Patent US4552873A successfully refreshed from Google Patents.
US4552873A
Expired / Lapsed
US
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Carbapenem compounds, and compositions containing them
Assignee: Sankyo Co Ltd
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Filing: 1982-08-13
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Granted: 1985-11-12
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Expires: 2002-08-13
Abstract
Abstract Compounds of formula (I): <IMAGE> (I) [wherein: R1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups; R2 represents a group of formula <IMAGE> in which <IMAGE> represents an alicyclic amine group having from 4 to 8 ring atoms, optionally having a single double bond, optionally containing an additional hetero-atom and optionally having an oxo group on the ring; X represents a hydrogen atom, an alkyl group, an alkoxy group, an alkylthio group, an alkylsulphinyl group, an alkylsulphonyl group, a hydroxy group, a halogen atom or various substituted alkyl groups; Y represents a hydrogen atom, an alkyl group, an aliphatic acyl group or an acylimidoyl group; and R3 represents a carboxy group or a protected carboxy group] and pharmaceutically acceptable salts thereof have valuable antibacterial activity, especially in vivo.
Inventors
- 👤 Tetsuo Miyadera
- 👤 Yukio Sugimura
- 👤 Toshihiko Hashimoto
- 👤 Teruo Tanaka
- 👤 Kimio Iino
- 👤 Tomoyuki Shibata
- 👤 Shinichi Sugawara
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 11:53
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; C07D477/00; C07D477/10; C07D477/12; C07D477/16; C07D477/20; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/12; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
75 words
Compounds of the formula (I): ##STR66## wherein R 1 is hydroxyethyl, R 2 is ##STR67## wherein ##STR68## is a 3-pyrrolidinyl group, X is hydrogen and Y is a group of the formula ##STR69## wherein R 5 and R 6 are the same or different and each is hydrogen or an alkyl group having from 1 to 4 carbon atoms, R 3 is a carboxy group or a protected carboxy group; and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
75 words
Compounds of the formula (I): ##STR66## wherein R 1 is hydroxyethyl, R 2 is ##STR67## wherein ##STR68## is a 3-pyrrolidinyl group, X is hydrogen and Y is a group of the formula ##STR69## wherein R 5 and R 6 are the same or different and each is hydrogen or an alkyl group having from 1 to 4 carbon atoms, R 3 is a carboxy group or a protected carboxy group; and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
11 words
The compounds of claim 1, wherein Y is an acetimidoyl group.
Claim 4
Dependent Claim
12 words
The compounds of claim 1, wherein R 3 is a carboxy group.
Claim 5
Dependent Claim
14 words
The compounds of claim 1 in the form of the sodium or potassium salt.
Claim 6
Dependent Claim
14 words
The compounds of claim 2 in the form of the sodium or potassium salt.
Claim 7
Dependent Claim
9 words
The compound of claim 1 which is 2-(1-acetimidoylpyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-2-carbapenem-3-carboxylic acid.
Claim 8
Dependent Claim
9 words
The compound of claim 1 which is 2-(1-formimidoylpyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-2-carbapenem-3-carboxylic acid.
Claim 9
Dependent Claim
102 words
A pharmaceutical composition comprising an effective amount of an antibacterial agent in admixture with a pharmaceutically acceptable carrier or diluent, wherein the antibacterial agent is selected from compounds of the formula (I): ##STR70## wherein R 1 is hydroxyethyl, R 2 is ##STR71## wherein ##STR72## is a 3-pyrrolidinyl group, X is hydrogen and Y is a group of the formula ##STR73## wherein R 5 and R 6 are the same or different and each is hydrogen or an alkyl group having from 1 to 4 carbon atoms, R 3 is a carboxy group or a protected carboxy group; and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
102 words
A pharmaceutical composition comprising an effective amount of an antibacterial agent in admixture with a pharmaceutically acceptable carrier or diluent, wherein the antibacterial agent is selected from compounds of the formula (I): ##STR70## wherein R 1 is hydroxyethyl, R 2 is ##STR71## wherein ##STR72## is a 3-pyrrolidinyl group, X is hydrogen and Y is a group of the formula ##STR73## wherein R 5 and R 6 are the same or different and each is hydrogen or an alkyl group having from 1 to 4 carbon atoms, R 3 is a carboxy group or a protected carboxy group; and pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim
14 words
The composition of claim 8, wherein in said formula Y is an acetimidoyl group.
Claim 12
Dependent Claim
12 words
The composition of claim 8, wherein R 3 is a carboxy group.
Claim 13
Dependent Claim
18 words
The composition of claim 8, wherein said compound is in the form of the sodium or potassium salt.
Claim 14
Dependent Claim
18 words
The composition of claim 9, wherein said compound is in the form of the sodium or potassium salt.
Claim 15
Dependent Claim
12 words
The composition of claim 8, wherein said antibacterial agent is 2-(1-acetimidoylpyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-2-carbapenem-3-carboxylic acid.
Claim 16
Dependent Claim
12 words
The composition of claim 8, wherein said antibacterial agent is 2-(1-formimidoylpyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-2-carbapenem-3-carboxylic acid.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-11-11 | 1989-05-13 | 1989-11-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-11-11 | 1993-05-13 | 1993-11-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-11-11 | 1997-05-13 | 1997-11-12 | $7700.00 | Window Closed / Lapsed |