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91. 发明授权

US5104979A Polyazo dyes with diazo components of the aminophenol and the amino diphenyl-sulfide, -sulfoxide or -sulfone series 失效
标题翻译：含有氨基苯酚和氨基二苯基硫醚，硅氧烷或磺化物系列的DIAZO组分的聚氧乙烯染料
公开(公告)号：US5104979A
公开(公告)日：1992-04-14
申请号：US559996
申请日：1990-07-31
申请人： Guenter Hansen , Georg Zeidler , Ortwin Schaffer
发明人： Guenter Hansen , Georg Zeidler , Ortwin Schaffer
IPC分类号： C09B33/00 , C07C317/36 , C07C323/66 , C09B33/02 , C09B33/24 , C09B35/50 , C09B45/24
CPC分类号： C09B45/24 , C07C317/36 , C07C323/66 , C09B33/02 , C09B33/24 , C09B35/50
摘要： Polyazo dyes useful for dyeing leather in the free form or as copper, chromium, iron, cobalt or nickel complexes have the formula ##STR1## where m is 0, 1 or 2, n is 0 or 1, p is from 1 to 2, q is from 0 to 1, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and the ring A are each as defined, and may be prepared from aniline derivatives of the formula ##STR2## where m is 0, 1, or 2, n is 0 or 1, and X, R.sup.1, R.sub.2 and R.sup.3 are each as defined.
摘要翻译：可用于以游离形式或作为铜，铬，铁，钴或镍络合物染色皮革的多偶氮染料具有通式为“IMAGE”，其中m为0,1或2，n为0或1，p为1至2， q为0至1，并且R 1，R 2，R 3，R 4，R 5，R 6，R 7，X，Y和环A各自如上所定义，并且可以由下式的苯胺衍生物制备：其中m为 0,1或2，n为0或1，X，R 1，R 2和R 3各自为定义。

92. 发明授权

US5015775A Alkyl aryl sulfones and method of preparing the same 失效
标题翻译：烷基芳基砜及其制备方法
公开(公告)号：US5015775A
公开(公告)日：1991-05-14
申请号：US175873
申请日：1988-03-31
申请人： James L. Reilly , Gordon R. Leader
发明人： James L. Reilly , Gordon R. Leader
IPC分类号： C07B61/00 , C07B45/04 , C07C315/00 , C07C317/14 , C07C317/20 , C07C317/22 , C07C317/24 , C07C317/30 , C07C317/32 , C07C317/36 , C07C319/20 , C07C323/65 , C07C323/67
CPC分类号： C07C317/00 , C07B45/04
摘要： Alkyl aryl sulfones of the formula R--SO.sub.2 --AR--Y.sub.n, wherein Ar is an aryl compound, Y is a substituent on the aryl compound and R is alkyl or cycloalkyl, and liquid mixtures of positional isomers of the same are prepared by reacting an aryl compound of the formula Ar--Y.sub.n, with an alkyl sulfonic acid of the formula R--SO.sub.3 H and a phosphorus reagent, preferably under heat. Particularly good yields and pure products are obtained using phosphorus pentoxide. Alkyl aryl sulfones produced by this method are a liquid mixture preferably containing at least two positional isomers, wherein no isomer is present in an amount of more than about 50% of the isomer mixture.

