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"Triazolo-pyrimidine intermediates"

Assignee: Nippon Pharmaceutical Development Institute Co
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Filing: 1989-05-26
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Granted: 1990-09-11
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Expires: 2009-05-26
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Abstract

Abstract There are disclosed a β-lactam compound represented by the formula (I): ##STR1## wherein R 1 represents an acyl group; M represents a hydrogen atom, a protective group of an eliminatable group which is easily hydrolyzable in a human body; B represents a group represented by the formula (b): ##STR2## where at least one of R 2 , R 3 and R 9 represent a group represented by the formula: -A-OR 4 where R 4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group of an eliminatable group which is easily hydrolyzable in a human body, and also when R 9 is -A-OR 4 , R 2 and R 3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; and Z represents a nitrogen atom or a group represented by the formula: C-R 10 where R 10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group, or its pharmaceutically acceptable salt, and a process for preparing the same, an intermediate for synthesis of the same and a medicinal composition for bacterially infectious disease therapy containing the same.

Inventors

  • 👤 Shigeo Shimizu
  • 👤 Hiroyuki Takano

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 16:22
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; C07D501/24; C07D501/36; C07D519/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55

Claims Analysis

Total Claims: 4
Claim 1
Independent Claim 213 words
A compound represented by the formula (VII'): ##STR23## where at least one of R 2 , R 3 and R 9 represent a group represented by the formula: --A--OR 4 where R 4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group or an eliminatable group which is easily hydrolyzable in a human body, and also when R 9 is --A--OR 4 , R 2 and R 3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; Z represents a nitrogen atom or a group represented by the formula: C--R 10 where R 10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group; and X represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom.
Claim 2
Dependent Claim 213 words
A compound represented by the formula (VII'): ##STR23## where at least one of R 2 , R 3 and R 9 represent a group represented by the formula: --A--OR 4 where R 4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group or an eliminatable group which is easily hydrolyzable in a human body, and also when R 9 is --A--OR 4 , R 2 and R 3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; Z represents a nitrogen atom or a group represented by the formula: C--R 10 where R 10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group; and X represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom.
Claim 3
Dependent Claim 80 words
A compound according to claim 1, wherein the protective group is selected from the group consisting of a diphenylmethyl group, a t-butyl group, a p-nitrobenzyl group and a trimethylsilyl group and the eliminatable group which is easily hydrolyzable in a human body is selected from the group consisting of an acetoxymethyl group, an α-acetoxyethyl group, a pivaroyloxymethyl group, an ethoxycarbonyloxymethyl group, an α-methoxycarbonyloxymethyl group, an α-methoxycarbonyloxyethyl group, an α- ethoxycarbonyloxyethyl group, a 1-indanyl, a phthalidyl group, and a 5-methyl-2-oxo-1,3-dioxol-4-yl-methyl group.
Claim 4
Dependent Claim 30 words
A compound according to claim 2, wherein the cycloalkyl group is selected from the group consisting of a cyclopropyl group, a cyclobutyl group, a cyclopentyl group and a cyclohexyl group.

References Cited (Backward Citations)

US3799926A Cited
US4528288A Cited
EP0150507A2 Cited
US4657172A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-09-10 1994-03-12 1994-09-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-09-10 1998-03-12 1998-09-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-09-10 2002-03-12 2002-09-11 $7700.00 Window Closed / Lapsed

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