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1. 发明授权

US3928427A N,N{40 -bridged-bis{8 2-alkyl-2-hydroxyethylamine{9 salts 失效
标题翻译： N，N {40-双 - 双{8 2-烷基-2-羟乙胺{9盐
公开(公告)号：US3928427A
公开(公告)日：1975-12-23
申请号：US33226773
申请日：1973-02-14
申请人： STERLING DRUG INC
发明人： DIANA GUY D , CUTLER ROYAL A
IPC分类号： C07C291/04 , C07C91/02
CPC分类号： C07C291/04
摘要： N,N''-Bridged-Bis(2-alkyl-2-Hydroxyethylamine)salts of the formula

are prepared by condensing an epoxide of the formula

and a diamine of the formula R''NH-X-NHR''. The products and dicarbanilates, acid-addition salts, N,N''-dioxides and N,N''diammonium quaternary salts derived therefrom have antibacterial activity in vitro and are useful as antibacterial agents.
摘要翻译：通过将式HOR'R'OH |||R-CH-CH2-NXN-CH2-CH-R的N，N'-桥连双 - [2-烷基-2-羟基乙胺]盐通过将式O || R-CH-CH 2和式R'NH-X-NHR'的二胺。由其衍生的产物和二羧酸酯，酸加成盐，N，N'-二氧化物和N，N'-二铵季盐在体外具有抗菌活性，可用作抗菌剂。

2. 发明授权

US3928366A Preparation of 2-substituted-6-pyridyl-nicotinic acids 失效
标题翻译： 2-取代-6-吡啶基 - 烟酸的制备
公开(公告)号：US3928366A
公开(公告)日：1975-12-23
申请号：US45280674
申请日：1974-03-20
申请人： STERLING DRUG INC
发明人： BRUNDAGE RUTH PAULINE , LESHER GEORGE Y
IPC分类号： C07D213/80 , C07D471/04 , C07D213/22
CPC分类号： C07D213/80 , C07D471/04
摘要： Intermediate 2-R1NH-6-Q''''''-nicotinic acid (V''), where R1 is lower-alkyl and Q'''''' is 4(or 3)-pyridyl or 4(or 3)-pyridyl having one or two lower-alkyl substituents, is prepared in the three steps of: hydrolyzing 1,2-dihydro-2-oxo-6-Q''''''-nicotinonitrile (VII) to produce 1,2-dihydro-2-oxo-6-Q''''''-nicotinic acid (VIII); halogenating VIII to produce 2-halo-6-Q''''''-nicotinic acid (VI''); and, reacting VI'' with R1NH2 to produce V''. Also shown are the steps of: reacting 2-halo-6-Q''''-nicotinic acid (VI), where Q'''' is as Q'''''' and also lower-alkyl, to produce 2-R1NH-6-Q''''-nicotinic acid (V); heating V with a lower-alkyl chloroformate or phosgene to produce 1-R1-7-Q''''-1H,4H-pyrido(2,3-d)(1,3)oxazine-2,4-dione (I''); converting I'' where Q'''' is CH3 to its 8-oxide and reacting the 8-oxide with a lower-alkanoic acid anhydride to produce I where 7-CH3 is converted to 7-(lower-alkanoyloxymethyl); reacting 1-R1-7-Q-1H,4H-pyrido(2,3-d)(1,3)oxazine-2,4-dione, where Q is as Q'''' and also lower-alkanoyloxymethyl, with R2-C( O)CH2COOR, where R2 is H or CH3 and R is lower-alkyl, to produce lower-alkyl 1-R11,4-dihydro-2-R2-4-oxo-7-Q-1,8-naphthyridine-3-carboxylate (III); and, hydrolyzing III to obtain 1-R1-1,4-dihydro-2-R2-4-oxo-7-Q''1,8-naphthyridine-3-carboxylic acid (IV), where Q'' is like Q but having hydroxymethyl in place of lower-alkanoyloxymethyl.
摘要翻译：中间体2-R1NH-6-Q“ - 烟酸（V'），其中R 1是低级烷基且Q”是4或（3） - 吡啶基或具有一个或两个的4（或3） - 吡啶基低级烷基取代基在三个步骤中制备：水解1,2-二氢-2-氧代-6-Q“ - 烟腈（Ⅶ），得到1,2-二氢-2-氧代-6-Q 烟酸（VIII）; 卤化VIII产生2-卤代-6-Q“ - 烟酸（VI'）; 并使VI'与R1NH2反应产生V'。还示出了以下步骤：使2-卤代-6-Q“ - 烟酸（VI）反应，其中Q”为Q“且为低级烷基，以产生2-R 1 NH-6-Q' - 烟酸（V）; 用氯甲酸低级烷基酯或光气加热V，得到1-R1-7-Q“-1H，4H-吡啶并[2,3-d] [1,3]恶嗪-2,4-二酮（I' ; 将Q“为CH 3的I'转化为8-氧化物，并使8-氧化物与低级链烷酸酐反应以产生I，其中7-CH 3转化为7-（低级 - 烷酰氧基甲基）; 使1-R1-7-Q-1H，4H-吡啶并[2,3-d] [1,3]恶嗪-2,4-二酮，其中Q为Q“，低级烷酰氧基甲基， C（= O）CH 2 COOR，其中R 2为H或CH 3且R为低级烷基，得到低级烷基1-R 1-1,4-二氢-2-基-2-氧代-7-Q-1， 8-萘啶-3-羧酸酯（III）; 并且水解III得到1-R 1 -1,4-二氢-2-基-2-氧代-7-Q'-1,8-二氮杂萘-3-羧酸（Ⅳ），其中Q'如Q，但是具有羟甲基代替低级烷酰氧基甲基。

