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11. 发明授权

US4599360A Ophthalmic anti-inflammatory agents 失效
标题翻译：眼科消炎药
公开(公告)号：US4599360A
公开(公告)日：1986-07-08
申请号：US639376
申请日：1984-08-09
申请人： Masaharu Fukami , Atsusuke Terada , Kazue Hasegawa
发明人： Masaharu Fukami , Atsusuke Terada , Kazue Hasegawa
IPC分类号： A61K9/08 , A61K31/19 , A61K31/215 , A61P27/02
CPC分类号： A61K31/215 , A61K31/19 , Y10S514/914
摘要： Compounds of formula: ##STR1## (wherein R represents hydrogen or methyl, >A--B-- represents a >CH--CH.sub.2 -- or >C.dbd.CH-- group; >C--Z represents a >C.dbd.O or >CH--OH group; and n represents 1 or 2) and ophthalmically acceptable salts and esters thereof are useful as ophthalmic anti-inflammatory agents.
摘要翻译：式（I）化合物（其中R表示氢或甲基，> AB-表示a> CH-CH 2 - 或> C = CH-基; CZ表示C = O或> CH-OH基; n 代表1或2）和眼用可接受的盐和酯可用作眼用抗炎剂。

12. 发明授权

US5698576A Use of imidazopyrazole derivatives as analgesics anti-inflammatory agents 失效
标题翻译：使用咪唑并吡唑衍生物作止痛剂抗炎剂
公开(公告)号：US5698576A
公开(公告)日：1997-12-16
申请号：US755290
申请日：1996-11-22
申请人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
发明人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
IPC分类号： A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D487/04 , C07D235/00
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725
摘要： Described herein are compounds of formula (I): ##STR1## �in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic!; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
摘要翻译：本文描述的是式（I）的化合物：其中：R 1和R 2是氢，任选取代的烷基，环烷基，烯基，芳烷基，芳基烯基，芳基，芳族杂环，氰基或卤素; R3是氢，任选取代的烷基，芳烷基或酰基; R 4和R 5是氢，任选取代的烷基，环烷基，烯基，芳烷基，芳基烯基，芳基或芳族杂环]; 及其药学上可接受的盐是具有抗溃疡和5-脂氧合酶抑制活性的止痛剂和抗炎剂。

13. 发明授权

US5232939A Use of imidazopyrazole derivatives as analgesics and anti-inflammatory agents 失效
标题翻译：咪唑并吡唑衍生物作为止痛剂和抗炎剂使用
公开(公告)号：US5232939A
公开(公告)日：1993-08-03
申请号：US798256
申请日：1991-11-18
申请人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
发明人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
IPC分类号： A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D487/04
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725
摘要： Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
摘要翻译：式（I）的化合物：其中（I）及其药学上可接受的盐是止痛剂和抗炎剂，并具有抗溃疡和5-脂氧合酶抑制活性。

14. 发明授权

US5021413A Analgesic thiomorpholins their preparation, and pharmaceutical compositions containing them 失效
标题翻译：止痛硫代吗啉类及其制剂，含有它们的药物组合物
公开(公告)号：US5021413A
公开(公告)日：1991-06-04
申请号：US397105
申请日：1989-08-22
申请人： Atsusuke Terada , Yoshio Iizuka , Kazuyuki Wachi , Kenji Fujibayashi
发明人： Atsusuke Terada , Yoshio Iizuka , Kazuyuki Wachi , Kenji Fujibayashi
IPC分类号： C07D211/26 , C07D241/04 , C07D265/30 , C07D279/12 , C07D409/06 , C07D417/06
CPC分类号： C07D265/30 , C07D211/26 , C07D241/04 , C07D279/12 , C07D409/06 , C07D417/06
摘要： Analgesic compounds are of the general formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).

