EP0150507A2
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EP
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Cephalosporin derivatives, processes for producing the same and compositions containing them
Assignee: Mochida Pharmaceutical Co Ltd
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Filing: 1984-12-28
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Granted: —
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Expires: 2004-12-28
Abstract
Abstract Novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in synthesis of cephalosporin derivative and processes for producing thereof are disclosed. The novel cephalosporin derivatives contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton. These compounds have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. They are extremely useful for the treatment of infectious diseases.
Inventors
- 👤 Haruo Ohnishi
- 👤 Hiroshi Kosuzume
- 👤 Masahiro Mizota
- 👤 Yasuo Suzuki
- 👤 Ei Mochida
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 16:32
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/47; C07D239/32; C07D239/38; C07D239/40; C07D277/00; C07D277/02; C07D277/20; C07D277/587; C07D417/00; C07D417/02; C07D417/12; C07D487/00; C07D487/02; C07D487/04; C07D513/00; C07D513/02; C07D513/04
Claims Analysis
Total Claims: 129
Claim 1
Independent Claim
242 words
A cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen or an amino-protecting group; Z represents a group: or wherein R 2 represents-a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group or methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R S represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxy-protecting group; and a bond shown by a wavy line represents a bond of anti-form or a syn-form, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 2
Dependent Claim
242 words
A cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen or an amino-protecting group; Z represents a group: or wherein R 2 represents-a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group or methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R S represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxy-protecting group; and a bond shown by a wavy line represents a bond of anti-form or a syn-form, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 3
Dependent Claim
37 words
A cephalosporin derivative and a salt thereof as well as a hydrate of the cephalosporin derivative and salt thereof as claimed in claim 1 wherein said bond shown by the wavy line is a bond of syn-form.
Claim 4
Dependent Claim
58 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Ia): wherein R 1 , R2, R3, R 4 , R 13 and the bond shown by the wavy line have the same significances as defined hereinabove, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 5
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a methyl group.
Claim 6
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxyl group, R 3 represents -a methyl group and R 4 represents a hydrogen atom.
Claim 7
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 3 each represents a hydrogen atom and R 4 represents a carboxyl group.
Claim 8
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxymethyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 9
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a carboxymethyl group.
Claim 10
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a carboxyl group.
Claim 11
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a carboxyl group and R 3 represents a hydrogen atom.
Claim 12
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxyl group, R 3 represents an isopropyl group and R 4 represents a hydrogen atom.
Claim 13
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxyl group, and R 3 and R 4 each represents a hydrogen atom.
Claim 14
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxyl group, and R 3 and R 4 each represents a methyl group.
Claim 15
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a methyl group, R 3 represents a carboxyl group and R 4 represents a hydrogen atom.
Claim 16
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a methoxycarbonyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 17
Dependent Claim
45 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a hydrazino carbonyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 18
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a carboxyl group, R 3 represents a hydroxy group and R 4 represents a hydrogen atom.
Claim 19
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a methoxy group.
Claim 20
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents an amino group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 21
Dependent Claim
44 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 represents a hydroxysulfonyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 22
Dependent Claim
42 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 3 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a chlorine atom.
Claim 23
Dependent Claim
92 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Ib): wherein R 1 represents a hydrogen atom or an amino-protecting group; R 2 represents a carboxyl group or a protected carboxyl group ;R i2 represents a hydrogen atom, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxyl-protecting group; and a bond shown by a wavy line represents a bond of anti-form or syn-form, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 24
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a hydrogen atom.
Claim 25
Dependent Claim
30 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a benzoyl'group.
Claim 26
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 2-furancarbonyl group.
Claim 27
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 2-thiophenecarbonyl group.
Claim 28
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 3-pyridinecarbonyl group.
Claim 29
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 2-pyrrolecarbonyl group.
Claim 30
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 3,4-methylenedioxybenzoyl group.
Claim 31
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a cyanomethylthioacetyl group.
Claim 32
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 3,4-diacetoxybenzoyl group.
Claim 33
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 22 wherein R 12 represents a 3,4,5-triacetoxybenzoyl group.
