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公开(公告)号：US4057544A
公开(公告)日：1977-11-08
申请号：US417527
申请日：1973-11-20
IPC分类号： C07D499/12 , A61K31/43 , A61P31/04 , C07D207/08 , C07D307/12 , C07D499/62 , C07D499/68 , C07D499/46
CPC分类号： C07D307/12 , C07D207/08
摘要： Novel penicillins of the formula ##STR1## wherein R is a branched chain alkyl group of from 3 to 14 carbon atoms, and their pharmaceutically acceptable salts, are easily absorbed in the blood and tissues through oral administration and show excellent antimicrobial activity against Gram-positive and Gram-negative bacteria, particularly against microorganisms of the genus Pseudomonas, such as Pseudomonas aeruginosa.
摘要翻译： 其中R为3〜14个碳原子的支链烷基及其药学上可接受的盐的新型青霉素通过口服给药容易地吸收在血液和组织中，并显示出优异的抗革兰氏阳性的抗微生物活性 和革兰氏阴性细菌，特别是针对假单胞菌属（Pseudomonas）的微生物，如铜绿假单胞菌（Pseudomonas aeruginosa）。
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2.发明授权Pharmaceutical preparation containing prostaglandin compound for rectal or vaginal administration 失效含有用于直肠或阴道给药的前列腺素化合物的药物制剂
公开(公告)号：US5491171A
公开(公告)日：1996-02-13
申请号：US232255
申请日：1994-07-27
申请人： Ken-ichi Nishimura , Akihisa Yoshimi , Takayoshi Mori , Nobuharu Kakeya , Masahiro Kikuchi , Nobuo Kondoh , Takeshi Uchida , Koichi Yamanouchi
发明人： Ken-ichi Nishimura , Akihisa Yoshimi , Takayoshi Mori , Nobuharu Kakeya , Masahiro Kikuchi , Nobuo Kondoh , Takeshi Uchida , Koichi Yamanouchi
IPC分类号： A61K9/02 , A61K31/557 , A61K47/12 , A61K31/20 , A61K31/19
CPC分类号： A61K9/02 , A61K31/557 , A61K47/12 , Y10S514/966 , Y10S514/967
摘要： A pharmaceutical preparation for rectal or vaginal administration, comprising a prostaglandin compound and an alkali metal salt of a fatty acid having 8 to 12 carbon atoms, and a method for administering a prostaglandin compound, comprising rectally or vaginally administering same in the presence of an alkali metal salt of a fatty acid.According to the present invention, absorption of prostaglandin from rectum or vagina can be enhanced.The prostaglandin can be stabilized in the preparation.
摘要翻译： PCT No.PCT / JP92 / 01431 Sec。 371日期：1994年7月27日 102（e）日期1994年7月27日PCT提交1992年11月5日PCT公布。 出版物WO93 / 08804 日期：1993年5月13日。一种用于直肠或阴道给药的药物制剂，其包含前列腺素化合物和具有8至12个碳原子的脂肪酸的碱金属盐，以及用于给予前列腺素化合物的方法，包括直肠或阴道给药相同 在存在脂肪酸的碱金属盐的情况下。 根据本发明，可以增强从直肠或阴道吸收前列腺素。 前列腺素可以在制剂中稳定。
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公开(公告)号：US5389625A
公开(公告)日：1995-02-14
申请号：US849019
申请日：1992-06-08
申请人： Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Ken-ichi Nishimura , Susumu Nishizawa , Nobuharu Kakeya
发明人： Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Ken-ichi Nishimura , Susumu Nishizawa , Nobuharu Kakeya
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/20 , C07D501/22
CPC分类号： C07D501/00 , Y02P20/55
摘要： Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.
摘要翻译： PCT No.PCT / JP90 / 01370 Sec。 371日期：1992年6月8日 102（e）日期1992年6月8日PCT 1990年10月24日PCT PCT。 出版物WO91 / 06549 日本1991年5月16日。式（I）r烷基和R 2的头孢菌素化合物是1-烷酰氧基烷基或1-烷氧基羰氧基烷基，其药学上可接受的盐，其制备方法及其药物用途。 头孢菌素化合物及其盐在消化道吸收方面优越，并且在消化道吸收时，作为水解产物在体内表现出广泛的抗微生物活性，此外，它们的甜度比蔗糖高10-400倍 。 因此，所述化合物可用作口服给药以预防和治疗细菌感染性疾病的药剂。
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4.发明授权
公开(公告)号：US4937242A
公开(公告)日：1990-06-26
申请号：US165705
申请日：1988-03-08
IPC分类号： A61K31/4427 , A61K31/455 , A61K31/55 , A61P3/00 , A61P9/12 , C07D211/90 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , C07D211/90 , C07D405/12
摘要： 1,4-Dihydropyridine derivatives of the general formula: ##STR1## wherein X.sup.1 and X.sup.2 independently represent hydrogen, fluoromethyl, fluoromethoxy, halogen, cyano, or nitro; R.sup.1 represents a lower alkyl; R.sup.2 represents acyl, alkoxycarbonyl, acylalkyl, an N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, heterocycle-alkyl, haloalkyl, alkenyl, or alkynyl; A represents an alkylene comprising a carbon atom to which 2 alkyls are bonded and having in total at least 5 carbon atoms; m represents the integer 1, 2 or 3; acid addition salts thereof; a method of production thereof; and pharmaceutical compositions containing such compound(s).Such compounds have pharmacological activities, in particular potent and long lasting hypotensive activity, coronary vasodilatation, cerebral vasodilatation, peripheral vasodilatation, renal vasodilatation and platelet aggregation inhibitory activity.
