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101. 发明授权

US5116827A Quinolinecarboxylic acid derivatives as solubilized pro-drugs 失效
标题翻译：喹啉羧酸衍生物作为溶解前体药物
公开(公告)号：US5116827A
公开(公告)日：1992-05-26
申请号：US671052
申请日：1991-03-18
申请人： Keith C. Murdock , Ving J. Lee
发明人： Keith C. Murdock , Ving J. Lee
IPC分类号： C07D233/52 , C07F9/6506 , C07F9/6558
CPC分类号： C07F9/65061 , C07D233/52 , C07F9/65583
摘要： The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.
摘要翻译：公开了产生具有增强的水溶性或脂溶性或毒性降低的前药的碱性含氮药物化合物的N-磷酸化。含有胺，脒，胍，异脲，异硫脲和双胍功能的药物可以转化成这种前药。前体药物在体内水解，释放磷酸盐后再生原药。

102. 发明授权

US5077282A Solubilized pro-drugs 失效
标题翻译：溶解的前药
公开(公告)号：US5077282A
公开(公告)日：1991-12-31
申请号：US671055
申请日：1991-03-18
申请人： Keith C. Murdock , Ving J. Lee
发明人： Keith C. Murdock , Ving J. Lee
IPC分类号： C07D233/52 , C07F9/6506 , C07F9/6558
CPC分类号： C07F9/65061 , C07D233/52 , C07F9/65583
摘要： The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.
摘要翻译：公开了产生具有增强的水溶性或脂溶性或毒性降低的前药的碱性含氮药物化合物的N-磷酸化。含有胺，脒，胍，异脲，异硫脲和双胍功能的药物可以转化成这种前药。前体药物在体内水解，释放磷酸盐后再生原药。

103. 发明授权

US5070082A Solubilized pro-drugs 失效
标题翻译：溶解的前药
公开(公告)号：US5070082A
公开(公告)日：1991-12-03
申请号：US671051
申请日：1991-03-18
申请人： Keith C. Murdock , Ving J. Lee
发明人： Keith C. Murdock , Ving J. Lee
IPC分类号： C07D233/52 , C07F9/6506 , C07F9/6558
CPC分类号： C07F9/65061 , C07D233/52 , C07F9/65583
摘要： The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guadinine, isourea, isothiourea an biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phsophoric acid.
摘要翻译：公开了产生具有增强的水溶性或脂溶性或毒性降低的前药的碱性含氮药物化合物的N-磷酸化。含有胺，脒，胍胺，异脲，异硫脲的药物可以转化为双胍类功能药物。前体药物在体内水解，再次释放原药，释放出盐酸盐。

104. 发明授权

US4880933A Nitro- or cyano-derivatives of 2-imino-imidazolines and 2-imino-tetrahydropyrimidines 失效
标题翻译： 2-亚氨基 - 咪唑啉和2-亚氨基 - 四氢嘧啶的硝基或氰基衍生物
公开(公告)号：US4880933A
公开(公告)日：1989-11-14
申请号：US130376
申请日：1987-12-08
申请人： Kozo Shiokawa , Shinichi Tsuboi , Koichi Moriya , Katsuhiko Shibuya
发明人： Kozo Shiokawa , Shinichi Tsuboi , Koichi Moriya , Katsuhiko Shibuya
IPC分类号： C07D233/44 , A01N43/00 , A01N43/50 , A01N43/54 , C07D213/61 , C07D233/48 , C07D233/52 , C07D239/16 , C07D239/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/06 , C07D417/06 , C07D417/14 , C07F9/6506 , C07F9/6558
CPC分类号： C07D401/04 , C07D233/48 , C07D233/52 , C07D239/16 , C07D239/18 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07F9/65061 , C07F9/65583
摘要： Novel intermediates for insecticides of the formula (I) ##STR1## wherein Y represents nitro or cyano;A represents an ethylene or trimethylene radical, which is optionally substituted; andZ can have many possible meanings.
摘要翻译：用于式（I）的杀虫剂的新型中间体其中Y表示硝基或氰基; A表示乙烯或三亚甲基，其任选被取代; Z可以有很多可能的含义。

105. 发明授权

US4647557A Novel heterocyclic derivatives bearing an amino radical, processes for their production and the pharmaceutical compositions containing them 失效
标题翻译：具有氨基的新型杂环衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4647557A
公开(公告)日：1987-03-03
申请号：US564918
申请日：1983-12-23
申请人： Gerard Moinet , Michel Schaeffer , Pierre Bessin , Jacqueline Bonnet
发明人： Gerard Moinet , Michel Schaeffer , Pierre Bessin , Jacqueline Bonnet
IPC分类号： A01N43/50 , A61K31/415 , A61P9/02 , A61P9/14 , C07C43/174 , C07D213/16 , C07D233/02 , C07D233/22 , C07D233/46 , C07D233/48 , C07D233/50 , C07D233/52 , C07D239/06 , C07D239/14 , C07D239/22 , C07D243/04 , C07D277/38 , C07D277/40 , C07D277/42 , C07D303/22 , C07D319/20 , C07D405/04 , C07D405/12 , C07D413/04 , A01N43/78 , C07D233/16 , C07D233/44
CPC分类号： C07D239/06 , C07C247/00 , C07C43/174 , C07D233/02 , C07D233/22 , C07D233/46 , C07D233/48 , C07D233/50 , C07D233/52 , C07D277/40 , C07D303/22 , C07D319/20 , C07D405/04 , C07D405/12
摘要： This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.
摘要翻译：本发明涉及具有氨基的新型杂环衍生物和制备所述化合物的方法。更具体地，本发明提供了杂环化合物，其杂环具有相同或不同的被游离或取代的氨基取代的两个杂原子。这些化合物可用作药物的活性成分。