Claim 34
Dependent Claim
90 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Ic): wherein R 1 represents a hydrogen atom or an amino-protecting group, R 5 represents a hydrogen atom or a methyl group, R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group, R 13 represents a hydrogen atom or a carboxy-protecting group, and the wavy line represents a bond of anti-form or syn-form, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 35
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 33 wherein R S represents a methyl group and R 6 represents a hydrogen atom.
Claim 36
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 33 wherein R 5 represents a hydrogen atom and R 6 represents a carboxyl group.
Claim 37
Dependent Claim
39 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative . and salt thereof as claimed in claim 33 wherein R 5 represents a hydrogen atom and R 6 represents an ethoxycarbonyl group.
Claim 38
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 33 wherein R 5 represents a hydrogen atom and R 6 represents a piperidinocarbonyl group.
Claim 39
Dependent Claim
74 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Id): wherein R 1 represents a hydrogen atom or an amino-protecting group, R 7 represents a hydrogen atom or a methyl group, R 13 represents a hydrogen atom or a carboxy-protecting group, and the wavy line represents a bond of anti-form or syn-form, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 40
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 38 wherein R 7 represents a hydrogen atom.
Claim 41
Dependent Claim
31 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 38 wherein R 7 represents a methyl group.
Claim 42
Dependent Claim
49 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Ie): wherein R 1 , R 13 and the wavy line have the same significances as defined hereinabove, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 43
Dependent Claim
51 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (If): wherein R 1 , R8, R9, R 13 and the wavy line have the same significances as defined hereinabove, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 44
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 42 wherein R 8 represents a hydrogen atom and R 9 represents a carboxyl group.
Claim 45
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 42 wherein R 8 represents a hydrogen atom and R 9 represents an amino group.
Claim 46
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 42 wherein R 8 represents a hydrogen atom and R 9 represents a methyl group.
Claim 47
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 42 wherein R 8 represents a carboxyl group and R 9 represents a methyl group.
Claim 48
Dependent Claim
50 words
A cephalosporin derivative as claimed in claim 1 which is represented by the general formula (Ig): wherein R 1 , R 13 and the wavy line have the same significances as defined hereinabove, and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 49
Dependent Claim
54 words
A cephalosporin derivative as claimed in claim 1 which is represented by general formula (Ih): wherein R 1 , R 10 , R 11 , R 13 and the wavy line have the same significances as defined hereinabove, and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof.
Claim 50
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 48 wherein R 10 represents a methyl group and R 11 represents a hydrogen atom.
Claim 51
Dependent Claim
38 words
A cephalosporin derivative and a salt thereof as well as a hydrate of said cephalosporin derivative and salt thereof as claimed in claim 48 wherein R 10 represents a hydrogen atom and R 11 represents a carboxyl group.
Claim 52
Dependent Claim
92 words
An intermediate compound in synthesis of a cephalosporin derivative represented by the general formula (XIII): wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group or a chlorine atom, and R 4 represents a hydrogen atom, a methyl group or a carboxyl group.
Claim 53
Dependent Claim
92 words
An intermediate compound in synthesis of a cephalosporin derivative represented by the general formula (XIII): wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group or a chlorine atom, and R 4 represents a hydrogen atom, a methyl group or a carboxyl group.
Claim 54
Dependent Claim
28 words
An intermediate compound as claimed in claim 51 wherein R 2 represents a carboxyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 55
Dependent Claim
26 words
An intermediate compound as claimed in claim 51 wherein R 2 and R 3 each represents a hydrogen atom and R 4 represents a carboxyl group.
Claim 56
Dependent Claim
28 words
An intermediate compound as claimed in claim 51 wherein R 2 represents a carboxymethyl group, R 3 represents a methyl group and R 4 represents a hydrogen atom.
Claim 57
Dependent Claim
26 words
An intermediate compound as claimed in claim 51 wherein R 2 and R 4 each represents a hydrogen atom and R 3 represents a carboxymethyl group.
