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71. 发明授权

US4973592A 1,3-diazocycloalkenes as muscarinic receptor blocking agents 失效
标题翻译： 1,3-二氮杂环烯烃作为毒蕈碱受体阻断剂
公开(公告)号：US4973592A
公开(公告)日：1990-11-27
申请号：US243942
申请日：1988-09-13
申请人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
发明人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
IPC分类号： C07D233/14 , A61K31/415 , A61K31/4166 , A61K31/505 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/12 , A61P35/00 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/18 , C07D233/22 , C07D233/26 , C07D233/32 , C07D233/46 , C07D233/48 , C07D233/52 , C07D239/06 , C07D239/08 , C07D239/24 , C07D243/04
CPC分类号： C07D239/06 , C07D233/48 , C07D239/24
摘要： New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.

72. 发明授权

US4900838A Acylation products of bis(2-imidazolin-2-ylhydrazones) of 9,10-anthracenedicarboxaldehyde 失效
标题翻译： 9,10-蒽二甲醛的双（2-咪唑啉-2-基腙）酰化产物
公开(公告)号：US4900838A
公开(公告)日：1990-02-13
申请号：US247989
申请日：1988-09-22
申请人： Keith C. Murdock
发明人： Keith C. Murdock
IPC分类号： C07D233/52 , C07F9/6506 , C07F9/6558
CPC分类号： C07F9/65583 , C07D233/52 , C07F9/65061
摘要： N-acylated derivatives of bis(2-imidazolin-2-ylhydrazones) of 9,10-anthracenedicarboxaldehyde, useful as anti-cancer agents against certain strains in mice, are disclosed and described, including processes for manufacture and use.
摘要翻译：公开和描述了用作抗小鼠中某些菌株的抗癌剂的9,10-蒽二甲醛的双（2-咪唑啉-2-基腙）的N-酰化衍生物，包括制备和使用方法。

73. 发明授权

US4845106A Heterocyclic thiazole compounds 失效
标题翻译：杂环噻唑化合物
公开(公告)号：US4845106A
公开(公告)日：1989-07-04
申请号：US68991
申请日：1987-07-01
申请人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
发明人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
IPC分类号： A01N43/78 , A01N20060101 , A01N33/18 , A01N43/00 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/647 , A01N43/653 , A01N43/66 , A01N43/72 , A01N43/74 , A01N43/76 , A01N43/80 , A01N43/82 , A01N43/84 , A01N43/86 , A01N43/88 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D20060101 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D213/00 , C07D213/61 , C07D233/20 , C07D233/52 , C07D239/06 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/00 , C07D277/10 , C07D277/18 , C07D279/00 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D419/06 , C07F9/6558
CPC分类号： C07D239/06 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/86 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D233/20 , C07D233/52 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/10 , C07D277/18 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07F9/65583
摘要： Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
摘要翻译：式中，n为0或1的新型杀虫剂，其中X为S，O，Y为N或Z为5或6元含氮杂环，R为 R9各自表示氢或特定的有机基团。

74. 发明授权

US4789681A Cytoprotective guanidine derivatives useful in ischemic diseases 失效
标题翻译：用于缺血性疾病的细胞保护胍衍生物
公开(公告)号：US4789681A
公开(公告)日：1988-12-06
申请号：US944949
申请日：1986-12-22
申请人： Giancarlo Sportoletti , Pietro Cremonesi , Moniquet Sarret
发明人： Giancarlo Sportoletti , Pietro Cremonesi , Moniquet Sarret
IPC分类号： A61K31/195 , A61K31/215 , A61K31/22 , A61K31/33 , A61K31/415 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , C07C67/00 , C07C239/00 , C07C279/14 , C07D233/44 , C07D233/52 , C07D233/88
CPC分类号： C07D233/88
摘要： Compounds of the general formula I ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 and R.sub.3, which are the same or different, represent hydrogen or methyl, or taken together, form the amidine system to which an imidazole or imidazoline ring is bound;R.sub.4 is a linear or branched C.sub.1 -C.sub.10 alkyl group; cycloalkyl, aryl, aralkyl or hetaryl group;R.sub.5 is hydrogen or methyl;A is a propylene chain optionally substituted by one or two methyl groups in one or more of the positions thereof; a chain of formula --HN--CH.sub.2 --CH.sub.2 -- or of formula --N.dbd.CH--CH.sub.2 --; a 1,4-cyclohexylene group optionally substituted by one or more methyl groups; a 1,4- phenylene group optionally substituted by one or more halogen atoms, alkyl groups or C.sub.1 -C.sub.4 alkoxy group with the proviso that, when R.sub.4 is methyl or ethyl and R.sub.1 =R.sub.2 =R.sub.3 =R.sub.5 are hydrogen, A is different from an unsubstituted propylene chain, are therapeutically useful as antilischemic, cytoprotective and cardioprotective agents.
摘要翻译：通式I的化合物（Ⅰ）其中R1是氢或甲基; R2和R3相同或不同，表示氢或甲基，或一起形成咪唑或咪唑啉环结合的脒体系; R4是直链或支链C1-C10烷基; 环烷基，芳基，芳烷基或杂芳基; R5是氢或甲基; A是在其一个或多个位置中任选被一个或两个甲基取代的丙烯链; 式-HN-CH2-CH2-或式-N = CH-CH2-的链; 任选被一个或多个甲基取代的1,4-亚环己基; 任选被一个或多个卤素原子，烷基或C 1 -C 4烷氧基取代的1,4-亚苯基，条件是当R 4为甲基或乙基且R 1 = R 2 = R 3 = R 5为氢时，A不同于未取代的丙烯链可用作抗缺血，细胞保护和心脏保护剂。

