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公开(公告)号：US4609650A
公开(公告)日：1986-09-02
申请号：US594034
申请日：1984-03-27
IPC分类号： A61K31/565 , C07J1/00 , C07J41/00 , A61K31/56
CPC分类号： C07J41/0044 , C07J1/0074
摘要： A novel steroid compound of the formula ##STR1## wherein A is a lower alkylene group; ##STR2## is an acyl group; and is a single bond or a double bond, and methods of producing the compound (I) as follows: ##STR3## and a pharmaceutical composition containing the compound (I). The compound (I) exhibits excellent antiandrogenic activity on oral administration and can be used for the treatment of prostatic hypertrophy.
摘要翻译： 式（I）的新型类固醇化合物，其中A为低级亚烷基;
是酰基; 并且是单键或双键，以及如下制备化合物（I）的方法：（I）和含有化合物（I）的药物组合物， 。 化合物（I）对口服给药具有优异的抗雄激素活性，可用于治疗前列腺肥大。 -
公开(公告)号：US4497809A
公开(公告)日：1985-02-05
申请号：US486820
申请日：1983-04-20
IPC分类号： A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07C69/63 , C07D20060101 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36
摘要： Cephalosporin derivatives of the formula: ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is a straight-chain or branched alkyl group of 5 to 7 carbon atoms, and their pharmaceutically acceptable salts, which are effective as orally administrable antibiotic agents against both gram-positive- and negative-bacteria, and the production and compositions thereof, are proposed.
摘要翻译： 下式的头孢菌素衍生物：其中R1是甲基或乙基，R2是5至7个碳原子的直链或支链烷基，以及它们的药学上可接受的盐，其作为口服给药的抗生素 提出了阳性和阴性细菌及其生产和组成。
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公开(公告)号：US4189479A
公开(公告)日：1980-02-19
申请号：US863071
申请日：1977-12-22
IPC分类号： C07D501/36
CPC分类号： C07D501/36
摘要： Novel cephalosporin derivatives, namely pivaloyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]-ceph-3-em-4-carboxylate and its pharmaceutically acceptable acid addition salts are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.
摘要翻译： 新颖的头孢菌素衍生物，即7β-[2-（2-氨基噻唑-4-基）乙酰氨基] -3 - [[[1-（2-二甲基氨基乙基）-1H-嘌呤-5-基]硫基]甲基的新戊酰氧基甲基] 发现3-头孢-3-烯-4-羧酸酯及其药学上可接受的酸加成盐可用作具有针对革兰氏阳性菌和革兰氏阴性细菌的广泛抗微生物活性的可口服抗生素。
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公开(公告)号：US5120841A
公开(公告)日：1992-06-09
申请号：US027433
申请日：1987-03-18
IPC分类号： C07D501/36 , A61K31/54 , A61K31/545 , A61K31/546 , A61P31/04 , C07C67/08 , C07D20060101 , C07D257/04 , C07D277/22 , C07D499/42 , C07D501/00 , C07D501/02 , C07D501/04 , C07D501/20 , C07D501/34 , C07D501/46 , C07D501/56
CPC分类号： C07D501/36
摘要： A compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is an unsubstituted or lower alkyl-substituted alicyclic alkyl group of 3 to 12 carbon atoms or a C.sub.3-6 alicyclic alkyl-substituted lower alkyl group or a pharmaceutically acceptable salt thereof, processes for preparing the same, a pharmaceutical composition thereof are provided. The compound has an improved absorbability and can be orally applied as antibiotics.
摘要翻译： 下式的化合物：其中R 1是氢原子或低级烷基; R2是3-12个碳原子的未取代或低级烷基取代的脂环族烷基或C3-6脂环族烷基取代的低级烷基或其药学上可接受的盐，其制备方法，其药物组合物。 该化合物具有改善的吸收性，可作为抗生素口服使用。
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公开(公告)号：US4826834A
公开(公告)日：1989-05-02
申请号：US909942
申请日：1986-09-22
IPC分类号： C07D519/00 , A61K31/545
CPC分类号： C07D519/00 , Y02P20/55
摘要： A compound having the general formula ##STR1## wherein, R.sup.0 is a hydrogen atom, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; Z is S, S.fwdarw.O,O or CH.sub.2 ; R.sup.4 is a hydrogen atom, a methoxy group, or a formamide group; R.sup.13 is a hydrogen atom, a methyl group, a hydroxyl group, or a halogen atom; A.sym. is a condensed triazolio group which may be substituted, or a pharmaceutically acceptable salt or ester thereof is novel and has an excellent antibacterial activity.
摘要翻译： 具有通式
的化合物，其中R 0是氢原子，含氮杂环基，酰基或氨基保护基; Z是S，S-> O，O或CH 2; R4是氢原子，甲氧基或甲酰胺基; R 13是氢原子，甲基，羟基或卤素原子; A（+）是可被取代的缩合的三唑基，或其药学上可接受的盐或酯是新颖的，具有优异的抗菌活性。 -
公开(公告)号：US4729992A
公开(公告)日：1988-03-08
申请号：US724927
申请日：1985-04-19
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： A compound of the formula: ##STR1## or a pharmaceutical acceptable salt thereof, processes for preparing the same and a pharmaceutical composition containing the compound or the salt thereof mentioned above are provided. The compound has antibiotic activity and has improved absorbability.