93. 发明授权

US4921872A Acaricidal agents based on azomethines of 2,3-diaminomaleic acid nitrile 失效
标题翻译：基于2,3-二氨基马来酸腈的偶氮甲碱的杀螨剂
公开(公告)号：US4921872A
公开(公告)日：1990-05-01
申请号：US149244
申请日：1988-01-27
申请人： Holger Heidenreich , Benedikt Becker
发明人： Holger Heidenreich , Benedikt Becker
IPC分类号： A01N37/34 , A01N35/10 , A01N37/40 , A01N37/42 , A01N37/44 , A01N37/48 , A01N37/50 , A01N41/10 , A01N47/02 , A01N47/04 , C07C20060101 , C07C67/00 , C07C253/00 , C07C253/18 , C07C255/06 , C07C255/30 , C07C255/32 , C07C255/61 , C07C313/00 , C07C317/32 , C07C317/36 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/45 , C07C323/62
CPC分类号： C07C255/00 , A01N37/44 , A01N37/50 , A01N47/04
摘要： A method of combating acarids which comprises applying to such acarids or to an acarid habitat an acaricidally effective amount of an azomethine of 2,3-diaminomaleic acid nitrile of the formula ##STR1## in which X represents halogen, halogenoalkyl or CN and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be identical or different and represent hydrogen, optionally substituted alkyl, optionally substituted alkoxy, halogen, CN, NO.sub.2, optionally substituted dialkylamino, alkoxycarbonyl, optionally substituted alkylthio, optionally substituted alkylthionyl, optionally substituted alkylsulphonyl, OH, SH or NH.sub.2. The compounds other than the 2-chloro-and 2,6-dichloro-toluylideneamino-compounds are new.
摘要翻译：一种抗螨剂的方法，其包括向所述螨或螨栖息地施用杀螨有效量的式（I）的2,3-二氨基马来酸腈的偶氮甲碱，其中X表示卤素，卤代烷基或CN， R 1，R 2，R 3和R 4可以相同或不同，表示氢，任选取代的烷基，任选取代的烷氧基，卤素，CN，NO 2，任选取代的二烷基氨基，烷氧基羰基，任选取代的烷硫基，任选取代的烷基硫酰基，任选取代的烷基磺酰基， SH或NH2。除2-氯 - 和2,6-二氯 - 甲苯亚甲基氨基化合物以外的化合物是新的。

94. 发明授权

US4895840A N-(aryl-,aryloxy-,arylthio-arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or n'n')alkylaminoalkyl ureas and cyanoguanidines 失效
标题翻译： N-（芳基 - ，芳氧基 - ，芳硫基 - 芳基亚磺酰基 - 和芳基磺酰基）烷基-N，N' - （或n'n'）烷基氨基烷基脲和氰基胍
公开(公告)号：US4895840A
公开(公告)日：1990-01-23
申请号：US60266
申请日：1987-06-10
申请人： James R. Shanklin, Jr.
发明人： James R. Shanklin, Jr.
IPC分类号： A61K31/17 , A61K31/00 , A61K31/275 , A61K31/34 , A61K31/341 , A61P9/06 , C07C67/00 , C07C239/00 , C07C275/14 , C07C275/24 , C07C279/28 , C07C313/00 , C07C317/28 , C07C317/32 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C323/20 , C07C323/44 , C07C323/65 , C07C335/08 , C07D213/40 , C07D213/64 , C07D213/70 , C07D213/71 , C07D295/13 , C07D307/38 , C07D307/40
CPC分类号： C07D213/40 , C07C317/28 , C07C317/42 , C07C323/44 , C07C335/08 , C07D295/13 , C07D307/38
摘要： Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.4 may together with the adjacent nitrogen form the heterocyclic ring structure 1-homopiperidinyl, 4-morpholinyl, 1-piperazinyl, 4-substituted-1-piperazinyl, 1-pyrrolidinyl or 1-piperidinyl and the pharmaceutically acceptable salts thereof are disclosed. A pharmaceutical method for administering the compounds for their cardiac antiarrhythmic effect and pharmaceutical compositions for the treatment of cardiac arrhythmia are also disclosed.