75. 发明授权

US4742060A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4742060A
公开(公告)日：1988-05-03
申请号：US821621
申请日：1986-01-21
申请人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
发明人： Kozo Shiokawa , Shinichi Tsuboi , Shinzo Kagabu , Koichi Moriya
IPC分类号： A01N43/78 , A01N20060101 , A01N33/18 , A01N43/00 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/647 , A01N43/653 , A01N43/66 , A01N43/72 , A01N43/74 , A01N43/76 , A01N43/80 , A01N43/82 , A01N43/84 , A01N43/86 , A01N43/88 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D20060101 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D213/00 , C07D213/61 , C07D233/20 , C07D233/52 , C07D239/06 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/00 , C07D277/10 , C07D277/18 , C07D279/00 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D419/06 , C07F9/6558 , A01N43/707 , A01N43/713 , C07D407/06 , C07D407/14 , C07D411/06 , C07D411/14
CPC分类号： C07D239/06 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/86 , A01N47/02 , A01N47/16 , A01N47/22 , A01N47/38 , A01N51/00 , A01N57/32 , C07D207/20 , C07D207/22 , C07D211/70 , C07D211/72 , C07D233/20 , C07D233/52 , C07D239/18 , C07D263/10 , C07D263/28 , C07D265/08 , C07D277/10 , C07D277/18 , C07D279/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07F9/65583
摘要： Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
摘要翻译：式中，n为0或1的新型杀虫剂，其中X为S，O，Y为N或Z为5或6元含氮杂环，R为 R9各自表示氢或特定的有机基团。

76. 发明授权

US4361575A Substituted 2-phenylamino-2-imidazolines and salts thereof 失效
标题翻译：取代的2-苯基氨基-2-咪唑啉及其盐
公开(公告)号：US4361575A
公开(公告)日：1982-11-30
申请号：US276703
申请日：1981-06-23
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler , Wolfgang Hoefke , Wolfram Gaida
IPC分类号： A61K31/415 , A61P9/06 , C07D233/50 , C07D233/52 , C07D233/06
CPC分类号： C07D233/50
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, methyl, trifluoromethyl, hydroxyl or amino;R.sub.4 is straight or branched alkyl of 1 to 5 carbon atoms, allyl or benzyl;R.sub.5 is methyl, ethyl or 2-dimethylamino-ethyl; andn is 0 or 1;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中R 1，R 2和R 3可以相同或不同，可以是氢，氟，氯，溴，甲基，三氟甲基，羟基或氨基; R4是1至5个碳原子的直链或支链烷基，烯丙基或苄基; R5是甲基，乙基或2-二甲基氨基 - 乙基; 并且n为0或1; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

77. 发明授权

US4297496A Nitrimine derivatives 失效
标题翻译：硝基胺衍生物
公开(公告)号：US4297496A
公开(公告)日：1981-10-27
申请号：US162340
申请日：1980-06-23
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 , C07D239/18
CPC分类号： C07D239/08 , A01N51/00 , C07D233/52 , C07D279/06
摘要： A 2-nitriamino-1,3-diazacyclohexane of the formula ##STR1## wherein R is hydrogen, alkyl of from one to six carbon atoms or alkanoyl of from one to seven carbon atoms, and R.sup.1 is hydrogen or alkyl of from one to six carbon atoms, useful as insecticides.
摘要翻译：其中R为氢，1至6个碳原子的烷基或1至7个碳原子的烷酰基的2-氮杂氨基-1,3-二氮杂环己烷，R 1为氢或一至六个碳原子，可用作杀虫剂。

78. 发明授权

US4195092A 2-(Substituted amino)-N-(3-substituted phenyl)-2-imidazoline-1-carbothioamides 失效
标题翻译： 2-（取代的氨基）-N-（3-取代的苯基）-2-咪唑啉-1-硫代甲酰胺
公开(公告)号：US4195092A
公开(公告)日：1980-03-25
申请号：US865091
申请日：1977-12-27
申请人： Terry W. Balko
发明人： Terry W. Balko
IPC分类号： A01N47/38 , C07D233/48 , C07D233/50 , C07D233/52 , C07D277/04 , C07D277/18 , C07D401/12 , C07D417/12 , A61K31/415
CPC分类号： C07D417/12 , A01N47/38 , C07D233/48 , C07D233/50 , C07D233/52 , C07D277/04 , C07D277/18
摘要： 2-(Substituted amino)-N-(3-substituted phenyl)-2-imidazoline-1-carbothioamides, useful as insecticides.
摘要翻译： 2-（取代的氨基）-N-（3-取代的苯基）-2-咪唑啉-1-硫代甲酰胺，可用作杀虫剂。