Claim 58
Dependent Claim
27 words
An intermediate compound as claimed in claim 51 wherein R 2 and R 4 each represents a a hydrogen atom and R 3 represents a carboxyl group.
Claim 59
Dependent Claim
26 words
An intermediate compound as claimed in claim 51 wherein R 2 and R 4 each represents a carboxyl group and R 3 represents a hydrogen atom.
Claim 60
Dependent Claim
43 words
An intermediate compound in synthesis of a cephalosporin derivative represented by the general formula (IIIa): wherein R 1 represents a hydrogen atom or an amino-protecting group, R 121 represents an acyl group and R 14 represents a hydrogen atom or a carboxyl-protecting group.
Claim 61
Dependent Claim
43 words
An intermediate compound in synthesis of a cephalosporin derivative represented by the general formula (IIIa): wherein R 1 represents a hydrogen atom or an amino-protecting group, R 121 represents an acyl group and R 14 represents a hydrogen atom or a carboxyl-protecting group.
Claim 62
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a benzoyl group.
Claim 63
Dependent Claim
30 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 121 represents a 2-furancarbonyl group.
Claim 64
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a 3-pyridinecarbonyl group.
Claim 65
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a 2-thiophenecarbonyl group.
Claim 66
Dependent Claim
30 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 121 represents a 3,4-methylenedioxybenzoyl group.
Claim 67
Dependent Claim
32 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a cyano- methylmercaptoacetyl group.
Claim 68
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 . represents a 2-pyrrolecarbonyl group.
Claim 69
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a 3,4-diacetoxybenzoyl group.
Claim 70
Dependent Claim
31 words
An intermediate compound and a salt thereof as well as a hydrate of the compound and the salt as claimed in claim 58 wherein R 12 ' represents a 3,4,5-triacetoxybenzoyl group.
Claim 71
Dependent Claim
336 words
A process for producing a cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen atom or an amino-protecting group; Z represents a group shown by: or wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R 5 represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxyl-protecting group and; a bond shown by a wavy line represents a bond of anti-form or syn-form; and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (II): wherein R 13 and Z have the same significances defined hereinabove; or a reactive derivative at the amino group thereof or a salt thereof with a compound represented by the general formula (III): wherein R 1 , R 12 and a bond shown by a wavy line have the same significances as defined hereinabove; or a reactive derivative at the carboxyl group thereof or a salt thereof and; if necessary, removing the amino-protecting group.
Claim 72
Dependent Claim
336 words
A process for producing a cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen atom or an amino-protecting group; Z represents a group shown by: or wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R 5 represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxyl-protecting group and; a bond shown by a wavy line represents a bond of anti-form or syn-form; and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (II): wherein R 13 and Z have the same significances defined hereinabove; or a reactive derivative at the amino group thereof or a salt thereof with a compound represented by the general formula (III): wherein R 1 , R 12 and a bond shown by a wavy line have the same significances as defined hereinabove; or a reactive derivative at the carboxyl group thereof or a salt thereof and; if necessary, removing the amino-protecting group.
Claim 73
Dependent Claim
125 words
A process for producing a cephalosporin derivative represented by the general formula (I): wherein R 1 , R12, R 13 , Z and a bond shown by a wavy line have the same significances as defined hereinabove and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (IV): wherein R 1 , R 12 , R 13 and a bond shown by a wavy line have the same significances as defined hereinabove, except that R 12 does not include an acyl group, with a thiol compound represented by general formula (V): wherein Z has the same significance as defined hereinabove, and, if necessary removing the amino-protecting group.
Claim 74
Dependent Claim
125 words
A process for producing a cephalosporin derivative represented by the general formula (I): wherein R 1 , R12, R 13 , Z and a bond shown by a wavy line have the same significances as defined hereinabove and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (IV): wherein R 1 , R 12 , R 13 and a bond shown by a wavy line have the same significances as defined hereinabove, except that R 12 does not include an acyl group, with a thiol compound represented by general formula (V): wherein Z has the same significance as defined hereinabove, and, if necessary removing the amino-protecting group.