95. 发明授权

US4853398A Leukotriene antagonists and use thereas 失效
标题翻译：白细胞三烯拮抗剂并在其中使用
公开(公告)号：US4853398A
公开(公告)日：1989-08-01
申请号：US038254
申请日：1987-04-13
申请人： F. P. Carr , Robert D. Dillard , Doris E. McCullough
发明人： F. P. Carr , Robert D. Dillard , Doris E. McCullough
IPC分类号： C07C69/734 , C07C51/00 , C07C51/08 , C07C51/347 , C07C59/68 , C07C59/74 , C07C59/90 , C07C59/92 , C07C65/21 , C07C65/24 , C07C65/34 , C07C67/00 , C07C69/738 , C07C69/92 , C07C201/00 , C07C213/00 , C07C217/86 , C07C217/90 , C07C217/92 , C07C223/02 , C07C225/16 , C07C253/00 , C07C253/30 , C07C255/53 , C07C255/55 , C07C255/56 , C07C313/00 , C07C317/22 , C07C317/24 , C07C317/36 , C07C317/40 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C323/36 , C07C323/62 , C07C323/65 , C07D257/04 , C07D285/10
CPC分类号： C07D257/04 , C07C255/00
摘要： This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.

96. 发明授权

US4843151A Monoazo dyes containing a 4'-methyl-3'-sulfo-5-acylamino-2-azo-1,1'-diphenylsulfone component 失效
标题翻译：含有4'-甲基-3'-磺基-5-酰基氨基-2-偶氮-1,1'-二苯砜组分的单偶氮染料
公开(公告)号：US4843151A
公开(公告)日：1989-06-27
申请号：US36423
申请日：1987-04-09
申请人： Rudolf Hurter
发明人： Rudolf Hurter
IPC分类号： C07C315/04 , C07C67/00 , C07C313/00 , C07C317/14 , C07C317/36 , C07C317/40 , C09B29/01 , C09B29/08 , C09B29/12 , C09B29/33 , C09B29/36
CPC分类号： C09B29/0003 , C09B29/0803 , C09B29/12 , C09B29/331 , C09B29/36
摘要： The monoazo dyes of the formula ##STR1## in which K is the radical of a coupling component of the aminobenzene, alkoxybenzene, hydroxybenzene, pyrazolone, aminopyrazole, pyrimmidine, indole, diphenylamine or acetoacetamide series, R is a substituted or unsubstituted C.sub.1-12 alkyl, cycloalkyl, aralkyl or aryl radical, X is a --CO-- or --SO.sub.2 -- group, a --COO-- group, R being attached to the oxygen atoms, or an --SO.sub.2 NH-- or ##STR2## group, R being attached to the nitrogen atom and Y being hydrogen or C.sub.1-4 alkyl, and Z is hydrogen or C.sub.1-4 alkyl, produce dyeings having good fastness to light and wet processing on polyamide material.
摘要翻译：式（1）的单偶氮染料其中K是氨基苯，烷氧基苯，羟基苯，吡唑啉酮，氨基吡唑，嘧啶，吲哚，二苯胺或乙酰乙酰胺系列的偶联组分的基团，R是取代或未取代的C1 -12烷基，环烷基，芳烷基或芳基，X是-CO-或-SO 2 - 基团，-COO-基团，R与氧原子连接，或-SO 2 NH-或者<！ - SIPO < 附着于氮原子，Y为氢或C 1-4烷基，Z为氢或C1-4烷基，产生对聚酰胺材料的光亮和湿加工牢度好的染色。

