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91. 发明授权

US6008316A Functionalized polyamines 有权
标题翻译：官能化多胺
公开(公告)号：US6008316A
公开(公告)日：1999-12-28
申请号：US146873
申请日：1998-09-03
申请人： Alvie L. Foster, Jr. , Ivonne C. Weidner , Klein A. Rodrigues , Allen M. Carrier
发明人： Alvie L. Foster, Jr. , Ivonne C. Weidner , Klein A. Rodrigues , Allen M. Carrier
IPC分类号： C11D3/26 , C07C279/00 , C07C279/26 , C08G73/00 , C08G73/02 , C11D3/00 , C11D3/37 , C11D3/386 , C11D3/39 , D06M15/61 , D06P1/52 , D06P5/06 , D06P5/08 , C08G12/00 , D06M13/256
CPC分类号： C11D3/386 , C08G73/00 , C08G73/02 , C11D3/0021 , C11D3/3723 , D06P1/5278 , D06P1/5285 , D06P5/06 , D06P5/08 , C11D3/39 , C11D3/3905
摘要： A functionalized polyamine comprising the reaction product of (A) a cyano- or guanidino-containing compound selected from the group consisting of cyanamides or salts thereof, dicyanamides or salts thereof, dicyandiamides or salts thereof, guanidines or salts thereof, biguanidines or salts thereof, and combinations thereof, and (B) a polyamine prepared from at least one monomeric amine, wherein the cyano- or guanidino-functional groups are attached to the polyamine or incorporated therein to form the functionalized polyamine, provided that the monomeric amine and the cyano- or guanidino-containing compound are present in the functionalized polyamine in a molar ratio of from 1.1:1 to 100:1, respectively. The functionalized polyamines are especially useful as anti-dye transfer and color protection agents in laundry detergent compositions.
摘要翻译：一种官能化多胺，其包含（A）选自氰基或胍基的化合物的反应产物，所述化合物选自氰酰胺或其盐，二氰胺或其盐，双氰胺或其盐，胍或其盐，双胍或其盐，及其组合，和（B）由至少一种单体胺制备的多胺，其中氰基或胍基官能团连接到多胺或并入其中以形成官能化的多胺，条件是单体胺和氰基 - 或含胍基的化合物分别以1.1:1至100:1的摩尔比存在于官能化的多胺中。官能化的多胺特别可用作衣物洗涤剂组合物中的抗染料转移和颜色保护剂。

92. 发明授权

US5019596A Pharmaceutical compositions having therapeutical activity based on mercaptoethansulphonic acid 失效
标题翻译：具有基于巯基乙磺酸的治疗活性的药物组合物
公开(公告)号：US5019596A
公开(公告)日：1991-05-28
申请号：US348171
申请日：1989-05-02
申请人： Alberto Reiner , Giuseppe Vita
发明人： Alberto Reiner , Giuseppe Vita
IPC分类号： A61K31/155 , A61K31/185 , A61K31/195 , A61K31/205 , A61K31/22 , A61P13/02 , A61P15/00 , A61P35/00 , C07C279/14 , C07C279/26 , C07C319/20 , C07C319/28 , C07C323/58 , C07C323/65 , C07C323/66
CPC分类号： A61K31/185 , C07C229/26 , C07C279/14 , C07C323/58 , C07C323/66
摘要： Derivatives of mercapthansulphonic acid are active in the therapy of the bladder carcinoma and in the therapy and prevention of the cistinic kidney calculi. The saline derivatives with basic aminoacids and their alkyl esters are moreover devoid of side effects. The saline derivatives are prepared by reacting, in aqueous or aqueous-alcoholic medium, equimolar amounts of mercaptoethansulphonic acid, just prepared from an organic or inorganic salt thereof, and of the desired aminoacid.
摘要翻译：巯基磺酸的衍生物在膀胱癌的治疗和治疗和预防小肠肾结石方面是有活性的。具有碱性氨基酸及其烷基酯的盐水衍生物还没有副作用。盐水衍生物通过在水性或含水醇介质中使等摩尔量的由其有机或无机盐制备的巯基乙磺酸和所需的氨基酸反应来制备。

