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1. 发明授权

US5756730A Process for preparing analgesic compounds 失效
标题翻译：镇痛药化合物的制备方法
公开(公告)号：US5756730A
公开(公告)日：1998-05-26
申请号：US789941
申请日：1997-01-28
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 , C07D403/14
CPC分类号： C07D265/30 , C07D211/26 , C07D241/04 , C07D279/12 , C07D409/06 , C07D417/06
摘要： A process for preparing a compound of the formula (I) ##STR1## in which, R.sup.1 and R.sup.2 are the same or different and each is 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 heterocyclic ring which is unsubstituted or substituted and is a 5-membered or 6-membered N-heterocycle which optionally has a further heteroatom which is oxygen, nitrogen or sulfur; E is methylene; ring A is a unsubstituted or unsubstituted aryl ring, or a substituted or an unsubstituted heteroaryl ring; R.sup.3 is a C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen, or R.sup.3 and R.sup.4 together are a group of the formula --(CR.sup.a R.sup.b).sub.m --C(.dbd.Y)-- (IV), wherein each of R.sup.a and R.sup.b is hydrogen or C.sub.1 -C.sub.3 alkyl, provided that there are not more than three alkyl groups in the formula (IV), m is 1, 2, or 3, and Y is two hydrogens or an oxygen; or a pharmaceutically acceptable salt thereof; which process comprises reacting an acid of the formula (II) ##STR2## with an amine of the following formula (III) ##STR3##
摘要翻译：制备式（I）化合物（Ⅰ）的方法，其中R 1和R 2相同或不同，各自为氢或C 1 -C 6烷基，或者R 1和R 2与其中的氮原子一起它们连接形成未取代或取代的杂环，并且是任选具有另外的氧，氮或硫杂原子的5元或6元N-杂环; E是亚甲基; 环A是未取代或未取代的芳基环，或取代或未取代的杂芳基环; R3是C1-C6烷基，R4是氢，R3和R4一起是式 - （CRaRb）mC（= Y） - （IV）的基团，其中R a和R b分别是氢或C 1 -C 3烷基条件是式（Ⅳ）中不超过三个烷基，m为1,2或3，Y为2个氢或氧; 或其药学上可接受的盐; 该方法包括使式（II）的酸（II）与下式（III）的胺反应：（III）

2. 发明授权

US5679674A Optically active thiomorpholine derivatives 失效
标题翻译：光学活性硫代吗啉衍生物
公开(公告)号：US5679674A
公开(公告)日：1997-10-21
申请号：US387897
申请日：1995-02-22
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： A61K31/54 , A61P25/04 , A61P29/00 , C07D20060101 , C07D279/12 , C07D417/06
CPC分类号： C07D279/12
摘要： Optically active carboxamide derivatives having analgesic activity and being useful as an analgesic agent. The compounds have a general formula: ##STR1## (in the above formula, R.sup.1 represents a hydrogen or halogen atom; R.sup.2 represents a halogen atom; R.sup.3 represents a pyrrolidino or piperidino group; Y represents a methylene or carbonyl group; and n is an integer of 1 or 2) and pharmacologically acceptable salts thereof.
摘要翻译： PCT No.PCT / JP93 / 01210 Sec。 371日期1995年2月22日 102（e）1995年2月22日PCT PCT 1993年8月27日PCT公布。公开号WO94 / 05646 日期：1994年3月17日具有止痛活性的光学活性羧酰胺衍生物，可用作止痛剂。该化合物具有以下通式：（I）（在上式中，R 1表示氢或卤原子; R 2表示卤素原子; R 3表示吡咯烷子基或哌啶子基; Y表示亚甲基或羰基; n为1或2的整数）及其药理学上可接受的盐。

3. 发明授权

US4622421A Phenylalkanoic acid derivatives and their use 失效
标题翻译：苯基链烷酸衍生物及其用途
公开(公告)号：US4622421A
公开(公告)日：1986-11-11
申请号：US798236
申请日：1985-11-14
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 , C07C69/73
CPC分类号： C07C59/54
摘要： Compounds of formula (I): ##STR1## (wherein R represents hydrogen or a C.sub.1 -C.sub.3 alkyl group) have analgesic, anti-inflammatory and immuno-regulatory activities. The compounds exist in the form of cis- and trans-isomers with respect to the cyclohexyl ring, as well as a number of optical isomers.