97. 发明授权

US4775411A Certain substituted 3-amino-2-benzoylcyclohex-2-enones 失效
标题翻译：某些取代的3-氨基-2-苯甲酰基环己-2-酮
公开(公告)号：US4775411A
公开(公告)日：1988-10-04
申请号：US872079
申请日：1986-06-09
申请人： Christopher G. Knudsen
发明人： Christopher G. Knudsen
IPC分类号： A01N33/08 , A01N33/10 , A01N35/06 , A01N35/08 , A01N37/22 , A01N37/34 , A01N37/44 , A01N41/06 , A01N41/10 , A01N43/36 , A01N43/78 , A01N43/84 , A01N47/02 , A01N47/18 , C07C67/00 , C07C213/00 , C07C225/20 , C07C225/22 , C07C239/14 , C07C253/00 , C07C255/24 , C07C255/56 , C07C301/00 , C07C311/16 , C07C313/00 , C07C317/14 , C07C317/32 , C07C317/36 , C07C317/48 , C07C317/50 , C07C323/22 , C07C323/62 , C07C323/65 , C07C323/67 , C07D277/04 , C07D295/10 , C07D295/116 , A01N33/02
CPC分类号： C07D295/116 , A01N35/06 , A01N37/44 , A01N41/10 , A01N43/78 , C07C255/00 , C07D277/04
摘要： A compound of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, nitro; cyano; C.sub.1 -C.sub.2 haloalkyl, or R.sup.a SO.sub.n - wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl; R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; or R.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms; R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; or C.sup.3 and R.sup.4 are oxo; R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; and R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n - wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)--wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkogxy; (12) SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined; or (13) --N(R.sup.c)C(O)R.sup.d wherein R.sup.c and R.sup.d are as defined; R.sup.9 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.10 is (a) hydrogen; (b) C.sub.1 -C.sub.6 alkyl, (c) C.sub.4 -C.sub.6 cycloalkyl, (d) substituted C.sub.1 -C.sub.6 alkyl, (e) phenyl; (f) substituted phenyl; (g) C.sub.1 -C.sub.6 alkoxy; (h) benzyl; (i) phenethyl; (j) C.sub.1 -C.sub.4 alkyl-C(O)-; (k) C.sub.1 -C.sub.4 alkyoxy-C(O)-; (1) C.sub.2 -C.sub.6 alkenyl; or (m) C.sub.2 -C.sub.6 alkynyl; and R.sup.9 and R.sup.10 together form a heterocyclic ring with the nitrogen to which they are attached containing 0, 1 or 2 additional hetero atoms (nitrogen, sulfur or oxygen).

