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1. 发明授权

US4597902A N-(arylthioalkyl)-N'-(aminoalkyl)ureas 失效
标题翻译： N-（芳硫基烷基）-N' - （氨基烷基）脲
公开(公告)号：US4597902A
公开(公告)日：1986-07-01
申请号：US746740
申请日：1985-06-20
申请人： James R. Shanklin, Jr. , Christopher P. Johnson, III
发明人： James R. Shanklin, Jr. , Christopher P. Johnson, III
IPC分类号： A61K31/13 , C07C317/28 , C07C323/44 , C07C335/08 , C07D209/48 , C07D307/38 , C07C127/17 , A61K31/07 , C07C157/07
CPC分类号： C07D209/48 , C07C255/00 , C07C317/28 , C07C323/00 , C07C323/44 , C07C335/08 , C07D307/38 , C07C2101/14
摘要： N-(arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue.
摘要翻译： N-（芳硫基烷基）-N' - （氨基烷基）脲和硫脲和具有式“IMAGE”的氧化衍生物，其中B是硫代，亚磺酰基或磺酰基; R 1和R 2是氢，低级烷基，环烷基，2-呋喃基，苯基，取代的苯基或苯基 - 低级烷基，R 3和R 4是氢，低级烷基，苯基或苯基 - 低级烷基，其中苯基是任选取代的，或者R 3和R 4与相邻氮形成杂环残基。

2. 发明授权

US4579969A Substituted 1,3-dibenzylureas and herbicidal compositions containing them 失效
标题翻译：取代的1,3-二苄基脲和含有它们的除草组合物
公开(公告)号：US4579969A
公开(公告)日：1986-04-01
申请号：US687131
申请日：1984-12-28
申请人： Tetsuo Takematsu , Yasutomo Takeuchi , Michiyuki Kohno , Akihiko Aoki , Koichi Moriya
发明人： Tetsuo Takematsu , Yasutomo Takeuchi , Michiyuki Kohno , Akihiko Aoki , Koichi Moriya
IPC分类号： A01N47/28 , C07C275/24 , C07C127/17
CPC分类号： A01N47/28 , C07C275/24
摘要： Substituted 1,3-dibenzylureas are represented by the following general formula: ##STR1## wherein X is a chlorine atom, a bromine atom, an iodine atom, a trifluoromethyl group, a methyl group or a methoxy group. These compounds are used as a herbicidal composition comprising at least one of said compounds and a carrier, if desired, together with a suitable adjuvant.
摘要翻译：取代的1,3-二苄脲由以下通式表示：其中X是氯原子，溴原子，碘原子，三氟甲基，甲基或甲氧基。如果需要，这些化合物与合适的佐剂一起用作除草组合物，其包含至少一种所述化合物和载体。

3. 发明授权

US4317819A Amine derivatives 失效
标题翻译：胺衍生物
公开(公告)号：US4317819A
公开(公告)日：1982-03-02
申请号：US213680
申请日：1980-12-05
申请人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith
发明人： John W. Clitherow , Barry J. Price , John Bradshaw , Michael Martin-Smith
IPC分类号： A61K31/155 , A61K31/335 , A61K31/38 , A61P1/00 , C07C67/00 , C07C209/00 , C07C211/27 , C07C213/00 , C07C217/48 , C07C239/00 , C07C275/12 , C07C279/04 , C07C279/28 , C07C301/00 , C07C311/64 , C07C325/00 , C07C335/08 , C07D233/64 , C07D295/096 , C07D307/38 , C07D307/42 , C07D307/52 , C07D333/14 , A61K31/17 , C07C127/17 , C07C129/12
CPC分类号： C07D295/096 , C07C279/28 , C07D307/38 , C07D307/42 , C07D307/52 , C07D333/14 , Y10S514/886 , Y10S514/926 , Y10S514/927
摘要： The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 and Alk represents a straight chain alkylene group of 1 to 3 carbon atoms,andR.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichy represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -- group, x represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
摘要翻译：本发明提供了通式（I）的化合物及其生理上可接受的盐，水合物和生物前体，其中Y和Z可以相同或不同，各自表示氧，硫，= CHNO 2或= NR 3，其中R 3 是氢，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢，低级烷基，环烷基，低级烯基，芳烷基或被氧原子间隔的低级烷基或基团> N-R6，其中R 6表示氢或低级烷基，或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环，其中与分子的其余部分结合通过2和5位的键，或苯环，其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - ， - O-或-S-; n表示0或1; m表示2,3或4，Alk表示1〜3个碳原子的直链亚烷基，R2表示低级烷基或 - （CH2）yE（CH2）xG，y表示2,3或4或可以当E是-CH 2 - 基时，x代表0或1; E表示-CH 2 - ， - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环，或G表示基团，其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。式（I）化合物具有作为选择性组胺H2拮抗剂的药理学活性。

