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61. 发明授权

US4965368A 5-oxy or thiomethyl substituted oxazolidine herbicide antidotes 失效
标题翻译： 5-氧基或硫代甲基取代的恶唑烷除草剂解毒剂
公开(公告)号：US4965368A
公开(公告)日：1990-10-23
申请号：US53881
申请日：1987-05-26
申请人： Eugene G. Teach
发明人： Eugene G. Teach
IPC分类号： A01N25/32 , C07C323/25 , C07D263/04 , C07D263/06 , C07D303/34
CPC分类号： C07D263/04 , A01N25/32 , C07C323/00 , C07C323/25 , C07D263/06 , C07D303/34
摘要： N-haloacyl oxazolidines substituted in the 5-position with oxy or thio containing groups as new compositions of matter useful as active herbicidal antidotes to protect against and decrease crop injury when used with thiolcarbamate herbicides, and when applied in various methods; improved herbicidal compositions and utility of said compositions to protect against and decrease phytotoxic injury to crops when employing thiolcarbamate herbicides and a two-part herbicide system consisting essentially of a first-part of one or more thiolcarbamate herbicides and a second part of an effective antidote compound therefor, said antidote compounds of the class 3-haloacyl oxazolidine having the formula ##STR1## wherein X is selected from the group consisting of oxygen and sulfur; R.sub.1 is selected from the group consisting of alkyl and alkenyl; R is selected from the group consisting of haloalkyl, alkylthio and p-tolylsulfonamido; R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen and lower alkyl, each having 1 to 3 carbon atoms, inclusive; provided that the carbon content of R.sub.1 +R is less than or equal to 6 carbon atoms and further provided that when XR.sub.1 is alkylthio, then R is other than haloalkyl having 3 to 4 carbon atoms, inclusive, and provided that when XR.sub.1 is methoxy, R is other than 2,3-dibromopropyl; and in addition a compound selected from the group of compounds consisting of 2,2-dimethyl-3(3-bromopropionyl)5-pentoxymethyl oxazolidine; 2,2-dimethyl-3(5-chlorovaleryl)5-isopropoxymethyl oxazolidine; 2,2-dimethyl-3(5-chlorovaleryl)5-allyloxymethyl oxazolidine.
摘要翻译：在5-位上用氧基或硫基取代的N-卤代酰基恶唑啉作为新的有用的除草剂的组合物，用于在与硫代氨基甲酸酯除草剂一起使用时防止和减少作物损伤，以及以各种方法施用时; 改进的除草组合物和所述组合物在使用硫代氨基甲酸酯除草剂时防止和减少对作物的植物毒性损伤的效用以及基本上由一种或多种硫代氨基甲酸酯除草剂的第一部分组成的两部分除草剂系统和第二部分有效解毒剂化合物因此，所述具有式“IMAGE”的3-卤代酰基恶唑烷类的解毒剂化合物，其中X选自氧和硫; R1选自烷基和烯基; R选自卤代烷基，烷硫基和对甲苯磺酰氨基; R2和R3独立地选自氢和低级烷基，每个具有1至3个碳原子; 条件是R1 + R的碳含量小于或等于6个碳原子，并且进一步规定，当XR1为烷硫基时，R不为具有3至4个碳原子的卤代烷基，并且条件是当XR1为甲氧基时， R不是2,3-二溴丙基; 以及选自由2,2-二甲基-3（3-溴丙酰基）-5-戊氧基甲基恶唑烷组成的化合物组的化合物; 2,2-二甲基-3（5-氯戊酰基）-5-异丙氧基甲基恶唑烷; 2,2-二甲基-3（5-氯戊酰基）-5-烯丙氧基甲基恶唑烷。

