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公开(公告)号：US4344955A
公开(公告)日：1982-08-17
申请号：US158975
申请日：1980-06-12
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/56 , C07D499/60 , C07D499/64 , C07D499/68 , C07D499/70 , C07D499/72 , C07D499/74 , C07D499/76 , C07D499/78
CPC分类号： C07D499/00 , A61K31/43
摘要： Anti-bacterially active penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom or optionally substituted alkoxy group,R.sub.3 denotes a hydrogen atom, COR.sub.4, SO.sub.2 -alkyl, SO.sub.2 -aryl or an optionally substituted alkyl group, but R.sub.2 and R.sub.3 do not simultaneously denote hydrogen atoms, andR.sub.4 denotes a hydrogen atom or any of many possible organic radicals.The compounds are also inhibitors of .beta.-lactamases so they can be used in conjunction with .beta.-lactamase-susceptible antibiotics. They are useful in fighting bacterial infection, in promoting animal growth and in preserving various materials.
摘要翻译： 其中R1表示氢原子或成酯基团的式为“IMAGE”或其盐的抗细菌活性青霉素1,1-二氧化物，R 2表示氢原子或任选取代的烷氧基，R 3表示氢 原子，COR 4，SO 2 - 烷基，SO 2 - 芳基或任选取代的烷基，但R 2和R 3不同时表示氢原子，R 4表示氢原子或许多可能的有机基团中的任何一种。 这些化合物也是β-内酰胺酶的抑制剂，因此它们可以与β-内酰胺酶敏感的抗生素联合使用。 它们有助于消灭细菌感染，促进动物生长和保存各种材料。
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公开(公告)号：US4344939A
公开(公告)日：1982-08-17
申请号：US154541
申请日：1980-05-29
IPC分类号： C07D499/32 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/44 , C07D499/46 , C07D499/60 , C07D499/64 , C07D499/70 , C07D499/74 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61K31/655 , C07D499/52 , C07D499/54 , C07D499/76
CPC分类号： C07D499/00
摘要： New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom,R.sub.3 denotes a hydrogen atom,R.sub.4 denotes a hydrogen atom, an optionally substituted naphthyl radical or a radical of the general formula ##STR2## and the remaining variables can be various organic radicals.
摘要翻译： 式（1）所示的新型青霉素1,1-二氧化物或其盐，其中R1表示氢原子或成酯基团，R2表示氢原子，R3表示氢原子，R4表示氢原子， 任选取代的萘基或通式为“IMAGE”的基团，其余的变量可以是各种有机基团。
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3.发明授权Substituted omicron-phenylenediamine derivatives, process for their preparation and their use as medicaments 失效取代的微米 - 苯二胺衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4246260A
公开(公告)日：1981-01-20
申请号：US21869
申请日：1979-03-19
IPC分类号： A61K31/265 , A61K31/40 , A61K31/435 , A61K31/55 , A61P33/00 , A61P33/10 , C07C67/00 , C07C231/00 , C07C233/25 , C07C233/43 , C07C239/00 , C07C279/24 , C07C313/00 , C07C317/40 , C07C317/42 , C07C323/41 , C07C323/43 , C07D295/15 , A61K31/325 , C07C125/06
CPC分类号： C07D295/15
摘要： The invention relates to new substituted o-phenylenediamine derivatives of the general formula ##STR1## in which R represents optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkinyl,X represents O, S, SO or SO.sub.2 andR.sup.1 and R.sup.2 are different from one another and individually represent ##STR2## in which R.sup.3 and R.sup.4 are identical or different and represent alkyl andR.sup.5 represents hydrogen, optionally substituted alkyl or optionally substituted alkoxy, and salts thereof.Also included in the invention are (1) methods for preparing the above-described compounds, (2) compositions containing the above-described compounds and (3) methods for the treatment of helminthiasis.