4. 发明授权

US4170657A Substituted(((phenyl)amino)carbonyl)-benzamides 失效
标题翻译：取代的（（（苯基）氨基）羰基） - 苯甲酰胺
公开(公告)号：US4170657A
公开(公告)日：1979-10-09
申请号：US796645
申请日：1977-05-13
申请人： Raymond H. Rigterink
发明人： Raymond H. Rigterink
IPC分类号： A01N47/34 , C07C275/54 , A01N9/12 , A01N9/20 , C07C127/17 , C07C127/22
CPC分类号： A01N47/34 , C07C275/54
摘要： Novel alkoxy or alkylthio substituted(((phenyl)amino)carbonyl)-benzamides are disclosed. The compounds of the instant invention are useful as insecticides and can be formulated to provide insecticidal compositions.
摘要翻译：公开了新的烷氧基或烷硫基取代的（（（苯基）氨基）羰基） - 苯甲酰胺。本发明的化合物可用作杀虫剂并且可配制成提供杀虫组合物。

5. 发明授权

US4145363A 4-Carbamoylamino-.alpha.-aminomethylbenzyl alcohol derivatives 失效
标题翻译： 4-氨基甲酰胺 - 氨基乙基苄醇衍生物
公开(公告)号：US4145363A
公开(公告)日：1979-03-20
申请号：US809998
申请日：1977-06-27
申请人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
发明人： Masuo Murakami , Kozo Takahashi , Kiyoshi Murase , Toshiyasu Mase , Hisashi Ida , Toichi Takenaka
IPC分类号： C07C275/40 , C07C127/17 , A61K31/17
CPC分类号： C07C275/40 , Y10S514/826
摘要： There are disclosed novel 4-substituted amino-.alpha.-aminomethylbenzyl alcohol derivatives represented by the formula: ##STR1## wherein X represents a halogen atom; Y represents a hydrogen atom or a halogen atom; R.sub.1 represents a lower alkyl group, a carbamoyl group, a mono- or di-lower alkyl-substituted carbamoyl group, a phenyl-substituted carbamoyl group, a lower alkoxycarbonyl group, a lower alkoxy-substituted lower alkoxycarbonyl group, a phenyl-substituted lower alkoxycarbonyl group, or a cycloalkyloxycarbonyl group; and R.sub.2 represents a lower alkyl group, a cycloalkyl group, or the group shown by the ##STR2## wherein R.sub.3 represents a hydrogen atom or a lower alkyl group and R.sub.4 represents a hydrogen atom, a hydroxy group, or a lower alkoxy group and the pharmaceutically acceptable nontoxic salts thereof. These compounds are antiasthmatic agents useful for the prophylaxis and treatment of asthma.

