US4560679A
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Organosilicon compounds and antitumor agents containing the compound as effective component
Assignee: Shin-Etsu Chemical Co Ltd
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Filing: 1983-10-17
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Granted: 1985-12-24
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Expires: 2003-10-17
Abstract
Abstract A novel organosilicon compound represented by a formula <IMAGE> wherein A is methylene, carbonyl or sulfonyl group; R, R1 and R2 are alkyl group, respectively; R3 is alkyl, substituted alkyl, alkenyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, pyridyl, substituted pyridyl, furyl, substituted furyl, thienyl, substituted thienyl group or cycloalkyl group together with the substituent A; R4 is hydrogen, alkyl or alkenyl group; and R5, R6, R7, R8, R9, R10, R11 and R12 are hydrogen, alkyl or substituted alkyl, respectively, a non-toxic salt thereof, a process for the preparation of said compound or salt, as well as an antitumor agent comprising as an effective agent at least one of said compound and salt.
Inventors
- 👤 Shigeshi Toyoshima
- 👤 Masayasu Kurono
- 👤 Ryoichi Unno
- 👤 Koichi Ito
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 18:20
CPC Classifications
C; C07; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/0803; C07F7/081; C07F7/0812; A; A61; A61P; A61P35/00
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
164 words
A novel organosilicon compound represented by a formula ##STR77## wherein A is methylene, carbonyl or sulfonyl, R, R 1 and R 2 are alkyl of 1 to 7 carbon atoms, respectively, R 3 is hydrogen, alkyl of 1 to 7 carbon atoms, alkyl of 1 to 7 carbon atoms substituted with halogen, alkenyl of 2 to 7 carbon atoms, phenyl, phenyl substituted with chloro, bromo, methyl or methoxy, naphthyl, naphthyl substituted with --OH or methoxy, pyridyl, cyclohexyl methyl substituted pyridyl, furyl, methyl substituted furyl, thienyl, methyl substituted thienyl or cycloalkyl when taken together with substituent A; R 4 is hydrogen, alkyl of 1 to 7 carbon atoms or alkenyl of 2 to 7 carbon atoms; and R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, or a non-toxic, salt thereof with the provision that R 4 is not alkyl when A is methylene and R 3 is hydrogen.
Claim 2
Dependent Claim
164 words
A novel organosilicon compound represented by a formula ##STR77## wherein A is methylene, carbonyl or sulfonyl, R, R 1 and R 2 are alkyl of 1 to 7 carbon atoms, respectively, R 3 is hydrogen, alkyl of 1 to 7 carbon atoms, alkyl of 1 to 7 carbon atoms substituted with halogen, alkenyl of 2 to 7 carbon atoms, phenyl, phenyl substituted with chloro, bromo, methyl or methoxy, naphthyl, naphthyl substituted with --OH or methoxy, pyridyl, cyclohexyl methyl substituted pyridyl, furyl, methyl substituted furyl, thienyl, methyl substituted thienyl or cycloalkyl when taken together with substituent A; R 4 is hydrogen, alkyl of 1 to 7 carbon atoms or alkenyl of 2 to 7 carbon atoms; and R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, or a non-toxic, salt thereof with the provision that R 4 is not alkyl when A is methylene and R 3 is hydrogen.
Claim 3
Dependent Claim
17 words
A salt of the organosilicon compound as claimed in claim 1, wherein said non-toxic salt is maleate.
Claim 4
Dependent Claim
51 words
An organosilicon compound as claimed in claim 1, wherein R, R 1 and R 2 are methyl group, respectively and R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, respectively, or a non-toxic salt thereof.
Claim 5
Dependent Claim
17 words
A salt of the organosilicon compound as claimed in claim 3, wherein said non-toxic salt is maleate.
Claim 6
Dependent Claim
50 words
An organosilicon compound as claimed in claim 1, wherein R, R 1 and R 2 are methyl group, respectively, R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, respectively and A is carbonyl group.
Claim 7
Dependent Claim
50 words
An organosilicon compound as claimed in claim 1, wherein R, R 1 and R 2 are methyl group, respectively, R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, respectively and A is sulfonyl group.
Claim 8
Dependent Claim
56 words
An organosilicon compound as claimed in claim 1, wherein R, R 1 and R 2 are methyl group, respectively, R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, respectively and -A-R 3 is alkenyl group, or a non-toxic salt thereof.
Claim 9
Dependent Claim
56 words
An organosilicon compound as claimed in claim 1, wherein R, R 1 and R 2 are methyl group, respectively, R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are hydrogen, respectively and -A-R 3 is cycloalkyl group, or a non-toxic salt thereof.
Claim 10
Dependent Claim
20 words
An antitumor composition comprising an antitiumor effective amount of at least one compound of claim 1 and a pharmaceutical carrier.
Claim 11
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-benzoyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 12
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-(p-chlorobenzoyl)-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 13
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-(1-naphthoyl)-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 14
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-nicotinoyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 15
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-(2'-furoyl)-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 16
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-thenoyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 17
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-acetyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 18
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-cyclohexylcarbonyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 19
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-octanoyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 20
Dependent Claim
14 words
An antitumor composition as claimed in claim 9, wherein said effective component is N-(p-toluenesulfonyl)-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 21
Dependent Claim
17 words
An antitumor composition as claimed in claim 9, wherein said effective component is a maleate of N-methyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 22
Dependent Claim
16 words
An antitumor composition as claimed in claim 9, wherein said effective component is maleate of N-allyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
Claim 23
Dependent Claim
16 words
An antitumor composition as claimed in claim 9, wherein said effective component is maleate of N-cyclohexyl-2-[(2-trimethylsilylethyl)thio]ethylamine.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-12-23 | 1989-06-24 | 1989-12-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-23 | 1993-06-24 | 1993-12-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-23 | 1997-06-24 | 1997-12-24 | $7700.00 | Window Closed / Lapsed |