US4136197A
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Hypoglycaemically and hypolipidaemically effective n-substituted carboxylic acid amides
Assignee: Roche Diagnostics GmbH
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Filing: 1977-04-06
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Granted: 1979-01-23
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Expires: 1997-04-06
Abstract
Abstract An N-substituted carboxylic acid amide of the formula ##STR1## wherein A is a valency bond or an oxygen or sulphur atom or a methylene, ethylene, vinylene, ethyleneoxa or ethylenethia radical, V is a trivalent hydrocarbon radical containing up to 4 carbon atoms, R 1 and R 2 each independently is hydrogen, a halogen atom, a hydroxyl group or an alkyl or alkoxy radical, R 3 is hydrogen, a hydroxyl group or an alkoxy radical, Y is an alkylene radical containing up to 3 carbon atoms, X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 6 carbon atoms, and D is a hydroxymethyl, formyl, free or esterified carboxyl or an N-substituted carbamoyl radical, or a physiologically compatible salt thereof, characterized by hypoglycaemic and hypolipidaemic activity.
Inventors
- 👤 Manfred Hubner
- 👤 Ruth Heerdt
- 👤 Elmar Bosies
- 👤 Hans Kuhnle
- 👤 Felix H. Schmidt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 11:12
CPC Classifications
C; C07; C07D; C07D335/00; C07D335/04; C07D335/10; C07D335/12; C07D335/20; A; A61; A61K; A61K31/00; A61K31/16; A61K31/165; A61P; A61P3/00; A61P3/08; C07C; C07C233/00; C07C233/01; C07C233/12; C07D311/00; C07D311/02; C07D311/78; C07D311/80; C07D311/82; C07D311/84; C07D311/90; C07D313/00; C07D313/02; C07D313/06; C07D313/10; C07D313/12; C07D337/00; C07D337/02; C07D337/06; C07D337/10; C07D337/12; C07C2603/00; C07C2603/02; C07C2603/04; C07C2603/06; C07C2603/10; C07C2603/12; C07C2603/18
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
109 words
An N-substituted carboxylic acid amide of the formula ##STR13## where A is a valency bond or a methylene, ethylene or vinylene radical, V is a trivalent hydrocarbon radical containing up to 4 carbon atoms, R 1 and R 2 each independently is hydrogen, a halogen atom, a hydroxyl group or an alkyl or alkoxy radical, R 3 is hydrogen, a hydroxyl group or an alkoxy radical, Y is an alkylene radical containing up to 3 carbon atoms, X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 6 carbon atoms, and D is a free or esterified carboxyl radical, or a physiologically compatible salt thereof.
Claim 2
Dependent Claim
109 words
An N-substituted carboxylic acid amide of the formula ##STR13## where A is a valency bond or a methylene, ethylene or vinylene radical, V is a trivalent hydrocarbon radical containing up to 4 carbon atoms, R 1 and R 2 each independently is hydrogen, a halogen atom, a hydroxyl group or an alkyl or alkoxy radical, R 3 is hydrogen, a hydroxyl group or an alkoxy radical, Y is an alkylene radical containing up to 3 carbon atoms, X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 6 carbon atoms, and D is a free or esterified carboxyl radical, or a physiologically compatible salt thereof.
Claim 3
Dependent Claim
95 words
A compound according to claim 1, wherein V is a radical selected from the group consisting of ##STR14## R 1 and R 2 each independently is hydrogen, fluorine, chlorine, bromine, a hydroxyl group, or an alkyl or alkoxy radical containing up to 5 carbon atoms, R 3 is hydrogen, a hydroxyl group, or an alkoxy radical containing up to 5 carbon atoms, X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 4 carbon atoms, D is a carboxyl, carboalkoxy radical wherein the alkoxy radical has up to 4 carbon atoms.
Claim 4
Dependent Claim
15 words
A compound according to claim 1, wherein A is a methylene, ethylene or vinylene radical.
Claim 5
Dependent Claim
23 words
A compound according to claim 1, wherein R 3 is a hydroxyl group or an alkoxy radical containing up to 5 carbon atoms.
Claim 6
Dependent Claim
12 words
A compound according to claim 1, wherein X is a valency bond.
Claim 7
Dependent Claim
14 words
A compound according to claim 1, wherein X is --CH 2 --CH 2 --.
Claim 8
Dependent Claim
14 words
A compound according to claim 1, wherein D is a hydroxymethyl or formyl radical.
Claim 9
Dependent Claim
22 words
A compound according to claim 1, wherein D is a carboalkoxy radical wherein the alkoxy radical has up to 4 carbon atoms.
Claim 10
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 3-{4-[2-(3-methylfluorenyl-(9)-acetamido)-ethyl]-phenyl}-propionic acid.
Claim 11
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 3-{4-[2-(2-{fluorenyl-(9)}-propionamido)-ethyl]-phenyl}-propionic acid.
Claim 12
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 2-methoxy-4-[2-(fluorenyl-(9)-acetamido)-ethyl]-benzoic acid.
Claim 13
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 4-[2-(fluorenyl-(9)-acetamido)-ethyl]-benzoic acid.
Claim 14
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 4-{2-(2-[fluorenyl-(9)]-propionamido)-ethyl]-benzoic acid.
Claim 15
Dependent Claim
28 words
A hypoglycaemic or hypolipidaemic composition of matter comprising a hypoglycaemically or hypolipidaemically effective amount of a compound according to claim 1 in admixture with a pharmacologically acceptable diluent.
Claim 16
Dependent Claim
34 words
A method for lowering the sugar or lipid level in the blood of a patient which comprises administering to such patient a hypoglycaemically or hypolipidaemically effective amount of a compound according to claim 1.
Claim 17
Dependent Claim
27 words
The method according to claim 15, wherein such compound is 3-{4-[2-(3-methylfluorenyl-(9)-acetamido)-ethyl]-phenyl}-propionic acid, 3-{4-[2-(2-{fluorenyl-(9)}-propionamido)-ethyl]-phenyl}-propionic acid, 2-methoxy-4-[2-(fluorenyl-9)-acetamido)-ethyl]-benzoic acid, 4-[2-(fluorenyl-(9)-acetamido)-ethyl]-benzoic acid, or 4-{2-(2-[fluorenyl-(9)]-propionamido)-ethyl}-benzoic acid, or a physiologically compatible salt thereof.
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) | 1982-01-22 | 1982-07-24 | 1983-01-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-01-22 | 1986-07-24 | 1987-01-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-01-22 | 1990-07-24 | 1991-01-23 | $7700.00 | Window Closed / Lapsed |