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91. 发明授权

US5350873A Optically active phenoxypropionic esters 失效
标题翻译：光学活性苯氧基丙酸酯
公开(公告)号：US5350873A
公开(公告)日：1994-09-27
申请号：US928568
申请日：1992-08-13
申请人： Volker Bach , Wolfgang Brox , Karl-Heinz Etzbach , Axel Paul , Karl Siemensmeyer
发明人： Volker Bach , Wolfgang Brox , Karl-Heinz Etzbach , Axel Paul , Karl Siemensmeyer
IPC分类号： C07C69/708 , C07C69/712 , C07C69/734 , C07C69/74 , C07C69/753 , C07C69/757 , C07C69/76 , C07C69/773 , C07C69/86 , C07C69/92 , C07C69/94 , C08F20/30 , C08G63/60 , C09K19/20 , C09K19/58
CPC分类号： C08G63/60 , C07C69/712 , C07C69/92 , C07C69/94 , C08F20/30 , C09K19/586
摘要： Optically active compounds of the formula I ##STR1## where R is C.sub.1 -C.sub.12 -alkyl or -perfluoroalkyl in which one or two non-adjacent CH.sub.2 or CF.sub.2 groups can also be replaced by --O-- and/or --CO-- and/or --CO--O-- and/or --CH.dbd.CH-- and/or --CH-halogen-- and/or --CHCN-- and/or --0--CO--CH-halogen-- and/or --O--CO--CHCN--, or is C.sub.1 -C.sub.12 -alkyl which can have a terminal chemically reactive group and in which a CH.sub.2 group can be replaced by --O--,A.sup.1 and A.sup.2 are each, independently of one another, 1,4-phenylene which is unsubstituted or substituted by one or two F and/or Cl and/or Br atoms and/or CH.sub.3 groups and/or CN groups and in which one or two CH groups can also be replaced by N, 1,4-cyclohexylene in which one or two non-adjacent CH.sub.2 groups can also be replaced by --O-- and/or --S--, 1,4-piperidinediyl, 1,4-bicyclo[2.2.2]octylene, 2,6-naphthalenediyl, decahydro-2,6-naphthalenediyl or 1,2,3,4-tetrahydro-2,6-naphthalenediyl,A.sup.3 is unsubstituted or substituted phenyl,Z is --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, --C.tbd.C-- or a single bond andm is 0, 1, 2 or 3.
摘要翻译：其中R是具有一个或两个不相邻的CH2或CF2基团的C1-C12-烷基或全氟烷基的式I的光学活性化合物（I）也可以被-O-和/或-CO- 和/或-CO-O-和/或-CH = CH-和/或-CH-卤素 - 和/或-CHCN-和/或-O-CO-CH-卤素 - 和/或-O-CO- CHCN-或可具有末端化学反应性基团并且其中CH 2基团可被-O-，A 1和A 2取代的C 1 -C 12 - 烷基彼此独立地为彼此独立的1,4-亚苯基，其为未被取代或被一个或两个F和/或Cl和/或Br原子和/或CH 3基团和/或CN基团取代，并且其中一个或两个CH基团也可被N，1,4-亚环己基代替，其中一个或两个或两个不相邻的CH 2基团也可以被-O-和/或-S-，1,4-哌啶二基，1,4-二环[2.2.2]亚辛基，2,6-萘二甲酸，十氢-2， 6-萘二基或1,2,3,4-四氢-2,6-萘二基，A3是未取代或取代的苯基，Z是-CO-O-，-O-CO-，-CH2CH2 - ， - OCH2 - ， - CH2O-，-C3OND C或单键，m为0,1,2或3。