93. 发明授权

US4900775A Solubilization of complexes of water-insoluble organic compounds by aqueous solutions of polyvinylpyrrolidone 失效
标题翻译：通过聚乙烯吡咯烷酮水溶液溶解水不溶性有机化合物络合物
公开(公告)号：US4900775A
公开(公告)日：1990-02-13
申请号：US161888
申请日：1988-02-29
申请人： Terry E. Smith , James R. Cho , Ian W. Cottrell
发明人： Terry E. Smith , James R. Cho , Ian W. Cottrell
IPC分类号： A61K31/155 , A01N25/10 , A61K9/08 , A61K31/34 , A61K47/32 , A61K47/48 , C07B61/00 , C07C209/90 , C07C211/52 , C07C279/26 , C08J3/21 , C08K5/31 , C08K5/32 , C08K5/43
CPC分类号： C08J3/21 , A01N25/10 , A61K47/48176 , C08K5/31 , C08K5/32 , C08K5/43 , C08J2339/06
摘要： A method for increasing the water-solubility of highly insoluble organic compounds by forming a complex product from the reaction between the organic compound and an aqueous solution of solid polyvinylpyrrolidone. The solubility of the organic compound can be increased at least 25-fold and the complex formed is highly stable at ambient conditions.
摘要翻译：通过从有机化合物和固体聚乙烯吡咯烷酮的水溶液之间的反应形成复合产物来提高高度不溶性有机化合物的水溶性的方法。有机化合物的溶解度可以增加至少25倍，形成的络合物在环境条件下高度稳定。

94. 发明授权

US4567174A Bis(1-substituted biguanide) derivatives 失效
标题翻译：双（1-取代双胍）衍生物
公开(公告)号：US4567174A
公开(公告)日：1986-01-28
申请号：US607703
申请日：1984-05-07
申请人： Philip N. Edwards , Michael S. Large
发明人： Philip N. Edwards , Michael S. Large
IPC分类号： C07C279/26 , C07D295/215 , C07D403/12 , A01N43/40 , A61K31/445
CPC分类号： C07D295/215 , C07C279/265
摘要： A bis(1-substituted biguanide) derivative of the formula:R.sup.3 R.sup.4 N.C(:NR.sup.5)NH.C(NR.sup.9)NR.sup.1 --X--NR.sup.2.C(:NR.sup.9)NH.C(:NR.sup.6)--NR.sup.7 R.sup.8 Vor a tautomeric form thereof, wherein R.sup.1, R.sup.2 and R.sup.9, which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R.sup.1, R.sup.2 and R.sup.9 is other than hydrogen; R.sup.3, R.sup.4, R.sup.7 and R.sup.8, which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R.sup.3, R.sup.4 and the nitrogen atom to which they are attached, or R.sup.7 and R.sup.8 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical, each of which may bear 1-3C alkyl substituents; R.sup.5 and R.sup.6 , which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and X is a 2-16C linking group which is a straight chain alkylene radical, or a straight chain alkylene radical bearing one or more 1-16C alkyl substituents, of which any pair or pairs which are attached to different carbon atoms, may be joined so as to form, together with the intervening carbon atom or atoms of the alkylene radical, a (5-7C)-cycloalkyl radical or radicals; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.
摘要翻译：一种下式的双（1-取代双胍）衍生物：R3R4N.C（：NR5）NHC（NR9）NR1-X-NR2C（NR9）NHC（NR6）-NR7R8V或互变异构体其中R1，R2和R9可以相同或不同，各自为氢，1-16C烷基，3-16C环烷基，（3-12C环烷基） - （1-4C烷基）基团，任选取代的苯基或萘基，任选取代的苯基（1-4C）烷基或萘基（1-4C）烷基或任选取代的二苯基甲基，条件是R 1，R 2和R 9中的至少一个不是氢; 可以相同或不同的R 3，R 4，R 7和R 8各自为氢，或如上所定义的烷基，环烷基，（环烷基）烷基，苯基，萘基，苯基烷基，萘基烷基或二苯基甲基，或2-16 烷氧基烷基或R3，R4及其所连接的氮原子，或者它们所连接的R7和R8及其氮原子可以相同或不同，分别为1-氮杂环丁烷基，1-吡咯烷基，哌啶子基，六亚甲基亚氨基，七亚甲基亚氨基，吗啉代或4-（1-8C烷酰基）-1-哌嗪基，其各自可以具有1-3C烷基取代基; R5和R6可以相同或不同，分别为氢或1-8C烷基; X是直链亚烷基的2-16C连接基团或具有一个或多个1-16C烷基取代基的直链亚烷基，其中连接到不同碳原子上的任何一对或者对可以连接与间插碳原子或亚烷基的原子一起形成（5-7C） - 环烷基或自由基; 及其酸加成盐，其制备方法，以及使用所述化合物的抗菌和抗真菌组合物和方法。