15. 发明授权

US4161538A Substituted phenylacetic acid derivatives and process for the preparation thereof 失效
标题翻译：取代苯乙酸衍生物及其制备方法
公开(公告)号：US4161538A
公开(公告)日：1979-07-17
申请号：US885527
申请日：1978-03-10
申请人： Atsusuke Terada , Kazuyuki Wachi , Eiichi Misaka
发明人： Atsusuke Terada , Kazuyuki Wachi , Eiichi Misaka
IPC分类号： C07C279/14 , A61K31/19 , C07C65/20
CPC分类号： C07C279/14 , C07C2101/08
摘要： 4-(2-Oxo- or hydroxyimino-cycloalkan-1-ylmethyl)phenylacetic acid derivative and nontoxic pharmaceutically acceptable salt thereof are useful as an anti-inflammatory agent. The above 2-oxo-compound may be prepared by (a) hydrolyzing and decarboxylating 4-(1-alkoxycarbonyl-2-oxocycloalkan-1-ylmethyl)phenylacetic acid ester derivative or (b) reacting p-halomethylphenylacetic acid ester derivative with an enamine of cycloalkanone and hydrolyzing the resulting product. And further, the above 2-hydroxyimino-compound may be prepared by (c) reacting 4-(2-oxocycloalkan-1-ylmethyl)phenylacetic acid derivative (the product of process (a) or (b)) with hydroxylamine or (d) reacting a dilithium salt of cycloalkanone oxime with p-halomethyl- or p-sulfonyloxymethyl-phenylacetic acid ester derivative and hydrolyzing the resulting product.
摘要翻译： 4-（2-氧代 - 或肟基 - 环烷基-1-基甲基）苯乙酸衍生物及其无毒的药学上可接受的盐可用作抗炎剂。上述2-氧代化合物可以通过（a）水解和脱羧4-（1-烷氧基羰基-2-氧代环烷烃-1-基甲基）苯乙酸酯衍生物或（b）使对卤甲基苯乙酸酯衍生物与烯胺的环烷酮并水解所得产物。此外，上述2-羟基亚氨基化合物可以通过（c）使4-（2-氧代环烷烃-1-基甲基）苯乙酸衍生物（方法（a）或（b）的产物）与羟胺或（d ）使环烷酮肟的二锂盐与对卤甲基 - 或对 - 磺酰氧基甲基 - 苯基乙酸酯衍生物反应并水解所得产物。

16. 发明授权

US5723481A Use of imidazopyrazole derivatives as analgesics and anti-inflammatory agents 失效
标题翻译：咪唑并吡唑衍生物作为止痛剂和抗炎剂使用
公开(公告)号：US5723481A
公开(公告)日：1998-03-03
申请号：US260896
申请日：1994-06-16
申请人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
发明人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
IPC分类号： A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D487/04 , C07D235/00
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725
摘要： Described herein are of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
摘要翻译：本文所述的具有式（I）：其中（I）及其药学上可接受的盐是具有抗溃疡和5-脂氧合酶抑制活性的止痛剂和抗炎剂。

17. 发明授权

US5665752A Use of imidazopyrazole derivatives as analgesics and anti-inflammatory agents 失效
标题翻译：咪唑并吡唑衍生物作为止痛剂和抗炎剂使用
公开(公告)号：US5665752A
公开(公告)日：1997-09-09
申请号：US418825
申请日：1995-04-07
申请人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
发明人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazawa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
IPC分类号： A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D487/04 , C07D235/00
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4188 , A61K31/422 , A61K31/4439 , A61K31/4725
摘要： Described herein are compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
摘要翻译：本文描述的是式（I）的化合物：其中药学上可接受的盐是止痛剂和抗炎剂，并具有抗溃疡和5-脂氧合酶抑制活性。

