Legochem Biosciences, Inc.

Legochem Bioscience Ltd.

The Green Cross Corporation

Young Lag Cho

Yong Zu Kim

Sung Ho Woo

Tae Kyo Park

Sang Eun Chae

Sung Yoon Baek

Hyang Sook Lee

Ho Young Song

Kyu Man Oh

Hyun Jin Kwon

Dae Hyuck Kang

Dae Yon Lee

Ju Hyun Park

Yeon Ok Kim

Min Soo Kim

Suk Ho Lee

Chul Soon Park

Chul-Woong Chung

Sung Min Kim

Seong Jin Kim

Hye Jin Heo

Hong Bum Lee

Joung Yul Yun

Hye Kyung Chang

Sang Hui Jo

Soo Bong Ha

Young Jae Yang

Sun Young Kim

Jinhwa Lee

Jeung Hie Choi

Soongyu Choi

Jong Un Cho

Hye Jin Kang

Kyuman Oh

Jungsub Choi

Yoo Hoon Kim

Young Zu Kim

Jae Yeon Kim

Hee Sock Park

Jeung Soon Choi

So-Hyun Yoon

Substituted dihydroisoxazole derivatives useful as inhibitors of &#x3b2;-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.

Compositions and methods for inhibiting &#x3b2;-lactamase

The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.

Crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and pharmaceutical composition comprising same

Compositions and methods for inhibiting beta-lactamase

The present invention relates to novel cephalosporin derivatives represented by X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

Cephalosporin derivatives and pharmaceutical compositions thereof

Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.

Oxazolidinone derivative and medical composition containing same

Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.

Method for preparing 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl) derivative and intermediate used therein

Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.

Method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives

Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.

Method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives

The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R, and Rare as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. Compounds of the present invention are effective ingredients for the broad spectrum of antibiotic resistance, exhibit low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.

The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.

FXa inhibitors with cyclic amidines as P4 subunit, processes for their preparations, and pharmaceutical compositions and derivatives thereof

Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.

Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof

Disclosed are novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions containing the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.

FXA inhibitors with cyclic amidoxime or cyclic amidrazone as P4 subunit, processes for their preparations, and pharmaceutical compositions and derivatives thereof

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Daejeon, South Korea

Young Lag Cho