3. 发明授权

US3919837A Method and apparatus for startup of a wet air oxidation unit provided with rotating air compressors driven by rotating expanders 失效
标题翻译：用于启动具有由旋转膨胀机驱动的旋转空气压缩机的湿式空气氧化装置的方法和装置
公开(公告)号：US3919837A
公开(公告)日：1975-11-18
申请号：US44888474
申请日：1974-03-07
申请人： STERLING DRUG INC
发明人： PRADT LOUIS A
IPC分类号： F04D25/04 , B01J14/00 , B01J19/00 , C02F11/08 , D21C11/14 , F02G3/00 , F02C1/00 , F02C7/26
CPC分类号： D21C11/14 , C02F11/08
摘要： Starting a wet oxidation unit by initially supplying a small part of full power to start the compressor-expander train, the resultant low volume of low pressure air being by-passed around the unit to expander inlet, heating and saturating this air, and allowing an increase in air and pressure volume providing additional power, and continuing this procedure until pressure is reached at which a small amount of this air can be admitted to the unit, gradually increasing the air to the unit and reducing the external heat and power to a shut-off point.
摘要翻译：通过初始供应一小部分全部功率启动压缩机 - 膨胀机列车启动湿式氧化装置，所得到的低容量低压空气被绕过该装置绕过扩张器入口，加热并使该空气饱和，并允许增加空气和压力容量，提供额外的动力，并继续此过程，直到达到少量这种空气可以进入单元的压力，逐渐增加到单元的空气并将外部热量和功率减少到关闭关闭点。

4. 发明授权

US3912626A Catalyzed process and catalyst recovery 失效
标题翻译：催化过程和催化剂回收
公开(公告)号：US3912626A
公开(公告)日：1975-10-14
申请号：US45186874
申请日：1974-03-18
申请人： STERLING DRUG INC
发明人： ELY ROBERT B , POGAINIS EDMUNDS M , HOFFMAN CLARENCE A
IPC分类号： C02F1/72 , C02F11/08 , C02B1/34
CPC分类号： C02F1/725 , C02F11/08
摘要： Wet air oxidation of sewage sludge or other wastewaters are catalyzed by copper or silver ions. The catalyst can be recovered by chemical precipitation processes, and recycled to the wet air oxidation system.
摘要翻译：污水污泥或其他废水的湿空气氧化被铜或银离子催化。催化剂可以通过化学沉淀法回收，再循环到湿空气氧化体系中。

