公开(公告)号：US06872725B2

公开(公告)日：2005-03-29

申请号：US10254697

申请日：2002-09-25

申请人： Kimberley C. Allen ,  Jerry D. Clark ,  Thomas P. Fraher ,  Jason A. Hanko ,  Kimberly L. Kolbert ,  Clay R. Little ,  Michael K. Mao ,  Patricia S. Miyake ,  Jodi L. Moe ,  Partha S. Mudipalli ,  Tobin C. Schilke ,  Christine B. Seymour ,  Ahmad Y. Sheikh ,  Gopichand Yalamanchili

发明人： Kimberley C. Allen ,  Jerry D. Clark ,  Thomas P. Fraher ,  Jason A. Hanko ,  Kimberly L. Kolbert ,  Clay R. Little ,  Michael K. Mao ,  Patricia S. Miyake ,  Jodi L. Moe ,  Partha S. Mudipalli ,  Tobin C. Schilke ,  Christine B. Seymour ,  Ahmad Y. Sheikh ,  Gopichand Yalamanchili

IPC分类号： A61K31/506 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  A31K31/506

CPC分类号： C07D401/14

摘要： Crystalline forms of the p38 kinase inhibitor N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole are provided. These crystalline forms include (a) a first anhydrous crystalline form possessing improved physical stability relative to other solid-state forms of the compound; (b) a second anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; (c) a third anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; and (d) solvated crystalline forms, hydrated crystalline forms, and crystalline salt forms of the compound that are useful, for example, as intermediate solid-state forms in the preparation of other crystalline forms of the compound. Also provided are combinations and pharmaceutical compositions comprising at least one of these crystalline forms, processes for preparing these crystalline forms and for preparing compositions comprising these crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of at least one of these crystalline forms.

摘要翻译： 提供p38激酶抑制剂N-（2-羟基乙酰基）-5-（4-哌啶基）-4-（4-嘧啶基）-3-（4-氯苯基）吡唑的结晶形式。 这些结晶形式包括（a）相对于化合物的其它固体形式具有改善的物理稳定性的第一无水结晶形式; （b）相对于化合物的其它固态形式具有独特性质的第二无水结晶形式; （c）相对于化合物的其它固体形式具有独特性质的第三无水结晶形式; 和（d）化合物的溶剂化结晶形式，水合结晶形式和结晶盐形式，其可用于制备化合物的其它结晶形式的例如中间体固体形式。 还提供了包含这些结晶形式中的至少一种，这些结晶形式的制备方法和用于制备包含这些结晶形式的组合物的组合和药物组合物，以及预防和/或治疗p38激酶介导的病症的方法， 受试者治疗有效量的这些结晶形式中的至少一种。

公开(公告)号：US07476744B2

公开(公告)日：2009-01-13

申请号：US09728040

申请日：2000-12-01

申请人： Leonard J. Ferro ,  Patricia S. Miyake

发明人： Leonard J. Ferro ,  Patricia S. Miyake

IPC分类号： C07D231/00

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

摘要： Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a therapeutically effective amount, wherein the compound is present in the form of solid particles, about 25% to 100% by weight of which are smaller than 1 micrometer. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders and have particular advantages where rapid onset of therapeutic effect is desired. The novel Form I and Form II crystalline forms of celecoxib are described. The crystalline forms have unique chemical and physical properties relative to other solid state forms of celecoxib and are characterized by their powder x-ray diffraction (PXRD) patterns, differential scanning calorimetric (DSC) thermograms, and other physical characterizations.

摘要翻译： 提供药物组合物，其包含一种或多种口服递送剂量单位，每一剂量单位包含治疗有效量的低水溶性选择性环加氧酶-2抑制化合物，其中该化合物以固体颗粒形式存在，约25％至100％ 其重量小于1微米。 该组合物可用于治疗或预防环氧合酶-2介导的病症和病症，并且在需要快速起效治疗效果方面具有特别的优点。 描述了塞来昔布的新型I型和II型结晶形式。 结晶形式相对于塞来昔布的其他固态形式具有独特的化学和物理性质，其特征在于它们的粉末x射线衍射（PXRD）图谱，差示扫描量热（DSC）热分析图和其它物理表征。