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11. 发明授权

US4661470A Ester derivatives of antibiotic L 17046 失效
公开(公告)号：US4661470A
公开(公告)日：1987-04-28
申请号：US797295
申请日：1985-11-12
申请人： Adriano Malabarba , Ambrogio Magni , Paolo Strazzolini , Bruno Cavalleri , Aldo Trani
发明人： Adriano Malabarba , Ambrogio Magni , Paolo Strazzolini , Bruno Cavalleri , Aldo Trani
IPC分类号： A61K38/00 , A61P31/04 , C07K1/113 , C07K9/00 , C07K14/195 , C07K14/41 , A61K37/02 , C07K5/12
CPC分类号： C07K9/008 , Y10S930/19
摘要： The present invention is directed to ester derivatives at the carboxylic function of the glycopeptidic antibiotic substance called antibiotic L 17046 with antimicrobial activity mainly against gram-positive bacteria.

12. 发明授权

US4576746A Novel .beta.-lactam acetic acid derivatives 失效
标题翻译：新型β-内酰胺乙酸衍生物
公开(公告)号：US4576746A
公开(公告)日：1986-03-18
申请号：US354572
申请日：1982-03-04
申请人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D205/08 , C07D477/00 , C07D477/04 , C07D487/04
CPC分类号： C07D477/04 , C07C67/343 , C07D205/08
摘要： New .beta.-lactam acetic acid derivatives I ##STR1## wherein R represents alkyl, alkyl substituted with amino, protected amino, mono- or di-alkylamino, hydroxy, protected hydroxy or alkoxy, and alkenyl, and their salts are useful as intermediates for preparing 1-azabicyclo [3.2.0]hept-2-ene antibiotics II ##STR2## The process for preparing the .beta.-lactam acetic acid derivatives I as well as the overall process which starting from the acids I leads to the antibiotics II are also claimed.
摘要翻译：新的β-内酰胺乙酸衍生物I其中R代表烷基，被氨基，被保护的氨基，一或二 - 烷基氨基，羟基，被保护的羟基或烷氧基和烯基取代的烷基及其盐可用作制备1-氮杂双环[3.2.0]庚-2-烯抗生素II制备β-内酰胺乙酸衍生物I的方法以及从酸I引入抗生素II开始的总体方法是也声称。

13. 发明授权

US4501919A Process for the production of serine derivatives 失效
标题翻译：生产丝氨酸衍生物的方法
公开(公告)号：US4501919A
公开(公告)日：1985-02-26
申请号：US152447
申请日：1980-05-22
申请人： Melvin V. Koch , Ambrogio Magni
发明人： Melvin V. Koch , Ambrogio Magni
IPC分类号： C07B41/02 , B01J31/02 , C07B31/00 , C07B61/00 , C07C67/00 , C07C227/16 , C07C229/22 , C07C229/36 , C07C255/59 , C07C51/353
CPC分类号： C07C227/16
摘要： Serine derivatives are synthesized by the condensation of an alkali metal salt of a glycine derivative and a carbonyl compound in the presence of a phase transfer catalyst.
摘要翻译：丝氨酸衍生物在相转移催化剂存在下，通过甘氨酸衍生物的碱金属盐与羰基化合物的缩合而合成。

14. 发明授权

US4459302A Acyl-1H-1,2,4-triazole derivatives 失效
公开(公告)号：US4459302A
公开(公告)日：1984-07-10
申请号：US87375
申请日：1979-10-23
申请人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
IPC分类号： A61K31/41 , C07D233/54 , C07D249/08 , C07D249/12 , C07D405/04
CPC分类号： C07D233/64 , C07D233/54 , C07D249/08 , Y10S514/841
摘要： New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenacyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, halo and dimethylamino;R.sub.2 may represent a (C.sub.1-4)alkyl radical or the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also represent a methylenedioxy group; with the proviso that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 wherein R.sub.5 and R.sub.6 are as above defined;and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.

15. 发明授权

US4427656A Antibiotic A/16686 factor A.sub.2, the process for the preparation thereof and the co-produced antibiotic A/16686 factors A.sub.1 and A.sub.3 失效
标题翻译：抗生素A / 16686因子A2，其制备方法和共同生产的抗生素A / 16686因子A1和A3
公开(公告)号：US4427656A
公开(公告)日：1984-01-24
申请号：US288718
申请日：1981-07-31
申请人： Bruno Cavalleri , Enrico Selva
发明人： Bruno Cavalleri , Enrico Selva
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , C12N1/20 , C12P1/06 , C12R1/045 , A61K35/00 , C12R1/45
CPC分类号： C12R1/045 , C12P1/06 , Y10S435/827
摘要： The present invention refers to a chlorine containing antibiotic substance, named antibiotic A/16686 factor A.sub.2, in an essentially pure form. The invention also relates to the process for the production of antibiotic A/16686 factors A.sub.2 by cultivation of an Actinoplanes strain and to the co-produced antibiotic A/16686 factos A.sub.1 and A.sub.3. Antibiotic A/16686 factors A.sub.1, A.sub.2 and A.sub.3 as well as the corresponding non-toxic physiologically acceptable acid addition salts are antimicrobial agents particularly active against gram-positive bacteria.
摘要翻译：本发明涉及一种基本上纯的形式的含氯抗生素物质，称为抗生素A / 16686因子A2。本发明还涉及通过培养Actinoplanes菌株和共同生产的抗生素A / 16686事实A1和A3生产抗生素A / 16686因子A2的方法。抗生素A / 16686因子A1，A2和A3以及相应的无毒生理学上可接受的酸加成盐是对革兰氏阳性细菌特别有活性的抗微生物剂。