5. 发明授权

US3907798A Preparation of 4H-pyrido{8 1,2-a{9 pyrimidin-4-ones from cyclic alkylidene 2-pyridylaminomethylenemalonates 失效
标题翻译：从环状亚烷基2-吡啶基氨基亚甲基戊二酸酯制备4H-吡啶并[1,2-a {9H-嘧啶-4-酮
公开(公告)号：US3907798A
公开(公告)日：1975-09-23
申请号：US35094873
申请日：1973-04-13
申请人： STERLING DRUG INC
发明人： LESHER GEORGE Y
IPC分类号： C07D215/38 , C07D319/06 , C07D471/04 , C07D487/04
CPC分类号： C07D215/38 , C07D319/06 , C07D471/04
摘要： Alkylidene Ar-aminomethylenemalonates, where Ar is an aromatic radical having one or two aromatic rings which can be benzenoid or five- or six-membered heteroaromatic, are prepared by reacting the appropriate aromatic-amine with a mixture of a trialkyl orthoformate or trialkyl orthoacetate and an alkylidene malonate. The alkylidene Ar-aminomethylenemalonates are then cyclized by heating to provide an improved process for preparing various heterocyclic compounds, e.g., a 4-hydroxyquinoline from an alkylidene anilinomethylenemalonate, a 4H-pyrido(1,2-a)pyrimidin4-one from an alkylidene 2-pyridylaminomethylenemalonate, a 4Hpyrimido(1,2-a)pyrimidine-4-one from an alkylidene 2pyrimidylaminomethylenemalonate. The cyclized products are useful as intermediates for the preparation of antimalarials and antiinflammatory agents.
摘要翻译：亚烷基Ar-氨基亚甲基戊二酸酯，其中Ar是具有一个或两个可以是苯或五元或六元杂芳基的芳环的芳基，其通过使适当的芳族胺与原甲酸三烷基酯或原乙酸三烷基酯的混合物和丙二酸亚烷基酯。亚烷基Ar-氨基亚甲基戊二酸酯然后通过加热环化以提供制备各种杂环化合物的改进方法，例如来自亚烷基苯胺基亚甲基丙二酸酯的4-羟基喹啉，4H-吡啶并[1,2-a]嘧啶-4-酮亚烷基2-吡啶基氨基亚甲基丙二酸酯，4-嘧啶基亚氨基亚甲基丙二酸亚苄基酯，4H-嘧啶并[1,2-a]嘧啶-4-酮。环化产物可用作制备抗疟药和抗炎剂的中间体。

6. 发明授权

US3898246A Indoles 失效
标题翻译：吲哚
公开(公告)号：US3898246A
公开(公告)日：1975-08-05
申请号：US34762073
申请日：1973-04-04
申请人： STERLING DRUG INC
发明人： BELL MALCOLM R , ZALAY ANDREW W
IPC分类号： C07D209/12 , C07D295/02 , C07D295/096 , C07D209/14
CPC分类号： C07D295/096 , C07D209/12 , C07D295/02 , Y10S514/843
摘要： The invention relates to novel 1-(4-(R1R2N-CnH2n-O)phenyl)-5-R42-(4-R3-phenyl)indoles having antifertility and hypocholesterolemic activities and to novel intermediates for their preparation.
摘要翻译：本发明涉及具有抗生育能力和降血胆固醇活性的新颖的1- [4-（R1R2N-CnH2n-O）苯基] -5-R4-2-（4-R3-苯基）吲哚及其制备新颖的中间体。

