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公开(公告)号：US4931433A
公开(公告)日：1990-06-05
申请号：US45256
申请日：1987-05-01
申请人： Richard L. Tolman
发明人： Richard L. Tolman
IPC分类号： C07D241/44 , A61K31/495 , A61K31/635 , A61P35/00
CPC分类号： A61K31/635 , A61K31/495
摘要： Compounds of formula I are formulated with a pharmaceutical carrier for the treatment of neoplastic disease sensitive to treatment with the compounds in animals including humans. ##STR1## wherein: Y is a substituent attached to any of the unsubstituted carbons on the quinoxaline ring selected from NO.sub.2, OCH.sub.3, H, chloro, CH.sub.3, bromo, hydroxy;X is selected from NO.sub.2, NH.sub.2, acylamide; andZ is hydrogen or halo.
摘要翻译： 式I化合物与用于治疗对包括人在内的动物化合物敏感的肿瘤疾病的药物载体一起配制。 其中：Y是选自NO 2，OCH 3，H，氯，CH 3，溴，羟基的喹喔啉环上任何未取代的碳上的取代基; X选自NO 2，NH 2，酰基酰胺; Z是氢或卤素。
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52.发明授权7,8-dihydro-4-(1-pierazinyl)-6H-thiopyrano-[3,2-d] pyrimidines as .beta.-blockers 失效7,8-二氢-4-（1-吡嗪基）-6H-噻喃并[3,2-d]嘧啶作为β-阻断剂
公开(公告)号：US4889856A
公开(公告)日：1989-12-26
申请号：US91471
申请日：1987-08-31
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： 7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.
摘要翻译： 7,8-二氢-4-（1-哌嗪基）-6H-噻喃并嘧啶具有β-肾上腺素能阻断性质，因此可用于治疗已知适用于β-阻断剂治疗的心血管疾病。 某些化合物可用于通过局部眼部给药治疗眼内压升高。
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53.发明授权Covalently-modified bacterial polysaccharides, stable covalent conjugates of such polysaccharides and immunogenic proteins with bigeneric spacers and methods of preparing such polysaccharides and conjugataes and of confirming covalency 失效共价修饰的细菌多糖，这种多糖的稳定共价缀合物和具有更广泛间隔区的免疫原性蛋白质和制备这种多糖和缀合物的方法以及确认共价
公开(公告)号：US4882317A
公开(公告)日：1989-11-21
申请号：US063607
申请日：1987-06-18
IPC分类号： A61K39/385 , A61K39/39 , A61K47/48 , C07K17/06 , C07K17/10 , G01N33/531
CPC分类号： G01N33/531 , A61K39/385 , A61K39/39 , A61K47/4823 , A61K47/48338 , C07K17/06 , C07K17/10 , A61K2039/55516 , A61K2039/55583 , A61K2039/6031 , A61K2039/627
摘要： Covalently modified bacterial polysaccharides and proteins; covalent conjugates of such polysaccharides linked by a bigeneric spacer, which permits proof of covalency and facilitates purification of conjugated materials, with immunogenic bacterial membrane or other proteins, which conjugates are useful components of bacterial vaccines; and methods of preparing such polysaccharides, proteins and conjugates and of confirming the covalency of the linkage between polysaccharides and proteins.
摘要翻译： 共价修饰细菌多糖和蛋白质; 这种多糖的共价缀合物通过增加的间隔基连接，其允许证实共价性并有利于共轭物质的纯化，其具有免疫原性细菌膜或其它蛋白质，所述缀合物是细菌疫苗的有用组分; 以及制备这种多糖，蛋白质和缀合物并确认多糖和蛋白质之间的连接的共价性的方法。
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公开(公告)号：US4876256A
公开(公告)日：1989-10-24
申请号：US188246
申请日：1988-04-29
申请人： Malcolm M. Coss , Richard L. Tolman
发明人： Malcolm M. Coss , Richard L. Tolman
IPC分类号： A61K31/495 , A61P3/04 , A61P3/08 , A61P3/10 , C07D213/74
CPC分类号： C07D213/74
摘要： Alkylpiperazinylpyridines of formula (I) are disclosed as hypoglycemic agents. ##STR1##
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公开(公告)号：US4863927A
公开(公告)日：1989-09-05
申请号：US48290
申请日：1987-05-11
IPC分类号： A61K31/505 , A61P31/12 , A61P31/22 , C07D239/54 , C07D239/553
CPC分类号： C07D239/54 , C07D239/553
摘要： 1-[2-(Hydroxymethyl)cycloalkylmethyl]-5-substituted uracils which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.
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公开(公告)号：US4782062A
公开(公告)日：1988-11-01
申请号：US48289
申请日：1987-05-11
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/00
CPC分类号： C07D473/00
摘要： 9-[2-(Hydroxymethyl)cycloalkylmethyl]guanines which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, their phosphate derivatives and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.
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公开(公告)号：US4361699A
公开(公告)日：1982-11-30
申请号：US305804
申请日：1981-09-28
IPC分类号： C07D473/34 , C07D473/00
CPC分类号： C07D473/00
摘要： This invention is concerned with a novel process for the preparation of N.sup.6 -alkyl-arprinocid (6-alkyl-amino-9-substituted benzyl purines). Such compounds are active anticoccidial agents. The process involves the preparation of a Schiff base from an acetal of dialkylformamide and reduction with a metal hydride.
