Abstract: The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.

Abstract: An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R0 represents hydrogen atom or the like; R1 represents C1-C3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH2(CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH2—, —NRaCH2— (wherein Ra represents hydrogen atom, optionally substituted C1-C4 alkyl group or the like) or the like.

Abstract: An antimicrobial combination medicament for injection comprising a ?-lactam compound represented by the formula [1], wherein R1 is lower alkyl or the like, R2 is H or lower alkyl group, X is O, S or NH; m and n are 0 to 4, provided that the sum of m and n is 0 to 4; Y1 is halogen or the like; and Y2 is hydrogen, optionally substituted lower alkyl group or the like; and carbapenems such as meropenem.

Abstract: Carbapenem compounds represented by the general formula [1] or pharmaceutically acceptable salts thereof: wherein R1 is C1-C3 alkyl or hydroxylated C1-C3 alkyl, R is hydrogen atom or a group which is hydrolyzed in vivo into a carboxy group, and G is a group represented by one of the formulae [G1], [G2], and [G3].

Abstract: A carbapenem compound represented by a following formula [1], wherein R1 is C1 to C3 alkyl or C1 to C3 alkyl substituted by hydroxy. R is hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body, A is a following formula [1a], wherein E is a 5 to 7 membered cyclic ring optionally containing 1 to 3 hetero atoms (excluding benzene ring) which forms a bicyclic ring in corporation with the benzene ring, Y is hydrogen atom, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethoxy, halogen atom or cyano group, or its pharmaceutically acceptable salt.

Abstract: A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing ?-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as ?-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.

Abstract: 1. A ?-lactam compound of the formula [1]; wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, —C(R3)?NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.

Abstract: Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: wherein Ring E is benzene ring or thiophene ring; R1 is optionally OH-substituted C1-3 alkyl; R2 and R3 represent each H, optionally substituted lower alkyl, etc.; R is H, or a group which is hydrolyzed in the living body to regenerate a carboxyl group, etc.; X is O or S; and Y represents H, lower alkyl, etc., or pharmaceutically acceptable salts thereof and medicaments containing said compound as the active ingredient.

Abstract: Carbapenem compounds represented by the general formula [1] or pharmaceutically acceptable salts thereof: wherein R1 is C1-C3 alkyl or hydroxylated C1-C3 alkyl, R is hydrogen atom or a group which is hydrolyzed in vivo into a carboxy group, and G is a group represented by one of the formulae [G1], [G2], and [G3].

Abstract: Novel preparations comprising bacterial cell wall skeleton components and determinations of bacterial cell wall skeleton components are provided. The invention comprises a paste consisting of bacterial cell wall skeleton components (bacteria-CWS) and an oil, and make it possible to provides a paste comprising bacteria-CWS wherein the paste has a viscosity of 0.2 to 0.7 poise (25° C.), an emulsion comprising the same, and a lyophilized formulation. The invention also make it possible to provides evaluation of a pharmaceutical composition comprising bacterial cell wall skeleton components as an effective ingredient, and an intermediate material thereof, assay of their strength, and identification of an effective ingredient by determining the long-chain fatty acid comprised in the bacterial cell wall skeleton components, or a derivative thereof.

Abstract: A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing ?-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as ?-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.

Abstract: 1.

Abstract: Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: 1

Abstract: Novel &bgr;-lactam compound of the formula [1]: wherein R1 is lower alkyl or hydroxy-substituted lower alkyl, R2 is H or lower alkyl, X is O or, S, R3 is H, metal or protecting group, W is a 6- or 7-membered nitrogen-containing heterocycle optionally being substituted at carbon atoms. Said &bgr;-lactam compound shows excellent antibacterial activity against Gram-positive bacteria, particularly against methicillin-resistant Staphylococcus aureus and methicillin-resistant and coagulase-negative Staphylococcus aureus.

Abstract: A &bgr;-lactam compound of the formula: wherein R1 is lower alkyl or OH-substituted lower alkyl, R2 is H or lower alkyl, X is O, S or NH, n is 1 to 3, R3 is —C(Ra)═NH (Ra is H, lower alkyl or substituted lower alkyl), or a salt thereof, or an ester thereof. These compounds show excellent antibacterial activity against Gram-positive bacteria, particularly against methicillin-resistant Staphylococci and methicillin-resistant and coagulase-negative Staphylococci.

Abstract: A novel .beta.-lactam compound of the formula ?1!: ##STR1## or a pharmaceutically acceptable salt thereof, which shows an excellent antibacterial activity against Gram-positive bacteria, especially against methicillin-resistant staphylococci and methicillin-resistant coagulase-negative staphylococci, and a process for producing the same. R.sub.1, R.sub.2, X, Y, Z are as defined in the specifacation.

Abstract: Novel and effective process for preparing a carbapenem compound of the formula (III): ##STR1## wherein R.sub.1 and R.sub.2 are each H or lower alkyl, R.sub.3 is lower alkyl, R.sub.4 is a protecting group, L is substituted or unsubstituted arylsulfonyloxy, lower alkanesulfonyloxy, halogeno-lower alkanesulfonyloxy, di-lower alkylphosphoryloxy, etc., and X is H or protected hydroxy, which comprises reacting a .beta.-lactam compound (I) with an acetic acid ester derivative (II), in the presence of base, followed by treating the product with an active esterifying agent for a hydroxy group, said compound (III) being useful as intermediate in preparing 1.beta.-alkylcarbapenem compounds having antibacterial activity.

Abstract: A beta-lactam compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, the same or different, each a hydrogen atom or a lower alkyl group, R.sub.3.sup.o is a lower alkyl group having a beta-configuration, R.sub.4 is a carboxyl-protecting group, X is a hydrogen atom or a protected hydroxyl group and COZ is a protected thiolcarboxyl group, which is useful as a valuable intermediate in the stereospecific production of 1-alkylcarbapenem compounds.

Abstract: Pyrrolidine derivatives of the formula (1): ##STR1## wherein R is a protective group of the amino group, intermediates for constructing the 2-positioned side chain of antibacterial penem and carbapenem compounds, are prepared by allowing ##STR2## to react with active esterifying agents in the presence of a base, further allowing the product to react with hydrogen sulfide in the presence of a base and then treating the product with a base.

Abstract: A beta-lactam compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, the same or different, each a hydrogen atom or a lower alkyl group, R.sub.3.sup.0 is a hydroen atom or a lower alkyl group having a beta-configuration, R.sub.4 is a carboxyl-protecting group, X is a hydrogen atom or a protected hydroxyl group and COZ is a protected thiolcarboxyl group, which is useful as a valuable intermediate in the stereospecific production of 1-alkylcarbapenem compounds.