摘要翻译： 本发明涉及通式为（I）的新的取代的邻苯二胺衍生物，其中R代表任选取代的烷基，任选取代的烯基或任选取代的炔基，X代表O，S，SO或SO 2，R 1和R 2是 各自独立地表示其中R 3和R 4相同或不同并且表示烷基且R 5表示氢，任选取代的烷基或任选取代的烷氧基及其盐的
。 本发明还包括（1）制备上述化合物的方法，（2）含有上述化合物的组合物和（3）治疗蠕虫病的方法。 -
4.发明授权Substituted benzenesulphonic acid esters, processes for their preparation and their use as medicaments 失效取代的苯磺酸酯，其制备方法及其作为药物的用途
公开(公告)号：US4194004A
公开(公告)日：1980-03-18
申请号：US847890
申请日：1977-11-02
IPC分类号： A01N47/20 , C07C67/00 , C07C301/00 , C07C303/30 , C07C309/72 , C07C309/76 , C07C325/00 , C07C335/28 , C07D295/15 , A61K31/27 , A61K31/255 , C07C143/68
CPC分类号： C07D295/15 , C07C309/72 , C07C309/76
摘要： Novel substituted benzenesulphonic acid esters, particularly useful as anthelmintics are provided. The novel compounds are those of the general formula ##STR1## in which R represents hydrogen, optionally substituted alkyl, cyano, alkoxy, halogen, trifluoromethyl, amino, acylamino or nitro,X represents SO.sub.3 andR.sup.1 and R.sup.2 are different from one another and individually represent one of the radicals ##STR2## wherein Y represents S andR.sub.3 represents hydrogen, optionally substituted alkyl or alkoxy,and salts thereof. Also included in the invention are methods for preparing the novel compounds, compositions containing them and methods for the use of the compounds and compositions.
摘要翻译： 提供了特别用作驱肠剂的新型取代苯磺酸酯。 新化合物是通式为其中R表示氢，任选取代的烷基，氰基，烷氧基，卤素，三氟甲基，氨基，酰氨基或硝基的通式（I）的化合物，X表示SO 3，R 1和R 2不同于 另一个并且各自独立地表示基团之一，其中Y表示S且R 3表示氢，任选取代的烷基或烷氧基，及其盐。 本发明还包括制备新化合物的方法，含有它们的组合物和使用该化合物和组合物的方法。
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公开(公告)号：US4015012A
公开(公告)日：1977-03-29
申请号：US579446
申请日：1975-05-21
IPC分类号： A61K31/155 , A61K31/165
CPC分类号： A61K31/155
摘要： New 4-acylaminophenylacetamidines of the formula: ##STR1## in which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要翻译： 新的具有3-8个碳原子的直链或支链烷氧基烷基或具有3-8个碳原子的直链或支链链烯氧基烷基的4-氨基苯基乙酰胺，其中R是具有3-8个碳原子的直链或支链烷氧基烷基，其中烷氧基部分或烯氧基部分可被烷氧基取代 或苯基，并且包括其无毒的药理学上可接受的盐。 该产品具有作为杀寄生虫剂的作用。
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公开(公告)号：US3970699A
公开(公告)日：1976-07-20
申请号：US505738
申请日：1974-09-13
IPC分类号： A61K31/165 , A61K31/155 , A61P33/10 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C239/00 , C07C257/14 , C07C257/20 , C07C103/34
CPC分类号： A61K31/155
摘要： New 4-acylaminophenylacetamidines of the formula: ##SPC1##In which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要翻译： 新的4-酰基氨基苯基乙酰胺的下式：
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公开(公告)号：US4064270A
公开(公告)日：1977-12-20
申请号：US505745
申请日：1974-09-13
IPC分类号： A61K31/165 , A61K31/155 , A61K31/40 , A61K31/495 , A61K31/535 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C239/00 , C07C257/14 , C07C257/20 , C07D295/15 , C07D295/00
CPC分类号： C07D295/15 , Y02P20/55
摘要： A new class of N'-(aminoacylaminophenyl) acetamidines: ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R.sup.3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics.The products are obtained by treating a suitable amino-acid or a carbonyl-activated amino-acid, with the appropriate N'-(4-aminophenyl)-N,N-dimethylacetamidine. In addition, the products are obtained by treating a suitable N'-(haloacylaminophenylacetamidine with an appropriate amine.
