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。
Abstract:
The present disclosure provides a process for the preparation of compounds of formula (III), compounds of formula (V), and corresponding salts of formula (IV). The compounds made by the methods and processes of the invention are particularly useful for administration in humans and animals.
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:
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:
A process for the preparation of a polyoxyalkylene-alpha,omega-dicarboxylic acid by reacting the corresponding polyoxyalkylene glycol with a stable free radical nitroxide in the presence of a NOx-generating compound and optionally, an oxidant and/or a solvent, at a temperature in the range of from 0 DEG C to 100 DEG C and thereafter separating out the polyoxyalkylene-alpha,omega-dicarboxylic acid.
Abstract:
Disclosed is a process for the production and purification of glycolic acid or glycolic acid derivatives by the carbonylation of formaldehyde in the presence of a homogeneous acid catalyst and a carboxylic acid. This invention discloses hydrocarboxylations and corresponding homogeneous acid catalyst and glycolic acid separations. The homogeneous acid catalyst is readily separated from the hydrocarboxylation reaction effluent and recycled and the carboxylic acid is readily removed from the glycolic acid and the carboxylic acid is recycled.
Abstract:
The present invention refers to a process for modifying epoxidized or non-modified vegetable oils. More specifically, it refers to the process through which vegetable oils and alcohols are converted into fatty acid alkyl esters through transesterification. The present invention also refers to the products obtained through the process disclosed herein.
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