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    • 1. 发明授权
    • Irinotecan preparation
    • 伊立替康制剂
    • US07846473B2
    • 2010-12-07
    • US11597435
    • 2005-05-31
    • Keisuke YoshinoShigenori NozawaMasashi IsozakiSeigo SawadaIkuo KatoTakeshi Matsuzaki
    • Keisuke YoshinoShigenori NozawaMasashi IsozakiSeigo SawadaIkuo KatoTakeshi Matsuzaki
    • A61K9/127
    • A61K9/1271A61K31/4745
    • Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.
    • 本发明提供了一种伊立替康制剂,其能够通过显着提高血液中的保留性,与常规已知的伊立替康脂质体制剂相比,可以高密度地在密闭囊泡载体中以高浓度和血液中长时间地支持伊立替康和/或其盐。 也就是说,包括由脂质膜形成的封闭囊泡的伊立替康制剂,其中伊立替康和/或其盐以至少0.07mol / mol(药物mol /膜总脂质摩尔)的浓度包封。 伊立替康制剂中的内部水相和外部水相之间存在离子梯度。 封闭的囊泡优选为脂质体,其中仅脂质体的外表面优选用含有亲水性聚合物的表面改性剂改性。
    • 3. 发明申请
    • Liposome Preparation Containing Slightly Water-Soluble Camptothecin
    • 含有轻微水溶性喜树碱的脂质体制备
    • US20080193509A1
    • 2008-08-14
    • US11629869
    • 2005-06-17
    • Keisuke YoshinoShigenori NozawaYoshitaka OgataYasuo KurosakiSeigo SawdaIkuo KatoTakeshi Matsuzaki
    • Keisuke YoshinoShigenori NozawaYoshitaka OgataYasuo KurosakiSeigo SawdaIkuo KatoTakeshi Matsuzaki
    • A61K9/127A61K31/4375
    • A61K9/1272A61K31/4745
    • The present invention aims at providing a slightly water-soluble camptothecin liposome preparation with an excellent retention in blood for a drug, which can stably hold a slightly water-soluble camptothecin compound for a long period of time, whereby hydrolysis of an α-hydroxylactone ring in blood is suppressed and the slightly water-soluble camptothecin compound is kept in a structure in which the ring is not opened and which makes the compound effective as an antitumor-active drug, and, moreover, the liability of the drug to leave a liposome is advantageously reduced, so that it is possible to maintain the drug concentration in plasma for a long period of time after administration. This object is achieved by the liposome preparation as described in the specification. The liposome preparation according to the present invention includes a liposome preparation including as lipid components for forming a membrane a phospholipid and a fatty acid, and containing as a drug a lightly water-soluble camptothecin compound.
    • 本发明的目的在于提供一种在血液中具有优异的药物保留性的轻微水溶性喜树碱脂质体制剂,其能够长时间稳定地保持轻微的水溶性喜树碱化合物,从而水解α-羟基内酯环 在血液中被抑制,轻微的水溶性喜树碱化合物保持在不打开环的结构中,并且使得化合物作为抗肿瘤活性药物有效,此外,药物离开脂质体的责任 有利地减少,使得可以在施用后长时间维持血浆中的药物浓度。 该目的通过如说明书中所述的脂质体制备来实现。 根据本发明的脂质体制剂包括脂质体制剂,其包含作为形成磷脂和脂肪酸的膜的脂质成分,并且作为药物含有轻度水溶性的喜树碱化合物。
    • 4. 发明授权
    • Phenanthroindolizidine compound and NFκB inhibitor containing same as active ingredient
    • 菲并吲哚哩啶化合物和含有与活性成分相同的NF&kgr B抑制剂
    • US09174979B2
    • 2015-11-03
    • US13125698
    • 2009-10-23
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • C07D471/04A61K31/437A61P29/00A61P35/00C07D491/147
    • C07D471/04C07D491/147
    • A novel compound having an excellent NFκB inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof:wherein, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group, or a halogen atom;R2 represents a hydroxyl group, or a lower alkyloxy group;R3 represents a hydrogen atom, a lower alkyl group, or a halogen atom;R4 represents a hydrogen atom or a lower alkyloxy group;R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6;R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5;R7 represents a hydrogen atom or a lower alkyl group; andR8 represents a hydrogen atom, a hydroxyl group, an amino group, or a lower alkylcarbonyloxy group (excluding the case where R1, R3, R4 and R7 are hydrogen atoms, R2 and R8 are hydroxyl groups, and R5 and R6 are methoxy groups).
