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1. 发明授权

US4137322A ML-236B carboxylic acid derivatives and their use as antihyperlipemic agents 失效
标题翻译： ML-236B羧酸衍生物及其作为抗高脂血症药物的用途
公开(公告)号：US4137322A
公开(公告)日：1979-01-30
申请号：US847044
申请日：1977-10-31
申请人： Akira Endo , Akira Terahara , Noritoshi Kitano , Akira Ogiso , Seiji Mitsui
发明人： Akira Endo , Akira Terahara , Noritoshi Kitano , Akira Ogiso , Seiji Mitsui
IPC分类号： C07F1/00 , C07F3/00 , C07F5/06 , C07C69/74 , A61K31/215 , C07C69/30
CPC分类号： C07F3/003 , C07F1/005 , C07F5/069
摘要： ML-236B carboxylic acid derivatives having the formula ##STR1## wherein R represents an alkyl group, a benzyl group optionally substituted with alkyl, alkoxy or halogen or a phenacyl group optionally substituted with alkyl, alkoxy or halogen; a group of 1/n M in which M represents a metal and n represents a valency of said metal; or a group of AH.sup.+ in which A represents an amino acid. These derivatives are derived from ML-236B by conventional procedures and have an antihyperlipemic activity.
摘要翻译：具有式（I）的ML-236B羧酸衍生物，其中R表示烷基，任选被烷基，烷氧基或卤素取代的苄基或任选被烷基，烷氧基或卤素取代的苯甲酰甲基; 一组1 / n M，其中M表示金属，n表示所述金属的化合价; 或一组AH +，其中A表示氨基酸。这些衍生物通过常规方法来自ML-236B，具有抗高脂血症活性。

2. 发明授权

US4172126A Method for the inactivation of microbial toxins and attenuation of vaccines 失效
标题翻译：灭活微生物毒素和减少疫苗的方法
公开(公告)号：US4172126A
公开(公告)日：1979-10-23
申请号：US846149
申请日：1977-10-27
申请人： Takashi Okonogi , Zenpachiro Hattori , Akira Ogiso , Seiji Mitsui
发明人： Takashi Okonogi , Zenpachiro Hattori , Akira Ogiso , Seiji Mitsui
IPC分类号： A61K36/44 , A61K39/00 , A61K39/02 , A61K39/08 , A61K39/12
CPC分类号： A61K39/00 , A61K36/44 , Y10S435/822 , Y10S435/842 , Y10S435/844 , Y10S435/885
摘要： A method for the inactivation of microbial toxins and attenuation of vaccines by treating the toxin or vaccine with a tannin, especially a condensed tannin derived from fruit of the genus Diospyros, particularly the persimmon, without loss of the desired antigenicity.
摘要翻译：一种通过用单宁处理毒素或疫苗，特别是衍生自Diospyros属的果实，特别是柿子的浓缩单宁而不损失所需抗原性的方法来灭活微生物毒素和减少疫苗。

3. 发明授权

US4198425A Mevalonolactone derivatives 失效
标题翻译：甲酰戊内酯衍生物
公开(公告)号：US4198425A
公开(公告)日：1980-04-15
申请号：US903575
申请日：1978-05-08
申请人： Seiji Mitsui , Akira Ogiso , Akira Indo
发明人： Seiji Mitsui , Akira Ogiso , Akira Indo
IPC分类号： A61K31/365 , A61K31/366 , A61P3/06 , A61P9/10 , C07C45/72 , C07C49/223 , C07C49/255 , C07D309/30
CPC分类号： C07D309/30 , C07C45/72
摘要： This invention concerns novel mevalonolactone derivatives having the formula ##STR1## wherein A represents a direct linkage, methylene, ethylene, trimethylene or vinylene group; R.sup.1 represents hydrogen atom, or an aliphatic acyl group, benzoyl group, or a benzoyl group substituted with hydroxy, lower alkoxy, aliphatic acyloxy or halogen; R.sup.2 represents hydrogen atom, a halogen atom or methyl group; and R.sup.3, R.sup.4 and R.sup.5 are same or different and each represents hydrogen atom, a halogen atom, a lower alkyl group with or without halogen as the substituent, phenyl group, or a phenyl group substituted with halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen, or a group represented by the formula R.sup.6 O-- (in the formula, R.sup.6 means hydrogen atom, an aliphatic acyl group, benzoyl group, phenyl group, a phenylalkyl group, cinnamyl group, or a group of benzoyl, phenyl, phenylalkyl or cinnamyl in all of which the aromatic ring is substituted with hydroxy, halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen as the substituent, or a lower alkyl group with or without halogen as the substituent).The compounds are useful for the treatment of hyperlipidemia.They may be prepared by halo-lactonizing the corresponding .gamma.,.delta.-unsaturated carboxylic acid derivatives and optionally dehalogenating the resulting product, or lactonizing the corresponding .delta.-hydroxy-carboxylic acid derivatives.
摘要翻译：本发明涉及具有下式的新型甲羟戊酸内酯衍生物：其中A代表直链，亚甲基，亚乙基，三亚甲基或亚乙烯基; R1表示氢原子，或脂族酰基，苯甲酰基或被羟基，低级烷氧基，脂族酰氧基或卤素取代的苯甲酰基; R2表示氢原子，卤素原子或甲基; 并且R 3，R 4和R 5相同或不同，各自表示氢原子，卤原子，具有或不具有卤素作为取代基的低级烷基，苯基或被卤素，低级烷氧基，脂族酰氧基或低级具有或不具有卤素的烷基或由式R6O-表示的基团（在式中，R6表示氢原子，脂族酰基，苯甲酰基，苯基，苯基烷基，肉桂基或苯甲酰基，苯基，其中所有芳基被羟基，卤素，低级烷氧基，脂族酰氧基或具有或不具有卤素作为取代基的低级烷基或具有或不具有卤素作为取代基的低级烷基取代的苯基烷基或肉桂基）。该化合物可用于治疗高脂血症。它们可以通过卤代 - 内酯化相应的γ，β-不饱和羧酸衍生物和任选地使得到的产物脱卤，或内酯化相应的δ-羟基 - 羧酸衍生物来制备。

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