Abstract: Provided is a compound represented by Formula (1).

Abstract: A process for producing crystals of a compound represented by the following formula (I): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.

Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.

Abstract: Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P1 and P2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The present invention also relates to a composition comprising at least 95% of the intermediate of Ertapenem of formula 2a.

Abstract: The present invention relates to an improved method for synthesizing meropenem trihydrate[(1R,5S,6S)-2-[((2?S,4?S)-2?-dimethylaminocarbozyl)pyrrolidin-4?-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid, trihydrate], which is a novel carbapenem antibiotic.

Abstract: The present invention provides a doripenem intermediate compound shown by formula (XIV), wherein PNB is p-nitrobenzyl, and HX is an acid; and when HX is a monobasic acid, n=1; and when HX is a polybasic acid, n=2. The present invention also provides a process for preparing the doripenem intermediate compound (XIV). In addition, the present invention provides a process for preparing doripenem (I) from the doripenem intermediate compound (XIV) in a simple manner, with a high yield and low production costs. The new mono-protected doripenem intermediate compound provided in the present invention contains only one protecting group, reducing the difficulty and complexity in the subsequent de-protection step by catalytic hydrogenation, increasing the yield of the catalytic hydrogenation reaction, and thus reducing the production cost of the final product. The process is easy to operate and suitable for industrialized production.

Abstract: Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw material. The crystalline form E can be easily filtered and dried, the properties in the drying process are stable, and the purity of the crystal is high and can be up to 98.5% or higher.

Abstract: The present invention relates to a process for the preparation of pure meropenem trihydrate.

Abstract: The present invention provides a doripenem intermediate compound shown by formula (XIV), wherein PNB is p-nitrobenzyl, and HX is an acid; and when HX is a monobasic acid, n=1; and when HX is a polybasic acid, n=2. The present invention also provides a process for preparing the doripenem intermediate compound (XIV). In addition, the present invention provides a process for preparing doripenem (I) from the doripenem intermediate compound (XIV) in a simple manner, with a high yield and low production costs. The new mono-protected doripenem intermediate compound provided in the present invention contains only one protecting group, reducing the difficulty and complexity in the subsequent de-protection step by catalytic hydrogenation, increasing the yield of the catalytic hydrogenation reaction, and thus reducing the production cost of the final product. The process is easy to operate and suitable for industrialized production.

Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

Abstract: The present invention relates to a process for the preparation of carbapenem compound of Formula (I), wherein P1 is hydrogen or a carboxyl protecting group, P3 is hydrogen or a hydroxyl protecting group, R1 is C1-3 alkyl, and A is selected from a group consisting of a) Formula (II), b) Formula (III), c) Formula (IV), d) Formula (V), e) Formula (VI), f) Formula (VII), wherein P2 is hydrogen or an amino protecting group, R2 and R3 may be same or different and are hydrogen, C1-5 alkyl, optionally substituted aryl, or optionally substituted heteroaryl, and X1 is O or S, or its stereoisomers, or salts thereof.

Abstract: The present invention relates to the crystalline form of carbapenems derivative or hydrate thereof and the preparation methods thereof. Specifically, the present invention relates to the crystalline form of carbapenem derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid as represented by formula (I) or hydrate thereof, characterized in that the X-ray powder diffraction pattern thereof using Cu-Ka radiation represented as 2? has characteristic peaks at 18.9±0.2, 19.4±0.2, 21.0±0.2, 21.7±0.2, and 23.4±0.2, the preparation methods thereof, and the use thereof in the preparation of medicament for treating and/or preventing infectious diseases, as well as a pharmaceutical composition comprising such compound and one or more pharmaceutical carriers and/or diluents.

Abstract: The present invention relates to an efficient process of synthesizing some known Ertapenem compounds and to provide new intermediate compounds of Meropenem and Doripenem. The process and the intermediate can substantially increase the effective yield and reduce the impurity generation. The present invention further provides a novel and effective process for recovering and purifying ertapenem compounds by utilizing a low cost, materials with chemical stability as a carrier for isolating ertapenem compounds from extracts.

Abstract: The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1?-C1? di-substituted carbapenem compounds, C5? substituted carbapenem compounds, C6?-C6? di-substituted carbapenem compounds and combinations thereof.

Abstract: The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which are useful for intravenous and intramuscular administration.

Abstract: Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw material. The crystalline form E can be easily filtered and dried, the properties in the drying process are stable, and the purity of the crystal is high and can be up to 98.5% or higher.

Abstract: The present invention relates to a process for the preparation of pure meropenem trihydrate.

Abstract: The present invention relates to a process for the preparation of sterile doripenem.

