US4687767A
Expired / Lapsed
US
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Certain 1-hydroxyethane, 1,1-di-phosphonic acid derivatives useful in treating calcium metabolism disturbances
Assignee: Roche Diagnostics GmbH
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Filing: 1985-07-26
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Granted: 1987-08-18
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Expires: 2005-07-26
Abstract
Abstract The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.
Inventors
- 👤 Elmar Bosies
- 👤 Rudi Gall
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 21:40
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; A; A61; A61P; A61P3/00; A61P3/12; A61P3/14; C07F9/547; C07F9/553; C07F9/576; C07F9/58; C07F9/645; C07F9/6503; C07F9/6506; C07F9/6515; C07F9/6518; C07F9/6527; C07F9/653
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
150 words
A diphosphonate compound of the formula: ##STR9## wherein Het is a substituted or unsubstituted heterocyclic selected from the group consisting of imidazole, or pyridine, 1,2,4- and wherein the substituents are selected from the group consisting of C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halogen selected from the group consisting of fluorine, chlorine, bromine, iodine; hydroxyl, carboxyl, an amino group optionally substituted by C 1 -C 4 alkyl or alkanoyl with up to 6 carbon atoms; benzyl and benzyl substituted by C 1 -C 4 alkyl, nitro, amino or aminoalkyl with 1 to 4 carbon atoms, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, hydroxy, or alkanoyl of up to 6 carbon atoms and R is a hydrogen atom or an alkyl of 1 to 4 carbon atoms; or a pharmacologically acceptable salt thereof.
Claim 2
Dependent Claim
150 words
A diphosphonate compound of the formula: ##STR9## wherein Het is a substituted or unsubstituted heterocyclic selected from the group consisting of imidazole, or pyridine, 1,2,4- and wherein the substituents are selected from the group consisting of C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halogen selected from the group consisting of fluorine, chlorine, bromine, iodine; hydroxyl, carboxyl, an amino group optionally substituted by C 1 -C 4 alkyl or alkanoyl with up to 6 carbon atoms; benzyl and benzyl substituted by C 1 -C 4 alkyl, nitro, amino or aminoalkyl with 1 to 4 carbon atoms, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, hydroxy, or alkanoyl of up to 6 carbon atoms and R is a hydrogen atom or an alkyl of 1 to 4 carbon atoms; or a pharmacologically acceptable salt thereof.
Claim 3
Dependent Claim
22 words
A compound according to claim 1 wherein each said alkyl is individually selected from the group consisting of methyl, ethyl and isopropyl.
Claim 4
Dependent Claim
24 words
A compound according to claim 8 wherein each said alkanoyl is individually selected from the group consisting of formyl, acetyl, propionyl, butyryl, and valeroyl.
Claim 5
Dependent Claim
24 words
A compound according to claim 1 wherein each said alkanoyl is individually selected from the group consisting of formyl, acetyl, propionyl, butyryl, and valeroyl.
Claim 6
Dependent Claim
12 words
The compound of claim 1 wherein the halogen is chlorine or bromine.
Claim 7
Dependent Claim
9 words
The compound of claim 1 wherein X is hydroxyl.
Claim 8
Dependent Claim
9 words
The compound of claim 1 wherein X is amino.
Claim 9
Dependent Claim
39 words
The compound of claim 1 wherein A is --(CH 2 ) n --wherein n is 2 to 5, ##STR10## wherein m is 2 to 5, --CH═CH--CH 2 --CH 2 --, --CH═CH--CH 2 --CH 2 --CH 2 -- or --CH═CH--CH═CH--.
Claim 10
Dependent Claim
37 words
A pharmaceutical composition for the treatment of calcium metabolism disorders containing an effective amount of the diphosphonate according to claim 1 for the treatment of calcium metabolism disorders, in combination with an inert conventional carrier or adjuvant.
Claim 11
Dependent Claim
29 words
A method for the treatment of calcium metabolism disturbances comprising administering to a mammal in need of said treatment an effective amount of a diphosphonate according to claim 1.
Claim 12
Dependent Claim
16 words
A pharmaceutical composition according to claim 6 having 1 to 100 mg of the active ingredient.
Claim 13
Dependent Claim
16 words
The method according to claim 7 wherein 1 to 100 mg of the diphosphonate, are administered.
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) | 1990-08-17 | 1991-02-16 | 1991-08-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-08-17 | 1995-02-16 | 1995-08-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-08-17 | 1999-02-16 | 1999-08-18 | $7700.00 | Window Closed / Lapsed |