95. 发明授权

US4224245A Method of making 1-(alkoxyphenyl)-5-(phenyl)biguanide compounds which are useful as agricultural fungicides 失效
标题翻译：制备可用作农业杀真菌剂的1-（烷氧基苯基）-5-（苯基）双胍化合物的方法
公开(公告)号：US4224245A
公开(公告)日：1980-09-23
申请号：US33244
申请日：1979-04-25
申请人： Louis Schneider , Bruce M. Resnick
发明人： Louis Schneider , Bruce M. Resnick
IPC分类号： A01N47/44 , C07C279/26 , C07C129/16
CPC分类号： C07C279/26 , A01N47/44
摘要： The present invention provides an improved method of making 1-(alkoxyphenyl)-5-(phenyl)biguanide compounds which are useful as agricultural fungicides, having the formula: ##STR1## where R is alkyl, linear of branched, having from 1-14 carbon atoms; and acid addition salts thereof.The method comprises the steps of (a) alkylating a nitrophenol with a suitable alkyl halide in a reaction solvent to form an alkoxynitrobenzene intermediate, (b) reducing the nitro group of the itermediate in situ by catalytic hydrogenation to form an alkoxyaniline, and (c) condensing the alkoxyaniline with phenyldicyandiamide to form the desired biguanide as the acid addition salt.The invention also includes a novel isolation and purification procedure for obtaining purified biguanide acid addition salts and purified free biguanide base.
摘要翻译：本发明提供一种制备可用作农业杀真菌剂的1-（烷氧基苯基）-5-（苯基）双胍化合物的改进方法，其具有下式：其中R是烷基，直链是支链的，具有1-14 碳原子及其酸加成盐。该方法包括以下步骤：（a）在反应溶剂中用合适的烷基卤烷基化硝基苯酚以形成烷氧基硝基苯中间体，（b）通过催化氢化原位还原硝酸的硝基以形成烷氧基苯胺，和（c ）将烷氧基苯胺与苯基二氰胺缩合形成所需的双胍类作为酸加成盐。本发明还包括用于获得纯化的双胍酸加成盐和纯化的游离双胍碱的新颖的分离和纯化方法。

96. 发明授权

US4198392A Oral compositions containing bis-biguanides with reduced staining tendencies 失效
标题翻译：具有降低染色趋势的双重双胍的口服组合物
公开(公告)号：US4198392A
公开(公告)日：1980-04-15
申请号：US922136
申请日：1978-07-05
申请人： Prem S. Juneja
发明人： Prem S. Juneja
IPC分类号： A61K8/43 , A61Q11/00 , C07C279/26 , C07C129/08 , A61K7/18 , A61K9/68 , A61K31/155
CPC分类号： C07C279/265 , A61K8/43 , A61Q11/00
摘要： Oral compositions such as toothpastes, mouthwashes, and the like containing particular substantive bis-biguanide compounds which inhibit the formation of plaque and caries.
摘要翻译：包含牙膏，漱口剂等的口服组合物含有抑制斑块和龋齿形成的特定实质性双双胍化合物。

