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    • 11. 发明申请
    • PHARMACEUTICAL COMPOSITIONS AND METHODS FOR MAKING AND USING THEM
    • 药物组合物及其制备和使用方法
    • WO2012099962A2
    • 2012-07-26
    • PCT/US2012021724
    • 2012-01-18
    • VICUS THERAPEUTICS LLCMAKI JOHNBASCOMB NEWELLTURNER TIMOTHY J
    • MAKI JOHNBASCOMB NEWELLTURNER TIMOTHY J
    • A61K31/455A61K9/06A61K9/12A61K9/70A61K31/133A61K31/20
    • A61K31/7068A61K9/0014A61K9/06A61K31/133A61K31/20A61K31/337A61K31/404A61K31/44A61K31/4439A61K31/455A61K31/4985A61K31/506A61K31/517
    • In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising combinations of beneficial ingredients that in alternative embodiments are serviceable as therapies or palliatives for treating, preventing or improving conditions, states and disease symptoms involving the use of targeted protein kinase inhibitors such as Multi-Kinase Inhibitors (MKIs) or Epidermal Growth Factor Receptor (EGFR) Inhibitors (EGFRIs), or the use of other oral oncolytics, such as capcitabine or erlotinib, known to be associated with drug-induced dermatological toxicity, e.g., in the amelioration or treatment of a cancer, a dermatitis, a rosacea, an eczema, an ichthyosis, or a related condition; and methods for making and using these compositions; and methods for making and using these compositions.
    • 在替代实施方式中,本发明提供了组合物,例如药物组合物和制剂,制剂,试剂盒和其他制造产品,例如包装在一起或分开包装在泡罩包装,有盖泡罩或泡罩卡中或包装在纸,塑料或 玻璃纸包装物(例如收缩包装物),其包含有利成分的组合,其在可选的实施方案中可用作治疗或预防或改善涉及使用靶向蛋白激酶抑制剂的病症,状态和疾病症状的疗法或缓和剂,例如多激酶 抑制剂(MKIs)或表皮生长因子受体(EGFR)抑制剂(EGFRIs),或已知与药物诱导的皮肤病学毒性有关的其他口服溶瘤剂如capcitabine或厄洛替尼的用途,例如改善或治疗 癌症,皮炎,红斑痤疮,湿疹,鱼鳞病或相关病症; 以及制造和使用这些组合物的方法; 以及制备和使用这些组合物的方法。
    • 15. 发明申请
    • 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS
    • 2-氨基吡啶衍生物作为GLUCOKINASE激活剂
    • WO2008091770A1
    • 2008-07-31
    • PCT/US2008/051194
    • 2008-01-16
    • ARRAY BIOPHARMA INC.AICHER, Thomas DanielBOYD, Steven ArmenCHICARELLI, Mark JosephCONDROSKI, Kevin RonaldGARREY, Rustam FerdinandHINKLIN, Ronald JaySINGH, AjayTURNER, Timothy M.
    • AICHER, Thomas DanielBOYD, Steven ArmenCHICARELLI, Mark JosephCONDROSKI, Kevin RonaldGARREY, Rustam FerdinandHINKLIN, Ronald JaySINGH, AjayTURNER, Timothy M.
