PRODRUGS OF ANTIBIOTIC 7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID Russian patent published in 2006 - IPC C07D501/59 A61K31/546 A61P31/04 

Abstract RU 2279435 C2

FIELD: organic chemistry, antibiotics, pharmacy.

SUBSTANCE: invention relates to compound of the formula: wherein R'1 means hydrogen atom; R'2 represents acyl group but with exception of glycyl that is cleaved by mammalian enzyme. Also, invention describes (7R)-7-[(Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(hydroxyimino)acetamido]-3-{3-[2-N-(L)-aspartylaminoethylthiomethyl]pyrid-4-ylthio}-3-cephem-4-carboxylic acid of the formula: or its pharmaceutically acceptable salt and pharmaceutical composition used in treatment or prophylaxis of bacterial infection and comprising the effective amount of one or more of indicated compounds. The claimed prodrugs show the enhanced solubility in water at neutral or near to neutral pH value as compared with the parent compounds.

EFFECT: improved and valuable properties of prodrugs.

15 cl

Similar patents RU2279435C2

Title Year Author Number
DERIVATIVES OF 7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID AND ANTIBACTERIAL COMPOSITIONS COMPRISING THEREOF 2000
  • Khekker Skott Dzh.
  • Cho Aehsop
  • Glinka Tomas V.
  • Kolkinz Trevor
  • Li Ving Dzh.
RU2225868C2
CEPHALOSPORIN DERIVATIVES, ANTIBACTERIAL COMPOSITION CONTAINING THEREOF, DERIVATIVES OF 2-AMINOTHIAZOLES AS INTERMEDIATES, AND METHOD OF PREPARATION THEREOF 1996
  • In-Seop Cho
  • Skott Kheker
  • Tomazh Glinka
  • Ving Dzh. Li
  • Zidzja Dzh. Zang
RU2172317C2
CEPHALOSPORIN ANTIBIOTICS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR TREATMENT OF INFECTION 2001
  • Glinka Tomash U.
RU2281948C2
METHOD OF PRODUCING CEFEM DERIVATIVES OR THEIR SALTS 0
  • Akio Miyake
  • Masakhiro Kondo
  • Masakhiro Fudzino
SU1595341A3
METHOD OF PRODUCING DERIVATIVES OF CEPHEM OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 0
  • Akio Miyake
  • Masakhiro Kondo
  • Masakhiro Fudzino
SU1538898A3
METHOD OF PRODUCING 7-/2-(2-AMINOTHIAZOLE-4-YL)-/Z/-2-(2-CARBOXY-PROP-2-OXYIMINO)ACETAMIDO/-3-/(1-METHYL-1-PYRROLIDINIUM)METHYL/-3-CEPHEM-4-CARBOXYLATE 0
  • Simpei Aburaki
  • Khadzime Kamati
  • Yukio Narita
  • Yun Okumura
  • Takayuki Naito
SU1326195A3
ANTIBACTERIAL CEPHALOSPORINS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF TREATMENT 1996
  • Asher Gerd
  • Ljudesher Jokhannes
RU2183212C2
METHOD OF PRODUCING 3-VINYLCEPHALOSPORINS OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS 0
  • Takao Takaya
  • Khisasi Takasugi
  • Takasi Masugi
  • Khideaki Yamanaka
  • Kodzi Kavabata
SU1186087A3
CEPHALOSPORIN DERIVATIVES AND PHARMACOLOGICALLY ACCEPTABLE NON-TOXIC SALTS, PHYSIOLOGICALLY HYDROLYSABLE ESTERS, SYN-ISOMERS AND OPTICAL ISOMERS, AND METHOD OF PREPARATION THEREOF 1994
  • Chan Sik Behng[Kr]
  • Dzhae Khong Eo[Kr]
  • Jong Min Vu[Kr]
  • Dzhong Chan Lim[Kr]
  • Deog Khl Jang[Kr]
  • Se Kho Kim[Kr]
  • Dzhae Khun Dzheon[Kr]
  • Mi Kjeong Seo[Kr]
  • Sam Sik Kim[Kr]
  • Tae Khi Li[Kr]
  • Jong Zu Kim[Kr]
  • Khun Seung Okh[Kr]
RU2091384C1
PROCESS FOR PREPARING 7-/ALPHA,ALPHA-DISUBSTITUTED ACETAMIDO-3-SUBSTITUTED-3-CEPHEM-4-CARBOXYLIC ACIDS OR THEIR LOWER ALKANOYLOXY-(LOWER)/-ALKYL ESTERS OR THEIR PHARMACEUTICALLY ACCEPTIC SALTS 0
  • Takao Takaya
  • Takasi Masugi
  • Khisasi Takasugi
  • Khiromu Kochi
SU993821A3

RU 2 279 435 C2

Authors

Ehkker Skott Dzh.

Cho Aehsop

Glinka Tomas V.

Kolkins Trevor

Li Ving Dzh.

Dates

2006-07-10Published

2001-03-20Filed