98. 发明授权

US4774333A Water-soluble triphendioxazine compounds and sulfonyl-containing precursors thereof, processes for the preparation thereof and use of the triphendioxazines as dyes 失效
标题翻译：水溶性三苯并二恶嗪化合物及其含磺酰基前体，其制备方法和使用三苯并恶嗪作为染料
公开(公告)号：US4774333A
公开(公告)日：1988-09-27
申请号：US13974
申请日：1987-02-12
申请人： Hartmut Springer , Walter Helmling , Gunther Schwaiger
发明人： Hartmut Springer , Walter Helmling , Gunther Schwaiger
IPC分类号： C09B19/00 , C07C67/00 , C07C313/00 , C07C315/04 , C07C317/22 , C07C317/36 , C07C319/20 , C07C323/65 , C07D498/04 , C09B62/503 , D06P1/384 , D06P3/66
CPC分类号： C09B62/5033
摘要： Water-soluble triphendioxazine compounds having fiber-reactive dye properties conforming to the general formula ##STR1## where: B is --O-- or --S-- or --NH-- or (C.sub.1 -C.sub.6)-alkylamino;R* is hydrogen or optionally substituted alkyl or aryl;W and W.sup.1 are each a bivalent, aliphatic or optionally alkyl-substituted cycloaliphatic or aliphatic-cycloaliphatic radical, which aliphatic radicals can be interrupted by --O--, --S--, sulfonyl, carbonyl, 1,4-piperidino, amino, alkylamino and/or alkanoylamino groups, orthe grouping --B--W.sup.1 --N(R*) and/or --N(R*)--W--B-- each represent the bivalent radical of a five- or six-membered saturated heterocycle which contains two nitrogen atoms, orthe grouping --B--W.sup.1 -- and/or --W--B-- each represent the bivalent radical of a five- or six-membered saturated heterocycle which contains two nitrogen atoms and which is bonded by one of the two nitrogen atoms via an alkylene group of 2 to 4 carbon atoms to the grouping --N(R*)--CO--G.sup.1 -- or --G--CO--A--N(R*);G and G.sup.1 are each a direct bond or a (C.sub.1 -C.sub.8)-alkylene or aliphatic-cycloaliphatic or cycloaliphatic radical;M is hydrogen, alkali metal or alkaline earth metal;X.sup.1 and X.sup.2 are each hydrogen, halogen, alkyl, alkoxy, aryloxy or optionally substituted aryl;Y is vinyl or ethyl having an alkali-eliminable substituent in the .beta.-position.The triphendioxazine compounds serves as dyes for carboxamido-containing fiber materials and hydroxyl-containing fiber materials.
摘要翻译：具有符合通式的纤维反应性染料性质的水溶性三苯并二恶嗪化合物，其中：B为-O-或-S-或-NH-或（C 1 -C 6） - 烷基氨基; R *是氢或任选取代的烷基或芳基; W和W1各自是二价，脂族或任选的烷基取代的脂环族或脂族 - 脂环族基团，脂族基团可以被-O - ， - S-，磺酰基，羰基，1,4-哌啶子基，氨基，烷基氨基和 /或烷酰基氨基，或分组-B-W1-N（R *）和/或-N（R *）-WB-各自表示含有两个氮原子的五元或六元饱和杂环的二价基团，或分组-B-W1-和/或-WB-各自表示五或六元饱和杂环的二价基团，其含有两个氮原子，并且其通过亚烷基与两个氮原子之一键合（R *）-CO-G1-或-G-CO-AN（R *）的2至4个碳原子; G和G1各自是直接键或（C1-C8） - 亚烷基或脂族 - 脂环族或脂环族基; M是氢，碱金属或碱土金属; X 1和X 2各自为氢，卤素，烷基，烷氧基，芳氧基或任选取代的芳基; Y是在β-位具有碱可消除取代基的乙烯基或乙基。三苯并二恶嗪化合物用作含甲酰胺的纤维材料和含羟基纤维材料的染料。