92. 发明授权

US5334740A Cyclohexanetriol derivatives 失效
标题翻译：环己烷三醇衍生物
公开(公告)号：US5334740A
公开(公告)日：1994-08-02
申请号：US851943
申请日：1992-03-13
申请人： Takashi Takahashi , Manzo Shiono
发明人： Takashi Takahashi , Manzo Shiono
IPC分类号： C07C69/732 , C07C33/14 , C07C35/17 , C07C43/178 , C07C43/188 , C07C43/196 , C07C47/267 , C07C49/337 , C07C49/35 , C07C69/734 , C07C401/00 , C07D261/20 , C07D311/74 , C07D311/76 , C07D317/20 , C07D317/46 , C07D493/04 , C07D498/04 , C07F7/18 , C07D311/02 , C07D262/20 , C07C69/74
CPC分类号： C07D493/04 , C07D261/20 , C07D311/76 , C07D317/46 , C07F7/1856 , Y02P20/55
摘要： Cyclohexanetriol derivatives represented by the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different, and each denotes a hydrogen atom or a protecting group of a hydroxyl group,X denotes an oxygen atom, .dbd.CHCH.sub.2 OR.sup.4, .dbd.CHCHO or .dbd.CHCO.sub.2 R.sup.5, Y denotes a hydrogen atom and Z denotes --OR.sup.6, or Y and Z together form a single bond; or X and Z together form .dbd.NO--, .dbd.CHCH(OR.sup.7)O-- or .dbd.CHCO.sub.2 -- and Y is a hydrogen atom, R.sup.4 and R.sup.6 denote a hydrogen atom or a protecting group of a hydroxyl group respectively, R.sup.5 denotes a lower alkyl group, and R.sup.7 denotes a hydrogen atom or a lower alkyl group.Said derivatives are useful as synthetic intermediates of 1-hydroxyvitamin D derivatives.
摘要翻译：式中，R 1，R 2和R 3相同或不同，表示氢原子或羟基保护基，X表示氧原子，= CHCH 2 OR 4 = CHCHO或= CHCO 2 R 5表示的环己烷三醇衍生物，Y表示氢原子，Z表示-OR6，或Y和Z一起形成单键; 或X和Z一起形成= NO-，= CHCH（OR7）O-或= CHCO2-，Y为氢原子，R4和R6分别表示氢原子或羟基的保护基，R5表示低级烷基，R7表示氢原子或低级烷基。所述衍生物可用作1-羟基维生素D衍生物的合成中间体。

93. 发明授权

US5324743A Leukotriene B.sub.4 antagonists 失效
标题翻译：白三烯B4拮抗剂
公开(公告)号：US5324743A
公开(公告)日：1994-06-28
申请号：US988615
申请日：1992-12-10
申请人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
发明人： Robert D. Dillard , J. Scott Sawyer , Michael J. Sofia
IPC分类号： C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D307/91 , C07D311/66 , C07D311/86 , A61K31/35 , C07D311/58
CPC分类号： C07D307/91 , C07C59/90 , C07C65/40 , C07C69/712 , C07C69/734 , C07C69/92 , C07D311/66 , C07D311/86
摘要： This invention provides certain 1,2,4,5 substituted benzene derivatives containing "acid" substituents derived from cyclic or heterocyclic moieties. These unique compounds are leukotriene B.sub.4 antagonists and formulations of these derivatives, and a method of using these derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
摘要翻译：本发明提供了含有衍生自环状或杂环部分的“酸”取代基的某些1,2,4,5取代的苯衍生物。这些独特的化合物是白三烯B4拮抗剂和这些衍生物的制剂，以及使用这些衍生物来治疗以白细胞三烯过度释放为特征的病症的方法。

