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1. 发明授权

US06379552B1 Method for resolving optical isomers 失效
标题翻译：拆分光学异构体的方法
公开(公告)号：US06379552B1
公开(公告)日：2002-04-30
申请号：US09347062
申请日：1999-07-02
申请人： Tetsuji Kitagawa , Atsushi Okamoto , Takashi Kanai , Katsuhiro Shibayama , Tomoyuki Aoki , Shinobu Yamakawa
发明人： Tetsuji Kitagawa , Atsushi Okamoto , Takashi Kanai , Katsuhiro Shibayama , Tomoyuki Aoki , Shinobu Yamakawa
IPC分类号： B01D1500
CPC分类号： C07B57/00
摘要： A method for efficiently resolving optical isomers, in which a discriminating liquid consisting of a discriminating agent capable of discriminating optical isomers and a diluent are brought into contact with a mixture containing said optical isomers in countercurrent flow, to resolve the optical isomers by adsorption separation, distillation separation, absorption separation or membrane separation, and recovered at an optical isomer content of 5 wt % or less for recycled use, under one or more of the following conditions: (a) the dielectric constant of the diluent is 30 or less and the viscosity of the discriminating liquid is 0.2 Pa·s or less at the temperature of the resolving operation; (b) the discriminating agent contained has the effect of splitting the 1H or 13C-NMR spectrum peak of the optical isomers when added and the diluent contained has a dielectric constant equal to or lower than the dielectric constant of the measuring solvent at the time of measuring the 1H or 13C-NMR spectrum; (c) the boiling point of at least one compound of the discriminating agent at the pressure of the resolving operation is higher than the boiling point of at least one compound of the diluent at the pressure of the resolving operation; (d) the boiling point of at least one compound of the diluent at the pressure of the resolving operation is higher than the boiling point of the optical isomers to be resolved, at the pressure of the resolving operation, by 10° C. or more; and (e) the concentration of the discriminating agent in the discriminating liquid is 10 wt % or more.
摘要翻译：光学异构体的有效解决方法是将由能够鉴别光学异构体的识别剂组成的识别液与稀释剂逆流流动地与包含所述光学异构体的混合物接触，从而通过吸附分离来分解光学异构体，蒸馏分离，吸收分离或膜分离，并在一种或多种以下条件下以5重量％以下的光学异构体含量回收再循环使用：（a）稀释剂的介电常数为30以下，鉴定液的粘度在分解操作的温度下为0.2Pa.s以下;（b）所含的鉴别剂具有在添加时分解光学异构体的1H或13C-NMR谱峰的作用，并且稀释剂含有介电常数等于或低于在测量1H或13C-NMR谱时测量溶剂的介电常数（c）解析操作压力下鉴别剂的至少一种化合物的沸点高于分解操作压力下至少一种稀释剂化合物的沸点;（d）在拆分操作压力下，至少一种稀释剂化合物的沸点高于分解操作压力下要拆分的光学异构体的沸点10℃或更高; 和（e）鉴别液中鉴别剂的浓度为10重量％以上。