Claim 75
Dependent Claim
138 words
A process for producing a cephalosporin derivative represented by the general formula (I'): wherein R 1 , R 13, Z and a bond shown by a wavy line have the same significances as defined hereinabove; R 12 ' represents an acyl group; and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (VI): wherein R 1 , R 13 , Z and a bond shown by a wavy line have the same significances as defined hereinabove, or a salt thereof with a compound represented by general formula (VII): wherein R 12 ' represents an acyl group, or a reactive derivative at the carboxyl group thereof or a salt thereof, and, if necessary, removing the amino-protecting group and/or the carboxyl-protecting group.
Claim 76
Dependent Claim
138 words
A process for producing a cephalosporin derivative represented by the general formula (I'): wherein R 1 , R 13, Z and a bond shown by a wavy line have the same significances as defined hereinabove; R 12 ' represents an acyl group; and a salt thereof as well as a hydrate of the cephalosporin derivative and the salt, the improvement which comprises reacting a compound represented by the general formula (VI): wherein R 1 , R 13 , Z and a bond shown by a wavy line have the same significances as defined hereinabove, or a salt thereof with a compound represented by general formula (VII): wherein R 12 ' represents an acyl group, or a reactive derivative at the carboxyl group thereof or a salt thereof, and, if necessary, removing the amino-protecting group and/or the carboxyl-protecting group.
Claim 77
Dependent Claim
67 words
A process for producing a thiol compound represented by the general formula (V'): wherein Z' represents a group: wherein R 2 , R 3 , R 4 and R 7 have the the same significances as defined hereinabove, which comprises reacting a compound represented by general formula (VIII'): wherein X represents a halogen atom and Z' has the same significances as defined hereinabove, with sodium hydrogen sulfide.
Claim 78
Dependent Claim
67 words
A process for producing a thiol compound represented by the general formula (V'): wherein Z' represents a group: wherein R 2 , R 3 , R 4 and R 7 have the the same significances as defined hereinabove, which comprises reacting a compound represented by general formula (VIII'): wherein X represents a halogen atom and Z' has the same significances as defined hereinabove, with sodium hydrogen sulfide.
Claim 79
Dependent Claim
58 words
A process for producing a thiol compound represented by the general formula (V'): wherein Z' represents a group: wherein R2, R 3 , R 4 and R 7 have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (IX'): wherein Z' has the same significance as defined hereinabove, with phosphorus pentasulfide.
Claim 80
Dependent Claim
58 words
A process for producing a thiol compound represented by the general formula (V'): wherein Z' represents a group: wherein R2, R 3 , R 4 and R 7 have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (IX'): wherein Z' has the same significance as defined hereinabove, with phosphorus pentasulfide.
Claim 81
Dependent Claim
92 words
A process for producing a compound represented by the general formula (IIIa): wherein R 14 represents a hydrogen atom or a carboxy-protecting group, and R l , R 12 ' and the wavy line have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (X): wherein R 1 , R 14 and the wavy line have the same significances as defined hereinabove, with a compound, i.e., an acid, represented by the general formula (VII): wherein R 12 ' has the same significance as defined hereinabove.
Claim 82
Dependent Claim
92 words
A process for producing a compound represented by the general formula (IIIa): wherein R 14 represents a hydrogen atom or a carboxy-protecting group, and R l , R 12 ' and the wavy line have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (X): wherein R 1 , R 14 and the wavy line have the same significances as defined hereinabove, with a compound, i.e., an acid, represented by the general formula (VII): wherein R 12 ' has the same significance as defined hereinabove.
Claim 83
Dependent Claim
117 words
A process for producing a compound represented by the general formula (IIIa): wherein R 1 , R 12 ', R 14 and a bond shown by a wavy line have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (XI): wherein X represents a halogen atom, and R 14 and a bond shown by a wavy line have the same significances as defined hereinabove, with a compound represented by the general formula (VII): wherein R 12 ' has the same significance as defined hereinabove and, then reacting the resulting product with a thiourea derivative represented by the general formula (XII): wherein R 1 has the same significance as defined hereinabove.
