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71. 发明授权

US4824844A Saccharine salts of substituted amines, fungicidal compositions and use 失效
标题翻译：取代胺的糖精盐，杀真菌剂和用途
公开(公告)号：US4824844A
公开(公告)日：1989-04-25
申请号：US118109
申请日：1987-11-05
申请人： Joachim Weissmuller , Paul Reinecke , Gerd Hanssler
发明人： Joachim Weissmuller , Paul Reinecke , Gerd Hanssler
IPC分类号： A01N43/80 , C07D211/14 , C07D211/22 , C07D265/30 , C07D275/06 , C07D295/02 , C07D295/03 , C07D295/08 , C07D295/084 , A01N43/84 , C07D417/02
CPC分类号： C07D275/06 , C07D211/22 , C07D295/03 , C07D295/092
摘要： Fungicidally active saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted cyclohexyl, cyclohexenyl or phenyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 and R.sup.4 independently of one another represent alkyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms andn represents the number 0 or 1.
摘要翻译：其中A代表任意取代的环己基，环己烯基或苯基，R 1表示氢或烷基，R 2表示氢或烷基，R 3和R 4彼此独立地表示烷基或烷基，与它们所键合的氮原子一起表示任选取代的饱和杂环基团，其可含有其它杂原子，n表示数字0或1。

72. 发明授权

US4692469A Propylamine derivatives 失效
标题翻译：丙胺衍生物
公开(公告)号：US4692469A
公开(公告)日：1987-09-08
申请号：US848661
申请日：1986-04-04
申请人： Jeffrey W. H. Watthey
发明人： Jeffrey W. H. Watthey
IPC分类号： C07C227/08 , C07C227/16 , C07D295/084 , A61K31/135
CPC分类号： C07D295/092 , C07C227/08 , C07C227/16 , Y10S514/91
摘要： Disclosed are e.g. certain novel 2-benzyl-3-(substituted)-phenoxypropylamines, their methods of synthesis and pharmaceutical compositions. Said compounds are useful as potent and centrally active serotonin uptake inhibitors for the treatment of psychotropic disorders, particularly depression.
摘要翻译：例如，某些新的2-苄基-3-（取代的） - 苯氧基丙胺，其合成方法和药物组合物。所述化合物可用作治疗精神病症，特别是抑郁症的有效和中枢活性的5-羟色胺摄取抑制剂。

73. 发明授权

US4686309A 3-phenyl-2-propeneamine derivatives, their preparation and compositions 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：US4686309A
公开(公告)日：1987-08-11
申请号：US702088
申请日：1985-02-15
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 , C07C91/16 , C07C67/02 , C07D211/70
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 6C), 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 contain 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6C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，R 7 = 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，其环含有5或6个C，任选地连接到苯环，应理解烷基和烷基部分含有1至4个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。

74. 发明授权

US4602930A Phenylpropylammonium salts, as growth regulants 失效
标题翻译：苯丙基铵盐，作为生长调节剂
公开(公告)号：US4602930A
公开(公告)日：1986-07-29
申请号：US727131
申请日：1985-04-25
申请人： Ernst Buschmann , Bernd Zeeh , Johann Jung , Hubert Sauter
发明人： Ernst Buschmann , Bernd Zeeh , Johann Jung , Hubert Sauter
IPC分类号： C07D295/06 , A01N43/34 , A01N43/36 , A01N43/40 , A01N43/46 , C07D211/14 , C07D295/02 , C07D295/037 , C07D295/073 , C07D295/08 , C07D295/084 , C07D295/096 , C07D295/10 , C07D295/112 , A01N33/04 , C07D207/08
CPC分类号： C07D295/037 , A01N43/36 , A01N43/40 , A01N43/46 , C07D295/073 , C07D295/092 , C07D295/096 , C07D295/112
摘要： Phenylpropylammonium salts of the formula ##STR1## where R.sup.1 denotes for instance alkyl or halogen, R.sup.2 denotes for instance alkyl or alkoxy, R.sup.3 denotes alkyl, alkenyl or alkynyl of up to 6 carbon atoms, R.sup.4 and R.sup.5 denote hydrogen or alkyl of up to 3 carbon atoms, m denotes one of the integers 0, 1, 2 and 3, n denotes one of the integers 0, 1 and 2, o denotes one of the integers 4, 5 and 6, X.sup..theta. denotes an anion, and the dashed bond may be hydrogenated when n is 0 or 1, and is hydrogenated when n is 2; the preparation of these compounds; and agents for regulating plant growth containing these compounds as active ingredients.
摘要翻译：其中R1表示例如烷基或卤素，R2表示烷基或烷氧基，R3表示至多6个碳原子的烷基，烯基或炔基，R4和R5表示氢或最多3个的烷基，碳原子，m表示整数0,1,2和3中的一个，n表示整数0,1和2中的一个，o表示整数4,5和6中的一个，Xθ表示阴离子，虚线表示当n为0或1时，键可以被氢化，并且当n为2时被氢化; 这些化合物的制备; 以及用于调节含有这些化合物作为活性成分的植物生长的药剂。