94. 发明授权

US5319139A Naphthalene derivatives 失效
标题翻译：萘衍生物
公开(公告)号：US5319139A
公开(公告)日：1994-06-07
申请号：US40026
申请日：1993-03-30
申请人： Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hirsohi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
发明人： Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hirsohi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
IPC分类号： A61K31/165 , A61K31/19 , A61K31/192 , A61K31/197 , A61K31/215 , A61K31/22 , A61K31/222 , A61K31/275 , A61P19/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07C39/40 , C07C43/20 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/84 , C07C59/90 , C07C69/157 , C07C69/734 , C07C69/738 , C07C235/34 , C07C251/48 , C07C255/41 , C07C233/00
CPC分类号： C07C255/41 , C07C251/48 , C07C39/40 , C07C43/202 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/90 , C07C69/734 , C07C69/738 , C07C2101/08
摘要： Compounds of the formula: ##STR1## where R.sup.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a lower alkoxy group;R.sub.3 is a group ##STR2## Z is represented by the formula: ##STR3## where R.sub.2 and R.sub.3 may be the same or different from each other and each stands for a hydrogen atom or a lower alkyl;Y is represented by the formula: --(CH.sub.2).sub.n -- where n is 0 or an integer of 1 to 2 or a group represented by the formula: ##STR4## where R.sup.2 and R.sup.3 may be the same or different from each other and each stands for a lower alkyl group; andR.sup.4 represents a group of the formula: ##STR5## where p is 0 or an integer of 1 to 3 and R.sup.12 is hydrogen, a halogen atom, a lower alkyl or a lower alkoxy group a hydrogen atom, R.sup.2 is a methoxy group, R.sup.3 is a hydroxy group and R.sup.4 is a benzyl group having anti-inflammatory activity.
摘要翻译：下式的化合物：其中R 1是氢原子或低级烷基; R2是低级烷氧基; R 3是一个基团Z由下式表示：其中R 2和R 3可以相同或不同，各代表氢原子或低级烷基; Y由下式表示： - （CH 2）n - 其中n为0或1至2的整数或由下式表示的基团：其中R 2和R 3可以彼此相同或不同，代表低级烷基; 并且R 4表示下式的基团：其中p为0或1至3的整数，R 12为氢，卤素原子，低级烷基或低级烷氧基，氢原子，R 2为甲氧基， R3是羟基，R4是具有抗炎活性的苄基。

95. 发明授权

US5298511A Alkanoic acid derivatives 失效
标题翻译：烷酸衍生物
公开(公告)号：US5298511A
公开(公告)日：1994-03-29
申请号：US948594
申请日：1992-09-23
申请人： David Waterson
发明人： David Waterson
IPC分类号： A61K31/19 , A61K31/215 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07B57/00 , C07C67/31 , C07C69/734 , C07C317/44 , C07C323/62 , C07D215/14 , C07D215/22 , C07D215/227 , C07C69/76 , C07C315/00 , C07C321/00 , C07D215/16
CPC分类号： C07D215/227 , C07C69/734 , C07D215/14
摘要： The invention concerns alkanoic acid derivatives of the formula I ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3 C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;n is 0, 1 or 2 and R.sup.1 is halogeno, (1-4 C)alkyl, (1-4 C)alkoxy or fluoro-(1-4 C)alkyl;each of R.sup.2 and R.sup.3 is (1-4 C)alkyl, (2-4 C)alkenyl or (2-4 C)alkynyl; andR.sup.4 is hydrogen or (1-4 C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
摘要翻译：本发明涉及式I（*化学结构*）I的链烷酸衍生物，其中Ar1是任选取代的苯基或萘基，或含有一个或两个氮杂原子并任选地含有另外的杂原子的10元双环杂环部分，氧和硫; A1是直接连接到X1或是（1-3C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; n为0,1或2，R 1为卤素，（1-4C）烷基，（1-4C）烷氧基或氟 - （1-4C）烷基; R2和R3各自为（1-4C）烷基，（2-4C）烯基或（2-4C）炔基; 和R4是氢或（1-4C）烷基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

96. 发明授权

US5243066A Alkyl 2-aryl-2,2-dialkoxyacetates, the preparation thereof and a method of using them for preparing arylglyoxylic esters 失效
标题翻译：亚苄基-2-亚氨基-2,2-二烷氧基乙酸酯，其制备方法及其制备芳基酯类的方法
公开(公告)号：US5243066A
公开(公告)日：1993-09-07
申请号：US907974
申请日：1992-07-02
申请人： Dieter Hermeling
发明人： Dieter Hermeling
IPC分类号： C07C69/734 , C25B3/02
CPC分类号： C25B3/02 , C07C69/734
摘要： Alkyl 2-aryl-2,2-dialkoxyacetates are prepared by electrochemical oxidation of alkyl 2-arylacetates and are used to prepare arylglyoxylic esters.
摘要翻译：烷基2-芳基-2,2-二烷氧基乙酸酯通过2-烷基乙酸烷基酯的电化学氧化制备，并用于制备芳基乙醛酸酯。