    • 提供了具有优异的NF&Kgr B抑制效果的新化合物,具体公开了下式(1)表示的化合物或其盐:其中,R1表示氢原子,低级烷基,低级烷氧基, 或卤素原子; R2表示羟基或低级烷氧基; R3表示氢原子,低级烷基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子,低级烷氧基,卤素原子,羟基或亚甲二氧基; R6表示与R5一起形成的氢原子,低级烷氧基或亚甲二氧基,或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; 并且R 8表示氢原子,羟基,氨基或低级烷基羰基氧基(R 1,R 3,R 4和R 7为氢原子的情况除外,R 2和R 8为羟基,R 5和R 6为甲氧基 )。
    • 5. 发明授权
    • Phenanthroindolizidine derivative and NFκB inhibitor containing same as active ingredient
    • 菲咯啉二氮茚衍生物和含有与活性成分相同的NFkappaB抑制剂
    • US08569327B2
    • 2013-10-29
    • US13124554
    • 2009-10-23
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • A61K31/403C07D221/18
    • C07D471/04
    • A novel compound having an excellent NFκB inhibitory effect is provided. Specifically disclosed is a compound represented by the following formula (1) or a salt thereof: wherein, R1 represents a hydrogen atom, a lower alkyl group, or the like; R2 represents a hydrogen atom, a lower alkyl group, a halogen atom, or the like; R3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group, or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6; R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxyl group, an amino group, a lower alkylcarbonyloxy group, or a halogen atom.
    • 提供了具有优异NFκB抑制作用的新型化合物。 具体公开的是由下式(1)表示的化合物或其盐:其中,R1表示氢原子,低级烷基等; R2表示氢原子,低级烷基,卤素原子等; R3表示氢原子,低级烷基,羟基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子,低级烷氧基,卤素原子,羟基或亚甲二氧基; R6表示与R5一起形成的氢原子,低级烷氧基或亚甲二氧基,或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; R8表示氢原子,羟基,氨基,低级烷基羰基氧基或卤素原子。
    • 6. 发明申请
    • PHENANTHROINDOLIZIDINE COMPOUND AND NFkB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT
    • 苯并噻唑类化合物和含有其作为活性成分的NFkB抑制剂
    • US20110201638A1
    • 2011-08-18
    • US13125698
    • 2009-10-23
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • Takashi IkedaSeigo SawadaTakashi YaegashiTakeshi MatsuzakiShusuke HashimotoRyuta Yamazaki
    • A61K31/437C07D471/04A61P29/00A61P35/00
    • C07D471/04C07D491/147
    • A novel compound having an excellent NFκB inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof:wherein, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group, or a halogen atom; R2 represents a hydroxyl group, or a lower alkyloxy group; R3 represents a hydrogen atom, a lower alkyl group, or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6; R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxyl group, an amino group, or a lower alkylcarbonyloxy group (excluding the case where R1, R3, R4 and R7 are hydrogen atoms, R2 and R8 are hydroxyl groups, and R5 and R6 are methoxy groups).
    • 提供了具有优异的NF&Kgr B抑制效果的新化合物,具体公开了下式(1)表示的化合物或其盐:其中,R1表示氢原子,低级烷基,低级烷氧基, 或卤素原子; R2表示羟基或低级烷氧基; R3表示氢原子,低级烷基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子,低级烷氧基,卤素原子,羟基或亚甲二氧基; R6表示与R5一起形成的氢原子,低级烷氧基或亚甲二氧基,或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; 并且R 8表示氢原子,羟基,氨基或低级烷基羰基氧基(R 1,R 3,R 4和R 7为氢原子的情况除外,R 2和R 8为羟基,R 5和R 6为甲氧基 )。