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1.发明公开USE OF COX-2 INHIBITORS IN THE TREATMENT AND PREVENTION OF OCULAR COX-2 MEDIATED DISORDERS 审中-公开COX-2抑制剂在治疗和预防COX-2依赖的眼疾USE
公开(公告)号：EP1299123A2
公开(公告)日：2003-04-09
申请号：EP01931074.7
申请日：2001-05-04
发明人： BANDYOPADHYAY, Rebanta , EVELETH, David , VAN HAARLEM, Tom , KARARLI, Tugrul, T. , SINGH, Satish, K.
CPC分类号： A61K45/06 , A61K9/0048 , A61K31/12 , A61K31/353 , A61K31/38 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/465 , A61K31/47 , A61K31/50 , A61K31/74 , A61K2300/00
摘要： The present invention provides methods for the treatment and prevention of ocular COX-2 mediated disorders using COX-2 inhibitors.
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公开(公告)号：EP1165072A2
公开(公告)日：2002-01-02
申请号：EP00982254.5
申请日：2000-12-06
CPC分类号： C07D231/12 , A61K9/145 , A61K9/146 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/209 , A61K9/5026 , A61K9/5047 , A61K31/135 , A61K31/137 , A61K31/415 , A61K31/42 , A61K31/44 , A61K45/06 , C07D213/61 , C07D261/08 , C07D307/58 , C07D311/58 , A61K2300/00
摘要： Pharmaceutical compositions are provided comprising particulate valdecoxib in an amount of about 1 mg to about 100 mg and one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.
摘要翻译： 提供了包含约1mg至约100mg量的颗粒性伐地考昔和一种或多种药学上可接受的赋形剂的药物组合物。 该组合物可用于治疗或预防环氧合酶-2介导的病症和障碍。
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公开(公告)号：EP1355631B1
公开(公告)日：2007-10-03
申请号：EP01965984.6
申请日：2001-08-17
发明人： LE, Trang, T. , KARARLI, Tugrul, T. , KONTNY, Mark, J. , SASTRY, Srikonda, V. , NYSHADHAM, Janaki, R. , PAGLIERO, Arthur, J., Jr.
IPC分类号： A61K9/20 , A61K31/635
CPC分类号： A61K9/0056 , A61K9/2077 , A61K31/415 , A61K31/635
摘要： A process is provided for preparing an oral fast-melt composition of a selective cyclooxygenase-2 inhibitory drug, the process comprising (a) a step of wet granulating the drug together with a binding agent comprising a saccharide of high moldability, and (b) a step of blending with the drug a saccharide of low moldability, wherein the above steps (a) and (b) occur in any order or simulatenously to result in formation of granules. The process optionally incorporates means to inhibit agglomeration of the drug, for example addition of a wetting agent. Optionally the process further comprises (c) a step of blending the granules with at least one of a lubricant, a sweetening agent and a flavoring agent to form a tableting blend, and (d) a step of compressing the tableting blend to form oral fast-melt tablets. Also provided is a composition prepared by such a process.
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公开(公告)号：EP1355631A2
公开(公告)日：2003-10-29
申请号：EP01965984.6
申请日：2001-08-17
发明人： LE, Trang, T. , KARARLI, Tugrul, T. , KONTNY, Mark, J. , SASTRY, Srikonda, V. , NYSHADHAM, Janaki, R. , PAGLIERO, Arthur, J., Jr.
IPC分类号： A61K9/20 , A61K31/635
CPC分类号： A61K9/0056 , A61K9/2077 , A61K31/415 , A61K31/635
摘要： A process is provided for preparing an oral fast-melt composition of a selective cyclooxygenase-2 inhibitory drug, the process comprising (a) a step of wet granulating the drug together with a binding agent comprising a saccharide of high moldability, and (b) a step of blending with the drug a saccharide of low moldability, wherein the above steps (a) and (b) occur in any order or simulatenously to result in formation of granules. The process optionally incorporates means to inhibit agglomeration of the drug, for example addition of a wetting agent. Optionally the process further comprises (c) a step of blending the granules with at least one of a lubricant, a sweetening agent and a flavoring agent to form a tableting blend, and (d) a step of compressing the tableting blend to form oral fast-melt tablets. Also provided is a composition prepared by such a process.
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公开(公告)号：EP1150959A1
公开(公告)日：2001-11-07
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.
