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2. 发明授权

US4770870A Method for reducing pain associated with the administration of 4-sulfido-oxazaphosphorines and 4-sulfoalkylthio-oxazaphorphorines 失效
标题翻译：降低与施用4-硫代 - 恶唑磷酸和4-磺基烷硫基 - 恶唑并吡喃相关的疼痛的方法
公开(公告)号：US4770870A
公开(公告)日：1988-09-13
申请号：US714845
申请日：1985-03-22
申请人： Hans-Jurgen Hohorst , Gernot Peter , Georg Voelcker , Erhardt Wrabetz
发明人： Hans-Jurgen Hohorst , Gernot Peter , Georg Voelcker , Erhardt Wrabetz
IPC分类号： A61K31/10 , A61K31/19 , A61K31/675 , C07F9/6584 , A61K31/66
CPC分类号： A61K31/675 , A61K31/10 , A61K31/19 , C07F9/65846 , Y10S514/922
摘要： Through the combined use of a 4-sulfido-oxazaphosphorine of the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are hydrogen, methyl, ethyl, 2-chloroethyl or 2-methanesulfonyloxyethyl and at least two of them are taken from the group consisting of 2-chloroethyl and 2-methanesulfonyloxyethyl, R.sub.4 is hydrogen or methyl, R.sub.5 is a C.sub.2 -C.sub.6 -hydroxyalkyl group or a C.sub.2 -C.sub.6 -mercaptoalkyl group of each of these groups with an additional mercapto group, or R.sub.5 is a carboxy-C.sub.1 -C.sub.10 alkyl group, a carb-C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.10 -alkyl group, a 2-amino-2-carboxyethyl group, a 2-amine-2-carb-C.sub.1 -C.sub.6 -alkoxy-ethyl group, a 2-C.sub.2 -C.sub.6 -alkanoylamino-2-carboxyethyl group, the glutathionyl group, a C.sub.2 -C.sub.6 -sulfoalkyl group or a C.sub.2 -C.sub.6 -sulfoalkyl group which contains a mercapto group or a physiologically compatible salt thereof in combination with a thion compound of the formula:R.sub.6 SR.sub.7 IIwhere R.sub.6 is the glutathionyl group or a C.sub.2 -C.sub.6 -alkyl group which is substituted once or twice by a hydroxy group, mercapto group, amino group, a C.sub.2 -C.sub.6 -alkanoylamino group, sulfo group, a carbo-C.sub.1 -C.sub.6 -alkoxy group or carboxy group and R.sub.7 is hydrogen or R.sub.7 is a C.sub.2 -C.sub.6 -sulfoalkylthio group if R.sub.6 represents a C.sub.2 -C.sub.6 -sulfoalkylthio group or a physiologically compatible salt of the compound of formula II, there is an improvement over known compounds in the chemotherapy of cancer illnesses, especially in having reduced toxicity and side effects. When a compound of formula II is administered simultaneously with a compound of formula I by way of a vein the normal pain associated with the administering of the compound of formula I is prevented.
摘要翻译：通过组合使用下式的其中R 1，R 2和R 3为氢的4-磺酰基 - 恶唑烷磷，其中R 1，R 2和R 3为氢，甲基，乙基，2-氯乙基或2-甲磺酰氧基乙基，并且其中至少两个取自由2-氯乙基和2-甲磺酰氧基乙基组成的基团，R 4是氢或甲基，R 5是这些基团的另外的巯基的C 2 -C 6羟基烷基或C 2 -C 6 - 巯基烷基，或者R 5是羧基 C 1 -C 10烷基，C 1 -C 6烷氧基-C 1 -C 10 - 烷基，2-氨基-2-羧乙基，2-胺-2-碳-C 1 -C 6烷氧基 - 乙基，2-C 2 -C 6烷酰基氨基-2-羧乙基，含有巯基的C 2 -C 6 - 磺基烷基或C 2 -C 6磺基烷基或其生理上相容的盐与硫醇组合 R6SR7II化合物，其中R6是谷胱甘肽基或被羟基，巯基，氨基，C2-C取代一次或两次的C 2 -C 6烷基 6-烷酰基氨基，磺基，碳-C 1 -C 6 - 烷氧基或羧基，且R 7为氢或R 7为C 2 -C 6 - 磺基烷硫基，如果R 6表示C 2 -C 6 - 磺基烷硫基或生理上相容的盐式II化合物对癌症疾病化学疗法中已知化合物的改善，特别是毒性和副作用降低。当式I化合物与式I化合物一起静脉给药时，可防止与给予式I化合物相关的正常疼痛。

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