97. 发明授权

US5237091A Naphthalene derivatives 失效
标题翻译：萘衍生物
公开(公告)号：US5237091A
公开(公告)日：1993-08-17
申请号：US890223
申请日：1992-05-29
申请人： Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hiroshi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
发明人： Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hiroshi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
IPC分类号： C07C39/40 , C07C43/20 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/90 , C07C69/734 , C07C69/738 , C07C251/48 , C07C255/41
CPC分类号： C07C255/41 , C07C251/48 , C07C39/40 , C07C43/202 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/90 , C07C69/734 , C07C69/738 , C07C2101/08
摘要： The present invention relates to a naphthalene derivative. More particularly, it relates to a naphthalene derivative exhibiting an excellent activity as a drug.
摘要翻译：萘衍生物本发明涉及萘衍生物。更具体地说，本发明涉及作为药物具有优异活性的萘衍生物。

98. 发明授权

US5220074A Optically active isoxazole derivatives and intermediates for preparation thereof as well as processes for producing the same 失效
标题翻译：光活性异恶唑衍生物及其制备中间体及其制备方法
公开(公告)号：US5220074A
公开(公告)日：1993-06-15
申请号：US906323
申请日：1992-06-30
申请人： Takashi Takahashi , Kazuhiko Sakaguchi
发明人： Takashi Takahashi , Kazuhiko Sakaguchi
IPC分类号： C07C43/178 , C07C43/315 , C07C45/29 , C07C45/51 , C07C45/56 , C07C45/66 , C07C47/277 , C07C49/255 , C07C49/753 , C07C69/734 , C07D261/20
CPC分类号： C07D261/20 , C07C43/1782 , C07C43/1787 , C07C43/315 , C07C45/29 , C07C45/296 , C07C45/515 , C07C45/56 , C07C45/66 , C07C47/277 , C07C49/255 , C07C49/753 , C07C69/734
摘要： The present invention relates to novel optically active isoxazole derivatives represented by general formula: ##STR1## which are useful as intermediates for synthesis of prostaglandin and a process for producing the same as well as novel aldehyde compounds represented by general formula: ##STR2## which are intermediates for preparing the compounds [XI] described above and a process for preparation thereof. In the compounds shown by these formulae, R.sup.1 represents an alkyl group or a cycloalkyl group which may have an alkoxy group or a group shown by -Ra-A-B (wherein Ra is an alkyl group; A is a hetero atom or an single bond; and B is an aromatic or hetero ring which may have a substituent(s)); and R.sup.2 and R.sup.3, which may be the same or different, each represents an aralkyl group, a silyl group or an acyl group.
摘要翻译：本发明涉及以通式表示的新颖的光学活性异恶唑衍生物：作为前列腺素合成的中间体及其制备方法，以及由通式表示的新型醛化合物：IMAGE > [IX]，它们是制备上述化合物[XI]的中间体及其制备方法。在这些化合物所示的化合物中，R 1表示可以具有烷氧基的环烷基或-R a-AB所示的基团（其中R a为烷基; A为杂原子或单键; 并且B是可以具有取代基的芳族或杂环）; 并且可以相同或不同的R 2和R 3各自表示芳烷基，甲硅烷基或酰基。