Claim 84
Dependent Claim
117 words
A process for producing a compound represented by the general formula (IIIa): wherein R 1 , R 12 ', R 14 and a bond shown by a wavy line have the same significances as defined hereinabove, which comprises reacting a compound represented by the general formula (XI): wherein X represents a halogen atom, and R 14 and a bond shown by a wavy line have the same significances as defined hereinabove, with a compound represented by the general formula (VII): wherein R 12 ' has the same significance as defined hereinabove and, then reacting the resulting product with a thiourea derivative represented by the general formula (XII): wherein R 1 has the same significance as defined hereinabove.
Claim 85
Dependent Claim
261 words
A pharmaceutical composition for treatment and prophylaxis of infectious diseases comprising at least one of a cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen atom or an amino-protecting group; Z represents a group shown by: or wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R 5 represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxyl/ protecting group and; a bond shown by a wavy line represents a bond of anti-form or syn-form; and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt.
Claim 86
Dependent Claim
261 words
A pharmaceutical composition for treatment and prophylaxis of infectious diseases comprising at least one of a cephalosporin derivative represented by the general formula (I): wherein R 1 represents a hydrogen atom or an amino-protecting group; Z represents a group shown by: or wherein R 2 represents a hydrogen atom, a methyl group, an amino group, a hydroxysulfonyl group, a carboxyl group, a carboxymethyl group, a protected carboxyl group, a protected carboxymethyl group, a methoxycarbonyl group or a hydrazino carbonyl group; R 3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxy group, a methoxy group, a carboxyl group, a carboxymethyl group or a chlorine atom; R 4 represents a hydrogen atom, a methyl group or a carboxyl group; R 5 represents a hydrogen atom or a methyl group; R 6 represents a hydrogen atom, a carboxyl group, an ethoxycarbonyl group or a piperidinocarbonyl group; R 7 represents a hydrogen atom or a methyl group; R 8 represents a hydrogen atom or a carboxyl group; R 9 represents a methyl group, an amino group or a carboxyl group; R 10 represents a hydrogen atom or a methyl group; R 11 represents a hydrogen atom or a carboxyl group; R 12 represents a hydrogen atom, a methyl group, a hydroxyl-protecting group or an acyl group; R 13 represents a hydrogen atom or a carboxyl/ protecting group and; a bond shown by a wavy line represents a bond of anti-form or syn-form; and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt.
Claim 87
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-methyl-s-triazolo[1,5-a]pyrimidin-7-yl)-thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2- ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 88
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-carboxy-5-methyl-s-triazolo[1,5-a]py- rimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 89
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(6-carboxy-s-triazolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 90
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-carboxymethyl-5-methyl-s-triazolo-[1,5-a] pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 91
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-carboxymethyl-s-triazolo[1,5-alpyrimi- din-7-yl)thiomethyl]-8-oxo-5-thia-1-aza-bicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 92
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-carboxy-s-triazolo[l,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2- ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 93
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2,6-dicarboxy-s-triazolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 94
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-hydroxyimino)acetamido]-3-[(2-carboxy-5-methyl-s-triazolo[1,5-a]pyrim- idin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 95
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-benzoyloxyimino)acetamido]-3-[t2-carboxy-5-methyl-s-triazolo[1,5-a]py- rimidin-7-yl)thiomethyl)-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 96
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(2-furancarbonyl)oxy- imino]acetamido]-3-[(2-carboxy-5-methyl-s-triazolo-[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 97
Dependent Claim
37 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6 R ,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(2-thiophenecarbonyl)-oxyimino]acetamido]-3-[(2-carboxy-5-methyl-s-tri- azolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia- l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 98
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(3-pyridinecarbonyl)-oxyimino]acetamido]-3-[(2-carboxy-5-methyl-s-tri- azolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 99
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(2-pyrrolecarbonyl)oxy- imino]acetamido]-3-[(2-carboxy-5-methyl-s-triazolo-[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-aza- bicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 100
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(3,4-methylenedioxybenzoyl)oxyimino]acetamido]-3-[(2-carboxy-5-methyl-s-triazolo[l,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 101
Dependent Claim
36 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-cyanomethylthioacetyl- oxyimino)acetamido]-3-[(2-carboxy-5-methyl-s-tri- azolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia- l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 102