摘要翻译： 一类新的N' - （氨基酰氨基苯基）乙酰胺：其中R1和R2相同或不同，代表氢，烷基，芳基或其取代的衍生物，或与它们所连接的氮原子一起， 杂环; 并且R 3是氢，烷基，芳基，芳烷基或包括其取代的衍生物的杂环部分。 该产品具有作为驱虫剂的功效。
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8.发明授权Anti-thrombotic pharmaceutical compositions comprising tricyclo-4H-1,4-benzothiazine derivatives and method of use therefor 失效包含三环-4H-1,4-苯并噻嗪衍生物的抗血栓形成药物组合物及其用途
公开(公告)号：US4636497A
公开(公告)日：1987-01-13
申请号：US770895
申请日：1985-08-29
IPC分类号： A61K31/54 , A61K31/5415 , A61P1/14 , A61P11/00 , A61P29/00 , A61P35/00 , A61P37/08 , C07D279/16 , C07D279/20 , C07D279/22 , C07D513/04 , A61K31/38 , C07D279/10
CPC分类号： C07D513/04 , C07D279/16 , C07D279/20
摘要： The present invention refers to novel anellated 4H-1,4-benzothiazines, several processes for the synthesis thereof, their use as pharmaceutical agents, in particular their use as lipoxygenase-inhibiting agents, pharmaceutical compositions containing the novel benzothiazines and a process for their manufacture.
摘要翻译： 本发明涉及新型的有机化合的4H-1,4-苯并噻嗪，其合成方法，它们作为药物的用途，特别是其作为脂氧合酶抑制剂的用途，含有新的苯并噻嗪类的药物组合物及其制备方法 。
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公开(公告)号：US4567188A
公开(公告)日：1986-01-28
申请号：US522069
申请日：1983-08-10
IPC分类号： A61K31/04 , A61K31/13 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P9/08 , A61P9/12 , C07C67/00 , C07C209/00 , C07C209/22 , C07C211/29 , C07C211/44 , C07C211/52 , C07C215/76 , C07C217/84 , C07C323/36 , C07D213/38 , C07D213/40 , C07D213/74 , C07D213/75 , A61K31/135 , C07C87/60
CPC分类号： C07D213/74 , C07D213/38
摘要： Compounds of the formula ##STR1## in which R.sup.1 is an optionally substituted aryl or heteroaryl radical,R.sup.2 is an alkyl or alkenyl radical which is optionally substituted by alkoxy or cycloalkyl, or an optionally substituted aryl or heteroaryl radical, and X is an optionally aklyl-substituted methylene radical or a direct bond, but if X is a direct bond R.sup.2 is not aryl,or physiologically acceptable acid addition salts thereof, exhibit activity on the circulation system particularly as hypotensive agents.
摘要翻译： 其中R 1为任选取代的芳基或杂芳基，R 2为任选被烷氧基或环烷基取代的烷基或烯基，或任选取代的芳基或杂芳基，且X为任选取代的烷基或烯基 - 取代的亚甲基或直接键，但是如果X是直接键，则R2不是芳基或其生理上可接受的酸加成盐，在循环系统上表现出特别是作为降压剂的活性。
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公开(公告)号：US4491595A
公开(公告)日：1985-01-01
申请号：US249249
申请日：1981-03-30
IPC分类号： A01N47/44 , C07C67/00 , C07C279/28 , C07C301/00 , C07C303/40 , C07C311/39 , C07D295/215 , C07C129/12 , A01N37/52
CPC分类号： C07D295/215 , C07C279/28
摘要： Trisubstituted cyanoguanidines of the formula ##STR1## in which R.sup.1 represents an optionally substituted phenyl or phenylalkyl radical, an alkyl radical with more than 1 carbon atom, a substituted alkyl radical, an alkenyl or alkinyl radical or an optionally substituted cycloalkyl radical,R.sup.2 represents an optionally substituted alkyl radical or an alkenyl or alkinyl radical andR.sup.3 represents an optionally substituted alkyl radical, an alkenyl or alkinyl radical, an optionally substituted cycloalkyl radical or an optionally substituted phenyl or phenylalkyl radical, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, which optionally contains an oxygen atom as a further hetero-atom,or a physiologically acceptable acid addition salt thereof, which possess fungicidal properties. Processes for their preparation are also taught.
摘要翻译： 其中R 1表示任选取代的苯基或苯基烷基，具有多于1个碳原子的烷基，取代的烷基，链烯基或炔基或任选取代的环烷基，其中R 3代表下式的三取代的氰基胍： 任选取代的烷基或烯基或炔基，R 3表示任选取代的烷基，烯基或炔基，任选取代的环烷基或任选取代的苯基或苯基烷基，或R 2和R 3与氮原子一起 它们是键合的，表示任选地含有氧原子作为另外的杂原子的任选取代的杂环基，或其生理上可接受的酸加成盐，其具有杀真菌性。 还介绍了其准备过程。
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