99. 发明授权

US5145766A Process for stabilizing magenta couplers and the corresponding image dyes in photographic materials 失效
标题翻译：用于稳定摄影材料中的魔法偶联剂和相应的图像染料的方法
公开(公告)号：US5145766A
公开(公告)日：1992-09-08
申请号：US699102
申请日：1991-05-13
申请人： David G. Leppard , David H. Steinberg , Henri Dubas
发明人： David G. Leppard , David H. Steinberg , Henri Dubas
IPC分类号： C07C69/712 , C07C69/017 , C07C69/732 , C07C69/734 , C07C69/92 , C07C309/73 , G03C1/34 , G03C7/34 , G03C7/392
CPC分类号： G03C7/39232 , C07C69/017 , C07C69/732
摘要： Compounds of the formula ##STR1## in which R is hydrogen or hydroxyl, R.sub.1 is alkyl, alkoxy, amino or aryl, and R.sub.2 is hydrocarbylcarbonyl or hydrocarbylsulfonyl, are highly suitable for stabilizing magenta couplers in photographic materials.
摘要翻译：其中R为氢或羟基，R1为烷基，烷氧基，氨基或芳基，R2为烃基羰基或烃基磺酰基的式“IMAGE”化合物非常适用于稳定摄影材料中的品红色成色剂。

100. 发明授权

US5140046A Phenylene derivatives, compositions and use 失效
标题翻译：苯衍生物，组合物和用途
公开(公告)号：US5140046A
公开(公告)日：1992-08-18
申请号：US567159
申请日：1990-08-13
申请人： Toshiyasu Mase , Kiyoshi Murase , Hiromu Hara , Kenichi Tomioka
发明人： Toshiyasu Mase , Kiyoshi Murase , Hiromu Hara , Kenichi Tomioka
IPC分类号： A61K31/195 , C07C45/71 , C07C47/575 , C07C59/70 , C07C59/72 , C07C65/21 , C07C65/24 , C07C69/712 , C07C69/734 , C07C233/81 , C07C235/56 , C07C235/64 , C07C255/60 , C07C271/28 , C07C275/40 , C07D257/04 , C07D285/12 , C07D285/125 , C07D285/135
CPC分类号： C07D257/04 , C07C235/56 , C07C235/64 , C07C255/00 , C07C255/60 , C07C271/28 , C07C275/40 , C07C45/71 , C07C47/575 , C07C59/70 , C07C59/72 , C07C65/21 , C07C65/24 , C07C69/712 , C07C69/734 , C07D285/125 , C07D285/135
摘要： Novel phenylene derivatives shown by the general formula ##STR1## where A represents a hydrogen atom, a phenyl group or a phenoxy group, n represents an integer of 3 to 10, R.sub.1 represents a hydrogen atom or a lower alkoxy group, X.sub.1 represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CONH--, B represents ##STR2## wherein R.sub.2 represents a hydrogen atom, a halogen atom, a nitro group, etc.), ##STR3## (wherein R.sub.3 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group), X.sub.2 represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, etc. and D represents a carboxy group, a lower alkoxycarbonyl group or ##STR4## which are useful as drugs, particularly SRS-A(slow reacting substance of anaphylaxis) antagonist, i.e. they are useful as prophylaxis and treatment for various allergic diseases (e.g. bronchial asthma, allergic rhinitis, urticaria) or, ischemic heart diseases, inflammation, etc. induced by SRS-A.
摘要翻译：其中A表示氢原子，苯基或苯氧基，n表示3〜10的整数，R 1表示氢原子或低级烷氧基，X 1表示-CH 2 CH 2的通式[IMAGE]所示的新型亚苯基衍生物 - ， - CH = CH-，-CONH-，+ E，crc / B /表示其中R2表示氢原子，卤素原子，硝基等），其中R3表示氢原子，羟基或低级烷氧基），X2表示-CH = CH-，-CH2CH2-等，D表示可用作药物的羧基，低级烷氧基羰基或“IMAGE”，特别是SRS -A（过敏反应缓慢反应物质）拮抗剂，即可用作预防和治疗由SRS-A引起的各种过敏性疾病（如支气管哮喘，过敏性鼻炎，荨麻疹）或缺血性心脏病，炎症等。

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