6. 发明授权

US4578513A Process for preparing phenylisopropylurea compounds 失效
标题翻译：制备苯基异丙脲化合物的方法
公开(公告)号：US4578513A
公开(公告)日：1986-03-25
申请号：US672038
申请日：1984-11-16
申请人： Balwant Singh , Paul S. Waterman
发明人： Balwant Singh , Paul S. Waterman
IPC分类号： C07B61/00 , B01J27/00 , C07C273/18 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/34 , C07C127/17
CPC分类号： C07C273/1854
摘要： A new and improved process for making phenylisopropylurea derivatives having the formula: ##STR1## wherein R.sup.1 is selected from hydrogen, halogen, alkyl, alkenyl, haloalkyl or R.sup.2 groups and R.sup.2 is selected from phenyl, alkyl-substituted phenyl alkoxy-substituted phenyl or haloalkyl-substituted phenyl is disclosed. The process comprises reacting a substituted urea of the formula: ##STR2## with an alkenyl aromatic compound of the formula: ##STR3## in a polar aprotic solvent, in the presence of an acid catalyst, preferably, sulfuric acid, substituted sulfonic acids or Lewis acids, and stirring the reaction mixture at a temperature of about 20.degree. to 80.degree. C. until formation of the precipitated phenylisopropylurea derivative is substantially complete.
摘要翻译：制备具有下式的苯基异丙基脲衍生物的新的和改进的方法：其中R1选自氢，卤素，烷基，烯基，卤代烷基或R2基团，R2选自苯基，烷基取代的苯基烷氧基取代的苯基或卤代烷基 - 取代的苯基。该方法包括在极性非质子溶剂中，在酸催化剂，优选硫酸，取代的磺酸或路易斯酸的存在下使下式的取代的脲与下式的链烯基芳族化合物反应：酸，并在约20℃至80℃的温度下搅拌反应混合物，直到形成沉淀的苯基异丙基脲衍生物基本上完成。

7. 发明授权

US4465509A Urea compounds and herbicidal compositions containing them 失效
标题翻译：尿素化合物和含有它们的除草组合物
公开(公告)号：US4465509A
公开(公告)日：1984-08-14
申请号：US424244
申请日：1982-09-27
申请人： Tetsuo Takematsu , Yasutomo Takeuchi , Michiyuki Kohno , Akihiko Aoki , Nobuo Aoki , Toshiro Watanuki , Koichi Moriya
发明人： Tetsuo Takematsu , Yasutomo Takeuchi , Michiyuki Kohno , Akihiko Aoki , Nobuo Aoki , Toshiro Watanuki , Koichi Moriya
IPC分类号： A01N47/28 , A01N9/20 , C07C127/17
CPC分类号： A01N47/28
摘要： Compound of the formula, ##STR1## wherein X is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxyl group, R.sup.1 is a methyl group or an ethyl group, R.sup.2 is a hydrogen atom, a lower alkyl group or an allyl group, and each of R.sup.3 and R.sup.4, independently, is a hydrogen atom, a methyl group or an ethyl group; provided that R.sup.1, R.sup.3 and R.sup.4 are not methyl groups simultaneously when both X and R.sup.2 are hydrogen atoms, and compositions containing these compounds exhibit herbicidal activity.
摘要翻译：下式的化合物，其中X是氢原子，卤素原子，低级烷基或低级烷氧基，R 1是甲基或乙基，R 2是氢原子，低级烷基或烯丙基，R 3和R 4各自独立地为氢原子，甲基或乙基; 条件是当X和R 2都是氢原子时，R 1，R 3和R 4不同时不是甲基，并且含有这些化合物的组合物表现出除草活性。