摘要翻译： 本发明涉及一种制备N6-烷基 - 丙氨蝶呤（6-烷基 - 氨基-9-取代的苄基嘌呤）的新方法。 这些化合物是活性抗球虫剂。 该方法包括从二烷基甲酰胺的缩醛制备席夫碱并用金属氢化物还原。
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公开(公告)号：US4277603A
公开(公告)日：1981-07-07
申请号：US19986
申请日：1979-03-12
IPC分类号： C07D239/54 , C07D239/545 , C07D471/04 , C07H15/18
CPC分类号： C07D239/545 , C07D471/04 , C07H15/18
摘要： This invention relates generally to a novel process for preparing 5-deazariboflavins by the cyclization of the corresponding 6-(N-substituted arylamino)uracils with trialkylorthoformate in the presence of a strong acid catalyst. An improved process for preparing the uracil intermediate is also disclosed. More particularly, it is concerned with the process for preparing 5-deazariboflavin by cyclizing 6-[3,4-dimethyl-N-(D-ribityl)anilino[uracil with trialkylorthoformate in the presence of a strong acid catalyst and hydrolyzing the resulting alkoxymethylene derivative. The corresponding uracil intermediate is prepared by reacting 6-chlorouracil with N-D-ribityl-3,4-xylidine.5-Deazariboflavins having the general Formula (I) herein below: ##STR1## wherein R.sub.7 is hydrogen or methyl, R.sub.8 is methyl, hydroxy or acyloxy and R.sub.10 is a ribityl group and the corresponding acyl and alkoxymethylene derivatives are useful as riboflavin antagonists with particular utility for the chemotherapy of coccidiosis in chickens or as intermediates for the preparation of said antagonists. The bis(alkoxymethylene) derivatives described herein are useful as prodrug forms of 5-deazariboflavins.When used for the treatment of coccidiosis, such compounds are administered to the animals by way of the feed and are effective in preventing coccidiosis when administered at levels of from about 0.0005% to about 0.05% by weight of the total feed consumed, the amount required for optimum prevention or control of the disease varying with the particular compound employed.
摘要翻译： 本发明一般涉及在强酸催化剂存在下，通过使相应的6-（N-取代的芳基氨基）尿嘧啶与三烷基原甲酸酯环化制备5-脱氮黄素的新方法。 还公开了一种制备尿嘧啶中间体的改进方法。 更具体地说，它涉及通过在强酸催化剂存在下使6- [3,4-二甲基-N-（D-核糖基）苯胺基[尿嘧啶与三烷基原甲酸酯]环化来制备5-脱氮黄素的方法，并水解得到的烷氧基亚甲基 衍生物。 通过6-氯尿嘧啶与N-D-核糖基-3,4-二甲苯胺反应制备相应的尿嘧啶中间体。 具有下述通式（I）的5-脱氮维生素：其中R 7是氢或甲基，R 8是甲基，羟基或酰氧基，R 10是ribityl基团，并且相应的酰基和烷氧基亚甲基衍生物可用作特定的核黄素拮抗剂 用于鸡的球虫病化疗或用作制备所述拮抗剂的中间体的效用。 本文所述的双（烷氧基亚甲基）衍生物可用作5-脱氮白蛋白的前药形式。 当用于治疗球虫病时，通过饲料将这些化合物施用于动物，并且当以所消耗的总饲料的约0.0005重量％至约0.05重量％的水平施用量时，有效地预防球虫病，所需量 用于最佳预防或控制随所用特定化合物变化的疾病。
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公开(公告)号：US4250174A
公开(公告)日：1981-02-10
申请号：US35367
申请日：1979-05-02
IPC分类号： A61K31/435 , A61P33/10 , C07D471/04 , A61K31/41 , C07D401/02 , C07D403/02
CPC分类号： C07D471/04
摘要： Imidazo pyridines with a carbamate group in the 2-position and a phenylthio, or phenylsulfinyl group in the 6-position are disclosed which also are substituted at the 3-position. The 3-position substituents may be halogen, substituted aminomethyl, acyl, and the like. The compounds are active anthelmintic agents. Compositions and methods for the use of such compounds against helmintic infections are also disclosed.
摘要翻译： 公开了2-位氨基甲酸酯基和6-位的苯硫基或苯基亚磺酰基的咪唑并吡啶，其也在3-位取代。 3-位取代基可以是卤素，取代的氨基甲基，酰基等。 这些化合物是活性的驱肠剂。 还公开了使用这种化合物抵抗疱疹感染的组合物和方法。
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60.发明授权
公开(公告)号：US4093714A
公开(公告)日：1978-06-06
申请号：US451639
申请日：1974-03-15
CPC分类号： C07H19/20
摘要： 9-.beta.-D-Arabinofuranosyl nucleotides of the following structure are disclosed: ##STR1## wherein AP is a 3' or 5' phosphorylated arabinofuranoside or the corresponding 3', 5' cyclic phosphate joined by a glycoside linkage to N.sup.9 of the aglycon component of said nucleotide, and Z is H, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkoxy, or hydroxy.Compounds prepared according to the invention exhibit antiviral activity in vitro, while others are precursors useful in the synthesis of bioactive compounds.
摘要翻译： 公开了以下结构的9-β-D-阿拉伯呋喃糖基核苷酸：其中AP是3'或5'磷酸化的阿拉伯呋喃糖苷或相应的3'，5'环状磷酸酯，其通过与糖苷配基的N9的糖苷键连接 的所述核苷酸，Z是H，C1-C6烷基，C7-C10芳烷氧基或羟基。
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