US4147780A
Expired / Lapsed
US
⏱️ 0.0 years remaining
α-Amino-phosphonous acids for inhibiting bacteria and yeast
Assignee: Novartis Corp
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Filing: 1977-05-23
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Granted: 1979-04-03
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Expires: 1997-05-23
Abstract
Abstract The present invention relates to new phosphonous acid derivatives, especially to alpha -amino-phosphonous acids and processes for their production. The new phosphonous acids are valuable chemotherapeutica in the treatment of pathogenic bacteria, gram-negative bacteria and yeast.
Inventors
- 👤 John G. Dingwall
- 👤 Eric K. Baylis
- 👤 Colin D. Campbell
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 05:18
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/48; A; A61; A61K; A61K31/00; A61K31/66; A61P; A61P31/00; C07F9/547; C07F9/553; C07F9/576; C07F9/58
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
175 words
A compound of the formula I ##STR12## or the corresponding zwitterion form in which R and R 1 may be the same or different and can be hydrogen, deuterium, a lower alkyl group, a lower alkyl group substituted by one or two --COOR 2 , --OR 2 or --SR 2 groups in which R 2 is hydrogen or a lower alkyl group, a lower alkenyl, a lower alkynyl, a cycloalkyl, an aryl group having 6 to 10 carbon atoms, an aryl group substituted by from one to three halogen atoms, --COOR 5 , --OR 5 or --SR 5 groups in which R 5 is hydrogen or lower alkyl, a lower alkyl group substituted by aryl, or a lower alkyl group substituted by aryl having from one to three halogen atoms, --COOR 5 , --OR 5 or --SR 5 groups in which R 5 is hydrogen or lower alkyl, and the salts thereof with pharmaceutically acceptable acids or bases and optical isomers thereof, with the proviso that R and R 1 may not both be hydrogen.
Claim 2
Dependent Claim
175 words
A compound of the formula I ##STR12## or the corresponding zwitterion form in which R and R 1 may be the same or different and can be hydrogen, deuterium, a lower alkyl group, a lower alkyl group substituted by one or two --COOR 2 , --OR 2 or --SR 2 groups in which R 2 is hydrogen or a lower alkyl group, a lower alkenyl, a lower alkynyl, a cycloalkyl, an aryl group having 6 to 10 carbon atoms, an aryl group substituted by from one to three halogen atoms, --COOR 5 , --OR 5 or --SR 5 groups in which R 5 is hydrogen or lower alkyl, a lower alkyl group substituted by aryl, or a lower alkyl group substituted by aryl having from one to three halogen atoms, --COOR 5 , --OR 5 or --SR 5 groups in which R 5 is hydrogen or lower alkyl, and the salts thereof with pharmaceutically acceptable acids or bases and optical isomers thereof, with the proviso that R and R 1 may not both be hydrogen.
Claim 3
Dependent Claim
85 words
A compound as claimed in claim 1 having the general formula I as defined in claim 13, in which R and R 1 are hydrogen, deuterium, lower alkyl, lower alkenyl, lower alkynl, lower alkyl substituted by aryl, or lower alkyl substituted by aryl which groups optionally is substituted by from one to three hydroxy or lower alkoxy groups or the salts thereof with pharmaceutically acceptable acids or bases and optical isomers thereof, with the proviso that R and R 1 may not both be hydrogen.
Claim 4
Dependent Claim
74 words
A compound as claimed in claim 1 having the general formula I as defined in claim 1, wherein R and R 1 are hydrogen, deuterium, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, secondary butyl, tertiary butyl, benzyl, benzyl substituted by one to three hydroxy or lower alkoxy groups or the salts thereof with pharmaceutically acceptable acids or bases all optical isomers thereof, with the proviso that R and R 1 may not both be hydrogen.
Claim 5
Dependent Claim
46 words
A compound as claimed in claim 1 having the general formula I as defined in claim 1, wherein R is methyl or isopropyl and R 1 is hydrogen, deuterium or methyl or the salts thereof with pharmaceutically acceptable acids and bases and all optical isomers thereof.
Claim 6
Dependent Claim
43 words
A compound as claimed in claim 1 having the general formula I as defined in claim 1, wherein R is methyl or isopropyl and R 1 is hydrogen or the salts thereof with pharmaceutically acceptable acids and bases and all optical isomers thereof.
Claim 7
Dependent Claim
21 words
A compound as claimed in claim 1, being the 1-amino-2-methylpropanephosphonous acid or the salts thereof with pharmaceutically acceptable acids and bases.
Claim 8
Dependent Claim
21 words
A compound as claimed in claim 1, being the 1-amino-1,2-dimethylpropanephosphonous acid or the salts thereof with pharmaceutically acceptable acids and bases.
Claim 9
Dependent Claim
22 words
A compound as claimed in claim 1, being the 1-amino-ethane phosphonous acid or the salts thereof with pharmaceutically acceptable acids and bases.
Claim 10
Dependent Claim
11 words
A compound as claimed in claim 1, being the (-)-1-amino-2-methylpropanephosphonous acid.
Claim 11
Dependent Claim
11 words
A compound as claimed in claim 1, being the (+)-1-amino-2-methylpropanephosphonous acid.
Claim 12
Dependent Claim
21 words
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound as claimed in claim 1, together with a pharmaceutical excipient.
Claim 13
Dependent Claim
26 words
A method of treating microbial diseases in a mammal, which consist in administering to said mammal enterally or parenterally a composition as claimed in claim 11.
References Cited (Backward Citations)
US3160632A
Cited
US3424788A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-02 | 1982-10-02 | 1983-04-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-02 | 1986-10-02 | 1987-04-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-02 | 1990-10-02 | 1991-04-03 | $7700.00 | Window Closed / Lapsed |