4. 发明授权

US4673761A Process for preparing anti-inflammatory cycloalkylidenemethylphenylacetic acid derivatives 失效
标题翻译：抗炎环烷基甲基苯乙酸衍生物的制备方法
公开(公告)号：US4673761A
公开(公告)日：1987-06-16
申请号：US750481
申请日：1985-06-28
申请人： Atsusuke Terada , Kazuyuki Wachi
发明人： Atsusuke Terada , Kazuyuki Wachi
IPC分类号： C07C59/86 , C07C51/00 , C07C51/347 , C07C51/353 , C07C51/373 , C07C67/00
CPC分类号： C07C51/347 , C07C51/353
摘要： Cycloalkylidenemethylphenylacetic acid derivatives of formula (I): ##STR1## (wherein R.sup.1 represents hydrogen or alkyl and n is an integer from 1 to 3) are prepared by reacting a benzaldehyde acid compound of formula (II): ##STR2## with an enamine derivative of formula (III): ##STR3## (wherein R.sup.2 and R.sup.3 are various organic groups) and then hydrolizing the product. The use of the acid of formula (II) rather than its corresponding ester enables the reaction to be effected with a good yield and under moderate and economical reaction conditions.
摘要翻译：式（I）的环亚烷基亚甲基苯基乙酸衍生物：其中R 1表示氢或烷基，n为1至3的整数）通过使式（II）的苯甲醛酸化合物：（IMA） II）与式（III）的烯胺衍生物：其中R 2和R 3是各种有机基团，然后使产物水解。使用式（II）的酸而不是其相应的酯使得能够以良好的产率和在中等和经济的反应条件下进行反应。

5. 发明授权

US4400534A Analgesic and anti-inflammatory agents 失效
标题翻译：止痛药和消炎药
公开(公告)号：US4400534A
公开(公告)日：1983-08-23
申请号：US331616
申请日：1981-12-17
申请人： Atsusuke Terada , Eiichi Misaka
发明人： Atsusuke Terada , Eiichi Misaka
IPC分类号： A61K31/19 , A61K31/045 , A61P25/04 , A61P29/00 , A61P43/00 , C07C51/487 , C07C59/11 , C07C59/54 , C07C59/00
CPC分类号： C07C59/54 , C07C51/487
摘要： Compounds of formula (I): ##STR1## its salts, and resolved forms thereof, especially the compound of formula (II): ##STR2## and its salts are new analgesic and/or anti-inflammatory agents. The agents are prepared by resolution at the 2-position of a suitable starting material such as the compound (IV): ##STR3## or an optionally partly resolved form thereof, with subsequent reduction and optional resolution to give the trans form.
摘要翻译：式（I）化合物：其盐及其分解形式，特别是式（II）化合物：其中，新的止痛剂和/或抗炎剂是新的。通过在合适的起始物质如化合物（IV）：（IV）或其任选的部分拆分的形式的2-位拆分制备试剂，随后还原和任选的分辨率得到反式。