62. 发明授权

US4931591A Novel 5-amino-4-hydroxyvaleryl derivatives 失效
标题翻译：新型5-氨基-4-羟基戊酰基衍生物
公开(公告)号：US4931591A
公开(公告)日：1990-06-05
申请号：US380711
申请日：1989-07-12
申请人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschl
发明人： Peter Buhlmayer , Vittorio Rasetti , Walter Fuhrer , James L. Stanton , Richard Goschl
IPC分类号： A61K38/00 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D233/54 , C07D233/64 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/18 , C07K5/02 , C07K5/078
CPC分类号： C07D233/64 , C07C53/136 , C07C57/58 , C07C59/48 , C07C59/68 , C07C59/84 , C07D209/16 , C07D209/42 , C07D209/52 , C07D215/48 , C07D263/04 , C07D263/06 , C07D295/13 , C07D307/81 , C07D401/12 , C07D403/12 , C07D405/12 , C07F7/1852 , C07F7/1856 , C07K5/0207 , C07K5/06139 , A61K38/00 , Y10S530/86
摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, A represents an optionally N-alkylated .alpha.-amino acid residue which is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as antihypertensives.

63. 发明授权

US4851387A 5-substituted amino-4-hydroxy-pentanoic acid derivatives and their use 失效
标题翻译： 5-取代的氨基-4-羟基 - 戊酸衍生物及其用途
公开(公告)号：US4851387A
公开(公告)日：1989-07-25
申请号：US106804
申请日：1987-10-13
申请人： Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Hajime Morishima , Kenji Matsuyama
发明人： Yutaka Koike , Masato Nakano , Shugo Atsuumi , Seiichi Tanaka , Hajime Morishima , Kenji Matsuyama
IPC分类号： A61K38/00 , C07D263/04 , C07D263/06 , C07D413/14 , C07K5/02
CPC分类号： C07D263/04 , C07D263/06 , C07D413/14 , C07K5/0207 , C07K5/0227 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： A 5-substituted amino-4-hydroxy-pentanoic acid derivative having the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an N-protecting group, R.sup.2, R.sup.3 and R.sup.5 may be any of a variety of groups including the side chains of amino acid residues, R.sup.4 is a hydrogen atom or a lower alkyl group, R.sup.6 is a group which is substituted by one or two hydroxyl groups, and R.sup.7 is any of a variety of groups, including a hydroxyl group, which compounds are renin inhibitors useful as hypotensive drugs, are disclosed.
摘要翻译：具有下式的5-取代的氨基-4-羟基 - 戊酸衍生物：其中R 1是氢原子或N-保护基，R 2，R 3和R 5可以是任何一种的包括氨基酸残基的侧链的基团，R4是氢原子或低级烷基，R6是被一个或两个羟基取代的基团，并且R7是包括羟基的任何基团，这些化合物是可用作降压药物的肾素抑制剂。