    • C07D417/14C07D495/04A61K31/4439
    • C07D495/04C07D417/14
    • Provided are compounds having the Formula (I) or salts thereof, wherein: L is O, S, SO, SO 2 , CHOH, C(O), or CH 2 ; D 2 is CR 12 or N; R 2 is aryl, heteroaryl, saturated or partially unsaturated cycloalkyl, or saturated or partially unsaturated heterocyclyl (optionally substituted with oxo), wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl are monocyclic or bicyclic and are further optionally substituted with one or more groups independently selected from C 1 -C 6 alkyl, F, Cl, Br, I, CF 3 , CN, OR 6 , C(=O)R 6 , C(=O)OR 6 , O(CH 2 ) n C(=O)OR 6 , C(=O)NR 6 R 7 , NO 2 and (1-6C alkyl)OR 6 ; R 3 is H, Br, OR 6 , SR 6 , C(O)OR 6 , C(O)NR 6 R 7 , C(O)R 6 , heteroaryl, or C 1 -C 6 alkyl substituted with one or more groups independently selected from V n -aryl, V n -OR 6 , V n - C(=O)OR 6 and V n -NR 6 R 7 ; R 11 is H or Cl; and R 13 is N-(1 -6C alkanoyl)piperidin-4-yl; that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
    • 提供具有式(I)或其盐的化合物,其中:L是O,S,SO,SO 2,CHOH,C(O)或CH 2 ; D 是CR 12或N; R 2是芳基,杂芳基,饱和或部分不饱和的环烷基或饱和或部分不饱和的杂环基(任选被氧代取代),其中所述芳基,杂芳基,环烷基和杂环基是单环或双环的, 被一个或多个独立地选自C 1 -C 6烷基,F,Cl,Br,I,CF 3 N,CN, C(= O)R 6,C(= O)OR 6,O(CH 2)2, C(= O)OR 6,C(= O)NR 6 R 7,NO 2和(1-6C烷基)OR 6; R 3是H,Br,OR 6,SR 6,C(O)OR 6,C(O) O)NR 6 R 7,C(O)R 6,杂芳基或C 1 -C 6烷基, 被一个或多个独立地选自以下的基团取代的亚烷基烷基:V n - 芳基,V n -OR 6,V C(= O)OR 6和V 6和-NR 6 R 7, SUP>; R 11是H或Cl; 和R 13是N-(1-6C烷酰基)哌啶-4-基; 其可用于治疗和/或预防由缺乏水平的葡糖激酶活性(例如糖尿病)介导的疾病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法,或者可以通过激活葡糖激酶治疗。
    • 16. 发明申请
    • CAN END
    • WO2005113351A1
    • 2005-12-01
    • PCT/US2005/016546
    • 2005-05-12
    • REXAM BEVERAGE CAN COMPANYTURNER, TimothyFORREST, Randall, G.GOPALASWAMY, Rajesh
    • TURNER, TimothyFORREST, Randall, G.GOPALASWAMY, Rajesh
    • B65D8/18
    • B65D17/08B65D17/06B65D17/4012B65D17/502B65D2517/0007B65D2517/0011B65D2517/0061B65D2517/0076B65D2517/0079B65D2517/0082Y10S220/906
    • A can end member (10) has a center panel (18), a circumferential chuck wall, and a transition wall. The center panel is centered about a longitudinal axis (50) and has a peripheral edge. The center panel also has a step portion located radially outwardly from the longitudinal axis. The step portion has an annular convex portion joined to an annular concave portion and displaces at least a portion of the center panel vertically in a direction parallel to the longitudinal axis. The curl defines an outer perimeter of the end member. The circumferential chuck wall extends downwardly from the curl to the transition wall. The transition wall connects the chuck wall with the peripheral edge of the center panel. The transition wall comprises a folded portion. The folded portion has a first leg (56), a second leg (62), and a third leg (68). The first leg is directly connected to the chuck wall and joined to the second leg by a concave annular portion. The second leg is joined to the third leg by a convex annular portion, and the third leg is joined to the center panel. The convex annular portion has a radius of curvature greater than 0.002 ins.
    • 罐端构件(10)具有中心面板(18),周向卡盘壁和过渡壁。 中心面板围绕纵向轴线(50)居中并且具有周边边缘。 中心面板还具有从纵向轴线径向向外定位的台阶部分。 台阶部分具有连接到环形凹部的环形凸部,并且在平行于纵向轴线的方向上垂直移动中心面板的至少一部分。 卷曲限定了端部构件的外周。 圆周卡盘壁从卷曲向下延伸到过渡壁。 过渡壁将卡盘壁与中心面板的周边边缘连接。 过渡壁包括折叠部分。 折叠部分具有第一腿部(56),第二腿部(62)和第三腿部(68)。 第一腿直接连接到卡盘壁上并通过凹入的环形部分连接到第二腿。 第二腿部通过凸状的环状部分与第三腿部接合,第三腿部与中心面板接合。 凸形环形部分具有大于0.002英寸的曲率半径。