ALDEHYDE-RELEASING COMPOUNDS
    1.
    发明申请
    ALDEHYDE-RELEASING COMPOUNDS 审中-公开
    甲醛释放化合物

    公开(公告)号:WO0228345A3

    公开(公告)日:2007-11-29

    申请号:PCT/AU0101254

    申请日:2001-10-05

    CPC classification number: A61K45/06 C07C69/003 C07C69/28 C07C69/36 C07C69/40

    Abstract: A method of treating cancer, comprising the step of administering to a subject in need thereof an effective amount of a compound or compounds which increase or supplement the intracellular levels of endogenous aldehyde, prior to, together with, or subsequent to the administration of a therapeutically-effective amount of a chemotherapeutic agent such as anthracyclines and anthracenediones, wherein the efficacy of the chemotherapeutic agent is enhanced relative to the efficacy of the chemotherapeutic agent alone. The compound may be an aldehyde-releasing compound (preferably formaldehyde), including known aldehyde-releasing compounds and two new classes of aldehyde-releasing compounds. One new class of aldehyde-releasing compounds of formula (II) release more than one equivalent of aldehyde Z-(L-M 1 -CHR-M 2 ) x (II) wherein x is an integer of 2 or more Z is a direct bond or a linking group of valency x; L is either a direct bond or a spacer group R is H or C1-4 alkyl, alkenyl or alkynyl; M 1 is a decomposable or hydrolysable group; and M 2 is a second decomposable or hydrolysable group. Another new class of aldehyde-releasing compounds include a radical based on an inhibitor of an aldehyde detoxifying agent, such as buthionine sulphoximine or crotonaldehyde.

    Abstract translation: 一种治疗癌症的方法,包括以下步骤:在有需要的受试者之前,在施用治疗性疾病之前,之后或之后施用有效量的增加或补充内源性醛的细胞内水平的化合物或化合物 - 化学治疗剂如蒽环类和蒽环类化合物的有效量,其中化疗剂的功效相对于单独的化学治疗剂的功效增强。 化合物可以是释放醛的化合物(优选甲醛),包括已知的释放醛的化合物和两种新类型的释放醛的化合物。 一类新的醛释放式(II)的化合物释放出多于一当量的醛Z-(LM 1 - )-CHR-M 2 O 2, (II)其中x是2或更大的整数Z是直接键或价数x的连接基团; L是直接键或间隔基R是H或C 1-4烷基,烯基或炔基; M 1是可分解的或可水解的基团; 和M 2是第二个可分解或可水解的基团。 另一种新的醛释放化合物包括基于醛解毒剂抑制剂的基团,例如丁硫氨酸亚磺酰亚胺或巴豆醛。

    INHIBITORS OF PHOSPHATIDYL MYO-INOSITOL CYCLE
    3.
    发明申请
    INHIBITORS OF PHOSPHATIDYL MYO-INOSITOL CYCLE 审中-公开
    PHOSPHATIDYL MYO-INOSITOL CYCLE的抑制剂

    公开(公告)号:WO00000206A1

    公开(公告)日:2000-01-06

    申请号:PCT/US1999/012824

    申请日:1999-06-25

    CPC classification number: C07C69/96 C07C69/013 C07F9/117 C07F9/4081

    Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-D-myo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor agents which effectively inhibit the growth of mammalian cells.

    Abstract translation: 本发明涉及3-脱氧-D-肌醇醚类脂质类似物作为磷脂酰肌醇-3-激酶信号传导和癌细胞生长抑制剂的制备和生物学活性。 本发明的化合物可用作有效抑制哺乳动物细胞生长的抗肿瘤剂。

    SACCHARIC ACID DERIVATIVES AS BUILDERS IN DETERGENTS OR CLEANING AGENTS
    4.
    发明申请
    SACCHARIC ACID DERIVATIVES AS BUILDERS IN DETERGENTS OR CLEANING AGENTS 审中-公开
    糖酸衍生物,如在洗涤或清洗剂,支架材料