Abstract: The present invention relates to the crystalline form of carbapenems derivative or hydrate thereof and the preparation methods thereof. Specifically, the present invention relates to the crystalline form of carbapenem derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-(4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid as represented by formula (I) or hydrate thereof, characterized in that the X-ray powder diffraction pattern thereof using Cu-Ka radiation represented as 2? has characteristic peaks at 18.9±0.2, 19.4±0.2, 21.0±0.2, 21.7±0.2, and 23.4±0.2, the preparation methods thereof, and the use thereof in the preparation of medicament for treating and/or preventing infectious diseases, as well as a pharmaceutical composition comprising such compound and one or more pharmaceutical carriers and/or diluents.

Abstract: The presently disclosed subject matter demonstrates that ThnG and ThnQ enzymes encoded by the thienamycin gene cluster in Streptomyces cattleya oxidize the C-2 and C-6 moieties of carbapenems, respectively. ThnQ stereospecifically hydroxylates PS-5 giving N-acetyl thienamycin. ThnG catalyzes sequential desaturation and sulfoxidation of PS-5, giving PS-7 and its sulfoxide. The ThnG and ThnQ enzymes are relatively substrate selective, but give rise to the oxidative diversity of carbapenems produced by S. cattleya, and orthologues likely function similarly in allied streptomyces.

Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

Abstract: The present invention includes novel carbapenem derivatives having structural formula (I) or (II): wherein R1, R2, R3, R4 are described in the specification. The present invention also provides pharmaceutical compositions comprising the novel carbapenem derivatives and the use of the novel carbapenem derivatives for treating infectious diseases.

Abstract: The present invention relates to novel carbapenem derivatives and belongs to pharmaceutical field. Specifically, the present invention relates to the compounds as represented by formula (1), pharmaceutically acceptable salts, hydrolysable esters, isomers and intermediates thereof, wherein R1, R2, R3, R4 are described as in the description. The present invention also relates to the processes for the preparation of these compounds, to the pharmaceutical compositions comprising these compounds, and to their use for the manufacture of a medicament for the treatment and/or prevention of infectious diseases.

Abstract: A process for the preparation of a carbapenem of formula (I): in amorphous form wherein R represents hydrogen or COOM and M represents hydrogen or sodium the process including condensing a compound of formula (II): wherein P? denotes a carboxy protecting group, with a compound of formula (III): wherein P? denotes a carboxy protecting group, in the presence of a base to yield a compound of formula (IV): deprotecting both the protecting groups in the compound of formula (IV) in the presence or absence of a sodium ion source, a solvent and in the presence or absence of CO2, gas, extracting the product into an aqueous medium, quenching the aqueous layer of into an alcohol at a temperature, and isolating the carbapenem compound of formula (I) in amorphous form.

Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)p yrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) and a crystal of said compound having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

Abstract: The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which is useful for intravenous and intramuscular administration.

Abstract: The present application describes deuterium-enriched meropenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P1 and P2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The present invention also relates to a composition comprising at least 95% of the intermediate of Ertapenem of formula 2a.

Abstract: The present invention provides a novel process for the preparation of the meropenem trihydrate of formula (I).

Abstract: A process for preparing purified Meropenem trihydrate that involves the dissolution of Meropenem in water in presence of base, adjusting the pH to 4.0-7.0, and adding solvent to yield Meropenem trihydrate.

Abstract: The present invention relates to an improved method for synthesizing meropenem trihydrate [(1R,5S,6S)-2-[((2?S,4?S)-2?-dimethylaminocarbozyl)pyrrolidin-4?-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid, trihydrate], which is a novel carbapenem antibiotic.

Abstract: The present invention relates to an improved process for the preparation of the carbapenem antibiotic of formula (I) or its salts, hydrates and esters. The present invention further provides novel crystalline form of compound of general formula (III), wherein R3 is p-nitrobenzyloxy carbonyl.

Abstract: Compounds useful as antimicrobials are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are derivatives having a carbapenem core, and are useful for treating a microorganism infection.

Abstract: The present invention relates to novel crystalline form of (4-Nitrobenzyl (4R,5S,6S)-(3-{(3S,5S)-5-[(dimethylamino)carbonyl]-1-[(4-nitrophenoxy)carbonxyl]pyrrolidin-3-yl}thio-6-[(1R)-1-hydorxyehtyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0].hept-2-ene-2-carboxylate) of compound Formula I as well as an improved process for the preparation of meropenem trihydrate of compound Formula II wherein, PNB represent P-nitro benzyl group and PNZ represent P-nitrobenzyloxycarbonyl group.