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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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公开(公告)号：US4026940A
公开(公告)日：1977-05-31
申请号：US624285
申请日：1975-10-20
IPC分类号： C07C309/70 , C07D307/12 , C07C143/68
CPC分类号： C07C309/70 , C07D307/12
摘要： .alpha.-Sulfophenylacetic acid derivatives of the general formula: ##STR1## (wherein R is a substituted or unsubstituted primary alcohol, cyclic alcohol or phenol compound residue), which are of value as intermediates of antibacterial agents, are selectively produced in a high yield by bringing a diester compound of the general formula: ##STR2## (wherein R has the same meaning as defined above) into contact with a strong acid.
摘要翻译： 通过以下方式选择性地制备具有下列通式的α-磺基苯乙酸衍生物：其中R为取代或未取代的伯醇，环醇或酚化合物残基）作为抗菌剂的中间体，以高产率由 得到通式如下的二酯化合物：其中R与上述定义相同）与强酸接触。
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7.发明授权Absorption-promoting compounds, compositions thereof with pharmaceuticals and/or bases for rectal administration and method of use 失效吸收促进化合物，其组合物与用于直肠给药的药物和/或碱基和使用方法
公开(公告)号：US4442090A
公开(公告)日：1984-04-10
申请号：US246953
申请日：1981-03-24
CPC分类号： A61K9/02 , A61K47/183 , Y10S424/15
摘要： Compounds satisfying four specific requirements, namely: (1) a log P value in the range of from 2.5 to 6, (2) a molecular structure with at least one carboxyl group, (3) a pKa value for the carboxyl group of not less than 2.5 and (4) absence of halo substitution, and nontoxic salts thereof promote absorption of pharmacologically-active substance through the rectum into the bloodstream and are effective to raise the concentration of such active substance in the bloodstream even when the active substance is usually unabsorbable or absorbable through the rectum only with considerable difficulty. The compounds are combined with pharmacologically-active ingredients, with pharmaceutical bases suitable for rectal administration of drugs and with appropriate combinations of both.
摘要翻译： 满足四个具体要求的化合物，即：（1）log值在2.5至6的范围内，（2）具有至少一个羧基的分子结构，（3）羧基的pKa值不低于 超过2.5和（4）不存在卤素取代，并且其无毒盐促进药物活性物质通过直肠吸收到血液中，并且有效地提高这种活性物质在血流中的浓度，即使活性物质通常是不可吸收的 或通过直肠吸收只有相当大的困难。 将化合物与药理学活性成分组合，其中适合于直肠给药的药物基质和两者的适当组合。
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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：US4048158A
公开(公告)日：1977-09-13
申请号：US645913
申请日：1975-12-31
IPC分类号： C07D499/04 , C07D499/00 , C07D499/62
CPC分类号： C07D499/00
摘要： Novel d-.alpha.-isobutylsulfobenzylpenicillin hemi-solvate crystals of the formula: ##STR1## (wherein A is a solvent selected from the class consisting of alcohols, ketones, ethers and esters) have excellent antibacterial activities and improved stability in terms of shelf-life.
摘要翻译： 下式的新型d-α-异丁基磺苄青霉素半溶剂化物晶体：其中A是选自醇，酮，醚和酯的溶剂，具有优异的抗菌活性和改善保质期的稳定性 。
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公开(公告)号：US3954826A
公开(公告)日：1976-05-04
申请号：US486835
申请日：1974-07-09
IPC分类号： C07C309/03 , C07C309/73 , C07D207/08 , C07D307/12 , C07D499/62 , C07C143/68
CPC分类号： C07D207/08 , C07C309/00 , C07D307/12
摘要： .alpha.-Sulfophenylacetic acid derivatives of the general formula: ##EQU1## (wherein R is a substituted or unsubsituted primary alcohol, cyclic alcohol or phenol compound residue), which are of value as intermediates of antibacterial agents, are selectively produced in a high yield by bringing a diester compound of the general formula: ##EQU2## (wherein R has the same meaning as defined above) into contact with a strong acid.
摘要翻译： 选择性地以高产率制备具有通式为-CHCOOH | SO 3 R（其中R为取代或未取代的伯醇，环醇或酚化合物残基）的α-磺基苯乙酸衍生物，其为抗菌剂的中间体 通过将具有通式：CH 3 | -CHCOO-C-CH 3 || SO 3 R CH 3（其中R具有与上述相同的含义）的二酯化合物与强酸接触。
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