Kyoto Pharmaceutical Industries, Ltd.

The Green Cross Corporation

Kyoto Yakuhin Kogyo Kabushiki Kaisha

Nobuharu Kakeya

Kazuhiko Kitao

Ken-ichi Nishimura

Susumu Nishizawa

Masayasu Kasai

Hiroyuki Muro

Takayoshi Mori

Satoru Hatano

Hiroshi Matsui

Akihisa Yoshimi

Masahiro Kikuchi

Koichi Yamanouchi

Takeshi Uchida

Fumio Fukata

Nobuo Kondoh

Satoshi Tamaki

Syouzi Kamiya

Pharmaceutical preparation containing prostaglandin compound for rectal

Cephalosporin compounds

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.

Cephalosporin compound and pharmaceutical composition thereof

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.

1,4-dihydropyridine derivatives and pharmaceutical composition thereof

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.

Antibiotic amino acid derivatives of cephalosporins

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.

Absorption-promoting compounds, compositions thereof with

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Nagaokakyo, Japan

Nobuharu Kakeya