6. 发明授权

US4254274A Cycloalkylidenemethylphenylacetic acid derivatives and process for the preparation thereof 失效
标题翻译：环亚烷基甲基苯乙酸衍生物及其制备方法
公开(公告)号：US4254274A
公开(公告)日：1981-03-03
申请号：US929937
申请日：1978-08-01
申请人： Atsusuke Terada , Shigeru Tanaka , Eiichi Misaka
发明人： Atsusuke Terada , Shigeru Tanaka , Eiichi Misaka
IPC分类号： C07C69/738 , A61K31/19 , A61K31/215 , A61P25/20 , A61P29/00 , C07C51/00 , C07C59/86 , C07C67/00 , C07C279/14 , C07C69/753
CPC分类号： C07C279/14
摘要： Novel 4-(2-oxo-1-cycloalkylidenemethyl)phenylacetic acid derivatives and non-toxic pharmaceutically acceptable salts thereof are useful as anti-inflammatory agents.The compounds may be prepared by reacting a p-formylphenylacetic acid ester derivative with an enamine of cycloalkanone and hydrolyzing the resulting product, or with a cycloalkanone in the presence of a base.
摘要翻译：新的4-（2-氧代-1-环丙基甲基）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。可以通过使对甲酰基苯基乙酸酯衍生物与环烷酮的烯胺反应并在碱的存在下水解所得产物或与环烷酮反应来制备化合物。

7. 发明授权

US5656758A Process for preparing analgesic compounds 失效
标题翻译：镇痛药化合物的制备方法
公开(公告)号：US5656758A
公开(公告)日：1997-08-12
申请号：US409865
申请日：1995-03-24
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 , C07D403/14 , C07D401/06 , C07D403/06
CPC分类号： C07D265/30 , C07D211/26 , C07D241/04 , C07D279/12 , C07D409/06 , C07D417/06
摘要： A process for preparing a compound 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 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), which comprises reacting an acid of the formula ##STR2## with an amine of the formula ##STR3##
摘要翻译：制备式（I）化合物的方法：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式杂环 E表示任选被C 1 -C 6烷基或芳烷基取代的亚甲基，硫，氧或亚氨基; 环A是任选取代的芳基或杂芳基环; R 3是氢或C 1 -C 6烷基，R 4是氢或R 3和R 4一起表示式（Ⅳ）的基团： - （CR a R a）m C（= Y） - （Ⅳ）（其中R a和R a是C 1 -C 6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，R 3是C 1 -C 6烷基，或者R 3和R 4一起代表式（Ⅳ）的基团，其包括使式ⅩⅧ的酸与式

8. 发明授权

US5354768A 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：US5354768A
公开(公告)日：1994-10-11
申请号：US975987
申请日：1992-11-13
申请人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazwa , Yoshio Iizuka , Kazuo Hasegawa , Keiichi Tabata
发明人： Atsusuke Terada , Kazuyuki Wachi , Hachio Miyazwa , 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## [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：式（I）化合物：其中：R 1和R 2为氢，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。

9. 发明授权

US5270327A 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：US5270327A
公开(公告)日：1993-12-14
申请号：US943386
申请日：1992-09-10
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 , A61K31/445 , A61K31/535 , A61K31/54 , C07D295/10
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 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 5-6-membered N-heterocyclic ring optionally having a further O, N, or S heteroatom; E represents methylene; ring A is an unsubstituted or substituted benzene or naphthalene; R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(=Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen with up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygens.
摘要翻译：式（I）的镇痛化合物：其中，R 1 R2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5-6元任选具有另外的O，N或S杂原子的N-杂环; E表示亚甲基; 环A是未取代或取代的苯或萘; R 3和R 4一起表示式（Ⅳ）的基团： - （CRaRa）mC（= Y） - （Ⅳ）其中Ra和Ra是C1-C6烷基或氢，最多达3个烷基，m是1 ，2或3，Y是两个氢或氧。

10. 发明授权

US4847272A Thianaphthene derivatives 失效
标题翻译：硫茚衍生物
公开(公告)号：US4847272A
公开(公告)日：1989-07-11
申请号：US007375
申请日：1987-01-27
申请人： Atsusuke Terada , Yoshiya Amemiya , Keiichi Matsuda , Takeshi Oshima
发明人： Atsusuke Terada , Yoshiya Amemiya , Keiichi Matsuda , Takeshi Oshima
IPC分类号： A61K31/381 , A61K31/415 , A61K31/44 , A61P7/02 , C07D333/54 , C07D333/56 , C07D333/68 , C07D409/06 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D409/06
摘要： Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R.sup.1 and R.sup.2 are hydrogen or alkyl, one of A.sup.1 and A.sup.2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment or prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.

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