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US4080498A Expired / Lapsed US ⏱️ 0.0 years remaining

7-Alpha-(2-aminothiazole)-acetamido-cephalosporins

Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1974-12-20
•
Granted: 1978-03-21
•
Expires: 1994-12-20
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Abstract

Abstract A compound of the formula: <IMAGE> wherein R1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR2 (where R2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R1), and Y represents acetoxy group or a group of formula -SR3 (where R3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

Inventors

  • 👤 Mitsuo Numata
  • 👤 Isao Minamida
  • 👤 Masayoshi Yamaoka
  • 👤 Mitsuru Shiraishi
  • 👤 Toshio Miyawaki

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 00:59
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; C07D501/24; C07D277/00; C07D277/02; C07D277/20; C07D277/32; C07D277/34; C07D277/36

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 82 words
A compound of the formula ##STR47## wherein R is a member selected from the group consisting of alkyl and substituted alkyl, the substituent of the substituted alkyl being selected from the group consisting of hydroxyl, mercapto, amino, morpholino, carboxyl, sulfo, carbamoyl, mono-, or di-alkyl amino, mono- or di-alkyl carbamoyl, alkoxy having from 1 to 12 carbon atoms, alkylthio, alkylsulfonyl, acetoxy, propionyloxy, valeryloxy, caproyloxy, benzoyloxy, phenylacetoxy, and morpholinocarbonyl, said alkyl having from 1 to 12 carbon atoms, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 82 words
A compound of the formula ##STR47## wherein R is a member selected from the group consisting of alkyl and substituted alkyl, the substituent of the substituted alkyl being selected from the group consisting of hydroxyl, mercapto, amino, morpholino, carboxyl, sulfo, carbamoyl, mono-, or di-alkyl amino, mono- or di-alkyl carbamoyl, alkoxy having from 1 to 12 carbon atoms, alkylthio, alkylsulfonyl, acetoxy, propionyloxy, valeryloxy, caproyloxy, benzoyloxy, phenylacetoxy, and morpholinocarbonyl, said alkyl having from 1 to 12 carbon atoms, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 13 words
A compound according to claim 1, wherein R is a substituted alkyl group.
Claim 4
Dependent Claim 8 words
7-[2-(2-aminothiazol-4-yl)acetamido]-3-[1-(2-N,N-dimethylaminoethyl)-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 8 words
7-[2-(2-aminothiazol-4-yl)acetamido]-3-[1-(2-N,N-dimethylaminoethyl)-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim 8 words
7-[2-(2-aminothiazol-4-yl)acetamido]-3-(1-carbamoylmethyltetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim 8 words
7-[2-(2-aminothiazol-4-yl)acetamido]-3-(1-carbamoylmethyltetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim 8 words
7-[2-(2-amino-thiazol-4-yl)acetamido]-3-(1-methyltetrazol-5-yl)-thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim 8 words
7-[2-(2-amino-thiazol-4-yl)acetamido]-3-(1-methyltetrazol-5-yl)-thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim 8 words
7-[2-(2-amino-thiazol-4-yl)acetamido]-3-[1(2-hydroxylethyl)-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim 8 words
7-[2-(2-amino-thiazol-4-yl)acetamido]-3-[1(2-hydroxylethyl)-tetrazol-5-yl]thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof.

References Cited (Backward Citations)

US3218318A Cited
US3516997A Cited
US3872115A Cited
US3890309A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-03-20 1981-09-19 1982-03-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-03-20 1985-09-19 1986-03-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-03-20 1989-09-19 1990-03-21 $7700.00 Window Closed / Lapsed

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