摘要翻译： 选择性环加氧酶-2抑制药塞来昔布以非晶形式提供。 还提供塞来考昔药物，其中塞来昔布以至少可检测量存在，作为无定形塞来昔布。 还提供了塞来昔布结晶抑制剂复合物，其包含与一种或多种结晶抑制剂例如聚合物紧密结合的本发明的无定形塞来昔布或塞来昔布药物物质的颗粒。 还提供了包含这种塞来昔布结晶抑制剂复合物和一种或多种赋形剂的药物组合物。 还提供了制备本发明的塞来昔布药物，本发明的塞来昔布结晶抑制剂复合物和本发明的药物组合物的无定形塞来昔布的制备方法。 还提供了一种治疗受试者的医疗状况或病症的方法，其中所述方法是用环氧合酶-2抑制剂进行治疗，包括以治疗有效量施用例如口服本发明组合物。
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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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公开(公告)号：EP1372645B1
公开(公告)日：2005-11-23
申请号：EP02725471.3
申请日：2002-04-02
发明人： KARARLI, Tugrul, T. , NEMA, Sandeep , KARIM, Aziz
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/19 , A61K31/00 , A61K31/122 , A61K31/365 , A61K31/415 , A61K31/42 , A61K31/444 , A61K31/50 , A61K47/02
摘要： A pharmaceutical composition comprises, in powder form, (a) at least one water-soluble therapeutic agent selected from selective COX-2 inhibitory drugs and prodrugs and salts thereof, for example parecoxib sodium, in a therapeutically effective total amount constituting about 30% to about 90% by weight, (b) a parenterally acceptable buffering agent in an amount of about 5% to about 60% by weight, and optionally (c) other parenterally acceptable excipient ingredients in a total amount not greater than about 10% by weight, of the composition. The composition is reconstitutable in a parenterally acceptable solvent liquid to form an injectable solution. A lyophilization process is provided for preparation of such a composition.
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8.发明授权
公开(公告)号：EP1175214B1
公开(公告)日：2004-11-24
申请号：EP00980850.2
申请日：2000-12-06
发明人： KARARLI, Tugrul, T. , KONTNY, Mark, J. , DESAI, Subhash , HAGEMAN, Michael, J. , HASKELL, Royal, J.
CPC分类号： A61K9/145 , A61K9/146 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/209 , A61K9/5084 , A61K9/5161 , A61K31/415 , A61K31/42 , A61K45/06 , C07D213/61 , C07D231/12 , C07D261/08 , C07D307/58 , C07D311/58 , A61K2300/00
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公开(公告)号：EP1372645A1
公开(公告)日：2004-01-02
申请号：EP02725471.3
申请日：2002-04-02
发明人： KARARLI, Tugrul, T. , NEMA, Sandeep , KARIM, Aziz
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/19 , A61K31/00 , A61K31/122 , A61K31/365 , A61K31/415 , A61K31/42 , A61K31/444 , A61K31/50 , A61K47/02
摘要： A pharmaceutical composition comprises, in powder form, (a) at least one water-soluble therapeutic agent selected from selective COX-2 inhibitory drugs and prodrugs and salts thereof, for example parecoxib sodium, in a therapeutically effective total amount constituting about 30% to about 90% by weight, (b) a parenterally acceptable buffering agent in an amount of about 5% to about 60% by weight, and optionally (c) other parenterally acceptable excipient ingredients in a total amount not greater than about 10% by weight, of the composition. The composition is reconstitutable in a parenterally acceptable solvent liquid to form an injectable solution. A lyophilization process is provided for preparation of such a composition.
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10.发明公开RAPIDLY DISINTEGRATING ORAL FORMULATION OF A CYCLOOXYGENASE-2 INHIBITOR 有权FAST DECAY END口服药物制备伐地考昔含
公开(公告)号：EP1309315A2
公开(公告)日：2003-05-14
申请号：EP01964122.4
申请日：2001-08-17
IPC分类号： A61K9/20 , A61K31/635 , A61K31/415
CPC分类号： A61K9/0056
摘要： A molded article such as a tablet is provided for administration to an oral cavity of a subject to treat or prevent a cyclooxygenase-2 mediated condition, disorder or disease. The molded article comprises a moldable blend of a therapeutically effective amount of a selective cyclooxygenase-2 inhibitory drug with a pharmaceutically acceptable excipient carrier system consisting predominantly of one or more carbohydrates, wherein ingredients and amounts thereof in the molded article and a process for preparing the molded article are selected such that the molded article exhibits rapid disintegration in the oral cavity, and wherein the moldable blend is prepared by a process step not requiring wet granulation.
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