2. 发明授权

US5478823A Composition for suppressing infiltration of eosinophils 失效
标题翻译：用于抑制嗜酸性粒细胞浸润的组合物
公开(公告)号：US5478823A
公开(公告)日：1995-12-26
申请号：US244891
申请日：1994-08-22
申请人： Katsuhiro Shibayama , Naoki Hirayama , Tetsuya Katou , Shu Matsumoto
发明人： Katsuhiro Shibayama , Naoki Hirayama , Tetsuya Katou , Shu Matsumoto
IPC分类号： C07D487/04 , A61K31/55 , A61K31/41 , A61K31/445 , A61K31/495 , A61K31/50
CPC分类号： C07D487/04
摘要： An agent for suppressing infiltration of eosinophils comprising as an effective ingredient a tricyclic triazolo derivative, which strongly suppresses infiltration of eosinophils into inflammatory regions, of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.5 cycloalkyl or substituted or non-substituted aryl; R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 independently represent hydrogen or lower alkyl; A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene with the proviso that it may contain one or more hetero atoms; 1 represents 0 to 2, n represents 1 to 3, -- represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.2 independently represent hydrogen or substituted or non-substituted aryl, CAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above, O--CHAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above or a condensed aromatic ring or a pharmaceutically acceptable salt thereof.
摘要翻译：抑制嗜酸性粒细胞浸润的药剂，其包含作为有效成分的三环三唑衍生物，其将强烈抑制嗜酸性粒细胞浸润至炎性区域的式（I）：其中R1表示氢，低级烷基，C3- C5环烷基或取代或未取代的芳基; R2和R3独立地表示氢，低级烷基，低级烷氧基或卤素; W表示C = O或CR 4 R 5，其中R 4和R 5独立地表示氢或低级烷基; A表示C1-C5直链或支链饱和或不饱和亚烷基，条件是其可以含有一个或多个杂原子; 1表示0〜2，n表示1〜3， - 表示单键或双键; Y表示N或C; Z表示C（B）Ar1Ar2其中B表示氢，羟基或甲氧基，Ar1和Ar2独立地表示氢或取代或未取代的芳基，CAr1Ar2其中Ar1和Ar2表示与上述相同的含义，O-CHAr1Ar2其中Ar1和Ar2 表示与上述相同的含义或稠合芳环或其药学上可接受的盐。

3. 发明授权

US5683998A Tricyclic triazolo derivatives, processes for producing the same and the uses of the same 失效
标题翻译：三环三唑衍生物，其制备方法及其用途
公开(公告)号：US5683998A
公开(公告)日：1997-11-04
申请号：US432714
申请日：1995-05-02
申请人： Katsuhiro Shibayama , Tetsuya Makino , Takayuki Imaoka , Tetsuya Katou , Masayuki Kaneko
发明人： Katsuhiro Shibayama , Tetsuya Makino , Takayuki Imaoka , Tetsuya Katou , Masayuki Kaneko
IPC分类号： C07D487/04 , C07D519/00 , A61K31/495 , C07D243/12
CPC分类号： C07D487/04
摘要： Novel tricyclic triazolo derivatives and pharmaceutically acceptable salts thereof, which are useful as anti-inflammation agents, anti-allergy agents or anti-PAF agents as well as processes for producing the same are disclosed. The triazolo derivatives of the present invention are represented by the formula (I): ##STR1## �wherein R.sup.1 represents hydrogen, lower alkyl or C.sub.3 -C.sub.5 cycloalkyl; R.sup.2 and R.sup.3 respectively represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 respectively represents hydrogen or lower alkyl); A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene which may contain one or more hetero atoms; l represents 0 to 2, n represents 1 to 3, . . . represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 (wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.2 respectively represent hydrogen or substituted or non-substituted aryl), CAr.sup.1 Ar.sup.2 (wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above), O--CHAr.sup.1 Ar.sup.2 (wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above) or condensed aromatic ring!.
摘要翻译：公开了可用作抗炎剂，抗过敏剂或抗PAF剂的新型三环三唑衍生物及其药学上可接受的盐及其制备方法。本发明的三唑衍生物由式（I）表示：其中R 1表示氢，低级烷基或C 3 -C 5环烷基; R2和R3分别表示氢，低级烷基，低级烷氧基或卤素; W表示C = O或CR4R5（其中R4和R5分别表示氢或低级烷基）; A表示可含有一个或多个杂原子的C1-C5直链或支链饱和或不饱和亚烷基; l表示0〜2，n表示1〜3。。。表示单键或双键; Y表示N或C; Z表示C（B）Ar1Ar2（其中B表示氢，羟基或甲氧基，Ar1和Ar2分别表示氢或取代或未取代的芳基），CAr1Ar2（其中Ar1和Ar2表示与上述相同的含义），O-CHAr1Ar2 （其中Ar1和Ar2表示与上述相同的含义）或稠合芳香环]。

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