106. 发明授权

US4574155A Process for preparing 2-hydrazino-1,3-diazacycloalk-2-ene hydrohalides 失效
标题翻译：制备2-肼基-1,3-二氮杂环戊烯-2-烯氢卤化物的方法
公开(公告)号：US4574155A
公开(公告)日：1986-03-04
申请号：US587414
申请日：1984-03-08
申请人： Thurairajah Padmanathan
发明人： Thurairajah Padmanathan
IPC分类号： C07D233/52 , C07D239/18 , C07D239/42 , C07D239/47 , C07D243/04 , C07D243/08 , C07D245/02 , C07D239/02
CPC分类号： C07D245/02 , C07D233/52 , C07D239/18 , C07D243/04
摘要： This invention provides a process for preparing a 2-hydrazino-1,3-diazacycloalk-2-ene hydrohalide. The process comprises reacting a one molar proportion of either tautomeric isomer of a 2-nitroamino-1,3-diazacycloalk-2-ene represented by the following formulas: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxyalkyl, phenyl, substituted phenyl, benzyl, or substituted benzyl, R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxyalkyl, hydroxyl, aryl, substituted aryl, aralkyl and substituted aralkyl, and n is an integer from 0 to 3 with about an equimolar proportion of an ammonium halide or hydrazonium halide, and about a 1 to 2 molar proportion of hydrazine hydrate in a composition selected from a C.sub.1 to C.sub.4 aliphatic alcohol, water or a mixture thereof, at a temperature from about ambient to the reflux, and isolating the end product as a monohydrohalide.This invention also provides a process for preparing a 2-hydrazino-1,3-diazacycloalk-2-ene dihydrohalide. The process comprises reacting a compound of the formula: ##STR2## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.6 alkyl, or C.sub.1 to C.sub.6 hydroxyalkyl, R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 to C.sub.6 alkyl, n is 0 to 3 and X is a halide ion, with hydrogen halide wherein the halide ion is the same as defined above in a C.sub.1 to C.sub.4 alkyl alcohol at about 0.degree. to 30.degree. C.; and recovering the corresponding 2-hydrazino-1,3-diazacycloalk-2-ene dihydrohalide.
摘要翻译：本发明提供了制备2-肼基-1,3-二氮杂环烷-2-烯氢卤化物的方法。该方法包括使一摩尔比例的由下式表示的2-硝基氨基-1,3-二氮杂环烯-2-烯的互变异构体：其中R 1是氢，C 1 -C 6烷基，C 1 -C 6羟烷基，C1-C6烷氧基烷基，苯基，取代的苯基，苄基或取代的苄基，R2和R3独立地是氢，C1-C6烷基，C1-C6烷氧基，C1-C6烷氧基烷基，羟基，芳基，取代的芳基，芳烷基和取代的芳烷基，并且n为0至3的整数，其中约等摩尔比例的卤化铵或卤化腙，以及约1至2摩尔比例的选自C1至C4脂族醇，水或混合物的组合物中的水合肼在约环境温度至回流温度下，分离作为单卤化氢的最终产物。本发明还提供了制备2-肼基-1,3-二氮杂环戊烯-2-烯二酸盐的方法。该方法包括使下式化合物：其中R 1为氢，C 1至C 6烷基或C 1至C 6羟基烷基，R 2和R 3独立地为氢或C 1至C 6烷基，n为0至3， X是卤化物离子，其中卤化物，其中卤素离子与上述定义相同，在C1至C4烷基醇中约0至30℃; 并回收相应的2-肼基-1,3-二氮杂环烯-2-烯二氢卤化物。

107. 发明授权

US4515954A Metal chelates of anthracene-9,10-bis-carbonylhydrazones 失效
标题翻译：蒽-9,10-双羰基腙的金属螯合物
公开(公告)号：US4515954A
公开(公告)日：1985-05-07
申请号：US500225
申请日：1983-06-06
申请人： Stanley A. Lang, Jr. , Keith C. Murdock
发明人： Stanley A. Lang, Jr. , Keith C. Murdock
IPC分类号： C07D233/52 , C07D233/06
CPC分类号： C07D233/52
摘要： This disclosure describes metal chelates of anthracene-9,10-bis-carbonylhydrazones and derivatives thereof useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the regression and/or palliation of leukemia and related cancers.
摘要翻译：本公开描述了用作抑制移植小鼠肿瘤生长和用于诱导白血病和相关癌症的消退和/或缓解的蒽-9,10-双羰基腙及其衍生物的金属螯合物。