    公开(公告)号:WO1996034845A1

    公开(公告)日:1996-11-07

    申请号:PCT/EP1996001679

    申请日:1996-04-22

    CPC classification number: C11D3/2086 C07C59/305 C11D3/221

    Abstract: The invention concerns novel saccharic acid derivatives of general formula (I): MO2C-CHOR1-CHOR2-CHOR3-(CHOR4)n-R5, in which M is a hydrogen atom or an alkali metal or alkaline earth metal atom, R1, R2, R3, R4 and R6, independently of one another, represent a hydrogen atom or a group of formula (II), in which M has the above meaning, n is 0 or 1, R5 is a hydrogen atom, a CH2OR6-, CHO- or COOM- group, the compound on average having to contain two succinyl groups. The derivatives can be used, alone or in combination with other builders, in detergents or cleaning agents, have good biodegradability and can be obtained by the addition of maleic acid anhydride to saccharic acids. These builders can replace (co)polymer carboxylates in detergents or cleaning agents. The invention further concerns a phosphate-free detergent containing the builders according to the invention.

    Abstract translation: 有权利通式(I)中,Mo2C的-CHOR1-CHOR2-CHOR3-(CHOR4)N-R 5,其中M是氢原子或碱金属或碱土金属原子,R1,R2,R3,R4和R6独立地的新糖酸衍生物 表示,其中M具有上述含义,且n为数值0或1个氢原子或一个基团的式(II)中,R5是氢原子,CH2OR6-,CHO或COOM基团,其中所述化合物为2,平均 必须包括琥珀酰基,其可单独使用或与在洗涤剂或清洁剂助洗剂的其它组合使用是可生物降解,并且可以通过添加马来酸酐与糖酸来获得。 这些助洗剂可以在洗涤剂或清洁剂代替(共)聚合的羧酸盐。 此外,无磷酸盐洗涤剂中描述,它包含了新颖的助洗剂。

    PROCESS FOR THE MANUFACTURE OF SEVOFLURANE
    10.
    发明申请
    PROCESS FOR THE MANUFACTURE OF SEVOFLURANE 审中-公开
    七氟醚制造工艺

    公开(公告)号:WO2011018466A1

    公开(公告)日:2011-02-17

    申请号:PCT/EP2010/061645

    申请日:2010-08-10

    Inventor: BRAUN, Max

    CPC classification number: C07C41/22 C07C67/31 C07C43/123 C07C69/708

    Abstract: A process for the manufacture of Sevoflurane CF 3 -CH(OCH 2 F)-CF 3 which comprises (a) manufacturing a substituted malonic acid derivative of formula (I) or (II): R 1 OOC-CH(OCH 2 X)-COOR 2 (I) or R 3 HNOC-CH (OCH 2 X)-CONHR 4 (II) wherein X is OH or a leaving group which can be substituted by nucleophilic substitution and R 1 , R 2 , R 3 , R 4 equal to or different from each other, are independently selected from H, an alkyl group having from 1 to 10 carbon atoms which is optionally substituted by at least one halogen atom,, an aralkyl group or an aryl group, (b) further reacting said malonic acid derivative as intermediate for the manufacture of Sevoflurane CF 3 -CH(OCH 2 F)-CF 3

    Abstract translation: 制备七氟醚CF 3 -CH(OCH 2 F)-CF 3的方法,其包括:(a)制备式(I)或(II)的取代的丙二酸衍生物:R1OOC-CH(OCH2X)-COOR2(I)或R3HNOC- CH(OCH 2 X)-CONHR 4(II)其中X是OH或可被亲核取代取代的离去基团,且R 1,R 2,R 3,R 4彼此相同或不同,独立地选自H, 任选被至少一个卤素原子取代的1至10个碳原子,芳烷基或芳基,(b)进一步使所述丙二酸衍生物作为制备七氟烷CF 3 -CH(OCH 2 F)-CF 3的中间体

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