75. 发明授权

US4588746A Propylamine derivatives 失效
公开(公告)号：US4588746A
公开(公告)日：1986-05-13
申请号：US568000
申请日：1984-01-04
申请人： Jeffrey W. H. Watthey
发明人： Jeffrey W. H. Watthey
IPC分类号： C07C227/08 , C07C227/16 , C07D295/084 , A61K31/185
CPC分类号： C07D295/092 , C07C227/08 , C07C227/16
摘要： Disclosed are e.g. certain novel 2-benzyl-3-(substituted)-phenoxypropylamines, their methods of synthesis and pharmaceutical compositions. Said compounds are useful as potent and centrally active serotonin uptake inhibitors for the treatment of psychotropic disorders, particularly depression.

76. 发明授权

US4495184A Morpholino propanol derivatives, fungicidal compositions and use 失效
标题翻译：吗啉代醇衍生物，杀真菌剂及用途
公开(公告)号：US4495184A
公开(公告)日：1985-01-22
申请号：US496673
申请日：1983-05-23
申请人： Hans-Joachim Knops , Wolfgang Kramer , Paul-Ernst Frohberger
发明人： Hans-Joachim Knops , Wolfgang Kramer , Paul-Ernst Frohberger
IPC分类号： C07D295/08 , A01N33/04 , A01N33/08 , A01N37/12 , A01N37/34 , A01N43/84 , A01N47/12 , A01N47/20 , A01N55/00 , A01N55/10 , C07C67/00 , C07C213/00 , C07C215/30 , C07C217/70 , C07C217/72 , C07C219/22 , C07C239/00 , C07C253/00 , C07C255/58 , C07C255/59 , C07C271/08 , C07C313/00 , C07C323/32 , C07D209/08 , C07D295/067 , C07D295/084 , C07F7/18
CPC分类号： C07D295/067 , A01N33/04 , A01N33/08 , A01N37/12 , A01N47/12 , A01N47/20 , A01N55/00 , C07D209/08 , C07D295/092 , C07F7/1856
摘要： A 1-phenyl-3-amino-propane derivative of the formula ##STR1## in which R.sup.1 and R.sup.2 independently represent alkyl radicals or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are bonded complete an optionally substituted heterocyclic radical of the formula ##STR2## and or additionally, if R.sup.4 represents the radical --O--CO--R.sup.5, --O--CO--NHR.sup.6 or --O--SiR.sub.3.sup.7, complete an optionally substituted heterocyclic radical of the formula ##STR3## R.sup.3 represents a hydrogen atom or an alkyl radical, R.sup.4 represents a hydroxyl group, halogen or the radical --O--CO--R.sup.5, --O--CO--NHR.sup.6 or --O--SiR.sub.3.sup.7,R.sup.5 represents an alkyl, alkenyl or halogenoalkyl radical or an optionally substituted aryl or aralkyl radical,R.sup.6 represents an alkyl or alkenyl radical or an optionally substituted aryl radical,R.sup.7 represents an alkyl radical each Y independently represents an alkyl radical, a halogen atom or a halogenoalkyl, alkoxy, alkylthio, halogenoalkoxy, halogenoalkylthio, cycloalkyl or cyano radical andn is 0, 1, 2 or 3,or a physiologically acceptable acid addition salt thereof which possesses fungicidal activity.
摘要翻译：其中R 1和R 2独立地表示烷基或R 1和R 2与它们所键合的氮原子一起形成的式“IMAGE”的1-苯基-3-氨基 - 丙烷衍生物与式或者另外，如果R 4代表基团-O-CO-R 5，-O-CO-NHR 6或-O-SiR 37，则完成式R 3的任选取代的杂环基代表氢原子或烷基基团，R 4表示羟基，卤素或-O-CO-R 5，-O-CO-NHR 6或-O-SiR 37基团，R 5表示烷基，烯基或卤代烷基或任选取代的芳基或芳烷基，R 6 表示烷基或烯基或任选取代的芳基，R 7表示烷基，每个Y独立地表示烷基，卤素原子或卤代烷基，烷氧基，烷硫基，卤代烷氧基，卤代烷硫基，环烷基或氰基，n为0， 1,2或3，或者一个生理学家其具有杀真菌活性的其可接受的酸加成盐。