97. 发明授权

USB403243I5 失效
公开(公告)号：USB403243I5
公开(公告)日：1976-03-30
申请号：US40324373
申请日：1973-10-03
IPC分类号： C07C279/26
CPC分类号： C07C279/26 , Y10S514/926 , Y10S514/927

98. 发明授权

US3888947A Bis-biguanides 失效
标题翻译： BIS-BIGUANIDES
公开(公告)号：US3888947A
公开(公告)日：1975-06-10
申请号：US25444072
申请日：1972-05-18
申请人： KEMA NORD AB
发明人： STEPHENSON RONALD ARTHUR , LAURSEN BENTE LISSY , MATTSSON OVE HENNING
IPC分类号： C07C279/26 , C07C101/00
CPC分类号： C07C279/265
摘要： The invention provides, as new compounds, salts of certain bactericidally active bis-biguanides bases with sequestering amino-carboxylic acids, the compounds being useful as bactericides. The invention also provides compositions containing these salts; the compositions preferably incorporate quaternary ammonium compounds as solubilizing agents for the salts.

99. 发明授权

US3879541A Antihyperglycemic methods and compositions 失效
标题翻译：抗高血糖方法和组合物
公开(公告)号：US3879541A
公开(公告)日：1975-04-22
申请号：US32421873
申请日：1973-01-16
申请人： BAYER AG
发明人： KABBE HANS-JOACHIM , HORSTMANN HARALD , PLUMPE HANS , PULS WALTER , PETERSEN SIEGFRIED
IPC分类号： C07C279/26 , A61K27/00
CPC分类号： C07C279/26
摘要： The blood sugar level of hyperglycemic animals can be reduced through administration of an N1-phenylbiguanide which is substituted in the N5-position by the group CH2R2 in which R2 is hydrogen, alkyl of 1 to 7 carbon atoms, alkoxyalkyl of 2 to 5 carbon atoms, cyclohexyl or vinyl, and optionally substituted by one or two groups in the phenyl ring. Solid, orally administered pharmaceutical compositions are also described. A typical embodiment is the use of N1-(4-chlorophenyl)-N5-(npropyl)biguanide hydrochloride which can be administered in a tablet, capsule or dragee.
摘要翻译：高血糖动物的血糖水平可以通过施用在N5位被CH2R2（其中R2是氢），1至7个碳原子的烷基，2至5个碳原子的烷氧基烷基的N 2 - 取代的N 1 - 苯基双胍，环己基或乙烯基，并且任选被苯环中的一个或两个基团取代。还描述了固体，口服给药的药物组合物。典型的实施方案是使用可以在片剂，胶囊或糖衣丸中施用的N1-（4-氯苯基）-N5-（正丙基）双胍盐酸盐。

100. 发明授权

US3860648A 1-(p-trifluoromethoxyphenyl)-biguanide 失效
标题翻译： 1-（对三氟甲基） - 溴
公开(公告)号：US3860648A
公开(公告)日：1975-01-14
申请号：US44190774
申请日：1974-02-12
申请人： RORER INC WILLIAM H
发明人： DIAMOND JULIUS , NOVICK JR WILLIAM J
IPC分类号： C07C279/26 , C07C317/42
CPC分类号： C07C317/42 , C07C279/26 , Y10S514/926 , Y10S514/927
摘要： 1-Aryl and aralkyl biguanides and their acid addition salts in suitable pharmaceutical dosage form are useful in the treatment of gastrointestinal disorders.
摘要翻译：合适的药物剂型中的1-芳基和芳烷基双胍及其酸加成盐可用于治疗胃肠道疾病。

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