99. 发明授权

US4760183A Process for the preparation of aromatic dialkylamines 失效
标题翻译：芳族二烷基胺的制备方法
公开(公告)号：US4760183A
公开(公告)日：1988-07-26
申请号：US893362
申请日：1986-08-05
申请人： Theodor Papenfuhs , Walter Kuhn
发明人： Theodor Papenfuhs , Walter Kuhn
IPC分类号： C07B43/04 , B01J23/00 , B01J23/40 , B01J27/00 , B01J27/045 , B01J31/00 , B01J31/02 , C07B31/00 , C07B61/00 , C07C67/00 , C07C209/00 , C07C209/26 , C07C209/28 , C07C209/36 , C07C211/27 , C07C211/44 , C07C211/48 , C07C213/00 , C07C213/02 , C07C215/76 , C07C217/80 , C07C217/84 , C07C227/00 , C07C227/04 , C07C227/18 , C07C229/54 , C07C229/64 , C07C231/00 , C07C231/12 , C07C233/43 , C07C233/78 , C07C313/00 , C07C315/04 , C07C317/36 , C07C317/40 , C07C317/48 , C07C85/08
CPC分类号： C07C209/26
摘要： A process for the preparation of aromatic dialkylamines of the formula (1) ##STR1## in which R denotes an alkyl-C.sub.1 -C.sub.6 group, X and Y each denote a hydrogen, fluorine or chlorine atom or a hydroxyl, alkyl-C.sub.1 -C.sub.4, alkoxy-C.sub.1 -C.sub.4, carboxyl, carbalkoxy-C.sub.1 -C.sub.5, alkyl-C.sub.1 -C.sub.4 --CO--NH--, ##STR2## sulfonic acid, alkyl-C.sub.1 -C.sub.4 sulfonate, sulfamoyl, alkyl-C.sub.1 -C.sub.4 -sulfonyl, hydroxy-alkylene-C.sub.1 -C.sub.4 -sulfonyl, phenylsulfonyl, hydroxyphenylsulfonyl, alkyl-C.sub.1 -C.sub.4 -phenylsulfonyl or alkoxy-C.sub.1 -C.sub.4 -phenylsulfonyl group, wherein compounds of the formula (2) ##STR3## in which R.sub.1 denotes a nitro or primary amino group, and X and Y have the mentioned meanings, are reductively dialkylated using at least equimolar amounts of an aldehyde of the formula (3) ##STR4## in which R has the abovementioned meaning, in alcohols, alkylbenzenes, glycol ethers, fatty acid dialkylamides or fatty acid alkyl esters or fatty acid glycol esters, and using catalytically activated hydrogen in the presence of a precious metal catalyst of group 8 of the periodic table, if appropriate in the presence of catalytic amounts of a trialkyl-C.sub.1 -C.sub.6 -amine, at 50.degree. C. to 150.degree. C. at a pressure of 20 bar to 100 bar.
摘要翻译：制备式（1）的芳族二烷基胺的方法其中R表示烷基-C 1 -C 6基团，X和Y各自表示氢，氟或氯原子或羟基，烷基 - C 1 -C 4烷氧基-C 1 -C 4羧基烷氧基-C 1 -C 5烷基-C 1 -C 4 -CO-NH-， C 4磺酸盐，氨磺酰基，C 1 -C 4 - 磺酰基，羟基 - 亚烷基-C 1 -C 4 - 磺酰基，苯磺酰基，羟苯基磺酰基，烷基-C 1 -C 4 - 苯基磺酰基或烷氧基-C 1 -C 4苯基磺酰基，其中式（2）其中R1表示硝基或伯氨基，X和Y具有上述含义，使用至少等摩尔量的式（3）的醛进行还原性二烷基化。）其中R具有上述含义，在醇，烷基苯，乙二醇醚，脂肪酸二烷基酰胺或脂肪酸烷基酯或脂肪酸二醇酯中，并在催化活化氢存在下使用催化活化氢如果在催化量的三烷基-C 1 -C 6 - 胺的存在下，在50℃至150℃，在20巴至100巴的压力下，周期表第8族的贵金属催化剂。

100. 发明授权

US4755599A 3-phenyl-2-propeneamine derivatives, their preparation and composition containing them 失效
标题翻译： 3-苯基-2-丙烯胺衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US4755599A
公开(公告)日：1988-07-05
申请号：US10558
申请日：1987-02-03
申请人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
发明人： Jean-Claude Barriere , Jean-Pierre Corbet , Claude Cotrel , Daniel Farge , Jean-Marc Paris
IPC分类号： A61K31/135 , A61K31/10 , A61K31/137 , A61K31/21 , A61K31/22 , A61P25/24 , A61P25/26 , C07C67/00 , C07C213/00 , C07C213/02 , C07C215/28 , C07C215/30 , C07C215/42 , C07C219/22 , C07C219/32 , C07C239/00 , C07C271/20 , C07C313/00 , C07C317/28 , C07C317/36 , C07C319/20 , C07C323/27 , C07C323/32 , C07C323/65 , C07D207/08 , C07D213/38 , C07D213/70 , C07D295/084 , C07D295/092 , C07D307/32 , C07F9/40 , C07D279/04 , C07C149/24 , C07D205/04 , C07D223/04 , C07D275/02 , C07D277/04 , C07D401/06
CPC分类号： C07D207/08 , C07D213/38 , C07D213/70 , C07D295/092 , C07D307/32 , C07F9/4006
摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups,(ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring,it being understood that the alkyl radicals and alkyl parts contains 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.
摘要翻译：本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N，或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6 C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，且R7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环包含5或6个C，任选地连接到苯环，应理解烷基和烷基部分包含1至4 C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。这些化合物可用作抗抑郁药。

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