77. 发明授权

US4476129A 4-[2-[Bis(halophenyl)methoxy]-ethyl]-.alpha.-(substituted phenyl)-1-piperazinealkanol derivatives, processes for their preparation and pharmaceutical preparations containing them 失效
标题翻译： 4- [2- [双（卤代苯基）甲氧基] - 乙基]-α-（取代苯基）-1-哌嗪烷醇衍生物，其制备方法和含有它们的药物制剂
公开(公告)号：US4476129A
公开(公告)日：1984-10-09
申请号：US509168
申请日：1983-06-29
申请人： Johan Gootjes , Hendricus H. van de Kamp
发明人： Johan Gootjes , Hendricus H. van de Kamp
IPC分类号： C07D295/08 , A61K31/495 , A61P1/08 , C07D295/084 , C07D295/10 , C07D295/108 , C07D241/04
CPC分类号： C07D295/108 , C07D295/092
摘要： The invention relates to new piperazine derivatives of the general formula ##STR1## in which R' and R.sup.2 each represents 1, 2 or 3 halogen atoms, which may be the same or different,R.sup.3 represents a hydrogen atom or 1, 2 or 3 halogen atoms, X represents a hydroxy, C.sub.1-4 alkoxy, phenylcarbamoyloxy or C.sub.1-4 alkylcarbamoyloxy group,Y represents a hydrogen atom or a C.sub.1-3 alkyl group, or X and Y together with the carbon atom to which they are linked represent a carbonyl group,m is 1, 2 or 3,n is 0 or 1, with the proviso that m+n is at most 3, and their acid addition and quaternary ammonium salts.Other features of the invention areprocesses for the preparation of compounds of formula I,pharmaceutical preparations comprising a compound of formula I.
摘要翻译：本发明涉及通式“IMAGE”I的新的哌嗪衍生物，其中R'和R 2各自表示1,2或3个可相同或不同的卤素原子，R 3表示氢原子或1,2或3 卤原子，X表示羟基，C 1-4烷氧基，苯基氨基甲酰氧基或C 1-4烷基氨基甲酰氧基，Y表示氢原子或C 1-3烷基，或X和Y与它们所连接的碳原子一起代表羰基，m为1,2或3，n为0或1，条件是m + n至多为3，以及它们的酸加成盐和季铵盐。本发明的其它特征是制备式I化合物的方法，包含式I化合物的药物制剂。

78. 发明授权

US4423045A Thiadizines 失效
公开(公告)号：US4423045A
公开(公告)日：1983-12-27
申请号：US321899
申请日：1981-11-16
申请人： David Brown , Robert I. Dowell , Rodney B. Hargreaves , Brian G. Main
发明人： David Brown , Robert I. Dowell , Rodney B. Hargreaves , Brian G. Main
IPC分类号： C07D417/04 , A61K31/53 , A61K31/535 , A61K31/54 , A61P9/04 , A61P9/08 , C07C327/38 , C07D253/06 , C07D273/04 , C07D285/16 , C07D285/18 , C07D295/084 , C07D295/194 , C07D317/00 , C07D417/02
CPC分类号： C07D253/06 , C07C255/00 , C07D273/04 , C07D285/16 , C07D295/092 , C07D295/194 , Y10S514/929
摘要： Novel heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is oxygen, sulphur or --NR.sup.3, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH.sub.2 --; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R.sup.4 and R.sup.5 are not both hydrogen; or wherein R.sup.4 and R.sup.5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate.These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.
摘要翻译：下式的新型杂环化合物：其中X为-CR 1 R 2 - 且Y为氧，硫或-NR 3，其中R 1，R 2和R 3可以相同或不同，各自为氢或直至 4个碳原子; 或X是氧，硫或-NH-，Y是-CH 2 - ; 其中R4和R5可以相同或不同，各自为氢，氰基，硝基，氨基或羟基或至多4个碳原子的烷硫基，或具有权利要求1中定义的各种其它含义，条件是R4和R5为不是氢; 或其中R4和R5连接在一起，使得与苯环A形成如权利要求1所定义的苯并杂环; 其中苯环A可任选地具有一个或多个其它取代基; 或其盐。这些化合物具有强心性质，其中一些具有外周血管扩张剂特性，可用于治疗急性或慢性心力衰竭。化合物的代表是N，N-二甲基 - 对 - （5,6-二氢-5-氧代-4H-1,3,4-噻二嗪-2-基）苯甲酰胺。还公开了制备含有它们的化合物和药物组合物的方法。