16. 发明授权

US4391817A Pyrrolo-diazepine derivatives and their pharmaceutical compositions 失效
标题翻译：吡咯并二氮杂衍生物及其药物组合物
公开(公告)号：US4391817A
公开(公告)日：1983-07-05
申请号：US381271
申请日：1982-05-24
申请人： Luigi Mariani , Giorgio Tarzia
发明人： Luigi Mariani , Giorgio Tarzia
IPC分类号： A61K31/55 , A61P25/08 , A61P25/20 , C07D487/04
CPC分类号： C07D487/04
摘要： A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.
摘要翻译：一类具有抗惊厥和抗焦虑活性的吡咯并二氮杂通式为其中R为（C 1 -C 4）烷基，R 1为氯，溴或硝基，R 2为氢或（C 1 -C 4）烷基并且R 3是氢，氯，溴，氟，三氟甲基或甲氧基。新化合物从其中R 1是通过卤化或硝化的氢的相应化合物开始制备。还描述了含有新的式I化合物的药物制剂。

17. 发明授权

US4276382A Antibiotic substances 失效
标题翻译：抗生素物质
公开(公告)号：US4276382A
公开(公告)日：1981-06-30
申请号：US718727
申请日：1976-08-30
申请人： Francesco Parenti , Carolina Coronelli , Giorgio Tamoni , Giancarlo Lancini
发明人： Francesco Parenti , Carolina Coronelli , Giorgio Tamoni , Giancarlo Lancini
IPC分类号： C12P1/04 , C12N1/20 , C12P21/00 , C12R1/045
CPC分类号： C12P1/04
摘要： The antibiotic gardimycin and process for producing said antibiotic by fermentation of strains belonging to the genus Actinoplanes.
摘要翻译：抗生素gardimycin和通过发酵属于Actinplanes属的菌株产生所述抗生素的方法。

18. 发明授权

US4274286A Powder flowability test equipment 失效
标题翻译：粉末流动性试验设备
公开(公告)号：US4274286A
公开(公告)日：1981-06-23
申请号：US64150
申请日：1979-08-06
申请人： Alberto Gioia
发明人： Alberto Gioia
IPC分类号： G01N1/10 , G01N11/02 , G01N33/00 , G01N11/04
CPC分类号： G01N11/02 , G01N2001/1006 , G01N2033/0091
摘要： An apparatus for measuring the flowability of powder utilizes a container having a bottom wall with an opening therein. The bottom wall may be changed to provide openings of different sizes. The test consists of allowing the powder to flow through successively smaller holes. The smallest hole size through which the powder will freely flow is a measure of its flowability.
摘要翻译：用于测量粉末流动性的装置利用具有其中具有开口的底壁的容器。可以改变底壁以提供不同尺寸的开口。测试包括允许粉末连续地流过更小的孔。粉末将自由流动的最小孔尺寸是其流动性的量度。

19. 发明授权

US4144234A Preparation of rifamycin P and Q derivatives 失效
标题翻译：制备利福霉素P和Q衍生物
公开(公告)号：US4144234A
公开(公告)日：1979-03-13
申请号：US796290
申请日：1977-05-12
申请人： Renato Cricchio
发明人： Renato Cricchio
IPC分类号： A61K31/425 , A61P31/04 , C07D498/08 , C07D513/18
CPC分类号： C07D498/08 , C07D513/18
摘要： A method for preparing thiazolorifamycin derivatives from rifamycin S and a cysteine ester to produce an intermediate product which is cyclized to thiazolorifamycin and the novel products formed therefrom.
摘要翻译：一种从利福霉素S和半胱氨酸酯制备噻唑霉素衍生物的方法，以产生环化成噻唑霉素的中间产物和由其形成的新产物。

20. 发明授权

US4143055A 2,4,6-Trisubstituted-2,3-dihydro-benzofuran derivatives 失效
标题翻译： 2,4,6-三取代-2,3-二氢苯并呋喃衍生物
公开(公告)号：US4143055A
公开(公告)日：1979-03-06
申请号：US890158
申请日：1978-03-27
申请人： Emilio Occelli
发明人： Emilio Occelli
IPC分类号： C07D307/79
CPC分类号： C07D307/79 , Y10S514/916
摘要： New 2,4,6-trisubstituted-2,3-dihydro-benzofuran derivatives of the following general formula ##STR1## wherein R is selected from hydrogen or methyl; one of R.sub.1 and R.sub.2 represents hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)alkanoyloxy, and the other one is selected from cyano, carboxy, carbo(C.sub.1-4)alkoxy, carbamoyl and a --NR.sub.3 R.sub.4 group, wherein R.sub.3 and R.sub.4 independently represent hydrogen (C.sub.1-4)alkyl, (C.sub.2-4)alkanoyl, carbo(C.sub.1-4)alkoxy, carbobenzyloxy, carbamoyl, mono- and di-(C.sub.1-4)alkylamino-(C.sub.1-4)alkyl, benzenesulfonyl, toluenesulfonyl, (C.sub.1-4)alkylsulfonyl or phenacylsulfonyl; and salts therewith of pharmaceutically acceptable acids. The compounds have antinflammatory, analgesic and antipyretic utility.

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