7. 发明授权

US3897431A 2-{8 {60 -Alkoxy-arylmethyl{9 -2-imidazolines and -1,4,5,6-tetrahydropyrimidines 失效
标题翻译： 2- {8 {6-烷氧基 - 芳基甲基{9-2-咪唑啉和-1,4,5,6-四氢嘧啶
公开(公告)号：US3897431A
公开(公告)日：1975-07-29
申请号：US35094973
申请日：1973-04-13
申请人： STERLING DRUG INC
发明人： BAILEY DENIS M
IPC分类号： C07C43/174 , C07C51/00 , C07D233/22 , C07D239/06
CPC分类号： C07D239/06 , C07C43/174 , C07C43/1742 , C07C51/00 , C07D233/22 , Y10S514/866 , Y10S514/869 , C07C65/24
摘要： 2-( Alpha -(Lower-alkoxy)- Alpha -R1-Ar-methyl)-2-imidazolines, -1,4,5,6-tetrahydropyrimidines and -4,5,6,7-tetrahydro-1H-1,3diazepines, having pharmacological properties, e.g., hypoglycemic, diuretic, anti-inflammatory, are prepared by heating a 2-(lower-alkoxy)-2-Ar-alkanenitrile with an alkanediamine, wherein 2, 3 or 4 carbon atoms respectively intervene between the two amino groups, in the presence of a catalytic amount of carbon disulfide or hydrogen sulfide, where R1 is hydrogen, lower-alkyl or lower-alkenyl, Ar is phenyl, naphthyl, indanyl, biphenylyl, cyclohexenyl, cyclohexyl and phenyl substituted by from one to three substituents selected from lower-alkyl, lower-alkoxy, halo, trihalomethyl, loweralkylmercapto, lower-alkylsulfonyl, di-(lower-alkyl)amino, amino, hydroxy, nitro, hydroxyamino and benzyloxy. The intermediate 2(lower-alkoxy)-2-Ar-alkanenitriles are prepared preferably by first reacting an aldehyde of the formula Ar-CHO with a tri(lower-alkyl) orthoformate to form the aldehyde di-(lower-alkyl) acetal, reacting the latter with an acyl halide to form the corresponding Alpha -halo-Ar-methyl lower-alkyl ether and reacting said ether with an alkali cyanide to yield said intermediate nitrile.
摘要翻译： 2- [α-（低级 - 烷氧基）-α-R1-Ar-甲基] -2-咪唑啉，-1,4,5,6-四氢嘧啶和-4,5,6,7-四氢-1H-1，通过加热2-（低级烷氧基）-2- Ar-烷腈与链烷二胺（其中2,3或4个碳原子分别干预）制备具有药理学性质的3-二氮杂，例如降血糖，利尿，抗炎，在两个氨基之间，在催化量的二硫化碳或硫化氢的存在下，其中R 1是氢，低级烷基或低级链烯基，Ar是苯基，萘基，茚满基，联苯基，环己烯基，环己基和被一个至三个选自低级烷基，低级烷氧基，卤素，三卤代甲基，低级烷基巯基，低级烷基磺酰基，二 - （低级 - 烷基）氨基，氨基，羟基，硝基，羟基氨基和苄氧基的取代基。中间体2-（低级烷氧基）-2- Ar-亚烷基腈优选通过首先使式Ar-CHO的醛与三（低级烷基）原甲酸酯反应形成醛二 - （低级 - 烷基）缩醛，使后者与酰基卤反应形成相应的α-卤代-Ar-甲基低级烷基醚，并使所述醚与碱金属氰化物反应，得到所述中间体腈。