79. 发明授权

US4187373A Novel dihydrobenzanthracene derivatives 失效
标题翻译：新型二氢苯并蒽衍生物
公开(公告)号：US4187373A
公开(公告)日：1980-02-05
申请号：US947976
申请日：1978-10-02
申请人： Ralph G. Child , Stanley A. Lang, Jr. , Ving J. Lee , Yang-i Lin
发明人： Ralph G. Child , Stanley A. Lang, Jr. , Ving J. Lee , Yang-i Lin
IPC分类号： C07C17/32 , C07C29/09 , C07C35/44 , C07C45/29 , C07C47/453 , C07C47/457 , C07C47/47 , C07C47/546 , C07C47/55 , C07C47/57 , C07C47/575 , C07D233/52 , C07D239/18 , C07D243/04 , C07D245/02 , C07D317/64 , C07D233/56 , C07D239/20
CPC分类号： C07D317/64 , C07C17/32 , C07C29/095 , C07C35/44 , C07C45/29 , C07C47/453 , C07C47/457 , C07C47/47 , C07C47/546 , C07C47/55 , C07C47/57 , C07C47/575 , C07D233/52 , C07D239/18 , C07D243/04 , C07D245/02 , C07C2103/24 , C07C2103/44 , Y10S514/908
摘要： This disclosure describes benzanthracene-5,12(or 7,12)-dicarboxaldehyde-bis-hydrazones and the 5,12(or 7,12)-dihydrobenzanthracene-5,12(or 7,12)-dicarboxaldehyde-bis-hydrazones useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the regression and/or pallation of leukemia and related cancers.
摘要翻译：本公开内容描述了苯并蒽-5,12（或7,12） - 二甲醛 - 双腙和5,12（或7,12） - 二氢苯并蒽-5,12（或7,12） - 二甲醛 - 双腙可用作为抗菌剂，用于抑制移植的小鼠肿瘤的生长，以及用于诱导白血病和相关癌症的消退和/或缓解。

80. 发明授权

US4076726A Amidino-hydrazone derivatives 失效
标题翻译：脒基腙衍生物
公开(公告)号：US4076726A
公开(公告)日：1978-02-28
申请号：US579633
申请日：1975-05-21
申请人： Harm Jan Panneman , Antonius Hermanus Nicolaas Maria Bruins
发明人： Harm Jan Panneman , Antonius Hermanus Nicolaas Maria Bruins
IPC分类号： C07C67/00 , C07C281/18 , C07C313/00 , C07C323/44 , C07D233/52 , C07D239/18 , C07C123/00 , C07D317/44
CPC分类号： C07C281/18 , C07D233/52
摘要： The invention relates to novel amidino-hydrazone derivatives of the general formula: ##STR1## in which the dotted lines mean one extra bond starting from the (guanidine-) carbon atom to one of the adjacent nitrogen atoms, andA stands for methylene, ethylene, propylene or butylene, which groups may optionally be substituted with alkyl (1-4 C),R stands for hydroxy, alkyl (1-4 C), alkylthio or alkoxy (1-4 C), halogen, trifluoromethyl, nitro, amino, hydroxymethyl, acyloxy or an alkylenedioxy group,N is the number 0, 1, 2, 3 or 4,R.sub.1, r.sub.4 and R.sub.5 represent hydrogen or alkyl (1-4 C), with the proviso that one of them is absent in view of the presence of the double bond,R.sub.2 and R.sub.3 stand for hydrogen, alkyl (1-4 C), aralkyl, aryl, hydroxy or amino, with the proviso thatR.sub.2 + r.sub.3 together may also represent a saturated or unsaturated alkylene group with 2 or 3 carbon atoms, orR.sub.3 + r.sub.4 together with the nitrogen atom may also stand for a heterocyclic five- or six-membered ring,As well as the pharmaceutically acceptable acid addition salts thereof, having valuable, antihypertensive and antithrombosis activities.
摘要翻译：本发明涉及以下通式的新颖的脒基腙衍生物：其中虚线表示从（胍） - 碳原子到相邻的氮原子之一起始的一个额外的键，A代表亚甲基，乙烯，丙烯或丁烯，这些基团可以任选被烷基（1-4C）取代，R代表羟基，（1-4C）烷基，烷硫基或烷氧基（1-4C），卤素，三氟甲基，硝基，氨基，羟甲基，酰氧基或亚烷基二氧基，N为0,1,2,3或4，R1，R4和R5代表氢或烷基（1-4C），条件是其中一个不存在于双键存在的观点，R2和R3代表氢，烷基（1-4C），芳烷基，芳基，羟基或氨基，条件是R2 + R3一起也可以表示饱和或不饱和的亚烷基与 2或3个碳原子或R3 + R4与氮原子一起也可以代表杂环五元或六元环，就像P 具有良好的可接受的酸添加剂，具有有价值，抗生素和抗凝血活性。

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