公开(公告)号：US5480899A

公开(公告)日：1996-01-02

申请号：US167798

申请日：1993-12-21

申请人： Shingo Yano ,  Tomoyasu Ohno ,  Kazuo Ogawa ,  Haruo Yamada ,  Tetsuhiko Shirasaka ,  Hiroyuki Kawamura ,  Shinichi Watanabe

发明人： Shingo Yano ,  Tomoyasu Ohno ,  Kazuo Ogawa ,  Haruo Yamada ,  Tetsuhiko Shirasaka ,  Hiroyuki Kawamura ,  Shinichi Watanabe

IPC分类号： C07D263/16 ,  C07D263/24 ,  C07D263/26 ,  C07D263/32 ,  C07D413/04 ,  A61K31/42

CPC分类号： C07D263/16 ,  C07D263/24 ,  C07D263/26 ,  C07D263/32 ,  C07D413/04

摘要： An oxazolidine derivative represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H, optionally halogenated alkyl, optionally halogenated alkoxy, OH, halo, NO.sub.2, amino optionally having acetyl or alkyl, COOH, alkoxycarbonyl, CN, alkanoyl, 2-oxazolyl, or R.sup.1 and R.sup.2 may be combined with each other to represent --(CH.sub.2).sub.p -- or --O(CH.sub.2).sub.q O-- (p is 3-5, q is 1-3) to form a ring, m and n are each 0 or 1, R.sup.4 and R.sup.5 are H or alkyl, X is C or N, Y is CH.sub.2 OH, CHO or COOR.sup.6 (R.sup.6 is alkyl, benzyl or H), A is alkylene, carbonyl or sulfonyl, B is alkylene, E is alkylene which may be substituted with halo or is alkenylene, Z is O or S, except for a compound wherein n is 0, m is 1 and Y is CH.sub.2 OH, and except for a compound wherein n is 0, Y is COOR.sup.6 (R.sup.6 is alkyl), a salt thereof, a process for its preparation, anti-hyperlipidemic composition containing the derivative as an active ingredient and a method for treating hyperlipidemia comprising administering the derivative.

摘要翻译： PCT No.PCT / JP93 / 00559 Sec。 371日期：1993年12月21日 102（e）日期1993年12月21日PCT提交1993年4月28日PCT公布。 出版物WO93 / 22298 （I）表示的恶唑烷衍生物其中R 1，R 2和R 3为H，任意卤代烷基，任选卤代烷氧基，OH，卤素，NO 2，任选具有乙酰基或烷基的氨基， COOH，烷氧基羰基，CN，烷酰基，2-恶唑基或R 1和R 2可以彼此结合以表示 - （CH 2）p - 或-O（CH 2）q O-（p为3-5，q为1-3 ）形成环，m和n各自为0或1，R4和R5为H或烷基，X为C或N，Y为CH2OH，CHO或COOR6（R6为烷基，苄基或H），A为亚烷基， 羰基或磺酰基，B是亚烷基，E是可以被卤素取代的亚烷基或亚烷基，Z是O或S，除了其中n是0，m是1且Y是CH 2 OH的化合物，除了其中 n为0，Y为COOR 6（R6为烷基），其盐，其制备方法，含有该衍生物作为活性成分的抗高血脂组合物和治疗高脂血症的方法，其包括给予该衍生物。

公开(公告)号：US5475118A

公开(公告)日：1995-12-12

申请号：US211950

申请日：1994-05-03

申请人： Shingo Yano ,  Tomoyasu Ohno ,  Kazuo Ogawa ,  Tetsuhiko Shirasaka

发明人： Shingo Yano ,  Tomoyasu Ohno ,  Kazuo Ogawa ,  Tetsuhiko Shirasaka

IPC分类号： A61K31/40 ,  C07D207/26 ,  C07D207/267

CPC分类号： C07D207/26

摘要： Disclosed are a 1-phenylpyrrolidone derivative having optical activity and represented by the formula (I) ##STR1## wherein R represents an optionally substituted optically active .alpha.-phenylethylamino group, a 1-phenylpyrrolidone derivative represented by the formula (I-a) ##STR2## and processes for preparing the 1-phenylpyrrolidone derivatives represented by the formulas (I) and (I-a), respectively.

摘要翻译： PCT No.PCT / JP93 / 01274 Sec。 371日期：1994年5月3日 102（e）日期1994年5月3日PCT提交1993年9月8日PCT公布。 第WO94 / 06767号公报 日期：1994年3月31日。公开是具有光学活性的1-苯基吡咯烷酮衍生物，由式（I）表示。其中R表示任选取代的光学活性α-苯乙基氨基，表示的1-苯基吡咯烷酮衍生物 分别通过式（Ia）（Ia）和由式（I）和（Ia）表示的1-苯基吡咯烷酮衍生物的制备方法。

公开(公告)号：US5401739A

公开(公告)日：1995-03-28

申请号：US142307

申请日：1993-11-23

申请人： Tomoyasu Ohno ,  Shingo Yano ,  Kosuke Fujiwara ,  Hirofusa Ajioka ,  Noriyuki Yamamoto ,  Shozo Yamada ,  Makoto Kajitani

发明人： Tomoyasu Ohno ,  Shingo Yano ,  Kosuke Fujiwara ,  Hirofusa Ajioka ,  Noriyuki Yamamoto ,  Shozo Yamada ,  Makoto Kajitani

IPC分类号： C07D285/24 ,  C07D417/12 ,  A61K31/54

CPC分类号： C07D417/12 ,  C07D285/24

摘要： A benzothiadiazine derivative, hydrate thereof and acid addition salt thereof, the derivative being represented by the general formula (I) ##STR1## wherein X is methylene or a nitrogen atom substituted with a lower alkyl, Y and Z are each methylene or carbonyl, A is phenylene or phenylene substituted with methoxycarbonyl, R.sub.4 is lower alkylene or lower alkenylene, R.sub.1 is a hydrogen atom, acetoxyacetyl, cyclohexylmethyl or benzyl wherein the benzene ring may be substituted with lower alkoxyl, halogen atom, nitro, lower alkyl, methylenedioxy or hydroxyl, R.sub.2 is lower alkyl or phenyl, and R.sub.3 is a hydrogen atom, halogen atom or lower alkoxyl with the exception of the case where X, Y and Z are each methylene, A is unsubstituted phenylene, R.sub.4 is lower alkylene and R.sub.1 is a hydrogen atom; and a peptic ulcer treating agent containing as an effective component the above derivative, hydrate thereof or acid addition salt thereof.

公开(公告)号：US4891369A

公开(公告)日：1990-01-02

申请号：US123631

申请日：1987-11-23

申请人： Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi ,  Tomoyasu Ohno

发明人： Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi ,  Tomoyasu Ohno

IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/42 ,  C07D499/44 ,  C07D499/86

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： Disclosed are 2.beta.-substituted-methylpenicillanic acid compounds of the formula ##STR1## wherein n is 0, 1 or 2; and ##STR2## is monocyclic or bicyclic heterocyclic ring group which has 2 to 4 nitrogen atoms as hetero atom in its ring structure and which may be optionally substituted with alkyl, alkoxycarbonyl, phenyl, formyl or benzyloxycarbonyl optionally having alkyl, nitro or a halogen atom on the benzene ring, with the proviso that said heterocyclic ring group is not 1,2,3-triazol-1-yl; or salts or esters thereof.These compounds are useful as .beta.-lactamase inhibitor.