64. 发明授权

US4670593A Haloacetamidines and the herbicidal use thereof 失效
标题翻译：卤乙酰胺及其除草用途
公开(公告)号：US4670593A
公开(公告)日：1987-06-02
申请号：US668122
申请日：1984-11-05
申请人： Eugene G. Teach
发明人： Eugene G. Teach
IPC分类号： C07C259/14 , C07C275/40 , C07C275/56 , C07D263/04 , C07D277/04 , C07D295/195 , C07C123/00
CPC分类号： C07D263/04 , C07C259/14 , C07C275/40 , C07C275/56 , C07D277/04 , C07D295/195
摘要： Dichloroacetamidines having the formula ##STR1## in which A and B are independently selected from hydrogen, fluorine, chlorine, bromine and methyl, provided that at least one of A or B is other than hydrogen;M is hydrogen or methyl;X is selected from the group consisting of trifluoromethyl, lower alkyl, nitro, chloro, bromo, fluoro, cyano, lower alkoxy acetyl, lower alkylthio, trifluoromethylthio, and 3,3-diloweralkyl ureido;Y is selected from the group consisting of hydrogen, lower alkyl, chloro, fluoro, nitro, trifluoromethyl, and lower alkoxy;Z is selected from the group consisting of hydrogen and chloro;R.sub.1 is selected from the group consisting of hydrogen, alkyl and allyl;R.sub.2 is selected from the group consisting of alkyl, allyl, benzyl, hydroxyalkyl, alkynyl, N-alkyl amido, alkoxyalkyl, dialkoxyalkyl, alkoxy, cyano alkyl, substituted phenyl wherein the substituent is selected from the group trifluoromethyl, dichloro and 3,3-dimethylureido; andR.sub.1 and R.sub.2 taken together with the nitrogen is selected from the group consisting of alkyl substituted oxazolidyl, morpholinyl, piperidinyl and pyrrolidinyl; and salts thereof; useful as herbicides.
摘要翻译：具有式“IMAGE”的二氯乙酰胺，其中A和B独立地选自氢，氟，氯，溴和甲基，条件是A或B中的至少一个不是氢; M是氢或甲基; X选自三氟甲基，低级烷基，硝基，氯，溴，氟，氰基，低级烷氧基乙酰基，低级烷硫基，三氟甲硫基和3,3-二低级烷基脲基; Y选自氢，低级烷基，氯，氟，硝基，三氟甲基和低级烷氧基; Z选自氢和氯; R1选自氢，烷基和烯丙基; R 2选自烷基，烯丙基，苄基，羟基烷基，炔基，N-烷基酰胺基，烷氧基烷基，二烷氧基烷基，烷氧基，氰基烷基，取代的苯基，其中取代基选自三氟甲基，二氯和3,3- 二甲基脲基; 并且R 1和R 2与氮一起选自烷基取代的恶唑烷基，吗啉基，哌啶基和吡咯烷基; 及其盐; 用作除草剂。

65. 发明授权

US4517012A Herbicide compositions 失效
标题翻译：除草剂组合物
公开(公告)号：US4517012A
公开(公告)日：1985-05-14
申请号：US363673
申请日：1982-03-30
申请人： Ferenc M. Pallos , Mervin E. Brokke , Duane R. Arneklev
发明人： Ferenc M. Pallos , Mervin E. Brokke , Duane R. Arneklev
IPC分类号： A01N43/40 , C07D209/08 , C07D209/48 , C07D261/14 , C07D263/04 , C07D277/18 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/12 , C07D307/14 , C07D307/52 , C07D307/68 , A01N37/00
CPC分类号： C07D263/04 , C07C243/00 , C07D209/08 , C07D209/48 , C07D261/14 , C07D277/18 , C07D285/135 , C07D295/185 , C07D307/12 , C07D307/14 , C07D307/52 , C07D307/68
摘要： Herbicidal compositions comprising an active thiolcarbamate herbicide and a haloacetamide compound as antidote therefore having the formula ##STR1## wherein R is C.sub.1 -C.sub.6 haloalkyl and R.sub.1 and R.sub.2 taken together form a structure selected from piperidinyl, alkylpiperidinyl and alkyltetrahydropyridyl.
摘要翻译：因此除草剂组合物包含活性硫代氨基甲酸酯除草剂和卤代乙酰胺化合物作为解毒剂，因此具有式“IMAGE”，其中R为C1-C6卤代烷基，R1和R2一起形成选自哌啶基，烷基哌啶基和烷基四氢吡啶基的结构。

66. 发明授权

US4415353A Herbicide compositions 失效
标题翻译：除草剂组合物
公开(公告)号：US4415353A
公开(公告)日：1983-11-15
申请号：US441963
申请日：1982-11-15
申请人： Ferenc M. Pallos , Mervin E. Brokke , Duane R. Arneklev
发明人： Ferenc M. Pallos , Mervin E. Brokke , Duane R. Arneklev
IPC分类号： A01N37/30 , A01N37/36 , A01N43/04 , A01N47/40 , A01N53/12 , C07D209/08 , C07D209/48 , C07D261/14 , C07D263/04 , C07D277/18 , C07D285/12 , C07D285/135 , C07D295/185 , C07D307/12 , C07D307/14 , C07D307/52 , C07D307/68 , A01N37/00 , A01N37/18
CPC分类号： C07D263/04 , C07C243/00 , C07D209/08 , C07D209/48 , C07D261/14 , C07D277/18 , C07D285/135 , C07D295/185 , C07D307/12 , C07D307/14 , C07D307/52 , C07D307/68
摘要： Herbicidal compositions comprising an active thiolcarbamate herbicide and an amide of dichloroacetic acid antidote therefor and the methods of use of such herbicidal compositions are described herein.
摘要翻译：本文描述了包含活性硫代氨基甲酸酯除草剂和二氯乙酸解毒剂的酰胺的除草组合物以及这种除草组合物的使用方法。