Abstract: An improved crystallization method for an azetidinone compound represented by the formula 1: , which is extremely useful as a common intermediate for the synthesis of 1?-methylcarbapenem compounds. The present method provides crystals having higher quality and stability than conventional crystals and excellent filterability at the time of recovery; and an azetidinone compound having a low content of impurity, and which has a controlled particle size distribution of crystals and improved handleability and stability. The crystallization is carried out by adding a hydrocarbon solvent to a solution in which an azetidinone compound extremely useful as a common intermediate for the synthesis of 1?-methylcarbapenem compounds is dissolved in the presence of a seed crystal in an amount of 200% by weight or less based on the weight of the azetidinone compound.

Abstract: The present invention relates to preparing carbapenem intermediates that are useful to produce Ertapenem, Meropenem and Doripenem; and provides an effective process for recovering ertapenem compounds.

Abstract: The present invention relates to preparing carbapenem intermediates that are useful to produce Ertapenem, Meropenem and Doripenem.

Abstract: The present invention relates to a process for the preparation of carbapenem compound of Formula (I), wherein P1 is hydrogen or a carboxyl protecting group, P3 is hydrogen or a hydroxyl protecting group, R1 is C1-3 alkyl, and A is selected from a group consisting of a) Formula (II), b) Formula (III), c) Formula (IV), d) Formula (V), e) Formula (VI), f) Formula (VII), wherein P2 is hydrogen or an amino protecting group, R2 and R3 may be same or different and are hydrogen, C1-5 alkyl, optionally substituted aryl, or optionally substituted heteroaryl, and X1 is O or S, or its stereoisomers, or salts thereof.

Abstract: An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

Abstract: The present invention relates to a process for preparing a carbapenem antibiotic composition. The present invention further relates to a carbapenem antibiotic composition substantially free of degradation impurities. The present invention further relates to a polymorphic form of ertapenem mono sodium designated as Form D and its preparation.

Abstract: The present invention includes novel carbapenem derivatives having structural formula (I) or (II): wherein R1, R2, R3, R4 are described in the specification. The present invention also provides pharmaceutical compositions comprising the novel carbapenem derivatives and the use of the novel carbapenem derivatives for treating infectious diseases.

Abstract: The present invention provides a 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives or their pharmaceutically acceptable salts show high oral absorption rate, and thus can be orally administered. The active metabolites thereof have a broad spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against methicillin-resistant Staphylococcus aurus (MRSA) and quinolone-resistant strains (QRS). In particular, the acid addition salts of the 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives are obtained in crystalline forms having excellent stability.

Abstract: An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

Abstract: The present invention relates to a process for the preparation of sterile doripenem.

Abstract: The present invention relates to a compound of the formula (I), pharmaceutically acceptable salts, hydrolysable esters, isomers and hydrates thereof, and hydrates of the said esters or salts, wherein R1, R2, R3 and are as defined in the description. The present invention further relates to a process for preparing the compounds, to pharmaceutical compositions comprising the compounds, and to the use of the compounds in the manufacture of a medicament for the treatment and/or prophylaxis of infectious diseases.

Abstract: Disclosed is a process for producing a carbapenem compound represented by Formula [1], which is characterized by allowing a base and a Lewis acid metal salt to coexist in the reaction of a compound represented by Formula [2] with a compound represented by Formula [3]. According to the process, a side-chain mercaptothiazole can be introduced into a ?-lactam skeleton efficiently in the production of a ?-lactam compound having an excellent antibacterial activity against a Gram-positive bacterium. [3] [2] [1] wherein R1 represents a lower alkyl group or the like; R2 represents hydrogen atom or the like; R3 represents a protective group for a carboxyl group; L represents an active ester of a hydroxy group; R4 represents hydrogen atom or the like; and R5 represents hydrogen atom or the like.

Abstract: A stable crystal (Form I crystal) of (4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-3-({4-[(5S)-5-methyl-2,5-dihydro-1H-pyrrol-3-yl]-1,3-thiazol-2-yl}thio)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid which has preferable properties and a process for preparation Form I crystal which is characterized of desolvating a solvated crystal of its compound.

Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.

Abstract: The present invention has its object to provide an easy process for producing (4R,5S,6S)-3-[[(3S,5S)-5-(dimethylaminocarbonyl)-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, excellent in antimicrobial activity. The present invention relates to a process for continuously producing (4R,5S,6S)-3-[[(3S,5S)-5-(dimethylaminocarbonyl)-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid without isolating/purifying the reaction intermediate.

Abstract: The present invention relates to novel carbapenem derivatives and belongs to pharmaceutical field. Specifically, the present invention relates to the compounds as represented by formulae (1) and (2), pharmaceutically acceptable salts, hydrolysable esters, isomers and intermediates thereof, wherein R1, R2, R3, R4 are described as in the description. The present invention also relates to the processes for the preparation of these compounds, to the pharmaceutical compositions comprising these compounds, and to their use for the manufacture of a medicament for the treatment and/or prevention of infectious diseases.