79. 发明授权

US4169200A Substituted 3,6-dihydro-1(2H)-pyridinylpropanols 失效
标题翻译：取代的3,6-二氢-1（2H） - 吡啶基丙醇
公开(公告)号：US4169200A
公开(公告)日：1979-09-25
申请号：US824378
申请日：1977-08-15
申请人： Frederic P. Hauck , Rita T. Fox , John R. Watrous
发明人： Frederic P. Hauck , Rita T. Fox , John R. Watrous
IPC分类号： C07D211/22 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/70 , C07D217/04 , C07D221/10 , C07D295/084 , C07D471/04 , C07D491/10 , C07D211/14 , C07D211/26
CPC分类号： C07D295/084 , C07D211/22 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/70 , C07D217/04 , C07D221/10 , C07D471/04 , C07D491/10
摘要： Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is ##STR2## AND N IS 0, 1 OR 2; HAVE USEFUL HYPOTENSIVE PROPERTIES.
摘要翻译：具有式“IMAGE”的化合物及其药学上可接受的盐，其中R 1是烷酰基; （i）（ii）（iii）（iv）（v）（vi）而N是0,1或2; 具有有用的HYPOTENSIVE属性。

80. 发明授权

US4157399A Benzo(B)thiophenes 失效
标题翻译：苯并（B）噻吩
公开(公告)号：US4157399A
公开(公告)日：1979-06-05
申请号：US857134
申请日：1977-12-05
申请人： Fritz Sauter
发明人： Fritz Sauter
IPC分类号： A61K31/38 , C07D295/084 , C07D295/185 , C07D333/64 , C07D333/66 , C07D409/04
CPC分类号： C07D295/185 , C07C323/00 , C07D295/092 , C07D333/64 , C07D333/66
摘要： The present invention relates to new derivatives of 2-phenyl -benzo(b)thiophene mono- or disubstituted on the nitrogen atom of formula ##STR1## in which X.sup.1 to X.sup.9 which are identical or different are hydrogen, alkyl having up to 3 carbon atoms, chlorine, bromine, methoxy or methylthio, R.sup.1 is hydrogen, alkyl having up to 8 carbon atoms, optionally chlorinated or methoxylated, phenyl optionally chlorinated or methoxylated, aralkyl having in all up to 9 carbon atoms, optionally chlorinated or methoxylated on the phenyl nucleus, R.sup.2 is hydrogen, phenyl,Or a radical of the formula ##STR2## in which A is two hydrogen atoms or one oxygen atom andR.sup.3 can assume the same meanings as given for R.sup.1, the meanings assumed by R.sup.1 and R.sup.3 being independent from one another, or R.sup.1 and R.sup.2 together form the radical of a Schiff base of formula.dbd.CH--R.sup.4 (III)in which R.sup.4 is not hydrogen, but can otherwise assume the same meanings as R.sup.3, or the group ##STR3## forms the radical of a heterocyclic secondary amine. The invention also relates to the acid addition salts of the above compounds, notably those which are pharmaceutically compatible. The compounds of formula I are useful in normalizing the blood lipid value.
摘要翻译：本发明涉及在式（I）的氮原子上单取代或二取代的2-苯基 - 苯并（b）噻吩的新衍生物，其中相同或不同的X 1至X 9为氢，烷基具有至多 3个碳原子，氯，溴，甲氧基或甲硫基，R1是氢，具有至多8个碳原子的烷基，任选被氯化或甲氧基化，任选被氯化或甲氧基化的苯基，具有全部高达9个碳原子的芳烷基，任选氯化或甲氧基化苯基核，R2是氢，苯基，其中A是两个氢原子或一个氧原子，R3可以表示与R1相同的含义，R1和R3假定为或者R 1和R 2一起形成其中R 4不是氢的式= CH-R 4（III）的席夫碱的基团，或者可以表示与R 3相同的含义，或者“IMAGE”形式杂环仲胺的基团。本发明还涉及上述化合物的酸加成盐，特别是与药学上相容的那些。式I的化合物可用于标准化血脂值。

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