67. 发明授权

US4347176A Compounds and methods of making same 失效
标题翻译：化合物及其制备方法
公开(公告)号：US4347176A
公开(公告)日：1982-08-31
申请号：US140157
申请日：1980-04-14
申请人： Nariman B. Mehta
发明人： Nariman B. Mehta
IPC分类号： A61K31/135 , A61K31/165 , A61K31/195 , A61K31/22 , A61K47/48 , A61K51/04 , C07C45/00 , C07C45/54 , C07C45/56 , C07C67/00 , C07C225/16 , C07C231/00 , C07C235/08 , C07C239/00 , C07C251/58 , C07D263/04 , C07D263/10 , C07K19/00 , C07G7/00 , C07C69/527 , C07C101/30 , G01N33/54
CPC分类号： C07D263/10 , A61K47/4833 , A61K51/0406 , C07C255/00 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04 , Y10S436/804 , Y10S436/822 , Y10S530/806
摘要： A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n --0--(CO).sub.m --(CH.sub.2).sub.p --COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N--0--(CH.sub.2).sub.q --COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, orR' is hydrogen and either(a) R.sub.3 is H and R.sub.4 is Cl and R.sub.5 is NO(CH.sub.2).sub.q CO--X where q is as defined for formula I and X is a group having formula III ##STR3## wherein R.sub.6 is a suitable radioisotope as described above, R.sub.7 is hydroxyl, and s is an integer from 1 to 4;(b) R.sub.4 is Cl, R.sub.5 is oxygen, and R.sub.3 is (CH.sub.2).sub.n --0--(CO).sub.m --(CH.sub.2).sub.p --CO--X where n, m, and p are as defined for formula I and X is as defined above; or(c) R.sub.3 is hydroxy, R.sub.5 is oxygen and R.sub.4 is a suitable radioisotope as defined above.The measure of radioactivity of the antisera bound radiolabeled competitor provides a measure of the amount of drug in the assayed biological fluid sample. A standard curve can be constructed from which the amount of drug in the assay sample can be interpolated. A kit is disclosed for practicing the radioimmunoassay.
摘要翻译：已经发现了用于生物液体中的安非他酮[（+/-） - 2-叔丁基氨基-3-氯苯丙酮]（一种抗抑郁药）的放射免疫测定方法。新的式（IMAGE）化合物，其中R2是氧，R1是（CH2）n-O-（CO）m-（CH2）p-COOH，其中n是0-5的整数，m是0或1， p是1至4的整数; 或R1是氢，R2是N-O-（CH2）q-COOH，其中q是1至3的整数，并且公开了制备它们的新方法和可用于其中的新的中间体。公开了用于提高安非他酮特异性抗血清的新型免疫原及其制备方法，其包括新化合物和合适的载体材料的缀合物。将药物与新的放射性标记的式（IMAGE）竞争剂一起加入到抗血清中，其中R'是如上所述的合适的放射性同位素，R 3是氢，R 4是Cl，R 5是氧，或者R'是氢，）R3是H，R4是Cl，R5是NO（CH2）qCO-X，其中q如式I所定义，X是具有式III的基团，其中R6是如上所述的合适的放射性同位素，R7是羟基，s为1至4的整数; （b）R4是Cl，R5是氧，R3是（CH2）n-O-（CO）m-（CH2）p-CO-X，其中n，m和p如式I所定义，X是如上所述; 或（c）R3是羟基，R5是氧，R4是如上定义的合适的放射性同位素。抗血清结合的放射性标记的竞争者的放射性测量值提供测定的生物流体样品中药物的量的量度。可以构建标准曲线，由此可以插入测定样品中的药物量。公开了用于实施放射免疫测定的试剂盒。