8. 发明授权

US4410697A Process for the preparation of N-aryl-N'-(mono- or di substituted)-urea derivatives 失效
标题翻译：制备N-芳基-N' - （单取代或二取代的） - 脲衍生物的方法
公开(公告)号：US4410697A
公开(公告)日：1983-10-18
申请号：US299030
申请日：1981-08-28
申请人： Sandor Torok , Lajos Voroshazy , Peter Galambos , Ivan Daroczi , Zoltan Ormenyi
发明人： Sandor Torok , Lajos Voroshazy , Peter Galambos , Ivan Daroczi , Zoltan Ormenyi
IPC分类号： C07C275/28 , C07C273/18 , C07C275/64 , C07D213/40 , C07D295/20 , C07D295/215 , C07C127/19 , C07C127/17
CPC分类号： C07D213/40 , C07C273/1836 , C07D295/215
摘要： The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, andR.sup.1 and R.sup.2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, orone of R.sup.1 and R.sup.2 may also stand for hydrogen,with the proviso that if one of R.sup.1 and R.sup.2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group,by reacting a carbamate of the general formula (II) with an amine of the general formula (III),R.sup.1 R.sup.2 N--CO--X (II)Aryl--NH.sub.2 (III)or a carbamate of the general formula (IV) with an amine of the general formula (V),Aryl--NH--CO--X (IV)R.sup.1 R.sup.2 NH (V)wherein R.sup.1, R.sup.2 and Aryl are as defined above and X is a lower alkoxy, phenoxy or substituted phenoxy group, in the presence of a tertiary amine catalyst. According to the invention a tertiary alkylamine containing altogether at least 6 carbon atoms and minimum one alkyl chain with at least 4 carbon atoms or a mixture of such tertiary alkylamines is applied as catalyst.
摘要翻译： PCT No.PCT / HU81 / 00003 Sec。 371日期1981年8月28日 102（e）日期1981年8月28日PCT提交1981年1月23日PCT公布。公开号WO81 / 02156 日本1981年8月6日。本发明涉及一种制备具有通式（I）的N-芳基-N' - （单或二取代） - 脲衍生物的新方法，其中芳基是任选取代的苯基，R 1和R 2各自代表任选取代的烷基，环烷基，烷氧基或苯基，或者R 1和R 2可以与相邻的氮原子一起形成含氮杂环基，另外的杂原子，或R 1和R 2中的一个也可以代表氢，条件是如果R 1和R 2中的一个是任选取代的苯基，另一个可以仅表示氢原子或任选取代的烷基或烷氧基，将通式（II）的氨基甲酸酯与通式（III）的胺，R1R2N-CO-X（Ⅱ）芳基-NH2（Ⅲ）或通式（Ⅳ）的氨基甲酸酯与通式（Ⅴ），芳基-NH-CO-X（Ⅳ）R1R2NH（Ⅴ）其中R1，R2和Aryl如上定义，X是低级烷氧基，苯氧基或取代的苯氧基，在叔胺催化剂存在下。根据本发明，将总共含有至少6个碳原子的叔烷基胺和具有至少4个碳原子的最小一个烷基链或这种叔烷基胺的混合物作为催化剂。

9. 发明授权

US4399076A 1,1-Disubstituted 2-vinyl- and 2-ethylcyclopropanes 失效
标题翻译： 1,1-二取代的2-乙烯基和2-乙基环丙烷
公开(公告)号：US4399076A
公开(公告)日：1983-08-16
申请号：US350669
申请日：1982-02-22
申请人： Richard G. Fayter, Jr. , Allen L. Hall
发明人： Richard G. Fayter, Jr. , Allen L. Hall
IPC分类号： C07C255/45 , C07C121/75 , C07C87/28 , C07C125/063 , C07C127/17
CPC分类号： C07C255/00
摘要： 2-Vinyl- and 2-ethylcyclopropanes having an aryl group and a nitrogen-containing radical substituted at the 1-position on the ring are provided. The novel 1,1-disubstituted 2-vinylcyclopropane and 2-ethylcyclopropane compounds of this invention have utility in herbicidal applications and are useful reactants. The 2-vinylcyclopropane derivatives are useful monomers for anionic and radical polymerizations.
摘要翻译：提供了具有在环上1位置被取代的芳基和含氮基团的2-乙烯基和2-乙基环丙烷。本发明的新型1,1-二取代的2-乙烯基环丙烷和2-乙基环丙烷化合物在除草应用中具有实用性，并且是有用的反应物。 2-乙烯基环丙烷衍生物是用于阴离子和自由基聚合的有用单体。

10. 发明授权

US4384140A 2-Chloroethyl urea derivatives 失效
标题翻译： 2-氯乙基脲衍生物
公开(公告)号：US4384140A
公开(公告)日：1983-05-17
申请号：US348724
申请日：1982-02-16
申请人： Peter Bregnedal , Jorn L. M. Buus
发明人： Peter Bregnedal , Jorn L. M. Buus
IPC分类号： A61K31/17 , A61K31/275 , A61K31/40 , A61P35/00 , C07C67/00 , C07C239/00 , C07C275/68 , C07C127/17
CPC分类号： C07C275/68
摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。本发明的新化合物可以由下式表示：其中X和Y相同或不同，并且选自苯基和环己基，所述苯基和环己基任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代，一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

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