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(3,4-diacetoxybenzoyl)-oxyimino]acetamido]-3-[(2-carboxy-5-methyl-s-tri- azoio[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia- l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 103
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-[Z-(3,4,5-triacetoxybenzoyl)oxyimino]acetamido]-3-[(2-carboxy-5-methyl-s-tri- azolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia- l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 104
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido)-3-[(2-carboxy-5-isopropyl-s-triazolo[1,5-a]-pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 105
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-carboxy-s-triazolo[1,5-aJpyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 106
Dependent Claim
34 words
A pharmaceutical composition as claimed. in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acet- mido]-3-[(2-carboxy-5,6-dimethyl-s-triazolo[1,5-a]-pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 107
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-I(5-carboxy-2-methyl-s-triazolo[1,5-a]-pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-aza- bicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 108
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-methoxycarbonyl-5-methyl-s-triazolo-[1.5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-aza- bicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 109
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-hydrazinocarbonyl-5-methyl-s-triazolo-[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-aza- bicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 110
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-carboxy-5-hydroxy-s-triazolo[1,5-a]py- rimidin-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 111
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-methyoxy-s-triazolo[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 112
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-amino-5-methyl-s-triazolo[1,5-a]pyrimi- din-7-yl)thiomethyl)-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 113
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-cyano-5-methyl-s-triazolo[1,5-a]pyrimi- din-7-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 114
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-hydroxysulfonyl-5-methyl-s-triazolo-[1,5-a]pyrimidin-7-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 115
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75.which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-chloro-s-triazolo[I,5-a]pyrimidin-7-yl)-thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2- ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 116
Dependent Claim
34 words
A pharmaceutical composition as, claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-hydroxy-5-methyl-s-triazolo[1,5-a]py- rimidin-2-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 117
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(6-carboxy-7-hydroxy-s-triazolo[1,5-a]py- rimidin-2-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt.thereof.
Claim 118
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(6-ethoxycarbonyl-7-hydroxy-s-triazolo-[1,5-a]pyrimidin-2-yl)thiomethyl]-8-oxo-5-thia-1-aza- bicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 119
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-hydroxy-6-piperidinocarbonyl-s-tri- azolo[1,5-a]pyrimidin-2-yl)thiomethyl]-8-oxo-5-thia- l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 120
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-carboxy-s-triazolo[4,3-a]pyrimidin-5-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]-oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 121
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]=3-[(7-carboxy-3-methyl-s-triazolo[4,3-a]py- rimidin-5-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 122
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-carboxy-5-hydroxy-s-triazolo[4,3-a]-pyrimidin-3-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 123
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z - methoxyimino)acetamido]-3-[(7-carboxy-s-triazolo[1,5-c]pyrimidin-5-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 124
Dependent Claim
35 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acet- amidol-3-[(7-amino-s-triazolo[1,5-c]pyrimidin-5-yl)-thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2- ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 125
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-methyl-s-triazolo[1,5-c]pyrimidin-5-yl)-thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2- ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 126
Dependent Claim
34 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(2-carboxy-7-methyl-s-triazolo[1,5-c]py- rimidin-5-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 127
Dependent Claim
36 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6 R ,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(5-hydroxy-7-methyl-s-triazolo[4,3-c]py- rimidin-3-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 128
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(7-methyl-5-oxo-5H-1,3,4-thiadiazolo-[3,2-a]pyrimidin-2-yl)thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
Claim 129
Dependent Claim
33 words
A pharmaceutical composition as claimed in claim 75 which comprises at least one of (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(Z-methoxyimino)acetamido]-3-[(6-carboxy-5-oxo-5H-1,3,4-thiadiazolo-[3,2-a]pyrimidin-2-yl)thiomethyl]-8-oxo-5-thia-l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and a salt thereof as well as a hydrate of said cephalosporin derivative and the salt thereof.
References Cited (Backward Citations)
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