68. 发明授权

US4278799A Continuous process for the production of dichloroacetamides 失效
标题翻译：连续生产二氯乙酰胺的方法
公开(公告)号：US4278799A
公开(公告)日：1981-07-14
申请号：US144500
申请日：1980-04-28
申请人： Alan H. Benke , Hue T. Morris , Louie A. Nady
发明人： Alan H. Benke , Hue T. Morris , Louie A. Nady
IPC分类号： C07D263/04 , C07C102/00
CPC分类号： C07D263/04
摘要： Dichloroacetylamides selected from the group consisting of:(a) N,N-diallyldichloroacetamide, and(b) N-dichloroacetyl oxazolidines having the formula ##STR1## in which R is hydrogen or C.sub.1 -C.sub.3 alkyl are produced in a continuous circulating process by reaction of dichloroacetyl chloride with respectively N,N-diallylamine or an oxazolidine having the formula ##STR2## in the presence of an aqueous solution of sodium hydroxide. The conduct of this process in a continuous circulating fashion produces the desired amide in greater yield than by the heretofore practiced batch processes.
摘要翻译：选自以下的二氯乙酰胺：（a）N，N-二烯丙基二氯乙酰胺和（b）具有式“IMAGE”的N-二氯乙酰基恶唑烷，其中R是氢或C 1 -C 3烷基，是在连续循环过程中通过反应的二氯乙酰氯与分别具有式“IMAGE”的N，N-二烯丙基胺或恶唑烷在氢氧化钠水溶液的存在下反应。以连续循环方式进行该方法以比迄今为止实施的批次方法更有效地产生所需的酰胺。

69. 发明授权

US4275198A Method for preparing basic dithienyl compounds 失效
标题翻译：碱性二噻吩基化合物的制备方法
公开(公告)号：US4275198A
公开(公告)日：1981-06-23
申请号：US170028
申请日：1980-07-18
申请人： Frank J. Stiefel
发明人： Frank J. Stiefel
IPC分类号： C07D263/04 , C07D333/20 , C07D409/14 , C07D409/06
CPC分类号： C07D263/04 , C07D333/20
摘要： Basic dithienyl compounds are prepared by hydrolysis of a compound of the formula ##STR1## wherein R is hydrogen or lower alkyl.
摘要翻译：碱式二噻吩基化合物是通过水解式（Ⅰ）化合物而制备的，其中R是氢或低级烷基。

70. 发明授权

US4201873A 9-Deoxy-9,10-didehydro-PGD.sub.2 analogs 失效
标题翻译： 9-脱氧-9,10-二脱氢-PGD2类似物
公开(公告)号：US4201873A
公开(公告)日：1980-05-06
申请号：US614244
申请日：1975-09-17
申请人： David C. Peterson
发明人： David C. Peterson
IPC分类号： C07C53/21 , C07C405/00 , C07D263/04 , C07D307/24 , C07D307/935 , C07D309/12 , C07D313/06 , C07D319/06 , C07D339/06 , C07F9/40 , C07C177/00
CPC分类号： C07D263/04 , C07C405/00 , C07C405/0025 , C07C53/21 , C07D307/24 , C07D307/935 , C07D309/12 , C07D313/06 , C07D319/06 , C07D339/06 , C07F9/4006
摘要： Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.
摘要翻译：具有以下环戊烷环结构的前列腺素类似物：与其制备中可用的中间体一起被公开，其制备方法和制备方法被公开。这些类似物对于一些与前列腺素相同的药理学目的是有用的，特别是特别是作为血小板聚集抑制剂。

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