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公开(公告)号：US4605651A
公开(公告)日：1986-08-12
申请号：US540676
申请日：1983-10-11
IPC分类号： C07D501/36 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , B60J10/08 , C07D20060101 , C07D501/04 , C07D501/24 , C07D501/32 , C07D501/34 , C07D501/44 , C07D501/46 , C07D501/54
CPC分类号： C07D501/36 , B60J10/248 , B60J10/86 , C07D501/34
摘要： 1. A cephalosporin derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two lower alkyl groups at the amino group thereof, R.sup.2 is an 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl or 5-methyl-1,3-dioxolen-2-on-4-ylmethyl group, R.sup.3 is a carbamoyloxymethyl group, which may optionally be substituted by one or two lower alkyl groups, or a heterocyclothiomethyl group, which may optionally be substituted by one or more appropriate substituents, and R.sup.4 is a hydrogen atom or a hydroxy group, or its non-toxic salt 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： 1.通式为其中R1是通过一个或两个低级烷基取代的α-，β-或γ-氨基酸残基（通过酯键键合）的头孢菌素衍生物 在其氨基上，R 2是1-烷酰氧基烷基，1-烷氧基羰氧基烷基，苯酞或5-甲基-1,3-二氧杂环戊烯-2-对4-基甲基，R3是氨基甲酰氧基甲基，其可以任选地被 一个或两个低级烷基或杂环硫基甲基，其可任选地被一个或多个适当的取代基取代，并且R4是氢原子或羟基，或其无毒性盐被用作可口服的抗生素 对革兰氏阳性和革兰氏阴性细菌均具有广泛的抗菌活性。
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公开(公告)号：US4943567A
公开(公告)日：1990-07-24
申请号：US228714
申请日：1988-05-27
申请人： Susumu Nishizawa , Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Syouzi Kamiya , Nobuharu Kakeya , Kazuhiko Kitao
发明人： Susumu Nishizawa , Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Syouzi Kamiya , Nobuharu Kakeya , Kazuhiko Kitao
IPC分类号： C07D277/20 , C07D277/38 , C07D285/08 , C07D501/20 , C07D501/34 , C07D501/36
CPC分类号： C07D277/587 , C07D285/08 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.
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3.发明授权
公开(公告)号：US4847286A
公开(公告)日：1989-07-11
申请号：US46882
申请日：1987-03-27
申请人： Satoshi Tamaki , Masaru Kitagawa , Hirokazu Tsuda , Susumu Nishizawa , Nobuhara Kakeya , Kazuhiko Kitao
发明人： Satoshi Tamaki , Masaru Kitagawa , Hirokazu Tsuda , Susumu Nishizawa , Nobuhara Kakeya , Kazuhiko Kitao
IPC分类号： A61K31/35 , A61K31/352 , A61P37/08 , C07D311/24 , C07D407/14
CPC分类号： C07D407/14 , C07D311/24
摘要： Cromoglycic acid derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (for ester bonding) whose amino group may optionally be substituted by at least one lower alkyl group, and R.sup.2 and R.sup.3 each independently is a lower alkyloxy-substituted or an unsubstituted lower alkyl group, an 1-alkanoyloxyalkyl group, an 1-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1,3-dioxol-2-on-4-ylmethyl group; nontoxic salts thereof; and pharmaceutical compositions containing such compounds. Since the compounds have antiallergic activity and are readily absorbable into the blood stream, they are useful as oral antiallergic agents.
摘要翻译： PCT No.PCT / JP86 / 00415 Sec。 371日期1987年3月27日 102（e）1987年3月27日PCT申请1986年8月13日PCT公布。 出版物WO87 / 01115 日本1987年2月26日。通式（Ⅰ）的亮氨酸衍生物（Ⅰ）其中R1是一个α-，β-或γ-氨基酸残基（用于酯键），其氨基可以任选被至少 一个低级烷基，R 2和R 3各自独立地为低级烷氧基取代或未取代的低级烷基，1-烷酰氧基烷基，1-烷氧基羰氧基烷基，苯酞基或5-甲基-1,3-二氧杂环戊烯 -2-对 - 4-基甲基; 无毒盐; 和含有这些化合物的药物组合物。 由于这些化合物具有抗过敏活性并且容易吸收到血液中，所以它们可用作口服抗过敏剂。
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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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5.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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6.发明授权
公开(公告)号：US4338306A
公开(公告)日：1982-07-06
申请号：US149132
申请日：1980-05-12
申请人： Kazuhiko Kitao , Ken-ichi Nishimura
发明人： Kazuhiko Kitao , Ken-ichi Nishimura
CPC分类号： A61K9/02 , A61K47/12 , Y10S424/15 , Y10S514/946 , Y10S514/966
摘要： Fatty acids having 8 to 14 carbon atoms, leucinic acid and nontoxic salts thereof promote the absorption of a pharmacologically-active substance through the rectum into the blood stream and effectively raise the concentration of such active substance in the blood stream even when said active substance is one which is usually absorbable through the rectum only with considerable difficulty.
摘要翻译： 碳原子数为8〜14的脂肪酸，亮氨酸及其无毒盐促进药物活性物质通过直肠向血液中的吸收，并有效地提高血液中的活性物质的浓度，即使所述活性物质为 通常通过直肠可以吸收的是相当困难的一种。
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7.发明授权
公开(公告)号：US4485033A
公开(公告)日：1984-11-27
申请号：US365021
申请日：1982-04-02
申请人： Kazuhiko Kitao , Ken-ichi Nishimura
发明人： Kazuhiko Kitao , Ken-ichi Nishimura
CPC分类号： A61K9/02 , A61K47/12 , Y10S424/15 , Y10S514/946 , Y10S514/966
摘要： Fatty acids having 8 to 14 carbon atoms, leucinic acid and nontoxic salts thereof promote the absorption of a pharmacologically-active substance through the rectum into the blood stream and effectively raise the concentration of such active substance in the blood stream even when said active substance is one which is usually absorbable through the rectum only with considerable difficulty.
摘要翻译： 碳原子数为8〜14的脂肪酸，亮氨酸及其无毒盐促进药物活性物质通过直肠向血液中的吸收，并有效地提高血液中此类活性物质的浓度，即使所述活性物质为 通常通过直肠可以吸收的是相当困难的一种。
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