摘要翻译： 提供下式的化合物或其药学上可接受的盐，其制备方法和含有上述化合物或其盐的药物组合物。 该化合物具有抗菌活性并具有改善的吸收性。
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公开(公告)号：US4316018A
公开(公告)日：1982-02-16
申请号：US147053
申请日：1980-05-06
IPC分类号： C07D501/00 , A61K20060101 , A61K31/545 , A61K31/546 , C07D20060101 , C07D501/02 , C07D501/04 , C07D501/06 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/56
CPC分类号： C07D501/36
摘要： Crystallized cephalosporin salts, particularly crystalline addition salt of pivaloyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylate with hydrochloric acid, tartaric acid or citric acid, which is very stable and is readily adsorbable through intestinal tract, with little individual differences, when the salt is applied orally.
摘要翻译： 3β-[2-（2-氨基噻唑-4-基）乙酰氨基] -3 - [[[1-（2-二甲基氨基乙基）-1H-嘌呤-5-基]]的新戊酰氧基甲基酯结晶加成盐， 硫代]甲基]头孢-3-烯-4-羧酸盐与盐酸，酒石酸或柠檬酸反应，当盐被口服时，它是非常稳定的并且通过肠道容易吸附，几乎没有个体差异。
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公开(公告)号：US4839351A
公开(公告)日：1989-06-13
申请号：US941069
申请日：1986-12-12
IPC分类号： C07D519/06 , A61K31/545 , A61P31/04 , C07D463/00 , C07D501/36 , C07D505/00 , C07D519/00
CPC分类号： C07D505/00 , C07D463/22 , Y02P20/55
摘要： A compound of the general formula: ##STR1## wherein R.sup.0 is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S.fwdarw.O, O or CH.sub.2 ; R.sup.4 is hydrogen, methoxy group or formamido group; R.sup.13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other,or a salt or ester thereof.and a process for preparing the same and a pharmaceutical composition thereof are disclosed.
摘要翻译： 通式为：其中R 0为氢，含氮杂环基，酰基或氨基保护基的化合物。 A是S，S-> O，O或CH 2; R4是氢，甲氧基或甲酰氨基; R 13是氢，甲基，羟基或卤素; A是通过将咪唑或吡唑环与5-或6-元含氮芳族杂环相结合而形成的任选取代的稠合环状基团，以共价C-N键或其盐或酯。 并公开了其制备方法及其药物组合物。
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9.发明授权
公开(公告)号：US5449902A
公开(公告)日：1995-09-12
申请号：US168884
申请日：1993-12-16
申请人： Kouzi Onishi , Norio Tada , Yoshinobu Yoshimura , Yoshiaki Kato
发明人： Kouzi Onishi , Norio Tada , Yoshinobu Yoshimura , Yoshiaki Kato
CPC分类号： H01J49/0431 , G01N30/728 , G01N35/085 , G01N2030/027 , G01N2030/8411
摘要： An apparatus for directly connecting an analytical column and a mass spectrometer comprising a fixed member having at least four holes which respectively introduce washing solution, eluate containing a component eluted from the analytical column, desalting solution and eluent for eluting the component, and a movable member rotated with respect to an axis having at least four tubes around the axis and mounting the four trapping columns, whereby the trapping columns are respectively washed, trapped, desalted and eluted in parallel. Furthermore, a common trapping column may be used instead of the four trapping columns by controlling the apparatus with four analytical modes.
摘要翻译： 一种用于直接连接分析柱和质谱仪的装置，包括具有至少四个孔的固定构件，其分别引入洗涤溶液，含有从分析柱洗脱的组分的洗脱液，脱盐溶液和用于洗脱组分的洗脱液;以及可移动构件 相对于围绕轴线具有至少四个管的轴线旋转并安装四个捕集柱，由此分别洗涤，捕获，脱盐和洗脱平行的捕集柱。 此外，通过使用四种分析模式控制该装置，可以使用公共捕集塔来代替四个捕集塔。
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公开(公告)号：US4260607A
公开(公告)日：1981-04-07
申请号：US76545
申请日：1979-09-18
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36
摘要： A cephalosporin derivative of the formula: ##STR1## wherein R represents ##STR2## or its pharmaceutically acceptable acid addition salt is found to be useful as orally administrable antibiotics having broad anti-microbial activities against both Gram-positive and Gram-negative bacteria.
摘要翻译： 发现下式的头孢菌素衍生物：其中R代表“IMA”或其药学上可接受的酸加成盐，可用作对革兰氏阳性菌和革兰氏阴性菌具有广泛抗微生物活性的可口服抗生素。
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