18. 发明授权

US5512567A Analgesic compounds, their preparation, and pharmaceutical compositions containing them 失效
标题翻译：止痛化合物，它们的制备和含有它们的药物组合物
公开(公告)号：US5512567A
公开(公告)日：1996-04-30
申请号：US373469
申请日：1995-01-17
申请人： Atsusuke Terada , Yoshio Iizuka , Kazuyuki Wachi , Kenji Fujibayashi
发明人： Atsusuke Terada , Yoshio Iizuka , Kazuyuki Wachi , Kenji Fujibayashi
IPC分类号： C07D211/26 , C07D241/04 , C07D265/30 , C07D279/12 , C07D409/06 , C07D417/06 , A61K31/495 , A61K31/50 , C07D413/06
CPC分类号： C07D265/30 , C07D211/26 , C07D241/04 , C07D279/12 , C07D409/06 , C07D417/06
摘要： Analgesic compounds of the formula (I); ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents oxygen or an imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is an aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen; provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).
摘要翻译：式（I）的止痛化合物; （I）其中，R 1和R 2各自表示氢或C 1 -C 6烷基，或者R 1和R 2与它们所连接的氮原子一起形成杂环; E表示氧或任选被C 1 -C 6烷基或芳烷基取代的亚氨基; 环A是任选取代的芳基或杂芳基环; R3是氢或C1-C6烷基，R4是氢或R3和R4一起代表式（Ⅳ）的基团： - （CRaRa）mC（= Y） - （Ⅳ）其中Ra和Ra是C1-C6烷基或氢，最多3个烷基，m为1,2或3，Y为2个氢或氧; 条件是当E表示亚甲基时，则R 3是C 1 -C 6烷基或R 3和R 4一起表示式（Ⅳ）的基团。

19. 发明授权

US4595699A Immune system regulation using novel phenylalkanoic acid derivative 失效
标题翻译：使用新的苯基链烷酸衍生物进行免疫系统调控
公开(公告)号：US4595699A
公开(公告)日：1986-06-17
申请号：US600372
申请日：1984-04-16
申请人： Atsusuke Terada , Shunji Naruto , Yoshio Iizuka
发明人： Atsusuke Terada , Shunji Naruto , Yoshio Iizuka
IPC分类号： A61K31/19 , A61P25/04 , A61P29/00 , A61P37/00 , C07C51/00 , C07C59/54 , C07C67/00 , C07C69/76 , C07C63/33
CPC分类号： C07C59/54
摘要： A method of regulating the immune system of a mammal, which comprises administering to said mammal an immuno-regulatory agent, wherein said agent is selected from the group consisting of compounds of the formula (I): ##STR1## (wherein R represents hydrogen or a C.sub.1 -C.sub.3 alkyl group) and pharmaceutically acceptable salts and esters thereof.
摘要翻译：一种调节哺乳动物免疫系统的方法，其包括向所述哺乳动物施用免疫调节剂，其中所述药剂选自式（I）的化合物：其中R 表示氢或C1-C3烷基）及其药学上可接受的盐和酯。

20. 发明授权

US4461912A Phenylacetic acid derivatives, their preparation and compositions containing them 失效
标题翻译：苯乙酸衍生物，它们的制备和含有它们的组合物
公开(公告)号：US4461912A
公开(公告)日：1984-07-24
申请号：US447474
申请日：1982-12-06
申请人： Atsusuke Terada , Shunji Naruto , Eiichi Misaka
发明人： Atsusuke Terada , Shunji Naruto , Eiichi Misaka
IPC分类号： C07C69/732 , A61K31/19 , A61K31/215 , A61P29/00 , C07C51/00 , C07C51/347 , C07C59/54 , C07C67/00 , C07C62/30 , C07C59/00
CPC分类号： C07C59/54
摘要： Phenylacetic derivatives of formula (I): ##STR1## (wherein R represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group and n represents an integer from 1 to 3) and salts and esters thereof have analgesic, antipyretic and anti-inflammatory activity and may be prepared by reducing the corresponding acid or ester having an oxo group at the 2-position of the cycloalkylidene ring system and, if necessary, salifying the resulting product.
摘要翻译：式（I）的苯乙酸衍生物：其中R表示氢原子或C1-C3烷基，n表示1〜3的整数），其盐和酯具有止痛，解热，并且可以通过在环烷叉环体系的2-位还原相应的具有氧代基团的酸或酯（如果需要）使所得产物成盐来制备。

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