EP0061162A2
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EP
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Cephalosporin derivatives, pharmaceutical compositions containing the same and production thereof
Assignee: Kyoto Pharmaceutical Industries Ltd
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Filing: 1982-03-19
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Granted: —
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Expires: 2002-03-19
Abstract
Abstract Novel cephalosporin derivatives represented by the general formula wherein R 1 is a lower alkyl group, and acid addition salts thereof are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.
Inventors
- 👤 Kakaya Nobuharu
- 👤 Kitao Kazuhiko
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 11:08
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20
Claims Analysis
Total Claims: 33
Claim 1
Independent Claim
19 words
A compound of the formula wherein R 1 is a lower alkyl, or its pharmaceutically acceptable acid addition salt.
Claim 2
Dependent Claim
19 words
A compound of the formula wherein R 1 is a lower alkyl, or its pharmaceutically acceptable acid addition salt.
Claim 3
Dependent Claim
13 words
The compound according to claim 1 which is in the form of hydrochloride.
Claim 4
Dependent Claim
14 words
The compound according to claim 1 which is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylate.
Claim 5
Dependent Claim
15 words
The compound according to claim 1 which is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 6
Dependent Claim
14 words
The compound according to claim 4 which is in the form of crystalline hydrate.
Claim 7
Dependent Claim
14 words
The compound according to claim 4 which is in the form of crystalline monohydrate.
Claim 8
Dependent Claim
20 words
The compound according to claim 3 which is optically active and has the specific rotation of + 48° (c=l, methanol).
Claim 9
Dependent Claim
21 words
The compound according to claim 4 which is optically active and has the specific rotation of + 43° (c=l, 95% ethanol).
Claim 10
Dependent Claim
15 words
The compound according to claim 1 which is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-ethoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 11
Dependent Claim
15 words
The compound according to claim 1 which is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-isobutoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 12
Dependent Claim
15 words
The compound according to claim 1 which is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-n-propoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 13
Dependent Claim
36 words
An orally administrable pharmaceutial composition for treatment of infectious diseases caused by bacteria, comprising as an active ingredient a compound of the formula wherein Rl is a lower alkyl or its pharmaceutucally acceptable acid addition salt.
Claim 14
Dependent Claim
36 words
An orally administrable pharmaceutial composition for treatment of infectious diseases caused by bacteria, comprising as an active ingredient a compound of the formula wherein Rl is a lower alkyl or its pharmaceutucally acceptable acid addition salt.
Claim 15
Dependent Claim
14 words
The pharmaceutical composition according to claim 12, wherein the acid addition salt is hydrochloride.
Claim 16
Dependent Claim
18 words
The pharmaceutical composition according to claim 12, wherein the active ingredient is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylate.
Claim 17
Dependent Claim
19 words
The pharmaceutical composition according to claim 12, wherein the active ingredient is the syn isomer of l-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 18
Dependent Claim
18 words
The pharmaceutical composition according to claim 15, wherein the active ingredient is in the form of crystalline hydrate.
Claim 19
Dependent Claim
18 words
The pharmaceutical composition according to claim 15, wherein the active ingredient is in the form of crystalline monohydrate.
Claim 20
Dependent Claim
25 words
18 : The pharmaceutical composition according to claim 14, wherein the active ingredient is optically active and has the specific rotation of +48° (c=l, methanol)
Claim 21
Dependent Claim
27 words
The pharmaceutical composition according to claim 15, wherein the active ingredient is optically active and has the specific rotation of [a]D 5 + 43° (c=l, 95% ethanol)
Claim 22
Dependent Claim
19 words
The pharmaceutical composition according to claim 12, wherein the active ingredient is the syn isomer of 1-(ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-ethoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 23
Dependent Claim
20 words
The pharmaceutical composition according to claim 12, wherein the active ingredient is the syn isomer of 1-( ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-isobutoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 24
Dependent Claim
20 words
The pharmaceutical composition according to claim 12, wherein the active ingredient is the syn isomer of 1-( ethoxycarbonyloxy)ethyl 7-[2-(2-aminothiazol-4-yl)-2-n-propoxyiminoacetamido]-3-cephem-4-carboxylate hydrochloride.
Claim 25
Dependent Claim
17 words
The pharmaceutical composition according to any of claims 12 - 22, which also contains an organic acid.
Claim 26
Dependent Claim
23 words
The pharmaceutical composition according to Claim 23, wherein the organic acid is an aliphatic carboxylic acid which contains at least two carboxyl groups.
Claim 27
Dependent Claim
16 words
The pharmaceutical composition according to Claim 23, wherein the aliphatic carboxylic acid is a hydroxy acid.
Claim 28
Dependent Claim
18 words
The pharmaceutical composition according to any of Claims 23-25, which is in the form of a solid preparation.
Claim 29
Dependent Claim
28 words
The pharmaceutical composition according to Claim 25, which also contains at least one member selected from the group consisting of alkali metal carbonates and alkali metal hydrogen carbonates.
Claim 30
Independent Claim
42 words
A method of preparing orally administrable compositions for the treatment of bacteria-caused infectious diseases, which comprises mixing a cephalosporin derivative of the general formula: wherein R 1 is a lower alkyl group or a acid addition salt thereof with an organic acid.
Claim 31
Independent Claim
42 words
A method of preparing orally administrable compositions for the treatment of bacteria-caused infectious diseases, which comprises mixing a cephalosporin derivative of the general formula: wherein R 1 is a lower alkyl group or a acid addition salt thereof with an organic acid.
Claim 32
Independent Claim
152 words
A method of producing cephalosporin derivatives of the general formula wherein R 1 is a lower alkyl group, pharmaceutically acceptable acid addition salts thereof, and crystalline hydrates of these, which comprises reacting a compound of the general formula wherein R 1 is as defined above and R 2 is H or an amino-protecting group, or a reactive derivative thereof with a compound of the general formula wherein X is an atom or group which is reactive with the carboxyl group or a reactive derivative thereof, eliminating the protective group R 2 if R 2 is such, or reacting a compound of the general formula wherein R 1 and R 2 are as defined above, or a reactive derivative thereof with a compound of the general formula optionally converting the product to an acid addition salt, and optionally recrystallizing the final product from an aqueous solvent, aqueous hydrochloric acid or an organic solvent.
Claim 33
Independent Claim
152 words
A method of producing cephalosporin derivatives of the general formula wherein R 1 is a lower alkyl group, pharmaceutically acceptable acid addition salts thereof, and crystalline hydrates of these, which comprises reacting a compound of the general formula wherein R 1 is as defined above and R 2 is H or an amino-protecting group, or a reactive derivative thereof with a compound of the general formula wherein X is an atom or group which is reactive with the carboxyl group or a reactive derivative thereof, eliminating the protective group R 2 if R 2 is such, or reacting a compound of the general formula wherein R 1 and R 2 are as defined above, or a reactive derivative thereof with a compound of the general formula optionally converting the product to an acid addition salt, and optionally recrystallizing the final product from an aqueous solvent, aqueous hydrochloric acid or an organic solvent.
References Cited (Backward Citations)
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