8. 发明授权

US3895036A 9-Amino-3-(amino or nitro)-1,5-dioxaspiro{8 5.5{9 undecane derivatives 失效
标题翻译： 9-氨基-3-（氨基或硝基）-1,5-二氧杂螺[{8,55}十一烷衍生物
公开(公告)号：US3895036A
公开(公告)日：1975-07-15
申请号：US46238974
申请日：1974-04-19
申请人： STERLING DRUG INC
发明人： GELOTTE KARL O , SURREY ALEXANDER R
IPC分类号： C07D319/08 , C07D319/06 , A61K31/335
CPC分类号： C07D319/08
摘要： 9-(Ac1NH)-3-Q-3-R-9-R''-1,5-dioxaspiro(5.5)undecane (I), where R and R'' are each hydrogen or lower-alkyl, Ac1 is hydrogen or lower-alkanoyl and Q is NO2 or NH2, are useful intermediates for the preparation of antifertility agents, namely, 3-(Ac4NH)-9(Ac3NH)-3-R-9-R''-1,5-dioxaspiro(5.5)undecane (II), where Ac3 is lower-alkanoyl or 4-Q1-benzoyl, Ac is 4-Q2-benzoyl, Q1 and Q2 are each lower-alkoxy or polyhalo-lower-alkoxy, and, R and R'' are each hydrogen or lower-alkyl. II is prepared by diacylating I where Ac1 is hydrogen and Q is NH2 (VII) or by monoacylating I where Ac1 is lower-alkanoyl and Q is NH2 (VI). VI and VII are prepared stepwise as follows: 4-(Ac5NH)-4-R''-cyclohexanol (X), where Ac5 is lower-alkanoyl, is oxidized to produce 4-(Ac5NH)-4R''-cyclohexanone (III); III is reacted with 2-NO2-R-1,3propanediol (IV) to produce 9-(Ac5NH)-3-nitro-3-R-9-R''-1,5dioxaspiro(5.5)undecane (V); V is reduced to produce 3-amino-9(Ac5NH)-3-R-9-R''-1,5-dioxaspiro(5.5)undecane (VI); and, VI is hydrolyzed to produce 3-R-9-R''-1,5-dioxaspiro(5.5)undecan-3,9diamine (VII). Methods of preparing X are given. Bis(polyhaloacetyl) derivatives of VII are prepared.
摘要翻译： 9-（Ac1NH）-3-Q-3-R-9-R'-1,5-二氧杂螺[5.5]十一烷（I），其中R和R'各自为氢或低级烷基，Ac1为氢或低级 - 烷酰基和Q是NO 2或NH 2，是制备抗生素剂的有用的中间体，即3-（Ac4NH）-9-（Ac3NH）-3-R-9-R'-1,5-二氧杂螺[5.5] 十一碳烷（II），其中Ac 3是低级烷酰基或4-Q1-苯甲酰基，Ac是4-Q2-苯甲酰基，Q1和Q2各自是低级烷氧基或多卤代低级烷氧基，R和R'各自为氢或低级烷基。 II通过二酰化I制备，其中Ac1是氢，Q是NH2（VII）或通过单酰化I，其中Ac1是低级烷酰基，Q是NH2（VI）。 VI和VII分步制备如下：4-（Ac 5 NH）-4-R'-环己醇（X），其中Ac 5是低级 - 烷酰基，被氧化生成4-（Ac5NH）-4-R'-环己酮（III ）; III与2-NO 2 -R-1,3-丙二醇（IV）反应，生成9-（Ac5NH）-3-硝基-3-R-9-R'-1,5-二氧杂螺[5.5]十一烷（V ）; V被还原以产生3-氨基-9-（Ac 5 NH）-3-R-9-R'-1,5-二氧杂螺[5.5]十一烷（VI）; 并将VI水解，得到3-R-9-R'-1,5-二氧杂螺[5.5]十一烷-3,9-二胺（VII）。给出了X的制备方法。制备VII的双（多卤乙酰）衍生物。

9. 发明授权

US3895017A 3-Acetyl-1-alkyl-1,4-dihydro-4-oxo-1,8-naphthyridines and intermediates 失效
标题翻译： 3-乙酰基-1-烷基-1,4-二氢-4-氧代-1,8-萘啶和中间体
公开(公告)号：US3895017A
公开(公告)日：1975-07-15
申请号：US45392874
申请日：1974-03-22
申请人： STERLING DRUG INC
发明人： LESHER GEORGE Y , BRUNDAGE RUTH PAULINE
IPC分类号： C07D471/04 , C07D31/36
CPC分类号： C07D471/04
摘要： Process of reacting 2-amino-6-Q''-pyridine (I) with lower-alkyl (lower-alkoxy)methyleneacetoacetate (II) to produce lower-alkyl Alpha -(6-Q''-2-pyridylaminomethylene)acetoacetate (III''), heating lower-alkyl Alpha -(6-Q-2-pyridylaminomethylene)acetoacetate (III), to produce 3-acetyl-1,4-dihydro-7-Q-4-oxo-1,8naphthyridine (IV) which is tautomeric with 3-acetyl-4-hydroxy-7Q-1,8-naphthyridine (IVA), reacting IV (or IVA) with a loweralkylating agent to produce 3-acetyl-1-(lower-alkyl)-1,4-dihydro7-Q-4-oxo-1,8-naphthyridine (V) and converting V to 1-(loweralkyl)-1,4-dihydro-7-Q-4-oxo-1,8-naphthyridine-3-carboxylic acid (VI), where Q is lower-alkyl, hydroxymethyl, loweralkanoyloxymethyl, 4(or 3)-pyridyl or 4(or 3)-pyridyl having one or two lower-alkyl substituents, and Q'' is like Q but excluding lower-alkanoyloxymethyl. The compounds of formula VI are known antibacterial agents. Also given are alternative routes of preparing III and IV where Q is lower-alkanoyloxymethyl by reacting the N-oxides of III and IV, respectively, where Q is methyl with a lower-alkanoic acid anhydride.
摘要翻译：使2-氨基-6-Q'-吡啶（I）与低级烷基（低级烷氧基）亚甲基乙酰乙酸酯（II）反应生成低级烷基α-（6-Q'-2-吡啶基氨基亚甲基）乙酰乙酸酯（III' ），加热低级烷基α-（6-Q-2-吡啶基氨基亚甲基）乙酰乙酸酯（III），得到3-乙酰基-1,4-二氢-7-Q-4-氧代-1,8-萘啶（IV）其与3-乙酰基-4-羟基-7-Q-1,8-二氮杂萘（IVA）是互变异构体，使IV（或IVA）与低级烷基化剂反应以产生3-乙酰基-1-（低级烷基） -1,4-二氢-7-Q-4-氧代-1,8-二氮杂萘（V）并将V转化为1-（低级烷基）-1,4-二氢-7-Q-4-氧代-1 （VI），其中Q是具有一个或两个低级烷基取代基的低级烷基，羟甲基，低级烷酰氧基甲基，4（或3） - 吡啶基或4（或3） - 吡啶基， Q'如Q，但不包括低级烷酰氧基甲基。式VI化合物是已知的抗菌剂。还给出了制备III和IV的替代途径，其中Q是低级烷酰氧基甲基，分别通过使III和IV的N-氧化物与低级链烷酸酐反应。

