US4112089A
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4-Substituted-1,3-dithiolan-2-ylidene malonates and pharmaceutical compositions containing the same
Assignee: Nihon Nohyaku Co Ltd
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Filing: 1977-02-08
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Granted: 1978-09-05
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Expires: 1997-02-08
Abstract
Abstract A 1,3-dithiolan-2-ylidene malonate derivative having the formula, <IMAGE> (I) wherein R1 and R2, which may be same or different, represent individually a C1-C4 alkyl group; and R3 represents a chloromethyl group, a phenyl group, a group of the formula <IMAGE> (where R4 and R5 represent individually a C1-C4 alkyl group, or may form, in combination, a lower alkylene group which is sometimes intercepted by an oxygen atom), or a group of the formula <IMAGE> (where M represents a hydrogen atom or a salt-forming residue; and A represents a lower alkylene group, a lower alkylene group, a phenylene group or a cyclohexenylene group), has effects of stimulating, improving and recovering the functions of livers, and can prevent, alleviate and cure various liver damages of humans and animals when administered thereto either orally or parenterally.
Inventors
- 👤 Kuniaki Taninaka
- 👤 Hitoshi Kurono
- 👤 Tsutomu Kasai
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 03:22
CPC Classifications
C; C07; C07D; C07D339/00; C07D339/02; C07D339/06; A; A61; A61P; A61P1/00; A61P1/16; A61P3/00; A61P3/08; A61P39/00; A61P39/02; C02; C02F; C02F1/00; C02F1/46; C02F1/461; C02F1/46104; C02F1/46109
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
62 words
A compound represented by the general formula (I), ##STR29## wherein R 1 and R 2 , which may be same or different, represent individually a C 1 -C 4 alkyl group; and R 3 represents a group of the formula ##STR30## (where R 4 and R 5 form, in combination, a lower alkylene group which is sometimes intercepted by an oxygen atom).
Claim 2
Dependent Claim
62 words
A compound represented by the general formula (I), ##STR29## wherein R 1 and R 2 , which may be same or different, represent individually a C 1 -C 4 alkyl group; and R 3 represents a group of the formula ##STR30## (where R 4 and R 5 form, in combination, a lower alkylene group which is sometimes intercepted by an oxygen atom).
Claim 3
Dependent Claim
17 words
A compound in accordance with claim 1 comprising diisopropyl 4-pyrrolidinylacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
17 words
A compound in accordance with claim 1 comprising diisopropyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
17 words
A compound in accordance with claim 1 comprising di-n-butyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
17 words
A compound in accordance with claim 1 comprising diethyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
41 words
A pharmaceutical composition for preventing liver necrosis, fatty liver or hepatitis of animals including humans, which comprises an effective amount sufficient for said purpose of a compound having the general formula (I) defined in claim 1, and a pharmaceutically acceptable diluent.
Claim 8
Dependent Claim
19 words
The composition of claim 6 which contains the said compound in an amount of at least 0.01% by weight.
Claim 9
Dependent Claim
18 words
The composition of claim 7, wherein the compound is diisopropyl 4-pyrrolidinylacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
18 words
The composition of claim 6, wherein the compound is diisopropyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
18 words
The composition of claim 6, wherein the compound is di-n-butyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
18 words
The composition of claim 6, wherein the compound is diethyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
15 words
The composition of claim 6, wherein the compound is formulated into an administration unit form.
Claim 14
Dependent Claim
28 words
The composition of claim 12, wherein the administration unit form is any one of powder, granule, tablet, pill, sugar-coated tablet, capsule, ampoule, suppository, suspension, liquid, emulsion or injection.
Claim 15
Dependent Claim
42 words
A process for preventing liver necrosis, fatty liver or hepatitis of animals including humans which comprises administering orally or parenterally, to the animals an effective dose sufficient for said purpose of a compound having the general formula (I) defined in claim 1.
Claim 16
Dependent Claim
11 words
The process of claim 14, wherein the compound is administered orally.
Claim 17
Dependent Claim
26 words
The process of claim 15, wherein the dose of the compound is in the range from 0.1 to 500 mg per kg body weight per day.
Claim 18
Dependent Claim
11 words
The process of claim 14, wherein the compound is administered parenterally.
Claim 19
Dependent Claim
26 words
The process of claim 17, wherein the dose of the compound is in the range from 0.01 to 250 mg per kg body weight per day.
Claim 20
Dependent Claim
18 words
The process of claim 14, wherein the compound is diisopropyl 4-pyrrolidinylacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 21
Dependent Claim
18 words
The process of claim 14, wherein the compound is diisopropyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 22
Dependent Claim
18 words
The process of claim 14, wherein the compound is di-n-butyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 23
Dependent Claim
18 words
The process of claim 14, wherein the compound is diethyl 4-morpholinoacetoxy-1,3-dithiolan-2-ylidene malonate, or a pharmaceutically acceptable salt thereof.
Claim 24
Dependent Claim
17 words
The process of claim 14, wherein said necrosis, fatty liver or hepatitis is induced by chemical poisoning.
Claim 25
Dependent Claim
24 words
The process of claim 23, wherein the chemical causing said poisoning is carbontetrachloride, chloroform, bromobenzene, dimethyl-nitrosoamine, ethionine, a cadmium salt or a selenium salt.
References Cited (Backward Citations)
US3856816A
Cited
US3761596A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-09-04 | 1982-03-06 | 1982-09-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-09-04 | 1986-03-06 | 1986-09-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-09-04 | 1990-03-06 | 1990-09-05 | $7700.00 | Window Closed / Lapsed |