108. 发明授权

US4311838A Tetrahydro-2-nitrimino-2H-1,3-thiazine 失效
标题翻译：四氢-2-硝基喹啉-2H-1,3-噻嗪
公开(公告)号：US4311838A
公开(公告)日：1982-01-19
申请号：US262014
申请日：1981-05-11
申请人： Royston H. Davis , John H. Davies
发明人： Royston H. Davis , John H. Davies
IPC分类号： A01N51/00 , C07D233/52 , C07D239/08 , C07D279/06
CPC分类号： C07D239/08 , A01N51/00 , C07D233/52 , C07D279/06
摘要： Tetrahydro-2-nitrimino-2H-1,3-thiazine, useful as an insecticide.
摘要翻译：四氢-2-硝基嘧啶-2H-1,3-噻嗪，可用作杀虫剂。

109. 发明授权

US4284642A 1,3-Diaryl-2-imino-imidazolidines and compositions thereof 失效
标题翻译： 1,3-二芳基-2-亚氨基咪唑啉及其组合物
公开(公告)号：US4284642A
公开(公告)日：1981-08-18
申请号：US30149
申请日：1979-04-16
申请人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
发明人： Lajos Toldy , Zoltan Zubovics , Mariann Kurti , Inge Schafer
IPC分类号： A61K31/415 , A61K31/505 , A61P7/10 , A61P29/00 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/10 , C07D239/14 , C07D239/18 , C07D247/02
CPC分类号： C07D239/18 , C07D233/46 , C07D233/48 , C07D233/52 , C07D233/88 , C07D239/14 , C07D247/02 , Y10S514/869
摘要： The invention relates to new compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.5 each represent a phenyl group, optionally substituted,R.sup.2 stands for hydrogen, formyl group, carboxy group, lower alkoxycarbonyl group, hydroxy-(lower)-alkoxycarbonyl group, or a lower alkyl group, optionally substituted,R.sup.3 and R.sup.4 each represent hydrogen atom or a lower alkyl group, with the proviso that when R.sup.1 and R.sup.5 each represent a phenyl group, R.sup.2 and R.sup.3 may not stand for hydrogen.These compounds possess valuable biological properties, and can be applied primarily as antiphlogistic or diuretic agents.
摘要翻译：本发明涉及通式（I）的新化合物，其中R 1和R 5各自表示苯基，任选被取代，R 2代表氢，甲酰基，羧基，低级烷氧基羰基，羟基 - （低级） - 烷氧基羰基或任选取代的低级烷基，R 3和R 4各自表示氢原子或低级烷基，条件是当R 1和R 5各自表示苯基时，R 2和R 3可以不表示氢。这些化合物具有宝贵的生物学特性，可以主要用作消炎或利尿剂。

110. 发明授权

US4258181A Substituted 9,10-anthracenebishydrazones 失效
标题翻译：取代9,10-蒽二腙
公开(公告)号：US4258181A
公开(公告)日：1981-03-24
申请号：US36924
申请日：1979-05-07
申请人： Keith C. Murdock , Frederick E. Durr
发明人： Keith C. Murdock , Frederick E. Durr
IPC分类号： C07C281/14 , A61K31/15 , A61K31/17 , A61K31/415 , A61K31/505 , A61K31/54 , A61P35/00 , C07C15/28 , C07C17/32 , C07C47/453 , C07C47/457 , C07C47/47 , C07C47/55 , C07C47/57 , C07C47/575 , C07C67/00 , C07C239/00 , C07C241/00 , C07C251/80 , C07C251/86 , C07C281/18 , C07C325/00 , C07C337/08 , C07D213/42 , C07D213/77 , C07D233/52 , C07D233/88 , C07D239/18 , C07D239/42 , C07D243/04 , C07D295/12 , C07D295/13 , C07D307/52 , C07D317/70 , C07D333/20 , C07C109/16
CPC分类号： C07D295/13 , C07C17/32 , C07C251/72 , C07C281/18 , C07C47/453 , C07C47/457 , C07C47/47 , C07C47/55 , C07C47/57 , C07C47/575 , C07D213/42 , C07D213/77 , C07D233/52 , C07D239/18 , C07D243/04 , C07D307/52 , C07D317/70 , C07D333/20 , C07C2103/24
摘要： This disclosure describes anthracene-9,10-bis-carbonyl-hydrazones and derivatives thereof useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the regression and/or palliation of leukemia and related cancers.
摘要翻译：本公开描述了用作抑制移植的小鼠肿瘤生长以及用于诱导白血病和相关癌症的消退和/或缓解的蒽-9,10-双羰基 - 腙及其衍生物。

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