10. 发明授权

US3869443A N,N{40 -Heptamethylenebis(4-trifluoromethoxybenzamide)-{62 -cyclodextrin inclusion complex 失效
标题翻译： N，N {40-七亚甲基双（4-三氟甲氧基苯甲酰胺） - {62-环糊精包合物
公开(公告)号：US3869443A
公开(公告)日：1975-03-04
申请号：US36428973
申请日：1973-05-29
申请人： STERLING DRUG INC
发明人： LESHER GEORGE Y
IPC分类号： C07D209/48 , C07D295/092 , C08L3/02 , C08B25/02 , C07C103/30
CPC分类号： C07D209/48 , C07C255/00 , C07D295/088
摘要： 4-(Q-O)-4''-R1-N,N''-alkylenebis(benzamides), N,N''alkylenebis(3,4-methylenedioxybenzamides) or N,N''-alkylenebis(4(lower-alkoxy)benzamides), having endocrinological properties, where Q is lower-alkyl, lower-alkoxyalkyl, lower-alkenyl, halolower-alkyl, halo-lower-alkenyl, lower-cycloalkyl, phenyl and BN(lower alkyl) where BN is di-(lower-alkyl)amino or a saturated Nheteromonocyclic radical having from five to seven ring atoms and alkylene has at least five carbon atoms between its two connecting linkages and R1 is Q-O-, hydrogen, lower-alkoxy, lower-alkyl, halo, benzyloxy, hydroxy, di-(lower-alkyl)amino, nitro, amino or trihalomethyl are prepared preferably by reacting the appropriate diamine or N-(aminoalkyl)-benzamide with two or one molar equivalents, respectively, of the appropriate benzoyl halide. The instant application relates particularly to N,N''heptamethylenebis(4-trifluoromethoxybenzamide)- Beta cyclodextrin inclusion complex, having antifertility activity.
摘要翻译： 4-（QO）-4'-R1-N，N'-亚烷基双（苯甲酰胺），N，N'-亚烷基双（3,4-亚甲二氧基苯甲酰胺）或N，N'-亚烷基双[4-（低级烷氧基） ]，具有内分泌学性质，其中Q为低级烷基，低级烷氧基烷基，低级烯基，卤代低级烷基，卤代低级烯基，低级环烷基，苯基和BN-（低级烷基）（低级烷基）氨基或具有5-7个环原子的饱和N-杂单环基团，并且亚烷基在其两个连接键之间具有至少五个碳原子，并且R 1是QO-，氢，低级烷氧基，低级 - 烷基，卤素苄基氧基，羟基，二 - （低级 - 烷基）氨基，硝基，氨基或三卤代甲基优选通过使合适的二胺或N-（氨基烷基） - 苯甲酰胺与适当的苯甲酰卤的2或1摩尔当量反应来制备。本申请特别涉及具有抗生育活性的N，N'-七亚甲基双（4-三氟甲氧基苯甲酰胺）-β-环糊精包合物。

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