Abstract: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an ?-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

Abstract: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an ?-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

Abstract: To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.

Abstract: An epoxysuccinamic acid derivartive represented by the formula: ##STR1## (wherein R.sup.1 is an alkyl group having 1 to 10 carbon atoms, a phenyl group or a benzyl group), a pharmaceutically acceptable salt thereof, and an intermediate thereof are disclosed The compound of Formula I is useful as a therapeutical agent for muscular atrophy diseases.

Abstract: An epoxysuccinic acid derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, and a pharmaceutically acceptable salt are useful as cathepsin B inhibitors.

Abstract: A cephalosporin derivative represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group of the amino group, R.sup.2 is a hydrogen atom or a protecting group of the hydroxyl group, R.sup.3 is a hydrogen atom or a protecting group of the carboxyl group, and R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, and the non-toxic salts thereof are useful as antibacterial agents.

Abstract: A cephalosporin derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group of the amino group, R.sup.2 is a hydrogen atom or a protecting group of the hydroxyl group, R.sup.3 is a hydrogen atom or a protecting group of the carboxyl group, X is a halogen atom, a cyano group, a vinyl group, a lower alkoxy group having 1 to 4 carbon atoms or a lower alkylthio group having 1 to 4 carbon atoms and n is an integer of 1 to 3, and a non-toxic salt thereof are useful as antibacterial agents for oral administration.

Abstract: Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

Abstract: Cephalosporin derivatives represented by the general formula ##STR1## wherein X represents a halogen atom, a hydroxyl group, a cyano group, a trifluoromethyl group, an amino group, a lower alkylcarbonylamino group, a lower alkoxy group, a lower alkylthio group, a lower alkoxycarbonyl group, a carbamoyl group, a substituted carbamoyl group, a carbamoyloxy group, a lower alkylcarbonyl group, a lower alkenyl group, an ethynyl group, a thiocyanate group, an .alpha.-carboxyaminomethyl group, a phenyl group, a pyridinyl group or an aminothiazolyl group, and n is an integer of 1 to 3, and the non-toxic salts thereof, are disclosed. These compounds are useful as antibacterial agents.

Abstract: Cephalosporin derivatives represented by the general formula ##STR1## Wherein X represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, an allyl group, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

Abstract: Novel cephalosporin compounds having the general formula ##STR1## wherein X represents hydrogen atom or hydroxy group, and the non-toxic pharmacologically acceptable salts thereof are disclosed. These compounds are useful as antibacterial agents.

Abstract: Novel penicillin derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or hydroxy, are produced by acylating ampicillin, amoxicillin or a salt thereof with 4-hydroxy-pyrazino[2,3-f]quinoline-3-carboxylic acid or its functional derivative. They have high anti-pseudomonas activity and other antibacterial activity against gram-positive and gram-negative bacteria, and are of extremely low toxicity.