of nitric oxide synthase using the S-[2-[(1Iminoethyl)amino]ethyl] -2-methyl-L-cysteine maleate hydrochloride.
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公开(公告)号：EP1490064B1
公开(公告)日：2009-11-18
申请号：EP03713478.0
申请日：2003-02-14
发明人： DEVADAS, Balekudru , WALKER, John , SELNESS, Shaun, R. , BOEHM, Terri, L. , DURLEY, Richard, C. , DEVRAJ, Rajesh , HICKORY, Brian, S. , RUCKER, Paul, V. , JEROME, Kevin, D. , MADSEN, Heather, M. , ALVIRA, Edgardo , PROMO, Michele, A. , BLEVIS-BAL, Radhika, M. , MARRUFO, Laura, D. , HITCHCOCK, Jeff , OWEN, Thomas , NAING, Win , XING, Li , SHIEH, Huey, S. , LIU, Shuang , SCOTT, Ian, L. , SAMBANDAM, Aruna , MCGEE, Kevin F.
IPC分类号： A61K31/4412 , A61P29/00 , C07D213/69 , C07D401/06 , C07D409/06 , C07D213/70 , C07D213/64 , C07D213/74 , C07D405/06 , C07D213/84 , C07D401/10 , C07D405/12 , C07D401/12 , C07D213/75 , C07D401/14 , C07D213/79 , C07D401/04 , C07D405/04 , C07D413/10 , C07D215/22 , C07D405/14
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
摘要： Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
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公开(公告)号：EP1150959B1
公开(公告)日：2008-02-27
申请号：EP00982255.2
申请日：2000-12-06
发明人： HAGEMAN, Michael, J. , HE, Xiaorong , KARARLI, Tugrul, T. , MACKIN, Lesley, A. , MIYAKE, Patricia, J. , ROHRS, Brian, R. , STEFANSKI, Kevin, J.
IPC分类号： C07D231/12 , A61K31/415 , A61P29/00
CPC分类号： C07D231/12 , A61K9/0007 , A61K9/14 , A61K9/145 , A61K9/146 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/209 , A61K9/5084 , A61K9/5161 , A61K31/415 , A61K31/635 , A61K47/34 , C07D213/61 , C07D261/08 , C07D307/58 , C07D311/58
摘要： The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.
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68.发明授权
公开(公告)号：EP1427706B1
公开(公告)日：2007-05-30
申请号：EP02763656.2
申请日：2002-09-19
发明人： METZ, Suzanne , CLARE, Michael , CRICH, Joyce, Z. , HAGEN, Timothy, J. , HANSON, Gunnar, J. , HUANG, He , HOUDEK, Stephen, J. , STEALEY, Michael, A. , VAZQUEZ, Michael, L. , WEIER, Richard, M. , XU, Xiangdong
IPC分类号： C07D231/56 , C07D491/04 , C07D495/04 , C07D495/12 , C07D471/04 , A61K31/415 , A61K31/435
CPC分类号： C07D231/56 , C07D471/04 , C07D491/04 , C07D495/04 , C07D495/14
摘要： The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
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69.发明公开
公开(公告)号：EP1753731A2
公开(公告)日：2007-02-21
申请号：EP04724083.3
申请日：2004-03-29
发明人： DURLEY, Richard , DEVADAS, Balekudru , MADSEN, Heather , HICKORY, Brian , PALMQUIST, Katherine , SELNESS, Shaun
IPC分类号： C07D239/52 , C07D239/46 , A61K31/513 , C07D401/06 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/12
CPC分类号： C07D239/47 , C07D239/52 , C07D401/06 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/12
摘要： Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
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70.发明公开
公开(公告)号：EP1715887A1
公开(公告)日：2006-11-02
申请号：EP05702331.9
申请日：2005-01-24
IPC分类号： A61K38/27
摘要： The present invention provides a chemically modified human Growth Hormone (hGH) prepared by attaching a polyethylene glycol butyraldehyde moiety to the N-terminal phenylalanine of the protein. The chemically modified protein according to the present invention may have a much longer lasting hGH activity than that of the un-modified hGH, enabling reduced dose and scheduling opportunities. The present invention also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial.
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